Stereospecific and non-stereospecific effects of ibuprofen on human platelet and polymorphonuclear leukocyte functions.
This study compares biological activities of racemic ibuprofen (rac-IBU) and its S(+) and R(-) enantiomeres in human platelet and polymorphonuclear cells (PMN). Rac-IBU inhibited cyclooxygenase-related platelet functions (aggregation, thromboxane (TX) B2 formation) in vitro, the S-(+) enantiomer being 40-100-times more active than the R-(-) form. rac-IBU also inhibited PMN functions (O2- generation, beta-glucuronidase release). These effects in PMN were not stereospecific. The data suggest cyclooxygenase-independent actions of ibuprofen in human PMN which may contribute to its antiinflammatory effects in vivo.
Villanueva
M
M
Institut für Pharmakologie, Heinrich-Heine-Universität Düsseldorf, FRG.
Heckenberger
R
R
Palmér
M
M
Schrör
K
K
D001792:Blood Platelets / Q000187:drug effects* / Q000201:enzymology; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology; D015777:Eicosanoids / Q000096:biosynthesis; D005966:Glucuronidase / Q000378:metabolism; D006801:Humans; D007052:Ibuprofen / Q000494:pharmacology*; D066298:In Vitro Techniques; D009504:Neutrophils / Q000187:drug effects*; D010101:Oxygen Consumption / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D013237:Stereoisomerism; D013481:Superoxides / Q000378:metabolism
D016861:Cyclooxygenase Inhibitors; D015777:Eicosanoids; D010975:Platelet Aggregation Inhibitors; D013481:Superoxides; D005966:Glucuronidase; D007052:Ibuprofen