Document Detail


Action profile of the antiobesity drug candidate oleoyl-estrone in rats.
MedLine Citation:
PMID:  20339368     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Oleoyl-estrone (OE) has been presented as a potential antiobesity therapeutic, but the published series of studies from one laboratory has not yet been independently confirmed, and the exact mechanism of action is unknown. Based on the hypothesis that OE has potential for the treatment of obesity, male and female rats were chronically treated with several doses of OE to evaluate the impact of this compound on energy metabolism. Body weight, body composition, energy balance parameters and the expression of hypothalamic neuropeptides regulating food intake as well as key markers of the reproductive system were examined. OE impressively reduced food consumption and body weight gain in both sexes. Although a major part of the loss in body weight could be explained by decreased fat mass, a substantial loss of lean mass also occurred after OE administration. The loss of weight can be sufficiently explained by the suppression of food consumption, as there were no major changes in energy expenditure, locomotor activity or respiratory quotient. In situ hybridization data showed no significant change in the expression of key neuropeptides and hormone receptors regulating feeding behavior after OE treatment. Cocaine-amphetamine-regulated transcript (CART) mRNA levels were decreased in the arcuate nucleus of OE-treated rats. Hypogonadism and low plasma testosterone levels were found in OE-treated males, whereas females showed substantially increased liver size. The present data suggest that OE decreases food intake and body weight but also appears to cause a significant impact on the hypothalamus-pituitary-reproductive axis.
Authors:
Sabine Strassburg; Paul T Pfluger; Nilika Chaudhary; Patrick Tso; Matthias H Tschöp; Stefan D Anker; Ruben Nogueiras; Diego Perez-Tilve
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-03-25
Journal Detail:
Title:  Obesity (Silver Spring, Md.)     Volume:  18     ISSN:  1930-739X     ISO Abbreviation:  Obesity (Silver Spring)     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-24     Completed Date:  2011-06-07     Revised Date:  2012-08-13    
Medline Journal Info:
Nlm Unique ID:  101264860     Medline TA:  Obesity (Silver Spring)     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2260-7     Citation Subset:  IM    
Affiliation:
Obesity Research Center, Department of Internal Medicine, University of Cincinnati-Metabolic Diseases Institute, Cincinnati, Ohio, USA.
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MeSH Terms
Descriptor/Qualifier:
Adipose Tissue / drug effects
Animals
Anti-Obesity Agents / pharmacology*,  therapeutic use
Arcuate Nucleus / drug effects,  metabolism
Body Fluid Compartments / drug effects
Energy Intake / drug effects*
Estrone / analogs & derivatives*,  pharmacology,  therapeutic use
Female
Hypogonadism / chemically induced
Hypothalamo-Hypophyseal System / drug effects
In Situ Hybridization
Liver / drug effects,  pathology
Male
Nerve Tissue Proteins / genetics,  metabolism
Obesity / drug therapy,  metabolism*,  pathology
Oleic Acids / pharmacology*,  therapeutic use
Organ Size / drug effects
Pituitary-Adrenal System / drug effects
RNA, Messenger / metabolism
Rats
Rats, Sprague-Dawley
Sex Factors
Testosterone / blood
Weight Gain / drug effects*
Chemical
Reg. No./Substance:
0/Anti-Obesity Agents; 0/Nerve Tissue Proteins; 0/Oleic Acids; 0/RNA, Messenger; 0/cocaine- and amphetamine-regulated transcript protein; 0/oleoyl-estrone; 53-16-7/Estrone; 58-22-0/Testosterone

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


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