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Registration Number

0215U001389, 0112U000828 , R & D reports

Title

3.Pharmacodynamic aspects of antimicrobial activity of new аrylaliphatic aminoalcohol derivatives

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Head

Vrynchanu Nina, Доктор медичних наук

Registration Date

26-02-2015

Organization

State Establishment "Institute of Pharmacology and Toxicology National Academy of Medical Science of Ukraine"

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125 new аrylaliphatic aminoalcohol derivatives were the object of research. The purpose of the study - to assess the antibacterial and antifungal activity of new аrylaliphatic aminoalcohol derivatives, find out the basic mechanisms of antimicrobial activity. For achievement of this purpose there were used a complex of modern physico-chemical, biochemical, pharmacological and microbiological research methods. Microbiological studies showed that monodirectional antibacterial activity found in 12, antifungal action - in 6, the wide range of action - in 35 substances among 125 tested new аrylaliphatic aminoalcohol derivatives. During the study it was identified substances with antibacterial (KVM-25 - gram-positive bacteria; KVM-176 and KVM-114 - gram-negative bacteria), antifungal activity (KVM-96, KVM-177, KVM-191) and wide range of actions (KVM-194 and KVM-204), which was carried out in-depth studies. New аrylaliphatic aminoalcohol derivatives able to prevent filming and destroy biofilms formed by bacteria and fungi. The study of the effect of new аrylaliphatic aminoalcohol derivatives on the ultrastructure of bacteria and fungi showed that the tested substances influence the membrane apparatus to suppress intracellular processes. Membranetropic activity of test substances is confirmed by studies on the permeability of the cell membrane of bacteria and fungi. Compounds able to inhibit microbial processes of energy, inhibit oxygen consumption, NAD- and FAD-dependent respiratory chain links. S. aureus cells decreased, and the cells C. albicans - increased content of DNA and RNA in the presence of subinhibitory concentrations of new аrylaliphatic aminoalcohol derivatives. Substances cause damage to the cell wall of gram-negative bacteria, recorded changes in the composition of lipopolysaccharide of E. coli. In the cells of C. albicans fungi observed inhibition of synthesis of ergosterol. Toxicity studies showed that new аrylaliphatic aminoalcohol derivatives belong to the Class III (moderately toxic substances), IV class (low toxic substances), V class (practically non-toxic) and Class VI toxicity (relatively harmless substances). Most of the substances have no adverse effects on the mucous membranes of the eyes of animals at concentrations of 0.1% - 0.5%. On an experimental model of onychomycosis (caused by Aspergillus niger) in concentrations 1.0 and 5.0 MIC substance KVM-204 shows efficacy in a single prophylactic, therapeutic and prophylactic and therapeutic modes.

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Волчков Олександр Олександрович
Гриневич Світлана Вікторівна
Дронова Марія Леонідівна
Дудікова Дар'я Маратівна
Недашківкька Вера Володимирівна
Суворова Зінаїда Сергіївна
Цикоза Аліна

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2020-04-02