N. Ivanovska et al., EFFECT OF SOME HYDROXYCOUMARINS ON COMPLEMENT-MEDIATED HEMOLYSIS IN HUMAN SERUM, Methods and findings in experimental and clinical pharmacology, 16(8), 1994, pp. 557-562
Coumarin derivatives are known to possess antiinflammatory and antimet
astatic 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 methylat
ed derivatives and non-cell system participating in inflammatory proce
sses, comprised of serum complement proteins, were investigated in vit
ro. 7-Methylesculin, esculin 5Ac and esculetin 2Ac exhibited good inhi
bition on classical pathway (CP) activity and scoparone strongly reduc
ed alternative pathway (AP) activity in normal human serum (NHS). Some
of the hydroxycoumarins were able to enhance hemolysis. Seven derivat
ives were tested in C1 and C3 functional assays, as 7-methylesculin ap
peared 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 sim
ultaneously in vitro.