期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 15, 页码 2998-3004出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.05.030
关键词
Aza resveratrol; Chalcone; Parallel; Anti-inflammatory; Acute lung injury
资金
- National Natural Science Foundation of China - China [81402783, 21272179, 21472142]
- Zhejiang Provincial Natural Science Foundation - China [LQ14H310003]
- Wenzhou Public Welfare Science and Technology Project - China [2014Y0398]
- National '863' Project - China [2011AA02A113]
Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. It has been reported that both resveratrol and chalcone derivatives could ameliorate lung injury induced by inflammation. A series of paralleled Aza resveratrol-chalcone compounds (5a-5m, 6a-6i) were designed, synthesized and screened for anti-inflammatory activity. A majority showed potent inhibition on the IL-6 and TNF-alpha expression-stimulated by LPS in macrophages, of which compound 6b is the most potent analog by inhibition of LPS-induced IL-6 release in a dose-dependent manner. Moreover, 6b exhibited protection against LPS-induced acute lung injury in vivo. These results offer further insight into the use of Aza resveratrol-chalcone compounds for the treatment of inflammatory diseases, and the use of compound 6b as a lead compound for the development of anti-ALI agents. (C) 2015 Elsevier Ltd. All rights reserved.
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