长柱重楼总皂苷体外抗肿瘤活性及毒性研究  

Antitumor activity in vitro and toxicity of the total saponins from Paris forrestii

作　　者：杨蓉蓉 王跃虎[2] 施敏 陈雪梅 陈英杰 王鹏 周轶平 

机构地区：[1]昆明医科大学药学院/云南省天然药物药理重点实验室,昆明650500 [2]中国科学院昆明植物研究所资源植物与生物技术重点实验室,昆明650201 [3]昆明医科大学基础医学院,昆明650500

出　　处：《中国临床药理学杂志》2018年第4期439-442,共4页The Chinese Journal of Clinical Pharmacology

基　　金：云南省教育厅科学研究基金重点基金资助项目(2014Z060);云南省科技厅-昆明医科大学应用基础研究联合专项基金资助项目(2014FB011)

摘　　要：目的研究长柱重楼总皂苷(PCT3)体外抗肿瘤活性及毒性。方法用改良二甲基四氮唑盐法检测PCT3、顺铂对人肺癌细胞株(A-549)和人肝癌细胞株(HEPG-2)的增殖抑制作用。小鼠一次性腹腔注射52,74,105,150mg·kg^(-1)PCT3,检测PCT3的半数致死量(LD50),并观察肝组织病理切片的变化,用比色法测定PCT3的溶血作用。结果 PCT3对A-549和HEPG-2细胞增殖抑制的半数抑制浓度(IC50)分别为11.71和2.36μg·mL^(-1),顺铂对A-549和HEPG-2细胞增殖抑制的IC_(50)分别为6.31和5.33μg·mL^(-1).PCT3对小鼠的LD_(50)为92.40 mg·kg-,其对动物的整体健康状态有一定的影响,具有一定的肝毒性。PCT3的溶血率随着浓度的增加而增加,其溶血的半数有效量为4.31μg·mL^(-1)。结论 PCT3对人癌细胞株A-549和HEPG-2细胞的增殖均有较强的抑制作用,对HEPG-2细胞的增殖抑制作用强于A-549细胞。同时,PCT3有一定的肝毒性和溶血活性,其溶血活性与细胞毒活性有较明显的相关性。Objective To study the antitumor activity in vitro and toxicity of the total saponins from Paris forrestii（ PCT3）. Methods Inhibitory effect of PCT3 on the proliferation of human lung cancer（ A-549）and human hepatoma cells（ HEPG-2） was measured via 3-（ 4,5-dimethylthiazol-2 yl）-2,5-diphenylt etrazoliumbromide assay; PCT3 was injected at the dose of 52,74,105,150 mg·kg^-1 to detect the half lethal dose（ LD50）; Hemolytic effect of PCT3 was determined by colorimetric method. Results The 50% inhibitory concentration（ IC50）values of PCT3 were 11. 71 μg·mL^-1 and 2. 36 μg·mL^-1 on A-549 and HEPG-2 cells,respectively. The IC50 values of cisplatin were 6. 31μg·mL^-1 and 5. 33 μg·mL^-1 on A-549 and HEPG-2 cells,respectively. LD50 of PCT3 was 92. 40 mg·kg^-1,and it showed a certain hepatic toxicity and certain inhibitory effects on overall health status of the animal; The hemolytic activity of PCT3 was dose dependent,and the half effective dose（ ED50） was 4. 31 μg·mL^-1. Conclusion PCT3 had obvious inhibitory effect on the proliferation of A-549 and HEPG-2 cell lines,the later is stronger than the former. Acute toxicity test in mice showed that PCT3 had a certain toxicity; PCT3 had remarkable hemolytic activity,there was a significant correlation between hemolytic activity and cytotoxic activity.

关 键 词：长柱重楼 总皂苷 体外抗肿瘤活性 急性毒性 溶血作用 

分 类 号：R28[医药卫生—中药学]