A szemikarbazid-szenzitív aminoxidáz enzim élettani és farmakológiai jelentosége

Translated title of the contribution: Semicarbazide-sensitive amine oxidase: Its physiological and pharmacological significance

K. Magyar, Mészáros Zsuzsa, P. Mátyus

Research output: Contribution to journalArticle

Abstract

Although the existence of plasma and tissue bound semicarbazide-sensitive amine oxidases (SSAOs) has been recognized earlier, the physiological and pharmacological relevance of the enzyme still remains uncertain. Recent data suggest that elevated serum SSAO activity might cause endothelial injury. Formation of cytotoxic metabolites (e.g. formaldehyde, methylglyoxal and hydrogen peroxide) and increased oxidative stress might lead to initiation or progression of atherosclerosis. Significant positive correlation was found between serum SSAO activity and severity of atherosclerosis, and diabetic macrovascular complications. Effective and selective inhibitors of human SSAO might exert cytoprotective effect on endothelial cells. It was published, that mexiletine slightly inhibits SSAO activity. Compounds, having similar structure to mexiletine, were synthesized and studied relating to SSAO activity. The reference substance was MDL-72974A, one of the most potent, non-selective SSAO inhibitors known. Unfortunately, our new compounds did not reach the potency of the reference substance, using human serum samples. In conclusion, we suppose that vascular and soluble SSAO enzymes might have different inhibitor sensitivity. Further studies are required to determine whether the soluble or vascular isoform of SSAO will be the main therapeutic target in the future.

Original languageHungarian
Pages (from-to)189-196
Number of pages8
JournalOrvoskepzes
Volume77
Issue number3
Publication statusPublished - 2002

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Amine Oxidase (Copper-Containing)
Pharmacology
Mexiletine
Blood Vessels
Atherosclerosis
Serum
Pyruvaldehyde
Diabetes Complications
Enzymes
Hydrogen Peroxide
Formaldehyde
Protein Isoforms
Oxidative Stress
Endothelial Cells

ASJC Scopus subject areas

  • Medicine(all)

Cite this

A szemikarbazid-szenzitív aminoxidáz enzim élettani és farmakológiai jelentosége. / Magyar, K.; Zsuzsa, Mészáros; Mátyus, P.

In: Orvoskepzes, Vol. 77, No. 3, 2002, p. 189-196.

Research output: Contribution to journalArticle

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