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DISCOVERY, FERMENTATION, BIOLOGICAL AS WELL AS IONOPHORE PROPERTIES AND TAXONOMY OF THE PRODUCING CULTURE
CHAO-MIN LIU, T. E. HERMANN, A. DOWNEY, B. LA T. PROSSER, E. SCHILDKNE ...
1983 Volume 36 Issue 4 Pages
343-350
Published: 1983
Released on J-STAGE: April 12, 2006
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A hitherto undescribed Nocardia culture has been isolated from an Australian soil sample and found to produce novel polyether antibiotics X-14868A, X-14868B, X-14868C and X-14868D.
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S. N. SEHGAL, H. BAKER, C. P. ENG, K. SINGH, CLAUDE VÉEZINA
1983 Volume 36 Issue 4 Pages
351-354
Published: 1983
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Demethoxyrapamycin is a new antifungal antibiotic which is co-produced with rapamycin by
Streptomyces hygroscopicus.It was isolated as a minor component during recovery of rapamycin. Its antifungal and antitumor activity is compared with that of rapamycin.
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S. N. SEHGAL, HELEN CZERKAWSKI, ALICIA KUDELSKI, K. PANDEV, R. SAUCIER ...
1983 Volume 36 Issue 4 Pages
355-361
Published: 1983
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A streptomycete was isolated from a Guatemala soil sample and found to inhibit Gram-positive bacteria including mycobacteria. The antibiotic-producing microorganism was characterized, identified as a new species and named
Streptomyces ravidus. The antibiotic principle was extracted with organic solvent from the mycelium, isolated in crystalline form and named ravidomycin. Ravidomycin is mainly active against Gram-positive bacteria including mycobacteria. It shows only weak activity against Gram-negative organisms and no activity against fungi. Ravidomycin exhibits potent antitumor activity against P388 lymphocytic leukemia, Colon 38 tumor and CD8F1 mammary tumor. Acute toxicity in mice is low.
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S. SANTIKARN, S. J. HAMMOND, D. H. WILLIAMS, A. CORNISH, M. J. WARING
1983 Volume 36 Issue 4 Pages
362-364
Published: 1983
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Fast atom bombardment mass spectrometry has been used to determine the molecular weights of a number of new antibiotics of the triostin group which have both the natural quinoxaline-2-carboxyl chromophores replaced by substituted analogues.
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ROBERTO SPAGNOLI, LEONARDO CAPPELLETTI, LUCIANO TOSCANO
1983 Volume 36 Issue 4 Pages
365-375
Published: 1983
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Transformation of erythronolide B to new antibiotics was attempted by feeding this compound during the fermentation of
Streptomyces antibioticus ATCC 31771, a blocked mutant of an oleandomycin producing strain. As a result, four new active compounds were obtained with hybrid structures between erythromycin and oleandomycin. They were identified as 3-
O-oleandrosyl-5-
O-desosaminyl-15-hydroxyerythronolide B (
I), 3-
O-oleandrosyl-5-
O-desosaminylerythronolide B (
II), 3-
O-oleandrosyl-5-
O-desosaminyl-(8
S)-8-hydroxyerythronolide B (
III) and 3-
O-oleandrosyl-5-
O-desosaminyl-(8
R)-8, 19-epoxyerythronolide B (
IV). They were found to be less active, but more stable to acid, than erythromycin A. From their relative biogenetical relationship together with the structure elucidated some hypotheses about late stages of oleandomycin biosynthesis are inferred too.
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H. A. KIRST, G. M. WILD, R. H. BALTZ, E. T. SENO, R. L. HAMILL, J. W. ...
1983 Volume 36 Issue 4 Pages
376-382
Published: 1983
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The physicochemical characterization and proof of structure are reported for several new macrolide antibiotics related to tylosin which have been obtained by fermentation of mutant strains of
Streptomyces fradiae.
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LAURENCE H. HURLEY, J. STEFAN ROKEM
1983 Volume 36 Issue 4 Pages
383-390
Published: 1983
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The biosynthesis of the antitumor antibiotic, CC-1065, has been investigated by radioactive isotope techniques, in combination with chemical degradation of CC-1065. Tyrosine, dopa, serine and methionine (S-CH
3CH group) have been shown to be precursors of CC-1065. Tyrosine is proposed to be a precursor of all three benzodipyrrole subunits, while dopa is only apparently incorporated into subunits B and C. Serine is postulated to contribute three 2C units, with loss of C-1, to all three subunits of CC-1065. The S-CHCH
3CH group of methionine probably contributes four C-1 units to CC-1065 of which one is incorporated with considerable loss of tritium, most probably into the cyclopropane ring of subunit A.
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V. MECHANISM OF ACTION OF THE COMPONENT VA-2
KATO TANI, TOUTARO YAMAGUCHI
1983 Volume 36 Issue 4 Pages
391-397
Published: 1983
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Effects of VA-2, a component of quinoid antibiotic M-92, on the incorporation of radioisotope-labeled compounds into the cells of
Staphylococcus aureus were studied. Deoxyribonucleic acid (DNA) synthesis was immediately inhibited by the addition of VA-2. Significant inhibitions of ribonucleic acid and protein syntheses and minor reduction of peptidoglycan synthesis were observed after a short delay. VA-2 immediately induced the degradation of DNA prelabelled with [
14C]thymidine in the cells of
S. aureus. In the examinations using
E. coli enzyme and calf thymus DNA as a template, VA-2 prevented DNA-dependent DNA polymerase reaction. The inhibition of DNA polymerase I reaction was fairly reversed by increasing the concentration of template DNA, but slightly by that of the enzyme. Agarose gel electrophoresis showed that VA-2 elicited an extensive cleavage of PM2 cccDNA. VA-2 caused a primary conversion of the cccDNA to ocDNA at a low concentration (0.2 μg/ml), while at high concentrations (2.0 and 20 μg/ml) it cleaved the cccDNA to ocDNA and linear DNA progres sively. These cleavages were observed even at 0°C as well as at 37°C, and were enhanced with the addition of a reducing agent such as 2-mercaptoethanol or sodium borohydride.
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CHING-PONG MAK, KAPA PRASAD, FRIEDERIKE TURNOWSKY
1983 Volume 36 Issue 4 Pages
398-406
Published: 1983
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Clavulanic acid analogs lacking the C-3 carboxyl group are potent inhibitors of both plasmid and chromosomally mediated β-lactamases. They exhibit only low intrinsic antibacterial activity, but potentiate the activity of ampicillin and cephaloridine against β-lactamase producing
Escherichia coli and
Enterobacter cloacae in vitro. No synergism was observed in β-lactamase negative strains. The
E. coli TEM 1 and the
E. cloacae P99 enzymes are inhibited in a progressive and irreversible manner by these compounds.
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VERSATILE METHODS FOR DISPLACEMENT OF THE C-3 SULFUR SIDE CHAIN OF CARBAPENEMS WITH OTHER THIOL GROUPS
KEN-ICHI YAMAMOTO, TAKEO YOSHIOKA, YASUYUKI KATO, KUNIO ISSHIKI, MASAY ...
1983 Volume 36 Issue 4 Pages
407-415
Published: 1983
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Carbapenem derivatives substituted at the C-3 position were synthesized (1) by treating carbapenem
S-oxides with various mercaptans in the presence of a base (Fig. 3), or (2) by alkylating or acylating 3-thiol carbapenems (Fig. 4).
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M. J. BASKER, R. J. BOON, S. J. BOX, E. A. PRESTIGE, G. M. SMITH, S. R ...
1983 Volume 36 Issue 4 Pages
416-422
Published: 1983
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The carbapenem antibiotics, which include the olivanic acids and the thienamycins, have a broad-spectrum of antibacterial activity but only thienamycin itself shows appreciable activity against
Pseudomonas aeruginosa. The zwitterionic nature of thienamycin was reproduced in the olivanic acid series by preparing the deacetyl derivatives of MM 17880 and MM 22380-compounds NA 26975 and NA 26978. The latter derivative showed anti-pseudomonas activity and had an antibacterial spectrum similar to thienamycin itself. In contrast the
O-sulfated analogue, NA 26975, was no more active than the parent compound against
P. aeruginosa. Both deacetyl compounds were more stable than the parent natural products to a mouse kidney enzyme preparation and gave higher urinary recoveries in the mouse.
Pharmacokinetic studies with MM 13902 in various animal species showed that the compound was rapidly eliminated from the blood and gave only low urinary recoveries. Similar findings were observed also in human volunteers given MM 13902. The nephrotoxicity reported for thienamycin/MK 0787 in the rabbit was not seen with the olivanic acids MM 13902, MM 17880, MM 22382 and MM 22383 when tested under the same conditions.
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MASAZO TAJIMA, KAKUYO SAWA, KUNITOMO WATANABE, KAZUE UENO
1983 Volume 36 Issue 4 Pages
423-428
Published: 1983
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Two hundred anaerobic isolates from clinical specimens were examined for β-lactamase production by Nitrocefin methodology. Altogether, 77 strains were β-lactamase producers. Organisms belonging to Bacteroides melaninogenicus group, i.e., B. intermedius and B. bivius, were found to have a significant frequency of β-lactamase production. Substrate profile and sensitivity to the β-lactamase inhibitors, sulbactam, clavulanic acid, cloxacillin, and cefmetazole, a cephamycin derivative, were determined for these enzymes. All enzymes hydrolyzed cephalosporins more rapidly than penicillins. Cefmetazole was not hydrolyzed at all. Strains of B. fragilis, B. thetaiotaomicron, B. uniformis, B. ovatus and B. oralis produced β-lactamases sensitive to all four inhibitors. Strains of B. intermedius, B. bivius and B. disiens produced enzymes of different nature which were inhibited only by cefmetazole. B. vulgatus enzyme was inhibited by three of the four inhibitors. These results suggest that the β-lactamases of the genus Bacteroides may be classified by substrate profile and inhibitor pattern.
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TAKESHI MURAKAMI, CHUHEI NOJIRI, HIROMI TOYAMA, ERIKO HAYASHI, YUJIRO ...
1983 Volume 36 Issue 4 Pages
429-434
Published: 1983
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Pock forming ability of fifteen plasmids isolated from antibiotic-producing Streptomyces was examined with polyethylene glycol mediated protoplast transformation. Four plasmids (pSF765, pSF689, pSF674 and pSF601) were found to have pock forming ability on
Streptomyces lividans 66. Each putative transformants isolated from the center of pock regions harbored plasmids with same restriction enzyme cleavage sites as original plasmids. The plasmids from the transformants produced pock, which were morphologically identical to the original plasmids.
Transformation frequency of
S. lividans 66 with pSF689 from
S. lividans 66 was at least 500-fold higher (5×10
5 transformants per 1μg DNA) than that with the plasmid isolated from the original strain (10
3 transformants per 1μg DNA). In case of pSF765 the transformation frequency was not changed (about 10
5 transformants per 1μg DNA) by replications
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ROBERTO SPAGNOLI, LUCIANO TOSCANO
1983 Volume 36 Issue 4 Pages
435-437
Published: 1983
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TAKAO OKAZAKI, MICHIHISA ONO, ATSUSHI AOKI, RIKIYA FUKUDA
1983 Volume 36 Issue 4 Pages
438-441
Published: 1983
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AKINOBU INOUE, TAKASHI DEGUCHI, MAYUMI YOSHIDA, KUNIKATSU SHIRAHATA
1983 Volume 36 Issue 4 Pages
442-444
Published: 1983
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MASA HAMADA, SHINICHI KONDO, HIKARU NAKAMURA, TAKAKO IKEDA, DAISHIRO I ...
1983 Volume 36 Issue 4 Pages
445-447
Published: 1983
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HIRONOBU IINUMA, HIKARU NAKAMURA, HIROSHI NAGANAWI, TORU MASUDA, SHUIC ...
1983 Volume 36 Issue 4 Pages
448-450
Published: 1983
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KIYOTO ISHII, SHINICHI KONDO, YOSHIO NISHIMURA, MASA HAMADA, TOMIO TAK ...
1983 Volume 36 Issue 4 Pages
451-453
Published: 1983
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KIYOTO ISHII, YOSHIO NISHIMURA, SHINICHI KONDO, HAMAO UMEZAWA
1983 Volume 36 Issue 4 Pages
454-456
Published: 1983
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MASAYA NAKAGAWA, YOICHI HAYAKAWA, HIROYUKI KAWAI, KANJI IMAMURA, HIDEO ...
1983 Volume 36 Issue 4 Pages
457-458
Published: 1983
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BRUCE B. JARVIS, VIVEKANANDA M. VRUDHULA
1983 Volume 36 Issue 4 Pages
459-461
Published: 1983
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