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Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review
Agonists of the nuclear receptor PPARγ are therapeutically used to combat hyperglycaemia associated with the metabolic syndrome and type 2 diabetes. In spite of being effective in normalization of blood glucose levels, the currently used PPARγ agonists from the thiazolidinedione type have serious si...
Autores principales: | , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier Science
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4212005/ https://www.ncbi.nlm.nih.gov/pubmed/25083916 http://dx.doi.org/10.1016/j.bcp.2014.07.018 |
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author | Wang, Limei Waltenberger, Birgit Pferschy-Wenzig, Eva-Maria Blunder, Martina Liu, Xin Malainer, Clemens Blazevic, Tina Schwaiger, Stefan Rollinger, Judith M. Heiss, Elke H. Schuster, Daniela Kopp, Brigitte Bauer, Rudolf Stuppner, Hermann Dirsch, Verena M. Atanasov, Atanas G. |
author_facet | Wang, Limei Waltenberger, Birgit Pferschy-Wenzig, Eva-Maria Blunder, Martina Liu, Xin Malainer, Clemens Blazevic, Tina Schwaiger, Stefan Rollinger, Judith M. Heiss, Elke H. Schuster, Daniela Kopp, Brigitte Bauer, Rudolf Stuppner, Hermann Dirsch, Verena M. Atanasov, Atanas G. |
author_sort | Wang, Limei |
collection | PubMed |
description | Agonists of the nuclear receptor PPARγ are therapeutically used to combat hyperglycaemia associated with the metabolic syndrome and type 2 diabetes. In spite of being effective in normalization of blood glucose levels, the currently used PPARγ agonists from the thiazolidinedione type have serious side effects, making the discovery of novel ligands highly relevant. Natural products have proven historically to be a promising pool of structures for drug discovery, and a significant research effort has recently been undertaken to explore the PPARγ-activating potential of a wide range of natural products originating from traditionally used medicinal plants or dietary sources. The majority of identified compounds are selective PPARγ modulators (SPPARMs), transactivating the expression of PPARγ-dependent reporter genes as partial agonists. Those natural PPARγ ligands have different binding modes to the receptor in comparison to the full thiazolidinedione agonists, and on some occasions activate in addition PPARα (e.g. genistein, biochanin A, sargaquinoic acid, sargahydroquinoic acid, resveratrol, amorphastilbol) or the PPARγ-dimer partner retinoid X receptor (RXR; e.g. the neolignans magnolol and honokiol). A number of in vivo studies suggest that some of the natural product activators of PPARγ (e.g. honokiol, amorfrutin 1, amorfrutin B, amorphastilbol) improve metabolic parameters in diabetic animal models, partly with reduced side effects in comparison to full thiazolidinedione agonists. The bioactivity pattern as well as the dietary use of several of the identified active compounds and plant extracts warrants future research regarding their therapeutic potential and the possibility to modulate PPARγ activation by dietary interventions or food supplements. |
format | Online Article Text |
id | pubmed-4212005 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Elsevier Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-42120052014-11-06 Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review Wang, Limei Waltenberger, Birgit Pferschy-Wenzig, Eva-Maria Blunder, Martina Liu, Xin Malainer, Clemens Blazevic, Tina Schwaiger, Stefan Rollinger, Judith M. Heiss, Elke H. Schuster, Daniela Kopp, Brigitte Bauer, Rudolf Stuppner, Hermann Dirsch, Verena M. Atanasov, Atanas G. Biochem Pharmacol Part of the Special Issue: Metabolism 2014 – Alterations of metabolic pathways as therapeutic targets Agonists of the nuclear receptor PPARγ are therapeutically used to combat hyperglycaemia associated with the metabolic syndrome and type 2 diabetes. In spite of being effective in normalization of blood glucose levels, the currently used PPARγ agonists from the thiazolidinedione type have serious side effects, making the discovery of novel ligands highly relevant. Natural products have proven historically to be a promising pool of structures for drug discovery, and a significant research effort has recently been undertaken to explore the PPARγ-activating potential of a wide range of natural products originating from traditionally used medicinal plants or dietary sources. The majority of identified compounds are selective PPARγ modulators (SPPARMs), transactivating the expression of PPARγ-dependent reporter genes as partial agonists. Those natural PPARγ ligands have different binding modes to the receptor in comparison to the full thiazolidinedione agonists, and on some occasions activate in addition PPARα (e.g. genistein, biochanin A, sargaquinoic acid, sargahydroquinoic acid, resveratrol, amorphastilbol) or the PPARγ-dimer partner retinoid X receptor (RXR; e.g. the neolignans magnolol and honokiol). A number of in vivo studies suggest that some of the natural product activators of PPARγ (e.g. honokiol, amorfrutin 1, amorfrutin B, amorphastilbol) improve metabolic parameters in diabetic animal models, partly with reduced side effects in comparison to full thiazolidinedione agonists. The bioactivity pattern as well as the dietary use of several of the identified active compounds and plant extracts warrants future research regarding their therapeutic potential and the possibility to modulate PPARγ activation by dietary interventions or food supplements. Elsevier Science 2014-11-01 /pmc/articles/PMC4212005/ /pubmed/25083916 http://dx.doi.org/10.1016/j.bcp.2014.07.018 Text en © 2014 The Authors https://creativecommons.org/licenses/by/3.0/This work is licensed under a Creative Commons Attribution 3.0 Unported License (https://creativecommons.org/licenses/by/3.0/) . |
spellingShingle | Part of the Special Issue: Metabolism 2014 – Alterations of metabolic pathways as therapeutic targets Wang, Limei Waltenberger, Birgit Pferschy-Wenzig, Eva-Maria Blunder, Martina Liu, Xin Malainer, Clemens Blazevic, Tina Schwaiger, Stefan Rollinger, Judith M. Heiss, Elke H. Schuster, Daniela Kopp, Brigitte Bauer, Rudolf Stuppner, Hermann Dirsch, Verena M. Atanasov, Atanas G. Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title | Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title_full | Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title_fullStr | Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title_full_unstemmed | Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title_short | Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review |
title_sort | natural product agonists of peroxisome proliferator-activated receptor gamma (pparγ): a review |
topic | Part of the Special Issue: Metabolism 2014 – Alterations of metabolic pathways as therapeutic targets |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4212005/ https://www.ncbi.nlm.nih.gov/pubmed/25083916 http://dx.doi.org/10.1016/j.bcp.2014.07.018 |
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