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- W2296371837 abstract "Organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3) are liver specific transporters that mediate the uptake of a broad range of drugs into hepatocytes, including statins, antibiotics and many anticancer drugs. Compounds which alter transport by one or both of these OATPs could potentially be used to target drugs to hepatocytes or to improve bioavailability of drugs that are cleared by the liver. In this study, we applied a bioassay guided isolation approach to identify such compounds from the organic extract of Rollinia emarginata Schlecht (Annonaceae). Fractions of the plant extract were screened for effects on OATP1B1- and OATP1B3-mediated transport of 0.1 μM estrone-3-sulfate and estradiol-17β-glucuronide. A rare compound, quercetin 3-O-α-l-arabinopyranosyl(1→2) α-l-rhamnopyranoside, was isolated that had distinct effects on each OATP. OATP1B1-mediated transport of both model substrates was strongly inhibited, as was OATP1B3-mediated transport of estradiol-17β-glucuronide. However, OATP1B3-mediated uptake of estrone-3-sulfate was stimulated 4- to 5-fold. Kinetic analysis of this stimulation revealed that the apparent affinity for substrate was increased (Km reduced from 100μM to 10μM), while the Vmax was significantly reduced. These results demonstrate a mechanism through which the hepatic uptake of drug OATP substrates could be stimulated." @default.
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- W2296371837 date "2010-04-01" @default.
- W2296371837 modified "2023-09-27" @default.
- W2296371837 title "Isolation of a modulator of the liver specific Organic Anion Transporting Polypeptides (OATPs) 1B1 and 1B3 from Rollinia emarginata Schlecht (Annonaceae)" @default.
- W2296371837 doi "https://doi.org/10.1096/fasebj.24.1_supplement.758.7" @default.
- W2296371837 hasPublicationYear "2010" @default.
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