The effect of the blockers of calcium channels on the development of myocardial ischaemia in rats with an occlusion of the coronary artery was examined. An occlusion of the coronary artery was carried out in rats anaesthetized with pentobarbital by tightening the ends of the ligature freely placed under the left coronary artery - ramus interventricularis seven days prior to ligation. The ischaemia-induced changes in the R-wave and ST-segment were recorded using ECG. The occlusion of the coronary artery produced arrhythmias, a significant elevation of the ST-segment and a slight increase in the heart rate. The blockers of calcium channels with different pharmacological properties - verapamil, nifedipine and diltiazem influenced the ischaemia-induced changes with different intensity. Nifedipine (0.02 mg.kg-1, i.v., 30 min prior to occlusion), verapamil (0.2 mg.kg-1, i.v., 10 mins prior to ischaemia), and diltiazem (0.3 mg.kg-1, i.v., 10 mins prior to ischemia) significantly reduced the increased elevation of the ST-segment. The highest effect on the above-mentioned model was shown by verapamil.
Resistant strains of Escherichia coli were obtained by stepwise cultivation in subinhibitory concentrations of two antimicrobially active amine oxides. Changes in the chemical composition of the outer membrane of the resistant strains were accompanied also by different antigenic reactions. New precipitation lines were revealed by double immunodiffusion and immuno-electrophoretic methods. The results of immunochemical analysis confirm the findings that the resistance to amphiphilic compounds is associated with the outer membrane which limits the access of antimicrobially active molecules to their sites of action in the cytoplasmic membrane.
The paper presents data on the consumption of psycho-active drugs in the urban population, which are expressed by the number of packages and costs. The consumption of the group of agents under study represents 6.2% of total costs of drugs within the framework of out-patient care. The results of a one-year survey have revealed that the curve of the consumption of psycho-active drugs for the whole population after calculation per one person possesses the shape of a 2nd degree parabola. Consumption of psycho-active drugs per one person is significantly higher in women than in man and it consistently grows with the age.
Experiments carried out on male mice (ICR) demonstrated a protective effect of premedication with the preparation Sho-Saiko-To (TJ 9, Tsumura and Comp.) against the hepatotoxic effects of CCl4 and T1-acetate, which were manifested by increased peroxidation of lipids and increased depletion of reduced glutathion in liver homogenates.
Ethanolic extracts of aerial parts of the plants Echinacea angustifolia DC, Echinacea purpurea L. (Moench), Rudbeckia fulgida var. sullivantii, Boyton et Beadle, and Rudbeckia speciosa Wenderoth show immunomodulating activity. The mice were treated in vivo for 5 days and the activity was tested for and observed on day 7. An immunostimulatory effect was observed on the phagocytic, metabolic and bactericidal activities of peritoneal macrophages. The ethanolic extracts of both Echinacea plants also increased the total weight of the spleens as compared to the effect of the Rudbeckia plants and the control group which received saline.
The antipyretic activity of binuclear (diacetoxybenzoato)-copper(II) aquacomplexes [Cu2(2,Y-DAB)4(H2O)2] (Y = 4 and 5) as well as cupric acetylsalicylate [Cu2(AcSal)4] was assayed in a rabbit model of endotoxin-induced fever. The complexes and uncomplexed carboxylic acids (administered i.p. in a dose of 20 mg/kg) exhibited even a subnormothermic course in lowering of febrile animals' body temperature in the order: 2,5-diacetoxybenzoic acid (-0.09 degree C) < 2,4-diacetoxybenzoic acid (-0.35 degree C) < Cu(AcSal)2(-0.39 degree C) approximately equal to acetylsalicylic acid (-0.40 degree C) < Cu(2,4-DAB)2.H2O (-0.61 degree C) < Cu(2.5-DAB)2.H2O (-0.97 degree C). On the other hand, the mean value of untreated fevered animals was +0.67 degree C.
The antimicrobial activities of a group of copper(II) chelates with the composition [Cu(TSB)(L)] or [Cu(TSB)(L')]. (TSB = N-salicylidene-L-alpha-alaninate dianion, L = imidazole and its alkyl derivatives, L' = pyrazole and 3,5-dimethylpyrazole) were studied. Bis-diazole complexes with L' = pyrazole and 3,5-dimethylpyrazole were found to be the most active against S. aureus (MIC = 78 and 20 micrograms.cm-3), less effective against C. albicans (156 micrograms.cm-3), T. terrestre and M. gypseum (100 micrograms.cm-3). The observed biological properties of complexes are discussed in relation to their proposed structures.
The present paper reports the results of a survey of contemporary medical prescriptions of solutions, suspensions and emulsions used in dermatological practice. The obtained results were compared with the district prescription lists from Slovakia. The analysis of contemporary prescription was carried out in 27 districts in the years 1987 and 1989. The results show that 112 drugs are prescribed in the preparation of solutions. Most solutions are composite and 90% of solutions are hydrophilic. An analysis of suspensions revealed that in hydrophilic suspensions the liquid media water-glycerol or spirit-water prevail, and in hydrophobic suspensions nearly always plant oils are used. Emulsions are represented in topical extemporaneous preparations in a smaller amount than solutions and suspensions; it is 0.7% in the set under study.
By pyrrolidinoethylalcohol addition on 2-, 3- and 4-alkoxy-substituted phenylisocyanate in non-aqueous toluene medium a series of 30 compounds of the type Pyrrolidinoethylesters of 2-, 3- and 4-alkoxy substituted phenylcarmabim acids were prepared. Pharmacological evaluation results shown after comparing with cocaine and procaine standards that these compounds have a higher index of effectiveness in both types of local anaesthesia. The maximum effectiveness of surface anaesthesia shows Pyrrolidinoethylester of 2-octyloxy phenylcarbamic acid which is 204-times more effective as cocaine. The maximum effectiveness of infiltration anaesthesis shows Pyrrolidinoethylester of 2-heptyloxy phenylcarbamic acid which is 66-times more effective as procaine. Prepared compounds are more effective in the case of surface anaesthesia as in the case of infiltration anaesthesia and they have comparatively high values of partition coefficients P' and P' cal. Comparison of prepared compounds effectiveness and analogic piperidinoethylesters shows that in more cases they are either equal or nearer effective. The values of their P' and P' cal correlate with these results.
The activity of peptidases (trypsin from bovine pancreas and trypsin-like enzymes from the liver rat homogenate) was influenced by five preparation of Kampo medicine, TJ-9 (Sho-Saiko-To), TJ-15 (Oren-Gedoku-To), TJ-23 (Toki-Shakuyaku-San), TJ-96 (Saiboku-To), and TJ-114 (Sairei-To) and studied in relation to their effect on the uptake of free oxygen radicals demonstrated earlier. On the basis of increased activity of trypsin and trypsin-like enzymes and the previously found capability of uptaking free oxygen radicals, the mechanism of action of the Kampo preparations may be assumed to be connected not only with a direct support of enzymes of digestion and increased activity of peptidases, capable of eliminating oxidatively damaged proteins, but with an antioxidative effect as well, which prevents increased cumulation of oxidatively damaged macromolecules and the action of superoxide radicals developed earlier by the well-known and trypsin-stimulated conversion of xanthinedehydrogenase to xanthinoxidase.
Using screening methods, the anti-inflammatory and antipyretic activities of mononuclear otahedral complexes [composition:Cu(2,YDHB)2.H2O;dihydroxybenzoate ion - DHB; Y(n)-4(8).5(4) and 6(8)] and the corresponding carboxylic acids were studied. On paw dextran edema (rats, an effective dose of 10 mg/kg), a higher efficacy of the complexes was found as compared with the acids. All compounds significantly reduced the endotoxin pyretic reaction (rabbits, in a single dose of 20 mg/kg; in the case of the first two complexes half-dose was administered). Marked toxic effects were determined for Cu(II) salts when they were administered i.p. The observed biological activities of complexes are discussed in relation to their proposed structures.
TJ-15 (Oren-Gedoku-To) inhibited enzymatically (NADPH or CumOOH) and non-enzymatically (Fe-askorbate) induced lipid peroxidation in the rat liver microsomes as assessed by the TBA-reactive product accumulation. TJ-23 (Toki-Shakuyaku-San) had little effect on either system. The protective effect of TJ-15 against lipid peroxidation could not be fully accounted for by its action on microsomal electron transfer, as evaluated by studying the kinetics of reduction of cytochrome C. In a free solution TJ-15 and TJ-23 effectively scavenged OH., radicals, as indicated by the inhibition of ethylene production from KMBA, and O2-. anion radicals, as assessed by the inhibitory effect on the rate of NBT reduction. The present results suggest that TJ-15, yet not TJ-23, is capable to reach hydrophobic intra-membrane sites at concentrations at which it is an effective antioxidant. Thus TJ-15 may be a potentially useful protective agent against free radical-mediated damage.
The present paper analyzes the formal equivalence of expressing the consumption of medicines in financial and physical units. The study was carried out on a representative sample of population; for the sake of the need of analytical expression also the factor of the age in the consumption of drugs measured per 1 inhabitant was taken into consideration. A highly close relationship between the two specific variables is observed. On this basis the postulate of the validity of equivalence is formulated. The paper points to the stability of this formal equivalence also in the conditions of the action of the seasonal component and the pragmatic significance of the obtained results for pharmaco-epidemiological studies is stressed.
The present paper aimed to examine a possible influence of the antioxidant butylhydroxyanisole (BHA) on the extent of atherosclerotic changes in coronary arterioles, in arcus aortae, and on the influencing of the extent of myocardial necroses. The model of atherosclerosis was worked out by administering 1% cholesterol diet to Japanese quails for the period of 40 days. The above-mentioned changes were examined on histological preparations and they were evaluated morphometrically. Quantification and morphometry of atherosclerotic changes in the individual experimental groups are shown in Table 1 and statistical evaluation of findings using the t-test in Tables 2, 3 and 4. The protective effect of butylhydroxyanisole was demonstrated to be statistically significant in the examination of the extent of atheromatous changes in arterioles. In arcus aortae, the findings were neither extensive, nor statistically significant. The findings concerning the extent of necroses in the myocardium provide documentary evidence for subendothelial micronecroses in the group with BHA in contrast to blended necroses in the group with Epavit + cholesterol. The model of cholesterol diet used in Japanese quails proved to be suitable to examine the pathogenesis of atherosclerosis and its possible influencing by pharmaceuticals. The dose of butylhydroxyanisole (BHA), 20 mg.kg-1, was selected in the optimal manner with regard to possible inhibition of atherosclerotic changes.
In a systematic study of the relationship between the chemical structure and beta-adrenolytic activity, eleven derivatives of the 4-alkoxysubstituted phenylcarbamic acids were prepared. 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. Negative chronotropic and antidysrhythmic activity were also evaluated. All of the compounds studied were local anesthetically active and their indexes of efficiency were 3-50 fold higher in comparison with standards cocaine and procaine. The acute toxicity of the compounds was within the acceptable limits.
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The present paper describes a method of dithiadenoxide determination in blood plasma. Dithiadenoxide was reduced to dithiaden with zinc dust in acidified plasma. The solution was alkalified and dithiaden extracted into n-hexane and isolated on a thin layer of silica gel using the system chloroform--n-heptane-methanol (60:22:18). After spraying the plate with a solution of m-nitrophenyldiazoniumfluoroborate in acid medium, dithiaden stains were evaluated densitometrically in the absorption maximum of the reaction product at 565 nm (RF = 0.37). Detection limit of dithiadenoxide in the proposed method is 0.004 microgram in an applied amount.
Salvia officinalis L. is an essential oil containing plant, which does not wildly grow in the territories of the Czech and Slovak Republics but it can be successfully cultivated. It is a perennial half-shrub, from which non-flowering herbaceous sprouts or leaves are collected for pharmaceutical purposes. After drying at a temperature not exceeding 35 degrees C they are the plant drugs Herba salviae or Folium salviae. In PhBs, Herba salviae is official. The drug contains mainly ethereal oil (1-2%), diterpenes, triterpenes and tannin. The pharmacopoeial criterion of quality is the content of essential oil, which is produced in an increased amount in the plant in warm summer months. Herba salviae and the extracts prepared from it are used as an antiseptic agent, an antiphlogistic agent, in the inflammations of the oral cavity and gingivitis and also as a stomachic and an antihydrotic agent. Its utilization in cosmetics and food industry is also of importance.
The term poisoning (intoxication) means a health damage due to the effects of a chemical substance which was absorbed into the organism and which produced biochemical changes or even death of the organism. Many metals at higher concentrations induce an undesirable intervention into the enzymic systems though in trace amounts they catalyze many enzymic reactions. Chemicalization, which affects not only industrial and agricultural production but the household, personal hygiene and cosmetics as well, brings new chemical compounds which can increase risks of intoxication on unsuitable use. The living and working environment increases the danger of intoxication with metals or their compounds. The present paper pays attention to complexion-able compounds which are of fundamental importance in the treatment of intoxications with heavy metals.