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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.

An evaluation of anti-ulcer effects of mono- and dibasic carbamate local anaesthetics was performed using two experimental models of gastric ulcers, i.e. those induced by stress, or by ligation of the pylorus. These models have been found not to be identical. In the case of stress-induced ulcers, no experimental animal died as compared to the second experimental group with a 30% mortality rate due to the more frequent occurrence of ulcer perforations. Result similarities of both models could only be found with respect to the range of damage of the mucous membrane of the stomach. A premedication with a majority of basic carbamates decreased the incidence and range of ulcer lesion. The anti-ulcer activity of monobasic carbamates was more significant when compared with dibasic compounds.

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.

Diabetes mellitus is a metabolic disorder which has affected several millions of population all over the world. It is characterized by an excess of sugar in the blood and urine, hunger, thirst and gradual loss of weight. Insulin is a hormone which regulates the carbohydrate and triacylglyceride metabolism through its action at several sites and facilitates the entry of glucose accumulation in the blood. Insulin also stimulates the synthesis of glucokinase and moderates the degree of gluconeogenesis. In the diabetic patient, there is an aberration in the functioning of insulin. Prior to the 1950s, control of diabetes was based entirely on insulin therapy. Unfortunately, some patients developed complications and thus need for some other therapy was realized. Presently control of NIDDM relies on compounds from two classes--sulphonylureas and biguanides. Although these drugs are widely accepted as being efficacious in treating some diabetics, they are ineffective in many others. Consequently, testing of many chemicals and plant extracts has continued. The object of the present paper is to bring up-to-date information on the hypoglycemic activity of plants, above all the plants occurring in our country, and those who se hypoglycemic activity has been scientifically documented in a more detailed way. Recent theories on the mechanism of action of these plants are also discussed.

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.

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 review paper is the first collected communication about the biological activity of 3-aryl-2H,4H-benz(e)(1,3)oxazine-2,4-diones and thiosalicylanilides. The substances of the above mentioned structures show a number of biological activities (antibacterial, antituberculous, antimycotic, anthelmintic, molluscocidal, neuroleptic, analgesic and anti-inflammatory) which can be modelled by structural changes. Only very few of them have been hitherto introduced into practice as anthelmintic agents, or agents with a special purpose (destroying the sea lamprey in Canadian lakes). In the group of 3-aryl-2H,3H-benz(e)(1,3)-oxazine-2,4-diones, i.e. substances developed from salicylanilides by the action of alkyl-chloroformiates, antibacterial activity is reported in refs. 3-12, antituberculous activity in refs. 13, 14, antimycotic activity in refs. 5, 6, 9, 12, 15, 16, anthelmintic activity in refs. 6,917-20, molluscocidal activity in refs. 6, 21, analgesic and anti-inflammatory activity in refs. 22-24, herbicidal activity in refs. 25, 26, allergenic activity in ref. 27. In the group of salicylanilides, antibacterial activity is reported in refs. 28-37, antimycotic activity in refs. 28-36, antiprotozoal activity in ref. 35, anthelmintic activity in refs. 28-40, 49, molluscocidal activity in refs. 7, 28-36. The present paper furthermore sums up the papers concerned with the toxicities of the above-mentioned agents. Though the peak of research of the groups of the above-mentioned structure was in the 1960s and 1970s, papers investigating their biological activity can be encountered also at present.

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 oyster fungus (Pleurotus ostreatus (Jacq. ex Fr.) Kumm., Pleurotaceae) is a wood-worming fungus with a significant use in the food industry. Out of the products of the primary and special metabolisms, which were found in fruit bodies in the 1970s, it is possible to mention mainly lipids, sterols, lipophilic vitamins, vitamins of the B group, mono-, oligo- and polysaccharides, amino acids, peptides, some enzymes and derivatives of aliphatic hydrocarbons as fragrant substances. Some of these substances exert antiviral, antineoplastic and hypocholesterolaemic activities. In the case of the hypocholesterolaemic effect, not all substances that take part in it have been isolated and identified yet. The fruit bodies of the oyster fungus became a basis for some dietetic preparations in the Czech Republic and Slovakia, e.g. HLIVETA Eritaden and PLEUROS 600. They are usable for the prevention and adjuvant treatment of hypercholesterolaemia. Besides this, the oyster fungus is a source of other substances that can be used in other fields of prevention or treatment.

The ethanolic extract from the roots Echinacea gloriosa L. (Moench), Echinacea angustifolia DC. and Rudbeckia speciosa Wenderoth shows immunomodulating activity. It was seen on the seventh day after five days of in vivo treatment of mice. The most marked immunostimulatory effect was observed on the lysosomal and peroxidal activity of peritoneal macrophages, and splenic cells after in vivo treatment with the ethanolic extract of the roots of R. speciosa Wenderoth.