ArticleEuropean journal of drug metabolism and pharmacokinetics
Metabolic assessment in liver microsomes by co-activating cytochrome P450s and UDP-glycosyltransferases.
Article in European journal of drug metabolism and pharmacokinetics. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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6 citing papers in PubMed, 33 citations in OpenAlex.
- Biosynthesis and Identification of Clenbuterol Metabolites in Urine and In Vitro Microsome Incubation Samples Using UHPLC-Q-Exactive Orbitrap Mass Spectrometry: A Comparison Between Human and Bovine Metabolism.Drug testing and analysis · 2025Article
- Novel Baicalein-Derived Inhibitors ofPathogens (Basel, Switzerland) · 2023Article
- In Vitro Liver Metabolism of Six Flavonoid C-Glycosides.Molecules (Basel, Switzerland) · 2021Article
- Metabolic map and bioactivation of the anti-tumour drug noscapine.British journal of pharmacology · 2012Article
- Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.Journal of medicinal chemistry · 2012Article
- Imidazolopiperazines: hit to lead optimization of new antimalarial agents.Journal of medicinal chemistry · 2011Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
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Abstract
A "dual-activity" microsomal system in which both CYPs and UGTs were active was evaluated for studies of metabolic stability and in-vitro metabolite profiling. In this "dual-activity" system, alamethicin, a pore-forming peptide, was used to activate UGTs in human liver microsomes without affecting CYP activity. Interference studies indicated that CYP cofactors had little effect on UGT surrogate activity as measured by glucuronidation of acetaminophen and trifluoperazine. Further, UGT cofactor, UDPGA (< 2 mM), did not inhibit the marker activity of five major CYPs including 1A2, 2C9, 2C19, 2D6 and 3A4, suggesting that both oxidation and glucuronidation can be co-activated in microsomes. In a comparison study, compounds with significant glucuronidation showed distinct stability profiles in the "dual-activity" system, compared to the conventional microsomal incubation in which only CYPs were active. For compounds with minor or no glucuronidation, the metabolic stability remained similar between the "dual-activity" system and the conventional microsomal incubation. The feasibility of this "dual-activity" system utilized for metabolite profiling was also investigated using tramadol as a model drug. It was found that oxidative metabolites of tramadol generated in the "dual-activity" system matched those detected in the conventional microsomal incubation. However, tramadol glucuronide was observed in the "dual-activity" system but not in the conventional micromosal incubation. Results clearly suggest that the "dual-activity" system is a valuable in vitro model for metabolism studies in drug discovery.
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