王彧博,裴月湖,陈刚,王海峰
WANG Yubo,PEI Yuehu,CHEN Gang,WANG Haifeng

• 1:锦州医科大学药学院
• 2:沈阳药科大学中药学院

摘要(Abstract)：

目的 研究太行白前的化学成分，测试分离得到的C_(21)甾体类化合物的细胞毒活性。方法 采用硅胶柱色谱、凝胶柱色谱、高效液相色谱等方法进行分离纯化，通过理化性质和波谱数据分析鉴定化合物的结构。以5-氟尿嘧啶作为阳性对照药，采用MTT法测定分离得到的3种C_(21)甾体类化合物对3种人肿瘤细胞株(HL-60、THP-1、Caco-2)的生长抑制作用。结果 分离得到10个化合物，分别鉴定为cynanside A(1)、tylophoside A(2)、白前苷D(glaucoside D,3)、α-viniferin(4)、丁香脂素(syringaresinol,5)、丁香脂素-O-β-D-吡喃葡萄糖苷(syringaresinol O-β-D-glucopyranoside,6)、焦谷氨酸甲酯(L-pyroglutamic acid methyl ester,7)、2,5-二羟基苯乙酮(2,5-dihydroxyacetophenone,8)、4-羟基苯乙酮(4-hydroxyacetophenone,9)、香草酸(vanillic acid,10)。化合物2对Caco-2细胞IC_(50)为9.39μmol·L~(-1)。5-氟尿嘧啶对上述细胞IC_(50)为6.76μmol·L~(-1)。结论 化合物1～10为首次从太行白前中分离得到，所测试的3个化合物(化合物1～3)对HL-60、THP-1、Caco-2细胞表现出不同程度的抑制作用，其中化合物2对Caco-2细胞的抑制作用较强。
Objective To study the chemical constituents from Cynanchum taihangense,and the cytotoxic activity of the C_(21) steroidal glycosides.Methods The compounds from 95% ethanol extract of Cynanchum taihangense were isolated by silica gel column, Sephadex LH-20 column and HPLC,and their structures were identified by ~1H-NMR,~(13)C-NMR,and comparison of chemical and physical data with authentic samples reported in literatures.The MTT assay was used to detect the cytotoxicity of the C_(21) steroidal glycosides against three human tumor cell lines(HL-60,THP-1 and Caco-2),and 5-fluorouracil was used as a positive control.Results Ten compounds were isolated and identified as cynanside A(1),tylophoside A(2),glaucoside D(3),α-viniferin(4),syringaresinol(5),syringaresinol O-β-D-glucopyranoside(6),L-pyroglutamic acid methyl ester(7),2,5-dihydroxyacetophenone(8),4-hydroxyacetophenone(9),vanillic acid(10).Compound 2 displayed cytotoxic activity on Caco-2 cell line with IC_(50) values of 9.39 μmol·L~(-1).Conclusion All of the compounds are obtained from Cynanchum taihangense for the first time.The tested compounds show different degree of inhibitory activity against HL-60,THP-1 and Caco-2 cells, and compound 2 displays significant and selective cytotoxic activity on Caco-2 cell.

关键词(KeyWords)： 太行白前;化学成分;结构鉴定;C_(21)甾体;细胞毒活性
Cynanchum taihangense;chemical constituent;structure identification;C_(21) steroidal glycosides;cytotoxicity

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 王彧博,裴月湖,陈刚,王海峰
WANG Yubo,PEI Yuehu,CHEN Gang,WANG Haifeng

DOI: 10.14066/j.cnki.cn21-1349/r.2021.0223

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