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1
Content available remote The effect of some ε-aminocaproic acid derivatives on platelet responses.
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EN
ε-Aminocaproic acid (EACA) is a synthetic low molecular drug with antifibrinolytic activity. However, treatment with this drug can be incidentally associated with an increased thrombotic tendency. The aim of the present work was to test synthetic EACA derivatives for their antiplatelet activities. We investigated the effect of three EACA derivatives with antifibrinolytic activity: I. ε-aminocaproyl-L-leucine hydrochloride (HClH-EACA-L-Leu-OH), II. ε-aminocaproyl-L-(S-benzyl)-cysteine hydrochloride (HClH-EACA-L-Cys(S-Bzl)-OH) and III. ε-aminocaproyl-L-norleucine (H-EACA-L-Nle-OH) on platelet responses (aggregation and adhesion) and on their integrity. It was found that: 1. as judged by LDH release test, none of the tested compounds, up to 20 mM, was toxic to platelets, 2. in comparison with EACA, all the synthetic derivatives inhibited much stronger the ADP- and collagen-induced aggregation of platelets suspended in plasma (platelet rich plasma) and aggregation of these cells in whole blood, 3. EACA and its derivatives exerted a similar inhibitory effect on the thrombin-induced adhesion of platelets to fibrinogen-coated surfaces. Since platelet activation and blood coagulation are tightly associated processes, the antiplatelet properties of EACA derivatives are expected to indicate reduced thrombotic properties of these derivatives compared to EACA.
EN
Chitosan derivatives were obtained by chemical (MW of 6 kDa, DD 99% - Ch6/99; MW13 kDa, DD 98% - Ch13/98) and enzymatic (MW of 5 kDa, DD 85% - Ch5/85; MW of 10 kDa, DD 85% - Ch10/85) depolymeri-sation of chitosan with a MW of 334 and 1000 kDa. Chitosan derivatives (almost identical MW pairs and different DD) possessed insignificant an-ticoagulant activity, did not promote human platelet aggregation and re-duced ADP or collagen-induced platelet aggregation. The studied sam-ples at a concentration of 2 mg/ml reduced the aggregation of platelets more than twice induced in 2x10-6M and 1x10-5M concentrations; at weak activation in 2x10-6M, the Ch10/85 sample was the most effective. The Ch6/99 and Ch13/98 samples were 20 times more effective at the inhibi-tion of collagen-induced platelet aggregation than the Ch10/85 sample. The latter can be explained by the greater value of positive charge (DD) and polydispersity (Mw/Mn) of chitosan samples obtained by chemical de-polymerisation
5
63%
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2002
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tom 53
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nr 4,1
EN
In retrospect, basic research in the fields of NO and cyclic GMP during thev past two decades appears to have followed a logical course beginning with the findings that NO and cyclic GMP are vascular smooth muscle relaxants, that nitroglycerin relaxes smooth muscle by metabolism to NO, progressing to the discovery that mammalian cells synthesize NO, and finally the revelation that NO is a neurotransmitter mediating vasodilation in specialized vascular beds. A great deal of basic and clinical research on the physiological and pathophysiological roles of NO in cardiovascular function has been conducted since the discovery that EDRF is NO. The new knowledge on NO should enable investigators in this field to develop novel and more effective therapeutic strategies for the prevention, diagnosis and treatment of numerous cardiovascular disorders. Since NO elicits a protective and beneficial action in many disease states, novel NO donor drugs for clinical use should prove to be very effective drugs for the treatment of essential hypertension, stroke, coronary artery disease, vascular complications of diabetes, impotency and other disorders involving the vascular system.
EN
ε-Aminocaproic acid (EACA) is a synthetic low molecular drug with antifibrinolytic activity. However, treatment with this drug can be incidentally associated with an in­creased thrombotic tendency. The aim of the present work was to test synthetic EACA derivatives for their antiplatelet activities. We investigated the effect of three EACA derivatives with antifibrinolytic activity: I. ε-aminocaproyl-L-leucine hydro­chloride (HCl*H-EACA-L-Leu-OH), II. ε-aminocaproyl-L-(S-benzyl)-cysteine hydrochlo­ride (HCl*H-EACA-L-Cys(S-Bzl)-OH) and III. ε-aminocaproyl-L-norleucine (H-EACA-L-Nle-OH) on platelet responses (aggregation and adhesion) and on their in­tegrity. It was found that: 1. as judged by LDH release test, none of the tested com­pounds, up to 20 mM, was toxic to platelets, 2. in comparison with EACA, all the syn­thetic derivatives inhibited much stronger the ADP- and collagen-induced aggrega­tion of platelets suspended in plasma (platelet rich plasma) and aggregation of these cells in whole blood, 3. EACA and its derivatives exerted a similar inhibitory effect on the thrombin-induced adhesion of platelets to fibrinogen-coated surfaces. Since platelet activation and blood coagulation are tightly associated processes, the antiplatelet properties of EACA derivatives are expected to indicate reduced throm- botic properties of these derivatives compared to EACA.
PL
Z 26 napojów alkoholowych (piwa, wina, wódki, koniaki) metodą destylacji próżniowej otrzymano destylat i pozostałość podestylacyjną. W napojach niedestylowanych i ich frakcjach oznaczono zawartość etanolu, pH, suchą masę i popiół.
EN
Vacuum distillation of 26 strong drinks (beer, wine, vodka, brandy) yielded distillate comprising ethanol and accompanying volatile compounds, and ethanol-free posdistillation residue comprising non-volatile compounds. Ethanol content, pH, dry mass and ash were determined in the non-distilled drinks and their individual fractions. Separation of ethanol from ist accompanying compounds is expected to enable determination of the effects of the latter on: coagulation system, fibrinolysis, and hemostatic function of blood platelets.
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