Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells

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• 作者：Feng Qiu^a ; ¹ ; ^{fengqiu2000@tom.com} ; ^{fengqiu20070118@163.com} ; Xiao-Long Hou^b ; ¹ ; Kyoko Takahashi^c ; Li-Xia Chen^a ; Junichi Azuma^b ; Ning Kang^d
• 关键词：Andrographolide ; CYP3A4 ; Caco-2 ; 1伪 ; 25-dihydroxyvitamin D3
• 刊名：Journal of Ethnopharmacology
• 出版年：2012
• 期刊代码：26_03788741
• 类别：pha
• 出版时间：1 June, 2012
• 卷：141
• 期：2
• 页码：709-713
• 文件大小：359 K

摘要

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 1伪, 25-dihydroxyvitamin D3 for 3 wks to induce the expression of CYP3A4, and then andrographolide (1, 10, 100 渭M) is added and treated for 72 h. Upon the further 4-h testosterone (250 渭M) or nifedipine (200 渭M) treatment, the basolateral medium samples and the Caco-2 monolayers are collected for analyses.

Results

Andrographolide (1, 10, 100 渭M) significantly down-regulates the mRNA level and protein level of CYP3A4, and inhibits nifedipine oxidation and testosterone 6尾-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.