甘草酸18位差向异构体不同配比和浓度对Caco-2细胞P-gp功能的影响  

Different proportion and concentration of Glycyrrhizic acid-18-epimers effect on P-gp function in Caco-2 cells

作　　者：赵燕燕[1,2] 孙东[1] 刘丽艳[3] 柳亚飞[1] 王静[1] 

机构地区：[1]河北大学化学与环境科学学院,河北保定071002 [2]河北大学药学院,河北保定071002 [3]河北大学医学实验中心,河北保定071000

出　　处：《河北大学学报（自然科学版）》2016年第3期249-256,共8页Journal of Hebei University(Natural Science Edition)

基　　金：河北省自然科学基金资助项目(H2013201203);河北大学医学学科专项资金建设项目(2014A1003)

摘　　要：研究甘草酸18位差向异构体18α-甘草酸(18α-Gly)与18β-甘草酸(18β-Gly)不同配比和浓度对结肠癌(Caco-2)细胞P-糖蛋白(P-gp)功能的影响,选择最佳浓度比例.建立细胞模型,选择甘草酸总浓度为1∶10∶30∶60∶120∶240μmol/L,18α-Gly与18β-Gly物质的量比分别为10∶0、8∶2、6∶4、5∶5、4∶6、2∶8、0∶10,根据细胞存活率,选择合适浓度比例,利用流式细胞仪测定细胞内荧光强度,寻找荧光强度最大的浓度比,即对P-gp抑制作用最强,P-gp功能最弱.研究结果表明甘草酸总浓度为1μmol/L时,随着18α-Gly比例的减少,荧光强度逐渐减弱,P-gp诱导作用逐渐增加.甘草酸总浓度为10μmol/L和60μmol/L时,随着两者物质的量比的变化,荧光强度变化明显;当总浓度为10μmol/L,n(18α-Gly)∶n(18β-Gly)=4∶6时,荧光强度较强,抑制作用明显;当总浓度为60μmol/L,两者物质的量比为5∶5时荧光强度最强,抑制作用最强.To evaluate the effect of glycyrrhizic acid 18 epimers,18α-glycyrrhizic acid（18α-Gly）and18β-glycyrrhizic acid（18β-Gly）at different proportion and concentration on the P-glycoprotein（P-gp）activity in colon cancer Caco-2cell to select their appropriate concentration and proportion in use.Making a cell model,selecting the total glycyrrhizic acid concentration of 1,10,30,60,120,240μmol/L and proportion of 10∶0,8∶2,6∶4,5∶5,4∶6,2∶8,0∶10,determining their optimum concentration and proportion by cell survival rate,and detecting the maximum fluorescence value by flow cytometer,that is,thestrongest inhibitory effect of P-gp and its weakest function.When the concentration of glycyrrhizic acid was1μmol/L,the fluorescence intensity became gradually weak and its induction fuction was strengthed gradually with the reduction in proportion of 18α-Gly.When the concentration of glycyrrhizic acid was 10μmol/L and60μmol/L,the fluorescence intensity changed significantly.When the concentration of glycyrrhizic acid was 10μmol/L and their proportion was n（18α-Gly）∶n（18β-Gly）=4∶6,the fluorescence intensity became stronger and its inhibitory effect was remarkable.When the concentration of glycyrrhizic acid was60μmol/L and their proportion was n（18α-Gly）∶n（18β-Gly）=5∶5,the fluorescence intensity was the highest,and the strongest inhibitory effect of P-gp appeared.

关 键 词：18Α-甘草酸 18Β-甘草酸 P-糖蛋白功能 CACO-2细胞 不同配比/浓度 

分 类 号：R285.5[医药卫生—中药学]