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At least 811 records · Page 45Linked to original sources
PubMed1992

Receptor kinetics and concentration-effect relation of cardiac glycosides.

Therapeutic and toxic actions of cardiac glycosides are attributed to an inhibition of Na, K-ATPase. The therapeutically relevant range is between 25% and 50% inhibition. There is a good correlation between the average steady state serum concentration of glycosides and their therapeutic action. However, therapeutic and toxic effects set in with a latency and therefore do not follow the daily variations in glycoside concentration. Although the effect follows the average serum concentrations, only the minimal concentration is measured. In principle this is only adequate if the ratio of average/minimal concentration is constant. A model calculation showed that with a constant average steady state concentration an increase in the distribution volume or a decrease in total body clearance with corresponding reduction of the daily dose lead to an increase of the minimal concentrations of 5-7%. This means a corresponding underestimation of the average concentration from the minimum concentration. However, the deviations are too small to be of clinical relevance.

Cardiac Glycosides↗
PubMed2004

[Determination of luteolin-7-O-glycoside in the herb of Dracocephalum rupestra by HPLC].

OBJECTIVE: To develop a method for determination of luteolin-7-O-glycoside in the roots, stems, leafs, flowers and aerial parts of Dracocephalum rupestra sampled in different seasons. METHOD: The samples were analyzed on an phenomenex C18 column, with mobile phase of methanol-acetonitrile-0.4% phosphoric acid (30:8:62) at flow rate 1.0 mL x min(-1) and detection at wavelength of 350 nm. RESULT: The content of luteolin-7-O-glycoside in different parts of D. rupestra was different maximum in leaves, while minimum in stems. Luteolin-7-O-glycoside in D. rupestra sampled before blossoming was the highest. CONCLUSION: The method simple, accurate and suitable for the quality evaluation of this plant medicine.

Chromatography, High Pressure Liquid↗
PubMed2005

[The place of cardiac glycosides in the treatment of chronic heart failure].

In a series of papers the authors analyze literature data on the use of cardiac glycosides for long term treatment of chronic heart failure. Part 1 is devoted to clinical pharmacology of glycosides with special emphasis on digoxin. In low doses digoxin produces no substantial effect on contractility of left ventricular myocardium but can cause worsening of its diastolic function. Favorable action of digoxin on clinical course and outcomes of chronic heart failure is most probably related to modulation of neuro-humoral systems. Data on factors influencing sensitivity to glycosides in various categories of patients with heart failure, their interaction with other drugs, and contraindications for digoxin are also presented.

Cardiac Glycosides↗
PubMed2005

[Synthesis of camptothecin glycosides by phase transfer-catalysis and its inhibitory activity against topo I].

AIM: To find new anticancer drug based on the structure of 10-hydroxy camptothecin. METHODS: Six camptothecin glycosides (7-12) were synthesized by phase transfer catalysis. The structures of all compounds synthesized were determined by 1H NMR, IR and MS. Their antitumor activity was evaluated on cancer cells in vitro, and inhibitory activity against Topo I was evaluated by molecular biologic method. RESULTS AND CONCLUSION: The result indicated that the yield of camptothecin glycosides by phase transfer catalysis is much higher than by the method from literature, camptothecin glycosides have much lower cytotoxicities on cancer cell in vitro, but have better inhibitory activity of topo I.

Antineoplastic Agents, Phytogenic↗
PubMed2006

[Study on purification of 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from Polygonum multiflori].

OBJECTIVE: To study the conditions and parameters of purifying 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from Polygonum multiflori. METHOD: Absorption capacity of four resins for 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside was compared. With the adsorption ability as indexes, the process of absorbing and purifying 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from P. multiflori with S-8 macroporous resin absorbent was selected by orthogonal design. RESULT: The S-8 resin was the best of the four resins. The optimum process condition was 50% ethanol as eluting solvent, the flow rate at 1.5 mL x min(-1), pH at 7-8, and the solution concentration at 0.2 g x mL(-1). The absorption capacity by this process was 36.89 mg x g(-1). CONCLUSION: The process is simple and convenient and the regeneration of resin is easy, so this method of purification is advisable.

Absorption↗
PubMed2006

Phenolic glycosides from Exostema mexicanum leaves.

Phytochemical investigation of the leaves of Exostema mexicanum led to the isolation of two novel acylated flavonol glycosides 6, 7 and three glycosides 1-4 structurally belonging to the group of 4-phenylcoumarins. One of them, 5-O-beta-D-glucopyranosyl-4'-hydroxy-7-methoxy-4-phenylcoumarin (2), turned out to be new. Furthermore, the 4-phenylcoumarin aglycone 3'-hydroxy-4',5,7-trimethoxy-4-phenylcoumarin (5) was obtained. The in vitro cytotoxicity of 3-5 against the cell line ECV-304 was evaluated; the aglycone 5 was highly cytotoxic, whereas the glycosidic compounds 3 and 4 were inactive.

Antineoplastic Agents, Phytogenic↗
PubMed2006

[Isolation and determination of homoeriodictyol-7-O-beta-D-glycoside in Viscum coloratum].

The homoeriodictyol-7-O-beta-D-glycoside was isolated from Viscum coloratum and identified by mass spectrometry and nuclear magnetic resonance (NMR) (1H NMR and 13C NMR). A method for determination of homoeriodictyol-7-O-beta-D-glycoside in Viscum coloratum was developed by using a Kromasil C18 column (200 mm x 4.6 mm i.d., 5 microm) with a mixture of acetonitrile and 0.5% glacial acetic acid solution (18:82, v/v) as mobile phase at a flow rate of 1.0 mL/min. The detection wavelength was set at 284 nm and temperature was set at 30 degrees C. The volume of injection was 10 miccro L. Good linear relationship (r = 0.9997) between the mass concentration and the peak area of homoeriodictyol-7-O-beta-D-glycoside was obtained in the range of 1.0-32.0 mg/L. The recoveries were found to be in the range of 96.0%-100.1%. The results of the experiments demonstrated that the established method is rapid and simple with good accuracy and reproducibility. The method is suitable for the quality control of Viscum coloratum from different sources.

Flavonoids↗
PubMed1991

[The current concepts of the effect of cardiac glycosides on sinus node function and atrioventricular conductivity].

The clinical aspects of the influence of cardiac glycosides on the sinus node and atrioventricular junction in health and dysfunction are reviewed. It has been shown that digitalis drugs do not produce any effect on sinus node automatism including that in dysfunction. Cardiac glycosides suppress enhanced atrioventricular conduction and do not affect it provided it remains within normal. The mechanisms by which cardiac glycosides may act are discussed: extracardiac, cholinomimetic (in the acute test and direct one) and influencing heart conduction components (when used continuously).

Cardiac Glycosides↗
PubMed1990

[The antifungal action of polygalacic acid glycosides].

Triterpenoid glycosides obtained from Solidago virgaurea L. and Bellis perennis L. (Asteraceae) inhibit the growth of human-pathogenic yeasts (Candida and Cryptococcus species). First results are given of the investigations on the mode of action and the relationships between structure and activity of these compounds. The intensity of growth inhibition is influenced particularly by the carbohydrate chains of the glycosides. Monodesmosidic as well as bisdesmosidic glycosides of polygalacic acid exert fungicidic effects.

Antifungal Agents↗
PubMed1990

Recognition of N-glycosidic carbohydrates on esophageal carcinoma cells by macrophage cell line THP-1.

Cell-to-cell contact between macrophages and tumor cells is an important initial reaction in a host defense mechanism against tumor cells. The authors have studied cell surface components of human esophageal carcinoma cells recognized by macrophages. Superoxide release from THP-1 cells, a human macrophage cell line, was analyzed in their interaction with a battery of human squamous cell carcinoma cell lines (TE) originated from esophageal cancer patients. The macrophage-triggering ability of TE 1 cell line, a high stimulant, was reduced after treatment with trypsin or tunicamycin, an inhibitor of N-glycosidic glycosylation. Addition of monosaccharides was efficient in competitive inhibition of these cellular interaction. Moreover, con-A-resistant mutation of TE 1 cells was found to reduce their macrophage-triggering ability, associated with increase of L-PHA-binding capacity, suggesting substitution to the GlcNAc beta(1----6)-linked lactosamine antenna in N-glycosidic carbohydrates. These findings suggest that terminal residues of N-glycosidic carbohydrates on some esophageal carcinoma cells may contribute to the recognition sites of macrophages.

Carcinoma, Squamous Cell↗
PubMedDate not supplied

[Endogenous digitalis-like substances and cardiac glycosides: facts and hypotheses].

The review presents the data on endogenous digitalis-like substances the effects of which are imitated by administered cardiac glycosides. It is suggested that the individual differences in the responses of patients to cardiac glycosides, a great range of doses of the drugs causing intoxication as well as the absence of a close correlation between the occurrence of therapeutic and toxic effects and blood plasma glycoside concentration are related to the change of the level of endogenous digitalis-like substances in the organism. The further study of the chemical structure of digitalis-like substances and the mechanism of their secretion opens up new possibilities for practical medicine.

Animals↗
PubMed1990

Targeting of plant glycoside-bearing liposomes to specific cellular and subcellular sites.

The possibility of using liposomes as an effective drug delivery system has been studied by incorporation of two plant glycosides of varying terminal sugar residues onto the surface of liposomes and examination of their distribution in different tissues. The two glycosides, corchorusin D and asiaticoside having glucose and rhamnose respectively at the terminal ends wee selected for the purpose. The hepatic uptake of liposomes made from egg lecithin, cholesterol and dicetyl phosphate and either of the two glycosides was compared. The hepatic uptake of asiaticoside bearing liposomes was reduced, whereas that of corchorusin D bearing liposomes was enhanced and was specific for glucose. Liver perfusion followed by cell separation showed that the uptake is mostly into the non-parenchymal cells of liver. The distribution of corchorusin D bearing liposomes was maximal in the lysosomal fraction of the non-parenchymal cells. Ways of using corchorusin D bearing liposomes as delivery systems for drugs or enzymes to lysosomes have been sought.

Agglutination Tests↗
PubMed1978

Metabolism of glycosides by Pseudomonas maltophilia.

A study of the abilities of 23 strains of Pseudomonas maltophilia to hydrolyze synthetically-prepared and naturally-occurring glycosides is presented. Direct detection of liberated aglycones was used to determine hydrolysis of the five most-commonly-used glycosides (amygdalin, arbutin, esculin, ONPG (o-nitrophenyl-beta-d-galactoside), and salicin). The capabilities of the strain for acid production from 17 glycoside substrates were also determined using a medium designed to minimize the production of acid-neutralizing end-products from peptones.

Amygdalin↗
PubMed1989

[Animal experiment studies of the ocular toxicity of cardiac glycosides].

The addition of different types of cardiac glycosides (strophanthin, digoxin, digitoxin) to the perfusion medium of isolated cat eyes, kept alive by extracorporeal perfusion, leads to changes in ERG. There is a dose-dependent reduction of the b-wave amplitude in scotopic and photopic electroretinogram (ERG). At the same time the implicit time of the potentials increases. In the scotopic-isolated P III component, both amplitude and implicit time increase. The concentrations inducing ERG changes that are fully reversible after cessation of drug application correlate well with the known toxic drug blood levels in humans. The disappearance rate of the drug induced effects was almost equal under these conditions (extracorporeal perfusion) for the different glycosides. In conclusion, our results indicate that at least part of the visual symptoms of glycoside intoxication are already evident at the retinal level.

Animals↗
PubMed1989

Antimicrobial and immunomodulating effects of some phenolic glycosides.

Several phenolic glycosides, i.e. acteoside, desrhamnosyl acteoside, and purpureaside A, B and C, exerted weak antibacterial effects on Escherichia coli. Acteoside had antiplasmid effects, including F'lac plasmid elimination, and inhibited kanamycin resistance transfer in E. coli. Acteoside, desrhamnosyl acteoside and purpureaside A displayed antiviral effect on Aujeszky virus. All of the phenolic glycosides decreased some human leucocyte functions, including rosette formation, mitogen-induced blast transformation and phagocytic activity in vitro. The purpureaside C had significant proinflammatory action, however, other phenolic glycosides showed neither proinflammatory nor antiinflammatory effect on carrageenin-induced inflammation in vivo.

Animals↗
PubMed1985

Characterization of digitalis-like factors in human plasma. Interactions with NaK-ATPase and cross-reactivity with cardiac glycoside-specific antibodies.

Much of the evidence for a physiologically important endogenous inhibitor of the sodium pump has been either contradictory or indirect. We have identified three discrete fractions in desalted deproteinized plasma from normal humans that resemble the digitalis glycosides in that they: are of low molecular weight; are resistant to acid and enzymatic proteolysis; inhibit NaK-ATPase activity; inhibit Na+ pump activity in human erythrocytes; displace [3H]ouabain bound to the enzyme; and cross-react with high-affinity polyclonal and monoclonal digoxin-specific antibodies but not with anti-ouabain or anti-digitoxin antibodies. An additional fraction cross-reacted with digoxin-specific antibodies but had no detectable activity against NaK-ATPase. The three inhibitory fractions differed from cardiac glycosides in that their concentration-effect curves in a NaK-ATPase inhibition and [3H]ouabain radioreceptor assays were steeper than unlabeled ouabain. This suggests that these inhibitors are not simple competitive ligands for binding to NaK-ATPase. In the presence of sodium, no fraction required ATP for binding to NaK-ATPase, and in the presence of potassium, only one fraction had the reduced affinity for the enzyme that is characteristic of cardiac glycosides. Unlike digitalis, all three NaK-ATPase inhibitory fractions stimulated the activity of skeletal muscle sarcoplasmic reticulum Ca-ATPase. The presence of at least three fractions in human plasma that inhibit NaK-ATPase and cross-react to a variable degree with different digoxin-specific antibody populations could explain much of the conflicting evidence for the existence of endogenous digitalis-like compounds in plasma.

Adenosine Triphosphate↗
PubMed1979

Facile syntheses of 1,2,4-triazole and s-triazine glycosides from glycosyl isothiocyanates.

Reaction of glycosyl isothiocyanates (la, b or c) with acyl or aroyl hydrazine gave the corresponding glycosyl thiosemicarbazides, and which were treated with Ac2O-H3PO4 to yield 1,2,4-triazole glycosides. Similar treatment of la, b or c with amidino compounds gave glycosylisothiobiurets, followed by N-bromosuccinimide (NBS) oxidation to give 1,2,4-triazole glycosides. Treatment of glycosylisothiobiurets with triethyl orthoformate gave the corresponding s-triazine glycosides.

Glycosides↗
PubMed1981

[The effect of cardiac glycosides and electrolytes on cell membrane sodium, potassium-adenosine triphosphatase].

A brief summary is given of the structure of the cell membrane and the enzyme system which actively transports Na+ and K+ ions across it. The function of different ions in this process is discussed as well as the effect of cardiac glycosides on ion transport. The utilization of electrolytes to combat cardiac glycoside poisoning and an indirect method for demonstrating the presence of cardiac glycosides in the organs of ruminants, suspected of being poisoned by these toxins, is described.

Animals↗