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目的研究软珊瑚来源的毛壳属真菌(Cheatomiumsp.)中的活性成分。方法采用多种分离手段对毛壳属真菌的乙酸乙酯提取物进行分离纯化,运用现代波谱技术并结合文献报道数据,鉴定化合物的结构;采用CCK-8方法对化合物的肝癌干细胞增殖抑制活性进行了体外测试。结果分离得到13个已知的麦角甾醇类化合物,其结构分别鉴定为:麦角甾醇(1),(22E,24R)-麦角甾-6,22-二烯-5α,8α-过氧-3β-醇(2),(22E,24R)-麦角甾-5,8(14),22-三烯-3β,15α-二羟基-7-酮(3),(22E,24R)-麦角甾-5,8(14),22-三烯-3β,15β-二羟基-7-酮(4),(22E,24R)-麦角甾-5,8,22-三烯-3β-羟基-7-酮(5),(22E,24R)-麦角甾-7,22-二烯-3β,5α,6α,9α-四醇(6),(22E,24R)-麦角甾-7,22-二烯-5α,6α-环氧-3β-醇(7),麦角甾-7,22-二烯-6β-甲氧基-3β,5α-二醇(8),(22E,24R)-麦角甾-7,22-二烯-3β,5α-二醇-6-酮(9),麦角甾-7,9(11),22-三烯-3β,5α,6α-三醇(10),(22E,24R)-麦角甾-7,22-二烯-3β,5α,6α-三醇(11),(22E,24R)-麦角甾-7,22-二烯-3β,5α,9α-三醇-6-酮(12),(22E,24R)-麦角甾-8,22-二烯-5α,6α-环氧-3β,7α-二醇(13)。在体外活性测试中,化合物3、4、6、8、13对人肝癌Huh7干细胞增殖显示不同程度的抑制活性。结论化合物5~13为首次从该属真菌中分离得到。本文是对麦角甾醇类化合物抑制肿瘤干细胞增殖活性的首次报道。
Objective To study the active ingredient in soft-shelled genus Chaatomium sp. Methods The ethyl acetate extracts of Chaetomium fungi were isolated and purified by a variety of separation methods. The structures of the compounds were identified by modern spectroscopic techniques combined with reported data. The inhibitory activities of the compounds against hepatoma stem cell proliferation were determined by CCK-8 In vitro testing. Results Thirteen known ergosterol compounds were isolated and their structures were identified as ergosterol (1), (22E, 24R) -ergosta-6,22-diene-5α, (22E, 24R) -ergosterol-5,8 (14), 22-trien-3β, 15α-dihydroxy-7- (4), (22E, 24R) -ergosta-5,8,22-trien-3β-hydroxy-7-one (22E, 24R) -ergosta-7,22-diene-3β, 5α, 6α, 9α-tetrol (6), (22E, 24R) 5α, 6α-epoxy-3β-ol (7), ergosta-7,22-diene-6β-methoxy-3β, 5α- diol (8), (22E, 24R) (9), ergost-7,9 (11), 22-triene-3β, 5α, 6α-triol (10), (22E, 24R) -ergosta-7,22-diene-3β, 5α, 6α-triol (11), (22E, 24R) -ergosta-7,22-diene-3β, (12), (22E, 24R) -ergosta-8,22-diene-5α, 6α-epoxy-3β, 7α-diol (13). Compounds 3, 4, 6, 8 and 13 showed different degrees of inhibitory activity on human hepatoma Huh7 stem cell proliferation in in vitro activity test. Conclusion Compounds 5-13 are isolated from this genus for the first time. This article is the first report on the inhibitory effect of ergosterol on tumor stem cell proliferation.