title: [Study of osteoprotective and hypolipidemic effects of estrogen 8α-analogues].
abstract: 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.
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: N D
authors.initials: ND
authors.lastname: Eschenko
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: F E
authors.initials: FE
authors.lastname: Putilina
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: O V
authors.initials: OV
authors.lastname: Galkina
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: V A
authors.initials: VA
authors.lastname: Vilkova
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: L I
authors.initials: LI
authors.lastname: Zacharova
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: A F
authors.initials: AF
authors.lastname: Fidarov
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: S N
authors.initials: SN
authors.lastname: Morozkina
authors.affiliation: Faculty of Biology and Chemistry Faculty, St.-Petersburg State University, St.-Petersburg, Russia.
authors.forename: A G
authors.initials: AG
authors.lastname: Shavva
mesh_terms: D000818:Animals; D045166:Estradiol Congeners / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006937:Hypercholesterolemia / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010024:Osteoporosis / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D045166:Estradiol Congeners; D000960:Hypolipidemic Agents
keywords: osteoprotective and cholesterolemic effects; synthetic estrogen analogues