The involvement of multidrug and toxin extrusion protein 1 in the distribution and excretion of berberine
Xiao, Ling1,2; Xue, Yaru1,2; Zhang, Cuifeng1,2; Wang, Le1,2; Lin, Yunfei1,2; Pan, Guoyu1,2
刊名XENOBIOTICA
2018
卷号48期号:3页码:314-323
关键词Berberine MATE1 hepatobiliary distribution excretion DDIs
ISSN号0049-8254
DOI10.1080/00498254.2017.1300707
文献子类Article
英文摘要1. Berberine (BBR), an isoquinoline alkaloid, has demonstrated multiple clinical pharmacological actions. As a substrate of multiple transporters in the liver, BBR is rarely excreted into the bile but can be found in the urine. The purpose of the present study was to investigate the role of multidrug and toxin extrusion protein 1 (MATE1) in the transport of BBR in the liver and kidney. 2. Using human MATE1 (hMATE1)-transfected HEK293 cells, BBR was shown to be a substrate of hMATE1 (K-m = 4.28 +/- 2.18 mu M). In primary rat hepatocytes, pH-dependent uptake and efflux studies suggested that the transport of BBR was driven by the exchange of H+ and involved Mate1. In rats, we found that pyrimethamine (PYR), an inhibitor of Mate1, increased hepatic and renal distribution of BBR and decreased systematic excretion of BBR. 3. These findings indicated that BBR is a substrate of MATE1 and that hepatic and renal Mate1 promote excretion of BBR into bile and urine, respectively. In conclusion, Mate1 plays a key role in the distribution and excretion of BBR, and we speculate that drug-drug interactions (DDIs) caused by MATE1 may occur between BBR and other co-administered drugs.
WOS关键词SANDWICH-CULTURED HEPATOCYTES ; P-GLYCOPROTEIN ; TRANSPORTER PROTEIN ; CATION ANTIPORTERS ; BILIARY-EXCRETION ; DRUG-INTERACTIONS ; RENAL CLEARANCE ; RAT HEPATOCYTES ; ORGANIC CATIONS ; MATE1
WOS研究方向Pharmacology & Pharmacy ; Toxicology
语种英语
出版者TAYLOR & FRANCIS LTD
WOS记录号WOS:000426958800010
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/272328]  
专题药物安全性评价中心
通讯作者Pan, Guoyu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China;
2.Univ Chinese Acad Sci, Beijing, Peoples R China
推荐引用方式
GB/T 7714
Xiao, Ling,Xue, Yaru,Zhang, Cuifeng,et al. The involvement of multidrug and toxin extrusion protein 1 in the distribution and excretion of berberine[J]. XENOBIOTICA,2018,48(3):314-323.
APA Xiao, Ling,Xue, Yaru,Zhang, Cuifeng,Wang, Le,Lin, Yunfei,&Pan, Guoyu.(2018).The involvement of multidrug and toxin extrusion protein 1 in the distribution and excretion of berberine.XENOBIOTICA,48(3),314-323.
MLA Xiao, Ling,et al."The involvement of multidrug and toxin extrusion protein 1 in the distribution and excretion of berberine".XENOBIOTICA 48.3(2018):314-323.
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