巻号一覧
37 巻, 3 号
選択された号の論文の17件中1～17を表示しています
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I. PRODUCTION, ISOLATION AND PROPERTIESMASATAKA KONISHI, MASAMI HATORI, KOJI TOMITA, MASARU SUGAWARA, CHIHARU ...1984 年 37 巻 3 号 p. 191-199
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーChicamycin is a new antitumor antibiotic produced by a strain of Streptomyces albus, No. J576-99. The antibiotic is extractable into organic solvents from the fermentation broth and is obtained in two active forms, chicamycins A and B, depending upon the isolation procedure used. Chicamycin A is not a natural antibiotic but the methanol adduct of naturally produced chicamycin B. Both forms of the antibiotic have weak antibacterial activity against some Gram-positive and acid-fast bacteria. They inhibit the growth of experimental tumors such as P388 mouse leukemia.抄録全体を表示PDF形式でダウンロード (3714K) -
II. STRUCTURE DETERMINATION OF CHICAMYCINS A AND BMASATAKA KONISHI, HIROAKI OHKUMA, NOBUAKI NARUSE, HIROSHI KAWAGUCHI1984 年 37 巻 3 号 p. 200-206
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーStructures of chicamycins A and B have been determined from a series of chemical degradation studies coupled with spectroscopic analysis. Chicamycin A is 2(S), 11(R), 11a(S)-1, 2, 3, 10, 11, 11a-hexahydro-2, 8-dihydroxy-7, 11-dimethoxy-5H-pyrrolo-[2, 1-c][1, 4]-benzodiazepin-5-one, and chicamycin B is 2(S), 11a(S)-1, 2, 3, 11a-tetrahydro-2, 8-dihydroxy-7-methoxy-5H-pyrrolo-[2, 1-c][1, 4]-benzodiazepin-5-one which is the demethanol form of chicamycin A. The structure of chicamycin B is closely related to that of neothramycin, differing only in the position of a hydroxyl substituent on the pyrrolidine ring.抄録全体を表示PDF形式でダウンロード (3098K) -
FERMENTATION, ISOLATION AND CHARACTERIZATIONLOUIS CHAIET, BYRON H. ARISON, RICHARD L. MONAGHAN, JAMES P. SPRINGER, ...1984 年 37 巻 3 号 p. 207-210
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーA new unsaturated glutamic acid analog, 4-amino-3-chloro-2-pentenedioic acid (ACPA) was isolated from a fermentation broth produced by a strain of Streptomyces. ACPA has a very narrow antibacterial spectrum, which is virtually limited to Micrococcus luteus.抄録全体を表示PDF形式でダウンロード (1598K) -
TAKEO YOSHIOKA, AZUMA WATANABE, IKUO KOJIMA, YASUTAKA SHIMAUCHI, MITSU ...1984 年 37 巻 3 号 p. 211-217
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーThe structures and stereochemistry of OA-6129D and E, new carbapenam compounds produced by Streptomyces sp. OA-6129, were determined by spectroscopic analysis and chemical transformation.抄録全体を表示PDF形式でダウンロード (3611K) -
YUKIMASA NOZAKI, SETSUO HARADA, KAZUAKI KITANO, AKIRA IMADA1984 年 37 巻 3 号 p. 218-226
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーThe antibacterial activities of twelve 5, 6-cis carbapenem antibiotics, including four semisynthetic derivatives of C-19393 H2 and S2, against 15 microorganisms were examined, and their structure-activity relations are discussed in relation to minimum inhibitory concentrations against Staphylococcus aureus and Escherichia coli as a Gram-positive and a Gram-negative standard strain, respectively. The contribution of chromosomal β-lactamase (amp C), permeability barrier, and penicillin-binding protein (PBP) 1B to the resistance of E. coli to these carbapenem antibiotics was examined using mutants lacking each of these cellular components.抄録全体を表示PDF形式でダウンロード (4300K) -
A COMPUTER GRAPHICS STUDYDONALD B. BOYD1984 年 37 巻 3 号 p. 227-234
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーAnalysis of X-ray crystallographic data for cephalosporins and 1-oxacephalosporins shows that, although the 1-methyl-1H-tetrazol-5-ylthiomethyl side chain at position 3 of a bicyclic β-lactam nucleus has certain conformational preferences, it also has considerable flexibility. Both the C4=C3-C3'-S and C3-C3'-S-C5″ torsional angles are frequently observed in the vicinity of ±90°. The distance between the tetrazole ring carbon C5″ and the 4-carboxyl carbon ranges from 4.07 to 5.65 Â. Mean bond lengths and bond angles for the 3 and 4 side chains are tabulated.抄録全体を表示PDF形式でダウンロード (3527K) -
MIEKO TAKEUCHI, YOSHIO SATO, KAZUO NITTA1984 年 37 巻 3 号 p. 235-238
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーAn efficient in vitro screening method for antitumor and/or antitumorigenic substances was established. The method is based on determining inhibitory effect of a compound on an RSV-induced tumorigenic process and the growth of the established tumor cells in a single assay system in the presence of normal cells. These effects were determined by inhibition of focus formation in a culture of chick embryo fibroblasts, while the nonspecific cytotoxic effect was determined by inhibition of the protein content of the same culture. The efficiency of this method in screening drugs was confirmed by testing various clinical and preclinical compounds.抄録全体を表示PDF形式でダウンロード (1918K) -
W. E. G. MÜLLER, R. K. ZAHN, A. MAIDHOF, H. C. SCHRÖDER, M. ...1984 年 37 巻 3 号 p. 239-243
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーStudying the treatment of NMRI mice with ip injections of bleomycin (BLM) for 5 days we found an approximate LD50 of 35 mg/kg; the toxicity of peplomycin (PEP) was slightly higher (LD50: approximately 25 mg/kg). The effect of the two drugs on growth of L5178y mouse lymphoma cells in NMRI mice was examined. BLM alone caused at a concentration of 2.5 mg/kg an almost complete inhibition of tumor cell growth; the same effect was determined with 1 mg PEP/kg. At these concentrations the drugs caused an increase of the survival time of 110% (BLM) or 104% (PEP). Given in combination, one-sixth of the optimal doses yielded an 100% increase of the median survival time. These results indicate a significant synergistic activity of the PEP-BLM combination on L5178y cell growth in vivo (FIC index: 0.34).抄録全体を表示PDF形式でダウンロード (2340K) -
NORIAKI INAMURA, TAKASHI FUJITSU, KUNIO NAKAHARA, MICHIYO ABIKO, YOKO ...1984 年 37 巻 3 号 p. 244-252
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーIntraperitoneal injection of squalene-treated cell wall skeleton of Nocardia rubra (N-CWS) caused increase in number of peritoneal exudate cells (PEC). Adherent macrophages obtained from N-CWS-treated PEC suppressed growth of methylcholanthrene-induced fibrosarcoma (Meth-A), when injected intradermally with the tumor cells into BALB/c mice. The macrophages showed strong cytotoxicity against Meth-A cells in vitro. When treated with 10 μg/ml of N-CWS in vitro, proteose peptone-induced macrophages acquired tumoricidal property but resident macrophages showed no cytotoxicity after the treatment. In the supernatant of spleen cells cultured for 72 hours in the presence of N-CWS (10 μg/ml), the presence of (a) factor(s) with macrophage activating effect was observed. This factor, shown to be identical to macrophage activating factor (MAF) in molecular weight, showed synergy with N-CWS in potentiating macrophage cytotoxicity against tumor cells.抄録全体を表示PDF形式でダウンロード (4870K) -
PETER H. CALCOTT, RAYMOND O. FATIG, III1984 年 37 巻 3 号 p. 253-259
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーAvermectin inhibits Mucor miehei and Artemia salina chitin synthesis and to a degree DNA synthesis in the former. The antibiotic interferes with chitin turnover in brine shrimp and inhibits Streptomyces antibioticus chitinase activity in vitro. In light of the proposed mode of action of avermectin and the anomolies in the literature, it is proposed that avermectin can kill susceptible organisms not only by a neurotoxic mechanism but also by inhibiting chitin turnover and synthesis at low concentration and thus the molting/ecdysis process.抄録全体を表示PDF形式でダウンロード (3453K) -
MAKOTO HORI, KYOKO NAITO, NOBUO SAKATA, YOSHIMASA UEHARA, HAMAO UMEZAW ...1984 年 37 巻 3 号 p. 260-266
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーGrowth of Escherichia coli in a nutrient medium was inhibited by 100 μg/ml of clazamycin and at this concentration, the viable cell number decreases slowly. Elongated cells were observed in the treated cultures. The bactericidal activity was abolished by high concentrations of either sucrose or sorbitol but not by chloramphenicol. Non-growing cells suspended in a medium devoid of both carbon and nitrogen sources were killed by clazamycin more rapidly than cells in a rich medium. Incorporation of radioactive thymidine, uridine, leucine and N-acetylglucosamine into cellular macromolecules was inhibited to a similar extent. Permeability of N-acetylglucosamine and leucine was blocked by clazamycin. On the other hand, membrane transport of thymidine was only slightly inhibited. Thymidine-derived radioactivity accumulated as dTTP in the cells suggesting that DNA synthesis was blocked at the polymerization step. DNA synthesis in toluene-treated cells was also sensitive to clazamycin while the repair DNA synthesis induced by bleomycin in these cells was not. DNA-repair deficient mutants of E. coli were as sensitive to clazamycin as their DNA-repair proficient counterparts.抄録全体を表示PDF形式でダウンロード (3687K) -
GARY D. GRAY, GRETA M. OHLMANN, CHARLES W. FORD, VINCENT P. MARSHALL1984 年 37 巻 3 号 p. 267-274
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーStudies on the interaction between antibiotics and polymorphonuclear leukocytes (PMLs) usually require the availability of radiolabeled antibiotic, that the antibiotic kill intraleukocyte pathogens, or that the antibiotic affect some function of the leukocyte. The system described here does not have the requirements above but depends instead upon anti-staphylococci activity. The key features of the system are that, following incubation, extracellular antibiotic was removed from PMLs by centrifugation, contact between Staphylococcus aureus 502A and the phagocyte-antibiotic complex was assured by centrifugation at 4°C in 96 well tissue culture dishes, phagocytosis was induced by incubation at 37°C, and assessment of surviving bacteria was accomplished by collecting [3H]thymidine labeled bacteria using a cell harvester. Antibiotics that were active in this system included naphthalenic ansamycins (rifamycins and streptovaricins), lincosaminides (clindamycins and pirlimycins), coumarins (novobiocin), erythromycin, tetracycline, tyrocidine and paulomycin.抄録全体を表示PDF形式でダウンロード (4204K) -
MASAFUMI NAKAO, TAKESHI NISHI, MASAHIRO KONDO, TAKESHI FUGONO, AKIRA I ...1984 年 37 巻 3 号 p. 275-284
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーThe therapeutic effects of seven antipseudomonal β-lactam antibiotics on experimental urinary tract infection caused by Pseudomonas aeruginosa P 9 in mice were compared, and the results were analyzed in relation to their in vitro antibacterial activities and pharmacokinetic properties. The CD50 values were (mg/kg): cefsulodin, 6.19; cefoperazone, 162; sulbenicillin, 167; ticarcillin, 184; azlocillin, 121; mezlocillin, 390; and piperacillin, 227. Cefsulodin was more active than the other antibiotics not only in therapeutic effects but also in in vitro antibacterial effects evaluated according to growth inhibitory, bactericidal, and bacteriolytic activities. It also penetrated and persisted well in the kidney of mice. The therapeutic effects of cefoperazone, azlocillin, and piperacillin were much less than expected from their in vitro antibacterial activities; the CD50 values were more than 18-fold as large as that of cefsulodin, whereas the differences of their MIC values were less than four-fold.抄録全体を表示PDF形式でダウンロード (4572K) -
A. S. NAVARRO, J. M. LANAO, A. DOMINGUEZ-GIL1984 年 37 巻 3 号 p. 285-292
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーA study was made of the serum levels and of the pharmacokinetic parameters of dibekacin after administration by intravenous infusion at a dose of 2 mg/kg of the drug to rabbits using different infusion times. The peak serum level (Cmax) was seen to decrease progressively on increasing infusion time. The maximum value of Cmax was obtained after administration of the antibiotic by single bolus injection with an average value of 18.297±9.694μg/ml, while the minimum value was obtained after intravenous infusion over 1 hour, with an average value of 6.597±1.250μg/ml. A series of linear relationships was established between different pharmacokinetic parameters and the infusion time and a decrease was observed in the pharmacokinetic parameters α, K12, K21 and K13 when the infusion time was increased. Changes were also observed in the distribution kinetics of dibekacin in the rabbit on varying the infusion conditions, suggesting alterations in the access and permanence of the antibiotic in tissues.抄録全体を表示PDF形式でダウンロード (3858K) -
MASATOMO FUKASAWA, HIROSHI NOGUCHI, SUSUMU MITSUHASHI, FUMITOSHI ISHIN ...1984 年 37 巻 3 号 p. 293-296
発行日: 1984年
公開日: 2006/04/19
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MICHAEL J. DRIVER, PETER H. BENTLEY, RONALD A. DIXON, ROBERT A. EDMOND ...1984 年 37 巻 3 号 p. 297-299
発行日: 1984年
公開日: 2006/04/19
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A NEW PYRROLO[1, 4]BENZODIAZEPINE ANTITUMOR AGENTT. KANEKO, H. WONG, T. W. DOYLE1984 年 37 巻 3 号 p. 300-302
発行日: 1984年
公開日: 2006/04/19
ジャーナル フリーPDF形式でダウンロード (1223K)
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