ArticleDrug metabolism and disposition: the biological fate of chemicals2013
Interaction of silymarin flavonolignans with organic anion-transporting polypeptides.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled it.
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Who cites it
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 51 citations in OpenAlex.
- Lipid-lowering statins and polyphenol-based supplementation: a scoping review on drug-food interaction potential.Frontiers in pharmacology · 2025Pooled it
- Article
- Rifampin- and Silymarin-Mediated Pharmacokinetic Interactions of Exogenous and Endogenous Substrates in a Transgenic OATP1B Mouse Model.Molecular pharmaceutics · 2024Article
- Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- Prediction of CYP-mediated silybin A-losartan pharmacokinetic interactions using physiological based pharmacokinetic modeling.Journal of pharmacokinetics and pharmacodynamics · 2022Article
- Pre-incubation with OATP1B1 and OATP1B3 inhibitors potentiates inhibitory effects in physiologically relevant sandwich-cultured primary human hepatocytes.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2021Article
- Chirality Matters: Biological Activity of Optically Pure Silybin and Its Congeners.International journal of molecular sciences · 2021Review
- Multi-factorial pharmacokinetic interactions: unraveling complexities in precision drug therapy.Expert opinion on drug metabolism & toxicology · 2021Review
- Prediction of Drug-Induced Hyperbilirubinemia by In Vitro Testing.Pharmaceutics · 2020Review
- Silymarin and Cancer: A Dual Strategy in Both in Chemoprevention and Chemosensitivity.Molecules (Basel, Switzerland) · 2020Review
- The involvement of human organic anion transporting polypeptides (OATPs) in drug-herb/food interactions.Chinese medicine · 2020Review
- A Pharmacokinetic Natural Product-Disease-Drug Interaction: A Double Hit of Silymarin and Nonalcoholic Steatohepatitis on Hepatic Transporters in a Rat Model.The Journal of pharmacology and experimental therapeutics · 2019Article
- Metabolism, Transport and Drug-Drug Interactions of Silymarin.Molecules (Basel, Switzerland) · 2019Review
- Interaction of soy isoflavones and their main metabolites with hOATP2B1 transporter.Naunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Pretreatment With Rifampicin and Tyrosine Kinase Inhibitor Dasatinib Potentiates the Inhibitory Effects Toward OATP1B1- and OATP1B3-Mediated Transport.Journal of pharmaceutical sciences · 2017Article
- Article
- Downregulation of Organic Anion Transporting Polypeptide (OATP) 1B1 Transport Function by Lysosomotropic Drug Chloroquine: Implication in OATP-Mediated Drug-Drug Interactions.Molecular pharmaceutics · 2016Article
- Pharmacokinetic Interactions between Drugs and Botanical Dietary Supplements.Drug metabolism and disposition: the biological fate of chemicals · 2016Review
- Milk Thistle Constituents Inhibit Raloxifene Intestinal Glucuronidation: A Potential Clinically Relevant Natural Product-Drug Interaction.Drug metabolism and disposition: the biological fate of chemicals · 2015Article
- Silymarin as a Natural Antioxidant: An Overview of the Current Evidence and Perspectives.Antioxidants (Basel, Switzerland) · 2015Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Organic anion-transporting polypeptides (OATPs) are multispecific transporters mediating the uptake of endogenous compounds and xenobiotics in tissues that are important for drug absorption and elimination, including the intestine and liver. Silymarin is a popular herbal supplement often used by patients with chronic liver disease; higher oral doses than those customarily used (140 mg three times/day) are being evaluated clinically. The present study examined the effect of silymarin flavonolignans on OATP1B1-, OATP1B3-, and OATP2B1-mediated transport in cell lines stably expressing these transporters and in human hepatocytes. In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17β-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated. OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC₅₀ values of 1.3, 2.2 and 0.3 µM, respectively), silybin A (IC₅₀ values of 9.7, 2.7 and 4.5 µM, respectively), silybin B (IC₅₀ values of 8.5, 5.0 and 0.8 µM, respectively), and silychristin (IC₅₀ values of 9.0, 36.4, and 3.6 µM, respectively). Furthermore, silymarin, silybin A, and silybin B (100 µM) significantly inhibited OATP-mediated estradiol-17β-glucuronide and rosuvastatin uptake into human hepatocytes. Calculation of the maximal unbound portal vein concentrations/IC₅₀ values indicated a low risk for silymarin-drug interactions in hepatic uptake with a customary silymarin dose. The extent of silymarin-drug interactions depends on OATP isoform specificity and concentrations of flavonolignans at the site of drug transport. Higher than customary doses of silymarin, or formulations with improved bioavailability, may increase the risk of flavonolignan interactions with OATP substrates in patients.
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