Studies on Cardioactive Steroids

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Abstract
In the present paper 32 genins and glycosides were tested for positive inotropic and arrhythmogenic activities at the isolated, spontaneously beating atrium of the guinea pig. It was found that: (a) substituents in C12-OHand C19-OH, respectively, diminished the efficacy 10-to 100-fold; (b) the acetylation at 16α-OH and 16β-OH, respectively, caused a 6- to 8-fold increase of efficacy, and (c) the esterification with acyl acids via hydroxyl groups at the sugar moiety caused a 2- to 10-fold decrease of efficacy depending on structure, number, and volume of the substituents. Similar results were gained with the cardioactive steroids at the (Na+-K+)-ATPase system and at the muscle tonus of the isolated guinea-pig ileum, demonstrating parallelism between these three parameters.

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