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P Svec

Publications and source records attributed to P Svec.

At least 37 records · Page 2Linked to original sources
PubMed2000

[Effects of a (fluorophenyl) piperazine derivative (substance IIIv) on cardiovascular function].

The present paper links up with the study of principal pharmacological effects of newly synthesized aryloxyaminopropanols substituted with 1,4-piperazine derivatives in the hydrophilic moiety of the molecule. The substance with the working name IIIv showing the highest beta-adrenolytical and vasodilating effect underwent further pharmacological evaluations with the aim of contributing to the elucidation of the mechanism of its action. After 7-day administration of the substance in two doses (5 and 50 mg.kg-1), the changes in the reactibility of arterial preparations were investigated on three models of the contraction of the isolated rat aorta (KCl, noradrenaline, and PGF2 alpha) from both qualitative and quantitative views. The results were also supplemented with organometric studies of the effect of the substance in rats.

Adrenergic beta-Antagonists↗
PubMed2000

[Anti-inflammatory activity of copper and zinc p-cresol dihydrate].

Using rat paw dextran-induced and carrageenan-induced edemas, the antiedematous activities of dihydrate of diaquatetrakis(p-cresotato)dicopper(II) complex (CupC) and diaquabis(p-cresotato)zinc(II) complex (ZnpC) were assayed plethysmometrically. Dihydrate of diaquabis(salicylato)copper(II) complex (CuS) and diaquabis(salicylato)zinc(II) complex (ZnS) were used as standards of comparison. All compounds were applied i.p. in a single dose of 50 mumol/kg body weight (calculated for the RCOO-fragment) 30 min before injecting the irritant. The antidextran/anticarrageenan activities of the species (expressed as a mean edema reduction) were found: CupC 46/74%--ZnpC 50/26%--CuS 71/52%--ZnS 63/10%. The relationships between the coordination-chemical properties and the biological effects of the corresponding complexes are discussed.

Animals↗
PubMed1999

Occurrence of Enterococcus spp. in waters.

We studied 630 bacterial strains isolated from surface waters and determined as enterococci on the basis of their growth on Slanetz-Bartley agar in typical colonies. The strains were tested and characterized by several key conventional tests for basic differentiation of enterococci and by commercial test kits. We identified 135 strains of E. foecium (21%), 115 E. faecalis (18%), 30 E. mundtii (5%), 27 E. hirae (4%), 22 E. casseliflavus (3%), 21 E. gallinarum (3%), 17 E. durans-E. hirae complex (3%), 5 E. durans (1%), and 1 strain of E. avium. 150 strains were classified only as Enterococcus sp. (25%) and 107 strains (17%) isolated from Slanetz-Bartley agar were not enterococci. We found that the non-enterococcal group consisted of other Gram-positive cocci and Gram-positive and Gram-negative rods. Based on the identification we tried to find a relation between taxonomic position of isolated strains and their colony morphology on Slanetz-Bartley agar. Our of the total of 523 identified enterococci, 345 strains (66%) formed purple colonies, 136 red colonies (26%), 37 pink colonies (7%) and 5 cream colored colonies (1%). There was no correlation among the color, size or colony morphology and the taxonomic characterization of enterococcal strains.

Bacteriological Techniques↗
PubMed1999

[Preparation and antiinflammatory activity of selected aqua-(aryloxyacetate) zinc complexes].

Mononuclear aqua(aryloxyacetato)zinc(II) complexes of the composition [Zn(H2O)2(ROCH2COO)2] (R = phenyl, o-, m-, p-tolyl) were prepared as potential anti-inflammatory agents. The results of elemental analysis and parameters of IR spectra allow to classify the above-mentioned compounds to the group of carboxylatozinc(II) complexes with a distorted octahedral structure. They were assayed in rat paw carrageenan-induced edema and antiedematous effects were compared to those of free acids. Salicylic acid and its zinc(II) and copper(II) salts were used as the standards of comparison. All compounds were administered i.p. in a single dose of 50 mumol/kg body weight (calculated for the carboxylate fragment). In general, the zinc(II) complexes tested were clearly more effective (expressed as a mean edema reduction of 58-70-68-59%), including zinc(II) salicylate dihydrate (64%), than the uncomplexed acids (37-26-50-48%). Copper(II) salicylate tetrahydrate (60%) and salicylic acid (57%) exhibited comparable effects under the same conditions. The observed activities of the complexes are discussed in relation to their structures as well as to the coordination-chemical properties of the acidoligands under study.

Animals↗
PubMed1998

[The present status and prospects of therapeutic use of beta-blockers in diseases of the cardiovascular system].

Beta-blockers are being revived as effective, safe, reasonably priced and well-tolerated drugs. Differences in the pharmacodynamic and pharmacokinetic properties of beta-blockers now make it possible to select for the therapy of the individual diseases from a wide range of available beta-blockers the most effective drug with the minimal undesirable effects. It is made possible by the progress in the development of this ATS group and particularly by the third generation of these compounds. A proof of the prospects of these drugs is provided by their extended indications as the first-choice drugs (myocardial infarction) as well as the generally extended possibilities of their therapeutic use (therapy of heart failure).

Adrenergic beta-Antagonists↗
PubMed1998

[Antiedematous activity of certain arylcarboxylate copper aquacomplexes].

Using rat paw carrageenan edema, the anti-inflammatory activity of nine selected arylcarboxylatocopper(II) aquacomplexes of the general composition Cu(RCOO)2.nH2O, where R represents 2-hydroxy-Y-methylphenyl, Y = 3 (n = 1.5), 4 (4) or 5 (2); 2-hydroxy-3,6-dimethylphenyl (n = 4); 2,5-diacetoxyphenyl (1); 2-methoxy-(1) and 4-methoxyphenyl (3); 2-furyl (3) and 2-thienyl (1), was assayed and compared to that of the free acids. Copper(II) salicylate tetrahydrate and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 mumol/kg body weight, calculated for the RCOO-fragment. m-Cresotato- (mean edema reduction 70%) and p-cresotatocopper(II) (80%) aquacomplexes were clearly more effective than copper(II) salicylate tetrahydrate (55%). The nonsubstituted hydroxyl of the salicylate skeleton of acidoligands is required for the activity of the complexes and of free acids tested. Isomeric cresotic acids (82-47-62%) and 2-furoic acid (48%) exhibited a higher effect than salicylic acid (42%). The relationship between the coordination-chemical properties and the biological effects of the complexes studied is discussed.

Animals↗
PubMed1998

[Antiedema activity of selected compounds with a gallate skeleton].

Using rat paw dextran-induced and carrageenan-induced edemas, the anti-inflammatory activity of gallic acid (I), triacetylgallic acid (II) and monohydrate copper(II) triacetylgallate (III) was assayed. All compounds tested were applied i.p. in a single dose of 50 mumol/kg body weight, calculated for the RCOO-fragment. The average antiedematous activities in dextran/carrageenan edemas were decreasing in the following order: III (55.9/41.8%) > I (38.6/31.1%) > II (-3.4/13.3%). The relationship between the biological effects found and gallic acid as well as its structural derivatives is discussed.

Animals↗
PubMed1998

[Anti-inflammatory activity of (cresoxyacetate)copper complexes].

In groups of mononuclear aqua(cresoxyacetato)copper(II) complexes of the composition [Cu(ROCH2COO)2(H2O)n] (R= 2- and 3-methylphenyl, n = 2; 4-methylphenyl, n = 3) and binu- clear phenazone(o-, m-, p-cresoxyacetato)copper(II) complexes of the composition [Cu2(ROCH2COO)4(phz)2] the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. The effects of the complexes were compared with each other and with those of the free acids. Salicylic acid and its cupric salt (tetrahydrate) were used as standards of comparison. All copounds were applied i.p. in a single dose of 50 mumol/kg body weight (calculated for the RCOO-fragment). In general, all Cu(II) complexes tested were clearly more effective (71-88%) than the corresponding free isomeric cresoxyacetic acids (47, 37, 45%), with the exception of diaquabis (o-cresoxyacetato)copper(II) complex (43%). Copper(II) salicylate tetrahydrate (57%) and salicylic acid (41%) were less active, too. The observed activities of complexes are discussed in relation to their structures.

Animals↗
PubMed1997

[Anti-inflammatory activity of aqua-bis(2,Y-diacetoxybenzoate)-copper complexes (Y=4, 5 or 6)].

In a group of binuclear copper (II) complexes of the composition [Cu2(RCOO)4(H2O)2] (R = 2,4-diacetoxyphenyl (I), 2,5-diacetoxyphenyl (II) and 2,6-diacetoxyphenyl (III)), the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. Copper (II) salicylate tetrahydrate (IV) and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 mumol/kg body weight, calculated for the R-COO-fragment. The Cu(II) complexes tested were clearly more effective than the corresponding free diacetoxybenzoic acids, with an exception for the 2,5-diacetoxy derivative. The average anti-inflammatory activities of copper (II) complexes were decreasing in the following order: III (71.0%) = (70.6%) > IV (57.4%) > II (18.0%). Of the acids, only 2,6-diacetoxybenzoic acid (45.2%) was effective at the level of salicylic acid (44.9%). The relationship between the coordination-chemical properties and the biological effects of the complexes tested is discussed.

Animals↗
PubMed1997

[Pharmaco-toxicologic evaluation of newly synthesized analogs of propafenone].

The basic pharmacological evaluation of five analogues of propafenone was the aim of the present paper. Antiarrhythmic activity of the compounds at 10(-5) mol.kg-1 was established in guinea-pigs using experimental arrhythmias induced by ouabain and aconitine. The beta-adrenolytic efficiency of the compounds was studied in the isolated spontaneously beating guinea-pig atria and expressed as pA2 values against isoprenaline tachycardia. All of the compounds studied were local-anaesthetically active and their indexes of efficiency were 1-5 fold higher in comparison with the standards cocaine and procaine. The acute toxicity of the compounds was within acceptable limits.

Adrenergic beta-Agonists↗
PubMed1996

Synthesis and local anesthetic activity--lipophilicity relationships for a homological series of phenylcarbamic acid esters. Note II.

A homological series of new esters of 2-alkoxyphenylcarbamic acid and one ester of 2,6-dimethylphenylcarbamic acid were synthesized and assayed for surface local anesthetic activity. All compounds were isolated as hydrochlorides and their structure proved by IR and for one homologue also by 1H and 13C NMR spectroscopy. A parabolic relationship was found between log activity and molecular lipophilicity (as measured by RM) and the number of carbons in the alkoxy group, thus confirming the results obtained in previous works.

Anesthetics, Local↗
PubMed1996

[The effect of piperazine analogs of aryloxyaminopropanol (IIIq and IIIb) on the occurrence of reperfusion dysrhythmias in an in vivo experiment on rats].

The present experimental study reports the beneficial effects of newly synthetized substances IIIq and IIIb in vivo. These aryloxyaminopropanol drugs have been shown to antagonize the contraction caused by calcium comparable to verapamil and flunarizine in the model of the isolated guinea pig terminal ileum. Effects of substances on both the incidence of arrhythmias during ischemia and the reperfusion period and mortality were investigated in the rat model ischemia-reperfusion injury. We can conclude that compound IIIq in a dose of 10(-6) mol/kg is effective in reducing the incidence of reperfusion-induced arrhythmias. Substance IIIb (10(-6) mol/kg) administered before ischemia was not able to suppress arrhythmias in the rat model of myocardial infarction and reperfusion.

Animals↗
PubMed1996

Lipid peroxidation during acute stress.

Lipid peroxidation (LPO) is one of the main events induced by oxidative stress. The aim of our study was to investigate the influence of 30 min cold-immobilization (model of acute stress used in this experiment) on LPO in the brain, heart, liver and stomach homogenates of the rats. LPO was determined by measuring of the contents of thiobarbituric acid reactive substances (TBARS), conjugated dienes (CD) and sulfhydryl groups (SH). Experimental stress induced enhancement of TBARS formation in the liver and increased level of the CD in the heart, stomach and liver, while in the brain both parameters were found to be decreased. The levels of TBARS were not changed in the heart and in the stomach, too. The concentrations of SH-groups were decreased in the heart, brain and stomach, while in the liver the parameter was found to be not changed. The results of this study showed the increase of LPO in the heart, stomach and liver under stress conditions. It could be supposed that LPO may be involved in mechanisms of stress injury in different tissues.

Alkenes↗
PubMed1996

[Use of the Streptotest kit for identification of enterococci isolated from human clinical material].

Enterococci are part of the common microflora of man and are isolated in large numbers also from the environment. Recently their presence in clinical material is increasing and they have become an important causal agent of nosocomial infections. From human clinical material (urine, vaginal smears, wounds) a total of 164 strains of enterococci was isolated. Identification of these isolates by means of the commercial STREPTOtest kit was not very successful (71.3%). The use of several supplementary tests and evaluation by the TNW programme improved successful identification (98.8%). The dominating species in clinical material was E. faecalis (94.5%), the second most frequent isolated species was E. faecium (3%). To achieve better identification of enterococci the authors recommend to supplement the kit by further tests (acidification of arabinose, ribose and pyruvate assimilation).

Bacteriological Techniques↗
PubMed1995

Localization, interaction, and RNA binding properties of the V(D)J recombination-activating proteins RAG1 and RAG2.

The RAG1 and RAG2 gene products are indispensable for activating somatic rearrangement of antigen receptor gene segments. The two proteins form a stable complex in primary thymocytes as well as when expressed in adherent cells. In both cell types, most cells localize RAG proteins at the periphery of the nucleus. However, when overexpressed in fibroblast cells, RAG1 is found largely in the nucleolus. Nucleolar localization of RAG1 is mediated by several domains containing stretches of basic amino acids, indicating that RAG1 has affinity for RNA or ssDNA. The RAG1 interacting proteins SRP1 and Rch1 directly bind to the nuclear localization signals of RAG1, which mediate the nuclear and nucleolar translocation of the protein. RAG1 appears to have a binary structure, each half containing multiple regions that can act as NLSs, binding sites for the SRP1/Rch1 family, and RNA binding domains.

3T3 Cells↗