荭草花中五种成分在Caco-2细胞中的吸收特性研究  

Study on absorption activity of five components of Polygonum orientale L. Flower in Caco-2 cell monolayer

作　　者：陈浩[1,2] 覃小丽 夏涛[1,2] 李月婷 巩仔鹏 李勇军[1,3,2] 郑林[1,3] CHEN Hao;QIN Xiao-li;XIA Tao;LI Yue-ting;GONG Zi-peng;LI Yong-jun;ZHENG Lin(Guizhou Provincial Key Lab of Pharmaceutics/State Key Laboratory of Functional and Utilization of Medical Plants;Engineering Research Center for the Development and Application of Ethnic Medicine TCM （Ministry of Education;School of Pharmacy,Guiyang Medical University,Guizhou 550004, China)

机构地区：[1]贵州医科大学贵州省药物制剂重点实验室/药用植物功效与利用国家重点实验室,贵州贵阳550004 [2]贵州医科大学药学院,贵州贵阳550004 [3]贵州医科大学民族药与中药开发应用教育部工程研究中心,贵州贵阳550004

出　　处：《中国药理学通报》2018年第6期764-769,共6页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81360664;81560630);贵州省科技计划项目(黔科合平台人才[2017]5601;[2016]5613/5677);贵阳市科技局项目(筑科合同[2017]30-29号)

摘　　要：目的 利用Caco-2单层细胞模型研究荭草花提取物的吸收摄取特性。方法 采用UPLC-MS/MS考察荭草花提取物在不同浓度、时间、温度、pH、P-糖蛋白抑制剂(维拉帕米)和环孢菌素A条件下Caco-2细胞的吸收差异。结果 荭草花提取物在Caco-2细胞中的吸收具有浓度和时间依赖性,其中槲皮素等5个成分在摄取90min后逐渐降低;且在37℃条件下吸收最好;槲皮素pH为5条件下,利于其吸收,其余成分均在pH为6有利于吸收;加入P-糖蛋白抑制剂维拉帕米和环孢菌素A后发现,槲皮素和山奈酚受P-糖蛋白抑制剂维拉帕米影响,摄取量明显增加。结论 荭草花提取物中槲皮素等5种成分的吸收机制主要表现为被动扩散,P-糖蛋白参与其槲皮素和山奈酚的摄取过程。Aim To observe the absorption activity of five components of Polygonum orientale L. Flower extract in Caco-2 cell monolayer. Methods The effects of different concentrations,time,temperature,pH and P-glycoprotein inhibitors on Caco-2 cells were investigated by UPLC-MS/MS. Results The absorption of five components of Polygonum orientale L. Flower extract presented a concentration-and time-dependent manner,and the uptake of quercetin was reduced in Caco-2 cells after 90 min. There was a highest intake at 37℃,and the uptake of four components was best in acid environment except for the quercetin at pH 6,which was best at pH5. The uptake of quercetin and kaempferol was significantly improved after the addition of P-glycoprotein inhibitors of verapamil. Conclusions The cellular uptake mechanisms of the five components of Polygonum orientale L. Flower extract is maninly through passive diffusion. P-glycoprotein is involved in the uptake of quercetin and kaempferol.

关 键 词：荭草花提取物 CACO-2细胞 P-糖蛋白抑制剂 吸收机制 UPLC-MS/MS 摄取 

分 类 号：R284.1[医药卫生—中药学] R322.45[医药卫生—中医学]