Identification of human UDP-glucuronosyltransferases involved in I3,II8-biapigenin glucuronidation in Vitro

IF 3.1 3区 医学 Q2 CHEMISTRY, ANALYTICAL Journal of pharmaceutical and biomedical analysis Pub Date : 2025-02-04 DOI:10.1016/j.jpba.2025.116735
Ming Li , Hua Sun , Jin-Ling Song , Xing Sun , Wei Li
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Abstract

I3,II8-biapigenin is a biflavonoid compound with diverse pharmacological effects. The present study aimed to investigate the glucuronidation of I3,II8-biapigenin in the human liver microsomes (HLMs) and recombinant human UDP-glucuronosyltransferases (UGTs). Three glucuronidation metabolites of I3,II8-biapigenin were detected in HLMs. Both recombinant human UGTs and chemical inhibitors studies demonstrated that UGT1A1, UGT1A3, UGT1A9 and UGT1A10 were involved in the glucuronidation of I3,II8-biapigenin. The present investigation provided information for the drug-drug interaction potentials of I3,II8-biapigenin when co-administrated with UGTs inhibitors or inducers.
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参与I3, ii8 -双芹菜素糖醛酸苷化的人udp -葡萄糖醛酸转移酶的体外鉴定
I3, ii8 -双芹菜素是一种具有多种药理作用的类双黄酮化合物。本研究旨在研究I3, ii8 -双芹菜素在人肝微粒体(HLMs)和重组人udp -葡萄糖醛酸糖基转移酶(UGTs)中的糖醛酸化作用。在HLMs中检测到I3、ii8 -双芹菜素三种糖醛酸化代谢物。重组人ugt和化学抑制剂的研究表明,UGT1A1、UGT1A3、UGT1A9和UGT1A10参与了I3、ii8 -双芹菜素的糖醛酸化。本研究为I3, ii8 -双芹菜素与UGTs抑制剂或诱导剂共同给药时的药物-药物相互作用电位提供了信息。
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来源期刊
CiteScore
6.70
自引率
5.90%
发文量
588
审稿时长
37 days
期刊介绍: This journal is an international medium directed towards the needs of academic, clinical, government and industrial analysis by publishing original research reports and critical reviews on pharmaceutical and biomedical analysis. It covers the interdisciplinary aspects of analysis in the pharmaceutical, biomedical and clinical sciences, including developments in analytical methodology, instrumentation, computation and interpretation. Submissions on novel applications focusing on drug purity and stability studies, pharmacokinetics, therapeutic monitoring, metabolic profiling; drug-related aspects of analytical biochemistry and forensic toxicology; quality assurance in the pharmaceutical industry are also welcome. Studies from areas of well established and poorly selective methods, such as UV-VIS spectrophotometry (including derivative and multi-wavelength measurements), basic electroanalytical (potentiometric, polarographic and voltammetric) methods, fluorimetry, flow-injection analysis, etc. are accepted for publication in exceptional cases only, if a unique and substantial advantage over presently known systems is demonstrated. The same applies to the assay of simple drug formulations by any kind of methods and the determination of drugs in biological samples based merely on spiked samples. Drug purity/stability studies should contain information on the structure elucidation of the impurities/degradants.
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