姜黄素
唾液酸酶
肺炎链球菌
微生物学
唾液酸
聚糖
IC50型
化学
毒力
细菌
结构-活动关系
酶
生物化学
体外
生物
神经氨酸酶
抗生素
糖蛋白
基因
遗传学
作者
Bo Ram Kim,Ji Young Park,Hyung Jae Jeong,Hyung-Jun Kwon,Su‐Jin Park,In-Chul Lee,Young Bae Ryu,Woo Song Lee
标识
DOI:10.1080/14756366.2018.1488695
摘要
Sialidases are key virulence factors that remove sialic acid from the host cell surface glycan, unmasking receptors that facilitate bacterial adherence and colonisation. In this study, we developed potential agents for treating bacterial infections caused by Streptococcus pneumoniae Nan A that inhibit bacterial sialidase using Turmeric and curcumin analogues. Design, synthesis, and structure analysis relationship (SAR) studies have been also described. Evaluation of the synthesised derivatives demonstrated that compound 5e was the most potent inhibitor of S. pneumoniae sialidase (IC50 = 0.2 ± 0.1 µM). This compound exhibited a 3.0-fold improvement in inhibitory activity over that of curcumin and displayed competitive inhibition. These results warrant further studies confirming the antipneumococcal activity 5e and indicated that curcumin derivatives could be potentially used to treat sepsis by bacterial infections.
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