Effects of oleoyl-estrone with dexfenfluramine, sibutramine or phentermine on overweight rats

Ferrer-Lorente, Raquel; Cabot, Cristina; Fernández-López, José Antonio; Remesar, Xavier; Alemany, M

doi:10.1016/j.ejphar.2005.02.044

Cited by 16 publications

(18 citation statements)

References 28 publications

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“…OE effects on weight, energy, lipid, and protein were similar to the previously reported ones (4,9,21,22). Rimonabant effects and its rapid effect on appetite agree with previous studies (11).…”

Section: Discussionsupporting

confidence: 81%

“…Rats were maintained under standard housing conditions in two-rat cages, and they were fed for five weeks a reduced cafeteria diet (21,22) ad libitum. At the end of this phase, the animals were already overweight, that is, weighed 26% more than the same-age controls.…”

Section: Methodsmentioning

confidence: 99%

“…The combination of drugs for the treatment of obesity has been a widely extended practice in the past, in part because of the slow pace of weight loss and the usually limited overall effect, in spite of insufficient prior testing, with dramatically deleterious effects in some cases (18 -20). OE has been found to produce in rats a synergic boosting of body fat loss both with a β 3 -adrenergic agent (21) and a serotoninergic drug, sibutramine (22), indicating that its mechanism of action was complementary of both thermogenesis and inhibition of appetite by enhancement of postsynaptic serotonin activity. Combination of OE and dietary restriction, however, showed no improvement over the administration of OE alone in the handling of body fat, but OE markedly improved the body metabolic and hormonal environment when compared with restricted diet alone (9).…”

Section: Introductionmentioning

confidence: 99%

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Effects of Combined Oleoyl-Estrone and Rimonabant on Overweight Rats

2007

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Abstract. Oleoyl-estrone (OE) decreases appetite, maintains energy expediture, induces lipolysis (sparing protein), and decreases cholesterolemia and insulin resistance. Rimonabant (SR141716) is a cannabinoid-receptor inhibitor that decreases appetite and mobilizes fat. We studied whether their combination improves their slimming effects. Male overweight rats received daily gavages of 5.3 mg / kg OE, 10 mg/ kg rimonabant, or both drugs during 10 days. Body weight and composition, energy balance, adipose tissue weight, and serum hormones and metabolites were measured. OE halved food intake and maintained energy expenditure at the expense of body fat. Rimonabant effects on appetite and energy balance were less marked, resulting in lower lipid mobilization. OE and rimonabant followed the OE pattern, with no additive or synergic effects. Glycemia was maintained, but OE decreased insulin, GLP-1, and cholesterol, whilst rimonabant increased cholecystokinin and cholesterol, and decreased NEFA. Both drugs decreased leptin and triacylglycerols; ghrelin was unchanged. The results hint at different mechanisms of action of both drugs: we can assume that OE effects do not involve the cannabinoid pathway. OE does not seem to act, either, after 10 days, through the secretion of ghrelin or the intestinal appetite-controlling peptides tested.

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Section: Discussionsupporting

confidence: 81%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Effects of Combined Oleoyl-Estrone and Rimonabant on Overweight Rats

2007

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“…3,9 Although phentermine (0-5 mg kg À1 ) has been shown to decrease acute food intake in various rodent models following a single injection, the present findings are consistent with other reports showing little (o3%) or no change in body weight with sustained administration of phentermine (5 mg kg À1 d À1 , i.p. injection in lean rats; 37 5 mg kg À1 d À1 by oral gavage; 14 5 mg kg À1 d À1 by osmotic mini-pump). 20 Interestingly, several doses of phentermine that were not effective as a monotherapy (2.5 and 5.0 mg kg À1 d À1 ) augmented amylin's anorexigenic effects, inducing up to a 30% reduction in food intake.…”

Section: Discussionmentioning

confidence: 99%

“…Rodent models suggest that phentermine causes weight loss via effects on caloric intake and metabolic rate. 14 Sibutramine inhibits the reuptake of central noradrenaline and serotonin and stimulates thermogenesis in rodents. 15,16 Depending upon the trial design, clinical studies have revealed that both agents elicit statistically significant weight loss ranging from 4-8% (placebo-corrected).…”

Section: Introductionmentioning

confidence: 99%

Antiobesity effects of the β-cell hormone amylin in combination with phentermine or sibutramine in diet-induced obese rats

Roth¹,

Trevaskis²,

Wilson³

et al. 2008

Int J Obes

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Objective: To characterize the interactive effects of amylin with phentermine or sibutramine on food intake, body weight/ composition and gene expression in diet-induced obese (DIO) rats. Design: DIO rats were intraperitoneally injected with a single dose of amylin (10 mg kg À1 ) and/or phentermine (1 mg kg À1 ) or chronically infused with amylin (100 mg kg À1 d À1 ) or vehicle with or without phentermine (0.5-10 mg kg À1 d À1 ) or sibutramine (3 mg kg À1 d À1 ) using two surgically implanted subcutaneous osmotic mini-pumps. Measurements: Twenty-four hour food intake, locomotor activity and components of meal microstructure (meal size, latency, duration and intermeal interval) were measured following acute administration (amylin, phentermine or amylin þ phentermine). Body weight and composition (for amylin and/or sibutramine or phentermine) and metabolism-related gene mRNA expression in the liver (fatty acid synthase, stearoyl-CoA desaturase-1 and carnitine palmitoyltransferase-1) and brown fat (b-adrenergic receptors and uncoupling protein-1) were measured (for amylin and/or phentermine) after sustained infusion (2 weeks). Results: Acute co-administration of amylin (10 mg kg À1 ) and phentermine (1 mg kg À1 ) reduced acute food intake (up to 19 h) more than either monotherapy. In two studies, sustained subcutaneous infusion of amylin for 2 weeks decreased cumulative food intake (22%) and vehicle-corrected body weight gain (B4-8%). Phentermine's anorexigenic (10-17%) and weightreducing effects (B0-5%) were only evident at the highest dose tested (10 mg kg À1 d À1 ). Combination of amylin (100 mg kg À1 d À1 ) and phentermine reduced food intake (30-43%), body weight (8-12%) and adiposity to a greater extent than either monotherapy. Amylin prevented phentermine-induced reductions in UCP-1 mRNA in brown adipose tissue. When amylin þ sibutramine were infused, mathematically additive decreases in food intake (up to 45%) and body weight (up to 12%) were evident. Similar to amylin þ phentermine treatment, amylin þ sibutramine mediated weight loss was attributable to significant reductions in fat mass. Conclusions: Combined treatment of DIO rats with the pancreatic b-cell hormone amylin and phentermine or sibutramine resulted in additive anorexigenic, weight-and fat-reducing effects.

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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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Effects of oleoyl-estrone with dexfenfluramine, sibutramine or phentermine on overweight rats

Cited by 16 publications

References 28 publications

Effects of Combined Oleoyl-Estrone and Rimonabant on Overweight Rats

Effects of Combined Oleoyl-Estrone and Rimonabant on Overweight Rats

Antiobesity effects of the β-cell hormone amylin in combination with phentermine or sibutramine in diet-induced obese rats

Oleoyl‐Estrone

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