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KENNETH L. Jr. RINEHART, RONALD M. STROSHANE
1976 Volume 29 Issue 4 Pages
319-353
Published: 1976
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TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION
MASAYUKI OHSHIMA, NOBORU ISHIZAKI, KIMIHIKO ABE, MASUFUMI UKAWA, YASUM ...
1976 Volume 29 Issue 4 Pages
354-365
Published: 1976
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Antibiotic DE-3936 was isolated from the fermentation broth of a streptomycete No. 9735-1, which is identified as a strain of
Streptomyces hygroscopicus. The antibiotic is a hydrophobic compound having the molecular formula of C
44H
75O
14Na and is active against Gram-positive bacteria, mycobacteria, mycoplasma and protozoa. especially coccidia. Its chemical and biological properties indicate that antibiotic DE-3936 belongs to the group of polyether antibiotics and is identical with lonomycin.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. VIII
JUN'ICHI SHOJI, HIROSHI HINOO, YOSHIHARU WAKISAKA, KENZO KOIZUMI, MIKA ...
1976 Volume 29 Issue 4 Pages
366-374
Published: 1976
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Thiocillins I and It were isolated from the culture broth of
Bacillus cereus G-15, and thiocillins II and III from that of
Bacillus badius AR-91. Also, the former two were probably produced by
Bacillus megatherium I-13. These antibiotics active against Gram-positive bacteria are soluble in a mixture of chloroform and methanol, show characteristic ultraviolet absorptions (maxima at
ca. 275 nm and
ca. 348 nm), and contain a high content of sulfur, as much as approximately 15%. They are related to each other and also to micrococcin P, but differentiated by chromatographic behaviours.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. IX
JUN'ICHI SHOJI, RYUZI SAKAZAKI, YOSHIHARU WAKISAKA, KENZO KOIZUMI, MIK ...
1976 Volume 29 Issue 4 Pages
375-379
Published: 1976
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A new peptide antibiotic, brevistin, was isolated from the culture broth of
Bacillus brevis 342-14. Brevistin is an acylpeptide with an approximate empirical formula of C
63H
91N
15O
18 containing aspartic acid, threonine, glycine, valine, isoleucine, phenylalanine, tryptophan and 2, 4-diaminobutyric acid. The antibiotic is soluble in acid and alkaline water. Its hydrochloride is soluble in methanol. Brevistin is active against Ggam-positive bacteria
in vitro and
in vivo, and is of low toxicity to mice.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. X
JUN'ICHI SHOJI, TOSHIYUKI KATO
1976 Volume 29 Issue 4 Pages
380-389
Published: 1976
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Acid hydrolysis revealed the constituent amino acids of brevistin as follows: aspartic acid (D-form 2, L-form 1), L-threonine (1), glycine (1), sum of L-valine and L-isoleucine (1), [L-phenylalanine (1), L-tryptophan (1), and 2, 4-diaminobutyric acid (D-form 1, L-form 1). The constituent fatty acid was elucidated to be anteisononanoic acid by gas chromatography-mass spectrometry. A lactone linkage was proved between phenylalanine and the hydroxy group of threonine. Opening the lactone ring with dilute alkali afforded brevistinic acid. Deacylation with an enzyme preparation, Polymyxin Acylase, gave deacyl brevistinic acid. Cleavage reaction with N-bromosuccinimide, sequential analysis by EDMAN degradation and some additional evidences clarified the total structure of brevistin.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. XIII
JUN'ICHI SHOJI, RYUZI SAKAZAKI, YOSHIHARU WAKISAKA, KENZO KOIZUMI, MIK ...
1976 Volume 29 Issue 4 Pages
390-393
Published: 1976
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A new antibiotic, named laterosporamine, was isolated from the culture broth of
Bacillus laterosporus 340-19. The antibiotic is active against Gram-positive and Gram-negative bacteria
in vitro and
in vivo. It is a water-soluble basic substance, positive to ninhydrin, SAKAGUCHI's and DRAGENDORFF's reagents. A non-peptidic structure with an approximate empirical formula C
17H
35N
7O
4 was suggested.
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D. H. BERG, R. P. MASSING, M. M. HOEHN, L. D. BOECK, R. L. HAMILL
1976 Volume 29 Issue 4 Pages
394-397
Published: 1976
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A new antibiotic, designated A30641, having
in vitro activity against Gram-positive bacteria and fungi has been isolated from a strain of
Aspergillus tamarii. Chemical and physical characterization indicate that it is a member of the class of antibiotics containing the epidithiodiketopiperazine moiety.
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TADASHI ARAI, KATSUKIYO YAZAWA, YUZURU MIKAMI, AKINORI KUBO, KATSUHIRO ...
1976 Volume 29 Issue 4 Pages
398-407
Published: 1976
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Under novel conditions of culture,
Streptomyces lavendulae No. 314 was found to produce new antibiotics, chlorocarcins and mimosamycin in addition to streptothricin. The antibiotics are extracted from culture filtrate with organic solvents and further purified by silica gel chromatography. Chlorocarcins A, B, and C are closely related basic antibiotics which are active against gram-positive bacteria, EHRLICH carcinoma and L 1210 leukemia of mice. Mimosamycin is a neutral antibiotic which is mainly active against mycobacteria. Production, isolation and physicochemical properties of the antibiotics are described.
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YUZURU MIKAMI, KOJI YOKOYAMA, AKIRA ÔMI, TADASHI ARAI
1976 Volume 29 Issue 4 Pages
408-414
Published: 1976
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A strain of
Streptomyces, No. 314 identified as a
Streptomyces lavendulae produced under a novel condition of culture, four new antibiotics, mimosamycin and chlorocarcins A, B, and C. Among the components of chlorocarcin complex, chlorocarcin A was found to be most biologically active. This antibiotic inhibited the growth of
Staphylococcus aureus FDA 209P and
Corynebacterium diphtheriae at the concentrations of 0.1 and 0.003 mcg/ml, respectively. Chlorocarcin A also exhibited antitumor activity on EHRLICH carcinoma, ascitic and solid forms, and mouse leukemia L1210. Mimosamycin proved to be mainly active on
Mycobacterium tuberculosis and inactive on the experimental murine tumors.
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TOSHIAKI YAMASHITA, NORIYUKI NAOI, KIYOSHI WATANABE, TOMIO TAKEUCHI, H ...
1976 Volume 29 Issue 4 Pages
415-423
Published: 1976
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The antitumor polypeptide, macromomycin (MCR) produced by
Streptomyces macromomyceticus, was purified by ammonium sulfate precipitation, ultrafiltration and chromatographic techniques using Amberlite IRA-410, DEAE Sephadex A-25 (Cl
- and OH
- type) and Sephadex G-50. Purified MCR was obtained as a white powder by lyophilization. MCR, thus purified, exhibited a single peak on Sephadex G-50 chromatography
with no detectable contaminant by ultracentrifugation and polyacrylamide gel electrophoresis. MCR is an acidic polypeptide having an isoelectric point of pH 5.4. It contains no arginine and methionine. The molecular weight was 11, 700, 12, 500 and 11, 400 by amino acid composition, gel filtration and analytical ultracentrifugation, respectively. MCR is labile as a lyophilized powder but is successfully stabilized by the addition of maltose.
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MICHAEL O. CHANEY, NOEL D. JONES, MANUEL DEBONO
1976 Volume 29 Issue 4 Pages
424-427
Published: 1976
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The crystal and molecular structures of the calcium complex of A23187 has been determined by X-ray diffraction studies.
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FURTHER CHARACTERIZATION AND C-TERMINAL STRUCTURE OF ACTINOCARCIN
TSUYOSHI KIHARA, SABURO SUZUKI, HIROSHI YONEHARA
1976 Volume 29 Issue 4 Pages
428-432
Published: 1976
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The amino-acid composition and molecular weight of actinocarcin, and C-terminal structure of actinocarcin are reported in this paper. By STEIN-MOORE'S and ultraviolet-absorption methods, the molar ratio of amino acids in actinocarcin was determined. The N-terminal amino acids are alanine and valine. The C-terminal amino acid, determined by hydrazinolysis, is tryptophan. The molecular weight is about 11, 000 as estimated by ARCHIBALD'S method and amino acid analysis. Three fragments, named BrCN-I, BrCN-II and BrCN-III, were obtained by cyanogen bromide cleavage. The structure of BrCN-III, namely the C-terminal structure of actinocarcin was determined by EDMAN degradation
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B. MEESSCHAERT, P. ADRIAENS, H. EYSSEN, E. ROETS, H. VANDERHAEGHE
1976 Volume 29 Issue 4 Pages
433-437
Published: 1976
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The synthesis of benzylpenicillin and 6-aminopenicillanic acid, labeled with tritium in the β-methyl group, is described. Benzylpenicillin S-sulfoxide benzyl ester is refluxed in benzene and tritiated water and is successively debenzylated and deoxygenated to (β-methyl-
3H)-benzylpenicillin. Removal of the side chain with a bacterial acylase gives (β-methyl-
3H)-6-aminopenicillanic acid.
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NOBUO MONJI, WITOLD MECHLINSKI, CARL P. SCHAFFNER
1976 Volume 29 Issue 4 Pages
438-443
Published: 1976
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Amphotericin B-
3H with a specific radioactivity in excess of 4 μCi/mg was produced by fermentation of
Streptomyces nodosus IMRU 3694 in a complex medium, using acetate-
3H as a precursor. The medium employed gave a production yield of 2.5-3.5 mg/ml of amphotericin B. The most efficient incorporation of acetate-
3H occurred when the precursor was added at 24 hours after inoculation. It was observed, that the amount of amphotericin A co-produced in the fermentation broth with amphotericin B was significantly reduced by the addition of ethanol to the production medium. Complete inhibition of amphotericin A production was achieved at a level of 2% ethanol in the fermentation medium without an appreciable effect on the yield of amphotericin B. Methanol, 1-propanol, 2-propanol and 1-butanol lowered the yield of both antibiotics indiscriminately. The syntheses of amphotericin B-
3H-Na desoxycholate (carboxyl-
14C) complex and amphotericin B-
3H methyl
14C-ester are also described.
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MINORU NISHIDA, TAKEO MURAKAWA, TOSHIAKI KAMIMURA, NAOHIKO OKADA, HIRO ...
1976 Volume 29 Issue 4 Pages
444-459
Published: 1976
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FR10612, like cephalexin, is a broad-spectrum oral cephalosporin derivative. The antimicrobial activity of FR10612 against clinical isolates was similar to cephalexin; however, at a low inoculum size its activity was greater than cephalexin against
Klebsiella pneumonia and
Proteus mirabilis strains. Like cephalexin, the
in vitro bactericidal activity of FR10612 was more influenced by the duration of contact with the test organism than by drug concentration. The bactericidal activity of FR10612 against
E. coli 317 was greater than that of cephalexin in an
in vitro model system which simulated the serum levels of FR10612 and cephalexin achieved in healthy volunteers after a single oral dose. The protein binding of FR10612 to human and animal serum was extremely low. FR10612 was resistant to β-lactamases from gram-negative bacilli. It showed resistance similar to cephalexin, but was more resistant to β-lactamases than were cephaloridine, cephalothin and cefazolin. The protective effect of FR10612 in mice infected with various pathogens was greater than cephalexin. The serum levels of FR10612 in rats were higher and more prolonged than those of cephalexin. Tissue levels of FR10612 in rats also persisted for a long time period reflecting the serum levels. In healthy volunteers, rabbits and monkeys the serum levels of FR10612 were initially lower than those of cephalexin but persisted for a longer time period. The total 24-hour urinary excretion of FR10612 in healthy volunteers after oral administration was almost the same as that of cephalexin, but the excretion rate of FR10612 was slower, and the urinary levels were more persistent than those of cephalexin.
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J. A. YURCHENCO, M. W. HOPPER, T. D. VINCE, G. H. WARREN
1976 Volume 29 Issue 4 Pages
460-465
Published: 1976
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The therapeutic properties of nafcillin, oxacillin and erythromycin were determined in mice infected with a strain (Evans) of
Staphylococcus aureus shown to be tolerant to the bactericidal action of penicillinase-resistant derivatives of penicillin. The therapeutic activity of these agents was also correlated with the extent of colonization of kidneys by resistant clones of
S. aureus Evans. The CD
50 values or potency ratios proved that nafcillin was highly active against this organism, whereas oxacillin and erythromycin were capable of protecting the animals to a lesser degree . Of the agents studied, only nafcillin was capable of preventing or interfering with the colonization of the kidneys by
S. aureus Evans. Although the exact interpretation and application of these data in the management of clinical problems remains to be determined, the observations suggest important differences between nafcillin and oxacillin
in vivo and that it is difficult to predict the antibacterial efficacy of these drugs solely from MIC and MBC data.
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GIANCARLO LANCINI, GIUSEPPE SARTORI
1976 Volume 29 Issue 4 Pages
466-468
Published: 1976
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M. G. BRAZHNIKOVA, V. B. ZBARSKY, D. TRESSELT, K. ECKARDT
1976 Volume 29 Issue 4 Pages
469-471
Published: 1976
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VINCE POZSGAY, JÓZSEF TAMÁS, GÁBOR CZIRA, TONI WI ...
1976 Volume 29 Issue 4 Pages
472-476
Published: 1976
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SATOSHI OMURA, TAKAAKI NISHIKIORI, RUIKO OIWA, YUZURU IWAI, ROKUROU MA ...
1976 Volume 29 Issue 4 Pages
477-478
Published: 1976
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YASUHIRO SUMINO, SHUN-ICHI AKIYAMA, KONOMI HAIBARA, MITSUKO ASAI, KOME ...
1976 Volume 29 Issue 4 Pages
479-482
Published: 1976
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