微生物来源的免疫抑制活性化合物SIPI-18-1和SIPI-18-2的研究

目的：从微生物代谢产物中筛选和分离新的免疫抑制药物。方法：应用本实验室已经建立的免疫抑制活性体外筛选模型，从几千株放线菌中筛选出十几株免疫抑制活性阳性菌株包括链霉菌SIPI 97-84；通过链霉菌SIPI 97-84的发酵、上清液的乙酸乙酯提取和硅胶柱层析等方法，从其发酵液中分离出免疫抑制活性的化合物SIPI-18-1和SIPI-18-2，并测定化合物的特性和图谱数据及生物学活性。结果：通过理化性质、质谱、紫外、红外和核磁共振等图谱数据的分析，确定SIPI-18-1和SIPI-18-2化合物的结构；生物学活性研究发现SIPI-18-1化合物具有中等强度的免疫抑制活性。结论：链霉菌SIPI 97-84产生的两个活性化合物均属于安沙类抗生素，分别与文献报道的曲张链菌素(Streptovaricin)C和G结构一致；免疫抑制活性属于首次发现。

Studies on the Immunosuppressant SIPI-18-1 and SIPI-18-2 from a Microorganism

AIM:To screen and isolate new immunosuppressant drugs from microorganisms. METHOD: Using the screening model in vitro, more than 10 strains from thousands of actinomycetes are shown to be positive including Streptomyces SIPI97 84; by fermentation, ethyl acetate extraction, silica gel column chromatography etc. Compounds SIPI 18 1 and SIPI 18 2 have been isolated from the broths; the properties and spectra of the compounds were determined and the biological activities were analyzed. RESULT: By the analyses of their physico chemical properties, MS, UV, IR and NMR spectra data, the structures of SIPI 18 1 and SIPI 18 2 have been identified. Besides, SIPI 18 1 showed moderate immunosuppressant activity. CONCLUSION: Compounds SIPI 18 1 and SIPI 18 2 produced by Streptomyces SIPI97 84 were identical as streptovaricin C and G, respectively; the immunosupressant activity of SIPI 18 1 found here is first reported.