Synthesis, Characterization, and Anti-Inflammatory Activities of Methyl Salicylate Derivatives Bearing Piperazine Moiety

Autor: Menghua Li, Lisheng Wang, Liang Pengyun, Yin Yong, Lichuan Wu, Liu Xu, Hua Yang, Jingfen Li
Rok vydání: 2016
Předmět:
Lipopolysaccharides
0301 basic medicine
Lipopolysaccharide
medicine.drug_class
Anti-Inflammatory Agents
Pharmaceutical Science
Xylenes
Carrageenan
030226 pharmacology & pharmacy
Article
Piperazines
Anti-inflammatory
Analytical Chemistry
salicylate
Mice
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
In vivo
Drug Discovery
medicine
Animals
Edema
Moiety
Physical and Theoretical Chemistry
anti-inflammatory activity
Molecular Structure
biology
Organic Chemistry
inflammation
piperazine
derivatives
Interleukin
Salicylates
Disease Models
Animal
Piperazine
RAW 264.7 Cells
030104 developmental biology
Gene Expression Regulation
chemistry
Biochemistry
Cyclooxygenase 2
Chemistry (miscellaneous)
biology.protein
Cytokines
Molecular Medicine
Tumor necrosis factor alpha
Cyclooxygenase
Zdroj: Molecules; Volume 21; Issue 11; Pages: 1544
Molecules
ISSN: 1420-3049
Popis: 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 compounds M15 and M16 were 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 compound M16 was 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, compound M16 was 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.
Databáze: OpenAIRE
Externí odkaz: