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Interaction of progesterone derivatives with the digitalis target enzyme: impact of glycosidation on inhibitory potency.

Abstract：

:As a function of the structural modification of the steroid nucleus, the inhibitory interaction of 11 progesterone derivatives with human Na/K-ATPase (Na+/K(+)-transporting ATPase, EC 3.6.1.37), through C3-O-rhamnosylation, is either much decreased or weakly up to strongly increased, so that the rhamnosyl residue contributes to the complementary Gibbs energy of interaction, at the most, the same Gibbs energy increment as realized in ouabain. After C3 beta-O-rhamnosylation, the activity of some progesterone derivatives considerably surpasses that of 3 beta-O-rhamnosyl-chlormadinolacetate, which has been known to elicit positive inotropy in cats. The progesterone derivatives (aglycons and glycosides), that have been analysed more closely, produce their effects by the same molecular mechanism of interaction with Na/K-ATPase as characteristic for digitalis aglycons and glycosides. The results promise to pave the way for the identification of the chemical nature of endogenous digitalis and for the design of novel inotropic drugs.

journal_name

Pharmacol Res

journal_title

Pharmacological research

authors

Weiland J,Schönfeld W,Menke KH,Repke KR

doi

10.1016/s1043-6618(05)80102-1

subject

Has Abstract

pub_date

1991-01-01 00:00:00

pages

27-32

issue

1

eissn

1043-6618

issn

1096-1186

pii

S1043-6618(05)80102-1

journal_volume

23

pub_type

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