Qian-Cutrone Jingfang, Huang Stella, Shu Yue-Zhong, Vyas Dolatrai, Fairchild Craig, Menendez Ana, Krampitz Kimberly, Dalterio Richard, Klohr Steven E, Gao Qi
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
J Am Chem Soc. 2002 Dec 11;124(49):14556-7. doi: 10.1021/ja028538n.
Two novel antitumor alkaloids, Stephacidin A and B, were isolated from the solid fermentation of Aspergillus ochraceus WC76466. 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 IC50 value 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.
从赭曲霉WC76466的固体发酵物中分离出两种新型抗肿瘤生物碱，即Stephacidin A和B。这两种生物碱对多种人类肿瘤细胞系均表现出体外细胞毒性；然而，Stephacidin B显示出更强且更具选择性的抗肿瘤活性，尤其是对前列腺睾酮依赖性LNCaP细胞，其IC50值为60 nM。基于核磁共振数据和X射线晶体学确定了Stephacidin A和B的结构。Stephacidin B具有15个环和9个手性中心，是自然界中结构最复杂、最新型的生物碱之一。
