Vézina C, Kudelski A, Sehgal S N
J Antibiot (Tokyo). 1975 Oct;28(10):721-6. doi: 10.7164/antibiotics.28.721.
A streptomycete was isolated from an Easter Island soil sample and found to inhibit Candida albicans, Microsporum gypseum and Trichophyton granulosum. The antibiotic-producing microorganism was characterized and identified as Streptomyces hygroscopicus. The antifungal principle was extracted with organic solvent from the mycelium, isolated in crystalline form and named rapamycin. Rapamycin is mainly active against Candida albicans; minimum inhibitory concentration against ten strains ranged from 0.02 to 0.2 mug/ml. Its apparent activity against Microsporum gypseum and Trichophyton granulosum is lower because of its instability in culture media on prolonged incubation required by these fungi. No activity was observed against gram-positive and gram-negative bacteria. Acute toxicity in mice is low.
从复活节岛土壤样本中分离出一种链霉菌，发现它能抑制白色念珠菌、石膏样小孢子菌和颗粒状毛癣菌。对产生抗生素的微生物进行了表征，并鉴定为吸水链霉菌。抗真菌成分用有机溶剂从菌丝体中提取，分离成晶体形式，命名为雷帕霉素。雷帕霉素主要对白色念珠菌有活性；对10个菌株的最低抑菌浓度范围为0.02至0.2微克/毫升。由于其在这些真菌所需的长时间培养的培养基中不稳定，它对石膏样小孢子菌和颗粒状毛癣菌的明显活性较低。未观察到对革兰氏阳性菌和革兰氏阴性菌的活性。小鼠急性毒性较低。
