Avaliação da atividade anti-inflamatória intestinal do composto LQFM 021 na colite experimental
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2017-09-29
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Universidade Federal de Goiás
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Inflammatory bowel disease (IBD) is an idiopathic, chronic and recurrent disease that affect the gastrointestinal tract (GT); by convention is represented by two major subtypes being ulcerative colitis (UC) and Crohn's Disease (CD). IBD has a multifactorial etiology with causes still unknown, and has gained importance over the last decades due to the significant increase in its incidence, mainly in underdeveloped countries The increase in incidence justifies the need for further studies to understand its physiopathology, as well as suggestion of more effective therapies, financially accessible and with fewer side effects. The compound 5- (1- (3-fluorophenyl) -1H-pyrazol-4) -2H-tetrazole (LQFM021), synthesized at the Laboratory of Pharmaceutical Chemistry of the Faculty of Pharmacy at the Federal University of Goiás is a piperazine derivative considered a promising candidate for the development of new anti-inflammatory drugs, since this class of chemical compounds have a broad spectrum of biological activities already identified. Thus, the aim of the present study was to describe the effects of LQFM021 on the inflammatory bowel process. For this, experimental colitis was induced with TNBS (2,4,6-Trinitrobenzenesulfonic acid) in 50% ethanol, the animals were divided into two control groups and five treatment groups with 7,5; 15; 30; 60 and 120 mg/kg/day of LQFM 021. The results obtained in this study showed that the dosages of LQFM021 presented positive results in relation to the evaluated parameters. The intestines of the dose of 120 mg/kg presented the lowest extension of the lesion (2.50 ± 1.04), macroscopic damage (5 ± 1.51), colon weight/length (122.98 ± 9.63), and reduced adherence to other organs and diarrhea in 71.42% and 85.71%, respectively. The histological assays corroborate with the macroscopic analyses, and the dose of 120 mg/kg the epithelial tissue presented the best cellular organization. It is possible to conclude that the LQFM021 compound used in the present study was able to reduce the severity and extent of TNBS-induced acute damage and con potentidy be a therapeutic target for IBD.
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RICETO, Érika Bezerra de Melo. Avaliação da atividade anti-inflamatória intestinal do composto LQFM 021 na colite experimental. 2017. 101 f. Dissertação (Mestrado em Ciências Biológicas) - Universidade Federal de Goiás, Goiânia, 2017.