CAJ | 학술논문

人参皂苷F1通过激活孕烷X受体诱导CYP3 A4的表达
인삼조감F1통과격활잉완X수체유도CYP3 A4적표체
Ginsenoside F1 induces CYP3 A4 expression through activation of human pregnane X receptor

万方数据

中国药理学通报中國藥理學通報 중국약이학통보
Chinese Pharmacological Bulletin
2015年 11期 1536-1539,1540 ,共5页

油文亭%周涛%马增春%梁乾德%汤响林%肖成荣%谭洪玲%肖勇%王宇光%高月

유문정%주도%마증춘%량건덕%탕향림%초성영%담홍령%초용%왕우광%고월

人参皂苷 F1%PXR%CYP3A4%荧光实时定量 PCR%mRNA%酶活性人參皂苷 F1%PXR%CYP3A4%熒光實時定量 PCR%mRNA%酶活性
인삼조감 F1%PXR%CYP3A4%형광실시정량 PCR%mRNA%매활성
ginsenoside F1%PXR%CYP3 A4%quanti-tative PCR%mRNA%enzyme activity

目的：探索人参皂苷F1( ginsenoside F1)是否通过激活孕烷X受体(PXR)实现对CYP3A4基因表达及酶活性的诱导作用。方法利用本实验室构建的PXR-CYP3A4稳定转染HepG2工程细胞株结合荧光素酶报告基因技术，检测人参皂苷F1对PXR的转录激活效应；用不同浓度的人参皂苷F1处理LS174T细胞，并通过Q-PCR和酶活性试剂盒检测CYP3A4的mRNA表达和酶活性变化。结果不同浓度人参皂苷F1作用于LS174T细胞以后，可以浓度依赖性地诱导CYP3A4 mRNA 水平的表达，并且增强其酶活性；同时， PXR-CYP3A4稳定转染HepG2工程细胞株结合荧光素酶报告基因检测结果亦表明，人参皂苷F1能够浓度依赖性地增强PXR的转录激活效应。结论本研究揭示了人参皂苷F1可诱导CYP3A4的基因表达并增强其酶活性，这一过程可能与人参皂苷F1对孕烷X受体的激活有关。
목적：탐색인삼조감F1( ginsenoside F1)시부통과격활잉완X수체(PXR)실현대CYP3A4기인표체급매활성적유도작용。방법이용본실험실구건적PXR-CYP3A4은정전염HepG2공정세포주결합형광소매보고기인기술，검측인삼조감F1대PXR적전록격활효응；용불동농도적인삼조감F1처리LS174T세포，병통과Q-PCR화매활성시제합검측CYP3A4적mRNA표체화매활성변화。결과불동농도인삼조감F1작용우LS174T세포이후，가이농도의뢰성지유도CYP3A4 mRNA 수평적표체，병차증강기매활성；동시， PXR-CYP3A4은정전염HepG2공정세포주결합형광소매보고기인검측결과역표명，인삼조감F1능구농도의뢰성지증강PXR적전록격활효응。결론본연구게시료인삼조감F1가유도CYP3A4적기인표체병증강기매활성，저일과정가능여인삼조감F1대잉완X수체적격활유관。
Aim To study the effect of ginsenoside F1 on the enzyme activity and expression of gene of CYP3 A4 through activation of pregnane X receptor ( PXR ) . Methods With different concentrations of ginsenoside F1 treated on LS174T cells, the expression of CYP3A4 mRNA was determined by Q-PCR, and the enzyme activity was measured by P450-GloTM CYP3A4 assay according to the manufacturer′s instructions, fur-ther PXR-CYP3 A4 stable translation HepG2 cell lines were used to test ginsenoside F1 activates PXR by re-porter gene screening assay. Results The results re-vealed that the levels of CYP3 A4 gene and protein ex-pression were significantly increased by ginsenoside F1 in a concentration-dependent manner. At the same time, reporter gene screening showed that ginsenoside F1 could also enhance the transcriptional activity of PXR. Conclusion Ginsenoside F1 can significantly up-regulate the gene expression and enzyme activity of CYP3A4 via the PXR-CYP3A4 pathway.