Author | Moreira, Magna S. Alexandre | |
Author | Takiya, Christina M. | |
Author | Arruda, Luciana B. de | |
Author | Pascarelli, Bernardo | |
Author | Gomes, Raquel N. | |
Author | Faria Neto, Hugo Caire C. | |
Author | Lima, Lidia M. | |
Author | Barreiro, Eliezer J. | |
Access date | 2019-12-19T12:58:58Z | |
Available date | 2019-12-19T12:58:58Z | |
Document date | 2005 | |
Citation | MOREIRA, Magna S. Alexandre et al. LASSBio-468: a new achiral thalidomide analogue which modulates TNF-a and NO production and inhibits endotoxic shock and arthritis in an animal model. International Immunopharmacology. v. 5, p. 485-494, 2005. | pt_BR |
ISSN | 1567-5769 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/38704 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | restricted access | pt_BR |
Subject in Portuguese | Choque endotóxico | pt_BR |
Subject in Portuguese | Fator de necrose tumoral alfa | pt_BR |
Subject in Portuguese | Lipopolissacarídeo | pt_BR |
Title | LASSBio-468: a new achiral thalidomide analogue which modulates TNF-a and NO production and inhibits endotoxic shock and arthritis in an animal model | pt_BR |
Type | Article | pt_BR |
DOI | 10.1016/j.intimp.2004.10.017 | |
Abstract | As part of a program researching the synthesis and immunopharmacological evaluation of novel synthetic compounds, we
have described the immune modulatory profile of the new achiral thalidomide analogue LASSBio-468 in the present work. This
compound was planned as an N-substituted phthalimide derivate, structurally designed as a hybrid of thalidomide and aryl
sulfonamides, which were previously described as tumor necrosis factor-alpha (TNF-a) and PDE4 inhibitors. LASSBio-468
was recently demonstrated to inhibit the TNF-a production induced by lipopolysaccharide (LPS), in vivo. Here, we investigated
whether this compound would affect chronic inflammation processes associated with the production of this pro-inflammatory
cytokine. Treatment with LASSBio-468 before a lethal dose injection of LPS in animals greatly inhibited endotoxic shock. This
effect seems to be mediated by a specific down regulation of TNF-a and nitric oxide production, regulated mainly at the RNA
level. In another model, histopathological analysis indicated that this compound also inhibited adjuvant-induced arthritis in rats.
Taken together, our data demonstrated a potent anti-inflammatory effect of LASSBio-468, suggesting its use as a potential drug
against chronic inflammatory diseases. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Faculdade de Farmácia. Departamento de Fármacos. LASSBio-Laboratóio de Avaliação e Síntese de Substâncias Bioativas. Rio de Janeiro, RJ, Brasil / Universidade Federal de Alagoas. Departamento de Fisiologia. Maceió, AL, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Ciências Biomédicas. Departamento de Histologia e Embriologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Microbiologia Prof. Paulo de Góes. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Ciências Biomédicas. Departamento de Histologia e Embriologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Farmacodinâmica. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Farmacodinâmica. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Faculdade de Farmácia. Departamento de Fármacos. LASSBio-Laboratóio de Avaliação e Síntese de Substâncias Bioativas. Rio de Janeiro, RJ, Brasil. | pt_BR |
Subject | Endotoxic shock | pt_BR |
Subject | TNF-@ | pt_BR |
Subject | NO | pt_BR |
Subject | LPS | pt_BR |
Subject | LASSBio-468 | pt_BR |
e-ISSN | 1878-1705 | |
Embargo date | 2025-01-01 | |