Cargando…
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...
Autores principales: | , , , , , , , , |
---|---|
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 |
_version_ | 1785014026073276416 |
---|---|
author | 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. |
author_facet | 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. |
author_sort | Blokhin, Mikhail E. |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-10047834 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-100478342023-03-29 Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome 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. Curr Issues Mol Biol Article 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. MDPI 2023-03-08 /pmc/articles/PMC10047834/ /pubmed/36975514 http://dx.doi.org/10.3390/cimb45030144 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article 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. Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title | Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title_full | Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title_fullStr | Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title_full_unstemmed | Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title_short | Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome |
title_sort | terpene-containing analogues of glitazars as potential therapeutic agents for metabolic syndrome |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10047834/ https://www.ncbi.nlm.nih.gov/pubmed/36975514 http://dx.doi.org/10.3390/cimb45030144 |
work_keys_str_mv | AT blokhinmikhaile terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT kuranovsergeyo terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT khvostovmikhailv terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT fomenkovladislavv terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT luzinaolgaa terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT zhukovanataliaa terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT elhajjarcham terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT tolstikovatatianag terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome AT salakhutdinovnarimanf terpenecontaininganaloguesofglitazarsaspotentialtherapeuticagentsformetabolicsyndrome |