摘要
本实验以虫草素为母核,合成三个虫草素衍生物,研究其体外抗肿瘤活性以及在大鼠体内的药物代谢动力学。以人肝癌细胞HepG2为研究对象,通过MTT法测定三种虫草素衍生物对其抑制作用。通过HPLC方法考察三个虫草素衍生物大鼠血浆药物浓度随时间变化趋势,检测大鼠血浆中药物含量并评价其药动学特性。研究发现,虫草素衍生物对HepG2细胞的抑制率增加。虫草素及三个衍生物IC50值分别为0.12、0.11、0.07、0.06μM。虫草素衍生物Tmax时间延长,药物在体内存在时间延长;随着Cmax的升高,药物在体内的作用浓度升高。
In this study,three cordyceps derivatives were synthesized with cordycepin as the raw material to study their anti-tumor activity in vitro and pharmacokinetics in rats.The human hepatoma cell HepG2 was used as the research object,and the inhibitory effects of the three cordycepin derivatives on HepG2 were determined by MTT assay.The plasma drug concentration of three cordycepin derivatives was observed by HPLC method.The pharmacokinetics of rat plasma was evaluated.The results showed that,the inhibition rate of cordycepin derivatives on HepG2 cells is increased.The IC50 values of cordycepin and derivatives are 0.12,0.11,0.07,0.06 μM,respectively.The Tmax time of the cordycepin derivative is prolonged,and the time of the drug in the body is prolonged;when the Cmax is increased,the concentration of the drug in the body is increased.
作者
崔琳琳
王莹
李国玉
袁甜
CUI Lin-lin;WANG Ying;LI Guo-yu;YUAN Tian(Heilongjiang Provincial Key Laboratory of Drug Prevention and Treatment for Senile Diseases;College of pharmacy,Harbin University of Commerce,Harbin 150076,China)
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2020年第4期582-591,707,共11页
Natural Product Research and Development
基金
哈尔滨商业大学青年创新人才项目(17XN031)。
关键词
虫草素
修饰
活性
抗肿瘤
药动学
cordycepin
modification
activity
anti-tumor
pharmacokinetics
