Inhibition of chemiluminescence by carvedilol in the cell-free system, whole human blood and blood cells.
Carvedilol inhibits luminol-enhanced chemiluminescence of reactive oxygen metabolites in vitro. In this study it was found that, in the cell-free system, carvedilol dose-dependently decreased chemiluminescence in the following ranking order of radicals: hydroxyl radical > hydrogen peroxide > superoxide radical. The inhibition of myeloperoxidase was significant with carvedilol concentrations of 10 and 100 micromol/l and manifested in the concentration-dependent shift of chemiluminescence peaks to the right. In whole blood, carvedilol in concentrations of 10 and 100 micromol/l significantly inhibited chemiluminescence induced by both receptor-bypassing stimuli (A23187, PMA) and receptor-operating stimuli (fMLP, OpZ). Carvedilol dose-dependently inhibited chemiluminescence of isolated human polymorphonuclear leucocytes in the ranking order of stimuli: A23187 > OpZ > fMLP. In the presence of blood platelets, carvedilol did not substantially change chemiluminescence induced by fMLP and OpZ, while it was much more effective on chemiluminescence stimulated with calcium ionophore A23187. This could be the result of the supportive effect of serotonin liberated from platelets by A23187.
Nosál
R
R
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Slovak Republic. exfarano@savba.sk
Jancinová
V
V
Cíz
M
M
Drábiková
K
K
Lojek
A
A
Fábryová
V
V
D000328:Adult; D001773:Blood Cells / Q000187:drug effects*; D001792:Blood Platelets / Q000187:drug effects; D002227:Carbazoles / Q000494:pharmacology*; D000077261:Carvedilol; D045744:Cell Line, Tumor; D002474:Cell-Free System; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D007962:Leukocytes / Q000187:drug effects; D008163:Luminescent Measurements; D008297:Male; D008875:Middle Aged; D009195:Peroxidase / Q000037:antagonists & inhibitors / Q000378:metabolism; D011412:Propanolamines / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism
D002227:Carbazoles; D004791:Enzyme Inhibitors; D011412:Propanolamines; D017382:Reactive Oxygen Species; D000077261:Carvedilol; D009195:Peroxidase