[Transcriptional regulation of cytochrome P450 3A4 by four kinds of traditional Chinese medicines].
OBJECTIVE
To screen a group of traditional Chinese medicines with effect on pregnane X receptor (PXR)-mediated transcription regulation of P450 3A4 (CYP3A4); and to study whether they can induce the expression of CYP3A4 with a dose, time-dependent manner.


METHODS
Transient cotransfection reporter gene assays were performed with pCI-hPXR-neo, pGL3-CYP3A4-Luc and beta-galactosidase expression plasmid in HepG2 cells.


RESULTS
Rhizoma Curcumae, Atractylodes lancea, A. macrocaphala and Poria cocos could induce transcriptional expression of CYP3A4. In the dose-effect study, 24 h after induction, 500 mg x L(-1) Rhizoma Curcumae, A. lancea, A. macrocaphala and Poria cocos, respectively, could induce the CYP3A4 gene expression with (6.82 +/- 0.09), (6.76 +/- 0.20), (5.49 +/- 0.13) and (4.97 +/- 0.07) folds, as compared with 0.1% DMSO treated cells. In the time-effect study, 500 mg x L(-1) Rhizoma curcumae, A. lancea, A. macrocaphala and Poria cocos for 48 h could induce the CYP3A4 gene expression with (7.74 +/- 0.54), (7.34 +/- 0.10), (5.54 +/- 0.11) and (5.32 +/- 0.18) folds, compared with 0.1% DMSO treated cells.


CONCLUSIONS
Rhizoma Curcumae, A. lancea, A. macrocaphala and Poria cocos could induce the expression of CYP3A4 gene transcription through activating PXR.
Dong
Hai-Yan
HY
Institute of Pharmaceutical Biotechnology and Bioengineering, Fuzhou University 350002, China.
Shao
Jing-Wei
JW
Chen
Jian-Feng
JF
Wang
Tao
T
Lin
Feng-Ping
FP
Guo
Yang-Hao
YH
D045744:Cell Line, Tumor; D051544:Cytochrome P-450 CYP3A / Q000235:genetics*; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D006801:Humans; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000378:metabolism; D014158:Transcription, Genetic / Q000187:drug effects*
D004365:Drugs, Chinese Herbal; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human