杜仲中五环三萜类及其抗肿瘤活性

Pentacyclic triterpenoids from Eucommia ulmoides and their antitumor activities

目的研究杜仲Eucommia ulmoides Oliver中五环三萜类及其抗肿瘤活性。方法杜仲二氯甲烷提取物采用硅胶、Sephadex LH-20进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。MTT法测定其抗肿瘤活性,PI和Hoechst染色检测凋亡。荧光探针标记Hela细胞的溶酶体和线粒体,并观察两者形态的变化。结果从中分离得3个化合物,分别鉴定为到桦木酸(1)、羽扇豆醇(2)、3-O-laurylbetulinic acid(3)。化合物1～3对Hela、MDA-MB-231、T47D细胞的生长抑制率随化合物浓度增高而增加;均能有效诱导Hela细胞发生凋亡;显著抑制了溶酶体的生成,且诱导线粒体破碎。结论化合物3为首次从该植物中分离得到,化合物1～3有较强的抗肿瘤活性。

AIM To study the pentacyclic triterpenoids from Eucommia ulmoides Oliver and their antitumor activities.METHODS The methylene dichloride extract from E.ulmoides was isolated and purified by silica and Sephadex LH-20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their antitumor activities were detected by MTT assay,and apoptosis was detected through PI and Hoechst staining.In addition,the lysosome and mitochondria in Hela cells were labeled using fluorescence probe,and their morphological changes were observed.RESULTS Three compounds were isolated and identified as betulinic acid(1),lupeol(2),3-O-laurylbetulinic acid(3).The growth inhibition rates of compounds 1-3 on Hela,MDA-MB-231 and T47D cells increased with the concentrations increasing.They could effectively induce the apoptosis of Hela cells and markedly suppress the lysosome production and induce mitochondrial fragmentation.CONCLUSION Compound 3 is isolated from this plant for the first time,and compounds 1-3 have strong antitumor activities.