A representative of arylcyanomethylenequinone oximes effectively inhibits growth and formation of hyphae in Candida albicans and influences the activity of protein kinases in vitro

作者：Maslyk Maciej; Janeczko Monika; Demchuk Oleg M; Boguszewska Czubara Anna; Golczyk Hieronim; Sieroslawska Anna; Rymuszka Anna; Martyna Aleksandra; Kubinski Konrad^*

来源：Saudi Pharmaceutical Journal, 2018, 26(2): 244-252.

DOI：10.1016/j.jsps.2017.12.004

• Arylcyanomethylenequinone oximes
• Antifungal agents
• Candida albicans
• Hyphae
• Phosphorylation

In this study, we applied various assays to reveal new activities of phenylcyanomethylenequinone oxime-4-(hydroxyimino) cyclohexa-2,5-dien-1-ylidene](phenyl) ethanenitrile (4-AN) for potential antimicrobial applications. These assays demonstrated (a) the antimicrobial effect on bacterial and fungal cultures, (b) the effect on the in vitro activity of the kinase CK2, (c) toxicity towards human erythrocytes, the Caco-2 cancer cell line, and embryonic development of Zebrafish. We demonstrated the activity of 4-AN against selected bacteria and Candida spp. The MIC ranging from 4 mu g/ml to 125 mg/ml proved effective in inhibition of formation of hyphae and cell aggregation in Candida, which was demonstrated at the cytological level. Noteworthy, 4-AN was found to inhibit the CK2 kinase with moderate potency. Moreover, at low concentrations, it did not exert any evident toxic effects on human erythrocytes, Caco-2 cells, or Zebrafish embryos. 4-AN can be a potential candidate as a novel drug against Candida infections.

• 出版日期2018-2