Antibiotics

Proc R Soc Lond B Biol Sci, 1980 Oct 15, 209(1177), 473 - 87
Electrostatic components of drug-receptor recognition . II . The DNA-binding antibiotic actinomycin; Dean PM et al.; The semiempirical molecular orbital method PCILO has been used to study the electronic charge distribution and conformation of the antibiotic actinomycin . Molecular electrostatic potential fields have been constructed in three-dimensional space round the molecule and displayed stereoscopically together with contour maps in the orthogonal planes relative to that of the chromophore . It was found that the drug has a considerable dipole moment and that the electrostatic fields can be separated into two large regions; an area of positive potential surrounds the chromophore and one of negative potential is directed away from the peptide rings . In this and the preceding paper these observations are discussed with respect to drug-receptor recognition phenomena . Pattern-matching of complementary electrostatic fields between the drug and polynucleotide receptor can be discerned.

J Antibiot (Tokyo), 1980 Oct, 33(10), 1107 - 13
New anticoccidial antibiotics, WS-5995 A and B . I . Isolation and characterization; Ikushima H et al.; WS-5995 A, B and C are produced by a new strain of Streptomyces designated Streptomyces auranticolor . These antibiotics were purified by solvent extraction followed by chromatography on silica gel and then crystallized . WS-5995 A (C19H12O6, m.p., 289 approximately 291 degrees C) and WS-5995 B (C19H14O6, sublimation at 300 degrees C) protect chickens from infection with Eimeria tenella, a species of coccidia, which produces morbidity or mortality in chickens . WS-5995 C (C19H14O 7, m.p . 288 approximately 290 degrees C), a biologically inactive component, was found to be converted to WS-5995 A on treatment with trifluoroacetic anhydride.

J Antibiot (Tokyo), 1980 Oct, 33(10), 1103 - 6
Streptomyces auranticolor Sp . Nov., a new anticoccidial antibiotics producer; Ikushima H et al.; A new species of Streptomyces is described and designated Streptomyces auranticolor (FERM-P No . 5365) which produces new anticoccidial antibiotics, designated as WS-5995 A and WS-5995 B . The organism is characterized by gray spore mass color, spiral spore chain with smooth spores, non-chromogenic reaction, soluble pigment, and carbon utilization characteristics . It differs from previously described streptomycetes on the basis of carbon utilization, and pigment production.

J Antibiot (Tokyo), 1980 Oct, 33(10), 1098 - 102
BBM-928, a new antitumor antibiotic complex . II . Taxonomic studies on the producing organism; Tomita K et al.; An actinomycete strain No . G455-101 isolated from a soil sample collected in Luzon Island, Philippines produced a new antitumor antibiotic complex BBM-928 . The organism was determined to be a new species of the genus Actinomadura and designated Actinomadura luzonensis nov . sp . The type strain, No . G455-101, has been deposited under the number ATCC 31491.

Antimicrob Agents Chemother, 1980 Oct, 18(4), 586 - 92
Permeabilizing and hemolytic action of large and small polyene antibiotics on human erythrocytes; Brajtburg J et al.; The effects of large polyenes (heptaenes and the "degenerate heptaene" nystatin) on human erythrocytes were found to occur in three separate stages . Stage I was a reversible increase in cell membrane permeability to monovalent cations and occurred at low antibiotic concentrations . At intermediate antibiotic concentrations, an irreversible increase in cell membrane permeability to cations (stage II) occurred, which then led to swelling of cells and hemolysis (stage III) . Hemolysis could be prevented by sucrose, mannitol, or melezitose, but stages I and II still occurred under these conditions . The effects of the small polyenes (pentaenes and a tetraene) occurred in only one stage . Changes in cell membrane permeability (stages I and II) were not noted before hemolysis (stage III) even in the presence of carbohydrate . Carbohydrates gave only weak, transient protection from the hemolytic action of small polyenes, probably because the membrane damage induced by these antibiotics was more extensive than that induced by the large polyenes . In the presence of sucrose, large polyenes were able to inhibit the hemolytic action of small polyenes, implying that both antibiotics have the same binding sites.

J Reprod Med, 1980 Oct, 25(4), 173 - 7
Premature rupture of the membranes: maternal and neonatal infectious morbidity related to betamethasone and antibiotic therapy; Miller JM Jr et al.; A retrospective study of patients delivering in 1976-77 at Duke University Medical Center was performed to assess the impact of betamethasone and prophylactic antibiotics on infectious morbidity in mothers with premature rupture of the membranes (PROM) at 26 to 34 weeks' gestation and in their neonates . Ninety-five records were reviewed for evidence of maternal and neonatal infection and perinatal mortality . Betamethasone had no impact on maternal or neonatal infection . Antibiotics given concurrently with betamethasone significantly reduced the incidence of maternal and/or neonatal infection (18.0% vs . 0) . Perinatal mortality increased when the duration of the latent period was 72 hours and greater because of factors other than infection.

J Clin Pathol, 1980 Oct, 33(10), 995 - 1001
Light-scattering methods for antibiotic sensitivity tests; Murray J et al.; The total intensity of light scattered in the angular range 30 degrees-130 degrees by a suspension of bacteria can be used as the basis of a method of antibiotic sensitivity testing . A procedure is given in which the bacteria are incubated in the presence of antibiotic, as a test, and in its absence, as a control, for 60 minutes . An incubation time of 90 minutes gives slightly more reliable results . With this increased incubation time it is necessary to measure the intensity of scattered light only at a single fixed angle or, at most, a few angles . Measuring the angular dependence of the scattered intensity does not allow the incubation period to be reduced.

Antibiotiki, 1980 Oct, 25(10), 764 - 9
{Carminomycin induction of single-stranded DNA breaks in the normal and tumorous cells of mice administered the antibiotic intravenously}; Trenin AS; The effect of carminomycin administered intravenously to albino mice on the sedimentation character of the ascitic cell DNA of mouse lymphadenosis NK/Li, as well as the cells of the lungs, kidneys, liver, heart and spleen in alkaline sucrose gradients was studied . It was found that carminomycin in a dose of 3.5 mg/kg (LD50) induced DNA single-strand breaks in the cells of the lungs, kidneys, liver and heart . At the same time the single-strand breaks were not detected in the tumor cells NK/Li and the cells of the spleen . The results are indicative of correlation between sensitivity of the cells to carminomycin and a decreased capacity of the antibiotic for induction of single-strand breaks in DNA . Probably, the cell ability for DNA repair is an important factor defining the antitumor selective effect of carminomycin . Induction of the single-strand breaks reflects the role of the excision repair in healing the damages induced by carminomycin.

Antimicrob Agents Chemother, 1980 Oct, 18(4), 506 - 10
Enzymatic method for rapid and sensitive determination of beta-lactam antibiotics; Frere JM et al.; A rapid and sensitive procedure for the estimation of beta-lactam antibiotics is described which makes use of the ability of these antibiotics to inactivate the R39 DD-carboxypeptidase . Depending on the values of the kinetic parameters which govern the reaction, the antibiotics fall into two groups . The lower limit for the quantitative estimation of the antibiotics of groups I and II is about 5 and 50 pmol/ml, respectively . The procedure has been adopted to biological fluids such as human sera and cows' milk.

J Antibiot (Tokyo), 1980 Oct, 33(10), 1183 - 92
Mutual pro-drugs of beta-lactam antibiotics and beta-lactamase inhibitors; Baltzer B et al.; The principle of combining a beta-lactam antibiotic with a beta-lactamase inhibitor in a single molecule functioning as pro-drug for the two active components is illustrated by the linked esters 3 and 4 in which ampicillin and mecillinam, respectively, are combined with the beta-lactamase inhibitor penicillanic acid sulfone . It is shown that in man these esters are excellently absorbed from the gastro-intestinal tract and after absorption hydrolyzed with simultaneous liberation of the active components . As a result high blood and tissue levels of antibiotic and beta-lactamase inhibitor in a balanced ratio are attained . The advantages of "mutual pro-drugs" over simple combinations are discussed.

J Med Chem, 1980 Oct, 23(10), 1144 - 8
Structure-activity relationships of pyrrole amidine antiviral antibiotics . 2 . Preparation of mono- and tripyrrole derivatives of congocidine; Bialer M et al.; Representatives of three types of congocidine (1) analogues were synthesized . These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, and effects on the synthesis of HS DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase . All synthesized tripyrrole derivatives of congocidine were less cytotoxic and more active than the parent drug in all the three ant iviral tests.

JAMA, 1980 Sep 19, 244(12), 1353 - 4
Antibiotic activity in surgical incisions . The basis of prophylaxis in selected operations; Polk HC Jr et al.; Perioperative antibiotic administration to produce systemic effects reduces the frequency of operative wound infection in selected procedures . Controlled clinical trials now indicate that cephalothin sodium may not be effective in this role, whereas cephaloridine and cefazolin sodium have been beneficial . Review of estimates of incisional antibiotic concentrations taken during prospective patient studies display patterns compatible with these data . EAch drug reaches acceptable incisional concentrations, which are relatively well maintained for cephaloridine and cefazolin; cephalothin disappears from human incisions so rapidly as to provide little wound protection in operations lasting more than one hour.

Experientia, 1980 Sep 15, 36(9), 1025 - 7
The structure of a novel antitumor antibiotic, saframycin A; Arai T et al.; A structure is assigned to saframycin A, a novel antitumor antibiotic from Streptomyces lavendulae No . 314, on the basis of 13C NMR-spectral data.

Biochem J, 1980 Sep 15, 190(3), 765 - 70
Ribosomal resistance to the 12,13-epoxytrichothecene antibiotics in the producing organism Myrothecium verrucaria; Hobden AN et al.; An extract of Myrothecium verrucaria, a fungus which produces a range of 12,13-epoxytrichothecene toxins, was found to be resistant to T-2 toxin, one of its products . The epoxytrichothecenes are inhibitors of eukaryotic protein synthesis and normally bind to the 60S ribosomal subunit so as to inhibit peptidyltransferase activity . Ribosomes from M . verrucaria contain 60S subunits which are not subject to inhibition by T-2 toxin and are also resistant to certain other drugs such as anisomycin and homoharringtonine, but not sparsomycin or cycloheximide.

Experientia, 1980 Sep 15, 36(9), 1051 - 2
Antibiotic bioassay by flow microcalorimetry; Beezer AE et al.; A rapid, sensitive microcalorimetric bioassay of good reproducibility has been developed for the antibiotics penicillin-G, carbenicillin, ampicillin and cefoxitin . The use of growing organisms as responding agents allows discussion of the results for systems which may involve biological fluids.

Farmakol Toksikol, 1980 Sep-Oct, 43(5), 536 - 40
{Effect of preliminary antibiotic administration on the course of ether anesthesia}; Batrak GE et al.; The effect of pretreatment with benzylpenicillin, tetracycline hydrochloride and streptomycin sulfate on the course of either anesthesia was studied in experiments on animals . Benzylpenicillin and tetracyclin hydrochloride neither significantly changed the reactivity of the mouse body nor affected the course of ether anesthesia . Administration of streptomycin sulfate to mice and dogs was attended by the reduced function of the central nervous system . The course of ether anesthesia changed accordingly . The reaction of the animals who had been pretreated with streptomycin sulfate was determined by the species features . In white mice, the antibiotic increased the resistance to the toxic effect of ether while in the dogs, it decreased, on the contrary, the body resistance under anesthesia, thereby accelerating the animals' death.

J Antibiot (Tokyo), 1980 Sep, 33(9), 998 - 1004
The structure of lienomycin, a pentaene macrolide antitumor antibiotic . II . The location of the pentaene chromophore and of six isolated double bonds . The complete structure of the antibiotic; Pawlak J et al.; The locations of the isolated double bonds and of the pentaene chromophore in lienomycin (I) were established by chemical degradation of I followed by MS and 1H NMR examination of the products . The complete structure of the antibiotic is proposed.

J Antibiot (Tokyo), 1980 Sep, 33(9), 989 - 97
The structure of lienomycin, a pentaene macrolide antitumor antibiotic . I . The structure of the carbon skeleton and the location of functionalities; Pawlak J et al.; The structure of a novel type of pentaene macrolide named lienomycin (I) was established by selected chemical transformations of I followed by MS examination of the products . This report provides evidence on the structure of the carbon skeleton of I and on the location of functionalities.

J Antibiot (Tokyo), 1980 Sep, 33(9), 979 - 88
Studies on the ionophorous antibiotics . XXVI . The assignments of the 13C-NMR spectra of lonomycin A and mutalomycin; Seto H et al.; All resonances observed in the 13C-nmr spectra of the polyether antibiotics lonomycin A and mutalomycin have been assigned by the aid of biosynthetic method, selective proton decoupling as well as comparison with structurally related compounds.

J Antibiot (Tokyo), 1980 Sep, 33(9), 967 - 78
Papulacandins, a new family of antibiotics with antifungal activity . Structures of papulacandins A, B, C and D; Traxler P et al.; The structures of the papulacandins A, B, C and D, new antibiotics of Papularia sphaerosperma have been established by means of spectral analysis and degradation reactions . Base catalysed hydrolysis of the main product papulacandin B (1) gave two new hydroxylated long-chain unsaturated fatty acids 5 and 6 along with a hitherto unknown spirocyclic diglycoside 7 . The structure of 7 was determined by further degradation reactions . The positions of attachment of the two fatty acids to the spirocyclic diglycoside 7 through ester-bonds were established by selective base catalysed hydrolysis of 1 and spectral analysis of 1 and some derivatives and degradation products thereof . The structures of papulacandin A (2), papulacandin C (3) and papulacandin D (4) were determined in an analogous way.

J Antibiot (Tokyo), 1980 Sep, 33(9), 961 - 6
New antibiotics, carbazomycins A and B . II . Structural elucidation; Sakano K et al.; The structures of carbazomycins A and B are elucidated to be 3,4-dimethoxy-1,2-dimethylcarbazole and 4-hydroxy-3-methoxy-1,2-dimethylcarbazole, respectively . Further, 13C-chemical shifts of carbazomycins and their derivatives are assigned simultaneously.

Br J Pharmacol, 1980 Sep, 70(1), 25 - 40
Interaction between synthetic analogues of quinoxaline antibiotics and nucleic acids: role of the disulphide cross-bridge and D-amino acid centres in des-N-tetramethyl-triostin A; Fox KR et al.; 1 {Ala3, Ala7} TANDEM is an analogue of des-N-tetramethyl-triostin A (TANDEM) in which both L-Cys residues of the octapeptide ring are replaced by L-Ala; accordingly it lacks the disulphide cross-bridge which limits the conformational flexibility of TANDEM . 2 In {L-Ser1} TANDEM the configuration of one of the serine residues is inverted, altering the disposition of one of the quinoxaline chromophores with respect to the peptide ring . 3 Both compounds interact weakly but detectably with natural DNAs as judged by spectral shifts and increases in the thermal denaturation ('melting') temperature Tm . They also raise the Tm of poly rA . poly rU . 4 Binding isotherms determined by solvent partition analysis with {Ala3, Ala7} TANDEM yield association constants of about 10(3) M-1 for its interaction with natural DNAs . A Scatchard plot for binding to poly(dA-dT) determined by solvent partition and spectrophotometric methods shows marked evidence of cooperativity with an intrinsic association constant 1.9 x 10(4) M-1, 8.7 nucleotides per binding site, and cooperativity parameter 15 . 5 Binding of {Ala3, Ala7} TANDEM to short rod-like fragments of poly(dA-dT) increases their contour length by almost the theoretical amount expected for an ideal process of bifunctional intercalation . 6 No effect of either compound on the winding of the DNA helix could be detected in sedimentation experiments with closed circular duplex PM2 DNA . 7 It is concluded that the cross-bridge of TANDEM greatly stabilizes its binding to DNA, most probably via entropic factors, but is not the only structural feature that influences its AT sequence-selectivity . The consequences of epimerising one of the D-Ser residues appear as disastrous as epimerising both . 8 The experimental details for the synthesis of {Ala3, Ala7} TANDEM and {L-Ser1} TANDEM are given in an appendix to this paper.

Plast Reconstr Surg, 1980 Sep, 66(3), 356 - 60
Antibiotic iontophoresis for the management of burned ear chondritis; Greminger RF et al.; A total of 11 ears in 8 patients were treated with iontophoresis utilizing either gentamicin sulfate or potassium penicillin . All patients experienced rapid healing with little or no deformity.

J Biochem (Tokyo), 1980 Sep, 88(3), 689 - 93
Estimation of the in vivo translational activity of rat liver mitochondria without use of an antibiotic; Kitagawa Y et al.; In order to estimate the in vivo translational activity of mitochondria without using cycloheximide, we developed a selective separation procedure for the mitochondrial translation products . The effects of cycloheximide and isotopic dilution kinetics on the precursor leucine pool indicate that the pH 11.5 insoluble mitochondrial fraction is greatly enriched in mitochondrial translation products.

Antibiotiki, 1980 Sep, 25(9), 690 - 1
{Use of antibiotics for preventing suppurative inflammatory complications in scleroplastic operations for myopic disease}; Savinykh VI; Sodium or potassium benzylpenicillin in a dose of 200000 units 6 times a day and streptomycin sulfate in a dose of 0.5 g twice a day were used intramuscularly during the postoperative period for prevention of purulent inflammatory complications in 172 out of 187 patients with myopic disease subjected to scleroplastic operations performed according to the methods of Shevelev-Kertin, N . N . Pivovarov and V . I . Savinykh . The antibiotic use decreased the period of the inpatient treatment from 28+/-2 to 14+/-2 days and lowered the levels of tenonitis and edema of the eye mucosa . No purulent dissolution of the orbital tissues was observed in the patients.

Antibiotiki, 1980 Sep, 25(9), 673 - 5
{Effect of antibiotic therapy on the functional state of the adrenal cortex in mice under irradiation}; Lebedev VG et al.; Therapeutic efficacy of ampicillin on mice subjected to total irradiation with gamma-rays in a dose of 850 Gy and the effect of the antibiotic therapy on adrenocortical function in the irradiated animals were studied . It was found that the daily use of ampicillin over a period of the 3rd to the 10th day after the irradiation increased the survival rate of the animals by 30 per cent against 100 per cent death of the animals in the control group . An increase in the average life span of the irradiated animals in the test group was observed . The levels of corticosterone in the peripheral blood plasma of the irradiated animals in the test group was observed . The levels of corticosterone in the peripheral blood plasma of the irradiated animals not treated with the antibiotic markedly increased by the 6th and 10th day after the irradiation . The therapeutic use of ampicillin resulted in a significant decrease in the hormone level by the 10th day after the irradiation as compared to that in the control animals . Normalization of adrenocortical function in the animals treated with ampicillin promotes an increase in the rate of recovery from radiation injury.

Antibiotiki, 1980 Sep, 25(9), 669 - 73
{Effect of polyene antibiotics on the increase in specific resistance due to inactivated antiviral vaccines}; Vil'ner LM et al.; The capacity of polyenic antibiotics, such as water soluble forms of amphotericin B, mycoheptin, nystatin and levorin to stimulate immunogenicity and interferonogenic activity of inactivated antiviral vaccines was shown . The protective effect of the vaccine against rabies or forest-spring encephalitis in albino mice was more pronounced on its two-fold use in combination with the antibiotic than that on its use alone . The most significant results were obtained with highly diluted vaccines supplemented with amphotericin B . In this case the resistance index was 2 times higher than on vaccination without amphotericin B . In comparative assays of 4 various lots of vaccines against rabies the ED50 of every inactivated vaccine corresponded to thrice as low levels of the antirabies antigen than on vaccination without the polyen . The problems of the mode of action of the polyenic antibiotics and antiviral inactivated vaccines used in combination are discussed.

Surg Gynecol Obstet, 1980 Sep, 151(3), 404 - 6
The selective use of systemic antibiotics in the treatment of burns; Wilkins TJ et al.; For the past ten years, we have followed a conservative program in using systemic antibiotics for the treatment of significant burns . Prophylactic antibiotics are not used except for scalds . Antibiotics are given selectively at the time of operation and, otherwise, are reserved for the treatment of specific infections . It has been unusual for a patient with a burn severity index, compatible with survival, to die of uncontrolled sepsis . Resistant bacteria and fungi have not been a problem . We attribute this to the selective use of antibiotics.

Biol Bull Acad Sci USSR, 1980 Sep-Oct, 7(5), 400 - 7
Effect of antibiotics on fatty acid composition of strains of E . coli K12 carrying R-plasmids; Andreev LV et al.; A dynamic approach was employed for a study of the reaction of the fatty acid pool of sensitive and resistant strains of E . coli K12 in response to the introduction of antibiotics . Bacteria whose resistance is controlled by plasmids exhibited a specific reaction - a reversible increase in the concentration of cis-9,10-methyl-enehexadecanoic acid . Strains of E . coli K12 (C600, J53, CSH-2) carrying plasmids RP4, R6K, R1 drd 19, pMB9, R386, RP1, RtS-1, were studied.

Ann Surg, 1980 Sep, 192(3), 356 - 64
Prophylactic antibiotics in vascular surgery . Topical, systemic, or both?
Pitt HA, Postier RG, MacGowan AW, Frank LW, Surmak AJ, Sitzman JV, Bouchier-Hayes D.
A prospective, randomized, blinded study was performed to determine whether prophylactic antibiotics would reduce the incidence of infection in peripheral vascular surgery and whether the route of antibiotic administration was important . Patients undergoing a vascular procedure with a groin incision were allocated to one of four groups with respect to prophylactic antibiotics . Group I received no antibiotic . Group II had topical cephradine instilled in their incisions prior to closure . Group III received a 24-hour perioperative course of intravenous cephradine, and Group IV received both topical and intravenous cephradine . Groin and abdominal incisional infections were significantly reduced (p < 0.01) among patients who received prophylactic antibiotics by either the topical, systemic, or combined routes of administration . No significant differences were noted among the three antibiotic groups . Profundoplasty, femoral embolectomy, and femoral aneurysm repair were each associated with an increased incidence of infection (p < 0.01) . Other risk factors were only important in patients not receiving antibiotics . Either intraoperative topical antibiotics or perioperative systemic antibiotics prevent infection in peripheral vascular surgery, but antibiotic administration by both routes is unnecessary.

Antibiotiki, 1980 Sep, 25(9), 643 - 7
{Variability of a Cephalosporium acremonium culture for 2 quantitative traits: antibiotic formation and proteolytic activity}; Shuvalova IA et al.; Exposure of Cephalosporium acremonium, strain 1435, to N-nitrozo-N-methylbiuret resulted in a changed variation coefficient with respect to two quantitative features--the antibiotic production and proteolytic activity . Correlation between the variation coefficient and mutagen exposure time was different for every feature . Positive correlation was found in variation with respect to the antibiotic production and proteolytic activity in populations of various Cephalosporium acremonium strains chosen with regard to one or two of the above features . The level and form of the correlation in variation of the above features in populations changed during selection . Selection according to the two quantitative features resulted in an increased correlation coefficient.

Antibiotiki, 1980 Sep, 25(9), 680 - 3
{Increase in the sensitivity and a simplification of the method for the separate determination of antibiotic activities in combined preparations (oletetrin) by using media with a varying pH value}; Makarova RA et al.; An agar-diffusion method for determination of oleandomycin and tetracycline low levels in solutions of the drug combination was developed . The medhod may be used for investigation of oletetrin absorption and distribution in humans and animals . It provides high accuracy in separate determination of oleandomycin and tetracycline activity in solutions of the drugs at a ratio of 1 : 2 . The same test-culture, Bac . subtilis, variant L2 is used for the assay of tetracycline and oleandomycin activity . The only differences are in the values of pH and the buffer solution and the standards.

Biokhimiia, 1980 Sep, 45(9), 1682 - 4
{Effect of the polycationic antibiotic polymyxin B on the respiratory activity of rat liver mitochondria}; Kapitanova NG et al.; the mechanism of the effect of the peptide antibiotic polymixin B on respiration of rat liver mitochondria was studied . It was shown that polymixin B at concentrations of (1,6--2,0) . 10(-3) M inhibits mitochondrial respiration in state 3 and 3u irrespective of the oxidation substrate used and activates oxygen consumption in state 4 at lower concentrations . It is assumed that the antibiotic affects mitochondrial respiration by changing the ionic permeability of the membranes.

J Gen Microbiol, 1980 Sep, 120(1), 95 - 104
Resistance to the antibiotics viomycin and capreomycin in the Streptomyces species which produce them; Skinner RH et al.; Viomycin capreomycin, antibiotics produced by Streptomyces vinaceus and S . capreolus respectively, are potent inhibitors of bacterial protein synthesis . Although these organisms are highly tolerant of their own products in vivo, their ribosomes are fully sensitive to the action of the drugs in vitro . However, they processes novel, antibiotic-inactivating enzymes (viomycin phosphotransferase, capreomycin phosphotransferase, capreomycin acetyltransferase) which, in addition to possible biosynthetic roles, may contribute to the resistances observed in vivo.

J Antibiot (Tokyo), 1980 Sep, 33(9), 1048 - 53
Effects of several anthracycline antitumor antibiotics on the transcriptional activity of isolated nucleoli; DuVernay VH et al.; The class II anthracycline antitumor antibiotics musettamycin, rudolfomycin, aclacinomycin and marcellomycin, which were shown in earlier studies to preferentially inhibit the synthesis of nucleolar RNA in intact tumor cells, were studied in an isolated nucleolar transcriptional assay . Their effects were compared with those of the nucleolar non-selective anthracyclines adriamycin, carminomycin and pyrromycin, as well as with the 10-descarbomethoxy-analogs of marcellomycin and rudolfomycin . The isolated nucleolar transcriptional assay was found to have linear activity for 30 minutes at 30 degrees C . At increasing concentrations of alpha-amanatin up to 200 micrograms/ml, the maximum degree of inhibition of transcriptional activity was found to be 6 approximately 7% . The ranking of nucleolar RNA synthesis inhibitory potencies of the class I and II anthracyclines and the 10-descarbomethoxy-analogs obtained previously in intact cells was reproduced in the isolated nucleoli assay system described here . Thus, evidence for the use of this assay as a screen for nucleolar active antitumor agents is presented.

Mycopathologia, 1980 Aug 29, 72(1), 13 - 9
Antifungal antibiotic sensitivity testing: use of Autobac 1 for standardization purposes; Seguela JP et al.; The authors used a semi-automatic device, Pfizer Autobac 1, to standardize antifungal antibiotic sensitivity testing . The first trials gave quite satisfying results for true (polyene) antibiotics, but more questionable results were obtained for imidazole derivatives and 5-fluorocytosine.

Biochim Biophys Acta, 1980 Aug 4, 600(2), 585 - 9
The influence of the fatty acid composition of Acholeplasma laidlawii membranes on the growth inhibitory activity of narasin, a polyether ionophorous antibiotic; Smith CK 2nd et al.; Narasin, apolyether ionophorous antibiotic capable of acting as a transmembrane carrier of cations, has a growth inhibitory effect on Acholeplasma laidlawii, permitting only 20% survival when present as 0.1 micrograms/ml in an undefined growth nutrient or fatty acid-deficient nutrient supplemented only with palmitic acid . When A . laidlawii is propagated in fatty acid-deficient nutrient supplemented with linoleic acid, however, the organisms become 40 times more sensitive to the growth inhibitory effect of this antibiotic . The actual fatty acid composition of the membranes would indicate that a higher degree of unsaturation enhances ionophore activity.

Chirurg, 1980 Aug, 51(8), 519 - 23
{Results of therapy combining peritoneal lavage and local application of antibiotics in 250 patients with acute perforating appendicitis}; Duyzings JW et al.; Since 1967, 2480 appendectomies have been performed at the St . Lucas Hospital (Amsterdam) and the St . Annadal Hospital (Maastricht), of which 250 were for perforated appendicitis . A so-called 'combined method' of treatment was used in all these cases: during the operation saline was used to lavage the peritoneal cavity with the patients in the reverse-Trendelenburg position . Antibiotics were left in the peritoneal cavity . No intraperitoneal drainage was performed, but the wound was drained for 5 days . Postoperative treatment consisted of nasogastric suction and parenteral antibiotics for 5 days in combination with anticoagulation . With thus combined approach one death was seen in 250 cases . There were 20 cases of wound infection (8%), 7 pelvic abscesses (2.8%), and 2 retroperitoneal abscesses . No thromboembolic complications were seen because of the use of routine anticoagulation . For 191 patients (77%), total hospitalization was less than 14 days . This method of treatment is compared with recent reports in literature.

J Reprod Med, 1980 Aug, 25(2), 63 - 6
C-reactive protein in the evaluation of antibiotic therapy for pelvic infection; Angerman NS et al.; C-reactive protein (CRP), an acute-phase reactant not found in normal serum, has previously been shown, by qualitative assay, to differentiate inflammatory from noninflammatory pelvic pathology . In this study, quantitative measures of serum CRP were obtained concomitantly with white blood counts (WBC) and erythrocyte sedimentation rates (ESR) in patients being treated for pelvic infection . CRP levels and their changes, which were not known to physicians treating the patients, accurately indicated those patients who would need supplementary antibiotics to achieve remission . WBC levels were misleading in over half the patients, and the ESR bore no relationship to the clinical situation . The data suggest that CRP may be used to assess the efficacy of antibiotic therapy in pelvic infection . Our successful use of single-agent therapy in most cases also suggests that the use of multiple antibiotics is unnecessary and that CRP levels can indicate when additional antibiotics are appropriate.

Antibiotiki, 1980 Aug, 25(8), 615 - 9
{Modern antibiotics in the clinical picture of infectious diseases}; Bilibin AF et al.; The number of various chemotherapeutics including antibiotics used in combined treatment of patients with various infectious diseases is rather significant . Recently some new valuable drugs have been recommended . Still, in spite of definite achievements in treatment of patients with infectious diseases there are some difficulties and problems mainly connected with therapy of patients with sepsis, chronic typhoid fever bacterial carriers and some other patients.

Antibiotiki, 1980 Aug, 25(8), 566 - 71
{Inactivation mechanism of polyene antibiotics . The change in the functional component of levorin during inactivation}; Bronov LV et al.; The inactivation process of levorin, a polyenic antibiotic was studied in the presence of oxygen . It was found that the biological activity did not sufficiently correlate with the optical density of the antibiotic solution . This indicates that destruction of the double bonds was not the only process resulting in the biological activity loss . In this connection methods for qualitative determination of the levorin main functional groups, i.e . aromatic and aliphatic amines and carbonyl groups were developed . The methods were used for the control of the changes in these functional groups on levorin inactivation . It was found that the inactivation level was directly proportional to the amount of the oxygen absorbed, 1 molecule of oxygen being required for inactivation of 2 levorin molecules . The number of the carbonyl groups and aromatic amines did not change during the inactivation process . In the first stages of inactivation the biological activity was directly proportional to the level of amino sugars . If the heptaen chromophore is not absorbed, 3 double bonds remain in inactivated levorin.

Acta Ophthalmol (Copenh), 1980 Aug, 58(4), 567 - 75
Bacterial flora in relation to cataract extraction . V . Effects of topical antibiotics on the preoperative conjunctival flora; Fahmy JA; In a randomized study comprising 60 patients, six different prophylactic regimens were evaluated for their effectiveness in eradicating bacteria on the conjunctivas before surgery . Gentamicin sulfate ophthalmic solution was the only antibiotic able to eliminate bacteria in almost all of the examined patients . The other drugs (chloramphenicol solution, oxytetracycline-polymyxin B ointment, sulphamethizole, bacitracin-neomycin and ristocetin-polymyxin B solutions) were not effective, although most of the isolated strains were sensitive to the respective antibiotics, probably because of the short treatment period (18 h) . The problem of prophylactic therapy of ophthalmology is discussed, and some guide lines are given.

J Antibiot (Tokyo), 1980 Aug, 33(8), 895 - 9
Have deoxystreptamine aminoglycoside antibiotics the same binding site on bacterial ribosomes?
Le Goffic F, Capmau ML, Tangy F, Caminade E.
(3H) Tobramycin was used as a probe to determine the relationship between the structure of aminoglycoside antibiotics and their ability to remove this drug from its higher affinity binding site on the ribosome . The dissacharide moieties (neamine, tobramine, gentamine) appeared to have a common binding site, whereas the kanosamine, garosamine and ribose moieties determined the specificity of this binding . Amikacin and butikacin behaved in an anomalous manner in spite of their close structural relationship to tobramycin.

J Gen Microbiol, 1980 Aug, 119(Pt 2), 397 - 404
Co-synthesis of penicillin following treatment of mutants of Aspergillus nidulans impaired in antibiotic production with lytic enzymes; Makins JF et al.; Mycelia from four mutants of Aspergillus nidulans impaired in penicillin production at separate genetic loci were treated with an enzyme complex capable of lysine cell walls, then mixed in all possible paired combinations and grown in osmotically buffered penicillin production media, containing 2-deoxyglucose and an unrefined mixture of polyoxins to prevent cell wall regeneration . The culture filtrates were assayed after 6 d and significant penicillin yields were observed in four of the six possible combinations . None of these pairs produced penicillin when grown together as normal mycelium, suggesting that intermediates of the penicillin biosynthetic pathway unable to diffuse from untreated mycelium could do so from enzyme-treated mycelium when cell wall regeneration was inhibited . A general method is thus available for examining biochemical pathways with mutants accumulating intermediates unable to cross the cell wall barrier.

Antibiotiki, 1980 Aug, 25(8), 595 - 606
{Ability of vancomycin-group antibiotics to induce or to inhibit thrombocyte agglutination}; Rak K et al.; The effect of 4 vancomycin antibiotics on factor VIII-dependent agglutination of thrombocytes was studied . Significant similarity, both quantitative and qualitative, between ristocetin and ristomycin was found . In this connection ristomycin may be used for determination of the so-called ristocetin cofactor . Actinoidin and vancomycin inhibited agglutination of platelets induced by ristocetin or ristomycin in platelet-enriched plasma with citrate or EDTA the same as in the system contaning platelets treated with formalin and did not inhibit agglutination induced by the bovine factor VIII . The 4 antibiotics induced precipitation of the plasma protein . Vancomycin was most active and actinoidin ws lest active in this respect . Ristocetin and ristomycin also possessed such capacity, the effect of the latter being higher . Actinoidin and vancomycin did not prevent the immediate effect of light absorption increasing due to addition of ristocetin or ristomycin to fixed platelets in concentrations completely inhibiting agglutination of platelets in the presence of the protein cofactor . Inhibition of this direct effect of ristocetin and ristomycin was observd only at higher concentrations, which indicated that this effect was not probably associated with agglutination . The results of the study on various ristomycin derivatives showed that methylated carboxylic groups and free hydroxyls of phenol may play the main role in ristomycin binding with the thrombocytic membrane and/or protein cofactor.

Can J Microbiol, 1980 Aug, 26(8), 874 - 80
Regulatory control of 3-deoxy-D-arabino-heptulosonic acid 7-phosphate synthetase in Streptomyces antibioticus; Murphy MF et al.; Streptomyces antibioticus possesses a tryptophan-inhibitable 3-deoxy-D-arabino-heptulosonic acid 7-phosphate (DAHP) synthetase whose synthesis is also repressed by L-tryptophan . Studies of the DAHP synthetase obtained by ammonium sulfate fractionation of a crude extract derived from S . Antibioticus revealed that the enzymic activity was only partially inhibited by tryptophan . Inhibition of the DAHP synthetase activity was strongly pH dependent at values below 7.0 . A number of tryptophan analogues was noted to inhibit the enzyme; by contrast, other aromatic amino acid end products failed to affect DAHP synthetase activity . Chorismic acid, a key intermediate in aromatic amino acid biosynthesis, was ineffective as an inhibitor when used alone; however, if supplied with L-tryptophan, a further reduction of DAHP synthetase activity (15--25%) was routinely observed.

Br Med J, 1980 Jul 12, 281(6233), 111 - 2
Antibiotics in surgical treatment of acute abscesses; Blick PW et al.; A four-way, double-blind, prospective trial of treatment of abscesses by incision, curettage, and primary closure with and without antibiotic cover (clindamycin injection before operation or capsules after operation, or both) was conducted . There was no appreciable difference in mean healing time between the patients given both the antibiotic injection and the antibiotic capsules and those given the injection and placebo capsules, whereas healing times in those given the placebo injection and antibiotic capsules or placebo only were appreciably longer . Four of the patients who were not given the antibiotic injection developed bacteraemia; one patient who was given the antibiotic injection also developed a bacteraemia, but this was caused by clindamycin-resistant bacteria . These results show that a single injection of an effective antibiotic before operation is sufficient to protect the patient against bacteraemia and permit optimum healing.

Br J Dermatol, 1980 Jul, 103(1), 51 - 9
Neutrophil chemotaxis in the presence of antibiotics: a re-evaluation using an agarose technique; Gange RW; Neutrophil chemotaxis in the presence of tetracycline and clindamycin was evaluated using an agarose technique . No significant inhibition of chemotaxis by these antibiotics could be demonstrated, in contrast to previously reported findings using the Boyden chamber technique for measurement of chemotaxis . Both agents caused a minor increase in movement towards a P . acnes derived chemotactic factor . Some reduction of chemokinesis by high concentrations of tetracycline was noted . No effect of the drugs upon generation of chemotactic activity from whole serum could be demonstrated . Normal cell movement occurred in the absence of extracellular calcium and magnesium, in contrast to reported findings using the Boyden chamber.

Can J Surg, 1980 Jul, 23(4), 366 - 9, 372
Use of a topical triple-antibiotic spray to reduce morbidity from pelvic infection after gynecologic operations; Wright VC et al.; To study the effect of a topical antibiotic spray in reducing postoperative morbidity when used during surgery, a randomized, double-blind study was done on 150 women who had a vaginal hysterectomy with or without colporrhaphy . The spray contained neomycin sulfate, polymyxin B sulfate and zinc bacitracin and was used in 75 patients; a placebo spray was used in the other 75 patients . The antibiotic spray significantly (P < 0.01) decreased the frequency of pelvic infections postoperatively--14.7% in the antibiotic group compared with 37.3% in the placebo group.

J Biomed Mater Res, 1980 Jul, 14(4), 487 - 97
Interaction of the absorbable hemostatic agent (IP760) with aminoglycosidic antibiotics; Boyle VJ; The linear, crosslinked amylose-succinate hemostatic agent, IP760, has been evaluated for its interaction with aminoglycosidic antibiotics . The highly structured polymer appears to act as a cationic exchange resin which binds the basic aminoglycosides . Binding of these agents to IP760 is reversed by increased pH and/or increased ionic strength . Dialysis experiments demonstrated that 85 and 90% of the bound gentamicin was released at pH 7.5 and 8.0, respectively, over a period of 36 hr . Formation of the IP760-antibiotic complexes suggests potential medicinal use for hemostatis and slow release of the antibiotic for prophylaxis of postsurgical contamination or infection

J Dairy Sci, 1980 Jul, 63(7), 1134 - 7
Sensitivities to antibiotics and seasonal occurrence of mastitis pathogens; Bishop JR et al.; In a 2-yr survey of the Clemson University's dairy herd, each sample of mastitic milk was cultured, and mastitis pathogens were isolated . Causative organisms then were subjected to disc assay of sensitivity to antibiotics . Antibiotics were penicillin, streptomycin, erythromycin, oxytetracycline, cephalothin (cephalosporin), ampicillin and novobiocin . The more widely used antibiotics--penicillin, streptomycin, and erythromycin--were relatively ineffective for bacterial sensitivity in vitro, whereas bacterial sensitivity in vitro for oxytetracycline and cephalothin was considerably more . These results also were true in vivo in treatment of animals in the University herd . Incidence of mastitis under our conditions of weather, housing, and management increased greatly during summer months with less increase during winter months.

Drugs, 1980 Jul, 20(1), 57 - 68
Adverse antibiotic drug interactions; Bint AJ et al.; There is enormous potential for drug interactions in patients who, today, often receive many drugs . Antibiotics are prominent amongst the groups of drugs commonly prescribed . Many interactions take place at the absorption stage . Antacids and antidiarrhoeal preparations, in particular, can delay and reduce the absorption of antibiotics such as tetracyclines and clindamycin, by combining with them in the gastrointestinal tract to form chelates or complexes . Other drugs can affect gastric motility, which in turn often controls the rate at which antibiotics are absorbed . Some broad spectrum antibiotics can alter the bacterial flora of the gut which may be related to malabsorption states . The potentiation of toxic side effects of one drug by another is a common type of interaction . Antibiotics which are implicated in this type of interaction are those which themselves possess some toxicity such as aminoglycosides, some cephalosporins, tetracyclines and colistin . Some of the most important adverse interactions with antibiotics are those which involve other drugs which have a low toxicity/efficacy ratio . These include anticoagulants such as warfarin, anticonvulsants such as phenytoin and phenobarbitone and oral antidiabetic drugs like tolbutamide . Risk of interaction arises when the metabolism of these drugs is inhibited by liver microsomal enzyme inhibitors such as some sulphonamides and chloramphenicol, or is enhanced by enzyme inducers such as rifampicin.

Ann Intern Med, 1980 Jul, 93(1), 1 - 8
Antibiotic therapy in Lyme disease; Steere AC et al.; We studied antibiotic efficacy in 113 patients with erythema chronicum migrans, the first manifestation of Lyme disease . Erythema chronicum migrans and its associated symptoms resolved faster in patients given penicillin or tetracycline (median duration, 4 and 2 days, respectively) than in untreated patients (10 days; P less than 0.001 and P = 0.005, respectively) . Erythromycin had no significant effect . Although the frequency of subsequent neurologic and cardiac abnormalities was similar in all four groups, significantly fewer patients given penicillin developed arthritis than did untreated patients (P = 0.001) . Among 15 patients with arthritis who were followed for at least 29 months, the total duration of joint involvement was shorter in penicillin-treated patients (median, 4 weeks) than in untreated patients (17 weeks; P = 0.019) . Although the clinical manifestations of the disease may fluctuate in frequency from year to year and influence apparent antibiotic effect, we conclude that penicillin therapy shortens the duration of erythema chronicum migrans and may prevent or attenuate subsequent arthritis.

Minerva Med, 1980 Jun 30, 71(26), 1873 - 8
{The use of a new antibiotic for local administration in burns}; Giuliani V et al.; A new antibiotic already available on the market (meclocyclin) was experimented on 27 patients aged 45 days to 66 yr with burns due to various causes . Tolerance was excellent in all cases and the average hospital stay was 16 days . Two ointments (one containing meclocyclin, the other containing a different bacteriostatic) were applied on symmetrical sites . The results were practically the same . The meclocyclin ointment can be regarded as preferable, however, owing to its excellent tolerance, and non-absorption into the circulation, so that sensitisation cannot occur even during protracted administration . Another ointment, containing meclocyclin and fluochinolone, was also used in the presence of hypertrophic or keloid pathological scars . Useful results were obtained with regard to both the extent of the damaged areas and the functional limitations sometimes observed . Treatment in these cases, however, was sometimes prolonged for months.

Biochemistry, 1980 Jun 24, 19(13), 3069 - 73
Mechanism of the antibiotic action of alpha-dehydrobiotin; Piffeteau A et al.; alpha-Dehydrobiotin, a naturally occurring biotin analogue, exhibits antibiotic properties {Hanka, L . J., Reineke, L . M., & Martin, D . G.(1969) J . Bacteriol . 100, 42--46} . It is shown in this paper that in addition to its activity as corepressor of the transcription of the biotin locus {Guha, A., Saturen, Y., & Szybalski, W . (1971) J . Mol . Biol . 56, 53--62} alpha-dehydrobiotin acts at the enzyme level . The synthesis of specifically tritiated alpha-dehydrobiotin has been achieved . By use of this labeled compound and a biotin-department strain of Escherichia coli, it has been demonstrated that alpha-dehydrobiotin can be linked covalently to proteins without further transformation . The fixation of biotin to apocarboxylases is inhibited irreversibly after preincubation with alpha-dehydrobiotin . This strongly supports the hypothesis that alpha-dehydrobiotin can be specifically linked to apocarboxylases in place of biotin and leads to carboxylases that are inactive . Thus, the antibiotic properties of alpha-dehydrobiotin would be partly due to the fact that it compete with biotin for the fixation on the apocarboxylases, producing irreversibly inactive enzymes.

Biochim Biophys Acta, 1980 Jun 20, 599(1), 280 - 93
Interaction between phospholipid bilayer membranes and the polyene antibiotic amphotericin B: lipid state and cholesterol content dependence; Bolard J et al.; The interaction between amphotericin B and egg yolk phosphatidylcholine, dimyristoyl (DMPC) and dipalmitoyl phosphatidylcholine (DPPC) phospholipid bilayer vesicles has been monitored by the circular dichroism (CD) spectra of amphotericin B at a 1 . 10(-5) M concentration . This method has revealed that amphotericin B may be present in a number of different forms depending on the time elapsed after the mixing, the cholesterol content of the vesicles and the vesicles' physical state . Some striking features of these CD detected species are the following: with egg yolk phosphatidylcholine and a molar cholesterol percentage lower than 25, at 25 degrees C several forms are coexistent, their amount is time-dependent; with dipalmitoyl or dimyristoyl phosphatidylcholines without cholesterol or with a cholesterol molar percentage lower than 25, in the gel state, a form different from the former appears very rapidly; with egg yolk phosphatidylcholine, DMPC and DPPC at a molar cholesterol percentage between 25 and 50 a new form is monitored, identical in the three cases and observed in the liquid crystalline state as well as in the gel state . In the case of the three phospholipids without cholesterol a definite interaction with the antibiotic is observed but with different characteristics according to the nature of lipid . With amphotericin B 'Fungizone' the same species are monitored but their appearance is much slower . Two explanations are proposed for the origin of the discrepancies between CD and electronic absorption.

Gann, 1980 Jun, 71(3), 308 - 12
Antitumor effect of a new antibiotic, neothramycin; Hisamatsu T et al.; A new anthramycin-group antitumor antibiotic, neothramycin, isolated from a Streptomyces culture, showed activity against experimental tumors such as lymphocytic leukemia P388 ascites sarcoma-180, hepatoma AH130, Walker carcinosarcoma-256 and mouse mammary adenocarcinoma (CCMT) . In particular, the tumor growth inhibition ratio was as high as 96% when neothramycin was injected intraperitoneally at a daily dose of 2 mg/kg into Wistar strain rats previously inoculated with Walker carcinosarcoma-256 by the subcutaneous route . Successive intraperitoneal injections of the compound were more effective than a single injection with the P388 system.

Res Commun Chem Pathol Pharmacol, 1980 Jun, 28(3), 497 - 504
Embryotoxicity and teratogenicity of the anthracycline antibiotic carminomycin in mice; Damjanov I et al.; Carminomycin, a new antitumor anthracycline antibiotic, has embryolethal, embryotoxic and teratogenic effects during early postimplantation stages of development in mice . These effects depend on the dose and route of administration and the gestational age of the exposed embryos.

Antibiotiki, 1980 Jun, 25(6), 440 - 4
{Surface activity of polyene antibiotics}; Etingova NI; The surface activity properties of polyenic antibiotics, such as amphotericin B, mycoheptin, levorin and nystatin were studied . The critical concentrations for the mycella formation were determined and the values of the polyenic antibiotic surface activity at various temperatures were estimated . It was found that the process of the mycella formation of polyenic antibiotics was defined by a positive change in the entropy . A thermodynamic analysis of the process of the mycella formation of the polyenic antibiotics in aqueous solutions was performed.

Nippon Heikatsukin Gakkai Zasshi, 1980 Jun, 16(2), 93 - 7
{Effects of some kinds of antibiotics on the electrical and mechanical activities of guinea-pig taenia coli (author's transl)}; Nakai Y; Effects of some kinds of antibiotics on the electrical and mechanical activities of guinea-pig taenia coli were investigated . The sucrose gap method was used for measurement of electrical activity and simultaneously isometric tension was recorded . Both cephalothin (2.4 mM) and lincomycin (2.2 mM) did not cause any effect on the spontaneous electrical and mechanical activities . Chloramphenicol (3.1 mM) completely abolished the spontaneous spike discharges and relaxed the smooth muscle in a short time, while clindamycin (2.2 mM) took a long time to produce an effect as same as chloramphenicol . Both chloramphenicol and clindamycin abolished the stimulus-induced spikes and Sr-spikes . All of these responses were reversible by washing out with normal Krebs solution . These results suggest that chloramphenicol and clindamycin may inhibit Ca2+ influx through the Ca2+ channels across the smooth muscle cell membrane.

J Antibiot (Tokyo), 1980 Jun, 33(6), 591 - 9
Characterization of aromatic heptaene macrolide antibiotics by high performance liquid chromatography; Mechlinski W et al.; High performance liquid chromatographic (HPLC) procedures were utilized for the rapid and efficient separation and characterization of the aromatic heptaene macrolide group of antifungal antibiotics . The instrument utilized a 350 nm phosphor converted ultraviolet detector and a mu Bondapak C18 column packing . Optimum resolution of eleven commercial aromatic heptaene macrolide preparations was obtained with solvent systems consisting of mixtures of acetonitrile and 0.05 M aqueous sodium citrate buffer, pH 5.3 . The presence of two distinct types of aromatic heptaene macrolides with numerous well-defined individual components has been established.

Antibiotiki, 1980 Jun, 25(6), 411 - 5
{Action of antibiotics on the growth and metabolic processes of streptomycetes and Nocardia}; Toropova EG et al.; New experimental data on the effect of novobiocin, ristomycin and nystatin on growth and metabolism of Streptomycetes and Nocardia are presented . The study of the organisms producing other antibiotics showed that they were tens, hundreds and even thousands times more sensitive to the tested biologically active compounds than the organisms producing these compounds . The protein synthesis and antibiotic biosynthesis proved to be most sensitive out of the processes studied . The findings showed that during their evolution the antibiotic-producing organisms have developed definite protective mechanisms which enable them to resist relatively high concentrations of their own metabolites (antibiotics) . This ensures them in their struggle for existence.

Antibiotiki, 1980 Jun, 25(6), 403 - 7
{Biosynthesis of the antibiotic, grizin, by prototrophic revertants of Streptomyces griseus biochemical mutants}; Kuklin VV et al.; Spontaneous and nitrosomethylbiuret-induced prototrophic revertants of various biochemical mutants of Str . griseus producing grisin, a streptothricin antibiotic, were isolated . The antibiotic production level of the revertants was studied . It was found that most of the prototrophic revertants synthesized much higher amounts of grisin than the initial biochemical mutants . It was also shown that a number of the prototrophic revertants of the methionine- and arginine-dependent mutants synthesized 20-23% higher amounts of grisin as compared to the control.

J Pharm Pharmacol, 1980 Jun, 32(6), 394 - 8
The use of liposomes as a model for drug absorption: beta-lactam antibiotics; Kimura T et al.; Liposomes were prepared from egg phosphatidylcholine-cholesterol-diacetylphosphate (80:20:5) and total lipid extracts of rat intestinal mucosa, and the permeabilty of the liposomal membrane to eight beta-lactam antibiotics was studied by using a dynamic dialysis method . Although all the antibiotics used here are ionized and poorly lipid-soluble at pH 6.5, some of them are orally active and efficiently absorbed from the small intestine . The release rate constants from the aqueous dispersion of drug-entrapped liposomes were approximately in the order of their absorbability . Intestinal lipid liposomes were more permeable to the antibiotics than egg lecithin liposomes and the release rate constants for the drugs from intestinal lipid liposomes were strongly correlative with their absorption rate constants, except for cephalothin and ampicilin, the deviations of which could be explained by their surface activity . It is suggested that lipid components of the intestinal mucosa and the bilayer structure may play an important role in the absorption process of the antibiotics . The validity of liposomes as a model for the intestinal absorption of drugs is also discussed.

Minerva Med, 1980 May 19, 71(20), 1453 - 8
{Effect of antibiotics on spontaneous and direct migration of human leukocytes . Preliminary findings}; De Simone C et al.; Like other human blood cells, neutrophiles can travel enter tissues spontaneously . This apparently casual journeying is arrested in the presence of infection and they migrate to the site of the lesion . Experiments in vitro have shown that tetracycline, rifamycin, chloramphenicol, and cefuroxine inhibit such migration . In the present paper, it is demonstrated that ampicillin and tauglycolcillin, a new semi-synthetic penicillin, exert no significant influence on either direct or spontaneous neutrophile migration.

Philos Trans R Soc Lond B Biol Sci, 1980 May 16, 289(1036), 169 - 72
Recent biosynthetic studies on beta-lactam antibiotics; Baldwin JE et al.; Recent experimental observations on the cell-free formation of penicillins and cephalosporins in protoplast lysates from C . acremonium are described . Conversion of radiolabelled penicillin N into deacetoxycephalosporin C is described . A proposal is made about the general types of mechanism involved in these conversions.

Experientia, 1980 May 15, 36(5), 550 - 2
The effect of two new peptide antibiotics, the hypelcins, on mitochondrial function; Takaishi Y et al.; The action on mitochondria of 3 peptide antibiotics, hypelcin-A, hypelcin-B, and alamethicin, was examined . The results showed that they are unique uncouplers of oxidative phosphorylation, with the same mechanism of action.

Z Kardiol, 1980 May, 69(5), 329 - 33
{The treatment of digitalis poisoning with antibiotics (author's transl)}; Hess T et al.; Digitalis intoxication occurs frequently and proves fatal in 5-10% of all cases . Treatment is limited to symptomatic measures . Glycoside-specific antibodies offer a new way of treatment of digitalis intoxication . In our experiments with cats, they were found to be highly effective in reversing digoxin-induced arrhythmias . Specific antibodies have previously been employed in a patient with suicidal digoxin intoxication . We report a case of nonsuicidal Lanatosid-C intoxication treated with F(ab')2-fragments of digoxin-specific antibodies from the sheep . The treatment was successful and without side-effects . Serum concentration of free digoxin and total digoxin measured during and after treatment showed a decrease of free and a sharp raise in total digoxin . For clinical use, antibody fragments are superior to intact antibodies . Problems and possible indications concerning the treatment of digitalis intoxication with antibodies are briefly discussed.

Antimicrob Agents Chemother, 1980 May, 17(5), 779 - 83
Concentrations of various antibiotics in serum and fluids accumulated in diffusion chambers implanted in various sites in rabbits; Georgopoulos A et al.; Diffusion chambers with Millipore membranes were implanted in soft tissue, kidneys, and peritoneal and pleural cavities of rabbits . Single doses of azlocillin, cefazolin, and gentamicin were injected intramuscularly and ampicillin was administered orally 2--5 weeks after implantation . The concentrations of the respective drugs in simultaneously collected samples of fluid from each diffusion chamber were measured and compared with concentrations found at the same time in serum . All chambers were tolerated well, and the method proved to be effective for collecting data on the distribution of drugs throughout the body.

Antibiotiki, 1980 May, 25(5), 383 - 7
{Clinical manifestations and the ways to prevent antibiotic allergy in nonspecific pulmonary pathology}; Gurin NG; Retrospective analysis of 555 cases with nonspecific pulmonary pathology was performed . Certain allergic reactions to antibiotics were revealed in 172 (30.8%) patients, while the physicians recorded such reactions only in 65 (11.7%) patients . Allergy to 2 or more drugs was more frequent . Antibiotic intolerance was mainly evident from the temperature increase (44%), skin eruption (22%), development or aggravation of the bronchospastic syndrome (12.2%), Quincke's edema (69%), blood eosinophilia (6.9%) and sometimes other reactions . The bronchospastic syndrome was largely observed in patients treated with antibiotic inhalations . Clinical manifestations of antibiotic allergy were concomitant in most cases . The temperature increase, skin eruptions and blood eosinophilia may be considered as the early manifestations of the allergy, while impairment of the bronchial patency as the late manifestation . Intolerance of antibiotics significantly lowers their efficiency . Rational use of antibiotics, due regard for the history of allergic reactions and in vitro tests for antibiotic susceptibility are important measures in prevention of allergic reactions to antibiotics.

Ann Microbiol (Paris), 1980 May-Jun, 131(3), 271 - 83
{Use of Autobac system in the study of the bacteriostatic effect of combinations of antibiotics (author's transl)}; Darbas H et al.; After determining the LSI80 (light scattering index 80) concentration X and Y of two antibiotics for a given bacteria by an automated light scatter photometric method, we use the same process to test the bacteriostatic effect of all the combinations between the values 2X, X, X/2, X/4, X/8 and 2Y, Y, Y/2, Y/4, Y/8 . The results read on the light scatter photometer are interpreted: --approximatealy by means of a simplified schematic diagram; --more precisely by drawing three curves: we begin with two inhibiton curves in order to determine the LSI50 concentrations (CLSI50) of each antibiotic, isolted and in the presence of defined concentrations of the complementary antibiotic; then from these CLSI50 we draw the bacteriostatic effect curve of the combination . When the LSI50 effect of the combination occurs with less than 50% of the CLSI50 of each isolated antibiotic, the combination is synergistic . It is antagonist if the bacteriostase is obtained with more than 100% of the CLSI50 of each isolated antibiotic . The intermediate percentages determine the indifferent effects . The additive effects come to an equilateral hyperbola passing through the points 50%-50%, 25%-75% . The Autobac system allows inoculum standardization, very simplified handlihg and automatic reading . It takes only 9 h to handle the complete process, including the determinations of the CLSI80 and the study of the combination . There is a high correlation between the results obtained and those given by the Patte and Chabbert "carre method".

Vestn Khir Im I I Grek, 1980 May, 124(5), 57 - 61
{Value of antibiotics in treated acute cholecystitis in elderly patients}; Sovtsov SA; The treatment of 673 patients with acute cholecystitis aged 70 and more was analyzed . Half of the patients were treated with antibiotics . Under study were 110 antibioticograms of bile of the operated patients . In 71% Escherichia coli was found sensible to tetracycline, chloramphenicol, monomycin and kanamycin . The results of the investigation show that use of antibiotics of the tetracycline order for the treatment of acute cholecystitic results in decreased mortality of patients aged 70 and older.

Arch Esp Urol, 1980 May-Jun, 33(3), 261 - 6
{Local antibiotic therapy in the treatment of chronic bacterial prostatitis}; Muntanola P et al.; In view of the great incidence of bacterial prostatitis and the small number of antibiotics which reach significant levels in the prostate gland, we have used Baert's local antibiotherapy on 24 patients suffering from chronic, bacterial prostatitis and in whom, previous treatment with trimethoprim-sulphamethoxazol had failed . 95.9% of sterilizations of prostate liquid growths were obtained six months after the treatment.

Antimicrob Agents Chemother, 1980 May, 17(5), 861 - 4
Effect of fatty acids on action of polyene antibiotics; Iannitelli RC et al.; Fatty acids cause a decrease in the absorption spectra of the antifungal polyene macrolide antibiotics nystatin, filipin, candicidin, and amphotericin B . For nystatin, filipin, and candicidin, this decrease in absorption could be correlated with the activity of the fatty acids in protecting the yeast Saccharomyces cerevisiae against the action of these antibiotics . With amphotericin B a correlation was observed between the decrease in absorption caused by certain derivatives of fatty acids and the protective action of these derivatives against the activity of amphotericin B on yeast . It is concluded that, like the sterols, fatty acids also interact with the polyene antibiotics and thereby reduce their effective concentrations.

Antibiotiki, 1980 May, 25(5), 375 - 81
{Experimental study of a new method of endolymphatic antibiotic administration and a trial of its clinical use}; Shcherbakova EG et al.; A new procedure for antibiotic administration via endolymphatic route was developed . Experiments performed on 34 dogs revealed differences in the pharmacokinetics of gentamicin in the central lymph after its administration in a dose of 4 mg/kg via endolymphatic and intramuscular routes: the maximum levels of 590 and 23 mg/kg were determined in 15 and 45 minutes respectively . In 1 hour the concentrations decreased to 17 and 10 mg/kg . When gentamicin was administered endolymphatically it remained in the lymph and blood in concentrations of 0.2 and 0.8 mg/kg respectively for 24 hours . The kinetics of gentamicin in the blood serum within the first 6 hours after its administration by both routes did not differ significantly . After endolymphatic administration high concentrations of gentamicin (56-36 mg/g) were determined in the paraaortal and retroperitoneal lymph nodes in 10-24 hours . Within the period of the 4th to the 13th day its concentrations of at least 5 mg/g were detected . The changes in the structure of the lymph nodes observed 18-48 hours after the antibiotic endolymphatic administration were reversible and returned to normal by the 96th hour . The first experience with the clinical use of the endolymphatic route of gentamicin administration showed its high efficacy in 84.8% of the patients with severe purulent inflammatory diseases of the organs of the abdominal cavity . The antibiotic was used in a dose of 80 mg once a day . The treatment course consisted of 5-6 infusions . Perspectives of the further experimental and clinical investigation of the procedure are indicated . Endolymphatic administration of antibiotics makes it possible to increase the efficacy of antibiotic therapy of a number of severe inflammatory infections.

Obstet Gynecol, 1980 May, 55(5 Suppl), 128S - 138S
Therapeutic considerations in the use of antibiotics in renal insufficiency; Whelton A; Virtually all antibiotics are excreted in part or in total by the kidneys . Therefore in various degrees of renal function impairment, systemic drug accumulation with dose-related toxicity may take place unless a readjustment is made in standard drug dosing principles . Good clinical practice dictates that the physician have some familiarity with the drug dosing changes that are necessary when patients with renal failure require antibiotic therapy . Correlation of the patient's renal function status with the selected antibiotic is the first step, after which drug dosing tables and nomograms serve as an immediate and practical guide to safe and effective therapy . Antibiotic dosing regimens in renal failure should always be monitored by analysis of serum drug levels when available to the clinician, as this is the best confirmation of safe and effective therapy . This review contains detailed metabolic and pharmacokinetic information that may be used as an additional clinical resource for the antibiotic therapy of patients with renal insufficiency.

Minerva Stomatol, 1980 May-Jun, 29(3), 163 - 82
{Fractures with loss of substance of the middle and upper third of the face: nosographic classification, surgical indications and the prevention of meningeal infections with the new antibiotic, cefuroxime}; Torrielli F et al.; Reference is made to considerable personal experience acquired in the treatment of craniofacial fractures, particularly those affecting the upper third of the face . An account is given of the anatomical and surgical features of the naso-ethmoid-frontal and temporo-orbito-sphenoid areas--now recognised as within the domain of maxillofacial surgery--and their symptomatologies . Particular attention is directed to the question of liquorrhoea and the possibility of ascendent infections of the meninges . Reduction is favoured with respect to the former, since forward and upward repositioning often leads to the regression of ethmoidal liquorrhoea . Exclusion of the frontal sinus is regarded as a "categorical imperative" as far as meningeal infection is concerned, and support is also given for its prevention with antibiotics . A personal preference is expressed for cefuroxim, a new antibiotic with particular potency and marked diffusibility within the cerebrospinal fluid.

J Antibiot (Tokyo), 1980 Apr, 33(4), 377 - 82
Studies on antibiotics BN-227 and BN-227-F, new antibiotics . II . Chemical structure of antibiotics BN-227 and BN-227-F; Itoh J et al.; The structure of a new antibiotic BN-227 was determined as I by physico-chemical methods . The X-ray analysis also suggested the structure of I . The structure of antibiotic BN-227-F was determined as II . The antibiotic BN-227-F was prepared by addition of a solution of ferric chloride to antibiotic BN-227.

J Antibiot (Tokyo), 1980 Apr, 33(4), 364 - 76
Mycinamicins, new macrolide antibiotics . I . Taxonomy, production, isolation, characterization and properties; Satoi S et al.; Mycinamicins, novel macrolide antibiotics were obtained from the culture broth of Micromonospora grisseorubida sp . nov . Isolation of five components, mycinamicins I, II, III, IV and V, was accomplished by silica gel adsorption or partition chromatography . Mycinsmicin I and II exhibit a strong UV absorption peak at 218 nm and have a shoulder at 240 nm . Mycinamicin III, IV and V show strong UV absorption peaks at 215 nm and around 280 nm . From their physicochemical and biological properties, the mycinamicins are classified as new macrolide antibiotics.

Antibiotiki, 1980 Apr, 25(4), 266 - 7
{Method of determining the concentration of the antibiotic nisin}; Baranova IP et al.; To accelerate determination of nizin concentrations by the agar-diffusion method it is suggested that Twin-80 be added to the agar . For making the media composition more simple, agarized phosphate buffer, pH 5.0, or agarized water, pH 7.0, is recommended to be used for the lower layer.

South Med J, 1980 Apr, 73(4), 533 - 4
Successful treatment of empyema with thoracocenteses and intrapleural antibiotics; Mittapalli MR; Daily thoracocentesis and treatment with an appropriate antibiotic instilled into the pleural space, continued until the returns are clear, may still have a significant role in the treatment of empyema, thereby avoiding the discomforts and disadvantages of chest tube insertion.

South Med J, 1980 Apr, 73(4), 444 - 7
Antibiotic-associated colitis: a persistent clinical problem; Davidson ED et al.; Examination of this series of 19 patients with antibiotic-associated pseudomembranous colitis revealed that most of the patients were given the antibiotics for trivial reasons . Many different antibiotics were identified as being related to the development of colitis . There were three deaths in this series; two of the 15 patients treated medically and one of the four treated surgically . The efficacy of all diagnostic procedures and medical therapies are discussed, and the role of surgery in treating patients with toxic state, sepsis, or perforation is presented.

J Antibiot (Tokyo), 1980 Apr, 33(4), 441 - 6
Antibiotics that specifically block translation in virus-infected cells; Lacal JC et al.; Several antibiotics including anthelmycin, blasticidin S, destomycin A, gougerotin, hygromycin B and edeine complex, known to powerfully block translation in cell-free systems, did neither inhibit protein synthesis in intact mouse L and 3T6 cells, nor in hamster BHK 21 cells, due to failure to cross the cell plasma membrane . However, after viral infection, these antibiotics exhibited a marked blockade of translation, that is related to the permeability changes induced by viral infection . The inhibition of protein synthesis by hygromycin B in virus-infected cells was studied over the time course of infection, both in encephalomyocarditis virus-infected mouse L cells and in Semliki forest virus-infected hamster BHK cells . We have observed that the entry of hygromycin B into virus-infected cells parallels the inhibition of cellular protein synthesis, i.e., the cells became permeable to this antibiotic at the time the shut-off of host translation occurred . A marked inhibition of picornavirus RNA synthesis by hygromycin B was also noticed, likely as a consequence of the inhibition of the viral replicase synthesis . Finally, a reduction in the virus yield by treatment of virus-infected cells with several antibiotics is also described . All these observations are considered in the context of the interference of viral infection with cellular functions and the potential use of inhibitors non-permeable to normal cells as antiviral agents.

Biochim Biophys Acta, 1980 Mar 28, 607(1), 171 - 80
Conformational analysis of nucleoside and nucleotide antibiotics prossessing five-membered base rings . A comparison of the glycosyl barrier for purine, pyrimidine and imidazole rings; Vijayaiakshmi KS et al.; The preferred conformations of the nucleosides comprising five-membered base rings viz., ribavirin, tetrazole, showdomycin and pyrazomycin and their 5'-nucleoside monophosphates have been explored by semiempirical potential energy calculations . The nature of the substituents on the five-membered base ring has been found to influence significantly the favoured glycosyl conformation and the hydrogen bonding between the base and the sugar . In the absence of any such hydrogen bonding, the imidazole nucleosides expectedly exhibit nearly 'free' rotation around the glycosyl bond for the commonly found C(3') endo and C(2') endo sugar ring conformations, thus increasing the probability of anti in equilibrium high-anti in equilibrium syn conformational interconversions as compared to common purine and pyrimidine nucleosides . However, the C(2') exo pucker imparts a high-energy barrier to glycosyl rotation, locking the base in the high-anti region . The conformation behaviour is significantly modified in the nucleoside 5'-monophosphates . The additional attractive interactions between the carboxamide and the phosphate groups favour the syn glycosyl conformation in the 5'-monophosphates of ribavirin as well as pyrazomycin smaller to guanosine 5'-monophosphate whereas the anti conformation is strongly favoured for the 5'-nucleotides of tetrazole and showdomycin similar to other common purine and pyrimidine nucleotides . The conformational properties of five-membered base ring nucleosides have a strong resemblance to purine nucleosides . Molecular modelling studies reveal that only the anti or high anti-glycosyl conformations of ribavirin can mimic the inosine base . It is suggested that experiments on the configurational isomers of ribavirin, viz., aravirin and cycloaravirin would conclusively establish the conformational specificity and biological function of ribavirin and analogues.

Br Med J, 1980 Mar 22, 280(6217), 836 - 8
Family trends in psychotropic and antibiotic prescribing in general practice; Howie JG et al.; A ten-year retrospective study of the consultations of 50 families with a city general practice was used to test the hypothesis that mothers who receive an excess of psychotropic drugs have children who receive an excess of psychotropic drugs have children who receive an excess of antibiotics for episodes of acute respiratory illness . The children of the 10 mothers classed as high psychotropic users were seen twice as often with acute respiratory illness and received twice as many antibiotics as the children of the mothers who had received no psychotropic medication . The association between high psychotropic and high antibiotic use was not linked in time, and indeed the time of highest antibiotic use coincided with the time when the mother received fewest psychotropic prescriptions . It is suggested that at many of these consultations the mother rather than the child should have been treated as the patient.

Biochemistry, 1980 Mar 4, 19(5), 865 - 70
Interaction of elongation factor Tu with the ribosome . A study using the antibiotic kirromycin; Sander G et al.; Elongation factor Tu (EF-Tu) dependent GTP hydrolysis normally requires the presence of ribosomes and aminoacyl-tRNA (aa-tRNA) . In the presence of the antibiotic kirromycin, the factor alone displays a GTPase activity that is enhanced by ribosomes and/or aa-tRNA {Wolf, H., Chinali, G., & Parmeggiani, A . (1974) Proc . Natl . Acad . Sci . U.S.A . 71, 4910-4914} . Using this system, we have found the following: (1) the 50S ribosomal subunit can substitute the 70S ribosome; (2) the 50S CsCl core a, b, and c particles {Sander, G., Marsh, R . C., Voigt, J., & Parmeggiani, A . (1975) Biochemistry 14, 1805-1814}, lacking an increasing number of proteins, can induce ca . 65, 45, and 25%, respectively, of the EF-Tu-kirromycin GTPase activity of control 50S subunits, in the presence of 30S subunits and aa-tRNA; (3) addition of proteins L7/L12 with L10, but not of proteins L7/L12 free from L10, restored the activity of all the 50S CsCl cores in the EF-Tu-kirromycin-dependent GTPase to 70-90% of the control; (4) proteins L7/L12, with or without contaminating L10, did not induce any EF-Tu-dependent GTPase activity, in contrast to a recent report {Donner, D., Villems, R., Liljas, A., & Kurland, C . G . (1978) Proc . Natl . Acad . Sci . U.S.A . 75, 3192-3195}, whether EF-Ts and/or kirromycin were present or not.

Pol J Pharmacol Pharm, 1980 Mar-Apr, 32(2), 217 - 24
Toxicological studies on the new veterinary antibiotic turimycin; Hartl A et al.; The acute toxicity of turimycin investigated in several animal species and following different routes of administration is low . In mice the LD50 values range from 320 mk/kg after iv injection up to more than 3000 mg/kg when administered orally . When lethal or sublethal doses of turimycin were given, animals either developed clonic convulsions and died within 24 hr, or recovered completely . The main pharmacological effect of turimycin is a reversible, dose dependent decrease in the blood pressure after intravenous injection of 10 to 15 mg/kg in cats and dogs . This may be due to the negative inotropic and chronotropic effect on heart muscle (isolated atria of guinea-pigs) and to the spasmolytic effect on the smooth muscle (rat ileum) . A temporary decrease of the renal filtration rate after administration of turimycin is probably caused by its influence on the blood pressure . In rats the hexobarbital sleeping time was increased after repeated administration of higher doses of turimycin . In a chronic study on dogs oral doses of 50 and 125 mg/kg of turimycin, given in capsules daily for 12 months, produced no functional or histopathological abnormalities.

Res Commun Chem Pathol Pharmacol, 1980 Mar, 27(3), 521 - 31
Alterations of mitochondrial respiration induced by aminoglycoside antibiotics; Weinberg JM et al.; In vitro gentamicin treatment stimulates State 4 mitochondrial respiration and inhibits State 3 and DNP-uncoupled respiration . These effects are qualitatively similar in both hepatic and renal mitochondria . Threshold gentamicin concentrations for these effects were between 1 and 2 mM for renal mitochondria while hepatic mitochondria were slightly more sensitive . Neomycin, kanamycin, and streptomycin had effects qualitatively similar to those of gentamicin on State 4, State 3, and DNP-uncoupled respiration . The potency of the aminoglycosides in producing these effects strongly correlated with the number of ionizable amino groups present on the aminoglycoside molecule suggesting that cationic charge is an important molecular determinant of aminoglycoside-induced mitochondrial toxicity.

J Pharm Sci, 1980 Mar, 69(3), 354 - 6
Serum protein binding alterations of selected cephalosporin antibiotics by fatty acids and their derivatives; Pitkin DH et al.; Saturated fatty acids containing 10--14 carbon atoms were more potent inhibitors of serum protein binding than those containing shorter or longer carbon chains . Introduction of unsaturation into chains containing 16 or 18 carbons increased their inhibitory potency . Triglycerides and fatty acid esters, chlorides, thiols, and amides had no inhibitory activity . When inhibition was observed, it was concentration dependent and occurred when the molar ratio of fatty acid to protein equaled or exceeded three . The change in percent serum protein binding in the presence of an effective inhibitor was the greatest with cephalosporins that were most highly bound in the absence of an inhibitor.

J Antibiot (Tokyo), 1980 Mar, 33(3), 280 - 3
FR-900137, a new antibiotic . II . Structure determination of FR-900137; Kuroda Y et al.; The structure of FR-900137, a new antibiotic produced by a new strain of Streptomyces has been established as methyl hydrogen N1-methyl N2-(L)-leucyl phosphorohydrazidate on the basis of spectroscopic and chemical evidence.

J Antibiot (Tokyo), 1980 Mar, 33(3), 267 - 71
FR-900148, a new antibiotic . II . Structure determination of FR-900148; Kuroda Y et al.; The structure of FR-900148, a new antibiotic produced by a strain of Streptomyces xanthocidicus, has been established as 1-N-valyl-3-chloro-2,5-dihydro-5-oxo-1H-pyrrole-2-carboxylic acid on the basis of spectroscopic and chemical evidence.

Clin Orthop, 1980 Mar-Apr, (147), 167 - 9
The effect of previous surgery, operating room environment, and preventive antibiotics on postoperative infection following total hip arthroplasty; Nelson JP et al.; In 711 consecutive total hip arthroplasty operations, approximately 80% of patients were followed one to 7 years . Per priman operations outnumbered hips having had previous operations 511 to 200 . The incidence of infection was higher in the hips having had previous operations (1.6 vs 3.5%) . The overall incidence of deep infection was 16/711, or 23% . Analysis of the influences of operating room environment and preventative antibiotics revealed that there was a marked decrease in the attack rate of deep infection (7.6 vs 0.6%) when the Clean Room, personnel-isolator system, and preventative antibiotics were used . Reduced intraoperative wound bacterial contamination is accompanied by a reduced incidence of sepsis.

Gastroenterology, 1980 Mar, 78(3), 431 - 4
Symptomatic relapse after oral vancomycin therapy of antibiotic-associated pseudomembranous colitis; Bartlett JG et al.; Twenty patients with antimicrobiol-associated diarrhea had a symptomatic relapse after oral vancomycin therapy . All patients had stool examinations which implicated C . difficile as the causative agent, and 16 had pseudomembranous colitis . Clinical courses were characterized by resolution of symptoms with recurrence of diarrhea at 4--21 days after vancomycin was discontinued . Studies of stools collected sequentially showed that vancomycin failed to eliminate C . difficile despite susceptibility to this agent with in vitro testing . A review of our records shows the incidence os symptomatic relapse is approximately 14% . This experience emphasizes the importance of adequate follow-up in patients treated with oral vancomycin for antibiotic-associated diarrhea or colitis due to C . difficile.

J Antibiot (Tokyo), 1980 Mar, 33(3), 310 - 6
A novel method for evaluating the outer membrane permeability to beta-lactamase-stable beta-lactam antibiotics; Kojo H et al.; A novel method is described which allows estimation of the outer membrane permeability to beta-lactamase-stable beta-lactams by determining antibiotic concentrations in the periplasm . The method is based on measurement of the inhibiting activity of beta-lactamase-stable beta-lactams on the hydrolysis of a substrate by periplasmic beta-lactamase . Application of the method to carbenicillin revealed that the high level of resistance to carbenicillin of an Escherichia coli strain acquiring the plasmid encoding ampicillin resistance resulted from the poor ability of carbenicillin to penetrate the outer membrane of E . coli.

Br Med J, 1980 Feb 2, 280(6210), 275 - 7
Rational use of antibiotic therapy after appendicectomy; Pinto DJ et al.; A prospective randomised trial was carried out on 263 patients admitted for appendicectomy . In those patients with normal or inflamed appendix only, wound sepsis occurred in five (5%) of the 96 patients receiving metronidazole compared with seven (7%) of the 91 controls . In patients with gangrenous or perforated appendices, however, 15 of the 32 patients (47%) receiving ampicillin and five (16%) of 31 patients receiving metronidazole developed a wound infection (p less than 0.025) . Therapeutic courses of metronidazole significantly reduced wound sepsis rate in those with gangrenous or perforated appendices . Together with another antibiotic it should form part of the management of such patients, but antibiotics are unlikely to reduce further the low rate of wound infection in patients with normal or inflamed appendices.

Poult Sci, 1980 Feb, 59(2), 268 - 73
Compatibility and anticoccidial activity of lasalocid in combination with roxarsone and antibiotics against Eimeria mixed infection in chicks; Schildknecht EG et al.; Lasalocid at the concentration of .0075% (68 g/ton) with and without roxarsone 45.4 g/ton was fed in combination with the growth promotants bacitracin methylene disalicylate 200 g/ton, bambermycins 2 g/ton, lincomycin 4 g/ton, nosiheptide 2.5 g/ton, zinc bacitracin 200 g/ton g/ton, and virginiamycin 20 g/ton exhibited a high degree of anticoccidial activity against mixed Eimeria infection in chickens in 9 day challenged battery trials . In these short term challenge trials chicks fed lasalocid, and the lasalocid growth promotant combinations, performed significantly better (P < .05) for growth and anticoccidial efficacy than those fed the growth promotants alone, and the infected, unmedicated controls . In almost all instances, the lasalocid-roxarsone-antibiotic combinations allowed for numerical increases in gains, improvement in feed conversion, and numerical decreases in lesions (in some cases, statistically significant (P < .05) over chicks fed lasalocid alone and/or the lasalocid antibiotic combination . The growth promotants did not interfere with the anticoccidial activity of lasalocid . The growth promotants fed alone exhibited no anticoccidial activity . However, when roxarsone was combined with the antibiotics, the combination resulted in numerically improved performance, reduced mortality, and in most instances, statistically significant decreases in lesions (P .05) over the infected, unmedicated control.

Chirurg, 1980 Feb, 51(2), 106 - 9
{Orthograde intestinal irrigation as a preoperative intestinal preparation . Reduction of the intestinal flora using antibiotics}; Huk I et al.; Whole gut irrigation is a now a well-established method of preoperative bowel preparation . Additional reduction of bacterial content is desirable . The influence of neomycin/bacitracin and clindamycin as well as the combination, as admixture to the whole gut irrigation, on the flora of the large intestine, was therefore investigated in a prospective controlled study . While neomycin/bacitracin caused only a reduction of aerobic, and clindamycin of the anaerobic bacteriae, the combination resulted in a nearly total eradication of detectable bacterial content at the time of operation.

J Antibiot (Tokyo), 1980 Feb, 33(2), 205 - 12
Macbecins I and II, new antitumor antibiotics . II . Isolation and characterization; Muroi M et al.; New antitumor antibiotics, macbecins I and II, were isolated from the culture broth of Nocardia sp . No . C-14919 . Macbecins I and II belong to the ansamycin group and have a benzoquinone and hydroquinone nucleus, respectively . Both showed antitumor activity against murine leukemia P 388 in vivo.

J Antibiot (Tokyo), 1980 Feb, 33(2), 144 - 56
Studies on the ionophorous antibiotics . XXV . The assignments of the 13C-NMR spectra of dianemycin and lenoremycin; Mizoue K et al.; All the resonances observed in the 13C-NMR spectra of polyether antibiotics, dianemycin and lenoremycin (Ro 21-6150) have been assigned by the aid of selective proton decoupling experiments, T1 value measurements and biosynthetic methods as well as comparison to model compounds such as monensin, nigericin, etheromycin and carriomycin.

J Antibiot (Tokyo), 1980 Feb, 33(2), 132 - 6
FR-900130, a novel amino acid antibiotic . II . Isolation and structure elucidation of the acetyl derivative of FR-900130; Kuroda Y et al.; FR-900130 is a new antibiotic having an acetylene moiety and is very unstable in aqueous solution . The antibiotic was isolated as the acetyl derivative by ion-exchange resin and adsorption chromatography . The structure has been determined to be L-2-amino-3-butynoic acid by spectral data of its derivatives.

Br J Surg, 1980 Feb, 67(2), 140 - 1
The delayed treatment of wounds of the hand and forearm under antibiotic cover; Morgan WJ et al.; In wounds of the hand and forearm treated within 4 h of injury, prophylactic clindamycin, in a dose of 150 mg 6-hourly for 5 days, did not reduce the infection rate . In wounds treated after 4 h the infection rate was reduced, but not significantly so . There was a significant reduction in the infection rate comparing all wounds treated within 4 h with those treated after 4 h . Early treatment of wounds is more important than prophylactic antibiotics, although these may have a part to play where late treatment is unavoidable.

J Pharm Sci, 1980 Feb, 69(2), 229 - 30
13C-NMR spectroscopy of three tetracycline antibiotics: minocycline hydrochloride, meclocycline, and rolitetracycline; Mazzola EP et al.; 13C-NMR data and spectral assignments are presented for tetracycline antibiotics minocycline hydrochloride, meclocycline, and rolitetracycline.

Antibiotiki, 1980 Feb, 25(2), 126 - 9
{Comparative study of rifampicin distribution in the body of pregnant and nonpregnant white rats exposed to the antibiotic by inhalation}; Zel'tser IZ et al.; When rifampicin was administered to albino rats in the form of inhalations, it was absorbed by the blood and penetrated into various organs, the levels of the antibiotic in the biosubstrates being dependent on its concentration in the inhalation air . Rifampicin distribution in the gravid animals was mainly of the same character as that in the nongravid rats . However, when the animals were exposed to the antibiotic effect during the whole period of the gravidity, a significant increase in the antibiotic levels in the blood and internal organs was observed.

J Histochem Cytochem, 1980 Feb, 28(2), 161 - 8
Evaluation of the polyene antibiotic filipin as a cytochemical probe for membrane cholesterol; Robinson JM et al.; Distribution of the filipin-cholesterol complexes has been studied by freeze-fractures techniques . While filipin-cholesterol complexes are formed in fixed as well as unfixed cells, the distribution of the complexes varies with fixation . Furthermore, filipin induces dramatic rearrangement of intramembrane particles in unfixed, but not in fixed, cells . Examination of thin sections of filipin-treated cells shows that filipin alone induces substantial cellular damage, while filipin treatment simultaneous to fixation or following fixation does not cause noticeable damage . For filipin to be an effective cytochemical probe of membrane structure, cellular damage must be minimized; this is best achieved by treating cells with filipin following glutaraldehyde fixation.

Cutis, 1980 Feb, 25(2), 216 - 8, 220
Topical antibiotic therapy of acne: laboratory investigation of vehicles, various antibiotics, and stability characteristics; Stoughton RB et al.; A new vehicle preparation has proved effective in enhancing the penetration of antibiotics . The vehicle seems to maintain stability of the incorporated antibiotic.

Anaesth Intensive Care, 1980 Feb, 8(1), 34 - 8
Antibiotics--their administration, choice and prophylactic use; Goodwin CS; A wider range of antibiotics is now available with the advent of two new cephalosporins--cefamandole and cefuroxime, and the first cephamycin--cefoxitin . These drugs may be particularly useful in the treatment of septicaemia, and when combined with ticarcillin are effective against nearly all pathogens . Cefuroxime can be given intramuscularly . Intravenous cotrimoxazole must be given in large doses to achieve therapeutic concentrations in the cerebrospinal fluid . The correct use of antibiotics for prophylaxis demands an accurate knowledge of the organisms likely to cause infection and the most efficient way of using the antibiotics to prevent that infection . There is little argument about the need for prophylaxis to prevent recurrent rheumatic heart disease or tetanus from a contaminated wound . However, in the various areas of surgery a wide range of antibiotics is used not always as a result of controlled trials having proved their value . Non-surgical situations for prophylaxis are briefly reviewed.

Antibiotiki, 1980 Feb, 25(2), 121 - 6
{Possibility of reversing the action of the membranotropic antibiotic, gramicidin S, on bacteria}; Bulgakov VG et al.; The study on the possibility of eliminating gramicidin S from the bacterial cells which had adsorbed it showed that a part of the labeled antibiotic bound by the bacteria may be washed out with buffer or salines . When the cells which had adsorbed gramicidin S were treated with lecithin emulsion, a significant part of the bound antibiotic was transferred to the lecithin liposomes . This turned the gramicidin S effect to the cells: significant but not complete reduction of the membrane barrier properties and dehydrogenase reactivation . Elimination of gramicidin S also reduced the colony forming capacity in a part of the cells.

Methods Find Exp Clin Pharmacol, 1980 Feb, 2(1), 45 - 51
Neuromuscular blocking activity of aminoglycoside antibiotics; Paradelis AG et al.; The aminoglycoside antibiotics possess neuromuscular blocking activity; the potency of those antibiotics tested appears to be as follows: gentamicin greater than streptomycin greater than amikacin greater than sisomicin greater than kanamycin = tobramycin greater than kanendomycin = dibekacin . The neuromuscular blockade produced by these antibiotics is not reversed by neostigmine, whereas it is reversed by calcium . Calcium not only has the ability to restore the neuromuscular transmission but also to exert protective action against the neuromuscular blocking activity of aminoglycoside antibiotics; these antibiotics are also potentially capable of interacting with non-depolarizing muscle relaxant drugs (d-tubocurarine, pancuronium) or propranolol, a beta-adrenergic receptor blocking agent . This interaction results in respiratory depression and/or prolonged apnoea . Our findings lead to the assumption that amino-glycoside antibiotics are involved in the process of acetylcholine release by nerve impulses, antagonizing calcium ions.

Arch Microbiol, 1980 Feb, 124(2-3), 229 - 32
In vitro degradation of guanosine 3',5'-bis(diphosphate) {ppGpp} by the spoT gene product {ppGppase} from auxotrophic strains of Escherichia coli: effects of various antibiotics and drugs; Richter D; The enzyme specifically hydrolyzing guanosine 3',5'-bis(diphosphate) {ppGpp} has been isolated from the ribosomal fraction of Escherichia coli; it released pyrophosphate from the 3'-position of ppGpp . The effects of various drugs and antibiotics known to interfere with protein and/or RNA synthesis were investigated in the ppGpp degrading reaction . It was determined that tetracycline, chlorotetracycline, and thiostrepton strongly inhibited the reaction, whereas levallorphan gave a moderate inhibition . Only the tetracycline-mediated inhibition could be reversed by manganese ions . Oxytetracycline, rifampicin, fusidic acid, kirromycin, streptomycin, puromycin, chloramphenicol, and morphine did not inhibit the decay reaction.

S Afr Med J, 1980 Jan 26, 57(4), 114 - 6
{Antibiotic peritoneal lavage in acute peritonitis resulting from septic abortion or a ruptured pyosalpinx}; Nel H; An analysis is given of 16 patients who presented with acute peritonitis during the years 1976-1978 and who were treated by means of antibiotic peritoneal lavage . The history and technique of peritoneal laage are discussed.

Biochim Biophys Acta, 1980 Jan 25, 595(2), 277 - 90
Selective release of non-electrolytes from liposomes upon perturbation of bilayers by temperature change or polyene antibiotics; Oku N et al.; A new system for assaying the permeability characteristics of liposomes was established using Amicon cells equipped with a membrane filter (pore size, 0.3 micrometer) . In this system, damage of liposomes during the assay procedure was negligible . Changes in permeability to non-electrolytes, such as glucose (Mr 180), sucrose (Mr 342), inulin (Mr 5000) and dextran (Mr 75000), induced by perturbation of the bilayers were examined with this system . The following results were obtained on the barrier properties of multilamellar liposomes modified by various treatments . 1 . Amphotericin B and nystatin did not cause any change in permeability to glucose of egg yolk phosphatidylcholine liposomes prepared in physiological saline and containing trace amounts of radioactive markers in their aqueous compartments . Both antibiotics, however, induced nonspecific release of glucose, sucrose, inulin and dextran from liposomes that contained 0.3 M glucose in their aqueous compartments . These antibiotics first seem to form pores through which small ions can permeate; Na+ and Cl- can enter the liposomes through these pores, whereas glucose in the liposomes cannot pass out . As a result, the liposomes become swollen with consequent severe disruption of their membranes . 2 . Filipin and digitonin disrupted the membrane structures, resulting in release of large molecules such as dextran even in the absence of an osmotic mechanism . 3 . Perturbation of the phase equilibrium by temperature change resulted in formation of 'pores' . The penetration of cations and anions through these 'pores' was apparently much faster than that of glucose, since when liposomes swollen in 0.3 M glucose were incubated in salt solution they were disrupted by an osmotic mechanism releasing not only glucose but also dextran . Most of the 'pores' were not large enough to allow passage of large non-electrolytes, such as inulin and dextran, since no appreciable amounts of these markers were released from liposomes under conditions where there should be no osmotic gradient . 4 . At a temperature well above the phase transition temperature, egg yolk phosphatidylcholine liposomes exhibited specific release of glucose . This process did not involve an osmotic gradient, indicating that it was mainly due to diffusion of the solutes through the bilayers.

Can Med Assoc J, 1980 Jan 12, 122(1), 49 - 52
Antibiotic misuse in a pediatric teaching hospital; Schollenberg E et al.; Antibiotic use at a pediatric teaching hospital was reviewed for a month . A total of 188 courses of therapy were evaluated with respect to choice of antibiotic, dosage and necessity of treatment . Errors in therapy were noted in 30% of the medical orders and 63% of the surgical orders . The most frequent error, unnecessary therapy, was found in 13% and 45% of the medical and surgical orders respectively . Error rates were highest for the most frequently ordered antibiotics, notably the penicillins . The magnitude of the problem appeared to be similar to that previously reported from general ana adult hospitals . The difficulties with solutions such as educational programs and compulsory consultation are discussed.

Arch Otorhinolaryngol, 1980, 229(3-4), 255 - 9
Occurrence of non-ototoxic antibiotic (cephazolin) in the inner ear; Tachibana M et al.; Cephazolin, a non-ototoxic antibiotic, and kanamycin, an ototoxic antibiotic, were administered to the guinea pig systemically and their tissue concentration was measured . Not only kanamycin but also cephazolin did occur in the inner ear as well as in the kidney and other tissues . Therefore, it is most likely that the accumulation of an antibiotic inside the inner ear forms only a sine qua non for its ototoxicity . The mechanism of the ototoxicity should exist in the antibiotic-vulnerable cells (hair cells) themselves.

Arch Otorhinolaryngol, 1980, 226(3), 129 - 33
Supra-normal sensitivity to ototoxic antibiotic of the developing rat cochlea; Carlier E et al.; A period of increased sensitivity to the ototoxic antibiotic amikacin was found in the cochlea of the developing rat . Starting either at birth, 10 or 30 days of age, rat were injected i.p . daily with 200 mg/kg of amikacine for 10 days . Only in the group injected with drug from 10 to 20 days of age was there evidence of a substantial (40-100 dB) permanent threshold shift (PTS) . To characterize the period of supra-normal sensitivity more precisely, independent groups of pups were injected with 50 mg/kg of amikacin from 10 to 20, 15 to 25, 20 to 30, and 30 to 40 days of age . Only those pups injeced from 10 to 20 or 15 to 25 days of age showed PTS (30-60 dB) . These data, taken together with those on rat cochlear maturation indicate that the sensitive period to ototoxicity starts at the age of onset of cochlear function (around day 10) and ends few days after the cochlea shows adult-like characteristics (3rd postnatal week).

Zentralbl Gynakol, 1980, 102(12), 659 - 63
{Prophylactic antibiotics in Cesarean section (author's transl)}; Schulze G; Report of maternal infections by 498 abdominal deliveries in the years 1968--1975 . Three groups of patients were analyzed retrospectively: 1 . group: patients without antibiotics; 2 . group: patients with prophylactic antibiotics; 3 . group: patients with secondary dose from antibiotics . - The maternal infections was lower significant in the second group . Although prophylactic antibiotics by cesarean section non indicated because of an ascent from hospital infections.

Cytobios, 1980, 28(110), 95 - 102
Effects of the antibiotics penicillin, streptomycin, and tetracycline on the karyology of Oedogonium gunnii Wittr . (Chlorophyceae); Srivastava S et al.; Effects of penicillin, streptomycin and tetracycline were seen on the karyology of a filamentous green alga, Oedogonium gunnii Wittr . Various nuclear and chromosomal aberrations such as, fragmentation of the chromosomes, extreme clumping and unequal groupings of the chromosomes, vacuolization of nuclei and nucleoli, and irregular anaphase chromatid breaks, were observed in the materials treated with 500 and 750 micrograms/ml streptomycin, and 250 and 500 micrograms/ml tetracycline, and which, however, were not seen with any of the concentrations of penicillin employed . With lower concentrations of the three antibiotics given continuously for longer duration, several aberrations were observed . The frequency of the aberrations did not seem to follow a regular pattern and varied with each antibiotic and the duration of treatment.

Biol Bull Acad Sci USSR, 1980 Jan-Feb, 7(1), 40 - 6
Effect of N-nitrosomethylurea on substrains of Fisher lymphadenosis L-5178 resistant to antitumoral antibiotics; Minenkova EA et al.; A cytogenetic analysis of variants of Fisher mouse lymphadenosis L-5178 resistant to the antitumoral antibiotics bruneomycin and rubomycin C showed that the cytogenetic characteristics of the changes in the tumor cell population correlate with the chemotherapeutic indices of the development of drug resistance . Cytogenetic and kinetic analyses showed that variants of Fisher lymphadenosis L-5178 resistant to bruneomycin and rubomycin C retain sensitivity to N-nitrosomethylurea (NMU) . The activity of NMU in an experiment on resistant substrains of lymphadenosis can serve as a basis for the clinical use of NMU in the treatment of lymphomas resistant to antibiotics.

Arch Otorhinolaryngol, 1980, 228(3), 163 - 70
Histological evaluation of ototoxic reaction due to some aminoglycoside antibiotics; Bamonte F et al.; Twenty-one days s.c . treatment with netilmicin, gentamicin, sisomicin, and kanamicin at different doses were performed in albino guinea pigs of both sexes . Block surface preparation of Corti's organ was carried out and missing OHCs and IHCs counted in selected areas of each turn . The animals treated with gentamicin and sisomicin showed a dose-depending missing of hair cells, preferably relative to the outer ones and quantitatively the same for both the antibiotics . Furthermore, a characteristic distribution of the damage progressively increasing from the apex to the basal turn of the cochlea was detected . Kanamicin at 267 and 400 mg/kg gave the complete destruction of OHCs and IHCs along the whole cochlea while at 178 mg/kg did not show any significant damage in comparison to the control group . Finally, netilmicin neither damaged Corti's organ nor statistically determined missing OHCs and IHCs at all the doses used . These histological results and the previous electrophysiological and reflexological observations obtained in the guinea pig show a higher safety of netilmicin in comparison to the other aminoglycosides used for the problem relative to ototoxicity.

Microbios, 1980, 27(107), 41 - 57
Chemical composition of the cell wall of Cryptostroma corticale: effects of antibiotics on cell morphology; Abbey SD et al.; The chemical composition of the cell wall from four strains of Cryptostroma cortical was examined and was found to be of the chitin-glucan type . The composition was consistent among the four strains . The effects of the antibiotics repamycin, ramihyphin, aculeacin-A, cytochalasin and polyoxin-D on cell morphology were studied, using electron and light microscopy.

Int Arch Allergy Appl Immunol, 1980, 63(2), 170 - 7
Saponin and other haemolysins (vitamin A, aliphatic amines, polyene antibiotics) as adjuvants for SRBC in the mouse . Evidence for a role for cholesterol-binding in saponin adjuvanticity; Bomford R; The hypothesis that the adjuvant, as well as the haemolytic, activity of saponin depends on binding to cholesterol in cell membranes is supported by showing that cholesterol absorbs out adjuvant activity, and inhibits immunopotentiation in vivo when added to the injection mixture . Also, out of a range of haemolytic substances, chosen for their known properties as adjuvants or for cholesterol binding, the only materials which displayed a comparable activity to saponin were the polyene antibiotics Nystatin and Amphotericin B, whose binding to membrane cholesterol causes similar morphological changes to that of saponin.

Infection, 1980, 8(3), 119 - 20
Mycoplasma pneumoniae infection, antibiotics and exanthema; Macfarlane J; A retrospective survey of 81 patients with serologically proven Mycoplasma pneumoniae infection revealed that 72% received two or more different antibiotics during their illness, ampicillin and other penicillins being most frequently used . Fifteen (18.5%) patients had a skin rash, most commonly an erythematous maculopapular rash . It is suggested that such rashes may be due to antibiotics and, unlike mucocutaneous vesicular rashes, are probably not a useful indication of mycoplasmal pneumonia.

Vet Med Nauki, 1980, 17(1), 64 - 9
{Morphological and enzymatic changes in chicks treated with antibiotics}; Veselinova A et al.; The live, kidney and skeletal muscules of 54 chickens fed experimentally with bacitrazin, gallimycin, oleandomycin, tetracyclin, tylan, chlornitromycin, streptomycin and penicillin, and of 10 control birds were investigated pathomorphologically and histochemically (succinate--and lactate-dehdrogenase and esterase) . Parenchymal dystrophy in the epithelial cells of the liver and kidney and areactive necrotic foci amid the parenchyma were assessed . Dystrophic and necrotic changes observed in the muscle fibres of treated birds . Reduced enzyme activity was proven . The studies indicate that the morphological and enzyme changes in the liver, kidney and skeletal muscules of chickens treated with bacitrazin, gallimycin, chlornitromycin and streptomycin are greater than these observed in birds fed with tylan, tetracyclin, olenadomycin and penicillin . It is proven that the morphological and enzyme changes established in healthy chickens fed with prophylactic antibiotic doses are due to the antibiotics applied.

Arkh Patol, 1980, 42(8), 14 - 8
{Macrophage reaction as a component part of the pathomorphosis in antibiotic therapy (proceedings)}; Khmel'nitskii OK et al.; The role of mononuclear phagocytes as universal carriers of biologically active substances in a focus of inflammation is clearly seen in mediated effect of polyenic antibiotic in experimental candidiasis . This function of macrophages is very important in the mechanism of action of polyenic antibiotics and is a component of pathomorphosis in antibiotic therapy, since it affects the relationship of cells in a forming inflammatory focus.

Infection, 1980, Suppl 1, 49 - 53
Significance of pleural and sputum concentrations for antibiotic therapy of bronchopulmonary infections; Lode H et al.; Tests were done with various antibiotics (ampicillin, carbenicillin, cefazolin, cefotaxime, cephradine, ticarcillin) in order to determine the significance of sputum and pleural concentrations for adequate therapy of bronchopulmonary infections . In a total of 19 chronic bronchitis patients, it was found that the attainable sputum concentrations were rather low and that individual fluctuations were great . No clear connection was evident between dosage and concentration of antibiotics in the sputum . In 17 patients with exudative pleurisy, test data yielded in pleural kinetics largely corresponded with data from animal experiment models . The pleural cavity can be described as a partial extracellular, extravascular compartment in which the concentration course probably correlates more to the interstitial lung concentrations than to that of the sputum.

Infection, 1980, Suppl 1, 21 - 4
The pharmacokinetic basis of optimal antibiotic dosage; von Hattingberg HM et al.; Pharmacokinetic parameters play an important part in the design of an optimal dosage schedule for a drug . These parameters are only of use to the clinician if they can be obtained reliably and without too much experimental or mathematical effort, and their predictive value is independent of elaborate pharmacokinetic models . The three cardinal parameters of clearance (CI), total volume of distribution (Vss) and mean time (T), are defined and different methods are described for their assessment in clinical practice . A more operational method for estimating T than the one recorded in the literature is recommended . The value of this new method is demonstrated by means of an evaluation of data on gentamicin from the literature which have not already been analysed pharmacokinetically, and a comparison with results obtained by classical and more costly methods.

Folia Microbiol (Praha), 1980, 25(3), 207 - 12
Spontaneous variability of Streptomyces glomeratus, a producer of the amthracycline antibiotics beromycins; Blumauerova M et al.; Spontaneous variants of the beromycin-producing strain Streptomyces glomeratus 3980 were divided into five groups (A-E) according to increasing antibiotic activity . The most active variants (group E) differed from the other types and the wild strain by a suppressed ability to produce aerial mycelium and melanoid piogment and by an increased production of propionic acid . Strains with a 12-fold higher antibiotic production capacity (with respect to strain 3980) were obtained by selection of superior segregants from submerged cultures of the E type.

Infection, 1980, 8(2), 58 - 62
A diffusion chamber technique for measuring concentrations of antibiotics in interstitial fluid; Laber G et al.; A method for collecting soft tissue interstitial fluid in experimental animals for the measurement of antibiotic concentrations is described . Diffusion chambers with permeable membranes of 0.45 micron porosity were implanted subcutaneously for four days in order to determine simultaneous concentrations of ampicillin and clindamycin in serum and chamber fluid after perioral administration in rabbits and of oxytetracycline after intravenous injection in dogs . The results are discussed in view of findings from other investigators using different types of tissue cages.

J Antibiot (Tokyo), 1980 Jan, 33(1), 29 - 35
Studies on new phosphonic acid antibiotics . IV . Structure determination of FR-33289, FR-31564 and FR-32863; Kuroda Y et al.; The structure of novel phosphonic acid antibiotics FR-33289, FR-31564, and FR-32863, produced by strains of Streptomyces, have been established as I, II, and III, respectively, on the basis of spectroscopic and chemical evidences.

J Antibiot (Tokyo), 1980 Jan, 33(1), 19 - 23
Studies on new phosphonic acid antibiotics . II . Taxonomic studies on producing organisms of the phosphonic acid and related compounds; Iguchi E et al.; A new species of Streptomyces which produces a new cell wall-inhibitory antibiotic, FR-900098 containing phosphonic acid in its molecule, is named and described . The species name proposed, Streptomyces rubellomurinus, refers to the aerial mass color . Streptomyces rubellomurinus subsp . indigoferus also produces FR-900098 and the related compound FR-33289 . FR-900098 related compounds, FR-32863 and FR-31564 are produced by Streptomyces lavendulae.

Antimicrob Agents Chemother, 1980 Jan, 17(1), 87 - 8
Inhibition of candidacidal activity of human neutrophil leukocytes by aminoglycoside antibiotics; Ferrari FA et al.; We have tested the effect of five aminoglycoside antibiotics (gentamicin, sisomicin, tobramycin, ribostamycin, and amikacin) on the candidacidal activity of human neutrophils in vitro; all of them are inhibitory and can be grouped into three significantly different levels of toxicity . Gentamicin in the most toxic and sisomicin is the least toxic.

Nucleic Acids Symp Ser, 1980, (8), s73 - 4
Structure of amipurimycin, a new nucleoside antibiotic produced by Streptomyces novoguineensis; Goto T et al.; Structure elucidation of a new 2-aminopurine nucleoside antibiotic amipurimycin has been carried out . It contains 2-aminopurine, cis-2-aminocyclopentane-1-carboxylic acid and a sugar moiety . A structure will be proposed for the antibiotic.

Boll Ist Sieroter Milan, 1980, 59(6), 612 - 8
{Influence of antibiotics on leukocyte migration}; De Simone C et al.; Polymorphonuclear granulocytes play an important role in the immediate unspecific host response, and a depression of their functions can be found in many patients with severe or recurrent infections . Therefore administration of drugs causing such impairment in PMN function may be regarded as an additional risk for negative side effects to the patient . In our report the influence of 13 antibiotics--amphotericin B, ampicillin, tauglicolcillin, amoxicillin, cloxacillin, dicloxacillin, cephaloridine, cefalexin, cefuroxime, chloramphenicol, gentamicin, rifamycin, fosfomycin--on the granulocyte spontaneous and induced migration is investigated under in vitro experimental conditions . Human PMN preincubated with the antibiotics appropriately brought to the desired concentrations (therapeutic dose, 1/10 and 10X) in Hepes-Medium 199-water solution pH 7.2, were washed three times and tested for spontaneous and induced migration under agarose . Our experiments demonstrate that amphotericin B, cefalexin, cephaloridine, cefuroxime, chloramphenicol, dicloxacillin, gentamicin and rifamycin can inhibit in vitro human PMN chemotaxis and/or random migration . Inhibition of intracellular respiratory enzyme synthesis, presence of inactive metabolites of the drug, alterations of cyclic AMP and GMP or of the membrane bound divalent cations can be responsible of the phenomenon.

Toxicology, 1980, 17(2), 195 - 9
Comparative toxicity of aminoglycoside antibiotics towards the lysosomes in a cell culture model; Tulkens P et al.; Cultured rat fibroblasts were used to compare the cellular toxicity of 4 aminoglycosides: accumulation of the antibiotic in the lysosomes, its adverse effect on phospholipases and consequently the intralysosomal accumulation of phospholipids . Gentamicin and Tobramycin are more noxious than Netilmicin and Amikacin . These data, when corrected for the lesser capture of Tobramycin by the kidney proximal tubules, closely match the toxicological evaluation of these aminoglycosides on the basis of animal and clinical studies.

J Hyg Epidemiol Microbiol Immunol, 1980, 24(1), 84 - 91
Sensitivity to macrolide antibiotics and lincomycin in Francisella tularensis holarctica; Kudelina RI et al.; Among the 345 F . tularensis holarctica strains isolated in Europe, Asia and North America, two variants were found: one sensitive and the other resistant to erythromycin, oleandomycin and lincomycin . These characteristics were not associated with virulence, antigenicity, biochemical activity or source of isolation and displayed high stability in passages in laboratory animals or multiple passages in culture media . The two variants are proposed to be designated as biotype (biovar) I, erythromycin sensitive (erys), and biotype (biovar)II, erythromycin resistant (eryR) . A predominance of biotype I was observed for western Europe, eastern Siberia and the Far East, as well as North America, whereas biotype II prevailed in central Europe, the European part of USSR, especially the south, and western Siberia . The distribution of biotype II largely coincided with the habitat area of Arvicola terrestris, from which it was isolated with the highest frequency . Within the areas of biotype II prevalence, erythromycin and other macrolide antibiotics, as well as lincomycin should not be used for tularemia therapy.

Scand J Infect Dis Suppl, 1980, Suppl 24, 195 - 203
Antibiotic-host defence interactions in vitro and in vivo; Forsgren A et al.; A markedly depressed chemotaxis was detected with an agarose gel technique when human leucocytes were incubated with fusidic acid and rifampicin in clinically obtainable concentrations . At high concentrations of newer well absorbed tetracyclines there was a definite depression and a less pronounced inhibition was detected for classical tetracycline . The incorporation of 14C-leucine into a trichloroacetic-acid insoluble form by human neutrophils was markedly depressed by the same antibiotics and it is suggested that some antibiotics acting by inhibition of protein synthesis also affect chemotaxis of human neutrophils . At therapeutic concentrations fusidic acid and rifampicin had a pronounced inhibiting effect on the incorporation of 3H-thymidine by human T-lymphocytes stimulated by PHA and B-lymphocytes by S . aurens, Cowan I . At concentrations above the therapeutic level inhibition was detected for doxycycline, erythromycin, clindamycin and nitrofurantoin . No apparent inhibition of neither chemotaxis by human neutrophils nor thymidine incorporation by lymphocytes could be detected for penicillins, cephalosporins, nalidixic acid, sulfamethoxazole and trimethoprim . Due to high albumin binding for some of the tested antibiotics and other factors involved, experiments were performed to test whether depression also takes place in vivo . The cellular immunity in mice was registered by monitoring the survival of transplanted heart grafts and the humoral immunity by quantitating plaque-forming cells and by titration of antibodies after immunization with sheep erythrocytes . Fusidic acid (500 mg/kg/day) and rifampicin (20 mg/kg/day, human therapeutic dose) had a highly significant effect (P less than 0.001) on the rejection of heart grafts and plaque-forming cells while the effect o serum antibodies was of low significance (P less than 0.02--P less than 0.01) . The effect of doxycycline (2.5 mg/kg/day) and fusidic acid (25 mg/kg/day) at human therapeutic dose on immunity in mice was slight but significant (P less than 0.02) . The relevance of experiments in mice to the situation in man is discussed . The migration of neutrophils into a skin chamber was shown to be dramatically reduced in eight healthy volunteers during a standard regimen of doxycycline.

Microbios, 1980, 28(112), 107 - 21
Flow microcalorimetric study of the effects of pH, metal ions and sterols on the interaction of polyene antibiotics with Saccharomyces cerevisiae NCYC239; Beezer AE et al.; The effects of pH, metal ions (calcium and magnesium) and sterols (cholesterol and ergosterol), on the interaction of polyene antibiotics with respiring Saccharomyces cerevisiae (NCYC 239) cells have been studied by flow microcalorimetry . The bioactivity of nystatin decreases as the pH of the medium increases toward neutral . Calcium and magnesium ions attenuate the biological effects of nystatin, amphotericin B and candicidin . The activities of filipin and pimaracin (natamycin) are unaffected by the presence of these ions . Ergosterol and cholesterol show similar effects . Some possible explanations for these observations are suggested.

Folia Biol (Praha), 1980, 26(5), 312 - 26
Immunosuppressive properties of the antibiotics cytostipin and vermiculine; Horakova L et al.; The properties of two antibiotics, cytostipin isolated from Penicillium stipitatum and vermiculine isolated from Penicillium vermiculatum, were examined in two systems for a rapid screening of current immunosuppressive agents {nucleolar test determining the degree of RNA synthesis in nucleoli of individual lymphocyte populations, and the reactivity of mouse lymphocytes to "T" (PHA) and "B" (LPS) mitogens} . Both antibiotics, distinctly suppressed the increase in number of "active" lymphocytes with compact nucleoli in the popliteal lymph node activated by SRBC . Incorporation of 3H-uridine into PHA-stimulated "T" lymphocytes was suppressed by both antibiotics, incorporation into LPS-stimulated "B" lymphocytes was inhibited by cytostipin but stimulated by vermiculine . The antibiotics were also tested in another two "classic" immune systems, the Jerne test and the GVH reaction . Both antibiotics in doses markedly inhibitory for GVH reaction did not suppress but significantly increased the number of the haemolytic plaques in spleens of SRBC-immunized mice.

J Med, 1980, 11(1), 39 - 48
Serial studies of leukocyte chemiluminescence: lack of effect of macrolide antibiotic therapy; Martin RR et al.; Antibiotics which affect protein synthesis have been reported to alter in vitro function of polymorphonuclear neutrophil leukocytes (PMNs) . We studied chemiluminescence of PMNs from 30 healthy adults during phagocytosis of opsonized zymosan . Similar chemiluminescence values were obtained before, during, and after oral therapy with erythromycin, rosaramicin, or placebo . While macrolide antibiotic therapy did not alter this PMN function, we conclude that chemiluminescence is a reproducible technique which is well suited for serial evaluation of PMN activity.

Arch Toxicol Suppl, 1980, 4, 399 - 401
Comparative studies on cardiotoxicity of some anthracycline antitumor antibiotics; Kirchner E et al.; Isolated atria of guinea-pigs showed negative inotropic and negative chronotropic responses after violamycin B I (V), carminomycin (C) and daunomycin (D), respectively . The mean effective concentrations in reducing amplitude (IC50) were 5.9 x 10(-4) mol x 1(-1) for V and 1.3 x 10(-4) mol x 1(-1) for C and D . In rabbits, intravenous injections of different doses of the antibiotics twice weekly for one month produced histopathological alterations in the myocardial tissue, which were smaller after D than after C or V.

Ann N Y Acad Sci, 1980, 346, 302 - 23
Photolabile antibiotics as probes of ribosomal structure and function; Cooperman BS; In summary, our studies have resulted in the development of new reagents and synthetic procedures for the introduction of both radioactivity and photolability into antibiotics; have provided examples of how PAGE analysis can be used to conveniently test various aspects of photoaffinity labeling of complex receptors, such as the ribosome; have revealed examples of unexpected photoreactivity, as in the case of puromycin; and have provided strong evidence regarding the three-dimensional location of the peptidyl transferase center and the site of that interaction of the 3' and of aminoacyl-tRNA with the 30S subunit . Work that is now in progress should provide similar detailed information regarding other functional sites in the ribosome.

Microbiol Immunol, 1980, 24(9), 777 - 87
Studies on the cross-resistance of Mycobacterium tuberculosis, strain H37Rv, to aminoglycoside- and peptide-antibiotics; Tsukamura M et al.; Various phenotypes of the resistance to aminoglycoside- and peptide-antibodies of Mycobacterium tuberculosis strain H37Rv were produced by single- and/or two-step selection of the parent strain . Mutants obtained by single-step selection with antibiotics were classified into ten phenotypes; one of single resistance, two of triple resistance, three of quadruple resistance, and four of sextuple resistance . There were two kinds of sextuple resistance (high resistance to enviomycin, viomycin, capreomycin, kanamycin, lividomycin) . One was isolated from the parent strain by single-step selection and could be eliminated by mutation to isoniazid resistance, the other was obtained by two-step selections and was not eliminated by mutation to isoniazid resistance . Interaction between mutation to streptomycin resistance and mutation to quadruple resistance (4R phenotype) was observed . Streptomycin resistance interfered with the formation of the 4R phenotype and produced a different phenotype, KR instead of the 4R phenotype . The existence of mutation of the 4R phenotype did not usually interfere with mutation to streptomycin resistance, but a small portion of the mutants with the 4R phenotype were altered in their phenotype from 4R to KR after addition of the mutation to streptomycin resistance . This effect of the mutation to streptomycin resistance was not observed in mutants which already had a mutation to klR phenotype (mutation to low concentrations of kanamycin only).

Br J Pharmacol, 1980, 71(1), 315 - 20
Synergistic effects of hypoglycaemic sulphonylureas and antibiotic ionophores upon calcium translocation; Couturier E et al.; 1 Hypoglycaemic sulphonylureas, such as tolbutamide and gliclazide, provoke the translocation of calcium from an aqueous medium into or across a hydrophobic region . The combined effect of sulphonylureas and antibiotic ionophores upon such a process was investigated . 2 The magnitude of the sulphonylurea-induced translocation of calcium was more marked in the presence than in the absence of A23187 . Gliclazide and tolbutamide also enhanced, although less markedly, X537A-mediated calcium translocation . The effect of the sulphonylureas was even less marked in the presence of both ionophores, which acted synergistically in causing calcium translocation . 3 A non-hypoglycaemic sulphonylurea and diazoxide failed to affect ionophore-mediated calcium translocation . Gliclazide failed to enhance X537A-mediated sodium translocation . 4 It is proposed that the primary site of action of hypoglycaemic sulphonylureas upon calcium-dependent physiological processes may correspond to a drug-induced facilitation of calcium transport across the plasma membrane, as mediated by native ionophores.

Arch Orthop Trauma Surg, 1980, 96(2), 79 - 82
The prophylactic use of antibiotics in alloarthroplasty of the hip joint for coxarthrosis; Schulitz KP et al.; In alloarthroplasty of the hip joint due to coxarthrosis a randomized prospective controlled study was performed to test the efficiency of prophylactic antibiotics in reducing the postoperative infection rate . The minimum follow-up time was 730 days . There were three infections (two superficial and one deep) in the group who received antibiotics (105 patients), 10 infections (two superficial and eight deep) in the control group (89 patients) . The overall rates of infections and also the rate of the deep wound infections were significantly lower in patients who received prophylactic antibiotics.

Pharmacology, 1980, 20(5), 268 - 74
Acetylcholine-releasing effect of primycin, a highly active antibiotic; Adam-Vizi V et al.; The effect of primycin, an antibiotic known to inhibit potassium conductance, was studied on acetylcholine (ACh) release from the nerve terminals of the Auerbach plexus and cortical slice of the rat . Primycin enhanced the resting release of ACh; however, it failed to affect the amount of ACh released by a single shock . It has no effect on Na+K+-activated ATPase . Its effect on Ach release was prevented by tetrodotoxin and by Ca removal . It is concluded that its effect on potassium conductance might account for its ACh-releasing effect: it produces depolarization and spontaneous firing.

J Bacteriol, 1980 Jan, 141(1), 156 - 63
Mechanism of the antibiotic action pyocyanine; Hassan HM et al.; Exposure of Escherichia coli growing in a rich medium to pyocyanine resulted in increased intracellular levels of superoxide dismutase and of catalase . When these adaptive enzyme syntheses were prevented by nutritional paucity, the toxic action of pyocyanine was augmented . The antibiotic action of pyocyanine was dependent upon oxygen and was diminished by superoxide dismutase and by catalase, added to the suspending medium . Pyocyanine slightly augmented the respiration of E . coli suspended in a rich medium, but greatly increased the cyanide-resistant respiration . Pyocyanine was able to cause the oxidation of reduced nicotinamide adenine dinucleotide, with O2- production, in the absence of enzymatic catalysis . It is concluded that pyocyanine diverts electron flow and thus increases the production of O2- and H2O2 and that the antibiotic action of this pigment is largely a reflection of the toxicity of these products of oxygen reduction.

Acta Biochim Biophys Acad Sci Hung, 1980, 15(1), 57 - 63
Effect of antibiotics influencing membrane function on the potassium transport of E . coli cells; Szogyi M et al.; The effect of polymixin, nigericin, gramicidin on the 42K-efflux of E . coli cells was studied . The 42K-efflux of the bacteria decreases in time according to an exponential function . The slopes of the linearized functions characterizing the efflux increase with increasing concentration of antibiotics . The frequency of events of the 42K-release as a parameter of antibiotics membrane interaction was determined on the basis of a theoretical model developed for the evaluation of our experimental data . In this way a quantitative comparison of the effectiveness of antibiotics was possible . We found, that the most effective antibiotic was polymixin, followed by nigericin and gramicidin.

Antibiot Chemother, 1980, 28, 102 - 8
Interactions of antineoplastic antibiotics and DNA; Gause GF et al.; Basic concepts of interaction of antineoplastic antibiotics with DNA are discussed and information concerning the effects of actinomycins, olivomycin and related antibiotics, anthracyclines, sibiromycin, mitomycin C, bruneomycin, and bleomycin is summarized.

Acta Anaesthesiol Belg, 1980, 31(4), 293 - 306
The comparative neuromuscular blocking effects of some aminoglycoside antibiotics; Rutten JM et al.; The neuromuscular blocking effects of aminoglycoside antibiotics were tested in the isolated phrenic nervediaphragm preparation of the rat . The neuromuscular blocking potencies were netilmicin equals sisomicin much greater than neomycin much greater than gentamicin much greater than tobramycin . The EC 50's (concentration resulting in 50 percent depression of the original twitch tension) were respectively 13.3 x 10(-4); 13.4 x 10(-4); 13.6 x 10(-4); 15.1 x 10(-4); and 95.3 x 10(-4) Mol/l for netilmicin, sisomicin, neomycin, gentamicin and tobramycin . When a threshold dose of pancuronium was added to the bathing fluid the EC 50's were diminished respectively by a factor of 0.4 (sisomicin and neomycin) 0.5 (tobramycin) and 0.6 (netilmicin and gentamicin) . Addition of a threshold dose of Org-NC45, a new steroidal non-depolarizing muscle relaxant, diminished the EC 50's to the same extent . The neuromuscular blocking effects of pancuronium and Org-NC45 themselves were potentiated by pretreatment of the preparations with a threshold dose of the aminoglycoside . Comparison of the results demonstrated the following potentiating effects: netilmicin equals sisomicin much greater than neomycin much greater than gentamicin greater than tobramycin . Which is in the same sequence s the neuromuscular blocking potencies of these drugs.

Br J Anaesth, 1980, 52 Suppl 1, 33S - 36S
Preliminary review of the interactions of ORG NC 45 with anaesthetics and antibiotics in animals; Krieg N et al.; In vitro (rat hemidiaphragm) and in vivo (rat and cat tibialis anterior muscle preparation) studies of the interactions between Org NC 45 and some i.v . anaesthetics and antibiotics were carried out . With the exception of ketamine 1 mg kg-1 none of the drugs tested in vivo significantly changed the time course of an Org NC 45 bolus injection . All of the drugs caused an enhancement of the neuromuscular block using infusions in vivo and also in the in vitro preparations . Org NC 45 seems to be potentiated in a manner similar to pancuronium.

Eur J Biochem, 1979 Dec 17, 102(2), 477 - 81
On the structure of the teichoic acid from the cell wall of Streptomyces antibioticus 39 . Localization of the phosphodiester linkages and elucidation of the monomeric units structure by means of 13C-nuclear-magnetic-resonance spectroscopy; Shashkov AS et al.; The cell walls of Streptomyces antibioticus 39 contain a glycosylated poly(glycerol phosphate), in which the repeating monomeric unit is O-alpha-D-galactopyranosyl-(1--3)-O-2-acetamido-2-deoxy-beta-D-galactopyranosyl-(1--1)-glycerol monophosphate . The localization of the phosphodiester linkages between hydroxyl groups at positions 2 and 3 of the adjacent glycerol residues and the structure of the glycoside were established by 13C nuclear-magnetic-resonance spectroscopy . The spectral data are also in accordance with the results of the methylation analysis and enzyme degradation of the glycoside.

J Membr Biol, 1979 Dec 14, 51(2), 161 - 84
Coupled transepithelial sodium and potassium transport across isolated frog skin: effect of ouabain, amiloride and the polyene antibiotic filipin; Nielsen R; Addition of the polyene antibiotic filipin (50 microM) to the outside bathing solution (OBS) of the isolated frog skin resulted in a highly significant active outward transport of K+ because filipin per se increases the nonspecific Na+ and K+ permeability of the outward facing membrane . The K+ transport was calculated from the chemically determined changes in K+ concentrations in the solution bathing the two sides of the skin . The active transepithelial K+ transport required the presence of Na+ in the OBS, but not in the inside bathing solution (IBS), and it was inhibited by the Na+, K+-ATPase inhibitor ouabain . The addition of Ba++ to the IBS in the presence of filipin in the OBS resulted in an activation of the transepithelial K+ transport and in an inhibition of the active Na+ transport . This is in agreement with the notion that Ba++ decreases the passive K+ permeability of the inward facing membrane . In the presence of amiloride (which blocks the specific Na permeability of the outward facing membrane) and Ba++ there was a good correlation between the active Na+ and K+ transport . It is concluded that the active transepithelial K+ transport is carried out by a coupled electrogenic Na-K pump, and it is suggested that the pump ratio (Na/K) is 1.5.

Jpn J Antibiot, 1979 Dec, 32 Suppl, S145 - 62
Preparatively useful reactions involving nitrogenous sugars and some applications with carbohydrate-containing antibiotics; Horton D; This work describes the development of useful synthetic methodology with simple sugars, practical applications for conversion of abundant precursors into modified sugars (especially amino and deoxy sugars) of importance in various groups of natural products, and the conversion of such products into compounds of biological or pharmacological interest, especially carbohydrate antibiotics and their analogs . Examples of synthetic methodology illustrate various routes to deoxygenated (saturated, alkenic, and acetylenic), and oxidized (carbonylic, aldehydic, and carboxylic) functionality from hydroxyl and amino precursors . Unusual modes of sugar protection by such procedures as kinetic acetonation are discussed, together with the use of diazo and hydrazino groups for access to novel structures, including extended carbon-chain sugars and sugar--heterocycle conjugates . The broad utility of 5-membered benzylidene acetals in regiospecific routes to alpha, beta-deoxycarbonyl sugars is the basis of general methodology for practical, large-scale synthesis of aminopolydeoxy sugars, with daunosamine as the prototype, of widely varied substitution-mode and stereochemistry . Implications of the foregoing are discussed in relation to several classes of antibiotics, especially the anthracyclines and analogs thereof . A range of 7-O-(amino sugar-substituted)daunomycinones have been synthesized, together with 3'-hydroxy-daunorubicin and adriamycin, and their antitumor and toxicological properties evaluated; prospects for useful total synthesis will be mentioned.

Antimicrob Agents Chemother, 1979 Dec, 16(6), 701 - 9
Incidence of antibiotic-resistant Escherichia coli associated with frozen chicken carcasses and characterization of conjugative R plasmids derived from such strains; Caudry SD et al.; Escherichia coli were isolated at concentrations of about 10(2)/ml from the fluid obtained after thawing each of five frozen chicken carcasses . Between 13 and 89% of the E . coli were resistant to mercury(II) or to at least one of eight antibiotics tested . Multiple resistance was more common than single resistance, and resistances to tetracycline, streptomycin, sulfathiazole, or chloramphenicol were more frequently encountered than was resistance to ampicillin or mercury(II) . Resistance to kanamycin, gentamicin, or trimethoprim occurred rarely . Upwards of 30% of the E . coli apparently carried conjugative plasmids and could transfer at least one of their resistance determinants to E . coli K-12 . Twenty-five conjugative R plasmids obtained in this way were characterized within strain K-12 by a variety of phenotypic criteria . Twenty could be assigned to the incompatibility groups Inc X, Inc N, Inc FI, or Inc I alpha.

Eur J Biochem, 1979 Dec, 102(1), 73 - 81
Mechanism of action of aminoglycoside antibiotics . Binding studies of tobramycin and its 6'-N-acetyl derivative to the bacterial ribosome and its subunits; Le Goffic F et al.; 6'-N-{14C}Acetyl-tobramycin and {3H}tobramycin were synthesized and their binding to Escherichia coli ribosomes and ribosomal subunits studied using equilibrium dialysis . THE 70-S ribosome, as well as its 50-S and 30-S subunits, bound tightly to 6'-N-acetyl-tobramycin . The binding of {3H}tobramycin to ribosomes was quite different . The 70-S ribosome was observed to possess several classes of binding sites; of these, one was determined to be of higher affinity and lower capacity, the 6'-N-{14C}acetyl-tobramycin site . The isotopic dilution method was used to define the specificity of the interaction . The selective binding of 6'-N-{14C}acetyl-tobramycin was highly reversible by tobramycin, kanamycins A, B, C and neomycin, but not by streptomycin or erythromycin . Gentamicin C1a was a poor inhibitor . This suggested that either the kanosamin or garosamin rings might be determinant in the binding of these molecules, as well as the 6'-amino group.

Jpn J Antibiot, 1979 Dec, 32 Suppl, S1 - 14
Studies on aminoglycoside antibiotics: enzymic mechanism of resistance and genetics; Umezawa H; The kanamycin inactivating enzyme, 3'-phosphotransferase and 6'-acetyltransferase were first found in 1967 and on the basis of the enzymic mechanism of resistance a new research approach to the development of active useful derivatives was explored . The enzymic mechanism of resistance was conclusively confirmed by the synthesis of 3'-deoxykanamycin A and 3',4'-dideoxykanamycin B which did not undergo inactivation by 3'-phosphotransferase and inhibited the growth of resistant strains . Besides APH(3') and AAC(6') described above, the following enzymes were found to be involved in the mechanism of resistance to aminoglycosides: APH(3''), APH(5''), APH(6), APH(2''), AAC(3), AAC(2'), AAD(3''), AAD(2''), AAD(4'), AAD(6) . Not only the removal of the group which undergoes the enzyme reaction but also the modification of the group binding to the enzyme has also given active derivatives such as amikacin etc . The substrate specificity of the enzymes, enzymes in the immobilized state, and the application of proton and 13C nmr for structure determination of reaction products are reviewed . It was noticed that all enzymes involved in resistance contain adenosine- and aminoglycoside-binding sites . These enzymes were thus suggested to be mainly different primarily in the positional relationships between these binding sites . It suggests a close evolutionary relationships of these enzymes . The role of these enzymes in the biosynthesis of aminoglycoside antibiotics is discussed and a general mode of the biosynthesis of aminoglycosides is proposed: a gene or gene set involved in biosynthesis of 2-deoxystreptamine which has no cytotoxicity is widely distributed and the deoxystreptamine produced is transformed to the final products.

Jpn J Antibiot, 1979 Dec, 32 Suppl, S73 - 90
Studies directed toward the total synthesis of antibiotics: (+)-spectinomycin; Hanessian S et al.; The presence of a dioxaspiro or a fused bicyclic ring system resulting from a diastereoselective intramolecular acetalization of keto diol or keto alcohol units respectively, is a unique structural feature among a number of biologically important natural products . The particular bond arrangement around the ketal carbon atom is, in part, a reflection of the preference for anomeric stereoselection in nature, either at the site of acetalization or in its vicinity . This phenomenon manifests itself in the constitutional structures of several ionophores (polyether type), in the antibiotic spectinomycin as well as other natural products . Synthetic efforts in this area will be discussed, with particular emphasis on spectinomycin as a challenging target.

Cancer Res, 1979 Dec, 39(12), 5150 - 4
Control of permeation of bleomycin A2 by polyene antibiotics in cultured Chinese hamster cells; Akiyama SI et al.; Control of permeation of bleomycin A2, a well-known antitumor antibiotic, in combination with various polyene macrolide antibiotics was analyzed in cultured Chinese hamster cells in vitro . Three polyene antibiotics, filipin, pentamycin, and pimaricin, were found to enhance the action of bleomycin A2 remarkably, while amphotericin B or nystatin could not . Although DNA synthesis and colony-forming activity of polyene-sensitive Chinese hamster V79 cells were synergistically inhibited by the combination of filipin and bleomycin A2, in a polyene-resistant subline (AMBR-1) derived from V79, they were only slightly affected in the presence of both drugs . The cellular uptake of {14C}bleomycin A2 by V79 was enhanced 2- to 4-fold in the presence of increasing doses of filipin or pentamycin, but not in the presence of amphotericin B . The treatment of V79 cells with filipin for 20 to 30 min was enought to block DNA synthesis almost completely when combined with 20 microgram belomycin A2 per ml . The pretreatment of the hamster cells with 6 microgram filipin per ml for 60 min continued to enhance the inhibitory action by bleomycin A2 of DNA synthesis up to 5 hr after the removal of filipin from the cultured medium.

Biochemistry, 1979 Nov 13, 18(23), 5123 - 7
Contrasts in the actions of protein antibiotics on deoxyribonucleic acid structure and function; Kappen LS et al.; The protein antibiotics neocarzinostain (NCS), macromomycin (MCR), and auromomycin (AUR), which is closely related to MCR, have been compared for their in vitro and in vivo actions on deoxyribonucleic acid (DNA) . NCS, markedly stimulated by 2-mercaptoethanol, is much more active in inducing strand scissions in superhelical pMB9 and linear duplex lambda DNA than AUR, which is slightly inhibited by 2-mercaptoethanol . Purified MCR, even at very high levels, does not give any significant amount of cutting with either DNA substrate . 2-Propanol stimulates the activity of NCS but inhibits that of AUR . On the other hand, the antioxidant alpha-tocopherol strongly inhibits DNA breakage by both drugs . The intercalating drugs ethidium bromide, daunorubicin, proflavin, and actinomycin D at low concentrations inhibit DNA scission by AUR . The levels of intercalators required to inhibit NCS activity to comparable levels are about 10 times higher than those for AUR . Although MCR has virtually no in vitro DNA cutting activity, it is, like AUR and NCS, cytotoxic, as measured by the inhibition of DNA synthesis and induction of DNA strand breakage in HeLa cells.

Nucleic Acids Res, 1979 Nov 10, 7(5), 1375 - 92
Aspects of specific protein-DNA interaction; multi-mode binding of the oligopeptide antibiotic netropsin to (A.T)-rich DNA segments; Reinert KE et al.; By means of titration viscometry a number of distinct modes could be resolved for the interaction between the antibiotic netropsin and DNA species of 50, 58, and 69 mole + (A+T) below r = 0.04 netropsin molecules bound per DNA phosphate group . The number of corresponding binding sites increases with a high power of the (A+T) content . The apparent association constants are very high (greater than 10(6) M-1, some perhaps greater than 10(6) M-1) and also rather different for most of the binding sites . It is suggested that some of these interaction modes differ in the number of hydrogen bonds formed between donors of the ligand and acceptors of the binding sites . The interaction modes were characterized quantitatively by their (species-independent) changes of DNA contour length and by the percentage of local DNA stiffening.

JAMA, 1979 Nov 2, 242(18), 1981 - 4
Antibiotic usage in a pediatric medical center; Naqvi SH et al.; Antibiotic usage in a large pediatric teaching hospital was evaluated during a three-month period . A total of 1,067 patients received antibiotics and 295 patient records were reviewed . One hundred sixty-nine courses of antibiotics were administered to surgical patients, 77% for surgical prophylaxis . One hundred forty-seven antibiotic courses administered to medical patients were therapeutic in 61.2% and in 35.3% were given because of suspicion of infection . Ampicillin was the most commonly used antibiotic; cephalosporins were used for surgical prophylaxis . Aminoglycosides were used commonly for suspected infection in medical patients . Antibiotic management was inappropriate in 66% of surgical patients and in 21% of medical patients . Not obtaining appropriate studies prior to and during therapy were common infractions on all services . Surgical prophylaxis was freqently inappropriate by reason of no indication, wrong drug or dose, or inappropriate timing.

Mol Biol (Mosk), 1979 Nov-Dec, 13(6), 1322 - 6
{Binding of actinomycin D analogues containing some substituents at position 7 of the antibiotic chromophore to DNA}; Mikhailov MV et al.; Spectrophotometric methods are used to study the binding to DNA of Actinomycin D (AMD) and its analogues: 7-nitro-AMD; 7-amino-AMD; 7-(Z-Val-Glo-NH)-AMD; 7-(AcO- . +H2-Val-Glo-NH)-AMD; 7-(AcO- . +H2-Val-Glo-Val-Glo-NH)-AMD . The binding constants are calculated from the binding isotherm of AMD and those of the AMD analogues to calf thymus DNA obtained by spectrophotometric titration . Introduction of smaller substituents such as the nitro or amino groups into position 7 of chromophore influences insignificantly the antibiotic binding to DNA, whereas bulky substituents cause a decrease in the affinity of the AMD analogues for DNA, although the spectral characteristics are not affected.

Biokhimiia, 1979 Nov, 44(11), 2005 - 12
{Photo-dependent conversions of cytochrome f in bean chloroplasts and leaves treated with polyene antibiotics}; Mazhorova LE et al.; The photo-dependent absorption changes of cytochrome f in bean chloroplasts and native leaves treated with the polyene antibiotics surgumycin and filipin were studied . Upon incubation of the chloroplasts or leaves with the antibiotics the value of the photo-induced signal of cytochrome f decreased considerably; however, the kinetics of the cytochrome oxidation under the effect of the exciting light and dark reduction remained unchanged . An addition of plastocyanin to the suspension of the antibiotic-treated chloroplasts, which contained no artificial donors and acceptors, only slightly increased the absolute value of the photo-induced signal of cytochrome f . An addition of plastocyanin to the chloroplasts containing the dichlorophenolindophenol-ascorbate-methylviologen system, sharply changed the kinetics of the cytochrome f photoconversions . A simultaneous registration of the photo-induced signal of cytochrome f and the photochemical activity of photosystem I of the antibiotic-treated chloroplasts revealed differences in the degree of inhibition of the photosystem I activity and decrease of the absolute value of the cytochrome f signal . The data obtained are discussed in terms of possible alternative pathways of electron transfer in the part of the electron transporting chain under study.

J Antibiot (Tokyo), 1979 Nov, 32(11), 1155 - 60
Orally active esters of cephalosporin antibiotics . II . Synthesis and biological properties of the acetoxymethyl ester of cefamandole; Wright WE et al.; The synthesis of the acetoxymethyl (AOM) ester of cefamandole (CM) is described . The sparingly soluble ester is shown to be well absorbed orally by mice, but only when administered in solution in a partially non-aqueous vehicle, 50% propylene glycol . Neither the ester in aqueous suspension nor the sodium salt of CM in solution is well absorbed orally . The rate of oral absorption of the ester from solution is very rapid as shown by the early peak time and shape of the plasma level curve . Oral bioavailability from solution is at least 60% and is apparently limited only by hydrolysis or precipitation of a variable portion of the ester dose in the intestinal lumen prior to absorption.

J Antibiot (Tokyo), 1979 Nov, 32(11), 1112 - 7
Antibiotics from basidiomycetes . IX . Oudemansin, an antifungal antibiotic from Oudemansiella mucida (Schrader ex Fr.) Hoehnel (Agaricales); Anke T et al.; From mycelial cultures of Oudemansiella mucida a crystalline optically active antibiotic, oudemansin (2), has been isolated; its structure is closely related to strobilurin A (1) . The relative configuration of oudemansin have been determined by X-ray analysis . The antibiotic exhibits strong antifungal properties and inhibits respiration in fungi, cells of the ascitic form of EHRLICH carcinoma, and rat liver mitochondria.

Cancer Treat Rep, 1979 Nov-Dec, 63(11-12), 1971 - 8
Treatment of mouse tumors with 7-con-O-methylnogarol and other analogs of the anthracycline antibiotic, nogalamycin; Neil GL et al.; The chemotherapeutic activity of analogs of the anthracycline antibiotic, nogalamycin, was investigated in the P388 and L1210 leukemias and the B16 melanoma in mice . Among the compounds tested, 7-con-O-methylnogarol was found to have superior activity . Depending on the route and schedule of administration, increases in lifespan (ILS) in excess of 100% were observed in all three tumor systems . Additional testing of 7-con-O-methylnogarol demonstrated significant activity in the murine colon 26 and colon 38 tumors and the CD8F1 mammary tumor . 7-Con-O-methylnogarol was not significantly effective against murine Lewis lung carcinoma, although ILSs of 38% and 29% were achieved in two experiments . Activity was observed against ip inoculated P388 leukemia after ip, sc, oral, and iv drug administration . 7-Con-O-methylnogarol was also highly active (ILS greater than or equal to 120%) after ip drug administration to mice with iv inoculated P388 leukemia . Significant ILS values resulted from a variety of schedules of administration against ip inoculated P388 leukemia and B16 melanoma . Experiments in which the time of single-dose administration was varied prior to the time of ip P388 leukemia inoculation showed that residual drug or bioactive drug-related materials remained in mice for 8 hours after 50 mg/kg administered ip and for 48 hours after 200 mg/kg administered sc.

Jpn J Antibiot, 1979 Nov, 32(11), 1101 - 6
{Experimental study of the biliary excretion of antibiotic (cefotiam) in the presence of biliary tract obstruction (author's transl)}; Yoshikawa N et al.; Excretion of a new semisynthetic analogue of cephalosporin, cefotiam (CTM), and cefazolin (CEZ) in bile was investigated in dogs with experimental obstruction of biliary tract . In the control group, peak concentrations of antibiotics in bile after 50 mg/kg intravenous administration were as follows: In CTM administrated groups, 5,302 micrograms/ml at one hour after administration; and in CEZ administrated group, 1,249 micrograms/ml after one hour . The total biliary excretory rates summed to 6 hours after administration of antibiotics were 7.8% in the CTM group, and 2.1% in the CEZ group . On the other hand, in the biliary tract obstruction group, the peak concentration in bile in CTM group was 65.7 micrograms/ml after 1 hours, and in CEZ group, 62.4 micrograms/ml after 2 hours . The total biliary excretory rate in the CTM group was 0.202%, while in the CEZ group 0.12% . The peak concentration and the excretory rate of CTM in bile was four times higher than that of CEZ in the control group . No significant difference was revealed in the peak concentration and the excretory rate in bile between CTM and CEZ in the biliary tract obstruction group.

Antibiotiki, 1979 Nov, 24(11), 828 - 31
{Characteristics of a strain of C . albicans resistant to polyene antibiotics}; Mikhailova MA et al.; It was found that a resistant strain R2 of C . albicans obtained as a result of passages on media containing increasing concentrations of amphotericin B differed from the initial strain by its lower pathogenicity . Treatment of the infection caused by the resistant strain on modeling of candidiasis in mice was not successful . The decrease in the average life span of the mice infected with the resistant strain R2 and treated with amphotericin B was lower than that in the control animals and such indices of the disease as the levels of the kidney dissemination and the cell vegetation even increased under the effect of amphotericin B . The results of the study suggest that the resistant strain R2 of C . albicans depend on amphotericin B in the host . The data obtained emphasize the necessity of determinining the antibiotic sensitivity of C . albicans strains isolated from patients.

Antimicrob Agents Chemother, 1979 Nov, 16(5), 554 - 60
Antibiotics and suppression of lymphocyte function in vitro; Banck G et al.; The effects on the mitogenic response of human T lymphocytes were studied for 20 different antibiotics . No apparent inhibitory effect could be detected for penicillins, cephalosporins, aminoglycosides, chloramphenicol, sulfamethoxazole, trimethoprim, nalidixic acid, and 5-fluorocytosine . There were effects at high concentrations with erythromycin, clindamycin, and rifampin, and these antibiotics could also be shown to depress the mitogenic response of B lymphocytes . With fusidic acid, nitrofurantoin, and doxycycline there was an inhibiting effect at low concentrations on the mitogenic responses of B and T lymphocytes and on in vitro antibody production . Protein synthesis in unstimulated lymphocytes was also inhibited . Some antibiotics thus may impair the function of human lymphocytes in vitro.

J Med Chem, 1979 Nov, 22(11), 1296 - 301
Structure--activity relationships of pyrrole amidine antiviral antibiotics . 1 . Modifications of the alkylamidine side chain; Bialer M et al.; Representatives of three types of side-chain analogues of distamycin A (1) were synthesized . These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, effects on the synthesis of HSV DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase . Distamycin A was the most active compound in all three antiviral tests, as well as the most toxic . However, several compounds, in particular the aromatic analogues 15 and 16, showed no toxicity under the experimental conditions used but were still very active in the three antiviral tests.

Boll Soc Ital Biol Sper, 1979 Oct 30, 55(20), 2118 - 23
{Changes in serum levels of antibiotics in experimental CCL4 poisoning . I . Gentamycin}; Uomo G et al.; The AA . studied gentamycin serum levels (1mg/Kg b.w.) in rats . The 50% of the animals studied where treated with CCl4 (1 ml/Kg b;w.) 24h previously, the remaining 50% recieved a placebo . The maximum serum levels where similar in both groups; but the antibiotic was removed more slowly (120-240min) in the groups which recieved CCl4 . The slower rimotion rate causes more serious histological changes in the kidney.

Hosp Med Staff, 1979 Nov, 8(11), 24 - 8
Assessing antibiotic usage in a community hospital; Hazaleus RE; Data from a study of aminoglycoside prescribing patterns at a community hospital resulted in the hospital infection control committee issuing recommendations that were subsequently approved as standard medical practice . These data and recommendations are presented in full.

Ophthalmic Surg, 1979 Oct, 10(10), 74 - 7
Toxicity of antibiotic combinations for vitrectomy infusion fluid; Morgan BS et al.; We have found that gentamicin 8 microgram/ml in various combinations with methicillin 25 microgram/ml, oxacillin 10 microgram/ml, clindamycin 10 microgram/ml and penicillin 80 microgram/ml to be nontoxic to the retina when used in vitreous replacement fluid.

Arch Orthop Trauma Surg, 1979 Oct, 95(1-2), 31 - 5
Antibiotic irrigation-perfusion treatment for chronic osteomyelitis; Boda A; This paper reports 125 antibiotic irrigation-perfusion treatments of chronic osteomyelitic patients . The localisation of the osteomyelitic process, the duration of the disease, the duration of the treatment, the age distributions of the patients, and the results of the treatment are noted . The study revealed that only one third of the patients healed after the irrigation-perfusion treatment . This rate falls short of the results reported in the literature . The possible causes are discussed and emphasis is given to the technical problems . On the basis of this survey the author is of the opinion that this method is to be employed only in exceptional cases of bone infections . The indication and contraindications are precisely defined.

Isr J Med Sci, 1979 Oct, 15(10), 811 - 6
Antibiotic usage in Kupat Holim (Sick Fund) clinics . A pilot survey and evaluation; Cohen SR et al.; A survey of antibiotic prescribing patterns of six physicians in two Sick Fund clinics was carried out during a one-month period . Over 1,200 antibiotic prescriptions and their therapeutic indications were reviewed . Ampicillin was the most commonly prescribed drug . Most of the prescriptions were for treatment of infections of the upper respiratory tract . Over one half of all antibiotic prescriptions were for presumably viral upper respiratory infections (URI), and half of all patients diagnosed as having viral URI received an antibiotic prescription . A method for measuring the quality of antibiotic usage by physicians in infections of the upper respiratory tract was developed and tested . The method is readily applicable to Sick Fund clinics and, in a trial run, proved capable of demonstrating large differences among physicians in their antibiotic prescribing habits for viral URI, tonsillitis, and otitis media.

Aust Fam Physician, 1979 Oct, 8(10), 1040 - 8
The use of antibiotics in general practice; Fraser A; The prescribing of antibiotics in extra-hospital practice has now reached a level of one sixth of all Australian Pharmaceutical Benefit scheme prescriptions . In the last documented year prescriptions for the penicillins alone amounted to almost eight millions . Is this wholesale prescribing of potent, expensive, and, at times, dangerous chemotherapy really justified . This article will examine the indications for overall use of antibiotics, the pitfalls of their careless prescribing, and briefly review the main indications for each group of drugs in regular use in family practice . The discussion will therefore not include some drugs which are ordinarily limited to hospital practice, nor many of the regimes used in serious or life threatening disease such as meningitis or septicaemia.

Antibiotiki, 1979 Oct, 24(10), 727 - 32
{Action of mitomycin C on the variability of Actinomyces hygroscopicus in forming a proteolytic complex of hygrolytin enzymes and the antibiotic, hygromycin B}; Pronina MI et al.; The lethal and mutagenic effect of mitomycin C in doses of 10 and 15 micrograms/ml on the spores and 24-hour culture of Act . hygroscopicus, strain O878 producing hygrolytin, a proteolytic enzyme and hygromycin B, an antibiotic was studied . It was found that mitomycin C had a high lethal effect on the organism . The lethal effect of the antibiotic depended on the stage of the culture development, mitomycin C dose and exposure time . The 24-hour culture was most sensitive to the effect of mitomycin in a dose of 50 micrograms/ml . Exposure to mitomycin increased the actinomycete variation with respect to the colony morphology and induction of new morphological mutations . Exposure of strain O878 to mitomycin C significantly increased the culture variation with respect to the quantitative features of production of the hygrolytin proteolytic enzyme complex and hygromycin B . The character of the strain induced variation with respect to the features studied was different which indicated the absence of correlation between them . The use of mitomycin C proved to be promising in selection of Act . hygroscopicus with a purpose of increasing the culture proteolytic and antibiotic activity.

Minerva Stomatol, 1979 Oct-Dec, 28(4), 355 - 8
{Initial clinical results from the use of a new antibiotic, Zimox, in dentistry and maxillofacial surgery}; Re G et al.; Zimox (amoxicillin) has been experimented in a variety of stomatological inflammatory forms and in maxillo-facial surgery . Results with respect to the type of inflammation, pain response, impaired function oedema and trismus in various forms of dysodontiasis are reported.

Mikrobiyol Bul, 1979 Oct, 13(4), 364 - 70
{Prophylactic use of antibiotics in biliary tract and stomach surgery (author's transl)}; Sayek I et al.; 115 patients undergoing elective surgery on biliary tract (80 patients), and stomach (35 patients) for duodenal ulcer were divided into three groups: some received prophylactic antibiotics, cephalothin sodium or sulfamethoxazole trimethoprim and some received none . The antibiotics were started preoperatively and continued postoperatively for three days . The wound infection rate was reduced from 7.1% in the control group to 2.3% in patients treated with cephalothin sodium and 3.2% in sulfamethoxazole trimethoprim treated group . In patients who had biliary tract surgery, the wound infection rate was reduced to 3.3% and 0% with cephalothin sodium and sulfamethoxasole-trimetoprim respectively from 10% in the control group . Only one patient who had gastric surgery who received sulfamethoxasole-trimetoprim prophylactically, developed wound infection postoperatively . The difference between the groups was not statistically significant (p > 0.05) . However the wound infection rate was higher in patients who had positive bile culture (p < 0.05).

Biochemistry, 1979 Sep 18, 18(19), 4230 - 7
Pyrrolo{1,4}benzodiazepine antibiotics . Biosynthetic conversion of tyrosine to the C2- and C3-proline moieties of anthramycin, tomaymycin, and sibiromycin; Hurley LH et al.; This paper descirbes biosynthetic labeling experiments on the conversion of tyrosine to the C2- and C3-proline units of anthramycin, tomaymycin, and sibiromycin . The biosynthetic fate of all of the aromatic and side-chain hydrogens has been determined in each antibiotic by using dual tagged (3H/14C) and 2H-labeled tyrosine molecules . In addition, experiments uing {15N}tyrosine and the tritiated D and L isomers of tyrosine have shed some light on the biochemical reactions which take place at tha alpha position of tyrosine . On the basis of results of all these experiments, a biosynthetic scheme had been proposed to rationalize the apparent inconsistencies which occur between the results for the three antibiotics . This scheme proposes that a common main pathway involving proximal extradiol cleavage of Dopa and condensation to form the pyrrolo ring leads ultimately to a C-7 branch point compound . Parallel pathways from this central branch point compound lead by well-known biochemical transformations to the C2-and C3-proline units of anthramycin, tomaymycin, and sibiromycin . The reactions in these parallel pathways are suggested to be "cosmetic or after events".

Biochemistry, 1979 Sep 18, 18(19), 4225 - 9
Pyrrolo{1,4}benzodiazepine antibiotics . Biosynthesis of the antitumor antibiotic sibiromycin by Streptosporangium sibiricum; Hurley LH et al.; The biosynthesis of the antitumor antibiotic sibiromycin by Streptosporangium sibiricum requires the construction of four units: the amino sugar from glucose; the anthranilate ring from DL-tryptophan probably via kynurenine; the aromatic methyl group from methionine; the propylidene proline from L-tyrosine with the loss of two aromatic carbons and addition of a C-1 from methionine . Retention of tritium from DL-{5-3H}tryptophan in sibiromycin suggest an NIH shift during hydroxylation of an intermediate.

Experientia, 1979 Sep 15, 35(9), 1168 - 9
Colchicine-induced resistance to antibiotic and amino-acid analogue in plant cell cultures; Zryd JP; Colchicine-resistant plant cell strains have been isolated from cell suspensions of carrot and sycamore . In the same way as colchicine-resistant animal cell strains, they show an increased resistance towards streptomycin and N-methylalanine . Cultivation under non selective conditions leads to a slow progressive loss of the resistance.

Nature, 1979 Sep 6, 281(5726), 80 - 2
Energy dependence and reversibility of membrane alterations induced by polyene macrolide antibiotics in Chlorella vulgaris; Malewicz B et al.; The requirement of metabolic energy for the interaction of polyene macrolide antibiotics with eukaryotic organisms remains a controversial subject (for review see ref . 1) It has been claimed that the lethal binding of these antibiotics to the sterol target component of the hydrophobic core of the membrane, in accordance with the model of de Kruijff and Demel, is an energy-dependent process . When energy production is reduced by removal of all metabolisable substrates or by adding metabolic inhibitors, polyene binding and antifungal effects are also reduced . Metabolic energy may be required to maintain binding site accessibility or to move antibiotic molecules to the active site . The interaction is also restricted at low temperatures, possibly because of the reduced thermal mobilities of the groups concerned with antibiotic uptake . However, it should be emphasised that the interaction of polyene macrolides with artificial lipid membranes is a purely physicochemical process, although the type of permeability pathways induced are similar to those observed in natural membranes . Using Chlorella vulgaris as a model organism, we demonstrate here that the interaction of polyene macrolides with sensitive cells and the induction of lethal membrane permeability changes are energy-dependent processes or purely physicochemical phenomena, depending on the structure of the antibiotic used.

Zentralbl Bakteriol {Orig A}, 1979 Sep, 244(4), 515 - 24
Sensitivity patterns of bacteria and antibiotic usage at the National Hospital of Norway in 1976 and 1978; Rollag H et al.; During the first three months of 1976 and 1978 the sensitivity patterns of bacteria and the antibiotic usage at the National Hospital of Norway was recorded . The computerized results showed that bacteria isolated at the department of pediatrics was more resistant to penicillins . Isolates from two other departments did not differ very much in their sensitivity patterns . Comparing the sensitivity patterns, a tendency of increased sensitivity to antibiotics from 1976 to 1978 was seen . Exception was the increasing resistance to gentamicin . Furthermore, tobramycin was found less effective than gentamicin on our isolates . The antibiotics most widely used at the hospital are the penicillins which account for more than 50 per cent of the usage . From 1976 to 1978 the usage of antibiotics increased about 30 per cent . A more extensive use of penicillin V and G, and sulfamethoxazole/trimethoprim was responsible for most of the increase . No clear cut relationship between the antibiotic usage and the changes in sensitivity patterns of the bacteria from 1976 to 1978 was seen . Our work confirms, the usefulness of using "daily defined doses", as recommended by WHO, for estimating the antibiotic usage in a hospital.

Ann Dermatol Venereol, 1979 Sep, 106(8-9), 683 - 9
{Cross sensitivity between aminoside antibiotics (author's transl)}; Samsoen M et al.; The great number of topical preparation containing neomycin and their frequent use for a long period induce a lot of contact dermatitis . It is interesting to detect the importance of cross sensitivity between aminosides among the patients whose dermatitis was caused by neomycin . 15 neomycin eczematous patients were investigated . The research about cross-sensitivity concerned 6 antibiotics: streptomycin, framycetin, ribostamycin, gentamycin, kanamycin, tobramycin . Patch-tests (20 p . 100 in petrolatum) were used in order to show this cross-sensitivity . The results of these tests are nearly the same as in the other studies, as for 5 of the antibiotics; but it is the first time, to our knowledge, that a cross-sensitivity between ribostamycin and neomycin is observed . The cross-sensitivity between these two aminosides can be explained by their chemical structure . There are four rings in neomycin: the main components are neamin and neobiosamin . Only three rings are found in ribostamycin: ribostamycin is constitued of neomycin lacking neosamin of neobiosamin . Thus the structure of the 3 rings of ribostamycin is identical with the structure of 3 out of 4 rings of neomycin . The study about cross-sensitivity between aminosides suggests two conclusions: 1 . The use of local antibiotics must be prescribed only when is it really necessary . 2 . It seems wise to avoid all systemic aminosid antibiotics for patients who are sensitized by neomycin ointment.

J Antibiot (Tokyo), 1979 Sep, 32(9), 878 - 83
Deltamycins, new macrolide antibiotics . III . Chemical structures; Shimauchi Y et al.; The structures of deltamycins A1,A2,A3 and A4 belonging to the basic macrolide family of antibiotics were determined mainly from their spectral properties . Deltamycin A4 was identified as carbomycin A having an isovaleryl group on the mycarose moiety of the molecule . Deltamycin A1,A2 and A3 possess similarities to the structure of deltamycin A4, but they have acetyl, propionyl and n-butyryl group, respectively, in the place of isovaleryl group of deltamycin A4 . These structures were confirmed by chemical synthesis from deltamycin X (4''-O-deacyldeltamycin) and the corresponding acyl chlorides.

Antimicrob Agents Chemother, 1979 Sep, 16(3), 362 - 5
Cochlear toxicity of butikacin (UK-18,892), a new semisynthetic aminoglycoside antibiotic, in guinea pigs; Carter AJ; The cochleotoxic potential of butikacin (UK-18,892), a new semisynthetic aminoglycoside, has been evaluated in neonatal guinea pigs in comparison with amikacin, gentamicin, and kanamycin A . All compounds produced a dose-related increase of the mean threshold sound intensity required to elicit Preyer's reflex . Butikacin produced a similar level of cochlear toxicity to that of kanamycin A, but tended to be less cochleotoxic than amikacin . Gentamicin was the least cochleotoxic.

Neurosurgery, 1979 Sep, 5(3), 339 - 43
Prevention of neurosurgical infection by intraoperative antibiotics; Malis LI; For the past 5 years at Mount Sinai Hospital, an intraoperative prophylactic antibiotic regime consisting of intramuscular gentamicin or tobramycin, intravenous vancomycin, and streptomycin irrigating solution, with no preoperative or post operative antibiotics, has provided complete protection against operative infections in neurological surgery . There have been 1732 major clean operative cases with no instance of operative infection and no complication due to the antibiotics.

Eur J Biochem, 1979 Sep, 99(2), 369 - 78
Netropsin . dG-dG-dA-dA-dT-dT-dC-dC complex . Antibiotic binding at adenine . thymine base pairs in the minor groove of the self-complementary octanucleotide duplex; Patel DJ; The structure of the netropsin . dG-dG-dA-dA-dT-dT-dC-dC complex (one antibiotic molecule/self-complementary octanucleodide duplex) and its dynamics as a function of temperature have been monitored by the nuclear magnetic resonances of the Watson-Crick protons, the nonexchangeable base and sugar protons and the backbone phosphates . The antibiotic forms a complex with the nucleic acid duplex at the dA . dT-containing tetranucleotide segment dA-dA-dT-dT, with slow migration amongst potential binding sites at low temperature . The downfield shifts in the exchangeable protons of netropsin on complex formation demonstrate the contributions of hydrogen-bonding interactions between the antibiotic and the nucleic acid to the stability of the complex . Complex formation results in changes in the glycosidic torsion angles of both thymidine residues and one deoxyadenosine residue as monitored by chemical shift changes in the thymine C-6 and adenine C-8 protons . The close proximity of the pyrrole rings of the antibiotic and the base-pair edges in the minor groove is manifested in the downfield shifts (0.3--0.5 ppm) of the pyrrole C-3 protons of netropsin and one adenine C-2 proton and one thymine N-3 base-pair proton on complex formation . The internucleotide phosphates of the octanucleotide undergo 31P chemical shift changes on addition of netropsin and these may reflect, in part, contributions from electrostatic interactions between the charged ends of the antibiotic and the backbone phosphates of the nucleic acid.

Antibiotiki, 1979 Sep, 24(9), 643 - 7
{Formation of antibiotic 2562 by a culture of the actinomycete, Streptomyces griseovariabilis}; Gauze GF et al.; An actinomycetous culture 2562 inhibiting the growth of gramnegative bacteria was isolated from a soil sample . The culture was classified as Streptomyces griseovariabilis . It was found that culture 2562 produced an antibiotic belonging to the group of novobiocin . It consists of 2 components . One of them is identical to chlorobiocin and the other is a minor component of this group . Some parameters of the antibiotic complex production by strain 2562 under submerged conditions were studied . Nutrient media providing the predominant biosynthesis of the first (main) or the second component of the antibiotic were developed.

J Bacteriol, 1979 Sep, 139(3), 984 - 92
High-frequency fusion of Streptomyces parvulus or Streptomyces antibioticus protoplasts induced by polyethylene glycol; Ochi K et al.; Conditions were established for the regeneration of protoplasts of Streptomyces parvulus and Streptomyces antibioticus to the mycelial form . Regeneration was accomplished with a hypertonic medium that contained sucrose, CaCl2, MgCl2, and low levels of phosphate . High-frequency fusion of protoplasts derived from auxotrophic strains of S . parvulus or S . antibioticus was induced by polyethylene glycol 4,000 (42%, wt/vol) . The frequency of genetic transfer by the fusogenic procedure varied with the auxotrophic strains examined . Fusion with auxotrophic strains of S . parvulus resulted in the formation of true prototrophic recombinants . Similar studies with S . antibioticus revealed that both stable prototrophic recombinants and heterokaryons were formed.

Rev Infect Dis, 1979 Sep-Oct, 1(5), 845 - 51
Effects of subminimal inhibitory concentrations of antibiotics on adhesiveness of Escherichia coli in vitro; Vosbeck K et al.; The adhesion of radiolabeled Escherichia coli (strain SS142) to monolayers of Intestine 407, a human epithelioid tissue culture cell line, was investigated . In this assay the adhesion of bacteria grown in the presence of subminimal inhibitory concentrations of tetracycline, clindamycin,, or trimethoprim-sulfametrole was reduced in a manner that was dose dependent . In contrast, at such concentrations nalidixic acid enhanced the adhesion of this bacterial strain, and other antibiotics-e.g., penicillin G, ampicillin, mecillinam, cephacetrile, cephalexin, cefotaxime, chloramphenicol, and streptomycin-did not affect its adhesiveness.

Postgrad Med J, 1979 Sep, 55(647), 653 - 6
The polyene macrolide antibiotics; Kerridge D; The mode of action of the polyene antibiotics is reviewed together with the effect of genetic and environmental factors on sensitive organisms . The future prospects of polyenes in the treatment of systemic mycoses are considered.

Eur J Biochem, 1979 Sep, 99(3), 517 - 24
Uptake and conversion of the antibiotic albomycin by Escherichia coli K-12; Hartmann A et al.; The antibiotic albomycin is transported into cells of Escherichia coli K-12 by the same uptake system as the iron-supplying ferrichrome complex . The iron-complexing hydroxamate moieties of albomycin and ferrichrome are structurally similar . During the phase of rapid iron uptake the chelators were not found in the cells . In order to understand the antibiotic activity of albomycin, it was labeled in the hydroxamate with tritium and in the presumed antibiotically active area with radioactive sulfur . While the tritium label was not retained by the cells, part of the sulfur label was taken up and concentrated 500-fold within the cell . The sulfur was not incorporated into proteins or nucleic acids since it was recovered as a low molecular weight component . Gel filtration on Bio-Gel P-2 revealed one tritium-labeled and two sulfur-labeled cleavage products in the incubation medium . We conclude that albomycin is actively transported via its ferrichrome-like portion into the cells and that the growth-inhibitory moiety is released by hydrolysis intracellularly and remains there.

J Bacteriol, 1979 Sep, 139(3), 770 - 4
Escherichia coli murein-DD-endopeptidase insensitive to beta-lactam antibiotics; Keck W et al.; A novel endopeptidase degrading the peptide cross-links in sacculi has been isolated from Escherichia coli and purified to homogeneity . The enzyme has a molecular weight of 30,000 and, in contrast to already known enzymes of similar specificity, remains fully active in the presence of beta-lactam antibiotics . In addition, it is exceptional in being inhibited by single-stranded deoxyribonucleic acid and by some polynucleotides . The possible role of the enzyme in cell division is discussed.

Ann Sclavo, 1979 Sep-Oct, 21(5), 635 - 45
{Comparative study of bacterial sensitivity to antibiotics with the "abac" automatic system and the agar diffusion disk method}; Cipriani S et al.; 654 bacterial strains isolated from different biological materials have been tested either with "abac" automatic system or diffusion system on disks according to the Bauer-Kirby standardized method . The higher discrepancy has been observed to Co-trimoxazol antibiotic . Some other discrepancies, non significative, are shown in figures . The use of "abac" provides increased efficiency and convenience improving the quality of routine antimicrobic susceptibility results.

J Antibiot (Tokyo), 1979 Sep, 32(9), 857 - 61
Herbicidins C and E, two new necleoside antibiotics; Takiguchi Y et al.; Streptomyces saganonensis No . 4075 used for production of herbicidins A and B has also produced other two antibiotics, herbicidins C and E in submerged culture . Isolation of the antibiotics was performed by adsorption on resinous adsorbent followed by elution with aqueous MeOH and completed by silica-gel chromatography . Physico-chemical characteriation revealed that herbicidins C and E are new nucleoside antibiotics having an adenine moiety in their structures . Herbicidins C and E indicated inhibitory activity against germination of chinese cabbage at 12.5 micrograms/ml and 25 micrograms/ml, respectively, and Anacystis nidulans, a blue green algae, at 100 approximately 200 micrograms/ml.

Antibiotiki, 1979 Sep, 24(9), 651 - 5
{Action of grisin on the variability of an Acinomyces griseus culture and the use of the same antibiotic as a selection agent in the selection of active variants}; Kuklin VV et al.; The effect of grisin on survival and variation of Actinomyces griseus producin grisin was studied . The efficiency of various concentrations of grisin on induction of variation according to the feature of the antibiotic production was compared . A possibility of increasing the productivity of strain . VNIIGenetics-115 by the use of the mutations of resistance to grisin is shown.

Tsitologiia, 1979 Sep, 21(9), 1036 - 40
{Use of the antibiotic, olivomycin, for the cytochemical study of chromatin}; Borodina VM et al.; The possibility to use the antibiotic olivomycin for fluorescence cytochemistry of chromatin properties has been shown . It is found that the binding of olivomycin to nuclei reveals the functional state of chromatin and changes in the course of its activation . The essential condition for the application of the method described is the use of ethanol-aceton fixative . When other fixatives are used, in particular 70% ethanol, olivomycin binding reflects differences in nuclear DNA amount, rather than those in chromatin properties . The advantages of the method described, in comparison with the commonly used technique, are associated with the high affinity of olivomycin to DNA, absence of olivomycin binding with RNA, simplicity of the staining procedures , and with rather a high stability of complexes formed between olivomycin and DNA.

Mikrobiologiia, 1979 Sep-Oct, 48(5), 814 - 9
{Chemical composition of the cell wall of Streptomyces chrysomallus which produces the antibiotic aurantin}; Streshinskaia GM et al.; The cell wall chemical composition of Streptomyces chrysomallus producing the antibiotic aurantin was studied . The cell wall represents 11--13% of the dry cell weight and contains three major polymers, namely, peptidoglycan, ribitol teichoic acid and a polysaccharide . Each muramic acid of peptidoglycan has a peptide subunit which consists of two alanine residues, glutamic acid and diaminopimelic acid residues . Peptide chains are connected with bridges consisting of one glycine residue . The poly(ribitol phosphate) chain contains glucosyl substituents and O-acetyl groups . The main monosaccharides of the polysaccharide are glucose and galactose; mannose, fucose and galactosamine are found in minor amounts . The composition of the cell wall changes during cell development and aging: the content of teichoic acid decreases while that of the polysaccharide increases . Possible factors causing these changes are discussed.

Clin Chem, 1979 Sep, 25(9), 1639 - 43
Aminoglycoside antibiotic measurement by bioluminescence, with use of plasmid-coded enzymes; Daigneault R et al.; We describe a bioluminescent assay for gentamicin in serum that is applicable to the measurement of other aminoglycosides as well . The assay is based on the measurement of residual ATP with the luciferase reaction after incubation of the antibiotic with a plasmid-coded enzyme . Two aminoglycoside-inactivating enzymes were used: an adenylytransferase and an acetyltransferase coupled to S-acetyl coenzymeA synthetase . We investigated the latter system further because of the good stability of the acetyltransferase, its recovery in high yield from bacteria, and its more favorable ATP/gentamicin mass ratio . Serum ATPases were inactivated at 60 degrees C for 20 min . The operating range of the assay was 0-15 mg of gentamicin per liter . The precision (CV) was 10.1% at a concentration of 2 mg/L and 1.1% at 10 mg/L . The method correlated well with a radio-enzymatic assay for mock unknown sera (r = 0.981) . The results were available within 2 h.

Fortschr Med, 1979 Aug 23, 97(32), 1350 - 5
{Antibiotics therapy in chronic bronchitis}; Nolte D; In chronic bronchitis antibiotic therapy is no causative therapy, because infection rarely is the beginning but the complication of an already existing airway disease . While sputum cultures are very limited in their value, blind chemotherapy of bacterial infections by substances like tetracycline, ampicilline, azidocilline or cotrimoxazole is allowed . In cases of additional obstruction a combination with corticosteroids sometimes may be useful.

Experientia, 1979 Aug 15, 35(8), 1034 - 5
Presumptive identification of aminoglycoside antibiotics by the pH susceptibility disc agar-diffusion method; Uri JV et al.; Using the pH (buffered) sensitivity discs for the agar-diffusion bioassay of aminoglycoside antibiotics, characteristic response curves were obtained . Since the nature of the activities observed are structure-related, this method can serve as a useful aid for primary identification of members of this class of antibiotics.

S Afr Med J, 1979 Aug 11, 56(6), 211 - 3
Some aspects of aminoglycoside antibiotic measurement; Botha P et al.; More than 2 years of experience in assaying aminoglycoside antibiotic levels have proved that the appropriate acetyltransferase employed in conjunction with 14C-acetyl co-enzyme A provides rapid, reproducible results (CV = 4+) . These results are available before the next administration is due, enabling the clinician to adjust the dose . This is especially indicated if there is impairment of renal function.

J Antibiot (Tokyo), 1979 Aug, 32(8), 791 - 800
Antitumor anthracycline antibiotics, aclacinomycin A and analogues . I . Taxonomy, production, isolation and physicochemical properties; Oki T et al.; Aclacinomycin A and B, two major components of a new antitumor antibiotic complex, and their 19 analogues were produced by a culture of strain No . MA144-M1, which was identified as Streptomyces galilaeus . They were isolated by chelation with copper ion and silicic acid chromatography, and characterized by physicochemical methods in the anthracycline group of antibiotics.

Antibiotiki, 1979 Aug, 24(8), 615 - 9
{Effect of the polyene antibiotic, roseofungin, on the liberation of the intracellular components from Candida guilliermondii cells and from rat erythrocytes}; Aitkhozhina NA et al.; Liberation of inorganic ions (potassium and phosphorus), nucleotides and protein from the cells of Candida guilliermondii and rat erythrocytes was studied . It was found that leakage of these components depended on the incubation time, antibiotic dose and amount of the cell material . The potassium ions proved to be most sensitive to the antibiotic: even at low concentrations of roseofungin (2-4 microgram/ml) the amount of the intracellular potassium changed . A decrease in the dry mass and volume concentration in the cells of Candida guilliermondii and lysis in the red blood cells were observed in addition to the leakage of the above intracellular components . The cells of Candida guiliermondii at the beginning of the semilogarithmic growth phase were especially sensitive to roseofungin . The coefficient of roseofungin distribution in the cells of Candida guiliermondu was evaluated . The maximum distribution coefficient was observed at roseofungin concentrations of 40 and 80 microgram/ml for the 4- and 18-hour cultures respectively . Therefore, the effect of roseofungin is characteristic of polyens.

Antibiotiki, 1979 Aug, 24(8), 574 - 81
{Methodological approaches to developing a method of regulated antibiotic biosynthesis}; Mamonova EI et al.; Methodologic approaches to the development of methods for controlled biosynthesis of antibiotics are discussed with reference to oxytetracycline biosynthesis . The method of acute experiments in conjunction with mathematical methods of experiment planning was used for determination of the substrate concentrations optimal for the culture growth and biosynthesis of oxytetracycline . It was found that such mathematic procedure provided simultaneous determination of optimal concentrations of all the substrates.

Antibiotiki, 1979 Aug, 24(8), 463 - 6
{Formation of the antibiotic complex 4041 by a culture of Actinoplanes ianthinogenes subsp . octamycini subsp . nov.}; Gauze GF et al.; A new variety of Actinoplanes, named Actinoplanes ianthinogenes subsp . octamycini Gause et Svechnikova is described . It produces an antibiotic complex consisting of purpuromycin and a new antibiotic belonging to the group of polyens, i . e . octamycin . Maximum accumulation of the above antibiotics in the mycelium was observed in the soybean-glycerol medium.

Am J Hosp Pharm, 1979 Aug, 36(8), 1083 - 7
Comparative auditory toxicity of aminoglycoside antibiotics in leukopenic patients; Bender JF et al.; The incidence of auditory toxicity resulting from therapy with ticarcillin (T) (12 g/sq m/day) in combination with gentamicin (G) (200 mg/sq m/day), amikacin (A) (600 mg/dq m/day), or netilmicin (N) (280 mg/sq m/day) was compared . Before administration of these antibiotic combinations to febrile, granulocytopenic patients, baseline audiograms were determined by a pharmacist using a portable audiometer . The before-therapy audiograms for 32 patients receiving T and G, 29 receiving T and A, and 29 receiving T and N were compared with the audiograms after the completion of therapy . The mean length of therapy was seven days . Two patients (6.2%) receiving T and G, one (3.4%) receiving T and N, and one (3.4%) receiving T and A developed auditory toxicity with bilateral decreases of at least 20 decibels at one or more frequencies . The incidence of auditory toxicity secondary to aminoglycoside exposure was low, and the relative auditory toxicity among the three aminoglycosides appeared to be similar.

Am J Ophthalmol, 1979 Aug, 88(2), 160 - 4
Effect of local anesthetics on intraocular penetration of subconjunctival antibiotics; Ellis PP et al.; The combination of the subconjunctival injection of lidocaine HCl or procaine HCl with the subconjunctival injection of penicillin G, methicillin, cephaloridine, or gentamicin did not influence their intraocular penetration or subsequent antibiotic activity in aqueous humor of experimental animals.

Clin Chem, 1979 Aug, 25(8), 1361 - 7
Determination of aminoglycoside antibiotics in biological fluids: a review; Maitra SK et al.; We describe current procedures for measuring aminoglycoside antibiotics . Although many of these techniques are suitable for clinical adaptation, selection of a method for use in a clinical laboratory will depend on the budget and availability of equipment and expertise.

J Cell Physiol, 1979 Aug, 100(2), 335 - 42
Polyene macrolide antibiotic cytotoxicity and membrane permeability alterations . II . Phenotypic expression in intraspecific and interspecific somatic cell hybrids; Fisher PB et al.; Cytotoxicity and membrane permeability alterations induced by the polyene macrolide antibiotics filipin (FIL) and pimaricin (PIM) have been compared in parental intraspecific and interspecific somatic cell hybrids . B82 (mouse) and B1 (hamster) cells were found to be more resistant than RAG (mouse) parental cells to both polyene macrolides as indicated by 24-hour survival, 72-hour viability, and growth rate . Analysis of both intraspecific and interspecific somatic cell hybrids indicated that polyene macrolide resistance was being expressed even in the presence of the polyene macrolide-sensitive (RAG) genome . Where one of the two parental cell types is relatively polyene macrolide resistant, the use of specific polyene macrolides may prove efficacious as half-selective agents in cell hybridization.

Chest, 1979 Aug, 76(2), 174 - 5
Coronary arterial bypass operations without antibiotic coverage; Sutherland RD et al.; In this study, six of 693 consecutive patients in 29 months who underwent only myocardial revascularization, without prophylactic systemic therapy with antibiotics, experienced infection of a clean wound . This incidence of infection (0.86 percent) in such patients is the lowest reported in the literature . Prevention of infection of clean mediastinal wounds in patients undergoing only myocardial revascularization is related to preoperative preparation of the skin and local antibiotic irrigation of the wound, rather than to prophylactic systemic therapy with antibiotics.

J Trop Pediatr Environ Child Health, 1979 Aug, 25(4), 101 - 3
The use of antibiotics in childhood diarrhea; Bachtin M et al.; PIP: A comparative study was undertaken in Indonesia to assess the effect of antibiotic therapy in the treatment of acute diarrheal disease in infants . 120 children, age 2-60 months, suffering form acute gastroenteritis with varying degrees of dehydration who were treated at the Gadjah Mada University Hospital in Yogyakarta, Indonesia, between August and December 1975, were included in the study . Approximately 1/2 the group was treated with antibiotics; the other 1/2 was not . Both groups received oral rehydration therapy . No significant differences were found between the 2 groups as to duration of the diarrhea and duration of hospitalization . It is concluded that antibiotics are not generally indicated in cases of acute diarrheal disease . The only requirements in treatment seems to be maintenance of the fluid electrolyte balance .

Int J Pept Protein Res, 1979 Aug, 14(2), 81 - 7
A lipophilic derivative of neocarzinostatin . A polymer conjugation of an antitumor protein antibiotic; Maeda H et al.; A lipophilic derivative of neocarzinostatin (NCS), an antitumor antibiotic, was prepared by reaction with a synthetic water-soluble polymer, {(styrene)1 approximately 3-(maleic acid 4 approximately 7/anhydride 1)} . The reaction was carried out at pH 8.6 for 3 h and aimed at modifying the two nonessential amino groups (alpha-amino of Ala-1, epsilon-amino of Lys-20) . The NCS-polystyrene (SMANCS) was purified on a column of Sephadex G-100 in 0.05 M ammonium bicarbonate and the main product was obtained as a single peak . The elemental analysis showed an increased C and a decreased N content . U.v . and i.r . absorption spectra for SMANCS showed the presence of styrene . SDS-acrylamide gel electrophoresis at pH 8.5 and the decreased N content suggested a molecular weight of about 25 000, indicating the numbers of polymers conjugated to be about six units, two of which were found attached to the two amino groups . SMANCS was soluble in organic solvents, in contrast to NCS, and in water . SMANCS exhibited increased chemical and biological stability and appeared to possess similar in vitro biological activity.

J Gen Microbiol, 1979 Aug, 113(2), 407 - 8
Complete lysis of glutamic acid-producing bacteria by the use of antibiotics which inhibit the biosynthesis of cell walls; Komatsu Y; A novel method for obtaining complete lysis of coryneform bacteria has been devised . Bacteria in the late-exponential phase of growth are treated with antibiotics which inhibit biosynthesis of the cell wall . Organisms treated in this way show increased sensitivity to lysis by added lytic enzymes . The preparation of DNA from this group of organisms is thus greatly facilitated.

Biochim Biophys Acta, 1979 Jul 26, 563(2), 336 - 42
DNA-binding antibiotics . X-ray structure of the distamycin A analog; Gurskaya GV et al.; The crystal structure of the antibiotic distamycin A analog containing two pyrrol carboxamide fragments has been determined . The space group of the crystals is P21/b; the unit-cell dimensions are a = 11.169, b = 21.535, c = 7.863 A, alpha = beta = 90 degrees, gamma = 122.45 degrees, Z = 4 . The structure is solved by direct methods, and refined with the full-matrix least-squares procedure . The data on the structure of the pyrrol carboxamide backbone allow the following conclusions to be made about the molecular structure of the distamycin type antibiotics: (i) the amide groups have normal trans-configuration with slightly shortened C-C and C-N bonds adjacent to the pyrrol rings, (ii) the N-methyl groups of the pyrrol rings and the oxygen atoms of the amide groups have the same orientation with respect to the backbone . In the distamycin A analog molecule the pyrrol rings and amide group between them are approximately coplanar.

J Antibiot (Tokyo), 1979 Jul, 32(7), 685 - 8
New antibiotic pigments related to fusarubin from Fusarium solani (Mart.) Sacc . II . Structure elucidations; Gerber NN et al.; Three antibiotic pigments isolated from Fusarium solani and related to fusarubin (4) were shown to be O-ethylfusarubin (2), hydroxidihydrofusarubin (3) and O-ethylhydroxydihydrofusarubin (1).

Clin Pharmacol Ther, 1979 Jul, 26(1), 36 - 40
Effects of three antibiotics on theophylline kinetics; Pfeifer HJ et al.; Nine healthy subjects received single doses of intravenous aminophylline (5 mg/kg) on four occasions separated by at least 1 wk . One trial was a control; the other three were performed during administration of therapeutic doses (250 mg every 6 hr) of tetracycline, erythromycin, and cephalexin . Theophylline concentrations in multiple plasma samples drawn during 24 hr after each dose were determined by high-pressure liquid chromatography . Mean kinetic variables for theophylline during control, tetracycline, erythromycin, and cephalexin trials, respectively, were: volume of distribution, 0.57, 0.61, 0.63, and 0.62 l/kg; elimination half-life (t1/2), 7.9, 9.2, 10.3, and 8.6 hr; total clearance, 0.90, 0.84, 0.78, and 0.89 ml/min/kg . In no case did differences between treatment conditions approach significance . Thus there is no consistent evidence of a kinetic interaction between theophylline and three commonly prescribed antibiotics.

Ann Microbiol (Paris), 1979 Jul, 130B(1), 33 - 42
{Inhibition of Escherichia coli haemagglutinations by antibiotics}; Roland F et al.; Escherichia coli has been associated with a colonization factor antigen responsible for the bacterial adherence to the intestinal mucosa . This colonization factor is also responsible for haemagglutination . Among 32 antibiotics tested, only tetracyclines, chloramphenicol and nafcillin inhibit haemagglutination . Tetracycline hydrochloride, tetracycline phosphate and doxycycline are the most effective, followed by oxytetracycline, minocycline, chloramphenicol and nafcillin . Doxycline at a concentration at 0.8 mg/ml in buffered saline, chloramphenicol at 12.8 mg and nafcillin at 31 mg inhibit haemagglutination in 2 h . The inhibition of haemagglutination occurs both with E . coli susceptible and resistant to doxycycline . Pretreatment of crythrocytes with doxycycline does not prevent inhibition of haemagglutination where as pretreatment of E . coli does, suggesting that doxycycline acted on the bacteria . Once haemagglutination had occurred, doxycycline can reverse the haemagglutination, "unhooking" the bacteria from the erythrocytes . These data raise the possibility that some antibiotics may prevent adherence of E . coli to the intestinal mucosa, regardless of the susceptibility or resistance of the bacteria by a direct effect on the colonization factor antigen . Furthermore, some antibiotics may be able to detach the bacteria once adherence to the mucosa has occurred.

Clin Pharmacokinet, 1979 Jul-Aug, 4(4), 297 - 309
Pharmacokinetics of antibiotics in pregnancy and labour; Philipson A; Few of the articles published on antibiotics and pregnancy are concerned with pharmacokinetics . It is particularly difficult to evaluate possible alterations in pharmacokinetic parameters that may be due to pregnancy . Most data available have been obtained in connection with abortion or delivery . Such data may not be representative for pregnancy as such . Marked changes in most organ systems, particularly in renal function, but in composition and amounts of body fluids as well, make it likely that several pharmacokinetic parameters change, possibly gradually as pregnancy progresses . Accumulated data for several beta-lactam antibiotics, and also for aminoglycosides indicate that antibiotics eliminated mainly by renal excretion will produce lower levels in serum or plasma in pregnant women than in other individuals . Also, the half-life of certain antibiotics in serum is shorter during pregnancy . Transplacental passage occurs for all antibiotics according to the physicochemical properties of the drug . Bolus injections to a pregnant woman are more efficient than continuous infusion in producing high levels of antibiotic in fetal serum and amniotic fluid . Fetal tissue levels are higher following multiple doses than after a single dose . Lower serum levels of antibiotics in pregnant women than in other individuals following the same dosage will be unsatisfactory as micr-organisms are less likely to be affected.

Am J Obstet Gynecol, 1979 Jul 1, 134(5), 506 - 11
The efficacy of prophylactic antibiotics in cesarean section; Gall SA; The objective of this investigation was to determine the effectiveness of cefazolin-cephalothin administration as a prophylactic regime in patients undergoing cesarean section . The study was to randomized, double-blind, placebo-controlled investigation . Cefazolin, 1.0 gm or placebo was administered intramuscularly on call to the operating room, and cephalothin, 2.0 gm, or placebo was administered intravenously at 6, 12, and 24 hours postoperatively . Ninety-five patients were included in the study with 49 in the placebo group and 46 in the drug group . Nineteen patients developed 28 infections in the placebo group while eight patients developed eight infections in the drug group (P = less than 0.05) . Eight patients in the placebo group developed infections at two or more sites whereas no patient in the drug-treated group developed multiple infections . No infant developed infection and no overgrowth of bacteria occurred . This study supports the concept of preoperative antibiotic administration being beneficial to the obstetric patient.

Surgery, 1979 Jul, 86(1), 23 - 9
Parenteral antibiotics in elective colon surgery? A prospective, controlled clinical study; Barber MS et al.; The addition of perioperative gentamicin and clindamycin to an oral antibiotic bowel preparation was studied in a prospective, randomized, double-blind series of patients undergoing elective colectomy . Fifty-nine patients completed the study, with all receiving mechanical preparation of the colon and oral neomycin and erythromycin base . Thirty-one of these patients also received a preoperative and postoperative intravenous dose of gentamicin and clindamycin, while 28 received placebos . The two groups of patients were similar in age, both habitus, pathologic diagnosis, concomitant disease, operative procedures, operative time, blood loss, and adequacy of mechanical preparation of the colon . The incidence of infectious complications related to colectomy was 1% (three of 28) in the placebo group and 7% (two of 31) in the group receiving intravenous gentamicin and clindamycin . There were no wound infections directly related to colectomy in either group . There was no statistically significant reduction of infectious complications with the addition of intravenous gentamicin and clindamycin to oral neomycin and erythromycin-base bowel preparation.

J Pharm Sci, 1979 Jul, 68(7), 812 - 6
GI absorption of beta-lactam antibiotics . III: Kinetic evidence for in situ absorption of ionized species of monobasic penicillins and cefazolin from the rat small intestine and structure-absorption rate relationships; Tsuji A et al.; Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ . Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were highly absorbed, depending on their lipophilicity through the GI membrane lipoidal barrier . The structure-absorption rate relationship was established with the unstirred layer model.

JAMA, 1979 Jun 29, 241(26), 2806 - 7
Surveillance of nosocomial infections by antibiotic monitoring; Feldman L et al.; Records of all patients receiving intravenous gentamicin sulfate during a 92-day interval were reviewed to detect nosocomial infections that had been missed by routine surveillance . Only 46 of 48 of the 99 treatment courses had been detected . In 96% of cases not detected by routine surveillance, use of gentamicin was considered justified . Of the patients missed by surveillance, 83% were in oncology wards, and 46% had severe neutropenia and fever of unknown origin . Antibiotic surveillance proved a useful adjunct in estimating the incidence of nosocomial infections in such patients.

Biochim Biophys Acta, 1979 Jun 13, 554(1), 39 - 50
Interaction of polyene antibiotics with sterols in phosphatidylcholine bilayer membranes as studied by spin probes; Ohki K et al.; Interaction of filipin and amphotericin B with sterols in phosphatidylcholine membranes has been studied using various spin probes; epiandrosterone, cholestanone, phosphatidylcholine with 12-nitroxide or 5-nitroxide stearate attached to 2 position and also with tempocholine at the head group . Filipin caused increase in the fluidity of cholesterol-containing phosphatidylcholine membranes near the center, while it rather decreased the fluidity near the polar surface . On the other hand, amphotericin B did not apparently affect the fluidity . In the electron spin resonance spectrum of steriod spin probes in the antibiotic-containing membranes, both bound and free signals were observed and the association constant was calculated from the siganal intensity . In the binding of steriods with filipin, both 3 and 17 positions were involved, while the 17 positions was less involved in the binding with amphotericin B . Phase change in the host membrane markedly affected the interaction of filipin with epiandrosterone probe . The bound fraction jumped from 0.4 to 0.8 on going to the crystalline state and increased further with decrease in temperature . The overall splitting of the bound signal also increased on lowering the temperature below phase transition . This change was attributed to aggregate formation of filipin-steriod complexes in the crystalline state . On the other hand, effect of phase transition was much smaller on the interaction of amphotericin B with the steriod probe.

Mol Gen Genet, 1979 Jun 7, 173(2), 159 - 70
Biogenesis of mitochondria 51: biochemical characterization of a mitochondrial mutation in Saccharomyces cerevisiae affecting the mitochondrial ribosome by conferring resistance to aminoglycoside antibiotics; Spithill TW et al.; An examination of the effect of the aminoglycoside antibiotics paromomycin and neomycin on mitochondrial ribosome function in yeast has been made . Both antibiotics are potent inhibitors of protein synthesis in isolated mitochondria . With isolated mitochondrial ribosomes programmed with polyuridylic acid (poly U), the drugs are shown to inhibit polyphenylalanine synthesis at moderately high concentrations (above 100 microgram/ml) . At lower concentrations (about 10 microgram/ml), paromomycin and neomycin cause a 2-3 fold stimulation in the extent of misreading of the UUU codons in poly U, over and above the significant level of misreading catalyzed by the ribosomes in the absence of drugs . Comparative studies have been made between a paromomycin sensitive strain D585-11C and a mutant strain 4810P carrying the par l-r mutation in mtDNA, which leads to high resistance to both paromomycin and neomycin in vivo . A high level of resistance to these antibiotics is observed in strain 4810P at the level of mitochondrial protein synthesis in vitro . Whilst the degree of resistance of isolated mitochondrial ribosomes from strain 4810P judged by the inhibition of polyphenylalanine synthesis by paromomycin and neomycin is not extensive, studies on misreading of the poly U message promoted by these drugs demonstrate convincingly the altered properties of mitochondrial ribosomes from the mutant strain 4810P . These ribosomes show resistance to the stimulation of misreading of the codon UUU brought about by paromomycin and neomycin in wild-type mitochondrial ribosomes . Although strain 4810P was originally isolated as being resistant to paromomycin, in all the in vitro amino acid incorporation systems tested here, the 4810P mitochondrial ribosomes show a higher degree of resistance to neomycin than to paromomycin . It is concluded that the parl-r mutation in strain 4810P affects a component of the mitochondrial ribosome, possibly by altering the 15S rRNA or a protein of the small ribosomal subunit . The further elucidation of the functions in the ribosomes that are modified by the parl-r mutation was hampered by the inability of current preparations of yeast mitochondrial ribosomes to translate efficiently natural messenger RNAs from the several sources tested.

Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 444 - 58
{Prevention of bacterial resistance to antibiotics (author's transl)}; Schito GC; Even though genetically determined, bacterial resistance to antibiotics are perpetuated only when a continual selection is present . Bacterial resistance caused by use of antibiotics is evident in the hospital setting . Since it has been demonstrated in the absence of section bacteria tend to return to a sensitive phenotype, the A . suggests that only with the rational use of antibiotics is the prevention of bacterial resistance possible.

J Gynecol Obstet Biol Reprod (Paris), 1979 Jun, 8(4), 359 - 64
{Study of transplacental transmission of beta-lactam antibiotics (author's transl)}; Bergogne-Berezin E et al.; The authors present the results of the study of transplacental transfer of 3 recent beta lactam antibiotics: amoxicillin, cephradin and cefoxitin . The experiment was carried out in 37 pregnant women who had a premature rupture of membranes or who were undergoing a cesarean section . In these patients antibiotherapy was indicated in view of a possible superinfection . The results of the study show a worthwhile transplacental penetration of the 3 drugs tested . The concentrations achieved in umbilical cord blood and amniotic fluid increase with time and finally exceed the levels measured in maternal blood, after a period of time varying from 2 to 4 hours according to the drug and the route of administration.

Ann Trop Med Parasitol, 1979 Jun, 73(3), 235 - 40
Length of antibiotic therapy in in-patients with primary pneumonias; Awunor-Renner C; Seventy-three subjects with primary pneumonia in a hospital in Northern Nigeria were given antibiotics until they had been afebrile for 24 hours . The average duration of therapy was 2.54 days (about 60 hours), which is considerably shorter than the current recommended practice . Subjects with hepatosplenomegalic schistosomiasis and tropical splenomegaly syndrome required antibiotics for a significantly longer period (3.75 days) than those without either of these conditions . Those with an antigenaemia did not require antibiotics for a significantly longer period than those without an antigenaemia . There were no deaths, no increase in morbidity and in virtually all cases complete resolution of the lung lesion occurred within the expected time . It is suggested that in primary pneumonia it is more rational to stop antibiotics after the patient has been afebrile for 24 hours . This leads to a shorter stay in hospital and to the use of less antibiotic.

J Antibiot (Tokyo), 1979 Jun, 32(6), 593 - 9
Bioconversion and biosynthesis of 16-membered macrolide antibiotics . XIII . Regulation of spiramycin I 3-hydroxyl acylase formation by glucose, butyrate, and cerulenin; Kitao C et al.; The effects of glucose, butyrate, and cerulenin on the formation of spiramycin I 3-hydroxyl acylase were investigated by using the cell-free extract prepared from the spiramycin-producing strain of Streptomyces ambofaciens KA-1028 . Glucose induced the formation of the acylase, and this induction was remarkably repressed by butyrate . Cerulenin, on the other hand, not only cancelled the repression by butyrate but also stimulated the formation of the acylase . The unsuccessful trapping of spiramycin I as an intermediate during the bioconversion from neospiramycin I to spiramycin III in the presence of cerulenin was due to the rapid acylation of spiramycin I caused by the acylase induced by cerulenin.

J Antibiot (Tokyo), 1979 Jun, 32(6), 565 - 8
The structure of a novel sugar component of polyene macrolide antibiotics: 2,6-dideoxy-L-ribohexopyranose; Zielinski J et al.; A novel carbohydrate has been isolated after acidic hydrolysis of nystatin A3, candidinin and polyfungin B and its structure established as 2,6-dideoxy-L-ribohexopyranose.

J Antibiot (Tokyo), 1979 Jun, 32(6), 555 - 8
The structure of nocamycin, a new antitumor antibiotic; Horvath G et al.; The structure of nocamycin, a new antitumor antibiotic, has been elucidated with the aid of mass- and PMR-spectroscopic investigation of the antibiotic and its various chemical transformation products . Nocamycin is structurally related to tirandamycins.

J Antibiot (Tokyo), 1979 Jun, 32(6), 549 - 54
Holomycin and an antibiotic (MM 19290) related to tunicamycin, metabolites of Streptomyces clavuligerus; Kenig M et al.; Streptomyces clavuligerus produces penicillin N, several cephalosporins and the beta-lactamase inhibitor clavulanic acid . The detection, isolation and properties of further metabolites of this culture, MM 21801 and MM 19290, are described . MM 21801 was identified as the antibiotic holomycin . MM 19290 was shown to be related to tunicamycin, an antibiotic complex obtained from cultures of Streptomyces lysosuperificus.

Antibiotiki, 1979 Jun, 24(6), 417 - 22
{Action of polyene antibiotics on actinomycetes with a varying lipid makeup}; Efimova TP et al.; The effect of polyenic antibiotics, such as nystatin, levorin, amphotericin B and mycoheptin on 93 representatives of various species of the ray fungi was studied . It was shown that resistance of the actinomycetes to the polyens was connected with the absence or insufficient content of sterols (0.001--0.008 per cent in the dry mycelium) . On addition of cholesterol to the nutrient media (100 microgram/ml) it was included into the membranes of some cultures and their sensitivity increased 2--60 times . Resistance of Actinomyces sp . LIA 0775 grown on the media with fats differing in their composition decreased 2--4 times . In these cases the culture lipids were characterized by lower content of phospholipids (35--45 per cent from the total lipids as compared to 70--80 per cent when grown on the control medium without fats) and significantly increased content of unsaturated fatty acids (3--4 times).

Antibiotiki, 1979 Jun, 24(6), 409 - 13
{Use of antibiotics in selecting a nystatin producer}; Lavrent'eva GI et al.; The lethal and mutagenic effect of streptomycin and nystatin on Act . noursei, strain 408 producing nystatin was studied . The survival of the spores of strain 408 on the medium with streptomycin decreased with an increase in the antibiotic concentration . Streptomycin had a selective effect on the nystatin-producing organism decreasing the frequency of morphologically changed and low active variants and revealing highly active and antibiotic stable variants . The survival of the spores of strain 408 on the medium with nystatin (20,000 units/ml) amounted to 35 per cent . Nystatin had an inhibitory effect on the organism producing it which was evident from delayed growth and significant modification variation of the colonies, as well as from a marked increase in the number of the variants characterized by low antibiotic production.

Fertil Steril, 1979 Jun, 31(6), 660 - 5
Ureaplasma urealyticum and human infertility: the effect of antibiotic therapy on semen quality; Swenson CE et al.; Semen characteristics were evaluated in 64 men visiting our infertility clinic before and after the eradication of genital infection with Ureaplasma urealyticum . Semen quality was also analyzed in 9 men who were unsuccessfully treated for genital Ureaplasma infection, 11 men who had negative cultures and received no treatment, and 11 men who had negative cultures but received empirical antibiotic therapy . A significant improvement in spermatozoal motility (both the speed of forward progession and the percentage of motile cells) was found in the group that was successfully treated for Ureaplasma infection . Improvements were not demonstrated in any of the other patient groups . A correlation was found between improved motility and a decrease in certain abnormal features of seminal cytology that appear to be associated with Ureaplasma genital infection.

Genetika, 1979 Jun, 15(6), 1007 - 14
{Yeast resistance to polyene antibiotics . I . Production of Saccharomyces cerevisiae mutants resistant to nystatin and their genetic analysis}; Levchenko AB et al.; 239 nistatin-resistant mutants were selected after UV-irradiation of yeasts . Phenotypical analysis has revealed two main groups of the mutants: 1) resistant to nistatin and resistant or sensitive (in different combinations) to haptaens; 2) resistant to nistatin and having an increased resistance to haptens . It is found that the sensitivity dominates over the resistance and hyper-resistance . Genetic analysis of the mutant collection has shown that the resistance to nistatin is determined by 5 nuclear genes (hysr) . Hyper-resistance is controlled by mutations in other genes, which are not connected with stable phenotype . Genes of hyper-resistance can be considered as minus-modificators of pleiothrophic cross-resistance, characteristic of hysr genes . Plus-modificator genes of polyenic resistance are described . The gene hysr1 is linked with its chromosome.

J Hyg (Lond), 1979 Jun, 82(3), 443 - 52
Serotypes of antibiotic resistant Escherichia coli isolated from the sewage of Palmerston North (New Zealand); Meekin GE et al.; Antibiotic resistant strains of Escherichia coli were isolated from the domestic sewage of Palmerston North . The ability of these strains to transfer the drug resistance markers to two different recipient E . coli strains was assessed . The 'O' and 'H' serotypes of all strains were determined and attempts at correlation with the drug resistance studies were made . Some typically 'human' serotypes were found as well as a number of rarely described ones . No correlation between serotype and resistance pattern was observed.

Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 620 - 9
{Lactamase and bacterial resistance to beta-lactam antibiotics (author's transl)}; Meinardi G et al.; Bacterial resistance to beta-lactam antibiotics, as indicated on sensitivity tests, is not always directly proportional to their beta-lactamase synthesis capacity . From the epidemiological viewpoint, therefore, it would appear important to look specifically for the various beta-lactamases in bacteria . Chemical and biological methods for this purpose are reviewed, with particular attention to those including special steps which render them speedy, economical and feasible in any laboratory . Practical examples are offered.

J Antibiot (Tokyo), 1979 Jun, 32(6), 646 - 53
Studies on the competition of polyene antibiotics for sterols; Patterson J et al.; The fractional change in the corrected fluorescence of pimaricin or filipin in the presence of a limiting amount of sterol and a competing polyene antibiotic has been used to estimate the relative affinity of amphotericin B, nystatin, filipin, and pimaricin for stigmasterol and for cholesterol . The relative affinities for cholesterol were filipin greater than amphotericin B greater than pimaricin greater than nystatin, while the relative affinities for stigmasterol were filipin greater than pimaricin greater than amphotericin B greater than nystatin . The data indicate that pimaricin and filipin can both interact simultaneously with about 30% of the cholesterol or stigmasterol . However, the stoichiometry of filipin and pimaricin alone for cholesterol and for stigmasterol in dilute aqueous solutions is 1 : 1 . In the experiments which indicated both pimaricin and filipin interact with the same sterol molecule changes in corrected fluorescence and the absorbance spectra were monitored; and these criteria indicated that both pimaricin and filipin had interacted with the sterols . Light-scattering measurements indicate large aggregates were not formed . Although the data shows in dilute aqueous solutions the stoichiometry of filipin and/or pimaricin for sterols is 1 : 1, in more complex solutions, other combinations or interactions are indicated especially for pimaricin.

Antibiotiki, 1979 Jun, 24(6), 454 - 8
{Effect of penicillin series antibiotics on the properties of Brucella}; Kondrat'eva OV et al.; Investigation of the properties of antibiotic-resistant variants obtained experimentally from various species of Brucella indicated that benzylpenicillin, ampicillin and ceporin induced significant changes in the main properties of Brucella, i.e . phagolysability, agglutinability, production of brucellacin and hydrogen sulfate, attitude to dyes . Only the nutrient requirements of Brucella did not change when it was grown on synthetic media which is of great importance for investigation of changed Brucella strains.

Antibiotiki, 1979 Jun, 24(6), 403 - 9
{Biochemical mutants of Actinomyces griseus, a producer of the antibiotic grisin . The isolation of the mutants and a study of the level of grisin antibiotic synthesis}; Kuklin VV et al.; Biochemical mutants of Actinomyces griseus producing grisin were obtained under the action of chemical mutagens . The mutants were divided into 2 groups . The mutants with impaired synthesis of amino acids of the aspartic acid family, i.e . lysine, homoserine and methionine were included into the 1st group . The 2nd group included the mutants with impaired synthesis of the other amino acids, i.e . histidine, arginine, tyrosine, phenylalanine and valine . The antibiotic production level in the biochemical mutants was studied . It was found that the level of the antibiotic production was decreased in most of the biochemical mutants . A necessity for increased fonds of lysine and arginine for biosynthesis of grisin was shown.

Anaesthesia, 1979 Jun, 34(6), 562 - 6
Aminoglycoside antibiotics and sympathetic ganglionic transmission; Taylor PJ et al.; The effects of streptomycin, gentamicin, tobramycin and amikacin on transmission in sympathetic ganglia have been studied using the guinea pig isolated hypogastric nerve-vas deferens preparation . These aminoglycoside antibiotics produce dose-related sympathetic blockade at concentrations greater than the common therapeutically effective antibiotic concentrations.

Biochemistry, 1979 May 29, 18(11), 2149 - 54
Antibiotic effects on the photoinduced affinity labeling of Escherichia coli ribosomes by puromycin; Grant PG et al.; The effect of ribosomal antibiotics on the photoinduced affinity labeling of Escherichia coli ribosomes by puromycin {Cooperman, B.S., Jaynes, E.N., Brunswick, D.J., & Luddy, M.A . (1975) Proc . Natl . Acad . Sci . U.S.A . 72, 1974; Jaynes, E.N . Jr., Grant, P.G., Giangrande, G., Wieder, R., & Cooperman, B.S . (1978) Biochemistry 17, 561} has been studied . Although blasticidin S, sparsomycin, lincomycin, and erythromycin are essentially without effect, major changes are seen on addition of either chloramphenicol or tetracycline . The products of photoincorporation have been characterized by one- and two-dimensional gel electrophoresis and by specific immunoprecipitation with antibodies to ribosomal proteins . In the presence of chloramphenicol, protein S14 becomes the major labeled protein . In the presence of tetracycline, L23 remains the major labeled protein, but the yield of labeled ribosomes is enormously increased, and the labeling is more specific for L23 . These results are discussed in terms of the known modes of action of these antibiotics and the photoreactivity of tetracycline.

S Afr Med J, 1979 May 12, 55(20), 807 - 8
The comparative efficacy and safety of aminoglycoside antibiotics; Folb PI; In this article a report submitted to the Director of Hospital Services of the Cape Provincial Administration is summarized . The object of the report was to make firm recommendations where possible as to the use of the aminoglycosides in the Cape hospitals, taking into account considerations of comparative efficacy, safety and cost.

Am J Vet Res, 1979 May, 40(5), 673 - 5
Critical evaluation of taeniacidal antibiotic S15-1 (SQ 21, 704) for removal of natural tapeworm infections in dogs and cats; Szanto J et al.; The new taeniacidal antibiotic S15-1 (SQ 21,704) was evaluated against naturally occuring infections of Taenia pisiformis in 53 dogs, Dipylidium caninum in 35 dogs, T taeniaformis in 18 cats, and D caninum in 33 cats . It all instances, the compound was administered in gelatine capsules in a single oral dose . The doses tested were between and 200 mg/kg of body weight in dogs and between 15 and 45 mg/kg in cats . In dogs, doses of 25 mg/kg and greater were 100% effective against T pisiformis, whereas a dose of 50 mg/kg was necessary to clear D caninum . In cats, a single oral dose of 22.5 mg/kg was 100% efficacious against T taeniaeformis, and a single dose of 45 mg/kg (the largest dose tested) clearly seven of eight cats of D caninum . The efficacy was limited to tapeworms only; there was no efficacy against nematodes . The antibiotic was well tolerated by both species with no drug-related vomiting or other side-effects observed.

J Antibiot (Tokyo), 1979 May, 32(5), 504 - 10
Interaction of aminoglycoside antibiotics with phospholipid liposomes studies by microelectrophoresis; Alexander AM et al.; Microelectrophoresis was found to be a rapid method for studying the interaction between aminoglycoside antibiotics and liposomes prepared from acid phospholipids . The ability to cause charge reversal of liposomes prepared from phosphatidyl inositol was ranked in the order neomycin greater than gentamicin greater than tobramycin greater than amikacin greater than kanamycin greater than ribostamycin greater than streptomycin greater than dihydrostreptomycin greater than Ca2+ . Similar results were obtained with liposomes prepared from a mixture (8: 2) of phosphatidyl choline and phosphatidic acid, but no effect was detectable with neutral liposomes made from phosphatidyl choline only . The results support the view that the attraction between positively charged nitrogen groups on the antibiotics and the negatively charged groups of acidic phospholipids are predominantly responsible for the interaction . Extension of the studies to ionic strengths and calcium concentrations similar to those found in vivo showed a reduction, but not elimination, of the observed effects.

J Med Chem, 1979 May, 22(5), 533 - 7
Conformational analogy between beta-lactam antibiotics and tetrahedral transition states of a dipeptide; Boyd DB; The three-dimensional structures of various penicillins and cephalosporins are compared to the spatial characteristics of glycylglycine and the tetrahedral adducts formed when a nucleophile attaches to the amide carbonyl carbon of this dipeptide . The dipeptide is taken to model the D-alanyl-D-alanine terminus of the precursors of bacterial cell-wall peptidoglycan cross-links . Least-squares fitting shows that the spatial match between the dipeptide and the antibiotic depends on the thiazolidine or dihydrothiazine ring conformation, as well as the conformation of the dipeptide . In general, the tetrahedral adducts fit somewhat better than the parent dipeptide . A previously unobserved 3-cephem conformer is found by molecular mechanics calculations to be less stable than the usual crystallographically observed conformer.

Cancer Treat Rep, 1979 May, 63(5), 817 - 20
Anthracycline antibiotic pharmacology and metabolism; Bachur NR; The anthracycline antibiotics show evidence of numerous interactions with cellular components and participation in several metabolic pathways . Small structural changes in the antibiotic molecule can produce major changes in intracellular localization and interaction . To date, we find that all of the anthracycline antibiotics form free radical intermediates through the catalysis of microsomal and nuclear electron-transport machinery . NADPH cytochrome P-450 reductase catalyzes the free radical formation . The free radical intermediates ("site-specific free radicals") may be causative of both toxicity and pharmaceutic action . The free radical intermediates degrade nonenzymatically to 7-deoxyaglycone metabolites which prove the existence of the free radical in vivo.

Arch Surg, 1979 May, 114(5), 580 - 3
Ecthyma gangrenosum: survival with individualized antibiotic therapy; Solem LD et al.; Five burn patients with ecthyma gangrenosum were treated with gentamicin sulfate in an individualized aminoglycoside regimen . Dosages greater than the currently recommended 3 to 5 mg/kg/day were necessary and ranged from 15 to 30 mg/kg/day . These increased dosages cannot be used routinely but only as serum level data indicate the need . Four of the five patients survived their course of ecthyma gangrenosum . The single fatality received a much smaller dosage of gentamicin as compared with the other four patients . No ototoxic or nephrotoxic reactions were noted in any of the patients.

What Is Genome?, What Is Cell Biology?, What Is Listeria Monocytogenes?, What Is Protein?, What Is Botulism?, r, Bacteriology, s, Microbe, i, Bacteria, n, Bacterium, i, Microbes, a, Microorganism, o, Salmonella typhimurium, c, Escherichia coli, s, Salmonella typhimurium, a, Escherichia coli, c, Multidrug resistant, a, Salmonella, o, Escherichia coli, a, Bacteriological, o, Antibiotics, o, Ps. fluorescens, a, Flavobacterium, a, Clostridia, c, Staphylococcus, i, Biofilms, n, B. anthracis, s, Haemophilus, e, Bacteria, r, Microorganisms, a, Bacteriophage, i, Cell suspensions

Scientific Publications - Work Done by Microbiology Reader Bioscreen C
Agricultural Microbiology Anaerobic Microbiology Antimicrobial Susceptibility Artificial Atmosphere Bioassay of Antibiotics Biofilm Microbiology Bioreactor Technology Biotechnology Cell Biology Clinical Microbiology Environmental Microbiology Experiments with Yeast	Fermentation Food Microbiology Functional Genomics Gene Technology Growth Media Development Growth Rate and Lag Time Industrial Microbiology Medical/Pharmaceutical Field Microbiological Assay Microbiological Research Microbiology of Cosmetics go to a specific theme...	Military Microbiology Molecular Microbiology Mutagenicity and Genotoxicity Oral Microbiology Patents Postantibiotic Studies Soil Microbiology Spore Microbiology Veterinary Microbiology Waste/Wastewater Treatment Water Microbiology Wine Microbiology

� 2005 Transgalactic Ltd (manufacturer of Bioscreen C software) | Privacy Statement | P.O. Box 1393, 00101 Helsinki, Finland, phone: +358 9 85172920, fax: +358 9 8749481, e-mail: microbiology@bionewsonline.com

Last modified: May 25, 2005