苦碟子中2个倍半萜内酯的牛血清白蛋白结合率的测定  

Determination of bovine serum albumin binding rates on two sesquiterpene lactones of Ixeris sonchifolia

作　　者：张秀平[1] 董鲁艳[1] 刘思燚 蔡伟[1] 王菲[1] 尚展鹏 张加余[2] 王子健[2] 卢建秋[3] 刘颖[2] 

机构地区：[1]北京中医药大学中药学院,北京100102 [2]北京中医药大学中医药研究院,北京100029 [3]北京中医药大学图书馆,北京100029

出　　处：《药物分析杂志》2017年第3期524-529,共6页Chinese Journal of Pharmaceutical Analysis

基　　金：国家重点基础研究发展计划(973计划;2012CB518406);国家自然基金青年科学基金(81503244)

摘　　要：目的:研究苦碟子中倍半萜内酯类化合物苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白的结合率。方法:采用HPLC法测定苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的总浓度及游离药物浓度,色谱分离采用Zorbax SB-C_(18)色谱柱(4.6 mm×250 mm,5μm),以水(A)-甲醇(B)为流动相,线性梯度洗脱(0~5 min,30%B→37%B;5~15 min,37%B→52%B;15~22 min,52%B→60%B),流速1.0mL·min^(-1),柱温30℃,检测波长272 nm,进样量10μL;在37℃条件下,应用平衡透析法测定苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白结合率。结果:低、中、高3个浓度下,苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白结合率分别为51.21%、54.72%、52.14%和50.63%、52.82%、50.28%。结论:苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z具有中等强度的蛋白结合率,且无明显的浓度依赖性。Objective：To determine the bovine serum albumin binding rate of Ixerin Z,11,13α-dihydroixerin Z on sesquiterpene lactones of Ixeris sonchifolia.Methods：The total concentration of Ixerin Z and 11,13α-dihydroixerin Z as well as the free drugs were determined by HPLC method.The separation was performed on a Zorbax SB-C_（18） column（4.6 mm×250 mm,5 μm）.A linear gradient elution of solvent water（A）and methanol（B）was applied with the following program：0-5 min,30% B → 37% B;5（-1）5 min,37% B → 52% B and 15-22 min,52% B → 60% B.The flow rate was set as 1.0mL·min（-1）.The temperature of column was set at 30 ℃.The detection wavelength was set at 272 nm.And the injection volume was 10 μL.The protein binding rates of Ixerin Z and 11,13α-dihydroixerin Z were determined by equilibrium dialysis method at 37 ℃.Results：The protein-binding rate of Ixerin Z and 11,13α-dihydroixerin Z at low,middle and high concentration were 51.21%,54.72%,52.14% and 50.63%,52.82%,50.28%,respectively.Conclusion：The two sesquiterpene lactones have moderate intensity protein-binding rate.And the binding rates are not remarkable concentration-dependent manner of Ixerin Z,11,13α-dihydroixerin Z.

关 键 词：苦碟子 倍半萜内酯 苦荬菜内酯Z 11 13α-二氢苦荬菜内酯Z 蛋白结合率 药代动力学参数 高效液相色谱 

分 类 号：R917[医药卫生—药物分析学]