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Novel Resveratrol Derivatives as Dual PDE4 Inhibitors and Free Radical Scavengers: Rational Design, Synthesis, and
Youzhi Wang1,2, Huizhen Shen1, Ying Liang1
1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
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A novel class of resveratrol derivatives as dual PDE4 (Phosphodiesterase 4) inhibitors and free radical scavengers for the treatment of COPD (chronic obstructive pulmonary disease) was developed in this study. In vitro, the most promising compound WYZ69 showed similar PDE4 inhibitory activity and anti-inflammatory activity to rolipram and better DPPH free radical scavenging ability and anti-lipid peroxidative activity than edaravone. In addition, compound WYZ69 turned out to be a novel ferroptosis inhibitor, which significantly inhibited ferroptosis as a free radical scavenger, decreased the levels of ROS (reactive oxygen species), increased the expression of GPX4 (Glutathione peroxidase 4), and decreased the expression of transferrin in A549 cells induced by a ferroptosis activator, RSL3 ((1S,3R)-RSL3). In vivo, it exhibited a half-life of 1.63 h in mice and moderate anti-inflammatory activity in mice induced by LPS (Lipopolysaccharide). Hence, these findings suggest that compound WYZ69 is a promising dual PDE4 inhibitor and free radical scavenger with anti-inflammatory and anti-ferroptosis activities for the treatment of COPD.
