Plastoquinone analogs: a potential antimicrobial lead structure intensely suppressing Staphylococcus epidermidis and Candida albicans growth


Mataracı Kara E., Bayrak N., Yıldırım H., Yıldız M., Ataman M., Özbek Çelik B., ...More

MEDICINAL CHEMISTRY RESEARCH, vol.30, no.9, pp.1728-1737, 2021 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 30 Issue: 9
  • Publication Date: 2021
  • Doi Number: 10.1007/s00044-021-02772-z
  • Journal Name: MEDICINAL CHEMISTRY RESEARCH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, Chimica, EMBASE, Veterinary Science Database
  • Page Numbers: pp.1728-1737
  • Keywords: Quinone analogs, Antibacterial activity, Antifungal activity, Antibiofilm activity, Staphylococcus epidermidis, Candida albicans, Cytotoxicity, 1,4-NAPHTHOQUINONE DERIVATIVES, ANTIBACTERIAL ACTIVITY, BIOLOGICAL EVALUATION, NATURAL-PRODUCTS, RESISTANCE, ANTIBIOTICS, BIOFILMS, MECHANISMS, ARYLAMINE, DRUGS
  • Istanbul University Affiliated: Yes

Abstract

The aim of this study was to evaluate the antimicrobial activity of twenty-five Plastoquinone analogs synthesized previously in a panel of seven bacterial strains (three Gram-positive and four Gram-negative bacteria) and three fungi. PQ1, which does not contain any substituent(s) on the phenyl ring, was the most potent compound against Staphylococcus epidermidis (8-fold more potent than Cefuroxime, MIC = 1.22 mu g/mL). The antifungal profile of all Plastoquinone analogs indicated that three analogs (PQ1, PQ2, and PQ7) displayed the best antifungal activity against Candida albicans, which was about the same activity with the reference standard (MIC = 4.88 mu g/mL). The structure-activity relationship study was also carried out to reveal important chemical features. After probing twenty-five Plastoquinone analogs for a potential antimicrobial lead structure, two analogs (PQ1 and PQ25) were selected for further investigation for biofilm evaluation. Based on the tests performed, there was a significant positive correlation between inhibition of the biofilm attachment and time. The results showed that both analogs (PQ1 and PQ25) are able to reduce biofilm mass. Finally, these findings endorse us further efforts to optimize two phenotypes of the Plastoquinone analogs (PQ1 and PQ25) to develop potential antimicrobial drug candidates.