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Chromone-3-aldehyde derivatives – sirtuin 2 inhibitors for correction of muscular dysfunction
- Source :
- Current Issues in Pharmacy and Medical Sciences. 32:45-50
- Publication Year :
- 2019
- Publisher :
- Walter de Gruyter GmbH, 2019.
-
Abstract
- The aim of the study was to evaluate experimentally, the myoprotective effect of new chromone-3-aldehyde derivatives in conditions of muscular dysfunction and to establish a potential mechanism of myoprotective activity – the blockade of the function of sirutin 2. Materials and methods. The effect of new chromone-3-aldehyde derivatives on the development of muscular dysfunction under the conditions of an electromiostimulation test, was studied. The degree of muscle fatigue was evaluated in the «grip-strength» and through test biochemical assays (determination of the activity of lactate dehydrogenase, creatine kinase, concentration of lactic and pyruvic acids, creatinine, myoglobin, and total protein) to determine the possible mechanism of action of the test compounds (5 new derivatives of chromone-3-aldehyde) and their effect on the function of sirtuin 2 was evaluated. Results. The study showed that chromone-3-aldehyde derivatives have a pronounced myoprotective effect associated with low toxicity (class 5 toxicity according to the GHS classification), which was confirmed by the results of the «grip-strength» test and biochemical tests data. Test compounds under the X3AC1, X3AOAC and X3AN codes evince sirtuin 2 inhibitory activity, which was reflected in a decrease in its concentration by 63.6% (p Conclusion. The study showed that chromone-3-aldehyde derivatives are promising subjects for further study with the goal of creating a drug with a high myoprotective effect and an optimal safety profile.
- Subjects :
- 0301 basic medicine
Pharmacology
chemistry.chemical_classification
biology
Stereochemistry
business.industry
General Medicine
Biochemistry
Aldehyde
03 medical and health sciences
chemistry.chemical_compound
030104 developmental biology
0302 clinical medicine
chemistry
Sirtuin
Chromone
biology.protein
Medicine
business
Molecular Biology
030217 neurology & neurosurgery
Subjects
Details
- ISSN :
- 23006676 and 2084980X
- Volume :
- 32
- Database :
- OpenAIRE
- Journal :
- Current Issues in Pharmacy and Medical Sciences
- Accession number :
- edsair.doi...........c0a4c488f419e855eddadbabcd287d91