Ohtsuka K, Watanabe M, Orikasa Y, Inouye S, Uchida K, Yamaguchi H, Kondo S, Takeuchi T
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd, Yokohama, Japan.
J Antimicrob Chemother. 1997 Jan;39(1):71-7. doi: 10.1093/jac/39.1.71.
The in-vivo antifungal activity of benanomicin A administered intravenously or subcutaneously was compared with that of amphotericin B and fluconazole using animal models of systemic infections with Candida albicans, Aspergillus fumigatus and Cryptococcus neoformans. The efficacy of benanomicin A in C. albicans infection was more pronounced when administered in multiple doses than in a single dose. This was also true of fluconazole, but not of amphotericin B, which showed no difference between single and multiple dosings. Benanomcin A eradicated C. albicans cells from the kidneys of infected mice in a manner comparable to that of amphotericin B, but more effectively than fluconazole. The histopathological findings obtained from the kidneys of the C. albicans-infected mice confirmed the therapeutic efficacy of benanomicin A. The subcutaneous ED50 values of benanomicin A were 1.30 mg/kg/day (C. albicans) and 19.0 mg/kg/day (A. fumigatus) which were intermediate between those of amphotericin B and fluconazole in the two models. The subcutaneous ED50 value of benanomicin A for C. neoformans was 21.5 mg/kg/day, which was higher than that of amphotericin B.
使用白色念珠菌、烟曲霉和新型隐球菌系统性感染的动物模型，比较了静脉注射或皮下注射贝纳霉素A与两性霉素B和氟康唑的体内抗真菌活性。在白色念珠菌感染中，贝纳霉素A多次给药时的疗效比单次给药时更显著。氟康唑也是如此，但两性霉素B并非如此，单次给药和多次给药之间没有差异。贝纳霉素A以与两性霉素B相当的方式从感染小鼠的肾脏中清除白色念珠菌细胞，但比氟康唑更有效。从白色念珠菌感染小鼠的肾脏获得的组织病理学结果证实了贝纳霉素A的治疗效果。贝纳霉素A的皮下半数有效剂量（ED50）值在两种模型中分别为1.30mg/kg/天（白色念珠菌）和19.0mg/kg/天（烟曲霉），介于两性霉素B和氟康唑之间。贝纳霉素A对新型隐球菌的皮下ED50值为21.5mg/kg/天，高于两性霉素B。
