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

Eschenko N.D.1 , Putilina F.E.1, Galkina O.V.1, Vilkova V.A.1, Zacharova L.I.1, Fidarov A.F.1, Morozkina S.N.1, Shavva A.G.1

1. Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20156106724      PubMed Id: 26716744
Year: 2015  Volume: 61  Issue: 6  Pages: 724-730
The aim of this work was to study the ability of some estrogen 8a-analogues, that have CH 3 -group in the C-3 position, exhibit osteoprotective and cholesterolemic effects. The properties of these analogues was comparisoned with effects of native estradiol and 17a-ethynylestradiol (EE). We showed that compounds 3 ((d,l)-17b-acethoxy-3-methoxy-8a-estra-1,3,5(10)-triene) and 4 ((d,l)-3-methoxy-8a-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-17b-acethoxy-3-methoxy- 13-ethyl-8a-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 8a-analogues may be used as basic constructions for structural modifications which is necessary as medications with while spectrum of biological properties.
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Keywords: osteoprotective and cholesterolemic effects, synthetic estrogen analogues

Eschenko, N. D., Putilina, F. E., Galkina, O. V., Vilkova, V. A., Zacharova, L. I., Fidarov, A. F., Morozkina, S. N., Shavva, A. G. (2015). Study of osteoprotective and hypolipidemic effects of estrogen 8a a-analogues. Biomeditsinskaya Khimiya, 61(6), 724-730.
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