Synthesis and Evaluation of Novel Thiazolidinedione Derivatives for Antidiabetic Activity

Swapna, D.; Sivagami, B; Manasa, K; Rajita, G; Alagarsamy,

doi:10.7897/2230-8407.07544

Cited by 5 publications

(2 citation statements)

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“…Diabetes is a disorder of carbohydrate, fat and protein metabolism caused due to insufficient production of insulin or due to its inhibitory action, which can be considered as a major cause of high economic loss which can in turn impede the development of nations 40 . Diabetes mellitus causes disturbances in the intake of glucose as well as glucose metabolism.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of in Vivo Antidiabetic Activity of Andrographis Echioides (L.) Nees

Ruba¹,

Doss²,

Ramasamy³

2016

Int. Res. J. Pharm.

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The aim of this study was to investigate the effect of ethanol extract of the whole plant of Andrographis echioides as antihyperglycemic, antihyperlipidemic and antioxidant effect in alloxan induced diabetic rats. Diabetes was induced in Wistar albino rats by administration of alloxan monohydrate (150mg/kg). The A. echioides at a dose of 100, 200 and 400mg/kg of body weight was administrated at single dose per day to diabetes induced rats for a period of 14 days. The effect of A. echioides on blood glucose, insulin, urea, creatinine, HbA1C, serum protein, albumin, globulin, serum enzymes [Serum glutamate pyruvate transaminases (SGPT), serum glutamate oxaloacetate transaminases (SGOT), alkaline phosphatase (ALP)], serum lipid profile, [total cholesterol (TC), triglycerides (TG), high density lipoprotein-cholesterol (HDL-C), low density lipoproteincholesterol (LDL-C), very low density lipoprotein-cholesterol (VLDL-C) and lipidperoxidation (LPO), superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX) and reduced glutathione (GSH) were measured in the diabetic rats. The A. echioides elicited significant reduction of blood glucose, lipid parameters except HDL-C, serum enzymes and LPO and significantly reduced insulin, HDL-C, SOD, CAT, GPX and GSH at the dose of 400mg/kg which was compared with the diabetic control. From the above results, it is concluded that ethanol extract of A. echioides whole plant possesses significant antihyperglycemic, antihyperlipidemic and antioxidant effects in alloxan induced diabetic rats.

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Section: Discussionmentioning

confidence: 99%

Evaluation of in Vivo Antidiabetic Activity of Andrographis Echioides (L.) Nees

Ruba¹,

Doss²,

Ramasamy³

2016

Int. Res. J. Pharm.

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“…However, these complexes were considerably less active against the corresponding current drugresistant strains. Recently, inert ruthenium complexes containing heterocyclic ligands have been investigated as antimicrobial agents [16][17][18][19][20] . The unique properties of the ruthenium(II) polypyridyl complexes are that they do not change their structure under physiological conditions and are stable in strong acids and bases.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Activities of Biimidazole Based Mixed Ligand Ruthenium(ii) Complexes

Kiruthika¹,

Sivasankari²,

Elayaperumal³

et al. 2016

Int. Res. J. Pharm.

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Ruthenium(II) complexes of the type [Ru(bpy)2(L)](PF6)2, where L=4,5-bis(4-dimethyaminophenyl)-1H,1'H-2,2'-biimidazole (1) and 4,5-bis(4fluorophenyl)-1H,1'H-2,2'-biimidazole (2) that combine the structure of bipyridine and substituted biimidazole derived from dimethylaminobenzil and fluorobenzil have been synthesized and characterized by elemental analyses and spectral (IR, UV-vis, EI-MS) techniques. The redox behavior of the complexes has been studied by cyclic and differential pulse voltammetry. The synthesized ligands and complexes have been tested for in vitro growth inhibitory activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and two fungi (Aspergillus niger and Candida albicans). The antimicrobial activities of the complexes showed better activity compared to that of the ligands.

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Mechanistic insight into the interactions between thiazolidinedione derivatives and PTP-1B combining 3D QSAR and molecular docking in the treatment of type 2 diabetes

Igunnu

Ambrose

Adigun

2020

Physical Sciences Reviews

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Protein tyrosine phosphatases (PTP) regulate various cellular processes and represent important targets for therapeutic intervention in various diseases. Studies have shown that partial or total cessation of the PTP-1B gene in normal and diabetic mice has led to resistance to weight gain and improved insulin response. Also, a further study showed that inhibition of PTP-1B or a reduction in its cellular abundance in mice resulted in similar effects and, as such, provided a rationale for the treatment strategy for type 2 diabetes. Thiazolidinedione (TZD) derivatives have been identified as new PTP-1B inhibitors but the mechanism of interaction between TZD derivatives and PTP-1B is still elusive. In this study, a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed, including multiple linear regression (MLR) and cross-validation, on a set of TZD derivatives as antidiabetic agents. MLR analysis was performed on 23 PTP-1B TZD derivatives to determine the relationships between physicochemical properties and antidiabetic properties of TZD derivatives. The training data set creates a QSAR model with a correlation coefficient (R2) of 0.8516, a Q2 (Leave-One-Out) cross-validation factor of 0.6473, r2 (correlation coefficient) for the external dataset is 0.8367 while r2 of predicted dataset is 0.8934 by the MLR Method. The MLR model was also validated by the standardization approach. We observed a high correlation between predicted and observed activity (experimental values), thus confirming and proving the high quality of QSAR models. Finally, molecular docking analysis was performed to better understand the interactions between the PTP-1B target and TZD derivatives. The model proposed in this project can be used to design new TZD derivatives with specific PTP-1B inhibitory activity.

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Synthesis and Evaluation of Novel Thiazolidinedione Derivatives for Antidiabetic Activity

Cited by 5 publications

References 0 publications

Evaluation of in Vivo Antidiabetic Activity of Andrographis Echioides (L.) Nees

Evaluation of in Vivo Antidiabetic Activity of Andrographis Echioides (L.) Nees

Antimicrobial Activities of Biimidazole Based Mixed Ligand Ruthenium(ii) Complexes

Mechanistic insight into the interactions between thiazolidinedione derivatives and PTP-1B combining 3D QSAR and molecular docking in the treatment of type 2 diabetes

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