Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cells
Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cells
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DOI：
10.1021/ja028538n
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发表时间：
2002-12-11
影响因子：
15
通讯作者：
Gao, Q
中科院分区：
文献类型：
--
作者：
Qian-Cutrone, JF;Huang, S;Gao, Q
从赭曲霉WC76466的固体发酵中分离得到两种新的抗肿瘤生物碱--千金藤素A和生物碱B。两种生物碱对多种人肿瘤细胞均有体外杀伤作用，但千金藤素B具有更强的抗肿瘤活性和选择性，特别是对前列腺睾酮依赖型LNCaP细胞的IC50值为60 nM。根据核磁共振数据和X-射线晶体结构确定了天冬氨酸A和B的结构。千金藤素B具有15个环和9个手性中心，是自然界中结构最复杂、最新颖的生物碱之一。
Two novel antitumor alkaloids, Stephacidin A and B, were isolated from the solid fermentation ofAspergillus ochraceusWC76466. Both alkaloids exhibit in vitro cytotoxicity against a number of human tumor cell lines; however, stephacidin B demonstrated more potent and selective antitumor activities, especially against prostate testeosterone-dependent LNCaP cells with IC50value of 60 nM. The structures of stephacidin A and B were established on the basis of the NMR data and X-ray crystallography. With 15 rings and 9 chiral centers, stephacidin B represents one of the most structurally complex and novel alkaloids occurring in nature.