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1051264 
Journal Article 
In vitro determination of the effect of Andrographis paniculata extracts and andrographolide on human hepatic cytochrome P450 activities 
Pan, Y; Abd-Rashid, BA; Ismail, Z; Ismail, R; Mak, JW; Pook, PC; Er, HM; Ong, CE 
2011 
Yes 
Journal of Natural Medicines
ISSN: 1340-3443
EISSN: 1861-0293 
65 
3-4 
440-447 
English 
21365364 
WOS:000291746900005 
We investigated the effects of Andrographis paniculata (AP) extracts and andrographolide on the catalytic activity of three human cDNA-expressed cytochrome P450 enzymes: CYP2C9, CYP2D6 and CYP3A4. In vitro probe-based high performance liquid chromatography assays were developed to determine CYP2C9-dependent tolbutamide methylhydroxylation, CYP2D6-dependent dextromethorphan O-demethylation and CYP3A4-dependent testosterone 6β-hydroxylation activities in the presence and absence of AP extracts and andrographolide. Our results indicate that AP ethanol and methanol extracts inhibited CYP activities more potently than aqueous and hexane extracts across the three isoforms. Potent inhibitory effects were observed on CYP3A4 and CYP2C9 activities (K (i) values below 20 μg/ml). Andrographolide was found to exclusively but weakly inhibit CYP3A4 activity. In conclusion, data presented in this study suggest that AP extracts have the potential to inhibit CYP isoforms in vitro. There was, however, variation in the potency of inhibition depending on the extracts and the isoforms investigated. 
Andrographis paniculata; Acanthaceae; Andrographolide; Cytochrome P450; In vitro; Drug-herb interaction 
IRIS
• Methanol (Non-Cancer)
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