ArticleThe Journal of pharmacology and experimental therapeutics2011
Isolation of modulators of the liver-specific organic anion-transporting polypeptides (OATPs) 1B1 and 1B3 from Rollinia emarginata Schlecht (Annonaceae).
Article in The Journal of pharmacology and experimental therapeutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 50 citations in OpenAlex.
- A modified grapefruit juice eliminates two compound classes as major mediators of the grapefruit juice-fexofenadine interaction: an in vitro-in vivo "connect".Journal of clinical pharmacology · 2013Trial
- Ursolic acid: context-dependent redox activity on oxidative stress and its toxicological implications.Archives of toxicology · 2026Review
- G45 and V386 in Transmembrane Domains 1 and 8 Are Critical for the Activation of OATP1B3-Mediated E17βG Uptake by Clotrimazole.Molecular pharmaceutics · 2024Article
- Investigating the interactions of flavonoids with human OATP2B1: inhibition assay, ICRSC medicinal chemistry · 2023Article
- Bioactive Compounds fromLife (Basel, Switzerland) · 2023Review
- Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B.Molecules (Basel, Switzerland) · 2022Article
- The Importance of Val386 in Transmembrane Domain 8 for the Activation of OATP1B3 by Epigallocatechin Gallate.Journal of agricultural and food chemistry · 2022Article
- Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule.Frontiers in pharmacology · 2021Review
- Evaluation of Antiplasmodial Activity of Hydroalcoholic Crude Extract and Solvent Fractions ofInfection and drug resistance · 2021Article
- Article
- A hybrid model to evaluate the impact of active uptake transport on hepatic distribution of atorvastatin in rats.Xenobiotica; the fate of foreign compounds in biological systems · 2020Article
- Gly45 and Phe555 in Transmembrane Domains 1 and 10 Are Critical for the Activation of Organic Anion Transporting Polypeptide 1B3 by Epigallocatechin Gallate.Journal of agricultural and food chemistry · 2019Article
- Evaluation of Antimalarial Activity of Hydromethanolic Crude Extract and Solvent Fractions of the Leaves ofJournal of experimental pharmacology · 2019Article
- The Antimicrobial Activity ofMolecules (Basel, Switzerland) · 2018Article
- Identification of Intestinal UDP-Glucuronosyltransferase Inhibitors in Green Tea (Drug metabolism and disposition: the biological fate of chemicals · 2018Article
- Prioritizing pharmacokinetic drug interaction precipitants in natural products: application to OATP inhibitors in grapefruit juice.Biopharmaceutics & drug disposition · 2017Article
- Identification of Novel Inhibitors of Organic Anion Transporting Polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3) Using a Consensus Vote of Six Classification Models.Molecular pharmaceutics · 2015Article
- Protein Kinase C-Independent Inhibition of Organic Cation Transporter 1 Activity by the Bisindolylmaleimide Ro 31-8220.PloS one · 2015Article
- Cell type-specific delivery of short interfering RNAs by dye-functionalised theranostic nanoparticles.Nature communications · 2014Article
- Herb-drug interactions: challenges and opportunities for improved predictions.Drug metabolism and disposition: the biological fate of chemicals · 2014Article
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4 authors at 2 institutions in 1 country.
Funding
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 that alter transport by one or both of these OATPs could potentially be used to target drugs to hepatocytes or improve the 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 the model substrates estradiol-17β-glucuronide and estrone-3-sulfate. We isolated three compounds, ursolic acid, oleanolic acid, and 8-trans-p-coumaroyloxy-α-terpineol, which inhibited estradiol-17β-glucuronide uptake by OATP1B1 but not OATP1B3. In addition, a rare compound, quercetin 3-O-α-l-arabinopyranosyl(1→2) α-L-rhamnopyranoside, was identified that had distinct effects on each OATP. OATP1B1 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 estrone-3-sulfate was increased (decreased K(m)), whereas the maximal rate of transport (V(max)) was significantly reduced. These results demonstrate a mechanism through which the hepatic uptake of drug OATP substrates could be stimulated.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.