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Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder
We synthesized twenty thiazolidin-4-one derivatives, which were then characterized by standard chromatographic and spectroscopic methods. From the in vitro glucose uptake assay, two compounds behaved as insulin sensitizers, where they enhanced glucose uptake in isolated rat diaphragm. In high-carboh...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Hindawi Publishing Corporation
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4065710/ https://www.ncbi.nlm.nih.gov/pubmed/24995315 http://dx.doi.org/10.1155/2014/620434 |
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author | Gowdra, Vasantharaju S. Mudgal, Jayesh Bansal, Punit Nayak, Pawan G. Manohara Reddy, Seethappa A. Shenoy, Gautham G. Valiathan, Manna Chamallamudi, Mallikarjuna R. Nampurath, Gopalan K. |
author_facet | Gowdra, Vasantharaju S. Mudgal, Jayesh Bansal, Punit Nayak, Pawan G. Manohara Reddy, Seethappa A. Shenoy, Gautham G. Valiathan, Manna Chamallamudi, Mallikarjuna R. Nampurath, Gopalan K. |
author_sort | Gowdra, Vasantharaju S. |
collection | PubMed |
description | We synthesized twenty thiazolidin-4-one derivatives, which were then characterized by standard chromatographic and spectroscopic methods. From the in vitro glucose uptake assay, two compounds behaved as insulin sensitizers, where they enhanced glucose uptake in isolated rat diaphragm. In high-carbohydrate diet-induced insulin resistant mice, these two thiazolidin-4-ones attenuated hyperglycemia, hyperinsulinemia, hypertriglyceridemia, hypercholesterolemia, and glucose intolerance. They raised the plasma leptin but did not reverse the diabetes-induced hypoadiponectinemia. Additionally, compound 3a reduced adiposity. The test compounds were also able to reverse the disturbed liver antioxidant milieu. To conclude, these two novel thiazolidin-4-ones modulated multiple mechanisms involved in metabolic disorders, reversing insulin resistance and thus preventing the development of type-2 diabetes. |
format | Online Article Text |
id | pubmed-4065710 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Hindawi Publishing Corporation |
record_format | MEDLINE/PubMed |
spelling | pubmed-40657102014-07-03 Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder Gowdra, Vasantharaju S. Mudgal, Jayesh Bansal, Punit Nayak, Pawan G. Manohara Reddy, Seethappa A. Shenoy, Gautham G. Valiathan, Manna Chamallamudi, Mallikarjuna R. Nampurath, Gopalan K. Biomed Res Int Research Article We synthesized twenty thiazolidin-4-one derivatives, which were then characterized by standard chromatographic and spectroscopic methods. From the in vitro glucose uptake assay, two compounds behaved as insulin sensitizers, where they enhanced glucose uptake in isolated rat diaphragm. In high-carbohydrate diet-induced insulin resistant mice, these two thiazolidin-4-ones attenuated hyperglycemia, hyperinsulinemia, hypertriglyceridemia, hypercholesterolemia, and glucose intolerance. They raised the plasma leptin but did not reverse the diabetes-induced hypoadiponectinemia. Additionally, compound 3a reduced adiposity. The test compounds were also able to reverse the disturbed liver antioxidant milieu. To conclude, these two novel thiazolidin-4-ones modulated multiple mechanisms involved in metabolic disorders, reversing insulin resistance and thus preventing the development of type-2 diabetes. Hindawi Publishing Corporation 2014 2014-06-03 /pmc/articles/PMC4065710/ /pubmed/24995315 http://dx.doi.org/10.1155/2014/620434 Text en Copyright © 2014 Vasantharaju S. Gowdra et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Gowdra, Vasantharaju S. Mudgal, Jayesh Bansal, Punit Nayak, Pawan G. Manohara Reddy, Seethappa A. Shenoy, Gautham G. Valiathan, Manna Chamallamudi, Mallikarjuna R. Nampurath, Gopalan K. Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title | Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title_full | Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title_fullStr | Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title_full_unstemmed | Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title_short | Synthesis, Characterization, and Preclinical Evaluation of New Thiazolidin-4-Ones Substituted with p-Chlorophenoxy Acetic Acid and Clofibric Acid against Insulin Resistance and Metabolic Disorder |
title_sort | synthesis, characterization, and preclinical evaluation of new thiazolidin-4-ones substituted with p-chlorophenoxy acetic acid and clofibric acid against insulin resistance and metabolic disorder |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4065710/ https://www.ncbi.nlm.nih.gov/pubmed/24995315 http://dx.doi.org/10.1155/2014/620434 |
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