新生隐球菌
微生物学
抗菌剂
细胞毒性
细菌
金黄色葡萄球菌
白色念珠菌
化学
生物
产气肠杆菌
鲍曼不动杆菌
铜绿假单胞菌
大肠杆菌
生物化学
遗传学
基因
体外
作者
Vitalii A. Palchykov,A. A. Gaponov,Nazar Manko,Nataliya Finiuk,О. Novikevych,Oleksandr Gromyko,Rostyslav Stoika,Nazariy T. Pokhodylo
出处
期刊:Ukrainian Biochemical Journal
[National Academy of Sciences of Ukraine (Co. LTD Ukrinformnauka)]
日期:2022-10-04
卷期号:94 (3): 68-80
标识
DOI:10.15407/ubj94.03.068
摘要
Cage amides and imides bearing bicyclo[2.2.1]- and bicyclo[2.2.2]-subunits were synthesized and evaluated both for antimicrobial activity toward five key ESKAPE pathogenic bacteria: one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (ATCC 43300), four Gram‐negative bacteria Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 700603), Acinetobacter baumannii (ATCC 19606) and Pseudomonas aeruginosa (ATCC 27853) and for antifungal activity towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). Compound VP-4539 with bicyclo[2.2.2]octene motif demonstrated the highest cytotoxic activity towards C. neoformans, while human keratinocytes of HaCaT line, murine fibroblasts of Balb/c 3T3 line and mitogen-activated lymphocytes of peripheral human blood were found to be tolerant to its action. VP-4539 compound did not intercalate into salmon sperm DNA indicating that its cytotoxicity is not related to intercalation into nucleic acid. Keywords: antifungal, antimicrobial, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octene, cytotoxicity, DNA intercalation, human keratinocytes, lymphocytes, сage compounds
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