Daily Oral Oleoyl‐Estrone Gavage Induces a Dose‐Dependent Loss of Fat in Wistar Rats

Grasa, Mar; Cabot, Cristina; Esteve, Montserrat; Yubero, Pilar; Masanés, R. M.; Blay, Mayte; Vila, Roser; López-Martí, J; López, José Antonio Fernández; Remesar, Xavier

doi:10.1038/oby.2001.22

Cited by 50 publications

(89 citation statements)

References 19 publications

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“…11 This is accomplished essentially by facilitating the use of fatty acids by the muscle and other peripheral tissues, 13 decreasing the oxidation of glucose and increasing its storage as glycogen, 10 and, at the same time, decreasing insulin resistance. 11,26 Under OE, glucose levels are maintained in spite of a marked decrease of insulin.…”

Section: Discussionmentioning

confidence: 99%

“…A fattening protocol previously published 20 was used; the animals were fed for 5 weeks with a modified cafeteria diet 11,17 (fattening period). Afterwards, they were transferred to wire mesh-bottomed cages and were maintained for 5 days exclusively on a pellet ('maintenance' type, from Panlab, Barcelona, Spain) ad libitum diet (stabilisation period).…”

Section: Methodsmentioning

confidence: 99%

“…The blood was recovered and allowed to clot; the serum was stored at À801C until processed. The stomach and intestinal contents were discarded; the rat remains were autoclaved, homogenised and used for the estimation of water, protein, lipid and energy content as previously described: 11 water was estimated by differential weighing before and after desiccation at 1101C; protein was estimated from the N content (Kjeldahl, using the 1007 Digestor and 1002 Distilling Unit, both from a Tecator Kjeltec System, Höganäs, Sweden) and conversion of N content into protein equivalence; 21 lipid by trichloromethane: methanol extraction; 22 and energy using a bomb calorimeter (C-7000 Ika, Heitersheim, Germany). The final body composition was determined from the percentages of body components measured experimentally and the estimated 'in vivo' net body weight.…”

Section: Methodsmentioning

confidence: 99%

“…6 The oral administration of OE to lean, genetically obese or dietary-obese rodents induces a marked loss of body fat, 7,8 primarily due to a decrease in voluntary food intake coupled with the maintenance of energy expenditure. 9 Glucose levels are maintained in spite of marked decreases in insulin and leptin, 10 a consequence of OE-elicited increase in insulin sensitivity/decrease in insulin resistance, 11 which results in the maintenance of liver glycogen stores regardless of the severe drainage of body energy. 10 Lipid mobilisation, however, does not massively increase circulating lipids, since lipid oxidation is also increased as shown by the lowering of the respiratory quotient, 5 and marked decrease in cholesterol levels 12 coupled with enhanced muscle lipoprotein lipase activity.…”

Section: Introductionmentioning

confidence: 99%

“…hunger pangs, hypoglycaemia), to enhance energy expenditure to speed up the process of fat disposal, or to maintain the weight loss during and after treatment. 16 OE has been used, so far without association to limited food intake, both in rodents and humans, [17][18][19] since OE limits food intake by itself, and prevents the fall in energy expenditure 5,11 that accompanies food deprivation. 4 In the present study, we have explored the combined effects of severely limited food intake and OE treatment, in order to determine whether hypocaloric diets enhance the slimming effects of OE on mature overweight male rats.…”

Section: Introductionmentioning

confidence: 99%

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Combined effects of oral oleoyl-estrone and limited food intake on body composition of young overweight male rats

2006

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Objective: The combined effects of limited food intake and OE treatment have been analysed in order to determine whether hypocaloric diets enhance the slimming effects of OE on mature overweight male rats. Two levels of dietary limitation at 50 and 25% of a standard intake were established, roughly corresponding to the human LCDs and VLCDs. Design: Wistar male rats (6 weeks old) were made overweight by a cafeteria diet. After transition to standard diet, they were subjected to food restriction: down to 50 or 25% with respect to the transition period. Half the animals were given daily oral gavages of 10 nmol/g oleoyl-estrone (OE), and the rest received only the vehicle during 10 days. Measurements: Changes in weight and body composition: water, lipid, protein or gross energy were determined by comparing the final pool size with that of day 0, calculated from the initial body weight and the composition of untreated rats. Energy and nitrogen balances were estimated. Plasma levels of metabolites and hormones were also measured. Results: OE induced changes in body composition similar to those elicited by a 50% reduction in food, with massive loss of lipid and energy. OE-treated rats ate less than the controls, but additional effects on body composition on reduced diet were minimal. OE improved metabolic homoeostasis: better maintained glycaemia, lower cholesterol and shallower hormonal changes, but at the expense of slightly increased protein mobilisation. Conclusions: The data presented suggest that no advantages are accomplished by combining OE treatment and hypocaloric diets compared with OE alone, at least under the experimental conditions tested, since the effects were not additive. Despite OE affecting food intake, mechanisms other than that are deemed responsible for the mobilisation of body fat, since intake alone cannot explain the effects on body weight, nor the metabolic and hormonal changes in OE-treated rats. It is concluded that the combination of food restriction and OE may result in unwanted increased protein mobilisation with no synergy between both slimming treatments.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Combined effects of oral oleoyl-estrone and limited food intake on body composition of young overweight male rats

2006

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Oleoyl‐Estrone

Remesar

Fernández-López

Alemany

2011

Medicinal Research Reviews

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Oleoyl-estrone (OE) is a powerful slimming agent that is also present in plasma and adipose tissue, where it is synthesized. It acts through the formation of a derivative W. OE effects (and W levels) are proportional to the dose. OE reduces food intake but maintains energy expenditure (thermogenesis). The energy gap is fulfilled with adipose tissue fat, sparing body protein and maintaining glycemia (and glycogen) with lower insulin and leptin levels. OE (in fact W) acts through specific receptors, different from those of estrogen. OE increases cholesterol catabolism, reducing hypercholesterolemia in obese rats. The main metabolic effect on adipose tissue is lowering of lipid synthesis, maintaining unchanged the intracellular lipolytic processes; the imbalance favors the progressive loss of fat, which is largely used by the muscle. OE administration induces additive effects with other antiobesity agents, such as β(3)-adrenergic agonists, forcing a massive loss of lipid. Corticosteroids markedly limit OE action by altering the liver control of lipogenesis. OE also inhibits the action of 17β-hydroxysteroid dehydrogenase, decreasing the synthesis of β-estradiol and testosterone. Discontinuous treatment allows for maximal efficacy both in rats and humans. OE has the advantage that the loss of fat is maintained and does not require additional dietary limitations.

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Intestinal oleoyl-estrone esterase activity in the Wistar rat

Serrano-Muñoz

Grasa

Gonzalez-Martinez

et al. 2008

J Endocrinol Invest

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Low-dose oral oleoyl-estrone (OE) (i.e. in dairy products) is hydrolysed to estrone, which promotes growth and fat deposition. However, pharmacological doses of OE are absorbed largely intact and elicit fat losses. Thus, in order to find out how the intestine handles OE, esterase activity (at pH 5, 7 or 8) was measured in rat stomach, duodenum, jejunum, ileum, cecum, large intestine, and liver using OE as substrate. There were no sex-related differences. Pure pancreatic cholesterol-ester esterase hydrolysed OE even in the absence of taurocholate. The differences in the pH-related activity distribution pattern and selective inhibition and taurocholate dependence show that, in addition to the luminal (i.e. pancreatic) cholesterol-ester esterase, other esterases hydrolyse OE; these combined activities may be sufficient to rapidly dispose of pharmacological doses of OE. Female rats received a tritium-labeled OE gavage; the luminal and tissue label content were measured up to 24 h. The high retention of label in the stomach suggest that this may be a significant site of absorption. The rapid decrease of label in intestinal lumen (and rat tissues) shortly after the administration, hint at rapid absorption and disposal. In conclusion, the high OE-esterase activity and early absorption of OE are indicative of upper gastro-intestinal tract absorption skipping most of the medium-tract esterases.

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Daily Oral Oleoyl‐Estrone Gavage Induces a Dose‐Dependent Loss of Fat in Wistar Rats

Abstract: Oral treatment with oleoyl-estrone resulted in the specific dose-related loss of fat reserves with little change to other metabolic parameters. These results agree with the postulated role of oleoyl-estrone as a ponderostat signal.

Cited by 50 publications

References 19 publications

Combined effects of oral oleoyl-estrone and limited food intake on body composition of young overweight male rats

Combined effects of oral oleoyl-estrone and limited food intake on body composition of young overweight male rats

Oleoyl‐Estrone

Intestinal oleoyl-estrone esterase activity in the Wistar rat

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