Evaluation of Antimicrobial and Antibiofilm Effects of Kojic Acid Derivatives against Bacteria and Fungi

Abstract

Objective: In this study, it was aimed to investigate the antibacterial and antifungal activities of kojic acid derivatives against Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus) and fungal strain (Candida albicans). Material and Methods: Antimicrobial activity profiles of the compounds were investigated by microdilution and disk diffusion method. Antibiofilm activities were investigated by spectrophotometric microplate method including crystal violet staining. Moreover, the impact of the compounds on both biofilm and cells was also clarified via scanning electron microscopy (SEM). Results: Minimum inhibitory concentration values were found between 16 μg/mL to 1024 μg/mL. The most potent substance, 3b bearing 3,4- dichlorobenzylpiperazine moiety, has been shown to have inhibitory effects at 16-64 μg/mL concentrations. It was determined that 3a and 3b had stronger inhibitory effects than the other substances against C. albicans. In addition, antibacterial activity was discovered to be greater against Gram-positive strains than Gram-negative. It was also shown by SEM that compound 3b caused significant deformation on the cell wall and membrane of E. faecalis strain and inhibited the biofilm structures of S. aureus and E. coli strains. Conclusion: Kojic acid derivatives were found to inhibit the growth of both bacterial and fungal pathogens at low concentrations. It was also shown that kojic acid derivatives were able to decrease biofilm formation. It is thought that, this will be a favourable scenario for novel therapeutic candidates since more novel compounds will be created, and the inhibitory mechanism will be explored in various research including phenotypic and genotypic experiments.

Keywords

• Kojic acid derivatives
• antimicrobial activity
• antibiofilm activity
• scanning electron microscopy

Kojik Asit Türevlerinin Bakteri ve Mantarlara Karşı Antimikrobiyal ve Antibiyofilm Etkilerinin Değerlendirilmesi

Abstract

Amaç: Bu çalışmada kojik asit türevlerinin Gram-negatif bakterilere (Pseudomonas aeruginosa ve Escherichia coli), Gram-pozitif bakterilere (Enterococcus faecalis ve Staphylococcus aureus) ve mantar kökenine (Candida albicans) karşı antibakteriyel ve antifungal aktivitelerinin araştırılması amaçlanmıştır. Gereç ve Yöntem: Bileşiklerin antimikrobiyal aktivite profilleri mikrodilüsyon ve disk difüzyon yöntemleri ile araştırıldı. Antibiyofilm aktiviteler kristal viyole ile boyamayı içeren spektrofotometrik mikroplaka yöntemi ile araştırıldı. Ayrıca bileşiklerin hem biyofilm hem de hücreler üzerindeki etkisi taramalı elektron mikroskobu (SEM) ile açıklığa kavuşturuldu. Bulgular: Minimum inhibitör konsantrasyon değerleri 16 μg/mL ile 1024 μg/mL arasında bulundu. En güçlü madde olan, 3,4-diklorobenzilpiperazin kısmını taşıyan 3b'nin 16-64 μg/mL konsantrasyonlarda inhibitör etkiye sahip olduğu gösterildi. 3a ve 3b'nin C. albicans'a karşı diğer bileşiklere göre daha güçlü inhibitör etkileri olduğu saptandı. Ek olarak, antibakteriyel aktivitenin Gram-pozitif suşlara karşı, Gram-negatif suşlara göre daha fazla olduğu belirlendi. Ayrıca bileşik 3b'nin, SEM ile E. faecalis suşunun hücre duvarı ve membranında önemli deformasyona neden olduğu ve S. aureus ve E. coli suşlarının biyofilm yapılarını inhibe ettiği gösterildi. Sonuç: Kojik asit türevlerinin düşük konsantrasyonlarda hem bakteriyel hem de fungal patojenlerin büyümesini engellediği belirlenmiştir. Ayrıca kojik asit türevlerinin biyofilm oluşumunu azaltabildiği gösterilmiştir. Bu, daha fazla yeni bileşik yaratılacağı ve engelleyici mekanizmanın fenotipik ve genotipik deneyler de dahil olmak üzere çeşitli araştırmalarda keşfedileceği için yeni terapötik adaylar için olumlu bir senaryo olacaktır

Keywords

• Kojik asit türevleri
• antimikrobiyal aktivite
• antibiyofilm aktivite
• taramalı elektron mikroskobu

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