[Human pregnane X receptor-mediated transcriptional regulation of CYP3A4 by extracts of 7 traditional Chinese medicines].
OBJECTIVE
To test whether 7 herbs stimulate human pregnane X receptor (PXR)-mediated CYP3A4 transcription.


METHODS
Transient cotransfection reporter gene assays were performed with human PXR expression plasmids and a reporter plasmid containing the XRES in the CYP3A4 gene promoter in HepG2 cells.


RESULTS
The aqueous extracts of Chrysanthemi Flos, Lycii Fructus, and Salviae Miltiorrhizae Radix et Rhizoma, and the methanol extracts of Chrysanthemi Flos, Crataegi Fructus, Lycii Fructus, Lonicerae Japonicae Flos, Dioscoreae Rhizoma,and Salviae Miltiorrhizae Radix et Rhizoma, activated human PXR-mediated transcription.


CONCLUSIONS
The aqueous extracts of Chrysanthemi Flos, Lycii Fructus, and Salviae Miltiorrhizae Radix et Rhizoma, and the methanol extracts of Chrysanthemi Flos, Crataegi Fructus, Lycii Fructus, Lonicerae Japonicae Flos, Dioscoreae Rhizoma, and Salviae Miltiorrhizae Radix et Rhizoma are inducers of CYP3A4 by activating PXR, and thus may influence the metabolism of other substrates on CYP3A4.
Institute of Nutrition and Food Safety, Zhejiang University, Hangzhou 310058, China.
Yuying
Y
Xu
Yin
Y
Zhang
Fan
F
Zhou
Yifan
Y
Zheng
Xinqiang
X
Zhu
D002460:Cell Line; D031202:Chrysanthemum; D027825:Crataegus; D051544:Cytochrome P-450 CYP3A / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D027742:Dioscorea; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D018014:Gene Transfer Techniques; D017930:Genes, Reporter; D056945:Hep G2 Cells; D006801:Humans; D031239:Lonicera; D032305:Lycium; D008516:Medicine, Chinese Traditional; D010936:Plant Extracts / Q000494:pharmacology*; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D027561:Salvia miltiorrhiza
D004365:Drugs, Chinese Herbal; D010936:Plant Extracts; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D051544:Cytochrome P-450 CYP3A