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Authors Wu PP, He H, Hong WD, Wu TR, Huang GY, Zhong YY, Tu BR, Gao M, Zhou J, Zhao SQ, Li DL, Xu XT, Sheng ZJ, Ward SA, O’Neill PM, Zhang K
Received 5 June 2018
Accepted for publication 2 August 2018
Published 24 October 2018 Volume 2018:11 Pages 1945—1957
DOI https://doi.org/10.2147/IDR.S176390
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Amy Norman
Peer reviewer comments 2
Editor who approved publication: Dr Joachim Wink
Background: Fusidic acid (FA) (WU-FA-00) is the only commercially available
antimicrobial from the fusidane family that has a narrow spectrum of activity
against Gram-positive bacteria.
Methods: Herein, the hydrogenation derivative (WU-FA-01) of FA was prepared
and both compounds were examined against a panel of six bacterial strains. In
addition, their anti-inflammatory properties were evaluated using a 12-O -tetradecanoylphorbol-13-acetate
(TPA)-induced mouse ear edema model.
Results: The results of the antimicrobial assay revealed that both WU-FA-00 and
WU-FA-01 displayed a high level of antimicrobial activity against Gram-positive
strains. Moreover, killing kinetic studies were performed and the results were
in accordance with the minimum inhibitory concentration and minimum
bactericidal concentration results. We also demonstrated that the topical
application of WU-FA-00 and WU-FA-01 effectively decreased TPA-induced ear
edema in a dose-dependent manner. This inhibitory effect was associated with
the inhibition of TPA‑induced upregulation of proinflammatory cytokines IL-1β,
TNF-α, and COX-2. WU-FA-01 significantly suppressed the expression levels of
p65, IκB-α, and p-IκB-α in the TPA-induced mouse ear model.
Conclusion: Overall, our results showed that WU-FA-00 and WU-FA-01 not only had
effective antimicrobial activities in vitro, especially to the Gram-positive
bacteria, but also possessed strong anti-inflammatory effects in vivo. These
results provide a scientific basis for developing FA derivatives as
antimicrobial and anti-inflammatory agents.
Keywords: fusidic acid, derivative, antimicrobial, anti-inflammatory