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1.
Burns ; 48(8): 1850-1862, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-35153109

RESUMO

BACKGROUND: Among the zones of coagulation, hyperemia and stasis that occur in the burned area, the most intense metabolic process and the highest sensitivity to recovery with treatment is the zone of stasis.This metabolic process is related to how well the tissues in the zone of stasis can cope with oxidative stress. If the tissues in the zone of stasis are saved, the burn area will potentially heal faster and with less scar. In this study, we examined the effects of taurine amino acids and apocynin molecules on saving the tissues in the burn zone of stasis. METHODS: The study was conducted with 48 rats. The burn zone of stasis was created according to the pattern previously described in the literature as comb burn model. In the 21-day study, biopsies were taken for histological examination on the 3rd, 7th and 21st days of the study. In addition, macroscopic photographic analysis was performed. Biopsies were taken for biochemical analysis on the 21st day. Histologically, inflammation, reepithelialization, and collagenization were evaluated, and the CD34 immunoreactivity was analysed. Biochemically, CAT, SOD, tGSH, TAS, TOS, MDA and PPC values were determined. RESULTS: In the histological examination, on the 3rd, 7th and 21st days, inflammation was found to be reduced in the groups given taurine and apocynin on the 3rd day. On the 7th day, better reepithelialization and collagenization were observed in the group given taurine. Significant reepithelialization, collagenization and hair follicle development were observed in the groups given taurine and apocynin on the 21st day. In the biochemical analysis, the effects of apocynin on antioxidant enzymes were determined to be prominent. While we found no significant difference on the 3rd and 7th days in the photographic analysis, taurine and apocynin were observed to act synergistically on the 21st day and significantly reduced the burned areas. CONCLUSION: On the 3rd day, taurine and apocynin prevented inflammation, the effects of taurine in the zone of stasis in the early period (7th day) are more pronounced, the effect of apocynin on antioxidant enzymes is more pronounced. In the late period (21st day), taurine and apocynin were found to be more effective in saving the zone of stasis by creating a synergistic effect.


Assuntos
Queimaduras , Ratos , Animais , Ratos Sprague-Dawley , Queimaduras/tratamento farmacológico , Queimaduras/patologia , Taurina/farmacologia , Taurina/uso terapêutico , Antioxidantes/farmacologia , Modelos Animais de Doenças , Inflamação
2.
Arch Pharm (Weinheim) ; 351(10): e1800165, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30168852

RESUMO

Pyrrole carboxamide rings are rarely used as active scaffold in designing inhibitors for enzymes. Herein, we described the structure-activity relationship for novel xanthine oxidase inhibitors based on the pyrrole carboxamide scaffold. A series of novel-substituted pyrrole carboxamide derivatives were synthesized and characterized; their in vitro and in silico inhibitory activities were determined against xanthine oxidase. Among these compounds, those which contain no substituent and one methyl group at the para-position of the phenyl moiety in the main structure, respectively, were found out as most active according to the xanthine oxidase inhibition activity study. In silico techniques reveal why these compounds display more activities than others, based on their binding interactions with xanthine oxidase and the surface scanning results of the enzyme. Furthermore, the binding energy calculations displayed good agreement with the experimental activity values.


Assuntos
Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Pirróis/farmacologia , Xantina Oxidase/antagonistas & inibidores , Animais , Bovinos , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Leite/enzimologia , Estrutura Molecular , Pirróis/síntese química , Pirróis/química , Relação Estrutura-Atividade , Xantina Oxidase/metabolismo
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