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A newly synthesized macakurzin C-derivative attenuates acute and chronic skin inflammation: The Nrf2/heme oxygenase signaling as a potential target

Title
A newly synthesized macakurzin C-derivative attenuates acute and chronic skin inflammation: The Nrf2/heme oxygenase signaling as a potential target
Author
배옥남
Keywords
Synthetic flavonoid; Anti-inflammatory activity; TPA-induced acute inflammation; Oxazolone-induced atopic dermatitis; NF-KAPPA-B; TRANSCRIPTION FACTORS NRF2; ATOPIC-DERMATITIS; TNF-ALPHA; ANTIINFLAMMATORY ACTIVITY; BIOLOGICAL EVALUATION; CONTACT-DERMATITIS; INDUCED EXPRESSION; HEME OXYGENASE; ACTIVATION
Issue Date
2016-09
Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
Citation
TOXICOLOGY AND APPLIED PHARMACOLOGY, v. 307, Page. 62-71
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.
URI
https://www.sciencedirect.com/science/article/pii/S0041008X16301971http://repository.hanyang.ac.kr/handle/20.500.11754/69318
ISSN
0041-008X; 1096-0333
DOI
10.1016/j.taap.2016.07.013
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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