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At least 19 recordsLinked to original sources
PubMed1978

Studies on antiviral glycosides. Synthesis and biological evaluation of various phenyl glycosides.

A variety of analogues and derivatives of phenyl glycosides were synthesized for examination of their biological activities and of the relationship between structure and antiviral activity. For antiviral activity, a 6-deoxy-6-halogeno-D-glucose residue was most suitable for the carbohydrate moiety and p-alkylphenyl groups for the aglycone moiety. Based on these results, p-(sec-butyl)phenyl 6-chloro-6-deoxy-beta-D-glucopyranoside and p-(sec-butyl)phenyl 6-deoxy-6-iodo-beta-D-glucopyranoside were prepared, and the former compound was found to be the most potent antiviral substance, in this series, against influenza and Herpes simplex virus. The anomeric configuration of phenyl glycosides did not contribute to the antiviral activity.

Antiviral Agents↗
PubMed1977

Immunization with dextransucrases, levansucrases, and glycosidic hydrolases from oral streptococci. II. Immunization with glucosyltransferases, fructosyltransferases, and glycosidic hydrolases from oral streptococci in monkeys.

The feasibility of immunizing monkeys with enzymes from oral streptococci in an attempt to reduce dental caries was investigated. Forty rhesus monkeys, Macaca mulatta, were used. Cariogenic streptococci, S mutans, were implanted into all the monkeys' mouths. There was no pathological effect resulting from immunization. Of the 40 animals, 30 retained the implanted flora throughout the experiment; the remaining 10 were reimplanted until the streptococci remained. In six months, gross carious lesions were evident with plaque. Inhibitiors present in the monkey sera after immunization inhibited glucosyltransferase, fructosyltransferase, and neuraminidase activities. It was presumed the inhibitors were antibodies. There was a reduction of 68.6% in the total carious lesions in the animals immunized intraorally with glucosyltransferase, 62.4% reduction in those injected with fructosyltransferase, and 57.4% reduction in total lesions in those immunized with glycosidic hydrolases after 19 months, as compared to the control group. There were no gross lesions apparent in the group immunized with glycosidic hydrolases. It appears that immunization with enzymes significantly reduces carries and is feasible in a primate model.

Animals↗
PubMed1976

[Serum glycoside level in old age. Problems of course control in glycoside therapy].

Many intoxications--up to 20%--and the often described "digitalis-incompatibility of old age" require a strict indication for this long term therapy and a critical discussion to conceptions like "old age-heart" and "insufficiency of old age-heart". The factors of uncertainty for efficient therapy -- unknown rates of resorption and elimination, mistakes in dosage by patients and interaction with other medicaments on account of the multimorbidity of old age -- demand a better control than only clinical observation and electrocardiography. In 25 patients the serum glycoside concentration was evaluated during several weeks at constant dose by radioimmunoassay and analyzed. Digoxin-assay has to be available as an "emergency-measure", since the early diagnosis of digitalis intoxication in old patients is often very difficult because of the ambiguous clinical picture. 63 patients of different age with normal function of the kidneys (endogenous creatinin-clearance, nephrography with iodine-131-hippuran) were treated with 0,75 mg digoxin/die orally and the serum glycoside concentration was evaluated after 8, 24 and 48 hours by radioimmunoassay; we only found a dependence on weight, but not on the age of our patients. In old age, digoxin is metabolized in the same way as in young age, but because of frequent kidney diseases, kidney function should be assessed carefully before long term digoxin therapy.

Age Factors↗
PubMed1976

[New aspects on the mode of action of cardiac glycosides].

A dissociation of the therapeutic from the toxic effects of cardiac glycosides has repeatedly been described. Whereas it is generally accepted that the toxic effects of cardiac glycosides are based on an inhibition of the Na+-K+-ATPase, the mechanism of action of therapeutic concentrations of cardiac glycosides still remains uncertain. To test the hypothesis, that cardiac glycosides might be transported into a distinct compartment of the myocardium with the Na+-K-ATPase acting as a carrier, the interaction of some inhibitors of this enzyme (digitoxin, dihydroouabain, cassaine, N-ethylmaleimide, p-hydroxy-mercuribenzoate, ethacrynic acid, spironolactone) with ouabain was studied at different levels of cardiac glycoside actions: Myocardial function, cardiac uptake and subcellular distribution and binding to the Na+-K+-ATPase. The following results were obtained: All cardioactive drugs (ethacrynic acid and spironolactone showed no such effects) reduced dose-dependently the inotropic action of ouabain and in high concentrations increased its toxicity. The same drugs inhibited dose-dependently the cardiac uptake of ouabain without affecting the subcellular distribution pattern of ouabain. The binding of ouabain to the Na+-K+-ATPase was influenced in a similar way by these drugs, showing a competitive type of interaction with digitoxin, dihydroouabain and cassaine and a non-competitive mechanism with N-ethylmaleimide and p-hydroxymercuribenzoate. These results support the concept of a cardiac glycoside-ATPase interaction as a basis for the therapeutic action of these drugs. This may be explained either by a direct influence of cardiac glycosides on the ATPase activity and/or by a carrier mediated cardiac glycoside-transport into a distinct compartment of the myocardial cell.

Action Potentials↗
PubMed1977

Clinical implications of differences in pharmacodynamic action of polar and nonpolar cardiac glycosides.

The principal effects of cardiac glycosides probably can be classified as parasympathomimetic or sympathomimetic. Data from animals and from man suggest that polar cardiac glycosides, such as ouabain and digoxin, possess greater parasympathomimetic (vagal) cardiac effect for a given amount of sympathomimetic (positive inotropic) cardiac effect than do less polar cardiac glycosides, such as digitoxin. Polar glycosides therefore offer some advantage in uncomplicated paroxysmal atrial tachycardia and in uncomplicated atrial flutter and atrial fibrillation when the principal desired effect is reduction in the number of atrial impulses reaching the ventricles or conversion to normal sinus rhythm. Non-polar glycosides offer an advantage when positive inotropicity is desired but when there is some degree of atrioventricular block or when inappropriate sinus bradycardia or anorexia, nausea, or vomiting are present. Ecotopic impulse formation when due to cardiac glycosides is a toxic manifestation of excessive sympathomimetic effect, but is aggravated by vagal-induced sinus bradycardia, so that both parasympathomimetic and sympathomimetic capability of cardiac glycosides must be considered when dealing with myocardial electrical instability.

Animals↗
PubMed1978

[The clinical significance of plasma glycoside concentrations in patients with cardiac pacemakers (author's transl)].

308 digitalized out-patients with artificial cardiac pacemakers were explored for signs of glycoside toxicity with simultaneous determination of digoxin plasma levels 12 hours after the last dose. The incidence of different side effects commonly attributed to overdigitalization did not allow prediction of toxic plasma levels. 55% of all glycoside levels were within the therapeutic range, 34% were below 0.7 ng/ml and only 11% above 2.0 ng/ml. With the most commonly prescribed maintenance doses of the glycosides used (digoxin 0.5 mg, beta-acetyldigoxin 0.4 mg, beta-methyldigoxin 0.2 mg, lanatosid C 1.0 mg) therapeutic plasma levels were reached regularly in 60-65% of the patients. A significant correlation existed between plasma glycoside concentrations and renal function as well as age, but glycoside concentrations could not be correlated with the age of the patients. There were no indications for interactions of the different glycosides prescribed with diuretics or oral antidiabetics.

Adult↗
PubMed1977

[Pharmacokinetics of cardiac glycosides and clinical consequences].

The purpose of pharmacokinetics of cardiac glycosides is to study the time courses of glycosides in biological fluids, tissues and excreta. The extent of accumulation of a given dose at uniform time intervals depends only from the overall elimination rate constant. By knowing the elimination rate constant the extent to which a cardiac glycoside would accumulate in the body following a fixed dosing regimen can be calculated. The higher accumulation in the central nervous system requires a much longer time. Therefore it may be assumed that the brain is a deep compartment for cardiac glycosides and this compartment cannot be detected by analysis of plasma glycoside concentrations. Central side effects of cardiac glycosides may occur at therapeutic plasma levels. In renal disease a lower maintenance dose of digoxin and methyldigoxin should be administered or the same dose less frequently. Digitoxin does not accumulate in patients with renal failure or in anuria since the extrarenal elimination of digitoxin is much higher compared to digoxin and methyldigoxin.

Biological Availability↗
PubMed1979

Cardenolide analogues: 10--characterization of cardiac glycosides by chemical ionization mass spectrometry.

The potential of chemical ionization mass spectrometry for the characterization of naturally occurring and semi-synthetic cardiac glycosides has been investigated. Methane, isobutane and ammonia were used as reactant gases. With the exception of ouabain, the ammonia chemical ionization mass spectra of the cardiac glycosides examined in this work contained abundant [M + NH4]+ions and abundant fragment ions formed by cleavage of glycoside bonds. Ammonia chemical ionization mass spectrometry was found to provide a rapid and sensitive method for the characterization of the products of glycosidation reactions. In contrast, the methane and isobutane chemical ionization mass spectra of the cardiac glycosides, with the exception of ouabain, did not contain protonated molecular ions and did not contain abundant fragment ions above m/z 400.

Ammonia↗
PubMed1977

Some pharmacological studies on the cardiotonic effects of furanosteroidal glycosides.

Cardiotonic effects and cardiotoxicities of three furanosteroidal glycosides were compared with those of standard cardiac glycosides (digitoxin, gitoxin, etc.). Furanosteroidal glycosides showed positive inotropic effects in both isolated guinea-pig atria and rabbit hearts. The positive inotropic effect of 17beta-(3-furyl)-5beta,14beta-androstane-3beta,14,16beta-triol-3-bisdigitoxoside(FGBD) corresponded to that of digitoxin in isolated guinea-pig atria and frog hearts. Intravenous and oral administration of FGBD and 17beta-(3-furyl)-5beta,14beta-androstane-3beta,14,16beta-triol-3-tridigitoxoside(FGTD) in higher doses induced cardiac arrest after vomiting, bradycardia, ventricular rhythm, and ventricular fibrillation in pigeons and cats. Comparison of lethal doses between intravenous and oral administration of cardiac glycosides in pigeons and cats suggested that gastrointestinal absorption of FGBD and FGTD is inferior to that of digitoxin but superior to that of gitoxigenin bisdigitoxoside and gitoxin. Cardiotonic effects of furanosteroidal glycosides were confirmed in isolated guinea-pig, rabbit and frog hearts.

Androstanes↗
PubMed1979

Investigation of cardiac glycoside levels in human post mortem blood and tissues determined by a special radioimmunoassay procedure.

Even after the introduction of radioimmunological methods the question of a cardiac glycoside causing or contributing to the death of a patient can not be answered satisfactorily. By means of a special radioimmunoassay procedure for digoxin as well as for the structurally related methyl- and acetylderivatives we measured the concentrations in human blood and post mortem tissues. We investigated the glycoside contents in the blood of intravenously digitalised (Novodigal) al) patients before and after death. At autopsy blood specimens were taken from the heart and the femoral vein. We found an increase of the glycoside level up to a highly toxic range (7--15 ng/ml) especially in the heart blood. Thus post mortem blood levels of digoxin and its derivatives are not suitable for a final decision in alleged cases of fatal poisonings. Measuring various concentrations in tussues and body fluids of the above cardiac glycosides mentioned revealed the kidney concentration to be of high value in confirming a digitalis poisoning. This organ and the heart show the highest tissue concentrations. Interpretations of fatal digitalis poisonings should be based on the additional knowlege of these concentrations. Individual cardiac glycosides may be analyzed by a combination of thin layer chromatography and radioimmunoassay.

Cardiac Glycosides↗
PubMedDate not supplied

Studies on a plasma cardiac glycoside assay based upon displacement of 3-H-ouabain from Na+-K+-ATPase.

We tested an assay system introduced for plasma glycoside measurements, basing on the displacement of 3-H-ouabain from Na+-K+-ATPase by unlabeled glycoside. ATPase preparations from hog, cat and guinea pig were used. Displacements were performed using 20 cardiac glycosides, genins and derivatives with different cardiac activity. Most of the glycosides and derivatives do not induce a continuous 3-H-ouabain displacement from the ATPase, but a very steep increase of unbound 3-H-ouabain between 10-minus 7 and 2 times 10-minus 7 M. Therefore this assay system shows a satisfactory discrimination only in a short concentration range. This behavior and a relatively low sensitivity make the ATPase displacement assay problematic for clinical and pharmacokinetical plasma glycoside measurements.

Adenosine Triphosphatases↗
PubMed1979

[Effect of triterpene glycosides on plasma membrane permeability for UV-absorbing substances in Saccharomyces carlsbergensis yeast cells].

The effect of triterpene glycosides of cauloside C from Caulophyllum robustum M, stichoposide A from Stichopus japonicus S. and theasaponine from Thea sinensis Z. on permeability of plasmic membranes of Saccharomyces carlsbergensis for UV-absorbing substances was studied. It was found that incorporation of 14C-uridine from the endocellular pool into the yeast acid-insoluble fraction decreased under the effect of the triterpene glycosides as a result of the precursor leakage from the cell into the medium. It was found that the triterpene glycosides stimulated the leakage of the UV-absorbing substances with an absorption maximum at 260 nm from the cells. The maximum membranotropic effect was observed at 30--40 degrees C and in the presence of monovalent potassium, sodium, ammonium and lithium ions in the medium. Cauloside C and theasaponine, pentacyclic glycosides had the highest effect on the permeability at pH 4.8--5.6, while stichoposide A, a tetracyclic glycoside, had the highest effect at pH 7.0.

Cell Membrane Permeability↗
PubMed1977

[Determination of glycoside concentrations in human tissue by means of radioimmunoassay (author's transl)].

After extraction of myocardial and skeletal muscle biopsy and autopsy specimens tissue glycoside concentrations can be determined by radioimmunoassay. Total tissue extraction of digoxin and beta-methyl-digoxin varies between 87 and 95%, the variation coefficient for repeated determinations is 10.2%. Glycoside concentrations of left ventricular papillary muscle obtained after mitral valve replacement were 69.0 +/- 25.05 ng/g with a tissue to serum relation of 46.6 +/- 8.96:1 and a correlation coefficient of r = 0.8442. In autopsy left ventricular papillary muscle glycoside concentrations were 105.2 +/- 27.35 ng/g with an almost identical tissue to serum relation of 46.2 +/- 9.57:1 and a corresponding serum concentration of 2.3 +/- 0.63 ng/ml. In adults glycoside concentrations of autopsy specimens of the right ventricle were significantly lower by 28 to 30% than those of the left ventricle. Glycoside concentrations of skeletal muscle specimens (m. pectorialis major) were 14.7 +/- 10.35 ng/g with a tissue to serum relation of 9.7 +/- 3.00:1 (r = 0.8377), which corresponds to approximately 1/5 to 1/4 of the concentrations of the left ventricular myocardium.

Aged↗