[Effects of Rhaponticum uniflorum on activity and mRNA expression of CYP3A1 in rats hepatocytes].
OBJECTIVE
To study effects of Rhaponticum uniflorum on the activities and mRNA expression of cytochrome P4503A1 in rats hepatocytes.


METHODS
Rat hepatocytes sandwich cultures were treated by Rhaponticum uniflorum in different concentrations (15.6, 31.2, 62.4 mg/ml) for 48 hours. The enzymic activities of CYP3A1 were reflected by the activities of liver microsomal erythromyeine N-demethylase (ERD). The level change in the mRNA expression were tested by RT-PCR.


RESULTS
After treatment with the medicine, there was concentration-dependent inhibition in both enzymic activity and mRNA level of CYP3A1 compared with the control. The rates of the inhibitory effect to CYP3A1 activity were 26.4%, 44.2% and 65.4% respectively, while those of the inhibitory effect to mRNA level were 29.4%, 49.8% and 56.0%.


CONCLUSIONS
Rhaponticum uniflorum inhibits the enzymic activity of CYP3A1 and lowers CYP3A1 expression at the transcriptive levels.
Wu
Ning
N
Bio-chemistry & Molecular Biology Teaching and Research Section, Guiyang Medical College, Guiyang 550004, China. wuninggy@126.com
Lei
Ting-wen
TW
Li
Hong-mei
HM
Wu
Qing-qing
QQ
Tang
Liang-hua
LH
D000818:Animals; D001189:Aryl Hydrocarbon Hydroxylases / Q000235:genetics* / Q000378:metabolism; D002478:Cells, Cultured; D051544:Cytochrome P-450 CYP3A; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005260:Female; D015971:Gene Expression Regulation, Enzymologic / Q000187:drug effects; D022781:Hepatocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D043843:Leuzea / Q000737:chemistry*; D008297:Male; D010946:Plants, Medicinal / Q000737:chemistry; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D020133:Reverse Transcriptase Polymerase Chain Reaction
D004365:Drugs, Chinese Herbal; D012333:RNA, Messenger; D001189:Aryl Hydrocarbon Hydroxylases; C465138:Cyp3a23-3a1 protein, rat; D051544:Cytochrome P-450 CYP3A