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In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone. | LitMetric

In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone.

Antibiotics (Basel)

Department of Molecular Biology and Genetics, Gebze Technical University, Gebze 41 400, Kocaeli, Türkiye.

Published: November 2022

AI Article Synopsis

  • Naphthoquinones, specifically the synthesized derivative 5,8-dihydroxy-1,4-naphthoquinone, demonstrate significant antimicrobial activity against various microorganisms, including bacteria and fungi.
  • The study determined MIC50 values for several pathogens, indicating its potent inhibitory effects, particularly on Staphylococcus aureus and Candida albicans.
  • Mechanistic investigations revealed that the compound primarily disrupts cell membranes, causing DNA damage and affecting respiratory activity in these microorganisms, highlighting its potential as a new drug candidate.

Article Abstract

Naphthoquinones are an important class of natural organic compounds that have antimicrobial effects. However, the mechanisms of their action remain to be elucidated. Therefore, the antimicrobial activity of the chemically synthesized naphthoquinone derivative, 5,8-dihydroxy-1,4-naphthoquinone, was investigated in this study against 10 different microorganisms. Its inhibitory activity was evident against Bacillus cereus, Proteus vulgaris, Salmonella enteritidis, Staphylococcus epidermidis, S. aureus, and Candida albicans, and its MIC50 values were determined to be 14, 10, 6, 2, 4, 1.2, and <0.6 µg/mL, respectively. Moreover, the crystal violet uptake, TTC dehydrogenase activity, protein/DNA leakage, and DNA damage of the compound in these microorganisms were also investigated to reveal the antimicrobial mechanisms. In addition, scanning electron microscopy was used to detect physiological damage to the cell membrane of S. epidermidis, S. aureus, and C. albicans, which was most severe in the crystal violet uptake assay. The overall results showed that 5,8-dihydroxy-1,4-naphthoquinone exhibited its effects on S. aureus, S. epidermidis, and C. albicans by various mechanisms, especially membrane damage and membrane integrity disruption. It also caused DNA leakage and damage along with respiratory chain disruption (78%) in C. albicans. Similarly, it caused varying degrees of reduction in the respiratory activity of S. aureus (47%), S. epidermidis (16%), B. cereus (12%), S. enteritidis (9%), and P. vulgaris (8%). Therefore, 5,8-dihydroxy-1,4-naphthoquinone proved to be a very effective antifungal and antibacterial agent and could be considered a new potential drug candidate, inspiring further discoveries in these microorganisms.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9687054PMC
http://dx.doi.org/10.3390/antibiotics11111537DOI Listing

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