中药猫人参中的抗肿瘤活性成分

Anti-tumor constituents from the roots of Actinidia valvata

目的对中药猫人参（镊合猕猴桃Actinidia valvataDunn.根）中的抗肿瘤活性成分进行研究。方法运用多种色谱分离方法进行分离纯化,通过1HNMR、13CNMR、MS等波谱技术确定化合物的结构,并采用MTT法测试了部分单体化合物的体外细胞毒活性。结果分离并鉴定了11个化合物,其中10个为三萜类化合物：2α,3α,24-三羟基乌苏烷-12-烯-28-酸（1）,积雪草酸（2）,科罗索酸（3）,2α,3α,23,24-四羟基乌苏烷-12-烯-28-酸（4）,2α,3α,24-三羟基乌苏酸-11-烯-13β,28-内酯（5）,2α,3α,24-三羟基齐墩果烷-12-烯-28-酸（6）,2α,3α,19α,24-四羟基乌苏烷-12-烯-28-酸（7）,2α,3α,24-三羟基乌苏烷-12,20（30）-二烯-28-酸（8）,2α,3β,24-三羟基乌苏烷-12-烯-28-酸（9）,齐墩果酸（10）;1个植物甾醇：β-谷甾醇（11）。采用MTT法测试了化合物1、2、3、4、7对A549（人肺癌细胞）、LOVO（人结肠癌细胞）、HepG2（人肝癌细胞）等3种人肿瘤细胞株的体外细胞毒活性。结论化合物3~8为首次从该植物中分离得到,其中2、3对LOVO和HepG2细胞株有一定的抗肿瘤活性,且随着单体化合物极性的增大,细胞毒活性下降。

Objective To study the anti-tumor constituents from the roots of Actinidia valvata Dunn..Methods Column chromatographic techniques were used to isolate and purify the chemical constituents of the plant and their structures were elucidated by spectroscopic analysis,including 1HNMR,13CNMR and MS.The cytotoxic activities of some individual compounds were examined by MTT assay.Results Ten triterpenoids： 2α,3α,24-trihydroxyurs-12-en-28-oic acid（1）,asiatic acid（2）,corosolic acid（3）,2α,3α,23,24-tetrahydroxyurs-12-en-28-oic acid（4）,2α,3α,13β,24-tetrahydroxyurs-11-en-28-oic acid-13-lactone（5）,2α,3α,24-trihydroxyolean-12-en-28-oic acid（6）,2α,3α,19α,24-tetrahydroxyurs-12-en-28-oic acid（7）,2α,3α,24-trihydroxyurs-12,20（30）-dien-28-oic acid（8）,2α,3β,24-trihydroxyurs-12-en-28-oic acid（9）,and oleanolic acid（10）,and one plant sterol β-sitosterol（11） were isolated from the CHCl3 fraction of the roots of Actinidia valvata Dunn..The cytotoxic activities of five compounds（1,2,3,4,and 7） against A549,LOVO and HepG2 cell lines were evaluated.Conclusion Compounds 3-8 are isolated from this plant for the first time.Compounds 2 and 3 possess cytotoxic activity against LOVO and HepG2 cell lines,and the cytotoxic activity decreases with the increase of polarity of individual compound.