摘要
目的:研究糙苏素的抗肿瘤作用及其对端粒酶活性和细胞周期的影响。方法:采用血清药理学与体内、外抑瘤实验相结合的方法,MTT法检测糙苏素含药血清对体外培养的人白血病K562细胞增殖的抑制作用,聚合酶链反应-酶联免疫吸附法检测K562细胞在糙苏素作用后端粒酶活性的变化,流式细胞仪分析细胞周期的改变;体内实验采用小鼠肝癌H22细胞株接种小鼠,连续给药14d,计算抑瘤率。结果:糙苏素含药血清在10%～50%剂量范围内对K562细胞有抑制作用,且呈剂量依赖关系(P<0.05);糙苏素作用后端粒酶活性出现抑制,且各给药组随糙苏素浓度增加抑制作用显著增强(P<0.01),同一浓度随作用时间延长,抑制作用逐渐增强(P<0.05);K562细胞的DNA合成后期/分裂期(G2/M)细胞含量显著增高(P<0.01);糙苏素(2.5、5、10mg·kg-1)灌胃能显著抑制小鼠移植性肝癌H22细胞的生长。结论:糙苏素具有抗肿瘤作用,其作用是通过抑制肿瘤细胞的端粒酶活性而实现的。
OBJECTIVE：To study the anti-tumor effect of phlomiol,and its influences on the activity of telomerase and cells phases.METHODS：Serologic pharmacological method,in vivo and in vitro anti-tumor experiments were adopted in the study.The inhibition effect of serum containing phlomiol on the proliferation of K562 tumor cells in vitro were detected by MTT method.The activity of telomerase in K562 tumor cell was determined by TRAP-PCR-ELISA.Flow cytometry was used to analyze the change of cell cycle.In vivo experiment,mice was inoculated with hepatic cancer H22 cells and the mice were orally administrated with phlomiol for 14 days.The inhibition rate of tumor was caculated.RESULTS：Serum containing 10%～50% phlomiol inhibited the proliferation of K562 tumor cells in vitro in dose-dependent manner（P〈0.05）.Phlomiol inhibited the activity of telomerase in K562 tumor cells.The inhibition effect was in dose-dependent manner（P〈0.01）.Meanwhile the inhibition effect increased gradually when the action time extended in the same dose of phlomiol group（P〈0.05）.The content of cell in K562 tumor cells were markedly increased in G2/M phase（P〈0.01）.Phlomiol（2.5,5,10 mg·kg^-1,i.g） inhibited the growth of implanted hepatic cancer H22 cells signiflcantly.CONCLUSION：The anti-tumor activity of phlomiol is performed by inhibiting the activity of telomerase in tumor cells.
出处
《中国药房》
CAS
CSCD
北大核心
2010年第39期3653-3655,共3页
China Pharmacy
基金
武警总部级课题(WKH2007-2)
