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Abstract Title:Schisandrol B protects against cholestatic liver injury through pregnane X receptors.
Abstract来源:
br j Pharmacol。 2017 04; 174(8):672-688。 EPUB 2017 3月16日。PMID: 28128437 Fan,Dongshun Li,瞄准Liu,Ma,Wen Xie,Peiqing Liu,Frank J Gonzalez,Min Huang,Huichang Bi
文章隶属关系:Hang Zeng
摘要:
实验方法: hepatopoteriation solb solb对肠内杂物的肝动物效应,造成肠内cho虫(lithochocic cholestation),由脂肪酸(LCA)诱导。代谢组分析和基因分析用于评估妊娠X受体(PXR)的参与。 Molecular docking, cell-based reporter gene analysis and knockout mice were used to demonstrate the critical role of the PXR pathway in the anti-cholestasis effects of SolB.
KEY RESULTS: SolB protected against LCA-induced intrahepatic cholestasis.此外,用SOLB治疗的治疗降低了胆固性小鼠的死亡率。代谢组学和基因分析表明,SOLB加速了胆汁酸的代谢,促进了胆汁酸排出液,并诱导了涉及PXR-Target基因CYP3A11,UGT1A1和OATP2的肝表达,这些表达涉及的肝脏表达在胆汁酸稳态中。机械研究表明,SOLB激活了人类细胞系中的人类PXR和上调的PXR靶基因。 Additionally, SolB did not protect Pxr-null mice from liver injury induced by intrahepatic cholestasis, thus providing genetic evidence that the effect of SolB was PXR-dependent.
CONCLUSION AND IMPLICATIONS: These findings provide direct evidence for the hepatoprotective effects of SolB against cholestasis by激活PXR。因此,SOLB可以为预防和治疗胆固性肝病提供一种新的有效方法。