Interaction of Human Renal Organic Anion Transporter OAT1 and OAT3 with Flavonoids

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An antioxidant effect of the flavonoids in food has been widely noticed as it may prevent the oxidative stress-associated chronic diseases including ischemic heart disease and diabetes mellitus. Flavonoids which are distributed widely in plants are classified into a flavonol, flavanol, flavanone, flavone, isoflavone and anthocyanidin. Of which quercetin, a flavanol, presents ubiquitously as a quercetin glycoside. Most of flavonoids including quercetin which are absorbed in the intestine enter the circulatory blood after they are converted to the conjugated metabolites, and are rapidly eliminated by the kidney into urine. Most studies have focused on the intestinal absorption of the flavonoids which may regulate a physiological function and efficacy of the flavonoids, however their elimination routes at the kidney have remained unknown. This study aims to clarify molecular mechanisms of renal elimination of the flavonoids by inhibiting their transports in view of regulation of their bioavailability in the body. By using the cells stably expressing organic anion transporters 1 (OAT1) and 3 (OAT3) which had been previously established by us, the inhibitory effects of extracellular flavonoids (0.01, 0.1, 1, 10, 100 uM) on the uptake of representative substrates,para-aminohippuric acid(PAH)for OAT1 and estrone sulfate(ES)for OAT3 were investigated. In results, the flavonoids including quercetin, kaempterol, apigenin, luteolin and naringenin inhibited the OAT1 and OAT3-mediated organic anion transports. Inhibitions by genistein and daidzein were only shown in the OAT1 transport and rutin neither inhibited the transport of OAT1 nor OAT3. OAT1 and OAT3 which exist at the basolateral side of the renal proximal tubules are known as the opening site for the uptake of organic anions and the present results suggested OATs may be a renal elimination route for the circulatory flavonoids.

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詳細情報 詳細情報について

  • CRID
    1050001338514561536
  • NII論文ID
    120006491196
  • NII書誌ID
    AA00629581
  • ISSN
    03855023
  • Web Site
    http://id.nii.ac.jp/1199/00001484/
  • 本文言語コード
    en
  • 資料種別
    journal article
  • データソース種別
    • IRDB
    • CiNii Articles

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