%0 Journal Article
%T Anti-senescence effects of 4-methoxychalcone and 4-bromo-4'-methoxychalcone on human endothelial cells.
%A Tien XY
%A Lee YK
%A Wong PF
%A Khor YS
%A Murugan DD
%A Abdullah I
%J Drug Discov Ther
%V 18
%N 3
%D 2024
%M 38987208
暂无%R 10.5582/ddt.2024.01034
%X Senolytics are drugs that specifically target senescent cells. Flavonoids such as quercetin and fisetin possess selective senolytic activities. This study aims to investigate if chalcones exhibit anti-senescence activities. Anti-senescence effect of 11 chalcone derivatives on the replicative senescence human aortic endothelial cells (HAEC) and human fetal lung fibroblasts (IMR90) was evaluated. Compound 2 (4-methoxychalcone) and compound 4 (4-bromo-4'-methoxychalcone) demonstrated increased cytotoxicity in senescent HAEC compared to young HAEC, with significant differences on IC50 values. Their anti-senescence effects on HAEC exceeded fisetin. Higher selectivity of compound 4 toward HAEC over IMR90 could be attributed to 4-methoxy (4-OMe) substitution at ring A (R1). Chalcone derivatives have potentials as senolytics in mitigating replicative senescence, warranting further research and development on chalcones as anti-senescent agent.