杠柳苷元的抗肿瘤作用研究

Anti-cancer Effects of Periplogenin

目的研究中药香加皮提取单体化合物杠柳苷元对体外培养S180、SGC-7901、A549、LOVO、MCF-7、Hep G2肿瘤细胞株的毒性作用，探讨杠柳苷元对荷瘤模型小鼠的抗肿瘤作用。方法四氮唑盐（MTT）法测定杠柳苷元对体外培养肿瘤细胞的毒性作用，移植性荷瘤动物模型评价杠柳苷元对整体动物的抗肿瘤作用。结果杠柳苷元对体外培养肿瘤细胞的毒性作用显著，对常见肿瘤细胞株的个数抑制浓度介于（O．46～1．50）~g／mL；荷瘤模型动物给予杠柳苷元10．0mg／kg剂量时，S180实体瘤抑瘤率达到51．O％±17．O％，使荷腹水瘤小鼠存活时间延长94．2±13．1％，与临床常用抗肿瘤药物FU相当（P〉0．05）；抗肿瘤作用有明显的剂量依赖关系；部分受试动物给药后出现食欲减退、脱毛、抗拒等不良反应，未见死亡。结论杠柳苷元有显著的抗肿瘤作用，同时也有一定的不良反应，其潜在开发价值有待进一步研究评价。

Objective To evaluate the cytotoxicity of periplogenin to S180, SGC7901, A549, LOVO, MCF7 and HepG2 cell culture, anti-cancer effect of periplogenin on S180 sarcoma xeno-grafted mice were evaluated thereafter. Methods MTY method was adopted to assay the cytotoxic principles of periplogenin against cancer cell cultures in vitro, anticancer effect of the compound was measured by elongation of survival time or weight decrease of sarcoma in xeno-grafted mice in vivo. Results Cytotoxic potencies of periplogenin to all neoplasm cell cultures were significant, 50% inhibition concentration to all tested cells were in the scope of （0. 46-1.50） μg/mL; After periplogenin were administrated to the S180 sarcoma xeno-grafted mice, average weight decrease of the solid tumor in 10. 0 mg/kg periplogenin treated group reached （51.0 ＋ 17. 0）%, and the average survival time in the same dosage of periplogenin treated mice with ascetic type of carcinoma were prolonged （94.2 ＋ 13.1 ）% comparing to that of saline treated group, the result showed no difference when compared with that in positive control group which treated with 10mg/kg of FU （ P 〉 0. 05 ）, an obvious positive dosage-effect relationship was noticed in the study. Drug adverse reactions such as anorexia, hair-losing and rejection were observed in a few tested animals, but no death was found. Conclusion Anti-cancer effects of peripiogenin were significant and adverse reacts were observed, developmental value of the compound as a lead required further validation by much research and evaluations.