7-表-10-去乙酰基三尖杉宁碱的HPLC分析方法及其溴化产物的抗癌活性研究(英文)  

Study on 7-Epi-10-deacetylcephalomannine:HPLC Assay and Its Bromination Products as Potent Antitumor Agents

作　　者：姜毅[1] 金晓英[1] 陈建民[1] 

机构地区：[1]复旦大学环境科学与工程系,上海200433

出　　处：《复旦学报（自然科学版）》2004年第4期621-627,共7页Journal of Fudan University：Natural Science

基　　金：ProjectsupportedbytheNationalScienceFoundationofChina(No.20377008)

摘　　要：分别在C18柱和MetachemTaxsil 3紫杉醇专用柱上研究了云南红豆杉粗提物中紫杉醇(1)、三尖杉宁碱(2)、7 表 10 去乙酰基紫杉醇(3)和7 表 10 去乙酰基三尖杉宁碱(4)的反相色谱行为.在MetachemTaxsil 3紫杉醇专用柱上,水:乙腈(54:46)的流动相使这四种色谱行为相近的化合物获得了基线分离.使用溴化法处理含有(2)和(4)的红豆杉粗提物,通过分离纯化得到了二溴 7 表 10 去乙酰基三尖杉宁碱的两个非对映异构体(5和6).体外活性实验结果表明,5和6对于人乳腺癌(MCF 7)、人肺癌(A549)和人卵巢癌的体外毒性比紫杉醇略强.7-Epi-10-deacetylcephalomannine (4) was firstly revealed as a closely eluting analogue to paclitaxel in bark extract of Taxus yunnanesis. Reverse phase chromatographic behaviors of standards mixture of paclitaxel (1), cephalomannine (2), 7-epi-10-deacetyltaxol (3) and 7-epi-10-deacetylcephalomannine (4) was systematically studied on two different RP-HPLC columns in isocratic mode and the optimum assay was achieved on Metachem Taxsil-3 column in 22 min with an isocratic elution of water: acetonitrile (54:46). Treatment of 4 with bromine yields two diastereomers of 2'', 3''-dibromo-7-epi-10-deacetylcephalomannine(5 and 6). The in vitro cytotoxicity of the two diastereomers, which was assessed in cell culture against MCF-7 breast cancer, A549 lung cancer and A2780 ovarian cancer, was a little stronger than that of paclitaxel.

关 键 词：7-表-10-去乙酰基三尖杉宁碱 HPLC分析方法 二溴-7-表-10-去乙酰基三尖杉宁碱 体外细胞毒性 紫杉科 

分 类 号：Q949.661[生物学—植物学] O657.72[理学—分析化学]