title: Synthesis, Characterization, and Anti-Inflammatory Activities of Methyl Salicylate Derivatives Bearing Piperazine Moiety.
abstract: In this study, a new series of 16 methyl salicylate derivatives bearing a piperazine moiety were synthesized and characterized. The in vivo anti-inflammatory activities of target compounds were investigated against xylol-induced ear edema and carrageenan-induced paw edema in mice. The results showed that all synthesized compounds exhibited potent anti-inflammatory activities. Especially, the anti-inflammatory activities of compoundsM15andM16were higher than that of aspirin and even equal to that of indomethacin at the same dose. In addition, the in vitro cytotoxicity activities and anti-inflammatory activities of four target compounds were performed in RAW264.7 macrophages, and compoundM16was found to significantly inhibit the release of lipopolysaccharide (LPS)-induced interleukin (IL)-6 and tumor necrosis factor (TNF)-α in a dose-dependent manner. In addition, compoundM16was found to attenuate LPS induced cyclooxygenase (COX)-2 up-regulation. The current preliminary study may provide information for the development of new and safe anti-inflammatory agents.
authors.affiliation: Department of Life Science, Huzhou Teachers' College, Huzhou 313000, China. ljfljf@hutc.zj.cn.
authors.forename: Jingfen
authors.initials: J
authors.lastname: Li
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. yinyong1220@163.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Yin
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. w_lsheng@163.com.
authors.forename: Lisheng
authors.initials: L
authors.lastname: Wang
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. gxulpyun@163.com.
authors.forename: Pengyun
authors.initials: P
authors.lastname: Liang
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. lixiaomeng0108@163.com.
authors.forename: Menghua
authors.initials: M
authors.lastname: Li
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. wendaoliuxu@163.com.
authors.forename: Xu
authors.initials: X
authors.lastname: Liu
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. wulichuan@126.com.
authors.forename: Lichuan
authors.initials: L
authors.lastname: Wu
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China. yanghua6316@sina.com.
authors.forename: Hua
authors.initials: H
authors.lastname: Yang
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002351:Carrageenan / Q000009:adverse effects; D051546:Cyclooxygenase 2 / Q000378:metabolism; D016207:Cytokines / Q000378:metabolism; D004195:Disease Models, Animal; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005786:Gene Expression Regulation / Q000187:drug effects; D008070:Lipopolysaccharides / Q000009:adverse effects; D051379:Mice; D015394:Molecular Structure; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D000067996:RAW 264.7 Cells; D012459:Salicylates / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014992:Xylenes / Q000009:adverse effects
chemical_list: D000893:Anti-Inflammatory Agents; D016207:Cytokines; D008070:Lipopolysaccharides; D010879:Piperazines; D012459:Salicylates; D014992:Xylenes; D000077489:Piperazine; D002351:Carrageenan; C077623:Ptgs2 protein, mouse; D051546:Cyclooxygenase 2; C033069:methyl salicylate
keywords: anti-inflammatory activity; derivatives; inflammation; piperazine; salicylate