A Complete Study of Farrerol Metabolites Produced in Vivo and in Vitro
| Autor: | Lantong Zhang, Qingzhong Jia, Caijuan Liang, Jintuo Yin, Yinling Ma, Hairong Wang, Yupeng Sun |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Pharmaceutical Science
Mass spectrometry 01 natural sciences UHPLC-Q-TOF-MS/MS Article Analytical Chemistry lcsh:QD241-441 03 medical and health sciences lcsh:Organic chemistry Tandem Mass Spectrometry In vivo Drug Discovery multiple data post-processing techniques Physical and Theoretical Chemistry Chromatography High Pressure Liquid 030304 developmental biology 0303 health sciences Rhododendron dauricum Molecular Structure biology Chemistry 010401 analytical chemistry Organic Chemistry in vitro Metabolism Methylation farrerol biology.organism_classification Metabolic Detoxication Phase II In vitro 0104 chemical sciences Metabolic pathway in vivo Biochemistry Chromones Chemistry (miscellaneous) Spectrometry Mass Matrix-Assisted Laser Desorption-Ionization Molecular Medicine Metabolic Detoxication Phase I Glucuronide Oxidation-Reduction metabolism |
| Zdroj: | Molecules Volume 24 Issue 19 Molecules, Vol 24, Iss 19, p 3470 (2019) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules24193470 |
| Popis: | Although farrerol, a characteristically bioactive constituent of Rhododendron dauricum L., exhibits extensive biological and pharmacological activities (e.g., anti-oxidant, anti-immunogenic, and anti-angiogenic) as well as a high drug development potential, its metabolism remains underexplored. Herein, we employed ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry coupled with multiple data post-processing techniques to rapidly identify farrerol metabolites produced in vivo (in rat blood, bile, urine and feces) and in vitro (in rat liver microsomes). As a result, 42 in vivo metabolites and 15 in vitro metabolites were detected, and farrerol shown to mainly undergo oxidation, reduction, (de)methylation, glucose conjugation, glucuronide conjugation, sulfate conjugation, N-acetylation and N-acetylcysteine conjugation. Thus, this work elaborates the metabolic pathways of farrerol and reveals the potential pharmacodynamics forms of farrerol. |
| Databáze: | OpenAIRE |
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