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http://www.repositorio.ufop.br/jspui/handle/123456789/7943
Título: | Inhibition of cysteine proteases by a natural biflavone : behavioral evaluation of fukugetin as papain and cruzain inhibitor. |
Autor(es): | Assis, Diego Magno Gontijo, Vanessa Silva Pereira, Ivan de Oliveira Santos, Jorge Alexandre Nogueira Camps, Ihosvany Nagem, Tanus Jorge Izidoro, Mario Augusto Tersariol, Ivarne Luis dos Santos Barros, Nilana Meza Tenório de Doriguetto, Antônio Carlos Santos, Marcelo Henrique dos Juliano, Maria Aparecida |
Palavras-chave: | Biflavones Protease inhibition Molecular docking Cysteine proteases |
Data do documento: | 2012 |
Referência: | ASSIS, D. A. et al. Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor. Journal of Enzyme Inhibition and Medicinal Chemistry, v. 2012, p. 1-10, 2012. Disponível em: <http://www.tandfonline.com/doi/full/10.3109/14756366.2012.668539>. Acesso em: 20 mai. 2017. |
Resumo: | Cruzain is the major cysteine protease of Trypanosoma cruzi, the infectious agent responsible for Chagas disease, and cruzain inhibitors display considerable antitrypanosomal activity. In the present work we elucidated crystallographic data of fukugetin, a biflavone isolated from Garcinia brasiliensis, and investigated the role of this molecule as cysteine protease inhibitor. The kinetic analyses demonstrated that fukugetin inhibited cruzain and papain by a slow reversible type inhibition with KI of 1.1 and 13.4 μM, respectively. However, cruzain inhibition was about 12 times faster than papain inhibition. Lineweaver–Burk plots demonstrated partial competitive inhibition for cruzain and hyperbolic mixed-type inhibition for papain. Furthermore, the docking results showed that the biflavone binds to ring C′ in the S2 pocket and to ring C in the S3 pocket through hydrophobic interactions and hydrogen bonds. Finally, fukugetin also presented inhibitory activity on proteases of the T. cruzi extract, with IC50 of 7 μM. |
URI: | http://www.repositorio.ufop.br/handle/123456789/7943 |
Link para o artigo: | http://www.tandfonline.com/doi/full/10.3109/14756366.2012.668539 |
DOI: | https://doi.org/10.3109/14756366.2012.668539 |
ISSN: | 1475-6374 |
Aparece nas coleções: | DEQUI - Artigos publicados em periódicos |
Arquivos associados a este item:
Arquivo | Descrição | Tamanho | Formato | |
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ARTIGO_InibitionCysteineProteases.pdf Restricted Access | 1,08 MB | Adobe PDF | Visualizar/Abrir |
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