Caco-2细胞模型研究川芎提取物中阿魏酸转运机制及白芷提取物对其转运的影响  

Transport mechanism of ferulic acid and the influence of Angelica dahurica extracts on absorption of ferulic acid by Caco-2 cell model

作　　者：梁新丽[1,2] 招丽君[2] 廖正根[2] 赵国巍[2] 尹蓉莉[1] 曹运朝[2] 

机构地区：[1]成都中医药大学,成都610075 [2]江西中医学院现代中药制剂教育部重点实验室,南昌300004

出　　处：《中药药理与临床》2012年第6期52-55,共4页Pharmacology and Clinics of Chinese Materia Medica

基　　金：国家自然科学基金资助项目(30960516);江西省自然科学基金资助项目(20114BAB215040)

摘　　要：目的:利用人源结肠腺癌细胞系Caco-2细胞单层模型,研究了川芎提取物中阿魏酸的吸收转运机制,以及白芷提取物对其吸收转运的影响。方法:建立人源结肠腺癌细胞系Caco-2细胞模型,利用此模型研究时间、药物浓度对川芎提取物中阿魏酸的转运影响与阿魏酸的双向转运特征;研究川芎中阿魏酸在有或无P-gp、MRP蛋白专属抑制剂存在时阿魏酸在Caco-2细胞模型的双向转运情况;并考察白芷提取物对川芎中阿魏酸吸收转运的影响。结果:阿魏酸在3h范围内转运速率保持恒定,在浓度范围(28～336mg/ml)内浓度与转运速率呈线性相关;加入P-gp和MRP蛋白抑制剂后,阿魏酸的AP侧转运增加,BL侧转运降低,PDR值下降;加入白芷有效成分(香豆素:0.45mg/ml、挥发油:0.72μl/ml、香豆素+挥发油:0.45mg/ml香豆素+0.72μl/ml挥发油)后阿魏酸的转运显著提高。结论:阿魏酸的转运过程可能为被动转运兼存在载体转运,阿魏酸的转运同时受P-gp和MRP外排影响,MRP影响较为明显,白芷有效成分对阿魏酸的转运有促进作用。To study the transport mechanism of ferulic acid and the effect of Angelica dahurica extracts on absorption of ferulic acid by Caco-2 cell model. Methods： The bidirectional transport, the effects of time, drug concentration, P-gp inhibitor and MRP inhibitor on the absorption of ferulic acid were observed. Then the influence of extract of Radix Angelicae Dahuricae on the transport of ferulic acid was stud- ied. Drug concentration was measured by HPLC and the apparent permeability coefficients （Papp） and apparent permeability ratio （PDR） were calculated. Results： The transport rate （Ka） of ferulic maintains constancy and the Ka change by concentrations. The apparent permea- bility coefficient （Papp） of ferulic acid from AP to BL increase and BL to AP decrease. The Papp of ferulic acid increase with the Angelica dahurica extractions. Conclusion： The transport mechanism of ferulic acid mainly is by passive paracellular transport pathway and involves carrier-mediated transport, and affected by the P-glycoprotein and MRP efflux protein. Angelica dahufica extractions can promote ferulic acid across the Caco-2 ceils.

关 键 词：阿魏酸 白芷提取物 CACO-2细胞 P-GP MRP 吸收机制 

分 类 号：R285[医药卫生—中药学]