续随子中千金二萜烷化合物抑制人妇科肿瘤细胞增殖活性的研究

Inhibitory effect of lathyrane diterpen factors from Euphorbia lathyris on the proliferation of gynecologic cancer cells

目的检测大戟科植物续随子中分离纯化的3种千金二萜烷化合物Euphorbia Factor L1(1)、Euphorbia Factor L2(2)和Euphorbia Factor L3(3)对子宫颈癌、子宫内膜癌、卵巢透明癌和卵巢囊腺癌等5种人妇科肿瘤细胞增殖的影响,探讨了千金二萜烷化合物结构与抑制肿瘤细胞增殖活性之间的构-效关系。方法利用四唑盐(MTT)比色法测定阳性对照顺铂和3种化合物对子宫颈癌、子宫内膜癌、卵巢透明癌和卵巢囊腺癌等5种人妇科肿瘤细胞增殖的影响。结果发现Euphorbia Factor L1(1)和Euphorbia Factor L3(3)对子宫颈癌细胞的增殖具有抑制作用,EC50分别为16.74和1.01μmol.L-1;Euphorbia Factor L3(3)对人卵巢透明癌和人卵巢囊腺癌细胞的增殖显示中等程度的抑制活性;Eu-phorbia Factor L2(2)即使在100μmol.L-1的高浓度下,对5种肿瘤细胞的增殖不显示抑制活性。结论 Euphorbia Fac-tor L3(3)对人妇科肿瘤细胞的增殖显示抑制活性,推测千金二萜烷化合物抑制肿瘤细胞增殖活性与母核上的环外双键及邻位取代基有关。

Aim Three lathyrane diterpen factors Euphorbia Factor L1~L3 were isolated from Euphorbia lathyris.Use MTT assay to evaluate the antitumor activities of three lathyrane diterpen factors to the cells of cervical cancer cell（HeLa）,endometrial adenocarcinoma cell（HEC-1）,Ovarian clear-cell cystadedocarcinome cell（SHIN3 and HOC-21） and ovarian clear-cell carcinoma cell（HAC-2）,and to explore the relationship between structure and activity.Method Use MTT assay to evaluate the antitumor activities of lathyrane diterpen-L-factors to the cell lines of HeLa,HEC-1,SHIN3,HOC-21 and HAC-2.Results Results indicated that Euphorbia Factor L1 and euphorbia factor L3 exhibited significant anti-growth effects on HeLa cell,and the value of EC50 HeLa cell were 16.74 μmol·L-1 and 1.01 μmol·L-1 exposure.Euphorbia Factor L3 demonstrated moderate inhibitory activities to HAC-2,SHIN3 and HOC-21 cells.Euphorbia factor L2 did not show activities against tested cells.Conclusion This result indicates that Euphorbia Factor L3 exhibits excellent anti-growth activities to five cell lines and that antitumor activity of lathyrane diterpenes-L-factors were related to the exo-double bond and the substitution adjacent to the double bond.