Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.4.21.5 (thrombin)
33,306 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In 260 male farmers (40-45 years) divided into 9 groups from different areas in France and Britain, coagulation, platelet aggregation, lipemia, fatty acids from plasma lipids and platelet phospholipids were determined in relation to the food intake evaluated by recall, weighing and chemical analysis of the diet. The clotting activity of platelets and their response to thrombin aggregation was significantly correlated on an individual basis with the intake of saturated fatty acids both in subsamples as well as in the whole study. Serum cholesterol was also significantly correlated with saturated fats but only on a group basis or on the totality of the study. Calcium, linolenic acid and alcohol in the diet were inversely related to certain platelet functions. Linoleic acid was inversely related to serum cholesterol and triglycerides. Dietary saturated fats were associated, with an increase in the platelet phospholipids not in saturated fatty acids but in 20:3 (n-9), known to promote platelet aggregation to thrombin, with a decrease in platelet cholesterol, also apparently regulating platelet functions. The present studies indicate that dietary saturated fats, calcium (hard water) and alcohol, influence platelet behaviour in a way strictly parallel to their known effect on coronary heart disease.
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PMID:Nutrients, platelet function and composition in nine groups of French and British farmers. 370 72

Successive thrombin modification by carbodiimide and aliphatic diamines decreases esterase and fibrin-coagulating activity of the enzyme. Modified thrombin causes no platelet aggregation. Water-soluble enzyme conjugates devoid of fibrinogen-coagulating action and possessing increased fibrinolytic affinity to the site of fibrin clot location have been obtained by covalent binding of chymotrypsin to modified thrombin.
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PMID:[Fibrinolytic action of an enzyme preparation covalently bound to modified thrombin]. 380 48

Pulmonary edema was induced by an intravenous infusion of bovine thrombin, 500 NIH/kg b.w., given in 5 min, in rats in which fibrinolysis had been inhibited by an intraperitoneal injection of the fibrinolysis inhibitor AMCA. Ninety minutes after termination of the thrombin infusion the lung weight was increased from 1.09 +/- 0.07 to 3.14 +/- 0.12 g due to edema. A high albumin concentration in the extravascular water indicated that the edema was a consequence of increased permeability in the microcirculation. In rats injected with the H1 histamine receptor antagonist mepyramine maleate and H2 receptor antagonist cimetidine after the thrombin infusion, the lung weight was significantly lower at 90 min (2.68 +/- 0.33 g), and the amount of edema as calculated morphometrically was slightly but significantly reduced. The concentration of albumin in the extravascular water (i.e. in the edema fluid) in rats subjected to histamine receptor blockade was unchanged, indicating that the slight decrease in edema was a result of decreased filtration pressure and not of an effect on microvascular permeability.
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PMID:Blockade of histamine receptors and thrombin-induced microembolic pulmonary edema in the rat. 383 50

The water extract of Hsien-Ho-T'sao (HHT) produced a dose-dependent inhibition on collagen-induced aggregation of platelet-rich plasma (PRP). The IC50 was about 3.5 mg/ml. In addition, HHT inhibited also the aggregation induced by ADP, A23187 or arachidonate in PRP. Greater inhibition was observed in the preparation of washed platelets. Increase of the calcium concentration in medium could not overcome the inhibitory effect of HHT. ATP release from platelets induced by collagen or A23187 was inhibited by HHT. In the presence of EDTA, ATP release caused by thrombin or A23187 was also inhibited by HHT. Malondialdehyde and thromboxane B2 formation was greatly inhibited by HHT in platelets challenged by collagen and thrombin. In arachidonate-stimulated platelets, thromboxane B2, but not malondialdehyde formation was inhibited. HHT showed more marked inhibition on aggregation in the presence of indomethacin, creatine phosphate/creatine phosphokinase or a combination of both. Hydrogen peroxide-induced hemolysis was marked reduced by HHT. It was concluded that HHT might have some membrane-active properties which interfered with the activation of phospholipase A2.
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PMID:Antiplatelet effect of hsien-ho-t'sao (Agrimonia pilosa). 392 4

Wakan-Yakus (traditional herbal drugs) such as Akyoh (Glutinum), Gaiyoh (Artemisiae folium), Sanshishi (Gardeniae fructus), Kizutsu (Aurantii fructus), and Taisoh (Zizyphi fructus) were studied in relation to their effects on blood coagulation-fibrinolysis. (1) All of the water extracts of the Wakan-Yakus prolonged aPTT and PT. The potency of the effectiveness on aPTT was in the order of Gaiyoh (Artemisiae folium) greater than Kizutsu (Aurantii fructus) greater than Sanshishi (Gardeniae fructus) greater than Taisoh (Zizyphi fructus) greater than Akyoh (Glutinum). (2) Gaiyoh (Artemisiae folium) greater than Kizutsu (Aurantii fructus) greater than Akyoh (Glutinum) greater than Taisoh (Zizyphi fructus) showed the antifibrinolytic effects in this order. On the other hand, Sanshishi showed the accelerating effect on fibrinolysis. (3) The inhibition modes of both thrombin and plasmin by Gaiyoh (Artemisiae folium) were shown to be competitive on Lineweaver-Burk plot. (4) Gaiyoh (Artemisiae folium) was gel-filtered on Sephadex G-25 column (1.5 X 90cm) equilibrated with distilled water at room temperature. Five fractions were obtained, and in the first to fourth fraction, strong anticoagulant effects on aPTT and PT were observed. We pooled first and second to make fraction I, and make fraction II from peak 3. The recovery rate was 4.2% by weight, and 36.7% by inhibition activity, and specific activity on the basis of inhibition to aPTT was 34.8% U/mg in the case with fraction II. Fraction I was found to be the same characteristically on blood coagulation. Fraction II was further purified by Sephadex LH-20 column (1.5 X 80 cm) at room temperature. Three fractions (Fraction IIa, IIb, IIc) were obtained, and the strong inhibitory effects was observed on both aPTT and PT in each fraction. The first fraction (fraction IIa) showed the strong inhibitory effect on aPTT, and the heightened specific activity with 17.6% as the recovery rate.
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PMID:Studies of Wakan-Yakus (traditional herbal drugs): especially on the effects of Gaiyoh (Artemisiae folium) on blood coagulation. 402 49

The following synthetic linear A alpha fibrinogen-like peptides were studied by NMR spectroscopy in aqueous solution: Ac-Asp(P10)-Phe(P9)-Leu-Ala-Glu-Gly(P5)-Gly(P4)-Gly(P3)-Val- Arg(P1)-Gly-(P1)-Pro-Arg(P3')-Val-NHCH3 (F-8), Ac-Phe-Leu-Ala-Glu-Gly-Gly(P4)-Gly(P3)-Val-Arg-Gly-Pro-NHCH3 (F-6), Ac-Leu-Ala-Glu-Gly-Gly(P4)-Gly(P3)-Val-Arg-Gly-Pro-NHCH3 (F-7), and Ac-Gly-Gly(P4)-Gly-(P3)-Val-Arg-Gly-Pro-NHCH3 (F-9). The temperature dependence of the amide proton chemical shift is smaller by approximately 22% for the Gly(P3) amide proton in F-9, F-6, and F-8 and is similarly smaller for the Gly(P4) amide proton in F-6 and F-8, but not F-9, relative to the other amide protons in these peptides. The exchange rates with solvent water for the Gly(P3) amide proton in each of these four peptides were determined by solvent spin saturation transfer experiments. The exchange rate constant for the Gly(P3) amide proton of F-8 was half that of the rate constant determined for this proton in F-9, F-7, and F-6. In conjunction with previously reported data for the rate of hydrolysis of the Arg(P1)-Gly(P1') bond by thrombin, these results suggest that there is a beta-bend at Gly(P5)-Gly(P4), possibly stabilized by salt links between Asp(P10) and Arg(P3') and between phosphorylated Ser(P14) and Arg(P7'), which brings Phe(P9) close to the hydrolyzable Arg-Gly bonds.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Mechanism of action of thrombin on fibrinogen: NMR evidence for a beta-bend at or near fibrinogen A alpha Gly(P5)-Gly(P4). 402 28

Esters of thiocholine were shown to inhibit the crosslinking of fibrin clots by the transamidating enzyme, fibrinoligase (thrombin-activated fibrin-stabilizing factor or activated Factor XIII). Inhibition depended on the nature of the acylating group with the phenylpropionyl, phenylbutyryl, and trans-cinnamoyl esters being most effective of the compounds tested so far. Use of the thiolesters made it possible for the first time to study the reactions of fibrinoligase in fully synthetic substrate systems. Enzyme-catalyzed acyl-group transfers from the thiol-esters to a fluorescent amine [N-(5-aminopentyl) - 5 - dimethylamino - 1 - naphthalenesulfonamide] could be readily demonstrated and measured.Trans-cinnamoylthiocholine reacted with fibrinoligase in a totally calcium-dependent manner in the absence of any added amine, thus providing the first evidence for an esterolytic pathway for this enzyme. Spectral qualities, as well as appreciable extent of solubility in water, would seem to make trans-cinnamoylthiocholine a specially suitable substrate for further studies.
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PMID:Thiolester substrates for transamidating enzymes: studies on fibrinoligase. 450 87

This study examined the role of colloids versus crystalloids in pulmonary edema associated with the increased pulmonary microvascular permeability secondary to thrombin-induced pulmonary microembolism. Each of 23 healthy dogs received an intravenous injection of thrombin and a fibrinolysis inhibitor, which induced a microembolic state with increased (fivefold) pulmonary lymphatic flow and a lymph/plasma (L/P) protein ratio typical of a permeability change. Seven dogs received no treatment, eight received 15 ml/kg 10% dextran 40 (D40), and eight received 60 ml/kg Ringer's lactate solution (RL). Pulmonary water was measured serially by thermal conductivity and terminally by wet/dry weights. This preparation produced significant hemolysis; however, L/P ratios of hemoglobin approached unity in all groups. Initially there was hemoconcentration, which was reversed by RL and even more so by D40. Both D40 and RL temporarily raised the pulmonary artery and pulmonary artery wedge pressures to 15 mm Hg; D40 more than doubled the cardiac output of control or RL subjects--this was associated with a reduced pulmonary arteriolar resistance (P less than 0.05). In the early stage PaO2 was better maintained with D40 (P less than 0.02). Lymph flow increased and was comparable in all groups, as were lung water and lung weight, which tripled in all three groups. Results of this study indicated that in the presence of a pulmonary microvascular leak, colloids in doses that produced comparable microvascular pressures did not increase lung water and did not accumulate in the pulmonary interstitium. Colloids were superior to crystalloids in maintaining cardiac output, pulmonary vascular resistance, and oxygen tension in the early period after microembolism.U
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PMID:Pulmonary microvascular leakage after microembolization and hemodilution. 617 75

The addition of thrombin to human platelets prelabeled with 32Pi led to significant loss of radioactivity in phosphatidylinositol 4,5-bisphosphate within 5 s, followed by recovery or even increase by 2 min. Loss of label from phosphatidylinositol phosphate was much less marked. Stimulated loss of label from phosphatidylinositol was not seen, while labeled phosphatidate increased severalfold. The principal labeled water-soluble phosphates observed, in addition to 32Pi and [32P] ATP, co-migrated with inositol diphosphate and inositol triphosphate. This suggests that a pool of polyphosphoinositides is constantly undergoing phosphodiesteratic cleavage and resynthesis. Thrombin addition led to rapid increase in radioactivity in inositol triphosphate, but not in inositol diphosphate. We conclude that this early consequence of the thrombin-platelet interaction is the result of an increase in the phosphodiesteratic cleavage of phosphatidylinositol bisphosphate.
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PMID:Thrombin-induced phosphodiesteratic cleavage of phosphatidylinositol bisphosphate in human platelets. 629 23

In 12 patients with arterial hypertension (stages I and II according to WHO), adrenergic stimulation was induced by the immersion of a hand in ice water for 2 min. Blood samples were withdrawn before, at the end of, and 15 min after the cold application: the experiment was repeated 2 h after the ingestion of 200 mg acebutolol, a selective betablocking agent. The following assays were performed: serum nonesterified fatty acid (NEFA), plasma beta-thromboglobulin (BTG) and PF4 with specific radioimmunoassays; thromboxane B2 (TXB2) in plasma was also estimated with radioimmunoassay, platelet sensitivity to exogenous prostacyclin; furthermore, the thrombin-induced thromboxane production before and after acebutolol ingestion as well as serum TXB2-levels were measured. The blood pressure and the heart rate were also monitored. After cold stimulation, a significant increase of NEFA, BTG, and plasma TXB2 was observed, which was still discernible 15 min after the application of cold. After acebutolol, the cold treatment led to a lower increase of blood pressure with a reduction of the heart rate, as well as to a diminished release of BTG, PF4 and TXB2 no changes in the reduced platelet sensitivity to prostacyclin were noticed.
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PMID:Platelet activation after adrenergic stimulation in hypertensive patients: effects of acebutolol. 635 66


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