Cispentacin, a new antifungal antibiotic. II. In vitro and in vivo antifungal activities.
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- OKI TOSHIKAZU
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- HIRANO MINORU
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- TOMATSU KOZO
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- NUMATA KEI-ICHI
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- KAMEI HIDEO
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
書誌事項
- タイトル別名
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- II. <i>IN VITRO</i> AND <i>IN VIVO</i> ANTIFUNGAL ACTIVITIES
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説明
Cispentacin ((-)-(1R, 2S)-2-aminocyclopentane-l-carboxylic acid) is a new antifungal antibiotic possessing potent anti-Candida activity. The 50% inhibitory concentration (IC50) and IC100 values of cispentacin against clinical isolates of Candida albicans were in the ranges 6.3-12.5 and 6.3-50μg/ml, respectively, by turbidimetric measurement in yeast nitrogen base glucose medium. No significant activity was seen against any yeasts and molds when tested by the agar dilution method using three different agar media; KNOPF'S agar, yeast extract - glucose - peptone agar and Sabouraud dextrose agar. This antibiotic demonstrated good therapeutic efficacy against a systemic Candida infection in mice by both parenteral and po administrations. The 50% protection dose (PD50) values after single iv and po administrations were 10 and 30mg/kg, respectively. It was also effective in a systemic infection with Cryptococcus neoformans and in both lung and vaginal infections with C. albicans in mice. Cispentacin did not induce acute lethal toxicity at 1, 000mg/kg by iv injection and 1, 500mg/kg by ip and po administrations in mice.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 42 (12), 1756-1762, 1989
公益財団法人 日本感染症医薬品協会