Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice

Rica Ingred G.; Netto Chaquip D.; Renno Magdalena N.Abreu Paula A.Costa Paulo R. R.da Silva Alcides J. M.Cavalcante Moises C. M.

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Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice

机译：Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice

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Pterocarpanquinone (+/-)-LQB-118 presents antineoplastic and antiparasitic properties and also shows great inhibitory effect on TNF-alpha 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-kappa B activation and KC level in lungs, with a pronounced inhibitory effect on TNF-alpha 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 alpha and beta. Results suggested that (+/-)-LQB-118 may bind to both receptors, with a similar orientation to 17-beta-estradiol. Together, these results showed that (+/-)-LQB-118 exhibits an anti-inflammatory effect, most likely by inhibiting TNF-alpha release and NF-kappa B activation, which may be related to the estrogen receptor binding. (C) 2016 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2016年第18期|4415-4423|共9页
作者
Rica Ingred G.; Netto Chaquip D.; Renno Magdalena N.Abreu Paula A.Costa Paulo R. R.da Silva Alcides J. M.Cavalcante Moises C. M.;
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作者单位

Univ Fed Rio de Janeiro, Inst Bioquim Med, BR-21941902 Rio De Janeiro, Brazil;

Univ Fed Rio de Janeiro, Polo Univ, Lab Quim, Campus UFRJ Macae Prof Aloisio Teixeira, BR-27930560;

Univ Fed Rio de Janeiro, Nucleo Ecol & Desenvolvimento Socioambiental Maca, Lab Modelagem Mol &Univ Fed Rio de Janeiro, Ctr Ciencias Saude, Inst Pesquisas Prod Nat, Lab Quim Bioorgan, BRUniv Fed Rio de Janeiro, Programa Pos Grad Prod Bioat & Biociencias, Lab Prod Bioat, Campus UFRJ;

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正文语种英语
中图分类药学;
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Inflammation; Pterocarpanquinone; LQB 118; TNF-alpha; Estrogen receptors;

Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice

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