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Title: Inhibition of cysteine proteases by a natural biflavone : behavioral evaluation of fukugetin as papain and cruzain inhibitor.
Authors: 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
Keywords: Biflavones
Protease inhibition
Molecular docking
Cysteine proteases
Issue Date: 2012
Citation: 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: <>. Acesso em: 20 mai. 2017.
Abstract: 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.
ISSN: 1475-6374
Appears in Collections:DEQUI - Artigos publicados em periódicos
DEQUI - Artigos publicados em periódicos

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