Cationic amphiphilic drugs and platelet phospholipase A2 (cPLA2)

Further studies on the mechanism of antiphagocyte-antioxidative effect of H1-antihistamines

“…Human blood collection and neutrophils separation were processed as described earlier [1,2]. For chemiluminescence (CL) studies, whole anticoagulated blood was diluted 50 times with PBS.…”

“…Besides their antihistaminic activities, H 1 -receptor antagonists possess other pharmacological properties; anti-infl ammatory action, inhibition of blood platelet function and antioxidative effects [1,2]. The mechanism(s) responsible for the nonspecifi c non-receptor operated activity of H 1 -antihistamines is not fully understood and may be at extra-and intracellular site of neutrophils (polymorphonuclear leukocytes).…”

H1- antihistamines and activated blood platelets

“…Blood was obtained from healthy male donors. Blood platelets were isolated by differential centrifugation as previously described [5,6]. Citrated blood, mixed with Tyrode's solution (1:1), was used for ADP (30 µmol/ L)-and PMA (0.1 µmol/L)-induced whole blood aggregation.…”

Antiplatelet activity of BRX-018, (6aS,cis)-Malonic acid 3-acetoxy-6a9-bis-(2-methoxycarbonyl-acetoxy)-6,6a,7,11b-tetrahydro-indeno[2,1-c]chromen-10-yl ester methylester

“…The stimulation of platelets with different stimuli resulted in the early activation of Ca 2+ -dependent cytosolic phospholipase A 2 (PLA 2 ), which hydrolyzes AA from the membrane phospholipids of platelets [9,10]. The liberated AA is metabolized via cyclooxygenase (COX) pathway to form endoperoxides, prostaglandins (PH), and the final products, thromboxane (TX) A 2 [11,12].…”