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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Published in:Current issues in molecular biology Vol. 45; no. 3; pp. 2230 - 2247
Main Authors: 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
Format: Journal Article
Language:English
Published: Switzerland MDPI 01-03-2023
MDPI AG
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Summary: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 ) 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.
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ISSN:1467-3045
1467-3037
1467-3045
DOI:10.3390/cimb45030144