Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice |
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| Institution: | 1. Instituto de Bioquímica Médica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Rio de Janeiro 21941-902, Brazil;2. Laboratório de Produtos Bioativos, Programa de Pós Graduação em Produtos Bioativos e Biociências, Universidade Federal do Rio de Janeiro Campus UFRJ-Macaé Professor Aloísio Teixeira, Macaé, Rio de Janeiro 27947-200, Brazil;3. Laboratório de Química, Pólo Universitário, Universidade Federal do Rio de Janeiro Campus UFRJ-Macaé Professor Aloísio Teixeira, Macaé, Rio de Janeiro 27930-560, Brazil;4. Laboratório de Modelagem Molecular e Pesquisa em Ciências Farmacêuticas, Núcleo em Ecologia e Desenvolvimento Sócio-Ambiental de Macaé, Universidade Federal do Rio de Janeiro Campus UFRJ-Macaé Professor Aloísio Teixeira, Macaé, Rio de Janeiro 27965-045, Brazil;5. Laboratório de Química Bioorgânica, Instituto de Pesquisas de Produtos Naturais, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Rio de Janeiro 21941-590, Brazil |
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| Abstract: | Pterocarpanquinone (+/−)-LQB-118 presents antineoplastic and antiparasitic properties and also shows great inhibitory effect on TNF-α release in vitro. Here, its anti-inflammatory activity was evaluated in a lipopolysaccharide (LPS)-induced lung inflammation model in C57BL/6 mice. LPS inhalation induced a marked neutrophil infiltration to the lungs which was reduced by intraperitoneal treatment with (+/−)-LQB-118 in a similar manner to that of dexamethasone and even better than that of acetylsalicylic acid. Moreover, (+/−)-LQB-118 administration resulted in decrease of NF-κB activation and KC level in lungs, with a pronounced inhibitory effect on TNF-α release, measured in bronchoalveolar lavage fluid. Trying to understand the anti-inflammatory mechanism by which (+/−)-LQB-118 acts, we performed a molecular modeling analysis, including docking to estrogen receptors α and β. Results suggested that (+/−)-LQB-118 may bind to both receptors, with a similar orientation to 17-β-estradiol. Together, these results showed that (+/−)-LQB-118 exhibits an anti-inflammatory effect, most likely by inhibiting TNF-α release and NF-κB activation, which may be related to the estrogen receptor binding. |
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| Keywords: | Inflammation Pterocarpanquinone LQB 118 TNF-α Estrogen receptors |
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