Study of osteoprotective and hypolipidemic effects of estrogen 8α-analogues

The aim of this work was to study the ability of some estrogen 8α-analogues, that have CH3-group in the C-3 position, exhibit osteoprotective and cholesterolemic effects. The properties of these analogues was comparisoned with effects of native estradiol and 17α-ethynylestradiol (EE). We showed that...

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Bibliographic Details
Published in:	Biomeditsinskaia khimiia Vol. 61; no. 6; p. 724
Main Authors:	Eschenko, N D, Putilina, F E, Galkina, O V, Vilkova, V A, Zacharova, L I, Fidarov, A F, Morozkina, S N, Shavva, A G
Format:	Journal Article
Language:	Russian
Published:	Russia (Federation) 01-11-2015
Subjects:	Animals Estradiol Congeners - chemical synthesis Estradiol Congeners - chemistry Estradiol Congeners - pharmacology Female Hypercholesterolemia - drug therapy Hypercholesterolemia - metabolism Hypercholesterolemia - pathology Hypolipidemic Agents - chemical synthesis Hypolipidemic Agents - chemistry Hypolipidemic Agents - pharmacology Osteoporosis - drug therapy Osteoporosis - metabolism Osteoporosis - pathology Rats Rats, Sprague-Dawley synthetic estrogen analogues osteoprotective and cholesterolemic effects
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Summary:	The aim of this work was to study the ability of some estrogen 8α-analogues, that have CH3-group in the C-3 position, exhibit osteoprotective and cholesterolemic effects. The properties of these analogues was comparisoned with effects of native estradiol and 17α-ethynylestradiol (EE). We showed that compounds 3 ((d,l)-17β-acethoxy-3-methoxy-8α-estra-1,3,5(10)-triene) and 4 ((d,l)-3-methoxy-8α-estra-1,3,5(10)-triene-17-one) had the same osteoprotective and cholesterolemic effects as EE. The utherotropic effects of compound 3 and EE were the same, while the utherotropic activity of 17-keto derivative (compound 4) was higher than effect of EE. The osteoprotective and cholesterolemic effects of compounds 5 and 6 (d- or l-17β-acethoxy-3-methoxy-13-ethyl-8α-gone-1,3,5(10)-triene) were approximately the same, however the utherotropic action of these compounds was different: the compound 5 had significantly lower activity, but the compound 6 had the same effect in comparison with EE. Thus, all studied estrogen 8α-analogues may be used as basic constructions for structural modifications which is necessary as medications with while spectrum of biological properties.
ISSN:	2310-6972
DOI:	10.18097/PBMC20156106724