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Characterization of the metabolic contributions of cytochrome P450 isoforms to bicyclol using the relative activity factor method.
Luo, Li-Jun; Liu, Xiao; Li, Yan; Li, Yang; Sheng, Li.
Afiliación
  • Luo LJ; State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • Liu X; Department of Drug Metabolism, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • Li Y; Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • Li Y; State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • Sheng L; Department of Drug Metabolism, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
J Asian Nat Prod Res ; 26(8): 918-929, 2024 Aug.
Article en En | MEDLINE | ID: mdl-38629733
ABSTRACT
Bicyclol is a hepatoprotective agent widely used for treating chronic hepatitis and drug-induced liver injuries in clinics. The purpose of the study was to elucidate the contribution of CYP450 enzymes to the metabolism of bicyclol using the relative activity factor approach. After incubation with human liver microsomes and recombinant human liver CYP450 enzymes, the calculated contribution of CYP3A4 and 2C19 to the metabolism of bicyclol was 85.6-90.3% and 9.2-9.7%, respectively. The metabolism was interrupted in the presence of CYP3A4 and 2C19 selective inhibitors. These findings help to predict or avoid metabolic drug-drug interactions or toxicity in clinical applications of bicyclol.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Bifenilo / Microsomas Hepáticos / Sistema Enzimático del Citocromo P-450 Límite: Humans Idioma: En Revista: J Asian Nat Prod Res Asunto de la revista: BOTANICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Bifenilo / Microsomas Hepáticos / Sistema Enzimático del Citocromo P-450 Límite: Humans Idioma: En Revista: J Asian Nat Prod Res Asunto de la revista: BOTANICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido