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Citrus Fruit-Derived Flavanone Glycoside Narirutin is a Novel Potent Inhibitor of Organic Anion-Transporting Polypeptides.

Research paper by Tokio T Morita, Takeshi T Akiyoshi, Ryo R Sato, Yoshinori Y Uekusa, Kazuhiro K Katayama, Kodai K Yajima, Ayuko A Imaoka, Yoshikazu Y Sugimoto, Fumiyuki F Kiuchi, Hisakazu H Ohtani

Indexed on: 21 Nov '20Published on: 20 Nov '20Published in: Journal of Agricultural and Food Chemistry



Abstract

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 IC values of narirutin for OATP1A2- and OATP2B1-mediated transport were 22.6 and 18.2 μM, 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 ( < 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. , which contains narirutin, potently inhibits OATP-mediated transport.