The influence of active components of Eleutherococcus senticosus on cellular defence and physical fitness in man.

The influence of active components of Eleutherococcus senticosus, contained in Taiga Wurzel preparation, were studied on cellular defence and physical fitness in man. 50 healthy volunteers of both sexes were selected, and basic clinical examination and laboratory tests were performed in all subjects. All were randomly subdivided into two study groups: group A with 35 subjects receiving Taiga Wurzel and group B with 15 subjects receiving Echinacea. 20 healthy males were randomly selected from both groups and underwent an ergospirometric study. The preparations were administered for 30 days as follows: Taiga Wurzel 25 drops three times daily, Echinacea 40 drops three times daily. After 1 month blood was drawn for control tests. Changes in the following blood parameters were observed in comparison to initial values in group A: total and LDL cholesterol, triglycerides and glucose. No alterations were seen in group B. The ergospirometric test revealed a higher oxygen plateau in group A (Taiga Wurzel). On the basis of the present study the following conclusions were drawn: active components in Eleutherococcus senticosus contained in Taiga Wurzel preparation affect cellular defence and physical fitness, as well as lipid metabolism.

The influence of exogenous antioxidants and physical exercise on some parameters associated with production and removal of free radicals.

Metabolic processes generate chemically active forms of oxygen, among which a prominent role is played by the superoxide ion. Cells are equipped with defence systems against the effects of superoxide radicals, superoxide dismutase is the most important one. The organism depends on the delivery of exogenous antioxidants, like selenium, vitamins E and C. Physical exercise triggers the production of superoxide radicals, which can at least partly be responsible for muscular damage. This work has studied the effect of Protection Zellaktiv (Smith Kline Beecham, Fink Naturarznei GmbH), a preparation containing selenium, vitamins C, E, B2, niacin and beta-carotene on the activities of superoxide dismutase and catalase, levels of glutathione malondialdehyde selenium, iron, zinc, triglicerides, total cholesterol, HDL- and LDL-cholesterol, before and after physical exercise. Muscle status was monitored by the activities of lactic dehydrogenase and creatine kinase. Protecton Zellaktiv was administered orally for one month, the measurements were repeated and the results before and after treatment were compared. It was found that treatment diminished the levels of malondialdehyde and zinc in serum, as well as cholesterol and triglicerides. Physical exercise before treatment decreased the levels of reduced glutatione, zinc and triglycerides. As expected, the levels of selenium were increased by the preparation. Protecton Zellaktiv suppressed the production of malondialdehyde during physical exercise. The preparation had a beneficial effect on lipid levels and it is inferred that lipid peroxidation was suppressed.

Effect of lecithin on the development of experimental atherosclerosis in rabbits.

Thirty male mongrel rabbits were divided into 3 equal groups: (1) controls, (2) animals receiving a high-fat diet (HFD) containing cholesterol and coconut oil, and (3) HFD + lecithin. The experiment lasted 12 weeks. In animals receiving a HFD (group II) the QRS interval (ECG) was significantly prolonged, and the concentration of lipid fractions (except for HDL-cholesterol) and malondialdehyde (MDA) in the blood was markedly elevated. Distinctly lower concentrations of zinc in the serum and cytochrome P-450 in the liver microsomes were observed. When administered together with the HFD, lecithin normalized QRS interval duration, inhibited the diet-induced lipid metabolism disturbances, reduced MDA concentrations and increased zinc concentrations in the serum. Elevated under the influence of lecithin, the content of cytochrome P-450 in the liver microsomes was shown. Surface area of the lipid deposits at 12 weeks, measured planimetrically averaged 24.43% in HFD-fed animals vs 9.28% in lecithin-treated rabbits. We conclude that lecithin is responsible, not only for the hypolipidaemic properties, but also for the antiatherosclerotic action in rabbits.

Comparative pharmacokinetics and bioavailability of flavonoid glycosides of Ginkgo biloba after a single oral administration of three formulations to healthy volunteers.

Eighteen healthy volunteers received three different formulations of Ginkgo biloba: capsules (A) and drops (B) (delivered by Agon Pharma), and tablets (C) (Tebonin-Dr. W. Schwabe) in equal an quantity, orally as a single dose, at an interval of at least five days. The pharmacokinetic parameters of the most important flavonoid glycosides: quercetin, kaempferol and isorhamnetin were established. The bioavailability was estimated using capsules as a standard formulation. Only the time to reach the peak concentration (tmax) of quercetin, kaempforol and isorhamnetin administered in the form of capsules, was significantly prolonged as compared with drops and tablets. Area under the curve (AUC) was the largest for formulation B for all the evaluated flavonoid glycosides, however the differences were not statistically significant. It is concluded that the three formulations of Ginkgo biloba extract are bioequivalent.

Extractum Fagopyri reduces atherosclerosis in high-fat diet fed rabbits.

A group of 30 male mongrel rabbits was divided into 3 subgroups: controls, animals receiving a high-fat diet (HFD) containing cholesterol and coconut oil, HFD + Extr. Fagopyri (EF) were treated for 12 weeks. Surface areas of lipid deposites after 12 weeks of treatment measured planimetrically in the intima of the aorta, averaged 86.5% in HFD-fed animals, but 68.6% in EF treated rabbits. The positive effect of EF was confirmed histopathologically. The finding of this study is that the EF administration results in the reduction of atherosclerotic plaque formation.

Ginkgo biloba extract inhibits the development of experimental atherosclerosis in rabbits.

Forty male mongrel rabbits were divided into 4 equal groups: (1) controls, (2) animals receiving a high-fat diet (HFD) containing cholesterol and coconut oil, (3) HFD + standardized. Ginkgo biloba extract (GB), and (4) HFD + rutin (as a well known substance it was used for comparison of pure single flavonol diglycoside activity with total extract). The experiment lasted 12 weeks. The most pronounced reduction in lipid metabolism disturbances and in the severity of plaque formation occurred after the GB had been administered. Lipid content in serum, liver homogenate and liver microsomes was depressed. HDL-cholesterol concentration was increased. Diminution of the malondialdehyde level in plasma was accompanied by an increase in the concentration of ascorbate free radicals in the liver in vitro. Testosterone concentrations in serum were normalized whilst the cytochrome P-450 content in liver microsomes was increased. Surface area of the lipid deposits at 12 weeks measured planimetrically averaged 85.5 % in HFD-fed animals vs 54.7 % in GB-treated rabbits. Quite distinct superiority of GB in antiatherosclerotic activity, as compared with rutin, was shown. These findings suggest that GB, in addition to lowering serum lipid level and possessing antioxidant properties in rabbits on an experimental diet, also affects metabolic processes in the liver and may modify lipid deposition in major arteries.

Clinical efficacy of 'essential' phospholipids in patients chronically exposed to organic solvents.

A total of 45 workers, who had been chronically exposed to a potentially hepatotoxic xylene-toluene-benzene mixture in the atmosphere, were treated for 3 months with 'essential' phospholipids. Routine biochemical tests and radioisotope investigations to assess liver damage were carried out both at baseline and after treatment. The liver:spleen index was increased in 71% of subjects and the mean isotope transit time in the liver was reduced in 90% of the patients after treatment. The biochemical parameters remained within the normal range throughout the treatment period. The results suggest that 'essential' phospholipids may be of value in the treatment of liver damage that has arisen as a result of chronic exposure to organic solvents.

Caffeine reduces the hepatotoxicity of paracetamol in mice.

Paracetamol causes extensive liver damage when taken in overdose quantities; however, it is less hepatotoxic when administered in combination with caffeine. The present work in mice was undertaken to study the effect of caffeine on mortality rates and biochemical and histological parameters of liver damage after administration of toxic doses of paracetamol. It was found that caffeine markedly increased the survival rate after administration of a dose of paracetamol that was lethal to 50% and 100% of mice, reduced liver damage as assessed by serum glutamic pyruvic and glutamic oxaloacetic transaminase activities, partially prevented the depletion of reduced glutathione and reduced histological changes to the liver accompanying paracetamol intoxication. The results support the possibility that caffeine might be useful for the treatment of paracetamol intoxication in humans.

Essential phospholipids modify immunological functions and reduce experimental atherosclerosis in rabbits.

Atherosclerosis was induced in male mongrel rabbits with a high-fat diet and the influence of essential phospholipids (EPL) on plaque formation, parameters of lipid metabolism and immunological functions was studied. When EPL were added to the high-fat diet there was a significant reduction in the area of atherosclerotic involvement of the aorta. The serum concentration of lipids decreased, often to normal values, and cholesterol esterified with polyunsaturated fatty acids appeared. Normalization of the malonyldialdehyde level in plasma was accompanied by a decrease in the concentration of ascorbate free radicals in blood and liver. The high-fat diet caused a depression of both non-specific and specific immune functions studied. With EPL in the diet the tests showed near normal or normal values. It is inferred from these results that a normal state of the immune system is important for preventing the progress of atherosclerotic changes. This is discussed with reference to the role of some immune cells in the metabolism of lipids and to participation of essential phospholipids in plasma membrane functions.

Padma 28 modifies immunological functions in experimental atherosclerosis in rabbits.

The effect of Padma 28 on selected parameters of humoral and cellular immune reactions in rabbits subjected to experimental atherosclerosis was studied. The drug significantly reduced the size of atherosclerotic plaques in the aorta and restored to a varying extent the immune functions studied. The possible mechanism by which Padma 28 may exert its anti-atherosclerotic action is discussed in the scope of the immunological theory of atherosclerosis.

Protective effect of selenium and vitamin E against changes induced in heart vessels of rabbits fed chronically on a high-fat diet.

The effect of selenium and vitamin E on lipid level in the blood serum, on the oxygen free radicals generation and on morphology of heart was tested after separate and combined administration to mongrel male rabbits fed on a high-fat diet (HFD). The lipid level and oxygen free radical generation was depressed markedly in animals fed on a HFD and receiving simultaneously selenium and vitamin E. In animals on a HFD the walls of the heart vessels were thickened, always to their complete obliteration. The presence of lipid droplets in endocardium could be observed as well. The hearts of the rabbits receiving selenium showed markedly fewer atheromatously changed vessels. Moreover, no accumulation of lipid droplets was seen in the endocardium of these animals. The least atherosclerotic alterations were observed in the myocardium of rabbits given HFD with addition of selenium and vitamin E in combination, no accumulation of lipids was shown in endocardium of these rabbits. An important finding of this study is, that the combination of selenium and vitamin E results in an intensified protective effect against changes evoked in the heart muscle of rabbits fed on a HFD.

Effect of selenium and vitamin E on the development of experimental atherosclerosis in rabbits.

Male mongrel rabbits, divided into 5 groups (1) controls, (2) animals receiving a high-fat diet (HFD) containing cholesterol and coconut oil, (3) HFD + selenium, (4) HFD + vitamin E, (5) HFD + selenium + vitamin E, were treated for 12 weeks. In the groups receiving selenium and/or vitamin E, the elevation of serum total lipids, beta-lipoproteins, total cholesterol and triglyceride was markedly suppressed. HDL cholesterol in these groups of animals was increased. The cytochrome P-450 content in liver microsomes was increased, and the concentration of malondialdehyde in the blood plasma of rabbits was significantly decreased, while thyroid hormones (T4, T3), cortisol and insulin level were increased. Surface area of the lipid deposits at 12 weeks measured planimetrically averaged 76% in HFD-fed animals but only 28% in selenium + vitamin E treated rabbits. The important finding of this study is that combination of selenium and vitamin E, results in an intensified effect on the improvement of metabolic processes and on the reduction of atherosclerotic plaque formation.

Hepatoprotective effect of selenium and vitamin E in rabbits fed a high-fat diet.

The high-fat diet consisted of cholesterol, hydrogenated coconut oil, and cholic acid. In the blood serum and in liver homogenate lipid content, cholesterol, and triglycerides were assayed. Cytochrome P-450 concentration in liver microsomes was also estimated. In animals receiving selenium and vitamin E, the content of lipid fractions in the blood serum and liver homogenate fell, while the cytochrome P-450 content in the liver microsomes was markedly elevated. The intensified protective effect of vitamin E and selenium applied in combination against changes induced in the liver of animals receiving a HFD was confirmed by macroscopic and microscopic examination of the organ.

Derivatives of (R,S)-1-N-(theophyllinyl-7'-ethyl)-amino-2-propanol with antiarrhythmic activity.

Three (R,S)-1-N-(theophyllinyl-7'-ethyl)-amino-2-propanol derivatives were obtained as soluble hydrochlorides and tested in four models of experimental arrhythmia. Two compounds 1a and 2 have shown antiarrhythmic properties and very low toxicity.

Inhibition of ethanol-induced changes in rats by Padma 28.

In male Wistar rats the protective effect of Padma 28 against changes induced by prolonged treatment with ethyl alcohol was investigated. Exposure of the animals to prolonged ethyl alcohol consumption caused a significant increase in AspAT (by 32%), A1AT (by 50%) and alkaline phosphatase (by 372%) activities as well as an increase in the levels of bilirubin (by 98%) and lipids in the blood serum and lipids in the liver homogenate. Padma 28 administration was found to exert a protective action against these changes: a significant reduction of blood total lipid, triacylglycerol, total cholesterol and bilirubin concentrations as well as in the activity of the liver enzymes was observed.

Endocrine functions in atherosclerotic rabbits.

Radioimmunoassay of serum thyroid hormones (T3 and T4), testosterone, estradiol, insulin and cortisol of rabbits fed on a high-fat diet (coconut oil, cholesterol, cholic acid) for three months and developing experimental atherosclerosis (confirmed by biochemical tests and morphological changes in the aorta) have revealed an increase in the content of estradiol and insulin, and a decline in the level of thyroid hormones and testosterone.

The influence of mestranol and chlormadinone given separately or in combination on the effects evoked by a high-fat diet in female rabbits.

The effect of mestranol and chlormadinone, the hormones contained in oral contraceptives: on lipid metabolism, some hemostatic parameters and on morphology of aorta, liver and heart was tested after separate or combined administration to mongrel female rabbits fed on a normal or high-fat diet (HFD). HFD administration led to typical atheromatous changes in the aortal intima. The hormones given together with HFD attenuated the augmentation of lipid serum level and the extent of atheromatous plaques in the intima. The percent content of alpha-lipoproteins was significantly lower in groups receiving HFD with or without the hormones than in the controls, but it was higher than in controls in the rabbits receiving the hormones alone. Chlormadinone given together with HFD potentiated atheromatous aortal changes, which occurred not only in the intima but also in the media. Mestranol given together with HFD significantly counteracted the development of atheromatous changes. Female rabbits receiving mestranol and chlormadinone displayed a significant increase in fibrinogen content, while those receiving mestranol showed an increased time of fibrinolysis. HFD produced a hepatic damage, which was augmented in rabbits concomitantly receiving the hormones. The hormones alone also displayed some, a less pronounced hepatotoxic action.

[Effect of essential phospholipids (EPL) on the course of chronic poisoning with organic solvents in rats]. / Wplyw niezbednych fosfolipidów (EPL) na przebieg przewleklego zatrucia rozpuszczalnikami organicznymi u szczurów.

Male Wistar rats were exposed in toxicological camera to the mixture of organic solvents. Composition and concentrations of the mixture were similar to the conditions in the production hall. The influence of essential phospholipids (EPL) on changes in the liver caused by the organic solvents were studied. Animals were exposed for 6 months. Histochemical and histological evaluation was performed after 2 and 6 months. In the liver of intoxicated animals marked vacuolar degeneration and diminution of glycogen contents were observed. Simultaneously, the protective effect of EPL was noted. It was expressed by distinctly decreased vacuolar degeneration, probably corresponding to neutral fat in hepatocytes as well as by normalization of glycogen contents.

[The effect of pollen on the changes in the liver of laboratory rats evoked by ethionine, carbon tetrachloride, allyl alcohol and galactosamine]. / Der Einfluss von Pollen auf die von Ethionin, Tetrachlorkohlenstoff, Allylalkohol und Galactosamin experimentell hervorgerufenene Veränderungen in der Leber von Laboratoriumsratten.

Doses of 50 mg/kg body weight and 200 mg/kg of Cernitin T 60 and Cernitin GBX may be used over 14 days for effective protection of rat liver cells from toxic action of ethionine. Application of CCl4 caused damage to the liver of rats. Such damage may be mitigated by both Cernitin preparations, particularly by Cernitin T 60. The damage was further reduced by Cernitin, following administration of allyl alcohol, with increase in transaminase, phosphatase, and bilirubin activities being used as criteria for measurement. The liver-protecting effect of Cernitin was confirmed in histopathological investigations. Cernitins prevented much of the damage actually caused by galactosamine.