Organic anion-transporting polypeptides contribute to the hepatic uptake of berberine
文献类型：期刊论文
| 作者 | Chen, Chen2; Wu, Zhi-Tao1; Ma, Lei-Lei1; Ni, Xuan1; Lin, Yun-Fei1; Wang, Le1; Chen, Ke-Ping2; Huang, Cheng-Gang1 ; Pan, Guoyu1
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| 刊名 | XENOBIOTICA
 |
| 出版日期 | 2015 |
| 卷号 | 45期号:12页码:1138-1146 |
| 关键词 | Berberine organic cation transporter organic anion-transporting polypeptides primary hepatocytes |
| ISSN号 | 0049-8254 |
| DOI | 10.3109/00498254.2015.1042537 |
| 文献子类 | Article |
| 英文摘要 | 1. The purpose of this study was to investigate the mechanism of hepatic uptake of berberine. Berberine accumulation in hepatocytes was found to be highly dependent on active uptake, which could not be explained by liver organic cation transporter (OCT) alone. 2. Our studies indicated that berberine uptake was significantly suppressed by rifampicin, cyclosporine A and glycyrrhizic acid, which act as specific inhibitors of different Oatp isoforms (Oatp1a1, Oatp1a4 and Oatp1b2) in rat hepatocytes. The combination of OCT and OATP inhibitors further reduced berberine accumulation in both rat and human hepatocytes. The uptake of berberine could be increased in human HEK293-OATP1B3 but not in OATP1B1-transfected HEK 293 cells. 3. Rifampicin could reduce the berberine liver extraction ratio (ER) and double its concentration in the effluent in isolated rat livers. Further in vivo study indicated that berberine plasma exposure could be significantly increased by co-administration of the OATP inhibitor rifampicin or the substrate rosuvastatin. 4. In conclusion, this study demonstrated that both OCT and OATP contribute to the accumulation of berberine in the liver. OATPs may have important roles in berberine liver disposition and potential clinically relevant drug-drug interactions. |
| WOS关键词 | DRUG-DRUG INTERACTIONS ; P-GLYCOPROTEIN ; IN-VITRO ; RATS ; BIOAVAILABILITY ; DISPOSITION ; INVOLVEMENT ; METABOLITES ; ABSORPTION ; PLASMA |
| 资助项目 | National Natural Science Foundation of China[81302836] ; Leading Science and Technology Projects[XDA01030600] ; State Key Program of the National Science Foundation of China[81030065] ; Hundred Talents Program of the Chinese Academy of Sciences, Major National Science and Technology Programs[2012ZX09301001-006] ; National High Technology Research and Development Program of China[2013AA032202] |
| WOS研究方向 | Pharmacology & Pharmacy ; Toxicology |
| 语种 | 英语 |
| WOS记录号 | WOS:000369949500011 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276680]  |
| 专题 | 上海中药现代化研究中心 药物安全性评价中心 |
| 通讯作者 | Huang, Cheng-Gang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Jiangsu Univ, Inst Life Sci, Zhenjiang, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Chen, Chen,Wu, Zhi-Tao,Ma, Lei-Lei,et al. Organic anion-transporting polypeptides contribute to the hepatic uptake of berberine[J]. XENOBIOTICA,2015,45(12):1138-1146. |
| APA | Chen, Chen.,Wu, Zhi-Tao.,Ma, Lei-Lei.,Ni, Xuan.,Lin, Yun-Fei.,...&Pan, Guoyu.(2015).Organic anion-transporting polypeptides contribute to the hepatic uptake of berberine.XENOBIOTICA,45(12),1138-1146. |
| MLA | Chen, Chen,et al."Organic anion-transporting polypeptides contribute to the hepatic uptake of berberine".XENOBIOTICA 45.12(2015):1138-1146. |
入库方式： OAI收割
来源：上海药物研究所
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