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目的对1株来源于南海红树林底泥的抗真菌抗生素链霉菌Streptomyces antibioticus No.H 41-51发酵物中的化学成分进行研究。方法对H41-51发酵物菌丝体乙醇提取物进行研究,通过液液分配萃取、硅胶柱、Sephadex LH-20柱层析和HPLC制备方法进行化合物的分离纯化,分离时以白色念珠菌为指示菌采用纸碟片法进行活性追踪;采用NMR、MS等光谱方法,并结合文献数据比对鉴定化合物结构。结果分离得到8个化合物,并分别将其鉴定为3,3-二吲哚-2-羟基-丙醇(1)、dankasterone(2)、4-hydroxy-17R-methylincisterol(3)、Calvasterol B(4)、Calvasterol A(5)、抗霉素A1a(6)、抗霉素A1b(7)和甘油醇-1-单油酸酯(8)。体外活性实验表明:化合物2~5对MCF-7、SF-268和NCI-H460细胞株表现出程度不等的细胞毒活性,化合物6和7表现出抗白色念珠菌活性。结论菌株H41-51发酵可产生多种不同结构类型和生物活性的次生代谢产物。化合物2~5对MCF-7、NCI-H460和SF-268细胞株具有细胞毒活性,化合物6、7具有抗白色念珠菌活性。
OBJECTIVE To study the chemical constituents of an antifungal antibiotic Streptomyces antibioticus No. H 41-51 from the mangrove sediment of the South China Sea. Methods The ethanol extract of mycelium of H41-51 was studied. The compounds were separated and purified by liquid-liquid partition, column chromatography on silica gel, Sephadex LH-20 column and HPLC. Candida albicans was used as an indicator The bacterial activity was tracked by the paper disc method. The structures of the compounds were identified by spectral methods such as NMR and MS, combined with the literature data. Results Eight compounds were isolated and identified as dankasterone (2), 4-hydroxy-17R-methylincisterol (3), Calvasterol B 4), Calvasterol A (5), antimycin A1a (6), antimycin A1b (7) and glycerol-1-monooleate (8). In vitro activity tests showed that compounds 2 to 5 showed varying degrees of cytotoxic activity against MCF-7, SF-268 and NCI-H460 cell lines, and compounds 6 and 7 showed anti-Candida albicans activity. Conclusion Fermentation of strain H41-51 can produce many kinds of secondary metabolites with different structure types and bioactivities. Compounds 2 to 5 have cytotoxic activity against MCF-7, NCI-H460 and SF-268 cell lines, and compounds 6 and 7 have anti-Candida albicans activity.