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

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posted on 2018-08-21, 07:09 authored by Bo Ram Kim, Ji-Young Park, Hyung Jae Jeong, Hyung-Jun Kwon, Su-Jin Park, In-Chul Lee, Young Bae Ryu, Woo Song Lee

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.

Funding

This research was supported by the KRIBB Research Initiative Program and part of the project titled “Development of the control of aquaculture infectious disease using natural resources,” funded by the Ministry of Oceans and Fisheries, Republic of Korea. J-. Y. Park and H-. J. Kwon were supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning [NRF-2016R1C1B2015753]. Also, this study was supported by Korea Coast Guard.

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