生理病理状态下荭草活性物质对转运体表达的影响

doi:10.3976/j.issn.1002-4026.2025089

山东科学

• 药理与毒理 •

生理病理状态下荭草活性物质对转运体表达的影响

罗秋芸^1a,1b,2，孙佳^1a，刘东辉^1a,1b，李勇军^1a，薛维娜^1a,1b,1c*

收稿日期：2025-08-29 修回日期：2025-11-05

基金项目:贵州省科技重大专项项目（黔科合重大专项字[2024]015）、贵州省现代中药创制全省重点实验室（黔科合平台ZSYS [2025] 019）

作者简介：罗秋芸（1988年—），女，硕士研究生，研究方向为药理学。E-mail:luoqiuyun817@163.com

*通信作者，薛维娜，女，副教授，硕士生导师，研究方向为药理学。E-mail: xwn824@126.com 电话：14785563829

1.贵州医科大学a.药学院中药功效成分发掘与利用全国重点实验室,b.贵州省现代中药创制全省重点实验室民族药与中药开发应用教育部工程研究中心，c医药卫生管理学院,贵州贵阳561113； 2.贵州省第三人民医院药剂科，贵州贵安新区 550008

收稿日期:2025-08-29 接受日期:2025-11-05 上线日期:2026-04-30
通信作者: 薛维娜 E-mail:xwn824@126.com
作者简介:罗秋芸（1988年—），女，硕士研究生，研究方向为药理学。E-mail:luoqiuyun817@163.com
基金资助:
贵州省科技重大专项项目（黔科合重大专项字[2024]015）、贵州省现代中药创制全省重点实验室（黔科合平台ZSYS [2025] 019）

Effects of active constituents from Polygonum orientale L. on the expression of transporters under physiological and pathological conditions

LUO Qiuyun^1a,1b,2，SUN Jia^1a，LIU Donghui^1a,1b ,LI Yongjun^1a，XUE Weina^1a,1b,1c*

1. a. State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy;b. Guizhou Provincial Key Laboratory of Modern Traditional Chinese Medicine Creation, Engineering Research Center for Development and Application of Ethnic Medicine and Traditional Chinese Medicine (Ministry of Education); c. School of Pharmaceutical and Health Administration,Guizhou Medical University, Guiyang 561113, China; 2. Department of Pharmacy, The Third People's Hospital of Guizhou Province, Guiyang, Guizhou 550008,China

Received:2025-08-29 Accepted:2025-11-05 Online:2026-04-30
Contact: XUE Weina E-mail:xwn824@126.com

摘要/Abstract

摘要： 荭草具有明确的抗心肌缺血作用，且其活性成分在生理和病理状态下的代谢过程存在显著差异，鉴于转运体在心肌缺血病理过程和外源物代谢中的作用，本研究拟探讨荭草活性物质在生理及病理状态下对大鼠肝脏转运体表达的影响。采用网络药理学筛选心肌缺血相关靶点，利用蛋白质相互作用（PPI）分析、基因本体（GO）和京都基因与基因组百科全书（KEGG）富集分析，结合文献调研，筛选与心肌缺血相关的肝脏转运体及通路；运用分子对接技术预测荭草活性成分与转运体调控蛋白的结合；并建立大鼠心肌缺血模型，采用实时荧光定量PCR（qRT-PCR）和蛋白免疫印迹法(Western blot)检测荭草提取物对肝脏转运体表达的影响。结果显示，网络药理学分析发现428个心肌缺血与转运蛋白的共同靶基因；PPI分析筛选出36个节点，GO和KEGG分析表明这些靶点显著富集于炎症反应、ABC转运蛋白及PPAR信号通路等，结合文献调研，发现BCRP、MRP、P-gp等7个肝脏转运体与心肌缺血相关；分子对接提示荭草活性成分与转运体上游调控蛋白具有较高亲和力。动物实验表明，在正常大鼠中荭草提取物可上调MRP1、MRP2、OATP2、OCT1、OCT2和P-gp的表达，而在心肌缺血模型大鼠中则下调BCRP、MRP2、OATP2、OCT1、OCT2和P-gp的蛋白表达。结果表明，在生理病理状态下，荭草活性成分具有调控肝脏转运体的能力，其机制可能与活性成分结合肝脏转运体上游调控蛋白有关。

关键词: 荭草, 心肌缺血, 转运体, 网络药理学, 分子对接, 实时荧光定量逆转录聚合酶链反应, 蛋白免疫印迹法

Abstract: Polygonum orientale L. has an anti-myocardial ischemia effect, and the metabolic processes of its active constituents exhibits considerabledifferences under physiological and pathological conditions. Consideringthe role of transporters in the pathological process of myocardial ischemia and the metabolism of xenobiotics, this study aims to investigate the effects of the active constituents in Polygonum orientale L. on the expressions of liver transporters in rats under physiological and pathological conditions.Network pharmacology was used to screen myocardial ischemia-related targets, followed by protein–protein interaction (PPI) analysis, Gene Ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses. Based on a literature review, hepatic transporters and pathways related to myocardial ischemia were identified. Morever, molecular docking was used to predict the binding affinity between the active constituents of Polygonum orientale L. and regulatory proteins of transporters. A rat model of myocardial ischemia was established, and the effects of Polygonum orientale L. extract on the expressions of hepatic transporters were detected using quantitative real-time PCR (qRT-PCR) and western blot. Results revealed that network pharmacology analysis identified 428 common target genes associated with myocardial ischemia and transport proteins. PPI analysis yielded 36 key nodes, and GO and KEGG analyses revealed substantial enrichment of these targets in inflammatory responses, ABC transporters, PPAR signaling pathway, among others. Based on the literature review, seven hepatic transporters, including BCRP, MRP, and P-gp, were observed to be associated with myocardial ischemia. Molecular docking suggested high binding affinity between active constituents of Polygonum orientale L. and upstream regulatory proteins of transporters. Furthermore, animal experiments revealedthat Polygonum orientale L. extract upregulated the expressions of MRP1, MRP2, OATP2, OCT1, OCT2, and P-gp in normal rats, and downregulated the protein expressions of BCRP, MRP2, OATP2, OCT1, OCT2, and P-gp in rats with myocardial ischemia. These results indicate that the active constituents of Polygonum orientale L. can regulate hepatic transporters under physiological and pathological conditions, and their mechanism may be related to their binding to upstream regulatory proteins of hepatic transporters.

Key words: Polygonum orientale L., myocardial ischemia, transporters, network pharmacology, molecular docking, qRT-PCR, western blot

中图分类号:

罗秋芸, 孙佳, 刘东辉, 李勇军, 薛维娜. 生理病理状态下荭草活性物质对转运体表达的影响[J]. 山东科学, 0, (): 1-.

LUO Qiuyun, SUN Jia, LIU Donghui , LI Yongjun, XUE Weina. Effects of active constituents from Polygonum orientale L. on the expression of transporters under physiological and pathological conditions[J]. Shandong Science, 0, (): 1-.

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生理病理状态下荭草活性物质对转运体表达的影响

Effects of active constituents from Polygonum orientale L. on the expression of transporters under physiological and pathological conditions

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