期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 68, 期 48, 页码 14182-14191出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.0c06132
关键词
OATP1A2; OATP2B1; grapefruit juice; jabara juice; food-drug interaction
资金
- Japan Research Foundation through JSPS Kakenhi [19K07173, 18K06758]
- Over the Counter (OTC) Self-Medication Promotion Foundation
- Keio University
- Grants-in-Aid for Scientific Research [19K07173, 18K06758] Funding Source: KAKEN
Organic anion-transporting polypeptides (OATPs) 1A2 and OATP2B1 are expressed in the small intestine and are involved in drug absorption. We identified narirutin, which is present in grapefruit juice, as a novel OATP inhibitor. The citrus fruit jabara also contains high levels of narirutin; therefore, we investigated the inhibitory potency of jabara juice against OATPs. The inhibitory effects of various related compounds on the transport activity of OATPs were evaluated using OATP-expressing HEK293 cells. The IC50 values of narirutin for OATP1A2- and OATP2B1-mediated transport were 22.6 and 18.2 mu M, respectively. Other flavanone derivatives from grapefruit juice also inhibited OATP1A2/OATP2B1-mediated transport (order of inhibitory potency: naringenin > narirutin > naringin). Five percent jabara juice significantly inhibited OATP1A2- and OATP2B1-mediated transport by 67 +/- 11 and 81 +/- 5.5%, respectively (p < 0.05). Based on their inhibitory potency and levels in grapefruit juice, the inhibition of OATPs by grapefruit juice is attributable to both naringin and narirutin. Citrus x jabara, which contains narirutin, potently inhibits OATP-mediated transport.
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