Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells
2012
Qiu, Feng | Hou, Xiao-Long | Takahashi, Kyoko | Chen, Li-Xia | Azuma, Junichi | Kang, Ning
AIM OF THE STUDY: The aim of this study is to examine the effects of andrographolide on intestinal enzyme cytochrome P450 3A4 (CYP3A4) and predict whether oral administration of andrographolide-containing remedy leads to herb–drug interaction. MATERIALS AND METHODS: Caco-2 cells are treated with 1α, 25-dihydroxyvitamin D3 for 3 wks to induce the expression of CYP3A4, and then andrographolide (1, 10, 100μM) is added and treated for 72h. Upon the further 4-h testosterone (250μM) or nifedipine (200μM) treatment, the basolateral medium samples and the Caco-2 monolayers are collected for analyses. RESULTS: Andrographolide (1, 10, 100μM) significantly down-regulates the mRNA level and protein level of CYP3A4, and inhibits nifedipine oxidation and testosterone 6β-hydroxylation. CONCLUSION: Oral administration of andrographolide likely leads to reduction of the metabolic activity of intestinal CYP3A4, therefore herb preparations containing andrographolide may result to herb–drug interactions in combination therapy.
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