In vitro antioxidant properties of calcium dobesilate.
Calcium dobesilate, a vascular protective agent, was tested in vitro for its scavenging action against oxygen free radicals. Calcium dobesilate was as potent as rutin to scavenge hydroxyl radicals (IC50 = 1.1 vs 0.7 microM, respectively). It was also able to scavenge superoxide radicals, but with 23 times less potency than rutin (IC50 = 682 vs 30 microM, respectively). Calcium dobesilate significantly reduced platelet activating factor (PAF)-induced chemiluminescence in human PMN cells and lipid peroxidation by oxygen free radicals in human erythrocyte membranes, although these actions required calcium dobesilate concentrations > or = 50 microM. Finally, in cultured bovine aortic endothelial cells, magnesium dobesilate reduced the increase in cytosolic free calcium induced by hydrogen peroxide and inhibited phenazine methosulfate-induced cell potassium loss. In conclusion, calcium dobesilate was effective in scavenging hydroxyl radicals in vitro, at therapeutically relevant concentrations. Conversely, higher concentrations of the compound were required to scavenge superoxide radicals or to protect the cells against the deleterious effects of intracellular reactive oxygen species. Further studies in vivo are required to determine if these antioxidant properties of calcium dobesilate can play a role in its vascular protective mechanisms.
Brunet
J
J
INSERM U400, Faculté de Médecine, Créteil, France.
Farine
J C
JC
Garay
R P
RP
Hannaert
P
P
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D001011:Aorta / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D002123:Calcium Dobesilate / Q000494:pharmacology*; D002417:Cattle; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D004910:Erythrocyte Membrane / Q000187:drug effects; D016166:Free Radical Scavengers / Q000494:pharmacology*; D006490:Hemostatics / Q000494:pharmacology; D006801:Humans; D017665:Hydroxyl Radical / Q000378:metabolism; D015227:Lipid Peroxidation / Q000187:drug effects; D008163:Luminescent Measurements; D009504:Neutrophils / Q000187:drug effects; D010972:Platelet Activating Factor; D011188:Potassium / Q000378:metabolism; D013481:Superoxides / Q000378:metabolism; D019820:Xanthine / Q000032:analysis; D014969:Xanthine Oxidase / Q000032:analysis
D000975:Antioxidants; D016166:Free Radical Scavengers; D006490:Hemostatics; D010972:Platelet Activating Factor; D013481:Superoxides; D019820:Xanthine; D017665:Hydroxyl Radical; D002123:Calcium Dobesilate; D014969:Xanthine Oxidase; D011188:Potassium; D002118:Calcium