Myeloperoxidase (MPO): Do We Need Inhibitors?

Myeloperoxidase (MPO) is known to cause oxidative stress and inflammation leading to cardiovascular disease (CVD) complications. MPO‐mediated oxidation of lipoproteins leads to dysfunctional entities altering the landscape of lipoprotein functionality. The specificity of guaiacol derivatives toward preventing MPO‐mediated oxidation to limit MPO's harmful effects is unknown. Diligent in silico studies were accomplished for a portfolio of compounds with guaiacol as a building block. The compounds’ activity toward MPO inhibition was also validated. The role of these chemical entities in controlling MPO‐mediated oxidation of lipoproteins (LDL and HDL) was shown to agree with our approach of developing powerful MPO inhibitors. The mechanism of MPO inhibition was demonstrated to be reversible in nature. This study reveals that there is great potential for guaiacol derivatives as therapeutics for CVD by modulating lipid profiles, reducing atherosclerotic plaque burden, and subsequently optimizing cardiovascular functions.

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Synthetic Guaiacol Derivatives as Promising Myeloperoxidase Inhibitors Targeting Atherosclerotic Cardiovascular Disease

Jayaraj

Parthasarathy

Rajagopalan

et al. 2020

ChemMedChem

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Genetic Variants rs1049255 CYBA and rs2333227 MPO are Associated with Susceptibility to Coronary Artery Disease in Russian Residents of Central Russia

Бушуева

2020

Kardiologiia

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Aim To study association of single-nucleotide polymorphisms rs1049255 CYBA and rs2333227 MPO with development of ischemic heart disease (IHD) in Russian residents of Central Russia.Material and methods The study material was DNA samples from 436 patients with IHD (265 men, 171 women; mean age, 61 years) and 370 sex- and age-matched arbitrarily healthy volunteers (209 men, 161 women; mean age, 60 years). Genotyping was performed by allelic discrimination with TaqMan probes.Results Comparative analysis of genotype frequency (log-additive regression model) showed that SNP rs1049255 CYBA (odds ratio, OR, 0.79 at 95 % confidence interval, CI, from 0.65 to 0.96; p=0.02) and rs2333227 MPO (OR 0.72 at 95 % CI from 0.55 to 0.95; p=0.02) were associated with a decreased risk of IHD adjusted for sex and age. Analysis of sex-specific effects showed that the protective effect of rs1049255 CYBA was evident only in men (OR 0.72 at 95 % CI from 0.55 to 0.94; p=0.16).Conclusion The study demonstrated a protective effect of rs1049255 CYBA and rs2333227 MPO with respect of IHD in Russians. The protective effect of rs1049255 CYBA was observed only in men.

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Myeloperoxidase (MPO): Do We Need Inhibitors?

Cited by 2 publications

References 166 publications

Synthetic Guaiacol Derivatives as Promising Myeloperoxidase Inhibitors Targeting Atherosclerotic Cardiovascular Disease

Synthetic Guaiacol Derivatives as Promising Myeloperoxidase Inhibitors Targeting Atherosclerotic Cardiovascular Disease

Genetic Variants rs1049255 CYBA and rs2333227 MPO are Associated with Susceptibility to Coronary Artery Disease in Russian Residents of Central Russia

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