ArticleFrontiers in pharmacology2018
Baicalein Enhances the Oral Bioavailability and Hepatoprotective Effects of Silybin Through the Inhibition of Efflux Transporters BCRP and MRP2.
Article in Frontiers in pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 37 citations in OpenAlex.
- Integrative Medicine for Liver Fibrosis: Bioactive Constituents and Therapeutic Potential of Scutellaria baicalensis.Chinese journal of integrative medicine · 2026Review
- Silymarin as a phytopharmaceutical agent: advances in mechanistic insights, formulation strategies, and pre-clinical applications.Frontiers in pharmacology · 2025Review
- A critical review of natural products driven correction of bile acid dysregulation: a therapeutic strategy for nonalcoholic fatty liver disease.Frontiers in pharmacology · 2025Review
- Bioactive Compounds Formulated in Phytosomes Administered as Complementary Therapy for Metabolic Disorders.International journal of molecular sciences · 2024Review
- Novel Strategies Enhancing Bioavailability and Therapeutical Potential of Silibinin for Treatment of Liver Disorders.Drug design, development and therapy · 2024Review
- Bovine Serum Albumin Nanoparticles Enhanced the Intranasal Bioavailability of Silybin in Rats.Pharmaceutics · 2023Article
- Baicalin provides protection against fluoxetine-induced hepatotoxicity by modulation of oxidative stress and inflammation.World journal of hepatology · 2022Article
- Protective effect of the curcumin-baicalein combination against macrovascular changes in diabetic angiopathy.Frontiers in endocrinology · 2022Article
- Hepatic organic anion transporting polypeptides mediate disposition of milk thistle flavonolignans and pharmacokinetic silymarin-drug interactions.Phytotherapy research : PTR · 2021Article
- Baicalin Enhanced Oral Bioavailability of Sorafenib in Rats by Inducing Intestine Absorption.Frontiers in pharmacology · 2021Article
- Baicalein Neutralizes Hypercholesterolemia-Induced Aggravation of Oxidative Injury in Rats.International journal of medical sciences · 2020Article
- Metabolism, Transport and Drug-Drug Interactions of Silymarin.Molecules (Basel, Switzerland) · 2019Review
- Elucidation of the Differences in Cinobufotalin's Pharmacokinetics Between Normal and Diethylnitrosamine-Injured Rats: The Role of P-Glycoprotein.Frontiers in pharmacology · 2019Article
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Although hepatoprotective properties of silybin are well documented, the clinical therapeutic efficacy is limited by its low bioavailability due to absorption rates, extensive phase II metabolism, and biliary excretion. As our previous study indicated that metabolic enzymes may have limited effects on the pharmacokinetic (PK) behavior of silymarin, here, we intended to increase the oral bioavailability and bio-efficacy of silybin through the inhibition of active efflux. In Caco-2 and transfected MDCKII cell models, flavone baicalein significantly inhibited the efflux of silybin as a BCRP and MRP2 inhibitor. In addition, baicalein reduced the biliary excretion index (BEI) and biliary clearance of silybin conjugates in the sandwich-cultured rat hepatocyte (SCH) model, indicating the inhibition of baicalein in biliary excretion of conjugated silybin metabolites. PK study demonstrated that baicalein significantly increased the area under the curve (AUC) and C
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