Elastase release by stimulated neutrophils inhibited by flavonoids: importance of the catechol group.
Pathogenesis of chronic inflammatory diseases is associated with excessive elastase release through neutrophil degranulation. In the present study, inhibition of human neutrophil degranulation by four flavonoids (myricetin, quercetin, kaempferol, galangin) was evaluated by using released elastase as a biomarker. Inhibitory potency was observed in the following order: quercetin > myricetin > kaempferol = galangin. Quercetin, the most potent inhibitor of elastase release also had a weak inhibitory effect on the enzyme catalytic activity. Furthermore, the observed effects were highly dependent on the presence of a catechol group at the flavonoid B-ring. The results of the present study suggest that quercetin may be a promising therapeutic agent in the treatment of neutrophil-dependent inflammatory diseases.
Kanashiro
Alexandre
A
Departamento de Física e Química, Faculdade de Ciências Farmacêuticas de Ribeirão Preto da Universidade de São Paulo, Avenida do Café, s/n, 14040-903, Ribeirão Preto, SP, Brasil.
Souza
Joel G
JG
Kabeya
Luciana M
LM
Azzolini
Ana Elisa C S
AE
Lucisano-Valim
Yara Maria
YM
D002396:Catechols / Q000494:pharmacology*; D004121:Dimethyl Sulfoxide / Q000494:pharmacology; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors* / Q000097:blood / Q000378:metabolism*
D002396:Catechols; D005419:Flavonoids; D010196:Pancreatic Elastase; D004121:Dimethyl Sulfoxide