The Metabolic Efficacy of a Cannabidiolic Acid (CBDA) Derivative in Treating Diet- and Genetic-Induced Obesity.
CBDA
Magel2
PWS
dyslipidemia
hepatic steatosis
hyperphagia
obesity
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
17 May 2022
17 May 2022
Historique:
received:
29
04
2022
revised:
15
05
2022
accepted:
16
05
2022
entrez:
28
5
2022
pubmed:
29
5
2022
medline:
1
6
2022
Statut:
epublish
Résumé
Obesity is a global medical problem; its common form is known as diet-induced obesity (DIO); however, there are several rare genetic disorders, such as Prader-Willi syndrome (PWS), that are also associated with obesity (genetic-induced obesity, GIO). The currently available therapeutics for treating DIO and GIO are very limited, and they result in only a partial improvement. Cannabidiolic acid (CBDA), a constituent of Cannabis sativa, gradually decarboxylates to cannabidiol (CBD). Whereas the anti-obesity properties of CBD have been reasonably identified, our knowledge of the pharmacology of CBDA is more limited due to its instability. To stabilize CBDA, a new derivative, CBDA-O-methyl ester (HU-580, EPM301), was synthesized. The therapeutic potential of EPM301 in appetite reduction, weight loss, and metabolic improvements in DIO and GIO was tested in vivo. EPM301 (40 mg/kg/d, i.p.) successfully resulted in weight loss, increased ambulation, as well as improved glycemic and lipid profiles in DIO mice. Additionally, EPM301 ameliorated DIO-induced hepatic dysfunction and steatosis. Importantly, EPM301 (20 and 40 mg/kg/d, i.p.) effectively reduced body weight and hyperphagia in a high-fat diet-fed
Identifiants
pubmed: 35628417
pii: ijms23105610
doi: 10.3390/ijms23105610
pmc: PMC9144717
pii:
doi:
Substances chimiques
Antigens, Neoplasm
0
Cannabinoids
0
Magel2 protein, mouse
0
Proteins
0
cannabidiolic acid
FJX8O3OJCD
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : EPM Group
ID : N/A
Références
Br J Pharmacol. 2018 Jan;175(1):100-112
pubmed: 29057454
Nutr Res Rev. 2010 Dec;23(2):270-99
pubmed: 20977819
Hum Mol Genet. 2016 Sep 1;25(17):3798-3809
pubmed: 27436578
Br J Pharmacol. 2007 Dec;152(7):1092-101
pubmed: 17876302
Braz J Psychiatry. 2019 Jan-Mar;41(1):9-14
pubmed: 30328956
Neurosci Lett. 2011 Feb 18;490(1):82-4
pubmed: 21172406
Lancet Neurol. 2016 Mar;15(3):270-8
pubmed: 26724101
Biochimie. 2019 Jun;161:34-45
pubmed: 31079617
Genet Med. 2012 Jan;14(1):10-26
pubmed: 22237428
J Endocrinol Invest. 2015 Dec;38(12):1249-63
pubmed: 26062517
Pharmacol Biochem Behav. 2011 Apr;98(2):268-72
pubmed: 21238476
Arterioscler Thromb Vasc Biol. 2009 Mar;29(3):416-23
pubmed: 19112166
Hum Mol Genet. 2007 Nov 15;16(22):2713-9
pubmed: 17728320
Obes Rev. 2021 Jul;22(7):e13210
pubmed: 33559362
Curr Hypertens Rep. 2018 Feb 26;20(2):12
pubmed: 29480368
Nat Methods. 2011 Dec 28;9(1):57-63
pubmed: 22205519
PLoS One. 2015 Dec 03;10(12):e0144270
pubmed: 26633823
Arch Gen Psychiatry. 2010 Mar;67(3):220-9
pubmed: 20194822
Phytomedicine. 2009 Oct;16(10):942-9
pubmed: 19345076
Obes Facts. 2016;9(3):158-73
pubmed: 27241181
Mol Cell Biochem. 2016 May;416(1-2):131-9
pubmed: 27067870
Mol Metab. 2016 Oct 22;5(12):1187-1199
pubmed: 27900261
Tetrahedron. 1965 May;21(5):1223-9
pubmed: 5879350
Behav Brain Res. 2018 Oct 1;351:1-3
pubmed: 29860002
Mol Metab. 2017 Oct;6(10):1113-1125
pubmed: 29031713
BMC Med. 2020 Jul 24;18(1):227
pubmed: 32703266
Obes Surg. 2019 Jan;29(1):268-276
pubmed: 30244333
Cell Metab. 2012 Aug 8;16(2):167-79
pubmed: 22841573
Clin Exp Pharmacol Physiol. 2021 Dec;48(12):1579-1588
pubmed: 34314523
Rev Paul Pediatr. 2018 Jul-Sep;36(3):345-352
pubmed: 30365815
Neurochem Res. 2005 Aug;30(8):1037-43
pubmed: 16258853
Br J Pharmacol. 2015 Oct;172(20):4790-805
pubmed: 26218440
Methods Find Exp Clin Pharmacol. 2007 May;29(4):269-72
pubmed: 17609739
Antioxidants (Basel). 2019 Dec 25;9(1):
pubmed: 31881765
Diabetes Metab Res Rev. 2021 Nov;37(8):e3458
pubmed: 33891377
Yale J Biol Med. 2012 Mar;85(1):19-28
pubmed: 22461740
Br J Pharmacol. 2010 Aug;160(7):1577-9
pubmed: 20649561
Am J Med Genet C Semin Med Genet. 2010 Aug 15;154C(3):365-76
pubmed: 20803659
Mol Psychiatry. 2019 Jan;24(1):18-33
pubmed: 29453413
ACS Chem Neurosci. 2015 Jul 15;6(7):1176-85
pubmed: 25781502
Am J Med Genet B Neuropsychiatr Genet. 2009 Dec 5;150B(8):1085-99
pubmed: 19199291
Curr Obes Rep. 2020 Sep;9(3):380-389
pubmed: 32607822
Chem Biol Interact. 2019 Oct 1;312:108819
pubmed: 31499052
Adv Exp Med Biol. 2017;960:1-17
pubmed: 28585193
Curr Opin Lipidol. 2014 Oct;25(5):387-93
pubmed: 25110901
Med Clin North Am. 2018 Jan;102(1):13-33
pubmed: 29156181
Mol Ther Methods Clin Dev. 2019 Mar 14;13:344-358
pubmed: 30989085
Eur J Endocrinol. 2017 Jun;176(6):R309-R324
pubmed: 28246151
Front Endocrinol (Lausanne). 2020 Mar 04;11:114
pubmed: 32194509