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

被引:3
作者
Maslyk, Maciej [1 ]
Janeczko, Monika [1 ]
Demchuk, Oleg M. [2 ]
Boguszewska-Czubara, Anna [3 ]
Golczyk, Hieronim [1 ]
Sieroslawska, Anna [4 ]
Rymuszka, Anna [4 ]
Martyna, Aleksandra [1 ]
Kubinski, Konrad [1 ]
机构
[1] John Paul II Catholic Univ Lublin, Inst Biotechnol, Dept Mol Biol, Ul Konstantynow 1I, PL-20708 Lublin, Poland
[2] Marie Curie Sklodowska Univ, Organ Chem Dept, Fac Chem, Ul Gliniana 33, PL-20614 Lublin, Poland
[3] Med Univ Lublin, Dept Med Chem, Ul Chodzki 4A, PL-20093 Lublin, Poland
[4] John Paul II Catholic Univ Lublin, Inst Biotechnol, Dept Anim Physiol & Toxicol, Ul Konstantynow 1I, PL-20708 Lublin, Poland
关键词
Arylcyanomethylenequinone oximes; Antifungal agents; Candida albicans; Hyphae; Phosphorylation; RESISTANCE; YEAST; PHOSPHORYLATION; MORPHOGENESIS; TRANSITION; EXPRESSION; DIMORPHISM; AGENTS; STATES; FORMS;
D O I
10.1016/j.jsps.2017.12.004
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
引用
收藏
页码:244 / 252
页数:9
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