Biomaterial Database

Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome. 2023

Mikhail E Blokhin, and Sergey O Kuranov, and Mikhail V Khvostov, and Vladislav V Fomenko, and Olga A Luzina, and Natalia A Zhukova, and Cham Elhajjar, and Tatiana G Tolstikova, and Nariman F Salakhutdinov

N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, 630090 Novosibirsk, Russia.

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/6Ay) 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.