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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
引用本文:姜毅,金晓英,陈建民.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[J].复旦学报(自然科学版),2004,43(4):621-627.
作者姓名:姜毅  金晓英  陈建民
作者单位:1. 复旦大学,环境科学与工程系,上海,200433
2. 复旦大学,环境科学与工程系,上海,200433;复旦大学,生命科学学院,生物多样性研究所,教育部生物多样性和生物工程重点实验室,上海,200433
基金项目:国家自然科学基金,20377008,
摘    要:分别在C18柱和Metachem Taxsii-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Metachem Taxsil-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.

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

Study on 7-Epi-10-deacetylcephalomannine:HPLC Assay and Its Bromination Products as Potent Antitumor Agents
Abstract.Study on 7-Epi-10-deacetylcephalomannine:HPLC Assay and Its Bromination Products as Potent Antitumor Agents[J].Journal of Fudan University(Natural Science),2004,43(4):621-627.
Authors:Abstract
Abstract: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.
Keywords:7-epi-10-deacetylcephalomannine  HPLC assay  2'  3'-dibromo-7-epi-10-deacetylcephalomannine
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