中国南海总合草苔虫抗癌活性成分研究:一个新的大环内酯的分离鉴定(英文)  

Studies on antineoplastic constituents from marine bryozoan Bugula neritina inhabiting South China Sea: isolation and structural elucidation of a novel macrolide

作　　者：林厚文[1] 刘皋林[1] 易杨华 姚新生[3] 吴厚铭[4] 

机构地区：[1]第二军医大学长征医院药学部,上海200003 [2]药学院海洋药物研究中心,上海200433 [3]沈阳药科大学,沈阳110015 [4]中国科学院上海有机化学研究所,上海200032

出　　处：《第二军医大学学报》2004年第5期473-478,共6页Academic Journal of Second Military Medical University

基　　金：ThisworkissupportedbytheNationalNaturalScienceFoundationofChina(29672050)NationalNewDrugR&DFoundation(96-901-05-183)ShanghaiNewDrugR&DFoundation(01431932).

摘　　要：目的:研究中国南海总合草苔虫中的抗癌活性成分。方法:通过分级萃取和多种硅胶柱层析(Sephadex LH-20凝胶过滤、ODS反相层析和HPLC)追踪分离抗癌活性成分;利用电喷雾离子质谱(ESI-MS)和高分辨(600 MHz)核磁共振二维谱技术鉴定化合物的结构。结果:分离得到一个新的具有显著抗肿瘤活性的大环内酯bryostatin 19(1)。同时还首次自中国海域的该种苔虫中分离鉴定了5个bryostatins类大环内酯抗癌活性化合物:bryostatin 4,5,6,10,18。Bryostatin 19显示很强的体外抗癌活性,对U937细胞的ED50值为3.2 nmol／L。结论:我国南海总合草苔虫资源丰富,并且含有新结构的抗癌活性草苔虫内酯。本研究结果为今后的新药研制与开发提供了参考。Objective:To investigate the antineoplastic constituents from marine bryozoan Bugula neritina in South China Sea. Methods: Antineoplastic compounds were screened by bioassay-guided method with partitive extraction and multiple column chromatographies(Sephadex LH-20,ODS and preparative HPLC). Structures of active compounds were determined by high-resolution 2D NMR(600 MHz) and ESI-MS techniques. Results: A new antineoplastic macrolide bryostatin 19(1) was isolated from this animal. Five known antineoplastic bryostatins :bryostatin 4(2) , bryostatin 5(3) ,bryostatin 6(4) ,bryostatin 18(5) and bryostatin 10(6),were for the first time obtained from this bryozoan in South China Sea. Bryostatin 19(1) shows strong inhibition activity against U937 cell line with ED50 value being 3. 2 nmol/L in vitro. Conclusion:The animal resource of Bugula neritina is abundant in South China Sea. It contains potential antineoplastic new macrolide of bryostatin series and will be developed as potentially useful source of anticancer agents in the future.

关 键 词：总合草苔虫 抗肿瘤药 草苔虫素 抗癌活性成分 

分 类 号：R282.77[医药卫生—中药学]