Comparative metabolism of tussilagone in rat and human liver microsomes using ultra‐high‐performance liquid chromatography coupled with high‐resolution LTQ‐Orbitrap mass spectrometry

Abstract

The HR-ESI-MS/MS fragmentation behavior of tussilagone and its metabolic profile in RLMs and HLMs were investigated for the first time. The results demonstrated that the biotransformation of tussilagone involved hydrolysis of ester bonds at C-14 and hydroxylation in the side chains at C-12, C-5' or C-6'. Among the CYPs, CYP3A4 played an important role in the hydroxylation reaction of tussilagone in vitro. Furthermore, the results indicated a species-related difference in the metabolism of tussilagone between RLMs and HLMs. This work provided basic information for the metabolism of tussilagone in RLMs and HLMs, which would help to better understand the pharmacological activities of tussilagone.

Metabolic profile of Rhizoma coptidis in human plasma determined using ultra‐high‐performance liquid chromatography coupled with high‐resolution mass spectrometry

“…In the present study, the possible ESI‐HR‐MS/MS fragmentation pathways of coptisine, berberine and palmatine were deduced to aid in the identification of the metabolites in human plasma because a comprehensive understanding of the mass fragmentation pathways of the parent compounds would be beneficial for metabolite characterization . In the positive ion mode, the fragment ions of coptisine at m/z 292.0986, 277.0744 and 264.1027 assigned as [M + − CO] + , [M + − CO − ▪CH 3 ] + and [M + − 2CO] + were observed.…”

“…In high-performance liquid chromatography coupled with highresolution mass spectrometry (HPLC/HRMS), compounds can be identified by accurate measurements of the mass/charge ratios (m/z) of their molecular and fragment ions, 45 making this technique widely popular for reliable metabolite identification. [46][47][48] Considering the importance of drug metabolism in the body, the present study aimed to investigate the metabolic profile of Rhizoma coptidis in human plasma after oral administration of Rhizoma coptidis extract using ultra-high-performance liquid chromatography coupled with highresolution LTQ-Orbitrap mass spectrometry. This study will be helpful for understanding the real metabolic profile of Rhizoma coptidis in humans and provide scientific evidence for its uses in traditional medicine.…”

Tussilagone Inhibits Osteoclastogenesis and Periprosthetic Osteolysis by Suppressing the NF-κB and P38 MAPK Signaling Pathways

“…Additionally, some scholars have studied the metabolic patterns and parameters of TUS and set a foundation for further systematic research in patients (Liu et al, 2008;Zhang et al, 2015;Cheng et al, 2018b). In terms of molecular mechanism, many studies have indicated that TUS suppresses exogenous-agent-stimulated inflammation by downregulating NF-kB signaling in different samples including human colonic tissues, airway epithelial cells, and dendritic and microglial cells (Park et al, 2014;Cheon et al, 2018;Choi et al, 2018;Hwang et al, 2018).…”

Tussilagone Inhibits Osteoclastogenesis and Periprosthetic Osteolysis by Suppressing the NF-κb and p38 MAPK Signaling Pathways

“…In recent years, several studies proved its beneficial effect in the treatment of diseases like diabetic obesity [20], cancers [19] and various inflammatory diseases [16-18, 22, 23]. Additionally, some scholars dedicated their studies to the metabolic patterns and parameters of TUS and set a foundation for further systematic research in patients [46][47][48].. In terms of molecular mechanism, the majority of retrieved literatures indicated that TUS suppresses exogenous-agent-stimulated inflammation by downregulating NF-κB signaling in different samples including human colonic tissues, airway epithelial cells, dendritic and microglial cells [16][17][18]24].…”