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Pure Appl. Chem. Vol. 73, No. 3, pp. 617-622 (2001)

Pure and Applied Chemistry

Vol. 73, Issue 3

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

Paulo C. Vieira1,**, Jair Mafezoli1, Mônica T. Pupo2, João B. Fernandes1, M. Fátima das G. F. da Silva1, Sérgio de Albuquerque2, Glaucius Oliva3, and Fernando Pavão3,4

1Departamento de Química, Universidade Federal de São Carlos, CP 676, São Carlos, SP, Brazil; 2Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil; 3Instituto de Física de São Carlos, Universidade de São Paulo, São Carlos, SP, Brazil; 4Instituto de Química de São Carlos, Universidade de São Paulo, São Carlos, SP, Brazil

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.

*Lecture presented at the 22nd IUPAC International Symposium on the Chemistry of Natural Products, São Carlos, Brazil, 3-8 September 2000. Other presentations are published in this issue, pp. 549-626.
**Corresponding author


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