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:3.4.21.4 (trypsin)
42,187 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We have analyzed the effects of aprotinin and Na2CaEDTA on phospholipase A2 activity and on the outcome of experimental pancreatitis in pigs. Hemorrhagic pancreatitis was induced in 29 piglets by infusing Na-taurocholate and trypsin into the pancreatic duct with simultaneous intravenous injection of secretin. Twelve animals serving as controls had no specific treatment. Nine animals were treated with aprotinin and eight pigs with Na2CaEDTA. Ten of the control animals died within 24 h of the induction of pancreatitis, and two of them lived for a week. In the aprotinin group three piglets died within 24 h and two died during the next day; four animals lived for a week. In the Na2CaEDTA group five animals died within 24 h and one the next day; two animals lived for a week. In all the animals serum phospholipase A2 activity increased significantly (p less than 0.01), there being no differences between the groups. In those animals that lived for a week the phospholipase A2 activities decreased on the 2nd day. This decrease was seen in both treated groups. Aprotinin prolonged the survival time of the animals. This prolongation was statistically significant (p less than 0.05, chi-square test, logrank test). Na2CaEDTA did not improve the prognosis of the animals. Neither of the drugs given influenced the serum phospholipase A2 activities during the first hours of the disease.
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PMID:Aprotinin and Na2CaEDTA in experimental hemorrhagic pancreatitis in pigs. 243 80

Acute pancreatitis (AP) is believed to result from intraparenchymal activation of trypsin and other digestive enzymes within the pancreas followed by autodigestion of the gland. Gabexate mesilate (FOY), a synthetic guanidino acid ester exhibiting potent and versatile inhibitory actions on a number of proteinases (e.g., trypsin, kallikrein, C1-r, C1 esterase, plasmin, thrombin, phospholipase A2), was examined for its ability to protect the rat pancreas against development of AP induced by pharmacological doses of ceruletide (CRT). Rats were i.v. infused for 6 h with either CRT (5 micrograms/kg/h) or CRT + FOY (50 mg/kg/h). In FOY-treated rats the serum amylase and trypsinogen concentrations were reduced by 60 and 80%, respectively, compared to rats infused with CRT alone. Histologically, the extent of acinar cell vacuolization in the pancreas was significantly reduced and interstitial edema, although not assessed by quantitative morphometric techniques, appeared to be qualitatively lessened in the FOY-treated rats. The ability of FOY to inhibit significantly AP produced by supramaximal doses of CRT, coupled with its inhibitory properties on components of the coagulation and complement cascades, stress the importance of continued research on this compound as a potential therapeutic agent for treatment of AP and its systemic sequelae.
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PMID:Gabexate mesilate (FOY) protects against ceruletide-induced acute pancreatitis in the rat. 244 41

We report the development of a simple and reliable method for the study of demyelination in vitro based on the measurement of 2':3'-cyclic nucleotide 3'-phosphodiesterase in isolated myelin. Using only small quantities of myelin (equivalent to 100 micrograms of myelin protein) the system was tested under conditions that are believed to approximate those found at the site of an inflammatory demyelinating lesion. Treatment with a combination of trypsin, phospholipase A2, and lysophosphatidylcholine was used to evaluate the method. This microsystem has the potential not only for testing the myelinotoxicity of soluble factors but also for investigating the involvement of inflammatory cells in the demyelinating process. Myelin degradation by elicited peritoneal macrophages could be demonstrated at relatively high densities of these cells. Nylon wool purified lymph node T cells from myelin basic protein-primed SJL/J mice, after selective expansion with antigen and interleukin 2, failed to induce any significant myelin breakdown unless a limited number of syngeneic activated macrophages were also present. T cells from mice that had been inoculated with keyhole limpet haemocyanin failed to show any effect. The advantages of this technique over other in vitro systems are that it enables the study of demyelination using syngeneic sources of myelin and defined cell populations.
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PMID:An in vitro micromethod for the quantitative assessment of central demyelination. 245 36

This study describes the effect on the function and structure of the saline-perfused cat pancreas of factors implicated in the pathogenesis of pancreatitis (bile acid, ethanol, pancreatic enzymes) after their addition to the perfusion fluid or their instillation into the pancreatic duct. Instillation of trypsin or chenodeoxycholic acid, but not ethanol, into the pancreatic duct resulted in a profound suppression of secretory function. The leakage of perfusion fluid and amylase from the gland was also abruptly increased. Intraarterial perfusion of trypsin also inhibited secretin-induced flow and cholecystokinin evoked enzyme secretion. Intraarterial bile acid inhibited fluid flow but augmented enzyme secretion in a concentration-dependent manner. In addition, massive or focal parenchymal necrosis was caused by sustained intraarterial perfusion of bile acid or trypsin, respectively. Elastase and phospholipase A had little influence on pancreatic function or structure when added to the perfusion fluid. These findings show that pancreatic structure and function can be disturbed by potentially toxic factors administered not only via the ductal system but also via the vascular route, and consequently suggest that an "internal reflux" mechanism could be involved in the pathogenesis of pancreatitis in addition to a "ductal reflux" mechanism.
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PMID:Analysis in the isolated perfused cat pancreas of factors implicated in the pathogenesis of pancreatitis. 245 94

In a prospective clinical trial 85 patients with acute pancreatitis were analysed for serum total amylase, pancreatic amylase, pancreatic lipase, trypsin, elastase 1, and immunoreactive phospholipase A2 (IR-PLA2). The diagnostic sensitivity of serum IR-PLA2 was comparable to that of serum total amylase, pancreatic amylase, and trypsin. The specificity of IR-PLA2 is superior to that of serum total amylase determination due to the fact that the IR-PLA2 determination is based on an antibody against human pancreatic PLA2.
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PMID:Diagnostic value of immunoreactive phospholipase A2 in acute pancreatitis. 246 45

The effects of gabexate mesilate (GM) on hemodynamics and phospholipase A2 activities (PLA2) during acute hemorrhagic pancreatitis (AHP) were studied in 17 piglets which were randomly divided into three groups: The control group (CG) received only the fluid replacement, whereas the pretreatment group (PG) was given an infusion of GM (20 mg/kg/5h), which was started 30 min before and in the treatment group (TG) 30 min after the induction of AHP. AHP was induced by infusing a mixture of trypsin and sodiumtaurocholate (1 ml/kg) into the pancreatic duct, and the animals were followed up for 5h. Two animals of the CG died, but no mortality was observed in the other groups. Histologically, acute hemorrhagic pancreatitis was detected in all animals, but no significant differences were observed between the groups. PLA2 activity in the serum increased rapidly after the induction of AHP in the CG, and it was significantly (P less than 0.05) higher 5h after the induction in the CG than in TG or PG. No significant differences developed between the groups in cardiac indices or hemodynamic pressure parameters during the 5h of surveillance, but the volume of secreted exudate into the peritoneal cavity was significantly (P less than 0.05) smaller in the PG than in the CG. In conclusion, GM treatment and pretreatment reduced mortality and the amount of the secreted ascitic fluid during AHP. Moreover, the activity of circulating PLA2 was inhibited in the groups receiving GM.
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PMID:The effect of gabexate mesilate on the outcome of acute hemorrhagic pancreatitis in pigs. 249 46

The present study investigates the mechanism of endothelium-dependent relaxation of vascular smooth muscle. Melittin, a polypeptide found in honeybee venom and a known activator of phospholipase A2, induced transient, endothelium-dependent relaxations of rat thoracic aortae contracted with norepinephrine. Higher concentrations of melittin induced relaxations followed by contractions. Prior incubation of melittin with trypsin abolished the changes in relaxation and contraction due to melittin. Melittin (10 micrograms/ml)-induced relaxations were associated with transiently elevated levels of cyclic GMP with a peak increase of 30-fold, which occurred 30 seconds after melittin exposure. Melittin (10 micrograms/ml) elevated cyclic AMP levels less than twofold and this effect was variable. A lower concentration of melittin (1 microgram/ml) elevated cyclic GMP levels approximately twofold, while exposure to 1 microgram/ml melittin in the presence of the cyclic GMP phosphodiesterase inhibitor, M&B 22948 (1 mM), increased cyclic GMP levels fivefold. Removal of the endothelium prevented the increased levels of cyclic GMP and cyclic AMP due to melittin. Exposure to the guanylate cyclase inhibitor, methylene blue, prevented the increased levels of cyclic GMP. Methylene blue, nordihydroguaiaretic acid, and the phospholipase A2 inhibitor, parabromophenacyl bromide, inhibited melittin-induced relaxations, while the cyclo-oxygenase inhibitor, indomethacin, was without effect. Arachidonic acid increased cyclic AMP levels but had no effect on cyclic GMP levels in the presence or absence of indomethacin. Relaxations to melittin, and to the endothelium-dependent vasodilators acetylcholine, trypsin, histamine, and the Ca2+ ionophore A23187, and/or the associated increased cyclic GMP levels, were reduced following exposure to melittin. Prior exposure to polyarginine (10 micrograms/ml), which induced endothelium-dependent relaxations that were prevented by methylene blue, also inhibited relaxations to the endothelium-dependent vasodilators. In contrast, relaxations to sodium nitroprusside were potentiated in tissues previously exposed to melittin. Removal of the endothelium by rubbing the intimal surface also potentiated relaxations to sodium nitroprusside. Scanning electron micrographs of the intimal surface demonstrated that melittin and polyarginine greatly damaged the endothelial cells. The present results suggest that polycation containing peptides induce endothelium-dependent relaxation through elevation of cyclic GMP levels within the smooth muscle.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Effects of melittin on endothelium-dependent relaxation and cyclic GMP levels in rat aorta. 253 55

Plasma exchange was performed in dogs with acute experimental pancreatitis to examine clearance of pancreatic enzymes. Plasma exchange of about 1.6 liters reduced levels of serum amylase, lipase, and phospholipase A2 in a graded fashion down to about 50%. Plasma exchange of 4 liters in a patient with severe pancreatitis produced similar clearance curves of amylase, lipase, trypsin and elastase levels.
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PMID:Effect of plasma exchange on acute pancreatitis. 258 Mar 63

Bacillus thuringiensis serovar, thuringiensis (HD-2) demonstrated antibacterial activity against 48 of 56 strains of B. thuringiensis and against some other Gram-positive species but not against Gram-negative species. The antibacterial activity was not inducible by mitomycin C or by ultraviolet irradiation, and additional activity was not liberated from cells by sonication. Upon dilution of the antibacterial substance, zones of inhibition diminished without the appearance of plaques. Gel filtration chromatography indicated an Mr greater than 950,000 for the bacteriocin (thuricin) in its native form. The native thuricin was sedimented by ultracentrifugation, but electron microscopy of the pellet failed to reveal phage particles or phage components. Nondenaturing polyacrylamide gel electrophoresis (PAGE) of thuricin demonstrated the association of bacteriocin activity with a protein band which migrated only slightly into a 5% gel. Sodium dodecyl sulfate (SDS)-PAGE of partially purified thuricin revealed five major bands. Thuricin activity was substantially reduced by treatment with chymotrypsin, pronase, subtilisin, trypsin, and heat at 96 degrees C but not by treatment with lysozyme, phospholipase C, papain, peptidase, or organic solvents. It exhibited a bactericidal and bacteriolytic effect on a sensitive strain, B. thuringiensis serovar, canadensis (MF4). Partially purified preparations of thuricin had phospholipase A activity which was adsorbed by sensitive cells but not by cells which were insensitive to thuricin. Antibacterial activity was blocked by preincubation of thuricin with phospholipid. Loss of a 150-mDa plasmid was correlated with loss of thuricin production.
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PMID:Thuricin: the bacteriocin produced by Bacillus thuringiensis. 272 45

A prostaglandin oligomeric derivative was synthesized by alkaline treatment of prostaglandin E1. This compound protected the perfused rat heart from global ischemia. This compound was found to inhibit several lipolytic and proteolytic enzymes in vitro. When phospholipase A2 from Naja naja venom was used as an enzyme and phosphatidylcholine was used as a substrate, 50 per cent inhibition was achieved at 50 microM of the prostaglandin derivative. When trypsin and casein were used as enzyme and substrate, 50 per cent inhibition was obtained at 80 microM. A possible mechanism of beneficial effect of this compound in protecting membranes during ischemia is discussed.
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PMID:A prostaglandin oligomeric derivative inhibits activities of phospholipase and protease: a possible mechanism of membrane protection during ischemia. 275 36


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