A newly synthesized macakurzin C-derivative attenuates acute and chronic skin inflammation: The Nrf2/heme oxygenase signaling as a potential target
- Authors
- Akram, Muhammad; Shin, Iljin; Kim, Kyeong-A; Noh, Dabi; Baek, Seung-Hoon; Chang, Sun-Young; Kim, Hyoungsu; Bae, Ok-Nam
- Issue Date
- Sep-2016
- Publisher
- ACADEMIC PRESS INC ELSEVIER SCIENCE
- Keywords
- Synthetic flavonoid; Anti-inflammatory activity; TPA-induced acute inflammation; Oxazolone-induced atopic dermatitis
- Citation
- TOXICOLOGY AND APPLIED PHARMACOLOGY, v.307, pp.62 - 71
- Indexed
- SCIE
SCOPUS
- Journal Title
- TOXICOLOGY AND APPLIED PHARMACOLOGY
- Volume
- 307
- Start Page
- 62
- End Page
- 71
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/13040
- DOI
- 10.1016/j.taap.2016.07.013
- ISSN
- 0041-008X
- Abstract
- Impaired immune responses in skin play a pivotal role in the development and progression of chemical-associated inflammatory skin disorders. In this study, we synthesized new flavonoid derivatives from macakurzin C, and identified in vitro and in vivo efficacy of a potent anti-inflammatory flavonoid, Compound 14 (CPD 14), with its underlying mechanisms. In lipopolysaccharide (LPS)-stimulated murine macrophages and IFN-gamma/TNF-alpha-stimulated human keratinocytes, CPD 14 significantly inhibited the release of inflammatory mediators including nitric oxide (NO), prostaglandins, and cytokines (IC50 for NO inhibition in macrophages: 4.61 mu M). Attenuated NF-kappa B signaling and activated Nrf2/HO-1 pathway were responsible for the anti-inflammatory effects of CPD 14. The in vivo relevance was examined in phorbol 12-myristate 13-acetate (TPA)-induced acute skin inflammation and oxazolone-induced atopic dermatitis models. Topically applied CPD 14 significantly protected both irritation- and sensitization-associated skin inflammation by suppressing the expression of inflammatory mediators. In summary, we demonstrated that a newly synthesized flavonoid, CPD 14, has potent inhibitory effects on skin inflammation, suggesting it is a potential therapeutic candidate to treat skin disorders associated with excessive inflammation. (C) 2016 Elsevier Inc. All rights reserved.
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