Document Detail


Long-acting estrogenic responses of estradiol fatty acid esters.
MedLine Citation:
PMID:  2515394     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Estradiol esters at C-17 and C-3 with palmitic, stearic and oleic acids were chemically synthesized and then evaluated for their long-acting estrogenic responses in ovariectomized rats. The duration of the biological effects was measured after a single subcutaneous dose of 0.1 mumol of each ester and compared with those observed with 17 beta-estradiol, estradiol 3-benzoate and estradiol 17-enanthate. Vaginal citology, uterophyc action, serum gonadotropins inhibition and 17 beta-estradiol levels were measured 0, 5, 10, 20, 30 and 60 days after injection. The results disclosed that most of the estradiol derivatives evaluated exhibited a long-acting estrogenic action. However, the monoesters at C-17 showed longer effects that monoesters at C-3, while the estradiol diesters exhibited the shortest effects. In addition as shown by its low serum levels, all estradiol esters with unsaturated fatty acids show a decreased E2 absorption. The overall results indicated that esterification of E2 with long chain fatty acids provided long-acting properties to it, being higher with C-17 esters. Whether some of these compounds could be employed in substitutive endocrine therapy remains to be established.
Authors:
M A Vazquez-Alcantara; M Menjivar; G A Garcia; J C Díaz-Zagoya; J Garza-Flores
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of steroid biochemistry     Volume:  33     ISSN:  0022-4731     ISO Abbreviation:  J. Steroid Biochem.     Publication Date:  1989 Dec 
Date Detail:
Created Date:  1990-02-27     Completed Date:  1990-02-27     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0260125     Medline TA:  J Steroid Biochem     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1111-8     Citation Subset:  IM    
Affiliation:
Departamento de Bioquimica, Facultad de Medicina, Universidad Nacional Autonoma de Mexico, D.F.
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MeSH Terms
Descriptor/Qualifier:
Animals
Esters / pharmacology
Estradiol / blood,  pharmacology*
Estradiol Congeners / chemical synthesis,  pharmacology*
Female
Follicle Stimulating Hormone / blood
Luteinizing Hormone / blood
Magnetic Resonance Spectroscopy
Ovariectomy
Radioimmunoassay
Rats
Rats, Inbred Strains
Spectrophotometry, Infrared
Spectrophotometry, Ultraviolet
Uterus / drug effects
Vagina / drug effects
Chemical
Reg. No./Substance:
0/Esters; 0/Estradiol Congeners; 50-28-2/Estradiol; 9002-67-9/Luteinizing Hormone; 9002-68-0/Follicle Stimulating Hormone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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