In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents

Thiazolidinediones (TZDs), used to treat type 2 diabetes mellitus, act as full agonists of the peroxisome proliferator-activated receptor gamma. Unfortunately, they produce adverse effects, including weight gain, hepatic toxicity, and heart failure. Our group previously reported the design, synthesi...

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Main Authors: Diana Alemán-González-Duhart, Samuel Álvarez-Almazán, Miguel Valdes, Feliciano Tamay-Cach, Jessica Elena Mendieta-Wejebe
Format: Article
Language:English
Published: Wiley 2021-01-01
Series:PPAR Research
Online Access:http://dx.doi.org/10.1155/2021/5100531
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author Diana Alemán-González-Duhart
Samuel Álvarez-Almazán
Miguel Valdes
Feliciano Tamay-Cach
Jessica Elena Mendieta-Wejebe
author_facet Diana Alemán-González-Duhart
Samuel Álvarez-Almazán
Miguel Valdes
Feliciano Tamay-Cach
Jessica Elena Mendieta-Wejebe
author_sort Diana Alemán-González-Duhart
collection DOAJ
description Thiazolidinediones (TZDs), used to treat type 2 diabetes mellitus, act as full agonists of the peroxisome proliferator-activated receptor gamma. Unfortunately, they produce adverse effects, including weight gain, hepatic toxicity, and heart failure. Our group previously reported the design, synthesis, in silico evaluation, and acute oral toxicity test of two TZD derivatives, compounds 40 (C40) and 81 (C81), characterized as category 5 and 4, respectively, under the Globally Harmonized System. The aim of this study was to determine whether C40, C81, and a new compound, C4, act as euglycemic and antioxidant agents in male Wistar rats with streptozotocin-induced diabetes. The animals were randomly divided into six groups (n=7): the control, those with diabetes and untreated, and those with diabetes and treated with pioglitazone, C40, C81, or C4 (daily for 21 days). At the end of the experiment, tissue samples were collected to quantify the level of glucose, insulin, triglycerides, total cholesterol, and liver enzymes, as well as enzymatic and nonenzymatic antioxidant activity. C4, without a hypoglycemic effect, displayed the best antioxidant activity. Whereas C81 could only attenuate the elevated level of blood glucose, C40 generated euglycemia by the end of the treatment. All compounds produced a significant decrease in triglycerides.
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spelling doaj-art-657f57396ca648bd91b9fce38dc12ba82025-02-03T01:04:21ZengWileyPPAR Research1687-47652021-01-01202110.1155/2021/5100531In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic AgentsDiana Alemán-González-Duhart0Samuel Álvarez-Almazán1Miguel Valdes2Feliciano Tamay-Cach3Jessica Elena Mendieta-Wejebe4Laboratorio de Biofísica y BiocatálisisLaboratorio de Biofísica y BiocatálisisLaboratorio de Biofísica y BiocatálisisLaboratorio de Investigación en Bioquímica AplicadaLaboratorio de Biofísica y BiocatálisisThiazolidinediones (TZDs), used to treat type 2 diabetes mellitus, act as full agonists of the peroxisome proliferator-activated receptor gamma. Unfortunately, they produce adverse effects, including weight gain, hepatic toxicity, and heart failure. Our group previously reported the design, synthesis, in silico evaluation, and acute oral toxicity test of two TZD derivatives, compounds 40 (C40) and 81 (C81), characterized as category 5 and 4, respectively, under the Globally Harmonized System. The aim of this study was to determine whether C40, C81, and a new compound, C4, act as euglycemic and antioxidant agents in male Wistar rats with streptozotocin-induced diabetes. The animals were randomly divided into six groups (n=7): the control, those with diabetes and untreated, and those with diabetes and treated with pioglitazone, C40, C81, or C4 (daily for 21 days). At the end of the experiment, tissue samples were collected to quantify the level of glucose, insulin, triglycerides, total cholesterol, and liver enzymes, as well as enzymatic and nonenzymatic antioxidant activity. C4, without a hypoglycemic effect, displayed the best antioxidant activity. Whereas C81 could only attenuate the elevated level of blood glucose, C40 generated euglycemia by the end of the treatment. All compounds produced a significant decrease in triglycerides.http://dx.doi.org/10.1155/2021/5100531
spellingShingle Diana Alemán-González-Duhart
Samuel Álvarez-Almazán
Miguel Valdes
Feliciano Tamay-Cach
Jessica Elena Mendieta-Wejebe
In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
PPAR Research
title In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
title_full In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
title_fullStr In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
title_full_unstemmed In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
title_short In Vivo and Ex Vivo Evaluation of 1,3-Thiazolidine-2,4-Dione Derivatives as Euglycemic Agents
title_sort in vivo and ex vivo evaluation of 1 3 thiazolidine 2 4 dione derivatives as euglycemic agents
url http://dx.doi.org/10.1155/2021/5100531
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