Baicalin-induced hepatocyte toxicity:The critical role of multidrug resistance-associated protein 2  

作　　者：Naohiro Oshima Kosuke Kusamori Ryo Takasaki Noriyasu Hada Makiya Nishikawa 

机构地区：[1]Laboratory of Pharmacognosy,Faculty of Pharmaceutical Sciences,Tokyo University of Science,Noda 278-8510,Japan [2]Laboratory of Biopharmaceutics,Faculty of Pharmaceutical Sciences,Tokyo University of Science,Noda 278-8510,Japan

出　　处：《Integrative Medicine Discovery》2025年第1期1-4,共4页

基　　金：supported by the JSPS KAKENHI(Grant Number:JP22K06676)。

摘　　要：Background:Scutellaria root(root of Scutellaria baicalensis),which has potent anti-inflammatory effects,is a component of useful traditional formulaes.Albeit a low frequency,it has been reported to cause severe interstitial pneumonia and liver dysfunction.Importantly,the hepatotoxicity induced by Scutellaria root can be controlled by the baicalin content,one of its major constituents.This study aimed to clarify the role of MRP2 in modulating baicalin-induced cytotoxicity in HepG2 cells,providing insights that inform safer use and assessment of baicalin.Methods:Cytotoxicity of HepG2 and MDCK cells was assessed using a cell counting kit-8 assay in the presence and absence of MK571,an MRP2 inhibitor.MRP2 expression levels were confirmed using agarose gel electrophoresis,and intracellular baicalin concentrations were measured using LC/MS.Results:Baicalin exhibited concentration-dependent cytotoxicity,with higher toxicity observed in MRP2-negative MDCK cells than in MRP2-positive HepG2 cells.Pre-treatment with MK571 increased baicalin-induced cytotoxicity in HepG2 cells and doubled the intracellular baicalin concentration.Conclusion:Our results indicated that MRP2 plays an important role in reducing baicalin-induced hepatocyte toxicity by decreasing intracellular baicalin levels.Monitoring MRP2 activity could serve as a critical predictive biomarker to identify individuals at higher risk of baicalin-induced hepatotoxicity,enabling personalized dosing strategies and minimizing adverse effects associated with Scutellaria root-containing formulae.

关 键 词：BAICALIN MRP2 cytotoxicity HepG2 cells Scutellaria root 

分 类 号：R28[医药卫生—中药学]