Novel Neuroprotective Lead Compound Ligustrazine Derivative Mass Spectrometry Fragmentation Rule and Metabolites in Rats by LC/LTQ-Orbitrap MS

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Xinyu ZhangHaimin Lei

Abstract

The neuroprotective evaluation of ligustrazine derivatives has become a research focus all over the world. A novel ligustrazine derivative, (3,5,6-Trimethylpyrazin-2-yl)methyl(E)-3-(4-((3,5,6-trimethylpyrazin-2-l)methoxy)phenyl)acrylate (T-CA), has shown protective effects against CoCl₂-induced neurotoxicity in a differentiated PC12 cell model and middle cerebral artery occlusion (MCAO) model in our previous studies. However, nearly none of the parent drugs existed after rapid metabolism due to uncertain reasons. Thus, the fragmentation regularities of mass spectra, and metabolites, of T-CA in rats were examined using liquid chromatography-electrospray ionizationion trap mass spectrometry (LC/LTQ-Orbitrap MS) in this research. The main fragment ion, mass spectrum characteristics, and the structural information were elucidated. When compared with a blank sample, we identified five kinds of T-CA metabolites, including three phase I metabolites and two phase II metabolites. The results showed that the metabolic pathways of T-CA in rats via oral administration were hydrolysis (ether bond rupture, ester bond rupture), oxidation, reduction, glucose aldehyde acidification, etc. In addition, three main metabolites were synthesized and ...Continue Reading

References

Oct 1, 2003·Clinical and Experimental Pharmacology & Physiology·Kar-Lok WongJuei-Tang Cheng
Oct 23, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Penglong WangHaimin Lei
Jan 22, 2014·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Valérie ThibertValérie Pichon
May 2, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Ren KongStephen T C Wong
Jul 18, 2015·Fundamental & Clinical Pharmacology·Wenlong LiRuichen Guo
Feb 27, 2016·Drug Discovery Today·Somdutta SahaJames R Brown
Feb 13, 2018·European Journal of Medicinal Chemistry·Jinmi ZouXinyong Liu

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Citations

Jul 25, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Juyuan LuoCun Liu

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Methods Mentioned

BETA
NMR

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