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Anti-inflammatory effects of ozenoxacin, a topical quinolone antimicrobial agent.


ABSTRACT: Ozenoxacin is a topical quinolone showing potent antimicrobial activities against Gram-negative and Gram-positive bacteria and is widely used for the treatment of inflammatory acne. However, the anti-inflammatory activities of ozenoxacin have not been examined so far. In the present study, we investigated the in vitro and in vivo anti-inflammatory effects of ozenoxacin. The production of interleukin (IL)-6 and IL-8 by human epidermal keratinocytes stimulated by heat-killed Cutibacterium acnes was significantly inhibited by ozenoxacin at concentrations from 1 to 30??g?ml-1. Likewise, the production of IL-6, IL-8, and tumor necrosis factor alpha by stimulated THP-1 cells, a human monocyte cell line, was inhibited by ozenoxacin at concentrations from 1 to 30??g?ml-1. The production of IL-1? by THP-1 was also inhibited by ozenoxacin at the concentration of 30??g?ml-1. Phosphorylation of the mitogen-activated protein kinases and degradation of I?B-?, an inhibitory factor of NF-?B in keratinocytes and THP-1 cells, was increased by stimulation with heat-killed C. acnes. Of these activated intracellular pathways, the p38 phosphorylation pathway was remarkably reduced by ozenoxacin in both keratinocytes and THP-1 cells. In addition, the application of 2% ozenoxacin suppressed the increase in the ear thickness of rats induced by an intracutaneous injection of heat-killed C. acnes. These findings suggest that ozenoxacin possesses an anti-inflammatory activity, which may contribute to its therapeutic effects on inflammatory acne.

SUBMITTER: Tabara K 

PROVIDER: S-EPMC7056637 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature

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Anti-inflammatory effects of ozenoxacin, a topical quinolone antimicrobial agent.

Tabara Keisuke K   Tamura Rie R   Nakamura Aki A   Mori Sachi S   Kitano Takamichi T   Fujikawa Koki K   Fujikawa Mika M   Okamoto Kazuaki K   Kanayama Shoji S   Uratsuji Hideya H   Ikeda Fumiaki F   Matsumoto Tatsumi T  

The Journal of antibiotics 20200123 4


Ozenoxacin is a topical quinolone showing potent antimicrobial activities against Gram-negative and Gram-positive bacteria and is widely used for the treatment of inflammatory acne. However, the anti-inflammatory activities of ozenoxacin have not been examined so far. In the present study, we investigated the in vitro and in vivo anti-inflammatory effects of ozenoxacin. The production of interleukin (IL)-6 and IL-8 by human epidermal keratinocytes stimulated by heat-killed Cutibacterium acnes wa  ...[more]

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