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Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome

Metabolic syndrome is a complex of abnormalities involving impaired glucose and lipid metabolism, which needs effective pharmacotherapy. One way to reduce lipid and glucose levels associated with this pathology is the simultaneous activation of nuclear PPAR-alpha and gamma. For this purpose, we synt...

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Detalles Bibliográficos
Autores principales: Blokhin, Mikhail E., Kuranov, Sergey O., Khvostov, Mikhail V., Fomenko, Vladislav V., Luzina, Olga A., Zhukova, Natalia A., Elhajjar, Cham, Tolstikova, Tatiana G., Salakhutdinov, Nariman F.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10047834/
https://www.ncbi.nlm.nih.gov/pubmed/36975514
http://dx.doi.org/10.3390/cimb45030144
Descripción
Sumario:Metabolic syndrome is a complex of abnormalities involving impaired glucose and lipid metabolism, which needs effective pharmacotherapy. One way to reduce lipid and glucose levels associated with this pathology is the simultaneous activation of nuclear PPAR-alpha and gamma. For this purpose, we synthesized a number of potential agonists based on the pharmacophore fragment of glitazars with the inclusion of mono- or diterpenic moiety in the molecular structure. The study of their pharmacological activity in mice with obesity and type 2 diabetes mellitus (C57Bl/6(Ay)) revealed one substance that was capable of reducing the triglyceride levels in the liver and adipose tissue of mice by enhancing their catabolism and expressing a hypoglycemic effect connected with the sensitization of mice tissue to insulin. It has also been shown to have no toxic effects on the liver.