Cargando…

Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs

The present study is aimed to investigate the anti-inflammatory, antioxidant and antidiabetic activities of three series of hydroxytriazenes based on sulfa drugs viz; Sulphathiazole (ST), Sulfisoxazole (SF) and Sulphamethoxazole (SM). Antidiabetic activities of the synthesized hydroxytriazenes were...

Descripción completa

Detalles Bibliográficos
Autores principales: Dayma, Varsha, Chopra, Jaishri, Sharma, Poonam, Dwivedi, Aparna, Tripathi, Indra P., Bhargava, Amit, Murugesan, Vanangamudi, Goswami, Ajay K., Baroliya, Prabhat K.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7472862/
https://www.ncbi.nlm.nih.gov/pubmed/32913908
http://dx.doi.org/10.1016/j.heliyon.2020.e04787
_version_ 1783579070679744512
author Dayma, Varsha
Chopra, Jaishri
Sharma, Poonam
Dwivedi, Aparna
Tripathi, Indra P.
Bhargava, Amit
Murugesan, Vanangamudi
Goswami, Ajay K.
Baroliya, Prabhat K.
author_facet Dayma, Varsha
Chopra, Jaishri
Sharma, Poonam
Dwivedi, Aparna
Tripathi, Indra P.
Bhargava, Amit
Murugesan, Vanangamudi
Goswami, Ajay K.
Baroliya, Prabhat K.
author_sort Dayma, Varsha
collection PubMed
description The present study is aimed to investigate the anti-inflammatory, antioxidant and antidiabetic activities of three series of hydroxytriazenes based on sulfa drugs viz; Sulphathiazole (ST), Sulfisoxazole (SF) and Sulphamethoxazole (SM). Antidiabetic activities of the synthesized hydroxytriazenes were investigated by α-glucosidase and α-amylase inhibition method and IC(50) values were recorded. The compounds presented significant α-glucosidase and α-amylase inhibition effect with IC(50) values ranging from 122 to 341 μg/mL. Anti-inflammatory activity was also investigated by carrageenan-induced paw edema (CPE) method, where % inhibition was up to 89% after 4 h of treatment and antioxidant properties of the similar compounds were assessed by DPPH and ABTS radical scavenging assays. Antioxidant capacity of all the hydroxytriazenes detected by ABTS assay, was significantly higher as compared to DPPH assay. The hydroxytriazenes having highest antioxidant capacity presented IC(50) values for compound ST-1 and ST-6 are 488 μg/mL for DPPH, 54.12 μg/mL for ABTS and 858.5 μg/mL for DPPH, 48.0 μg/mL for ABTS, respectively. These results suggested that ABTS assay may be more useful than DPPH assay for synthetic antioxidants. The findings from the molecular docking experiments may also expand the formation of new potent sulpha drugs based hydroxytriazenes targeting towards the subunit of C-terminal of human maltase-glucoamylase for the treatment of diabetes metabolic disorder. Overall, highlight the multifunctional role of hydroxytriazenes as antidiabetic, antioxidant and anti-inflammatory agents.
format Online
Article
Text
id pubmed-7472862
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher Elsevier
record_format MEDLINE/PubMed
spelling pubmed-74728622020-09-09 Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs Dayma, Varsha Chopra, Jaishri Sharma, Poonam Dwivedi, Aparna Tripathi, Indra P. Bhargava, Amit Murugesan, Vanangamudi Goswami, Ajay K. Baroliya, Prabhat K. Heliyon Article The present study is aimed to investigate the anti-inflammatory, antioxidant and antidiabetic activities of three series of hydroxytriazenes based on sulfa drugs viz; Sulphathiazole (ST), Sulfisoxazole (SF) and Sulphamethoxazole (SM). Antidiabetic activities of the synthesized hydroxytriazenes were investigated by α-glucosidase and α-amylase inhibition method and IC(50) values were recorded. The compounds presented significant α-glucosidase and α-amylase inhibition effect with IC(50) values ranging from 122 to 341 μg/mL. Anti-inflammatory activity was also investigated by carrageenan-induced paw edema (CPE) method, where % inhibition was up to 89% after 4 h of treatment and antioxidant properties of the similar compounds were assessed by DPPH and ABTS radical scavenging assays. Antioxidant capacity of all the hydroxytriazenes detected by ABTS assay, was significantly higher as compared to DPPH assay. The hydroxytriazenes having highest antioxidant capacity presented IC(50) values for compound ST-1 and ST-6 are 488 μg/mL for DPPH, 54.12 μg/mL for ABTS and 858.5 μg/mL for DPPH, 48.0 μg/mL for ABTS, respectively. These results suggested that ABTS assay may be more useful than DPPH assay for synthetic antioxidants. The findings from the molecular docking experiments may also expand the formation of new potent sulpha drugs based hydroxytriazenes targeting towards the subunit of C-terminal of human maltase-glucoamylase for the treatment of diabetes metabolic disorder. Overall, highlight the multifunctional role of hydroxytriazenes as antidiabetic, antioxidant and anti-inflammatory agents. Elsevier 2020-08-29 /pmc/articles/PMC7472862/ /pubmed/32913908 http://dx.doi.org/10.1016/j.heliyon.2020.e04787 Text en © 2020 Published by Elsevier Ltd. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Article
Dayma, Varsha
Chopra, Jaishri
Sharma, Poonam
Dwivedi, Aparna
Tripathi, Indra P.
Bhargava, Amit
Murugesan, Vanangamudi
Goswami, Ajay K.
Baroliya, Prabhat K.
Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title_full Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title_fullStr Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title_full_unstemmed Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title_short Synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
title_sort synthesis, antidiabetic, antioxidant and anti-inflammatory activities of novel hydroxytriazenes based on sulpha drugs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7472862/
https://www.ncbi.nlm.nih.gov/pubmed/32913908
http://dx.doi.org/10.1016/j.heliyon.2020.e04787
work_keys_str_mv AT daymavarsha synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT choprajaishri synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT sharmapoonam synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT dwivediaparna synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT tripathiindrap synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT bhargavaamit synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT murugesanvanangamudi synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT goswamiajayk synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs
AT baroliyaprabhatk synthesisantidiabeticantioxidantandantiinflammatoryactivitiesofnovelhydroxytriazenesbasedonsulphadrugs