Anti-senescence effects of 4-methoxychalcone and 4-bromo-4'-methoxychalcone on human endothelial cells.
Drug Discov Ther
; 18(3): 199-206, 2024.
Article
em En
| MEDLINE
| ID: mdl-38987208
ABSTRACT
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Senescência Celular
/
Células Endoteliais
/
Chalconas
/
Fibroblastos
Limite:
Humans
Idioma:
En
Revista:
Drug Discov Ther
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Malásia