Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes Obesity

Cathrine Laustrup Møller; Steen B. Pedersen; Bjørn Richelsen; Kilian W. Conde-Frieboes; Kirsten Raun; Kevin L. Grove; Birgitte Schjellerup Wulff

doi:10.1186/s13104-015-1539-4

Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes Obesity

Cathrine Laustrup Møller, Steen B. Pedersen, Bjørn Richelsen, Kilian W. Conde-Frieboes, Kirsten Raun, Kevin L. Grove, Birgitte Schjellerup Wulff

Research output: Contribution to journal › Article › peer-review

18 Scopus citations

Abstract

Background: The central melanocortin system is broadly involved in the regulation of mammalian nutrient utilization. However, the function of melanocortin receptors (MCRs) expressed directly in peripheral metabolic tissues is still unclear. The objective of this study was to investigate the lipolytic capacity of MC1-5R in differentiated adipocytes versus intact white adipose tissue. Results: Non-selective MCR agonist α-MSH, MC5R-selective agonist PG-901 and MC4R-selective agonist LY2112688 significantly stimulated lipolysis in intact white adipose tissue, whereas stimulation of MCRs in differentiated adipocytes failed to do so. The lipolytic response of MC5R was decreased in intact human white adipose tissue when co-treating with β-adrenergic antagonist propranolol, suggesting that the effect may be dependent on neuronal innervation via noradrenalin release. Conclusion: When developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties, effects on lipolysis in white adipose tissue may be physiologically relevant.

Original language	English (US)
Article number	559
Journal	BMC Research Notes
Volume	8
Issue number	1
DOIs	https://doi.org/10.1186/s13104-015-1539-4
State	Published - Oct 12 2015

Keywords

Glycerol
Lipolysis
MC4R
MC5R
Melanocortin receptor
NEFA
Propranolol
White adipose tissue

ASJC Scopus subject areas

General Biochemistry, Genetics and Molecular Biology

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10.1186/s13104-015-1539-4

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title = "Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes Obesity",

abstract = "Background: The central melanocortin system is broadly involved in the regulation of mammalian nutrient utilization. However, the function of melanocortin receptors (MCRs) expressed directly in peripheral metabolic tissues is still unclear. The objective of this study was to investigate the lipolytic capacity of MC1-5R in differentiated adipocytes versus intact white adipose tissue. Results: Non-selective MCR agonist α-MSH, MC5R-selective agonist PG-901 and MC4R-selective agonist LY2112688 significantly stimulated lipolysis in intact white adipose tissue, whereas stimulation of MCRs in differentiated adipocytes failed to do so. The lipolytic response of MC5R was decreased in intact human white adipose tissue when co-treating with β-adrenergic antagonist propranolol, suggesting that the effect may be dependent on neuronal innervation via noradrenalin release. Conclusion: When developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties, effects on lipolysis in white adipose tissue may be physiologically relevant.",

keywords = "Glycerol, Lipolysis, MC4R, MC5R, Melanocortin receptor, NEFA, Propranolol, White adipose tissue",

author = "M{\o}ller, {Cathrine Laustrup} and Pedersen, {Steen B.} and Bj{\o}rn Richelsen and Conde-Frieboes, {Kilian W.} and Kirsten Raun and Grove, {Kevin L.} and Wulff, {Birgitte Schjellerup}",

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doi = "10.1186/s13104-015-1539-4",

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AU - Møller, Cathrine Laustrup

AU - Pedersen, Steen B.

AU - Richelsen, Bjørn

AU - Conde-Frieboes, Kilian W.

AU - Raun, Kirsten

AU - Grove, Kevin L.

AU - Wulff, Birgitte Schjellerup

PY - 2015/10/12

Y1 - 2015/10/12

N2 - Background: The central melanocortin system is broadly involved in the regulation of mammalian nutrient utilization. However, the function of melanocortin receptors (MCRs) expressed directly in peripheral metabolic tissues is still unclear. The objective of this study was to investigate the lipolytic capacity of MC1-5R in differentiated adipocytes versus intact white adipose tissue. Results: Non-selective MCR agonist α-MSH, MC5R-selective agonist PG-901 and MC4R-selective agonist LY2112688 significantly stimulated lipolysis in intact white adipose tissue, whereas stimulation of MCRs in differentiated adipocytes failed to do so. The lipolytic response of MC5R was decreased in intact human white adipose tissue when co-treating with β-adrenergic antagonist propranolol, suggesting that the effect may be dependent on neuronal innervation via noradrenalin release. Conclusion: When developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties, effects on lipolysis in white adipose tissue may be physiologically relevant.

AB - Background: The central melanocortin system is broadly involved in the regulation of mammalian nutrient utilization. However, the function of melanocortin receptors (MCRs) expressed directly in peripheral metabolic tissues is still unclear. The objective of this study was to investigate the lipolytic capacity of MC1-5R in differentiated adipocytes versus intact white adipose tissue. Results: Non-selective MCR agonist α-MSH, MC5R-selective agonist PG-901 and MC4R-selective agonist LY2112688 significantly stimulated lipolysis in intact white adipose tissue, whereas stimulation of MCRs in differentiated adipocytes failed to do so. The lipolytic response of MC5R was decreased in intact human white adipose tissue when co-treating with β-adrenergic antagonist propranolol, suggesting that the effect may be dependent on neuronal innervation via noradrenalin release. Conclusion: When developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties, effects on lipolysis in white adipose tissue may be physiologically relevant.

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KW - Melanocortin receptor

KW - NEFA

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KW - White adipose tissue

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Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes Obesity

Abstract

Keywords

ASJC Scopus subject areas

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