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

Tokio Morita, Takeshi Akiyoshi, Ryo Sato, Yoshinori Uekusa, Kazuhiro Katayama, Kodai Yajima, Ayuko Imaoka, Yoshikazu Sugimoto, Fumiyuki Kiuchi, Hisakazu Ohtani

Research output: Contribution to journalArticlepeer-review

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 IC50 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 (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 × jabara, which contains narirutin, potently inhibits OATP-mediated transport.

Original languageEnglish
Pages (from-to)14182-14191
Number of pages10
JournalJournal of agricultural and food chemistry
Volume68
Issue number48
DOIs
Publication statusPublished - 2020 Dec 2

Keywords

  • OATP1A2
  • OATP2B1
  • food-drug interaction
  • grapefruit juice
  • jabara juice

ASJC Scopus subject areas

  • Chemistry(all)
  • Agricultural and Biological Sciences(all)

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