Inhibitory Effects of a Novel Chrysin-Derivative, CPD 6, on Acute and Chronic Skin Inflammation
- Title
- Inhibitory Effects of a Novel Chrysin-Derivative, CPD 6, on Acute and Chronic Skin Inflammation
- Author
- 배옥남
- Keywords
- skin inflammation; synthetic flavonoid; chrysin; chrysin derivatives; Nrf2; HO-1 signaling
- Issue Date
- 2019-05
- Publisher
- MDPI
- Citation
- INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, v. 20, No. 11, Article no. 2607
- Abstract
- The skin is an important physiological barrier against external stimuli, such as ultraviolet radiation (UV), xenobiotics, and bacteria. Dermal inflammatory reactions are associated with various skin disorders, including chemical-induced irritation and atopic dermatitis. Modulation of skin inflammatory response is a therapeutic strategy for skin diseases. Here, we synthesized chrysin-derivatives and identified the most potent derivative of Compound 6 (CPD 6). We evaluated its anti-inflammatory effects in vitro cells of macrophages and keratinocytes, and in vivo dermatitis mouse models. In murine macrophages stimulated by lipopolysaccharide (LPS), CPD 6 significantly attenuated the release of inflammatory mediators such as nitric oxide (NO) (IC50 for NO inhibition: 3.613 M) and other cytokines. In cultured human keratinocytes, CPD 6 significantly attenuated the release of inflammatory cytokines induced by the combination of IFN- and TNF-, UV irradiation, or chemical irritant stimulation. CPD 6 inhibited NFB and JAK2/STAT1 signaling pathways, and activated Nrf2/HO-1 signaling. In vivo relevancy of anti-inflammatory effects of CPD 6 was observed in acute and chronic skin inflammation models in mice. CPD 6 showed significant anti-inflammatory properties both in vitro cells and in vivo dermatitis animal models, mediated by the inhibition of the NFB and JAK2-STAT1 pathways and activation of Nrf2/HO-1 signaling. We propose that the novel chrysin-derivative CPD 6 may be a potential therapeutic agent for skin inflammation.
- URI
- https://www.mdpi.com/1422-0067/20/11/2607https://repository.hanyang.ac.kr/handle/20.500.11754/113678
- ISSN
- 1422-0067
- DOI
- 10.3390/ijms20112607
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
- Files in This Item:
- 2019.05_배옥남_Inhibitory Effects of a Novel Chrysin-Derivative, CPD 6, on Acute and Chronic Skin Inflammation.pdfDownload
- Export
- RIS (EndNote)
- XLS (Excel)
- XML