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

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...

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Bibliographic Details
Published in:Pure and applied chemistry 2001-01, Vol.73 (3), p.617-622
Main Authors: Vieira, Paulo C., Mafezoli, Jair, Pupo, Mônica T., Fernandes, João B., da Silva, M. Fátima das G. F., de Albuquerque, Sérgio, Oliva, Glaucius, Pavão, Fernando
Format: Article
Language:English
Subjects:
Crystallography
Enzymes
Protozoa
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Summary: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.
ISSN:0033-4545
1365-3075
DOI:10.1351/pac200173030617