中国中药杂志

2016, v.41(15) 2922-2926

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新补骨脂异黄酮在Caco-2细胞模型中的吸收机制研究
Absorption mechanism of neobavaisoflavone in Caco-2 cell monolayer mode

徐小昆;陈志永;李卓清;张翼敏;廖立平;周强;张紫佳;
XU Xiao-kun;CHEN Zhi-yong;LI Zhuo-qing;ZHANG Yi-min;LIAO Li-ping;ZHOU Qiang;ZHANG Zi-jia;The MOE Key Laboratory for Standardization of Chinese Medicines,Shanghai Key Laboratory for Compound Chinese Medicines,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine;Shanghai R&D Center for Standardization of Chinese Medicines;Department of Pharmacognosy,China Pharmaceutical University;

摘要(Abstract):

新补骨脂异黄酮为中药补骨脂中的黄酮类成分,具有抗菌、抗炎、抗癌、抗骨质疏松等多种药理作用。该文研究了新补骨脂异黄酮在Caco-2细胞模型中的吸收机制。采用Thermo Syncronis C18柱,流动相为甲醇-0.1%甲酸水溶液(90∶10),流速0.2 m L·min~(-1),电喷雾电离正离子模式(ESI+),以柳胺酚为内标物质建立新补骨脂异黄酮在Caco-2细胞孵育液中浓度的检测方法,考察时间、浓度、P-gp蛋白抑制剂维拉帕米、MRP-2蛋白抑制剂MK-571和BCRP蛋白抑制剂Ko143对新补骨脂异黄酮吸收的影响。研究结果表明,新补骨脂异黄酮在10~2 000μg·L~(-1)具有良好的线性,且专属性、基质效应、提取回收率、精密度、准确度和稳定性均符合测定要求。新补骨脂异黄酮在Caco-2细胞模型中的转运与时间和浓度呈正相关。15,30,50μmol·~(L-1)的新补骨脂异黄酮ER分别为1.64,1.94,0.99。与对照组相比,盐酸维拉帕米,MK-571,Ko143均可促进新补骨脂异黄酮的转运,其中盐酸维拉帕米和Ko143的作用较为显著。新补骨脂异黄酮在Caco-2细胞模型中的吸收以主动转运为主,同时存在被动转运,可能存在肠道转运蛋白的外排机制。
Neobavaisoflavone is one of flavonoids of traditional Chinese medicine Psoralea corylifolial. It has numerous biological properties such as antibacterial,anti-inflammatory,anti-cancer,and anti-osteoporosis effects. This paper aimed to investigate the absorption mechanism of neobavaisoflavone in Caco-2 cell monolayer model. The analyte and osalmide were separated on Thermo Syncronis C18 column with methanol-0. 1% formic acid solution(90∶ 10) as the mobile phase,at a flow rate of 0. 2 m L·min~(-1). The concentration of neobavaisoflavone was determined in eletrospray ionization( ESI) positive ion mode with osalmide as an the internal standard.The effects of time,concentration,P-gp inhibitor verapamil,MRP-2 inhibitor MK-571 and BCRP inhibitor Ko143 on the absorption of neobavaisoflavone were investigated. According to the results,neobavaisoflavone showed a good linearity within the concentration of 10-2 000 μg·L~(-1),and the results of its specificity,matrix effect,extraction recovery,precision,accuracy and stability all met the requirements. In the Caco-2 cell monolayer model,the transport volume of neobavaisoflavone was correlated positively with the time and concentration. The ER values of 15,30,50 μmol·L~(-1)neobavaisoflavone were 1. 64,1. 94,0. 99,respectively. As compared with the control group,all of verapamil hyduochloride,MK-571 and Ko143 could promote the transportation of neobavaisoflavone,and the effect was more obvious in verapamil hyduochloride and Ko143. The absorption of neobavaisoflavone may be mainly of active transport in Caco-2 cell monolayer model,and also involve passive transport. Excretion mechanism of intestinal transport protein may be also involved.

关键词(KeyWords): 新补骨脂异黄酮;Caco-2细胞;UPLC-MS/MS;吸收转运
neobavaisoflavone;Caco-2 cell;UPLC-MS/MS;absorption mechanism

Abstract:

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基金项目(Foundation): 国家自然科学基金面上项目(81473322);; 上海市自然科学基金项目(14ZR1441100);; 上海市教委科研创新项目(14YZO56);; 上海市中医药事业发展3年行动计划项目(ZYSNXD-GH-FFYJ)

作者(Author): 徐小昆;陈志永;李卓清;张翼敏;廖立平;周强;张紫佳;
XU Xiao-kun;CHEN Zhi-yong;LI Zhuo-qing;ZHANG Yi-min;LIAO Li-ping;ZHOU Qiang;ZHANG Zi-jia;The MOE Key Laboratory for Standardization of Chinese Medicines,Shanghai Key Laboratory for Compound Chinese Medicines,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine;Shanghai R&D Center for Standardization of Chinese Medicines;Department of Pharmacognosy,China Pharmaceutical University;

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