We have located links that may give you full text access.
Journal Article
Research Support, Non-U.S. Gov't
Comparative metabolism of tussilagone in rat and human liver microsomes using ultra-high-performance liquid chromatography coupled with high-resolution LTQ-Orbitrap mass spectrometry.
Rapid Communications in Mass Spectrometry : RCM 2015 September 31
RATIONALE: Tussilagone is a major component in Tussilago farfara that has been widely used as an anti-tussive herbal medicine for the treatment of bronchitis, cough and asthmatic disorders in the clinic. However, its metabolism has been poorly investigated. In order to clarify its in vitro metabolism, a comparative analysis of its metabolic profile in rat liver microsomes (RLMs) and human liver microsomes (HLMs) was carried out. Further, the cytochrome P450 isoforms (CYPs) involved in the metabolism were investigated.
METHODS: In this work, the biotransformation of tussilagone in RLMs and HLMs was compared using ultra-high-performance liquid chromatography coupled with high-resolution LTQ-Orbitrap mass spectrometry (UHPLC/HRMS) and the CYPs involved in the metabolism were further investigated by recombinant human CYP enzymes.
RESULTS: Totally, nine metabolites of tussilagone were identified in RLMs and HLMs based on the proposed MS/MS fragmentation pathways of tussilagone and the accurate MS/MS spectra. Among them, one metabolite (M9) was detected in both RLMs and HLMs while the other eight metabolites were only detected in HLMs. Three hydroxylation metabolites (M6, M7 and M8) were detected in the assay with individual recombinant P450s incubation. M6 was detected in all CYPs except CYP2A6 while M7 and M8 were only observed in CYP3A4.
CONCLUSIONS: 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.
METHODS: In this work, the biotransformation of tussilagone in RLMs and HLMs was compared using ultra-high-performance liquid chromatography coupled with high-resolution LTQ-Orbitrap mass spectrometry (UHPLC/HRMS) and the CYPs involved in the metabolism were further investigated by recombinant human CYP enzymes.
RESULTS: Totally, nine metabolites of tussilagone were identified in RLMs and HLMs based on the proposed MS/MS fragmentation pathways of tussilagone and the accurate MS/MS spectra. Among them, one metabolite (M9) was detected in both RLMs and HLMs while the other eight metabolites were only detected in HLMs. Three hydroxylation metabolites (M6, M7 and M8) were detected in the assay with individual recombinant P450s incubation. M6 was detected in all CYPs except CYP2A6 while M7 and M8 were only observed in CYP3A4.
CONCLUSIONS: 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.
Full text links
Related Resources
Trending Papers
The 'Ten Commandments' for the 2023 European Society of Cardiology guidelines for the management of endocarditis.European Heart Journal 2024 April 18
Challenges in Septic Shock: From New Hemodynamics to Blood Purification Therapies.Journal of Personalized Medicine 2024 Februrary 4
A Guide to the Use of Vasopressors and Inotropes for Patients in Shock.Journal of Intensive Care Medicine 2024 April 14
Prevention and treatment of ischaemic and haemorrhagic stroke in people with diabetes mellitus: a focus on glucose control and comorbidities.Diabetologia 2024 April 17
Diagnosis and Management of Cardiac Sarcoidosis: A Scientific Statement From the American Heart Association.Circulation 2024 April 19
Eosinophilic Esophagitis: Clinical Pearls for Primary Care Providers and Gastroenterologists.Mayo Clinic Proceedings 2024 April
Essential thrombocythaemia: A contemporary approach with new drugs on the horizon.British Journal of Haematology 2024 April 9
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app
All material on this website is protected by copyright, Copyright © 1994-2024 by WebMD LLC.
This website also contains material copyrighted by 3rd parties.
By using this service, you agree to our terms of use and privacy policy.
Your Privacy Choices
You can now claim free CME credits for this literature searchClaim now
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app