Design, synthesis, and anti-inflammatory activity of caffeoyl salicylate analogs as NO production inhibitors

被引:10
作者
Yu, Pan [1 ]
Xia, Chao-Jie [1 ]
Li, Dong-Dong [1 ]
Ni, Jun-Jun [1 ]
Zhao, Lin-Guo [1 ]
Ding, Gang [2 ]
Wang, Zhen-Zhong [2 ]
Xiao, Wei [2 ]
机构
[1] Nanjing Forestry Univ, Coll Chem Engn, 159 Long Pan Rd, Nanjing 210037, Jiangsu, Peoples R China
[2] Jiangsu Kanion Pharmaceut Co Ltd, 58 Haichang South Rd, Lianyungang 222001, Jiangsu, Peoples R China
关键词
Chlorogenic acid; Anti-inflammatory; Caffeoyl salicylate analogs; Nitric oxide synthase; CHLOROGENIC ACID; DATABASE;
D O I
10.1016/j.fitote.2018.05.029
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Chlorogenic acid (CGA) has been reported to exhibit potent anti-inflammatory activity. However, the development of anti-inflammatory agent based on CGA has not been investigated. In this paper, a series of caffeoyl salicylate compounds derived from CGA were designed, synthesized, and evaluated by LPS-induced nitric oxide synthase inhibition and QRT-PCR technique. Most compounds showed modest activity to inhibit production of nitric oxide (NO) in RAW 264.7 cells induced by lipopolysaccharides (LPS). Among these compounds, QRT-PCR and western blotting results indicated that compounds 6b, 6c, 6f, 6g and D104 that possess 5-member ring or 6-member ring caused a significant inhibition against expression of the iNOS2 in LPS-induced macrophages. In addition, cytotoxic assay displayed most derivatives have good safety in vitro. This new promising scaffold could be further exploited for the development of anti-inflammatory agent in the future.
引用
收藏
页码:25 / 33
页数:9
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