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Obestatin is an amidated peptide of 23 amino-acids with an alpha-helical secondary conformation. It was first isolated from rat stomach in 2005. Obestatin is a preproghrelin-derived peptide produced by many tissues or organs, including the stomach, pancreas, adipose tissue, skeletal muscle, and heart. Obestatin was originally identified as an anorexigenic peptide that reduces food intake and body weight by opposing the actions of ghrelin. It has also been considered to be an antidiabetic peptide that positively influences glucose and lipid metabolism. It may also play a role in the regulation of blood pressure as its plasma concentration increases in hypertensive patients. Obestatin may also have a role in the regulation of anxiety and memory improvement.
Obestatin is a 23-amino acid C-terminally amidated gastrointestinal peptide derived from preproghrelin and which forms an α helix. Although obestatin has a short biological half-life and is rapidly degraded, it is proposed to exert wide-ranging pathophysiological actions. Whilst the precise nature of many of its effects is unclear, accumulating evidence supports positive actions on both metabolism and cardiovascular function. For example, obestatin has been reported to inhibit food and water intake, body weight gain and gastrointestinal motility and also to mediate promotion of cell survival and prevention of apoptosis. Obestatin-induced increases in beta cell mass, enhanced adipogenesis and improved lipid metabolism have been noted along with up-regulation of genes associated with beta cell regeneration, insulin production and adipogenesis. Furthermore, human circulating obestatin levels generally demonstrate an inverse association with obesity and diabetes, whilst the peptide has been shown to confer protective metabolic effects in experimental diabetes, suggesting that it may hold therapeutic potential in this setting. Obestatin also appears to be involved in blood pressure regulation and to exert beneficial effects on endothelial function, with experimental studies indicating that it may also promote cardioprotective actions against, for example, ischaemia-reperfusion injury. This review will present a critical appraisal of the expanding obestatin research area and discuss the emerging therapeutic potential of this peptide for both metabolic and cardiovascular complications of diabetes.
Cowan, E., Burch, K. J., Green, B. D., & Grieve, D. J. (2016). Obestatin as a key regulator of metabolism and cardiovascular function with emerging therapeutic potential for diabetes. British journal of pharmacology, 173(14), 2165-2181.
The high prevalence of obesity and diabetes will lead to higher rates of morbidity and mortality. It is well known that ghrelin plays a potential role in obesity and diabetes. Obestatin, a novel 23 amino acid amidated peptide encoded by the same gene that encodes ghrelin, was initially reported to have opposite actions to ghrelin in the regulation of food intake, emptying of the stomach and body weight. Recent work suggests that obestatin also regulate beta-cell survival and insulin secretion. The ghrelin-obestatin system is, therefore, a promising target for the developing of new drugs for the treatment of obesity and diabetes. This review summarizes the interrelationship between obestatin, obesity and diabetes.
Ren, A. J., Guo, Z. F., Wang, Y. K., Lin, L., Zheng, X., & Yuan, W. J. (2009). Obestatin, obesity and diabetes. Peptides, 30(2), 439-444.