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Strategies for the isolation and identification of trypanocidal compounds from the Rutales

2001; International Union of Pure and Applied Chemistry; Volume: 73; Issue: 3 Linguagem: Inglês

10.1351/pac200173030617

1365-3075

Paulo C. Vieira, Jair Mafezoli, Mônica Tallarico Pupo, João Fernandes, Maria Fátima das Graças Fernandes da Silva, Sérgio de Albuquerque, Glaucius Oliva, Fernando Pavão,

Phytochemical compounds biological activities

Abstract Crude extracts of Rutales species were tested in vitro against the trypomastigote form of Trypanosoma cruzi at 4 mg/mL, and 20% of them showed significant activity (80%). Their inhibitory activity against the glycolytic enzyme GAPDH from T. cruzi has also been evaluated at the concentrations of 100 and 200 mg/mL. Additionally, the inhibitory activity of 13 purified coumarins were also assayed against T. cruzi-GAPDH. Chalepin was the most active substance with IC50 = 64 mM. The 3D structure of the complex chalepin-enzyme was elucidated by X-ray crystallography, revealing the architecture of the interactions between the inhibitor and the enzyme active site.