中国中药杂志

2015, v.40(17) 3444-3449

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以PXR受体为靶点的中药活性成分筛选及相关药理学研究
Pharmacology research on PXR as a potential target in screening bioactive components of Chinese material medica

王宇光;张娴勰;李晗;陆倍倍;周建明;刘浩生;胡东华;周涛;张亚欣;马增春;梁乾德;汤响林;肖成荣;谭洪玲;高月;
WANG Yu-guang;ZHANG Xian-xie;LI Han;LU Bei-bei;ZHOU Jian-ming;LIU Hao-sheng;HU Dong-hua;ZHOU Tao;ZHANG Ya-xin;MA Zeng-chun;LIANG Qian-de;TANG Xiang-lin;XIAO Cheng-rong;TAN Hong-ling;GAO Yue;Beijing Institute of Radiation Medicine;Tianjin University of Traditional Chinese Medicine;Anhui Medical University;Guangxi Medical University;

摘要(Abstract):

孕烷X受体(PXR)作为关键的转录因子调控CYP3A基因的诱导表达,在分子水平上揭示了PXR保护机体免受外源性物质的机制,同时也揭示了一类最主要的药物相互作用模式。PXR除了在药物代谢及药物相互作用中扮演重要角色外,越来越多的研究显示PXR及其调控的靶基因在维持机体内环境稳态,发挥重要生理功能方面扮演重要角色。因此有必要研究中药及天然产物对PXR调节及相关药理作用研究,为挖掘新的药理作用途径提供新的线索,该文就PXR研究进展及本实验室近年来的开展的相关工作进行综述。
Pregnane X receptor( PXR) is key transcription factors which mainly regulate the expression of CYP3 A genes. At the molecular level,PXR has been revealed the protection mechanism of the body against xenochemicals and a major mode of the drug-drug interactions. Besides playing an important role in drug metabolism and interactions,PXR and its target genes also play an important role in maintaining normal physiological function and homeostasis. Therefore,it is necessary to study the regulation of PXR and its related pharmacological effects of TCM and natural products,and to provide new clues for the new pharmacological pathway.

关键词(KeyWords): 孕烷X受体;细胞色素P450 3A;石胆酸;溃疡性结肠炎
pregnane X receptor;CYP3A;lithocholic acid;ulcerative colitis

Abstract:

Keywords:

基金项目(Foundation): 国家“重大新药创制”科技重大专项(2009ZX09501-304);; 国家重点基础研究发展计划(973)项目(2011CB505304,2012CB518402)

作者(Authors): 王宇光;张娴勰;李晗;陆倍倍;周建明;刘浩生;胡东华;周涛;张亚欣;马增春;梁乾德;汤响林;肖成荣;谭洪玲;高月;
WANG Yu-guang;ZHANG Xian-xie;LI Han;LU Bei-bei;ZHOU Jian-ming;LIU Hao-sheng;HU Dong-hua;ZHOU Tao;ZHANG Ya-xin;MA Zeng-chun;LIANG Qian-de;TANG Xiang-lin;XIAO Cheng-rong;TAN Hong-ling;GAO Yue;Beijing Institute of Radiation Medicine;Tianjin University of Traditional Chinese Medicine;Anhui Medical University;Guangxi Medical University;

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