[Effect of chronic administration of epaden and acetylsalicylic acid on the antithrombotic potential of blood vessel walls in rabbits]. / Vliianie khronicheskogo vvedeniia krolikam épadena i atsetilsalitsilovoi kisloty na protivotromboticheskii potentsial sosudistoi stenki.

The effect of a new domestic polyunsaturated fatty acid (PUFA) concentrate called epaden on the blood coagulation system was studied in comparison with acetylsalicylic acid (ASA). The antithrombotic potential of the blood vessel wall was determined by release of the inhibitors of thrombocyte aggregation, fibrinolysis activators, and anticoagulants in rabbits under immobilization induced stress conditions. In the control group, the immobilization stress resulted in a decrease of the collagen-induced platelet aggregation, a drop in the fibrinogen level, and an increase in the tissue-type plasminogen activator (t-PA) activity. The administration of ASA and epaden reduced a drop in the fibrinogen level caused by the immobilization stress. Animals receiving epaden showed a decrease in the ADP-induced platelet aggregation and an increase in the t-PA activity in comparison with the levels before modeling stressed conditions. No such effect was observed in the group treated with ASA. It is suggested that the additional antithrombotic effect of epaden observed under the immobilization stress conditions is related to a protective action of this substance on the vessel wall.

[Effect of combined administration of acetylsalicylic acid and antioxidants on cellular and plasma hemostasis]. / Vliianie sochetannogo primeneniia atsetilsalitsilovoi kisloty s antioksidantami na kletochnyi i plazmennyi gemostaz.

It was found that upsovit (acetylsalicylic acid, 330 mg; ascorbic acid, 200 mg), composition 1 (acetylsalicylic acid, 330 mg; ascorbic acid, 200 mg; hypoxen, 50 mg), and composition 2 (acetylsalicylic acid, 330 mg; ascorbic acid, 200 mg; hypoxen, 100 mg) inhibit thrombocyte aggregation in vitro. Hypoxen per se induces the aggregation of thrombocytes, but inhibited the ADP aggregation. Intravenous injections of upsovit in rabbits did not influence the ADP aggregation, but inhibited the collagen aggregation, while composition 2 inhibited the aggregation processes of both types. Besides, the intravenous injections of upsovit decreased the thromboplastin time and the activated partial thromboplastin time (APTT) and reduced the protein C activity, while influencing neither the heparin cofactor activity of antithrombin III nor the level of fibrinogen and its degradation products. In contrast, composition II did not change the thromboplastin time, APTT, and the protein C activity, but increased the heparin cofactor activity.

Hydrolysis of anandamide and eicosapentaenoic acid ethanolamide in mouse splenocytes.

The hydrolysis of anandamide has been studied in mouse splenocytes using tritiated anandamide analogs labeled in the acyl- or ethanolamide parts of the molecule. [3H]Anandamide undergoes rapid (t(1/2) = 2.5 min) uptake and hydrolysis, yielding ethanolamine and arachidonic acid. The anandamide hydrolysis in splenocytes is sensitive to inhibition by phenylmethylsulfonyl fluoride, and it is assumed that the observed activity is due to fatty acid amide hydrolase, which inactivates anandamide in central and peripheral tissues. Eicosapentaenoic acid ethanolamide and the 15-hydroxy-derivative of anandamide are shown to be amidohydrolase substrates as well. The fatty acids derived from hydrolytic cleavage of acylethanolamines undergo rapid oxidation by splenocyte lipoxygenase, yielding the corresponding 12-hydroxy-derivatives. Oxygenated ethanolamide derivatives were not found. The data suggest that polyenoic fatty acid ethanolamides are metabolic precursors of eicosanoids in splenocytes and that amide bond hydrolysis is the key point in switching of biological activity spectra between endocannabinoids and oxylipins.