A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro
Although farrerol, a characteristically bioactive constituent of <i>Rhododendron dauricum</i> 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...
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doaj-2737e543a31b4542a7599f912cf1d98c2020-11-25T02:10:07ZengMDPI AGMolecules1420-30492019-09-012419347010.3390/molecules24193470molecules24193470A Complete Study of Farrerol Metabolites Produced In Vivo and In VitroJintuo Yin0Yinling Ma1Caijuan Liang2Hairong Wang3Yupeng Sun4Lantong Zhang5Qingzhong Jia6Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaNational Clinical Drug Monitoring Center, Department of Pharmacy, Hebei Province General Center, Shijiazhuang 050051, ChinaDepartment of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaDepartment of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaDepartment of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaDepartment of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaDepartment of Pharmacology, Hebei Medical University, Shijiazhuang 050017, ChinaAlthough farrerol, a characteristically bioactive constituent of <i>Rhododendron dauricum</i> 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, <i>N</i>-acetylation and <i>N</i>-acetylcysteine conjugation. Thus, this work elaborates the metabolic pathways of farrerol and reveals the potential pharmacodynamics forms of farrerol.https://www.mdpi.com/1420-3049/24/19/3470farrerolUHPLC-Q-TOF-MS/MSmultiple data post-processing techniquesmetabolismin vivoin vitro |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Jintuo Yin Yinling Ma Caijuan Liang Hairong Wang Yupeng Sun Lantong Zhang Qingzhong Jia |
spellingShingle |
Jintuo Yin Yinling Ma Caijuan Liang Hairong Wang Yupeng Sun Lantong Zhang Qingzhong Jia A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro Molecules farrerol UHPLC-Q-TOF-MS/MS multiple data post-processing techniques metabolism in vivo in vitro |
author_facet |
Jintuo Yin Yinling Ma Caijuan Liang Hairong Wang Yupeng Sun Lantong Zhang Qingzhong Jia |
author_sort |
Jintuo Yin |
title |
A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro |
title_short |
A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro |
title_full |
A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro |
title_fullStr |
A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro |
title_full_unstemmed |
A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro |
title_sort |
complete study of farrerol metabolites produced in vivo and in vitro |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2019-09-01 |
description |
Although farrerol, a characteristically bioactive constituent of <i>Rhododendron dauricum</i> 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, <i>N</i>-acetylation and <i>N</i>-acetylcysteine conjugation. Thus, this work elaborates the metabolic pathways of farrerol and reveals the potential pharmacodynamics forms of farrerol. |
topic |
farrerol UHPLC-Q-TOF-MS/MS multiple data post-processing techniques metabolism in vivo in vitro |
url |
https://www.mdpi.com/1420-3049/24/19/3470 |
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