The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1.

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Whitley AC, Sweet DH, Walle T

The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1.

Drug Metab Dispos. 2005 Aug;33(8):1097-100. Epub 2005 May 3.

PubMed ID

15870380 [ View in PubMed

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Abstract

Ellagic acid (EA), a polyphenol present in berries, has been demonstrated to be preventive of esophageal and colon cancer in animals. Here, we have studied the ability of organic anion transporters (OATs) and organic anion-transporting polypeptides (OATPs) to transport EA. The accumulation of radiolabeled (14)C]EA, [(3)H]p-aminohippuric acid (PAH), [(14)C]glutarate, [(3)H]estrone sulfate, [(3)H]ochratoxin A, and [(3)H]taurocholic acid +/- inhibitor(s) was tested in OAT- and OATP-expressing oocytes. Oocytes expressing human (h)OAT1, rat (r)Oat1, and hOAT4 accumulated 6.5-, 7.1-, and 8.9-fold more EA, respectively, than did water-injected oocytes. This accumulation was prevented by the prototype OAT inhibitors bromosulfophthalein and probenecid. rOatp1, mouse (m)Oat2, hOAT3, and mOat5 showed no EA transport. The uptake of the prototype OAT substrate PAH in hOAT1-expressing oocytes was dose dependently and potently inhibited by EA with an IC(50)of 207 nM. In conclusion, we have demonstrated that the OAT family members hOAT1, rOat1, and hOAT4 mediate transport of EA, with a very high affinity for hOAT1.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Ellagic acid	Solute carrier family 22 member 11	Protein	Humans	Unknown	Not Available	Details
Ellagic acid	Solute carrier family 22 member 6	Protein	Humans	Unknown	Substrate Inhibitor	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Ellagic acid	Solute carrier family 22 member 6	IC 50 (nM)	270	N/A	N/A	Details