1,2-Diarylethanols-A New Class of Compounds That Are Toxic to E. coli K12, R2-R4 Strains.

Paweł Kowalczyk,Grzegorz Skiba,Mateusz Szymczak,Damian Trzepizur,Ryszard Ostaszewski,Karol Kramkowski

doi:10.3390/ma14041025

Abstract

An initial study of 1,2-diarylethanols derivatives as new potential antibacterial drugs candidates was conducted. Particular emphasis was placed on the selection of the structure of 1,2-diarylethanols with the highest biological activity of lipopolysaccharides (LPS) in the model strains of Escherichia coli K12 (without LPS in its structure) and R2–R4 (with different lengths of LPS in its structure). In the presented studies, based on the conducted minimum inhibitory concentration (MIC) and MBC tests, it was demonstrated that the antibacterial (toxic) effect of 1,2-diarylethanols depends on their structure and the length of LPS bacteria in the membrane of specific strains. Moreover, the oxidative damage of bacterial DNA isolated from bacteria after modification with newly synthesized compounds after application of the repair enzyme Fpg glycosylases was analysed. The analysed damage values were compared with modification with appropriate antibiotics; bacterial DNA after the use of kanamycin, streptomycin, ciprofloxacin, bleomycin and cloxicillin. The presented research clearly shows that 1,2-diarylethanol derivatives can be used as potential candidates for substitutes for new drugs, e.g., the analysed antibiotics. Their chemical and biological activity is related to two aromatic groups and the corresponding chemical groups in the structure of the substituent. The observed results are particularly important in the case of increasing bacterial resistance to various drugs and antibiotics, especially in nosocomial infections and neoplasms, and in the era of pandemics caused by microorganisms.

Highlights

Introduction published maps and institutional affilContamination of the hospital environment by pathogenic microorganisms is one of the important problems of hospital epidemiology
The analysis of the toxicity of 1,2-diarylethanols used in our research shows that it is strongly related to the length of the LPS in the analysed types of bacteria R2–R4
The conducted study confirms the usefulness of mass screening tests for inhibitors of specific bacteria, such as 1,2-diarylethanols that induce plasmid DNA damage, in order to identify the antibiotics with a new and innovative way of action—acting on all types of bacteria

Summary

Introduction

Introduction published maps and institutional affilContamination of the hospital environment by pathogenic microorganisms is one of the important problems of hospital epidemiology. A work published by Boyce in the pages of Infection Control & Hospital Epidemiology presents the role of alcohols as disinfectants in the hospital environment [1]. Applications in this area include ethyl alcohol, isopropyl alcohol and n-propanol. This process requires the presence of water, and aqueous alcohol solutions have a stronger effect than absolute alcohol [2]. Alcohols practically have no killing effect on bacterial spores, they iations

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