Vitamin D Receptor-Mediated Upregulation of CYP3A4 and MDR1 by Quercetin in Caco-2 Cells
- Authors
- Chae, Yoon-Jee; Cho, Kwan Hyung; Yoon, In-Soo; Noh, Chi-Kyoung; Lee, Hyo-Jong; Park, Yohan; Ji, Eunhee; Seo, Min-Duk; Maeng, Han-Joo
- Issue Date
- Jan-2016
- Publisher
- GEORG THIEME VERLAG KG
- Keywords
- multidrug resistance protein 1; P-glycoprotein; cytochrome P450 3A4; Caco-2 cells; quercetin; 1 alpha,25-dihydroxyvitamin D-3 (1,25(OH)(2)D-3); vitamin D receptor
- Citation
- PLANTA MEDICA, v.82, no.1-2, pp.121 - 130
- Journal Title
- PLANTA MEDICA
- Volume
- 82
- Number
- 1-2
- Start Page
- 121
- End Page
- 130
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/8694
- DOI
- 10.1055/s-0035-1557898
- ISSN
- 0032-0943
- Abstract
- To examine whether quercetin interacts with vitamin D receptor, we investigated the effects of quercetin on vitamin D receptor activity in human intestinal Caco-2 cells. The effects of quercetin on the expression of the vitamin D receptor target genes, vitamin D-3 24-hydroxylase, cytochrome P450 3A4, multidrug resistance protein 1, and transient receptor potential vanilloid type 6 were measured using quantitative polymerase chain reaction. The vitamin D receptor siRNA was used to assess the involvement of the vitamin D receptor. Vitamin D receptor activation using a vitamin D responsive element-mediated cytochrome P450 3A4 reporter gene assay was investigated in Caco-2 cells transfected with human vitamin D receptor. We also studied the magnitude of the vitamin D receptor activation and/or synergism between 1 alpha,25-dihydroxyvitamin D-3 [1,25(OH)(2)D-3] and quercetin-like flavonoids. Slight but significant increases in the mRNA expression of cytochrome P450 3A4, vitamin D3 24-hydroxylase, multidrug resistance protein 1, and transient receptor potential vanilloid type 6 were observed after 3 days of continual quercetin treatment. The silencing effect of vitamin D receptor by vitamin D receptor siRNA in Caco-2 cells significantly attenuated the induction of the vitamin D receptor target genes. Moreover, quercetin significantly enhanced cytochrome P450 3A4 reporter activity in Caco-2 cells in a dose-dependent manner, and the expression of exogenous vitamin D receptor further stimulated the vitamin D receptor activity. Quercetin-like flavonoids such as kaempferol stimulated the vitamin D receptor activity in a manner similar to that seen with quercetin. Taken together, the data indicates that quercetin upregulates cytochrome P450 3A4 and multidrug resistance protein 1 expression in Caco-2 cells likely via a vitamin D receptor-dependent pathway.
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