期刊
FITOTERAPIA
卷 89, 期 -, 页码 80-85出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2013.05.019
关键词
Rhinacanthin-C; Naphthoquinone; P-glycoprotein; MRP2; Caco-2 cells
资金
- 90th Anniversary of Chulalongkorn University Fund (Ratchadaphiseksomphot Endowment Fund)
- Higher Education Research Promotion
- National Research University Project of Thailand, Office of the Higher Education Commission [AS638A-56]
Rhinacanthin-C is a bioactive naphthoquinone ester found in Rhinacanthus nasutus Kurz (Acanthaceae). This compound has potential therapeutic value as an anticancer and antiviral agent. The purposes of this study were to determine the effects of this compound on the function and the expression of P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (MRP2), using the in vitro model of Caco-2 cells. The activities of P-gp and MRP2 were determined by following the intracellular accumulation of calcein and 5(6)-carboxy-2',7'-dichlorofluorescein in the uptake assays with fluorescence spectroscopy. The expression of P-gp after prolonged exposure was evaluated by flow cytometry with the use of a fluorescein isothiocyanate-conjugated anti-human P-gp antibody. Our results showed that the inhibitory effect of rhinacanthin-C was more potent toward P-gp than MRP2, and was reversible. Short-term exposure of Caco-2 cells with rhinacanthin-C (100 mu M) resulted in increase in P-gp expression without any significant change in its function. Extended exposure of Caco-2 cells to the naphthoquinone at the highest non-cytotoxic concentration (0.625 mu M) for 7 days had no effect on the expression and the function of P-gp. These findings suggested that rhinacanthin-C might raise the problem of herb-drug interaction when co-administered with other P-gp substrates. (c) 2013 Elsevier B.V. All rights reserved.
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