中文摘要：

目的研究左金方（由黄连和吴茱萸按质量比6：1组成）中的生物碱类成分并评价其对人消化道肿瘤细胞的细胞毒活性。方法采用硅胶、SephadexLH-20等柱色谱方法进行分离纯化，通过理化性质和谱学数据鉴定化合物结构；MTT法测定化合物对人胃癌细胞系NCI—N87细胞和人结肠腺癌细胞系Caco-2细胞增殖的抑制活性。结果从左金方70％乙醇提取物的正丁醇溶性部分分离得到了15个生物碱，分别鉴定为吴茱萸次碱（1）、吴茱萸碱（2）、瑞特西宁（3）、黄连碱（4）、吴茱萸果酰胺III（5）、8．三氯甲基-7，8-二氢巴马亭（6）、表小檗碱（7）、8-三氯甲基-7，8-二氢表小檗碱（8）、8-三氯甲基-7．8-二氢黄连碱（9）、巴马亭（10）、小檗碱（11）、1，2，3，4-四氢．1．羰基-β-咔啉（12）、降氧化北美黄连次碱（13）、氧化表小檗碱（14）、紫堇定（15）。化合物1、2、4和11对NCI-N87和Caco-2细胞增殖具有抑制活性，IC50值为12．61～91．18gmol／L。结论化合物8为新化合物；化合物1、2、4和11可能是左金方在消化道局部发挥抗肿瘤作用的主要有效成分。

英文摘要：

Objective To study the alkaloid constituents of Zuojin Formula, consisting of Coptidis Rhizoma and Euodiae Fructus, and to evaluate their cytotoxicities against the proliferation of cancer cells in human digestive tract. Methods The constituents were isolated and purified by column chromatography on silica gel and Sephadex LH-20, as wetl as the chemical structures of alkaloids were determined by physicochemical properties and spectral data analyses. The cytotoxicities assay against human gastric NCI-N87 and colon adenocarcinoma Caco-2 cell lines was carried out by MTT method. Results Fifteen alkaloids were obtained from the normal butanol soluble fraction of 70% ethanolic extract in Zuojin Formula and identified as rutaecarpine （1）, evodiamine （2）, rhetsinine （3）, coptisine （4）, wuchuyuamide III （5）, 8-trichloromethyl-7, 8-dihydropalmatine （6）, epiberberine （7）, 8-trichloromethyl-7, 8- dihydroepiberberine （8）, 8-trichloromethyl-7, 8-dihydrocoptisine （9）, palmatine （10）, berberine （11）, 1, 2, 3, 4-tetrahydro-l-oxo-β- carboline （12）, noroxyhydrastinine （13）, 8-oxo-epiberberine （14）, and corydaldine （15）. Compounds 1, 2, 4, and 11 showed the inhibitory activities against the proliferation of NCI-N87 and Caco-2 cell with the half inhibitory concentration of 12.61-91.18 gmol/L. Conclusion Compound 8 is a new compound. Compounds 1, 2, 4, and 11 may be the main effective components in Zuojin Formula against the proliferation of cancer cells in human digestive tract.