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FERMENTATION, ISOLATION, STRUCTURE DETERMINATION AND BIOLOGICAL ACTIVITIES
MAY D. LEE, AMEDEO A. FANTINI, NYDIA A. KUCK, MICHAEL GREENSTEIN, RAYM ...
1987 年 40 巻 12 号 p.
1657-1663
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The LL-D05139 complex, containing LL-D05139β and azaserine, was recovered from the fermentation filtrate of
Glycomyces harbinensis (NRRL 15337). A chemically defined medium was developed which favored the production of LL-D05139β. Antibiotic LL-D05139β was isolated from the fermentation filtrate by adsorption on granular carbon and further purified by chromatography on microcrystalline cellulose. Acid hydrolysis of LL-D05139β gave one molar equivalent each of alanine and serine. Both amino acids were found to have the L-configuration by GC analysis on a chiral column and alanine was assigned to be the
N-terminal amino acid by Edman degradation. This information coupled with IR, UV,
1H NMR,
13C NMR and MS spectral data allowed us to assign the structure of LL-D05139β as alanylazaserine. LL-D05139β demonstrated greater antibacterial and biochemical induction assay activities than azaserine. The two drugs showed similar antitumor activities.
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I. TAXONOMY OF THE PRODUCING ORGANISM, ISOLATION AND BIOLOGICAL PROPERTIES
TOSHIYUKI KAMEYAMA, ATSUSHI TAKAHASHI, SHOGO KURASAWA, MASAAKI ISHIZUK ...
1987 年 40 巻 12 号 p.
1664-1670
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Alteromonas haloplanktis strain SB-1123 isolated from deep-sea mud produced a new siderophore, bisucaberin. Bisucaberin rendered tumor cells susceptible to cytolysis mediated by murine peritoneal macrophages which were elicited by Proteose peptone and not yet activated by lymphokine. Bisucaberin exerted its sensitizing activity by both the preincubation with tumor cells and the addition to co-culture of macrophages and tumor cells. The activity of bisucaberin was specifically inhibited by ferric ion. Bisucaberin showed direct cytostasis for tumor cells but did not cause cytolysis in the absence of macrophages. Cytostasis by bisucaberin was attributable to the specific inhibition of DNA synthesis in tumor cells.
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II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE DETERMINATION
ATSUSHI TAKAHASHI, HIKARU NAKAMURA, TOSHIYUKI KAMEYAMA, SHOGO KURASAWA ...
1987 年 40 巻 12 号 p.
1671-1676
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The structure of bisucaberin, a new siderophore, was determined to be 1, 12-dihydroxyl, 6, 12, 17-tetraazacyclodocosane-2, 5, 13, 16-tetrone by spectroscopic analysis and X-ray crystallographic analysis. The molecule of bisucaberin consists of a cyclic dimer of 1-hydroxyl, 6-diazaundecane-2, 5-dione moiety and is closely related to nocardamine, the trimer of the same moiety.
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I. PRODUCTION, TAXONOMY AND ANTIBACTERIAL ACTIVITY
SHELDON B. ZIMMERMAN, CHERYL D. SCHWARTZ, RICHARD L. MONAGHAN, BARBARA ...
1987 年 40 巻 12 号 p.
1677-1681
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Difficidin and oxydifficidin, two novel macrocyclic polyene lactone phosphate esters were discovered in fermentation broths of each of two strains of
Bacillus subtilis: ATCC 39320 and ATCC 39374. Difficidin and oxydifficidin each showed a broad spectrum of activity against aerobic and anaerobic bacteria. Many of the susceptible aerobes and anaerobes were human pathogens resistant to one or more antibiotics. Difficidin and oxydifficidin when administered intraperitoneally protected mice against an otherwise lethal bacteremia caused by
Klebsiella pneumoniae (ED
50 in mg/kg of 1.31 and 15.6 respectively). Neither difficidin nor oxydifficidin were effective when administered via the subcutaneous route.
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II. ISOLATION AND PHYSICO-CHEMICAL CHARACTERIZATION
KENNETH E. WILSON, JAMES E. FLOR, ROBERT E. SCHWARTZ, HENRY JOSHUA, JA ...
1987 年 40 巻 12 号 p.
1682-1691
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The isolation of difficidin (
1) and oxydifficidin (
2) from fermentation broth of
Bacillus subtilis ATCC 39320 and the physico-chemical characterization of these labile antibiotics are described. The structures of the compounds represent a new class of antibiotics, characterized as highly unsaturated 22-membered macrolide phosphates. Difficidin and oxydifficidin undergo reversible thermal isomerization to
3 and
4 respectively. Biological evaluation of the isomers is presented.
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III. MODE OF ACTION OF DIFFICIDIN
MARCIA M. ZWEERINK, ANN EDISON
1987 年 40 巻 12 号 p.
1692-1697
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The mode of action of difficidin (DIF) was investigated. Upon addition of DIF to log phase cultures of
Escherichia coli, growth ceased immediately and small round cells accumulated after 30 minutes incubation. No cell lysis was observed. DIF was rapidly bactericidal to both growing and stationary phase cultures, and inhibited protein synthesis more rapidly than RNA, DNA, or cell-wall synthesis in growing cells. Protein synthesis was also inhibited in a cell-free system. The frequency of natural mutation to resistance in
E. coli was less than 1 in 10
10 cells.
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YUTAKA KIDO, TAROU FURUIE, KEITAROU SUZUKI, KYOKO SAKAMOTO, YOSHITO YO ...
1987 年 40 巻 12 号 p.
1698-1706
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
A streptothricin-like antibiotic, A-269A (referred to as A-269A hereafter) was isolated from the culture broth of
Streptomyces sp., strain No. A-269. In this paper, the characterization of the producer, and the production, isolation, physico-chemical properties and biological properties of A-269 A are reported. The structure of the antibiotic was also examined by
1H NMR,
13C NMR and fast atom bombardment mass spectra studies. From the spectroscopic data, A-269A was assumed to be a mixture of antibiotic LL-BL 136 and an isomeric compound in which the carbamoyl group is substituted on C-12' hydroxyl instead of C-10 hydroxyl.
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CHOUNG UN KIM, PETER F. MISCO, BING Y. LUH, MICHAEL J. M. HITCHCOCK
1987 年 40 巻 12 号 p.
1707-1715
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The synthesis of new carbapenems having various (substituted) quaternary heterocyclic alkylthio groups at the C-2 position is described. The
in vitro antibacterial activity and the dehydropeptidase-I susceptibility were examined. Some of these compounds (
e.g.,
11,
16,
26 and
27) showed an excellent wide spectrum of
in vitro antibacterial activity including activity against
Pseudomonas aeruginosa and greater stability than imipenem toward the dehydropeptidase-I.
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HARUO YAMASHITA, NOBUYOSHI MINAMI, KYOICHI SAKAKIBARA, SUSUMU KOBAYASH ...
1987 年 40 巻 12 号 p.
1716-1732
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The synthesis and antibacterial activity of sodium (3
S, 4
R)-3-[2-(2-aminothiazol-4-yl)-(
Z)-2-(
O-substituted oxyimmo)acetamido]-2-azetidinone-1-sulfonates having various substituted ethyl groups at the C-4 position are described. Among various substituents explored, the (substituted isothiuronio)ethyl groups were found to have strong antibacterial activity against a variety of Gram-negative bacteria, and moreover, the ethylene isothiuronium derivative exhibited moderate antibacterial activity against
Staphylococcus aureus.
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W. WEHRLI, W. ZIMMERMANN, W. KUMP, W. TOSCH, W. VISCHER, O. ZAK
1987 年 40 巻 12 号 p.
1733-1739
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
CGP 4832 (
5) is a new derivative of rifamycin S, showing a very high degree of activity against certain Gram-negative bacteria, with MICs as much as 400 times lower than those of rifampicin. CGP 4832 and rifampicin inhibit DNA-dependent transcription
in vitro to a similar extent, which excludes any difference in their effect on the target enzyme. The most plausible explanation for the potent activity of CGP 4832 is that it penetrates into bacterial cells by way of a specific mechanism. This hypothesis is corroborated by the high rate of mutations leading to bacterial strains resistant against CGP 4832.
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KAZURO SHIOMI, HIRONOBU IINUMA, HIROSHI NAGANAWA, KUNIO ISSHIKI, TOMIO ...
1987 年 40 巻 12 号 p.
1740-1745
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Biosynthetic studies on napyradiomycins were carried out based on the incorporation of [2-
13C]acetate and [1, 2-
13C]acetate. The alignment of acetate units suggested that the B and C rings of napyradiomycins are derived from a pentaketide, while ring A and the side chain may be synthesized from rnevalonate.
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JINYOU ZHANG, SAUL WOLFE, ARNOLD L. DEMAIN
1987 年 40 巻 12 号 p.
1746-1750
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Cephalosporin production by
Cephalosporium acremonium strain C-10 was suppressed when the organic nitrogen source (1.2% L-asparagine) was replaced by 1.2% (NH
4)
2SO
4. A higher level of (NH
4)
2SO
4 (3.5%) led to even greater suppression. Ammonium repression was exerted on formation of δ(L-α-aminoadipyl)-L-cysteinyl-D-valine (ACV) synthetase, together with that of expandase; a lesser effect by ammonium was observed on cyclase production. Inhibition of ACV synthetase activity byammonium was also observed (
ca. 50% inhibition at250mMNH
4+).
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PENELOPE J. B. SOMERS, RAYMOND C. YAO, LAWRENCE E. DOOLIN, MICHAEL J. ...
1987 年 40 巻 12 号 p.
1751-1756
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
A new method of screening for chitinase inhibitors in crude fermentation broths as a means of discovering new insecticidal leads has been developed. In this procedure soluble Remazol brilliant violet 5R dye-coupled chitin degradation products released from insoluble chitin azure substrate by hydrolysis with
Streptomyces griseus chitinase are filtered in 0.45 μm Millititer HA 96 well filtration plates and collected in 96 well microtiter plates. Inhibitors of this reaction are detected by a decrease in absorbance (570 nm) of the filtrate. A chitinase inhibitor, designated A82516, produced by culture A82516 was discovered using this screen. Purified A82516 was found to have an IC
50 of 3.7×10
-6 M for
S. griseus chitinase. At a test concentration of 0.27 mg/ml, A82516 was 100% effective in preventing development of house fly larvae to pupae. Allosamidin, a recently reported chitinase inhibitor
in vitro, has spectral properties identical to A82516.
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DIDIER C. FAUCHER, YVES LELIÉVRE, TERENCE CARTWRIGHT
1987 年 40 巻 12 号 p.
1757-1761
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Anti-collagenase activity was detected in the culture supernatant of an Actinomycete strain
S 4373. The molecule was purified by solvent extraction, medium pressure and high pressure reverse phase chromatography and finally by HPLC gel filtration. The pure product was analyzed by mass spectroscopy and was identified as actinonin, a known pseudopeptide antibiotic. The
Ki was determined as 1.4 μM and this value was confirmed using pure synthetic actinonin.
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M. LIMBERT, D. ISERT, N. KLESEL, C. MEICHSNER, G. SEIBERT, E. SCHRINNE ...
1987 年 40 巻 12 号 p.
1762-1767
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
Cefotaxime (CTX) and HRE 664 (a novel penem antibiotic) possess complementary
in vitro properties. Differences can be observed in their antibacterial spectra, their β-lactamase stability and -inhibition, and their affinity to penicillin-binding proteins. These differences suggested that combinations of the cephalosporin and the penem antibiotic would be advantageous and should be studied. The fractional inhibitory concentration values of checkerboard studies confirmed that CTX and HRE 664 act synergistically against various Gram-positive and Gram-negative bacteria. Fixed combinations containing 80% CTX and 20% HRE 664 possess broader antibacterial spectra and in certain cases higher antibacterial activities than each of the components alone. The combinations had improved activity against Staphylococci including methicillin-resistant strains, β-lactamase producing strains of
Enterobacter sp. and
Bacteroides fragilis. The combination as well as the single antibiotics had only limited activity against
Pseudomonas aeruginosa.
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KANKI KOMIYAMA, YUMIKO HIROKAWA, HIROKO YAMAGUCHI, SHINJI FUNAYAMA, KA ...
1987 年 40 巻 12 号 p.
1768-1772
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
The antitumor activity of a novel ansamycin antibiotic, trienomycin A, against various murine tumors was studied with two treatment schedules. The intraperitoneal injection of the antibiotic showed remarkable antitumor activity on sarcoma 180 and P388 leukemia at doses of 160 or 320 mg/kg, showing 151% and 100% increase in life span, respectively.
Trienomycin A inhibited the growth of Ehrlich and Meth A cells
in vitro at doses of 0.1 -0.4 μg/ml when the cells were exposed to the antibiotic for 72 hours. The incorporation of [
3H]thymidine into acid precipitable material in HeLa cells was slightly more marked than that of [
3H]uridine and [
3H]leucine when the cells were exposed to 0.04 or 0.08 μg/ml of trienomycin A for 4 hours. It appeared that trienomycin A showed antitumor activity by direct cytotoxic action.
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ROKURO MASUMA, KAZUKO OKUYAMA, YOSHITAKE TANAKA, RIMIKO HIROSE, HIROSH ...
1987 年 40 巻 12 号 p.
1773-1775
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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SUN HEE KIM, TAKAYOSHI OKABE, NOBUO TANAKA, HIDEO SUZUKI
1987 年 40 巻 12 号 p.
1776-1777
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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KEIKO OOGOSE, YUKIO HAFURI, ERIKO TAKEMORI, ERI NAKATA, YOSHIO INOUYE, ...
1987 年 40 巻 12 号 p.
1778-1781
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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ISAMI TAKAHASHI, EIJI KOBAYASHI, Kozo ASANO, MAYUMI YOSHIDA, HIROFUMI ...
1987 年 40 巻 12 号 p.
1782-1784
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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III. A NEW ISOTETRACENONE ANTIBIOTIC, GRINCAMYCIN
YOICHI HAYAKAWA, TAKAFUMI IWAKIRI, KANJI IMAMURA, HARUO SETP, NOBORU O ...
1987 年 40 巻 12 号 p.
1785-1787
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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NOBUYOSHI SHIMADA, SHIGERU HASEGAWA, SEIICHI SAITO, TAKAAKI NISHIKIORI ...
1987 年 40 巻 12 号 p.
1788-1790
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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I. INACTIVATION MECHANISM
TOYOSHIGE ENDO, KUMIKO FURUTA, AKIYO KANEKO, TOMO KATSUKI, KAORI KOBAY ...
1987 年 40 巻 12 号 p.
1791-1793
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー
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CHIAKI NISHIMURA, TOSHIO NISHIMURA, NOBUO TANAKA, HIDEO SUZUKI
1987 年 40 巻 12 号 p.
1794-1795
発行日: 1987/12/25
公開日: 2006/04/19
ジャーナル
フリー