Growth hormone secretagogue receptor antagonists

Costantino, Luca

doi:10.1517/13543776.2012.684946

Cited by 4 publications

(1 citation statement)

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“…The ghrelinergic system represents a promising pharmacologic target for the treatment of obesity and obesity-related diseases. Indeed, several studies have shown that inhibition of the ghrelin signalling pathway results in a reduction of food intake through decreased appetite and increased energy expenditure and fat catabolism, underlining the potential of ghrelin receptor antagonists, inverse agonist and other strategies targeting the ghrelin hormone in the development of anti-obesity therapeutics (for review see[7], [11]–[15]). …”

Section: Introductionmentioning

confidence: 99%

Devil's Claw to Suppress Appetite—Ghrelin Receptor Modulation Potential of a Harpagophytum procumbens Root Extract

et al. 2014

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Ghrelin is a stomach-derived peptide that has been identified as the only circulating hunger hormone that exerts a potent orexigenic effect via activation of its receptor, the growth hormone secretagogue receptor (GHS-R1a). Hence, the ghrelinergic system represents a promising target to treat obesity and obesity-related diseases. In this study we analysed the GHS-R1a receptor activating potential of Harpagophytum procumbens, popularly known as Devil's Claw, and its effect on food intake in vivo. H. procumbens is an important traditional medicinal plant from Southern Africa with potent anti-inflammatory and analgesic effects. This plant has been also used as an appetite modulator but most evidences are anecdotal and to our knowledge, no clear scientific studies relating to appetite modulation have been done to this date. The ghrelin receptor activation potential of an extract derived from the dried tuberous roots of H. procumbens was analysed by calcium mobilization and receptor internalization assays in human embryonic kidney cells (Hek) stably expressing the GHS-R1a receptor. Food intake was investigated in male C57BL/6 mice following intraperitoneal administration of H. procumbens root extract in ad libitum and food restricted conditions. Exposure to H. procumbens extract demonstrated a significant increased cellular calcium influx but did not induce subsequent GHS-R1a receptor internalization, which is a characteristic for full receptor activation. A significant anorexigenic effect was observed in male C57BL/6 mice following peripheral administration of H. procumbens extract. We conclude that H. procumbens root extract is a potential novel source for potent anti-obesity bioactives. These results reinforce the promising potential of natural bioactives to be developed into functional foods with weight-loss and weight maintenance benefits.

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Section: Introductionmentioning

confidence: 99%