In vitro inhibitory effects of plumbagin, the promising antimalarial candidate, on human cytochrome P450 enzymes
Asian Pacific Journal of Tropical Medicine
;
(12): 914-918, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-951672
ABSTRACT
Objective:
To investigate the propensity of plumbagin to inhibit the three isoforms of human cytochrome P450 (CYP), i.e., CYP1A2, CYP2C19, and CYP3A4 using human liver microsomes in vitro.Methods:
Inhibitory effects of plumbagin on the three human CYP isoforms were investigated using pooled human liver microsomes. Phenacetin O-deethylation, omeprazole hydroxylation and nifedipine oxidation were used as selective substrates for CYP1A2, CYP2C19 and CYP3A4 activities, respectively. Concentrations of paracetamol, 5-hydroxyomeprazole, and oxidized nifedipine were determined in microsomal incubation mixture using high-performance liquid chromatography.Results:
Plumbagin showed significant inhibitory effects on all CYP isoforms, but with the most potent activity on CYP2C19-mediated omeprazole hydroxylation. The IC
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Asian Pacific Journal of Tropical Medicine
Year:
2015
Type:
Article
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