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Palomares, Belen; Ruiz-Pino, Francisco; Navarrete, Carmen; Velasco, Inmaculada; Sánchez-Garrido, Miguel A.; Jimenez-Jimenez, Carla; Pavicic, Carolina; Vazquez, Maria J.; Appendino, Giovanni; Bellido, M. Luz; Calzado, Marco A.; Tena-Sempere, Manuel; Muñoz, Eduardo

VCE-004.8, A Multitarget Cannabinoquinone, Attenuates Adipogenesis and Prevents Diet-Induced Obesity

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  • Media type: E-Article
  • Title: VCE-004.8, A Multitarget Cannabinoquinone, Attenuates Adipogenesis and Prevents Diet-Induced Obesity
  • Contributor: Palomares, Belen; Ruiz-Pino, Francisco; Navarrete, Carmen; Velasco, Inmaculada; Sánchez-Garrido, Miguel A.; Jimenez-Jimenez, Carla; Pavicic, Carolina; Vazquez, Maria J.; Appendino, Giovanni; Bellido, M. Luz; Calzado, Marco A.; Tena-Sempere, Manuel; Muñoz, Eduardo
  • imprint: Springer Science and Business Media LLC, 2018
  • Published in: Scientific Reports
  • Language: English
  • DOI: 10.1038/s41598-018-34259-0
  • ISSN: 2045-2322
  • Keywords: Multidisciplinary
  • Origination:
  • Footnote:
  • Description: <jats:title>Abstract</jats:title><jats:p>Over the past few years, the endocannabinoid system (ECs) has emerged as a crucial player for the regulation of food intake and energy metabolism, and its pharmacological manipulation represents a novel strategy for the management of metabolic diseases. The discovery that VCE-004.8, a dual PPARγ and CB<jats:sub>2</jats:sub> receptor agonist, also inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway provided a rationale to investigate its effect in <jats:italic>in vitro</jats:italic> models of adipogenesis and in a murine model of metabolic syndrome, all processes critically regulated by these targets of VCE-004.8. In accordance with its different binding mode to PPARγ compared to rosiglitazone (RGZ), VCE-004.8 neither induced adipogenic differentiation, nor affected osteoblastogenesis. Daily administration of VCE-004.8 (20 mg/kg) to HFD mice for 3-wks induced a significant reduction in body weight gain, total fat mass, adipocyte volume and plasma triglycerides levels. VCE-004.8 could also significantly ameliorate glucose tolerance, reduce leptin levels (a marker of adiposity) and increase adiponectin and incretins (GLP-1 and GIP) levels. Remarkably, VCE-004.8 increased the FGF21 mRNA expression in white and brown adipose, as well as in a BAT cell line, qualifying cannabinoaminoquinones as a class of novel therapeutic candidates for the management of obesity and its common metabolic co-morbidities.</jats:p>
  • Access State: Open Access