Inhibitory Effects of Cranberry Juice and Its Components on Intestinal OATP1A2 and OATP2B1: Identification of Avicularin as a Novel Inhibitor

Tokio Morita, Takeshi Akiyoshi, Toshiaki Tsuchitani, Hiroki Kataoka, Naoya Araki, Kodai Yajima, Kazuhiro Katayama, Ayuko Imaoka, Hisakazu Ohtani

研究成果: Article査読

抄録

Organic anion-transporting polypeptide (OATP) 1A2 and OATP2B1 mediate the intestinal absorption of drugs. This study aimed to identify fruit juices or fruit juice components that inhibit OATPs and assess the risk of associated food-drug interactions. Inhibitory potency was assessed by examining the uptake of [3H]estrone 3-sulfate and [3H]fexofenadine into HEK293 cells expressing OATP1A2 or OATP2B1. In vivo experiments were conducted using mice to evaluate the effects of cranberry juice on the pharmacokinetics of orally administered fexofenadine. Of eight examined fruit juices, cranberry juice inhibited the functions of both OATPs most potently. Avicularin, a component of cranberry juice, was identified as a novel OATP inhibitor. It exhibited IC50values of 9.0 and 37 μM for the inhibition of estrone 3-sulfate uptake mediated by OATP1A2 and OATP2B1, respectively. A pharmacokinetic experiment revealed that fexofenadine exposure was significantly reduced (by 50%) by cranberry juice. Cranberry juice may cause drug interactions with OATP substrates.

本文言語English
ページ(範囲)3310-3320
ページ数11
ジャーナルJournal of agricultural and food chemistry
70
10
DOI
出版ステータスPublished - 2022 3月 16

ASJC Scopus subject areas

  • 化学 (全般)
  • 農業および生物科学(全般)

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