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Structure-activity relationships of saponins and cardiac glycosides. III. Beta-L-xylopyranosyl-(1-->6)-alpha- and -beta-D-glucopyranosides.

Comparisons of the biological activities of diosgenyl, methyl glycyrrhetinate or digitoxigenyl 3-O-beta-L-xylopyranosyl-(1-->6)-beta-D-glucopyranoside with those of other previously tested glycosides confirmed our assumption that both the hemolytic and antifungal activities of steroid saponins are generally parallel to each other, while almost all hemolytic triterpenoid saponins and nonhemolytic ones have no antifungal activity, and that cardiac diglycosides having a (1-->4) sugar linkage have stronger activities than those with a (1-->6) or a (1-->2) linkage. On the other hand, the case of the diosgenyl 3-O-beta-L-xylopyranosyl-(1-->6)-alpha-D-glucopyranoside didn't conform to the above assumption, but those of methyl glycyrrhetinate and digitoxigenyl did.

Adenosine Triphosphatases↗

LC-NMR applied to the characterisation of cardiac glycosides from three micropropagated Isoplexis species.

Species of the genus Isoplexis are of particular interest with respect to the biochemical pathway leading to the cardenolides. It is important to determine whether or not 5beta-configured compounds, typically produced by Digitalis species and used in medicine, are present together with their respective alpha-isomers in Isoplexis spp. Structure elucidation by LC-NMR of the products isolated from in vitro regenerated Isoplexis canariensis, I. chalcantha and I. isabelliana was carried out, and similarities were observed among the products of the three species, including the presence of digitoxigenin-type cardenolides in I. canariensis and xysmalogenin and canarigenin derivatives in I. chalcantha never previously reported in these species. Pregnane glycosides not found until now either in Isoplexis or Digitalis were also detected.

Cardiac Glycosides↗

[Optimization of therapy using cardiac glycosides].

By the estimation of the serum glycoside concentration during the last years numerous new recognitions have been got, particularly concerning the pharmacokinetics of the heart glycosides, which increasingly will be reflected in the clinical practice. Apart from thoughts on pharmacokinetics the author adopts a definite attitude to glycoside tolerance, to the influence of age and bodyweight as well as to the importance of disturbances of the renal function. Moreover it is referred to new aspects in the dosage of heart glycosides, in which case the revision of the central therapy recommendations seems to be necessary.

Adult↗

Nature of the Schwann cell electrical potential. Effects of the external ionic concentrations and a cardiac glycoside.

The effects on the Schwann cell electrical potential of external ionic concentrations and of K-strophanthoside were investigated. Increasing (K)(o) depolarized the cell. The potential is related to the logarithm of (K)(o) in a quasi-linear fashion. The linear portion of the curve has a slope of 45 mv/ten-fold change in (K)(o). Diminutions of (Na)(o) and (Cl)(o) produced only small variations in the potential. Calcium and magnesium can be replaced by 44 mM calcium without altering the potential. Increase of (Ca)(o) to 88 mM produced about 10 mv hyperpolarization. The cell was hyperpolarized by 11 mv and 4 mv within 1 min after applying K-strophanthoside at concentrations of 10(-3) and 10(-5)M, respectively. No variations of cellular potassium, sodium, or chloride were observed 3 min after applying the glycoside. The hyperpolarization caused by 10(-3)M K-strophanthoside was not observed when (K)(o) was diminished to 1 or 0.1 mM or was increased to 30 mM. At a (K)(o) of 30 mM, 10(-2)M strophanthoside was required to produce the hyperpolarizing effect. In high calcium, the cell was further hyperpolarized by the glycoside. The initial hyperpolarization caused by the glycoside was followed by a gradual depolarization and a decrease of the cellular potassium concentration. The results indicate that the Schwann cell potential of about -40 mv is due to ionic diffusion, mainly of potassium, and to a cardiac glycoside-sensitive ion transport process.

Animals↗