Bioorganic and Medicinal Chemistry Letters p. 1616 - 1619 (2017)
Update date:2022-08-03
Topics:
Wu, Jianzhang
Ren, Jiye
Yao, Song
Wang, Jiabing
Huang, Lili
Zhou, Peng
Yun, Di
Xu, Qing
Wu, Shoubiao
Wang, Zhankun
Qiu, Peihong
Novel structure compounds (WS) containing 3,4,5-trimethoxyphenyl and acyl pyrazole were designed and synthesized based combination principles. Among them, WS13 was screened out to possess desirable anti-oxidative activity in vitro. Cell survival assay and apoptosis experiment in H2O2 induced PC12 cells injury model all showed that its cytoprotection exhibited a concentration-effect manner. WS13 at 10?μM could remove ROS with equal effiency to edaravone. Further, it clearly activated Nrf2 nuclear translocation and upregulated GCLC mRNA transcription and protein expression in dose-dependent manner, and its cytoprotection was reversed by GCLC protein inhibitor. In total, WS13 with further promotion can serve as Nrf2-GCLC activator in anti-oxidative therapy.
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