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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Antifungal activities of rapamycin and its derivatives, prolylrapamycin, 32-desmethylrapamycin, and 32-desmethoxyrapamycin
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Antifungal activities of rapamycin and its derivatives, prolylrapamycin, 32-desmethylrapamycin, and 32-desmethoxyrapamycin

机译：雷帕霉素及其衍生物，前雷帕霉素，32-去甲基雷帕霉素和32-去甲氧基雷帕霉素的抗真菌活性

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摘要

The antifungal agent rapamycin is highly effective in inhibiting growth of yeast and mold strains. This study demonstrates that in liquid medium, rapamycin is more active than its derivatives (prolylrapamycin, 32-desmethylrapamycin, 32-desmethoxyrapamycin) against Candida albicans, Saccharomyces cerevisiae, and Fusarium oxysporum. All the rapamycins were more active than amphotericin B. Although four other molds were not inhibited in liquid medium, they were very sensitive to rapamycin and its derivatives when tested on agar. The latter assay showed that rapamycin is the most active and 32-desmethylrapamycin is more active than prolylrapamycin and 32-desmethoxyrapamycin. The conclusion of this study is that rapamycin is the most active antifungal agent of the compounds examined. The unexpected finding of high activity of rapamycin and its derivatives against filamentous fungi when assayed by the agar diffusion assay suggests that rapamycin or a derivative may hold promise for chemotherapy against pathogenic molds as well as yeasts. [References: 7]
机译：抗真菌药雷帕霉素对抑制酵母和霉菌菌株的生长非常有效。这项研究表明，在液体培养基中，雷帕霉素比其衍生物（脯氨酰雷帕霉素，32-去甲基雷帕霉素，32-去甲氧基雷帕霉素）对白色念珠菌，酿酒酵母和尖孢镰刀菌的活性更高。所有雷帕霉素都比两性霉素B更具活性。尽管在液体培养基中没有抑制其他四个霉菌，但在琼脂上测试时，它们对雷帕霉素及其衍生物非常敏感。后一种测定法显示雷帕霉素的活性最高，而32-去甲基雷帕霉素的活性高于脯氨酰雷帕霉素和32-去甲氧基雷帕霉素。这项研究的结论是雷帕霉素是所研究化合物中活性最高的抗真菌剂。当通过琼脂扩散测定法测定时，雷帕霉素及其衍生物对丝状真菌的高活性的出乎意料的发现表明，雷帕霉素或其衍生物可能对针对病原性霉菌和酵母的化学疗法具有前景。 [参考：7]

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