Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase

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Title
Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase
Author(s)
Bo Ram Kim; Ji Young ParkHyung Jae JeongHyung Jun KwonSu-Jin ParkIn Chul LeeYoung Bae RyuWoo Song Lee
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 33, pp. 1256-1265
Publication Year
2018
Abstract
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.
Keyword
CurcuminNan Asepsissialidase
ISSN
1475-6366
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/14756366.2018.1488695
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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