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PubMed2002

Light scattering and in vitro biocompatibility studies of poly (vinyl pyrrolidone) derivatives with amino-acid-dependent groups.

Two poly (vinyl pyrrolidone) (PVP) families with amino-acid residues (glycine, beta-alanine, gamma-aminobutiric acid and epsilon-aminocaproic acid) on the base of the co-polymer N-vinyl pyrrolidone and allyl-glycidyl ether (VP-AGE) and on the base of epoxidized PVP (EPVP) were synthesized. Static and dynamic light scattering measurements of these PVP derivatives in water showed that their structure/ behavior were similar to that of PVP. The bioreactivity was also similar to that of PVP. Further investigation of the immunoreactive properties of the derivatives in in vitro proliferation assays with fresh normal human peripheral blood lymphocytes and monocytes led to the determination of a costimulatory profile for each derivative in terms of polyclonal stimulation, specific antigen presentation, and immunoglobulin secretion. This profile allows the selection of an appropriate derivative as a carrier that would suit the immunoreactivity needs of the immobilized ligand.

Antigen Presentation↗
PubMed1994

Thrombolysis in thromboembolic diseases.

Thrombolysis in many manifestations of thromboembolic disease offers a valuable alternative to surgery. However, as thrombolysis is always associated with a bleeding hazard (though low) one should always weigh the risks against the expected benefits when the decision for or against this therapeutic option is made. Furthermore, in selecting the appropriate thrombolytic agent, one should be led by the urgency of reperfusion to maintain organ function. If one decides on an aggressive, high-dose, brief-duration regimen, reperfusion may be achieved more rapidly but may be incomplete in the majority of cases. On the other hand, by selecting an intermediate- or long-duration, low-dose regimen, reperfusion may happen too late to improve the patient's prognosis. Above all, one should keep in mind that the hazard of serious bleeding constantly increases with duration of thrombolysis. No matter which strategy is regarded as the best to resolve a clot in a particular patient with a particular type of thromboembolic disease, thrombolysis should be accompanied by high doses of i.v. heparin. Finally, if bleeding occurs in spite of all precautions taken, the new generation of fibrin-specific thrombolytic agents offers the advantage of short half-lives. In addition--in contrast to streptokinase--the hemostatic defect that they cause may be rapidly reversed by the infusion of antagonist drugs such as aprotinin, tranexamic acid, or epsilon-aminocaproic acid. This adds to the clinical safety profile of these thrombolytic agents.

Contraindications↗
PubMed2005

Analysis of ethyl glucuronide in human serum by capillary electrophoresis with sample self-stacking and indirect detection.

Ethyl glucuronide (EtG), a metabolite of ethanol, is a marker of recent alcohol consumption. In the past few years, its analysis in body fluids has attracted considerable attention because it closes a gap between short time and long time alcohol markers such as ethanol and carbohydrate-deficient transferrin, respectively. The capillary zone electrophoresis (CZE) analysis of EtG in model mixtures and human serum is reported using uncoated and coated fused-silica capillaries together with acidic buffers in the pH range between 3.2 and 4.4 and indirect detection. In these approaches, separation of EtG from endogenous macro- and microcomponents (anionic serum components of high and low concentration, respectively) is based upon transient isotachophoretic stacking referred to as sample self-stacking. The selection of a favorable bufferco-ion and pH is shown to be crucial for optimized sensitivity. Abuffercomposed of 10 mM nicotinic acid and epsilon-aminocaproic acid (pH 4.3) is demonstrated to provide a detection limit for EtG in serum of 0.1 microg/ml, a value that is relevant for clinical and forensic purposes.

Buffers↗
PubMed2005

Disseminated intravascular coagulopathy in aortic aneurysms.

Aneurysm-induced disseminated intravascular coagulopathy (DIC) constitutes a rare presentation form of aortic aneurysms. The majority of DIC cases are asymptomatic and this condition is usually diagnosed during the perioperative workup; yet, in a minority of cases, DIC leads to the diagnosis of the vascular abnormality. The management of aneurysm-induced DIC is based both on the treatment of the underlying disorder and on an active scrutiny of the hemodynamic and blood support requirements. Blood replacement therapy should be individualized, guided by the clinical situation of the patient (especially considering the bleeding risk or the presence of hemorrhages), and accompanied by a close monitoring of the coagulation status. Fresh frozen plasma is usually the preferred initial option to replace coagulation factors, but fibrinogen, cryoprecipitates, and platelet concentrates are adequate options in certain contexts. Heparins, both non-fractionated and low-weight molecular types, are the most widely accepted agents for achieving adequate control of the coagulation activation and consumption. Other antithrombotic drugs are under study, including antithrombin III and activated protein C, although only the latter has demonstrated a benefit in terms of survival in a comparative, randomized context. Antifibrinolytic agents such as gabexate mesilate, tranexamic acid, and epsilon-aminocaproic acid (EACA) have been used with conflicting results. These agents may have a role for patients with catastrophic bleeding resistant to other therapeutical options, but their relevance as a first line of treatment is, at present, undefined. An assessment of the multitude of therapeutic approaches available would seem to indicate that there is a lack of standardization in the management of these patients. Multi-center, randomized clinical trials are needed to elucidate the most adequate therapy in this context.

Journal Article↗
PubMed1999

Determination of fenoprofen in serum by capillary isotachophoresis.

A isotachophoretic method with conductivity detection was developed and validated to directly determine fenoprofen in human serum. The leading electrolyte contained hydrochloric acid (10 mmol/l), 6-aminocaproic acid (pH 4.8) and polyvinylpyrrolidone (0.1%). The terminating electrolyte was 4-morpholineethanesulfonic acid (5 mmol/l). The calibration curve was linear over the concentration range 0.02-0.40 mmol/l. Within-day standard deviation ranged from 0.001 to 0.004 and between-day standard deviation ranged from 0.001 to 0.004. The limit of determination was 0.02 mmol/l. The assay was employed to determine serum concentration of fenoprofen in patients.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1998

Plasma and recombinant thrombin-activable fibrinolysis inhibitor (TAFI) and activated TAFI compared with respect to glycosylation, thrombin/thrombomodulin-dependent activation, thermal stability, and enzymatic properties.

Thrombin-activable fibrinolysis inhibitor (TAFI) is a human plasma zymogen similar to pancreatic pro-carboxypeptidase B. Cleavage of the zymogen by thrombin/thrombomodulin generates the enzyme, activated TAFI (TAFIa), which retards fibrin clot lysis in vitro and likely modulates fibrinolysis in vivo. In the present work we stably expressed recombinant TAFI in baby hamster kidney cells, purified it to homogeneity from conditioned serum-free medium, and compared it to plasma TAFI (pTAFI) with respect to glycosylation and kinetics of activation by thrombin/thrombomodulin. Although rTAFI is glycosylated somewhat differently than pTAFI, cleavage products with thrombin/thrombomodulin are indistinguishable, and parameters of activation kinetics are very similar with kcat = 0.55 s-1, K(m) = 0.54 microM, and Kd = 6.0 nM for rTAFI and kcat = 0.61 s-1, K(m) = 0.55 microM, and Kd = 6.6 nM for pTAFI. The respective TAFIa species also were prepared and compared with respect to thermal stability and enzymatic properties, including inhibition of fibrinolysis. The half-life of both enzymes at 37 degrees C is about 10 min, and the decay of enzymatic activity is associated with a quenching (to approximately 62% of the initial value at 60 min) of the intrinsic fluorescence of the enzyme. Stability was highly temperature-dependent, which, according to transition state theory, indicates both high enthalpy and entropy changes associated with inactivation (delta Ho++ approximately equal to 45 kcal/mol and delta So++ approximately equal to 80 cal/mol/K). Both species of TAFIa are stabilized by the competitive inhibitors 2-guanidinoethylmercaptosuccinic acid and epsilon-aminocaproic acid. rTAFIa and pTAFIa are very similar with respect to kinetics of cleavage of small substrates, susceptibility to inhibitors, and ability to retard both tPA-induced and plasmin-mediated fibrinolysis. These studies provide new insights into the thermal instability of TAFIa, a property which could be a significant regulator of its activity in vivo; in addition, they show that rTAFI and rTAFIa are excellent surrogates for the natural plasma-derived species, a necessary prerequisite for future studies of structure and function by site-specific mutagenesis.

Animals↗
PubMed1964

THE EXCITATION AND DEPRESSION OF MAMMALIAN CORTICAL NEURONES BY AMINO ACIDS.

Amino acids related to L-glutamic and gamma-amino-n-butyric acid have been administered electrophoretically, and by pressure ejection, into the extraneuronal environment of single neurones in the pericruciate cortex of cats anaesthetized with allobarbitone or allobarbitone-urethane. Acidic amino acids related to glutamic acid, particularly N-methyl-D-aspartic acid, excited cortical neurones. Neutral amino acids related to gamma-amino-n-butyric acid, particularly 3-amino-1-propanesulphonic acid, depressed cortical neurones. Some of the depressants blocked the antidromic invasion of Betz cells by pyramidal volleys. There are no essential differences between the sensitivities of cortical and spinal neurones towards locally administered amino acids. A transmitter function of such amino acids within the mammalian central nervous system is considered unlikely.

Acetates↗
PubMed1979

Responses of the guinea-pig isolated olfactory cortex slice to gamma-aminobutyric acid recorded with extracellular electrodes.

1. Potential changes between the pial and cut surfaces of slices of guinea-pig olfactory cortex in vitro produced by gamma-aminobutyric acid (GABA) were recorded with extracellular electrodes. 2. GABA, superfused over the pial surface (0.1 to 10 mM), produced a pial-negative potential deflection, accompanied by inhibition of the postsynaptic response to lateral olfactory tract (LOT) stimulation. 3. This effect was replicated by the following compounds (potency relative to GABA = 1, in brackets): 3-aminopropanesulphonic acid (5.3), epsilon-aminovaleric acid (0.07), beta-alanine (0.07), beta-amino-nibutyric acid 0.05), epsilon-aminocaproic acid, alpha-amino-isobutyric acid, L-leucine (less than 0.02). 4. L-Glutamate (1 to 10 mM) produced a very large surface negative shift, with relatively less synaptic inhibition. Glycine (1 to 10 mM) produced less surface negatively, accompanied by synaptic inhibition. 5. Responses to GABA were antagonized more effectively than those to glycine by bicuculline (3 to 30 micrometer) and picrotoxin (1 to 30 micrometer). Strychnine (1 to 10 micrometer) incompletely inhibited responses to glycine. 6. It is concluded that, while the locus within the slice of these effects is uncertain, the preparation may be useful for testing the interaction of drugs with cerebral GABA receptors.

Action Potentials↗
PubMed1997

Basic fibroblast growth factor-induced angiogenic phenotype in mouse endothelium. A study of aortic and microvascular endothelial cell lines.

The mouse is the most commonly used species for in vivo studies on angiogenesis related to tumor development. Yet, to the best of our knowledge, very few reports on the in vitro interaction of the angiogenic basic fibroblast growth factor (bFGF) with mouse endothelial cells are available. Three mouse endothelial cell lines originated from aorta (MAECs), brain capillaries (MBECs), and heart capillaries (MHECs) were characterized for endothelial phenotypic markers, in vivo tumorigenic activity, and the capacity to respond in vitro to bFGF. These cells express angiotensin-converting enzyme, acetylated LDL receptor, constitutive endothelial nitric oxide synthase, and vascular cell adhesion molecule-1 and bind Griffonia simplicifolia-I lectin. When injected subcutaneously in nude mice, MAECs induced the appearance of slow-growing vascular lesions reminiscent of epithelioid hemangioendothelioma, whereas MBEC xenografts grew rapidly, showing Kaposi's sarcoma-like morphological features. No lesions were induced by injection of MHECs. MAECs, MBECs, and MHECs expressed both low-affinity heparan sulfate bFGF-binding sites and high-affinity tyrosine kinase receptors (FGFRs) on their surfaces. In particular, MAECs expressed FGFR-2/bek mRNA, whereas microvascular MBECs and MHECs expressed FGFR-1/flg mRNA. Accordingly, bFGF induced a mitogenic response and the phosphorylation of extracellular signal-regulated kinase-2 in all the cell lines. In contrast, upregulation of urokinase-type plasminogen activator expression was observed in bFGF-treated microvascular MBECs and MHECs but not in MAECs. Also, bFGF-treated MBECs and MHECs but not MAECs invaded a three-dimensional fibrin gel and formed hollow, capillary-like structures. The relevance of the modifications of the fibrinolytic balance of mouse microvascular endothelium in bFGF-induced angiogenesis was validated in vivo by a gelatin-sponge assay in which the plasmin inhibitors tranexamic acid and epsilon-aminocaproic acid given to mice in the drinking water inhibited neovascularization induced by the growth factor. In conclusion, differences in response to bFGF exist between large-vessel MAECs and microvascular MBECs and MHECs. Both in vitro and in vivo data point to a role of the profibrinolytic phenotype induced by bFGF in microvascular endothelial cells during mouse angiogenesis. Our observations make these endothelial cell lines suitable for further studies on mouse endothelium during angiogenesis and in angioproliferative diseases.

Animals↗
PubMed2004

Characterization of plasminogen as an adhesive ligand for integrins alphaMbeta2 (Mac-1) and alpha5beta1 (VLA-5).

Plasminogen (Pg) has been implicated in many biologic processes involving extracellular proteolysis. We investigated whether Pg, by virtue of its capacity to be deposited within the extracellular matrix, can serve as a ligand for cell surface integrins. We report here that Pg supports cell adhesion by engaging integrins alphaMbeta2 and alpha5beta1. The immobilized Glu-Pg, but not its derivatives with the N-terminal peptide lacking, plasmin and Lys-Pg, supported efficient adhesion that was abolished by anti-alphaMbeta2 and anti-alpha5beta1 integrin-specific monoclonal antibodies (mAbs). In addition, lysine binding sites of Glu-Pg contributed to cell adhesion inasmuch as tranexamic acid and epsilon-aminocaproic acid inhibited cell adhesion. The involvement of alphaMbeta2 and alpha5)beta1 in adhesion to Glu-Pg was demonstrable with blood neutrophils, U937 monocytoid cells, and genetically engineered alphaMbeta2-transfected human embryonic kidney (HEK) 293 cells. In alphaMbeta2, the alphaMI-domain is the binding site for Glu-Pg because the "I-less" form of alphaMbeta2 did not support cell adhesion and the recombinant alphaMI-domain bound Glu-Pg directly. In comparison with cell adhesion, the binding of soluble Glu-Pg to cells and the concomitant generation of plasmin activity was inhibited by anti-alpha5beta1 but not by anti-alphaMbeta2. These findings identify Glu-Pg as an adhesive ligand for integrins alphaMbeta2 and alpha5beta1 and suggest that alpha5beta1 may participate in the binding of soluble Glu-Pg and assist in its activation.

Amino Acid Sequence↗
PubMed2001

Prevention of the adverse effects of aprotinin in autologous fibrin glue.

To avoid the adverse effects of aprotinin (Apr) in autologous fibrin glue, we compared the inhibitory properties of four commercial anti-fibrinolytic agents (tranexamic acid (Tra), epsilon-aminocaproic acid (Ips), gabexate mesilate (Gab) and nafamostat mesilate (Naf)). The optimum conditions for the lysing of fibrin glue were an incubation temperature of 37 degrees C, and incubation medium containing urokinase at 100 U/ml and plasminogen at 100 mU/ml (for the washed glue), or neither (for unwashed glue). Fibrin glues without an anti-fibrinolytic agent were quickly lysed in the incubation medium, while those with an anti-fibrinolytic agent were slowly lysed dose-dependently. Naf was the most potent inhibitor and had high affinity for the glue, but the other agents were poor inhibitors and had low affinity. The inhibition potency (IP) of each agent did not correlate with hydrophobicity, but a good correlation was obtained between the remaining coefficient (RC) and hydrophobicity. Naf did not affect the adhesive strength of the glue. These results indicate that Naf is the most suitable anti-fibrinolytic agent to replace Apr.

Aprotinin↗
PubMed1982

Some properties of porcine carboxypeptidase N.

Some properties of carboxypeptidase N purified from pig serum have been investigated. The amino acid composition resembles that of human carboxypeptidase N, but differs markedly from that of porcine carboxypeptidase B. The enzyme contains a mass fraction of 0.1 carbohydrates. Both ester and peptide substrates are hydrolyzed at the same site. Peptide substrates are hydrolyzed if lysine or arginine is the C-terminal amino acid, and provided that the penultimate amino acid is not proline. Argininic acid and epsilon-aminocaproic acid are good inhibitors of the enzyme.

Amino Acids↗
PubMed1988

Evidence against in vivo presence of 2-(2-furoyl)-4(5)-(2-furanyl)-1H-imidazole, a major fluorescent advanced end product generated by nonenzymatic glycosylation.

The reaction of protein amino groups with glucose leads to the formation of a stable Amadori product via a Schiff base adduct, which is further converted to advanced glycosylation end products (AGE) with color and unique fluorescence characteristics. 2-(2-Furoyl)-4(5)-(2-furanyl)-1H-imidazole (FFI) was recently identified as a major fluorescent compound (Ponger, S., Ulrich, P.C., Bencsath, F.A., and Cerami, A. (1984) Proc. Natl. Acad. Sci. U.S.A. 81, 2684-2688). Its in vivo and in situ presence was further demonstrated by radioimmunoassays (Chang, J.C.F., Ulrich, P.C., Bucala, R., and Cerami, A. (1985) J. Biol. Chem. 260, 7970-7974). In the present study the occurrence of FFI in AGE-proteins was reassessed. The radioimmunoassay using anti-FFI antibody and high performance liquid chromatography failed to detect FFI in AGE samples obtained from bovine serum albumin, poly-L-lysine, oligo-L-lysine, and L-lysine. Even after acid hydrolysis or proteinase K digestion, FFI was undetectable. To our surprise, however, the addition of ammonia to these acid hydrolysate led to the production of FFI, suggesting the importance of acid hydrolysis and subsequent reaction with ammonia for the generation of FFI. This observation was fully supported by model experiments using AGE-samples prepared by incubating glucose with monoaminocarboxylic acids such as beta-alanine, gamma-aminobutyric acid, and epsilon-aminocaproic acid. Thus, a nonfluorescent FFI precursor is produced by acid hydrolysis, and its conversion to fluorescent FFI occurs upon subsequent reaction with ammonia, the evidence against the presence of FFI in AGE-proteins.

Ammonia↗
PubMed1983

Changes of the activity of acid phosphatase and beta-glucuronidase in isolated platelets of whole-body irradiated rats.

In the work presented here we paid our attention to studying changes of the activity of two lysosomal enzymes-acid phosphatase and beta-glucuronidase in platelets after whole-body irradiation and application of certain clinically applied antifibrinolytics (Antilysin Spofa and epsilon-aminocaproic acid) on the activity of these enzymes in isolated platelets. From the results it is obvious that the activity of acid phosphatase and beta-glucuronidase increases in platelets of irradiated rats with a maximum on the 11th day after irradiation. In the same time interval after irradiation the most remarkable thrombocytopenia was observed. The application of Antilysin or EACA to intact, non-irradiated rats affects remarkably neither the activity of the followed enzymes nor the count of platelets. A statistically significant thrombocytopenia, in a comparison with controls was found in whole-body irradiated rats who received EACA or Antilysin. The postirradiation increase of the level of acid phosphatase in platelets exerts a similar character in rats who received EACA or Antilysin as in those who were only irradiated with a difference that the increase of the level of this enzyme was essentially lower in all the time intervals of interest. The beta-glucuronidase level in platelets of rats, who received EACA, was essentially unchanged as compared to controls. The application of Antilysin altered remarkably the level of beta-glucuronidase in platelets of whole-body irradiated rats in a comparison with a level of this enzyme in platelets of rats who received no Antilysin. Most remarkable changes were observed in latter time intervals (11th and 15th day) when the beta-glucuronidase level in platelets of rats after the application of Antilysin was remarkably higher than that in solely irradiated rats.

Acid Phosphatase↗
PubMedDate not supplied

[Protease inhibitors as immunomodulators in experimental acute pancreatitis and staphylococcal infection].

The influence of protease-inhibiting preparations on the development of humoral immune response in diseases involving the development of secondary immunodeficiency (experimentally induced acute pancreatitis and staphylococcal infection) has been studied. Five injections of contrycal and epsilon-aminocaproic acid (epsilon-ACA), starting from day 1 after the induction of acute pancreatitis, normalized the immune response induced by sheep red blood cells 24 hours after operation. In staphylococcal infection protease-inhibiting preparations (contrycal, epsilon-ACA, Amben) produced a protective effect, increasing the survival rate and the mean survival time of the animals infected with staphylococci.

4-Aminobenzoic Acid↗