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Methods Find Exp Clin Pharmacol ; 16(8): 557-62, 1994 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-7760580

RESUMO

Coumarin derivatives are known to possess antiinflammatory and antimetastatic properties due to their direct action on cells, predominantly on macrophages. In the present study the interactions between esculin, esculetin, fraxin, fraxetin, as well as their acetylated and methylated derivatives and non-cell system participating in inflammatory processes, comprised of serum complement proteins, were investigated in vitro. 7-Methylesculin, esculin 5Ac and esculetin 2Ac exhibited good inhibition on classical pathway (CP) activity and scoparone strongly reduced alternative pathway (AP) activity in normal human serum (NHS). Some of the hydroxycoumarins were able to enhance hemolysis. Seven derivatives were tested in C1 and C3 functional assays, as 7-methylesculin appeared to be the strongest inhibitor of both activities. Esculin (En) and scopoletin (St) altered the effect of other complement activators (heat aggregated IgG, suramin, and zymosan) when applied with them simultaneously in vitro.


Assuntos
Proteínas do Sistema Complemento/fisiologia , Cumarínicos/farmacologia , Hemólise/efeitos dos fármacos , Soluções Tampão , Complemento C1/fisiologia , Complemento C3/fisiologia , Proteínas Inativadoras do Complemento/farmacologia , Via Alternativa do Complemento/efeitos dos fármacos , Via Clássica do Complemento/efeitos dos fármacos , Esculina/farmacologia , Humanos , Técnicas In Vitro , Escopoletina/farmacologia
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