左金丸类方的小檗碱、巴马汀、黄连碱和药根碱在Caco-2细胞转运的比较研究  

Comparative study of transport character of jatrorrhizine,coptisine,palmatine and berberine in Zuojin Wan and its similar formulae in Caco-2 cells

作　　者：张新峰[1] 裘福荣[1] 蒋健[1] 高成璐[1] 

机构地区：[1]上海中医药大学附属曙光医院药代动力学实验室肝肾疾病病证教育部重点实验室,上海201203

出　　处：《中华中医药杂志》2011年第5期999-1003,共5页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：高等学校博士学科点专项科研基金(No.200802680010);上海市自然科学基金(No.10ZR1430800);上海市教委重点学科中药临床药理学(No.J50303);国家"重大新药创制"病毒性肝炎中药新药临床评价研究技术平台(No.2008ZX09312-023);上海市申康医院发展中心临床药理学科研共享平台(No.SHDC12007202)~~

摘　　要：目的:研究左金丸类方中4种生物碱的转运特征并比较其差异。方法:采用LC-MS/MS法测定左金丸类方中4种生物碱在Caco-2细胞上的转运特征,研讨其转运差异的机制。结果:环孢素A和维拉帕米均可增加4种生物碱的Papp(AP-BL),降低其Papp(BL-AB);MK-571对其转运均无影响;左金丸中的4种生物碱的Papp(AP-BL)均较黄连组增大;甘露散、茱萸丸中的药根碱、黄连碱和小檗碱的Papp(BL-AP)均较黄连减小。结论:小檗碱、黄连碱、药根碱和巴马汀均为P-gp底物,而非MRP2底物;吴茱萸可能具有抑制P-gp活性的作用。To study the transport character and mechanisms of berberine,palmatine,jateorhizine and coptisine in Zuojin Wan and its similar formulae by using Caco-2 cell transport model and with ciclosporin A and verapamil as P-glycoprotein（P-gp） inhibitors and MK-571 as multidrug resistance-associated protein 2（MRP2） inhibitor.In the transport experiment,Papp（AP-BL） of the 4 alkaloids were lower than that at the Papp（BL-AB）;ciclosporin A and verapamil increased Papp（AP-BL） but decreased Papp（BL-AB） of the 4 alkaloids,and decreased ERs by more than 80%;MK-571 had no influence on the transmembrane transports of all the 4 alkaloids;Papp（AP-BL） of the 4 alkaloids in Zuojin Wan were larger than that of the 4 alkaloids in coptis chinensis;Papp（BL-AP） of jateorhizine,coptisine and Berberine in Ganlusan and Zhuyuwan were larger than that of the 3 alkaloids in coptis chinensis.Berberine,palmatine,jateorhizine and coptisine were all P-gp substrates other than MRP2 substrates;and Evodiae fructus might have inhibition effects on P-gp.

关 键 词：左金丸 类方 黄连 吴茱萸 P-糖蛋白 

分 类 号：R285.5[医药卫生—中药学]