Abstract
The aim of our research was to obtain new, more soluble and biologically active derivatives of ellagic acid through acylation of phenol hydroxyls and obtaining supramolecular complexes with cyclodextrins, as well as to study the ability of the derivatives synthesized to eliminate the microorganism resistance to aminoglycoside antibiotics (by the example of gentamicin). The article represents the research results of the acylated derivatives of ellagic acid and its supramolecular derivatives with β-cyclodextrins. The structure of the compounds synthesized has been confirmed by NMR1H -spectroscopy and HPLC with a multiwave ultraviolet-detector. It has been shown that in sub-effective concentrations (0.001% solution) in the absence of direct antimicrobial and antifungal properties, tetrasuccinyl-digallic acid (5) reveals the ability to reduce sensitivity to gentamicin in polyresistant strains of microorganisms and sensitivity to nystatin in fungi resistant to it. It has been found that clathrate complexes of ellagotanin with β-cyclodextrins have no antiresistant activity, as well as other acylated derivatives of ellagic acid.
Highlights
Целью исследований было получение новых, более растворимых и биологически активных производных эллаговой кислоты через ацилирование фенольных гидроксилов и получение супрамолекулярных комплексов с циклодекстринами, изучение способности синтезированных производных снимать резистентность микроорганизмов к аминогликозидным антибиотикам
The structure of the compounds synthesized has been confirmed by NMR1H -spectroscopy and HPLC with a multiwave ultraviolet-detector
It has been found that clathrate complexes of ellagotanin with β-cyclodextrins have no antiresistant activity, as well as other acylated derivatives of ellagic acid
Summary
Целью исследований было получение новых, более растворимых и биологически активных производных эллаговой кислоты через ацилирование фенольных гидроксилов и получение супрамолекулярных комплексов с циклодекстринами, изучение способности синтезированных производных снимать резистентность микроорганизмов к аминогликозидным антибиотикам (на примере гентамицина). В работе представлены результаты исследований синтезированных ацилированных производных эллаговой кислоты и ее супрамолекулярных производных с β-циклодекстрином. Что в субэффективных концентрациях (0,001% раствор) при отсутствии прямых антимикробных и антигрибковых свойств тетрасукцинил-дигалловая кислота (5) проявила способность восстанавливать чувствительность к гентамицину у полирезистентных штаммов микроорганизмов и чувствительность к нистатину у резистентных к нему грибов.
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