Abstract
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.
Highlights
The term “flavonoids” refers to a broad category of plant polyphenolics that are found in fruits, vegetables, beverages, and traditional Chinese medicines [1,2,3], and exhibit potent anti-oxidant, anti-inflammatory, anti-cancer, anti-bacterial, anti-viral, anti-allergic, and neuroprotective activities [3,4,5,6,7].The leaves of Rhododendron dauricum L. (RD), a plant used as a traditional Chinese medicine, are rich in flavonoids, some of which exhibit anti-inflammatory, anti-bacterial, and anti-oxidant activities [8]
With respect to pharmacokinetic and bioavailability studies of farrerol, a sensitive LC-MS method developed and validated for the quantitation of farrerol in rat plasma revealed that farrerol is rapidly absorbed and slowly eliminated in rats when administered orally, but is quickly eliminated when administered intravenously [34]. These results provide a theoretical foundation for the study of farrerol metabolites in plasma
Rat liver microsomes were prepared in the Department of Pharmaceutical Analysis of the School of Pharmacy, Hebei Medical University. β-Nicotinamide adenine dinucleotide phosphate (β-NADPH), uridine 50 -diphosphoglucuronic acid trisodium salt (UDPGA), alamethicin, MgCl2, and phosphate buffer saline (PBS, pH 7.4) were obtained from BD Biosciences (Woburn, MA, USA)
Summary
The term “flavonoids” refers to a broad category of plant polyphenolics that are found in fruits, vegetables, beverages, and traditional Chinese medicines [1,2,3], and exhibit potent anti-oxidant, anti-inflammatory, anti-cancer, anti-bacterial, anti-viral, anti-allergic, and neuroprotective activities [3,4,5,6,7].The leaves of Rhododendron dauricum L. (RD), a plant used as a traditional Chinese medicine, are rich in flavonoids, some of which exhibit anti-inflammatory, anti-bacterial, and anti-oxidant activities [8]. The term “flavonoids” refers to a broad category of plant polyphenolics that are found in fruits, vegetables, beverages, and traditional Chinese medicines [1,2,3], and exhibit potent anti-oxidant, anti-inflammatory, anti-cancer, anti-bacterial, anti-viral, anti-allergic, and neuroprotective activities [3,4,5,6,7]. (RD), a plant used as a traditional Chinese medicine, are rich in flavonoids, some of which exhibit anti-inflammatory, anti-bacterial, and anti-oxidant activities [8]. Farrerol (Figure 1) is a natural bioactive constituent of RD with extensive biological and pharmacological (e.g., anti-inflammatory, anti-bacterial, anti-oxidant, anti-immunogenic, and anti-angiogenic) activities [9,10,11,12,13]. A study on farrerol metabolite identification is expected to facilitate the development of new pharmaceuticals and provide new insights into the corresponding pharmacological mechanism of action.
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