金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收研究  

Intestinal absorption of puerarin,vitexin,rosmarinic acid,and caffeic acid in Jinlianhua Decoction

作　　者：李丹 方明月 王莎 陶嘉悦 汪静 刘斯琪 侯金才 王如峰 LI Dan;FANG Ming-yue;WANG Sha;TAO Jia-yue;WANG Jing;LIU Si-qi;HOU Jin-cai;WANG Ru-feng(Jingjinji United Innovation Pharmaceutical Research Company,Beijing 100025,China;School of Life Sciences,Beijing University of Chinese Medicine,Beijing 102488,China)

机构地区：[1]京津冀联创药物研究(北京)有限公司,北京100025 [2]北京中医药大学生命科学学院,北京102488

出　　处：《现代药物与临床》2023年第5期1102-1108,共7页Drugs & Clinic

基　　金：中央引导地方科技发展资金项目(206Z2502G)。

摘　　要：目的考察金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收特性,确定金莲花汤中活性成分。方法采用HPLC法测定肠吸收样品中咖啡酸、葛根素、牡荆素、迷迭香酸,以大鼠肠外翻吸收实验和Caco-2细胞模型转运实验计算各成分的累积吸收量、吸收速率常数和表观渗透系数。结果随着金莲花汤的质量浓度增加,咖啡酸、葛根素、牡荆素、迷迭香酸的吸收速率常数呈线性关系增加,符合零级吸收速率,且吸收率均小于1.4%,在肠道中吸收效果普遍较差,其中咖啡酸的吸收较为明显。各成分的表观渗透系数值大小为迷迭香酸>咖啡酸>葛根素>牡荆素。结论金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸均可在肠道中被吸收,吸收方式为被动扩散,咖啡酸和迷迭香酸可能是金莲花汤中发挥药效的活性物质,葛根素和牡荆素可能是前药。Objective To investigate intestinal absorption of puerarin,vitexin,rosmarinic acid,and caffeic acid in Jinlianhua Decoction,and to determine the active components.Methods The contents of of puerarin,vitexin,rosmarinic acid,and caffeic acid were detected by HPLC method.Cumulative absorption amount,absorption rate constant,and permeability coefficient(Papp)of each component were calculated using everted intestinal sac model and Caco-2 cell monolayer model.Results As the concentration of Jinlianhua Decoction increases,the absorption rate constants of caffeic acid,puerarin,vitexin,and rosmarinic acid increase linearly with a zero-order reaction.Their absorption rates were below 1.4%,the absorption effect in the intestine was generally poor,and the caffeic acid was the highest.The Papp values were rosmarinic acid>caffeic acid>puerarin>vitexin.Conclusion Puerarin,vitexin,rosmarinic acid,and caffeic acid in Jinlianhua Decoction can be absorbed in the intestine with passive diffusion.Caffeic acid and rosmarinic acid may be active substances in Jinlianhua Decoction,while puerarin and vitexin may be prodrugs.

关 键 词：金莲花汤 咖啡酸 葛根素 牡荆素 迷迭香酸 累积吸收量 吸收速率常数 表观渗透系数 

分 类 号：R286.02[医药卫生—中药学]