Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model

DANG Jue; LI Yan; LIU Mei-chen; LUO Lin; GONG Xiao-hong; ZHOU Yi-meng; TANG Yun-qiu; ZHENG Li; QUAN Yun-yun; LI Yun-xia; PENG Cheng

doi:10.13422/j.cnki.syfjx.20180706

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Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model

更新时间：2024-01-04

- Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 24, Issue 7, Pages: 1-6(2018)
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- DOI：10.13422/j.cnki.syfjx.20180706
  CLC： R285
- Published：2018
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DANG Jue, LI Yan, LIU Mei-chen, et al. Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(7): 1-6.
DOI：

DANG Jue, LI Yan, LIU Mei-chen, et al. Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(7): 1-6. DOI： 10.13422/j.cnki.syfjx.20180706.

摘要

目的：研究大黄中大黄酸、大黄素，附子中去甲乌药碱，以及大黄酸、大黄素与去甲乌药碱分别配伍后在Caco-2细胞模型上的转运过程。方法：以大黄酸、大黄素、去甲乌药碱的累积转运量及表观渗透系数（Papp）为指标，采用HPLC对大黄酸、大黄素、去甲乌药碱的含量进行检测，考察大黄酸、大黄素、去甲乌药碱在Caco-2细胞上的转运行为，以及大黄素、大黄酸分别配伍去甲乌药碱后转运行为的变化情况。结果：不同浓度去甲乌药碱的Papp均>1×10-7 cm ·s-1，外排与吸收比值接近1.5，配伍大黄酸、大黄素后去甲乌药碱的Papp显著上升（P<0.05）。大黄酸、大黄素配伍去甲乌药碱后前二者的Papp显著下降（P<0.05）。结论：去甲乌药碱是1个中等吸收的药物，其吸收方式主要为被动转运。大黄中大黄酸、大黄素可促进附子中去甲乌药碱的在肠吸收，而去甲乌药碱却会抑制大黄酸、大黄素的在肠吸收。

Abstract

Objective: Transport behaviors of rhein and emodin in Rhei Radix et Rhizoma and higenamine in Aconiti Lateralis Radix Praeparata were studied on Caco-2 cell model

and the change of transport behaviors after the compatibility of rhein

emodin with higenamine was inspected. Method: HPLC was used to analyzed the concentration of rhein

emodin and higenamine

then apparent permeability coefficients (Papp) and cumulative transport amounts were calculated.So as to investigate the bi-directional transport behavior of rhein

emodin and higenamine on Caco-2 cell

as well as the change of the transport behaviors of emodin and rhein. Result: Papp of higenamine with different concentrations was >1×10-7 cm · s-1

the ratio of permeability in the basolateral to apical direction was about 1.5 times that of the apical to basolateral direction.The transport amount of higenamine was significantly (P<0.05) increase in the presence of rhein and emodin.Whereas the transport amount of rhein and emodin was significantly (P<0.05) decrease in the presence of higenamine. Conclusion: Higenamine can be mediumly absorbed on the Caco-2 monolayer model by a passive transportation.Rhein and emodin can promote the intestinal absorption of higenamine

but higenamine can inhibit the intestinal absorption of rhein and emodin.

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