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Updated: Feb 25, 2026
Facilitating Drug Discovery: An Automated High-content Inflammation Assay in Zebrafish
Published on: July 16, 2012
Design, synthesis and biological evaluation of hesperetin derivatives as potent anti-inflammatory agent
Hai-Wen Ding1, Ai-Ling Huang1, Yi-Long Zhang1
1The Key Laboratory of Major Autoimmune Diseases, Anhui Province, Anhui Institute of Innovative Drugs, School of Pharmacy, Anhui Medical University, People's Republic of China; The Key Laboratory of Anti-inflammatory of Immune medicines, Ministry of Education, People's Republic of China; Institute for Liver Diseases of Anhui Medical University, People's Republic of China.
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.
