ArticleEuropean journal of drug metabolism and pharmacokinetics2017
Catechol-O-Methyltransferase and UDP-Glucuronosyltransferases in the Metabolism of Baicalein in Different Species.
Article in European journal of drug metabolism and pharmacokinetics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 32 citations in OpenAlex.
- Research Progress on the Antidepressant Effects of Baicalin and Its Aglycone Baicalein: A Systematic Review of the Biological Mechanisms.Neurochemical research · 2024Pooled it
- Preparation, immunological and pharmacological effects of flavonoids in Scutellariae radix: a review.Frontiers in pharmacology · 2025Review
- Exploring the Cardiovascular Protective Effects of Baicalin: A Pathway to New Therapeutic Insights.Current topics in medicinal chemistry · 2025Review
- Pharmacological properties of Polygonatum and its active ingredients for the prevention and treatment of cardiovascular diseases.Chinese medicine · 2024Review
- The Pharmacological Efficacy of Baicalin in Inflammatory Diseases.International journal of molecular sciences · 2023Review
- Baicalein as Promising Anticancer Agent: A Comprehensive Analysis on Molecular Mechanisms and Therapeutic Perspectives.Cancers · 2023Review
- Comparative Evaluation of the Antiglycation and Anti-α-Glucosidase Activities of Baicalein, Baicalin (Baicalein 7-Pharmaceutics · 2022Article
- Identification of herbal components as TRPA1 agonists and TRPM8 antagonists.Journal of natural medicines · 2021Article
- Discovery and characterization of naturally occurring potent inhibitors of catechol-RSC advances · 2021Article
- Classical Active Ingredients and Extracts of Chinese Herbal Medicines: Pharmacokinetics, Pharmacodynamics, and Molecular Mechanisms for Ischemic Stroke.Oxidative medicine and cellular longevity · 2021Review
- Regulatory Mechanisms of Baicalin in Cardiovascular Diseases: A Review.Frontiers in pharmacology · 2020Review
- Pharmacokinetics of B-Ring Unsubstituted Flavones.Pharmaceutics · 2019Review
- Pharmacokinetics and Bioavailability Enhancement of Baicalin: A Review.European journal of drug metabolism and pharmacokinetics · 2019Review
- Potential therapeutic effects of baicalin and baicalein.Avicenna journal of phytomedicineReview
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundBaicalein is the major bioactive flavonoid in some herb medicines and dietary plants; however, the detailed metabolism pathway of its major metabolite oroxylin A-7-O-β-D-glucuronide in human was not clear. It was important to illustrate the major metabolic enzymes that participate in its elimination for the clinic use of baicalein.
objectivesWe first revealed a two-step metabolism profile for baicalein and illustrated the combination of catechol-O-methyltransferase (COMT) and uridine diphosphate-glucuronosyltransferases (UGTs) in drug metabolism, further evaluated its bioactivity variation during drug metabolism.
methodsThe metabolism profiles were systematically characterized in different human biology preparations; after then, the anti-inflammatory activities of metabolites were evaluated in LPS-induced RAW264.7 cell.
resultsThe first-step metabolite of baicalein was isolated and identified as oroxylin A; soluble-bound COMT (S-COMT) was the major enzyme responsible for its biotransformation. Specially, position 108 mutation of S-COMT significantly decreases the elimination. Meantime, oroxylin A was rapidly metabolized by UGTs, UGT1A1, -1A3, -1A6, -1A7, -1A8, -1A9, and -1A10 which were involved in the glucuronidation. Considerable species differences were observed with 1060-fold K
conclusionThe detailed kinetic parameters indicated that COMT provide convenience for the next glucuronidation; monkey would be a preferred animal model for the preclinical investigation of baicalein. Importantly, oroxylin A should be reconsidered in evaluating baicalein efficacy against inflammatory diseases.
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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.