1. Design, synthesis and biological evaluation of hesperetin derivatives as potent anti-inflammatory agent
- Author
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Yi-Long Zhang, Taotao Ma, Chen Huang, Hai-Wen Ding, Ai-Ling Huang, Bo Li, Jun Li, and Xiao-Ming Meng
- Subjects
0301 basic medicine ,MAPK/ERK pathway ,Antioxidant ,medicine.drug_class ,MAP Kinase Signaling System ,medicine.medical_treatment ,Cell ,Anti-Inflammatory Agents ,Pharmacology ,Nitric Oxide ,Neuroprotection ,Anti-inflammatory ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,0302 clinical medicine ,In vivo ,Drug Discovery ,medicine ,Animals ,Chemistry ,Interleukin-6 ,Tumor Necrosis Factor-alpha ,Hesperidin ,Macrophages ,Hesperetin ,NF-kappa B ,General Medicine ,In vitro ,Mice, Inbred C57BL ,030104 developmental biology ,medicine.anatomical_structure ,RAW 264.7 Cells ,Biochemistry ,Liver ,030220 oncology & carcinogenesis ,Chemical and Drug Induced Liver Injury - Abstract
A flavonoid hesperetin is reported to have a variety of biological activities, including anticancer, antiviral, antioxidant, neuroprotective and anti-inflammatory properties. Thirty-one novel hesperetin derivatives were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells and CCl4-induced acute liver injury model. Among these compounds, 5b displayed the excellent anti-inflammatory activity on decreasing NO, IL-6 and TNF-α both in vitro and vivo. In addition, 5b could also reduce the release of NO, IL-6 and TNF-α production by LPS stimulated RAW 264.7 cell through MAPK and NF-κB signaling pathway in a concentration dependent manner. From in vivo study, it was also observed that 5b attenuated liver histopathologic changes in mouse models.
- Published
- 2017