Journal of the Brazilian Chemical Society | |
A new bianthron glycoside as inhibitor of Trypanosoma cruzi glyceraldehyde 3-phosphate dehydrogenase activity | |
Edângelo M. S. De Macedo2  Helton J. Wiggers1  Maria G. V. Silva2  Raimundo Braz-filho1  Adriano D. Andricopulo1  Carlos A. Montanari1  | |
[1] ,Universidade Federal do Ceará Departamento de Química Orgânica e Inorgânica Departamento de Química Analítica e Físico-QuímicaFortaleza CE ,Brazil | |
关键词: Senna martiana; Leguminoseae; bianthrone; anthraquinone; Trypanosoma cruzi; isothermal titration calorimetry; | |
DOI : 10.1590/S0103-50532009000500021 | |
来源: SciELO | |
【 摘 要 】
A phytochemical investigation of the ethanolic extract of stalks of Senna martiana Benth. (Leguminoseae), native specie of northeast Brazil, resulted in the isolation and spectroscopic characterization of a new bianthrone glycoside, martianine 1 (10,10'-il-chrysophanol-10-oxi10,10'-bi-glucosyl). Its identification was established by HRMS, IR and 2D NMR experiments. The evaluation of martianine trypanocidal activity was carried out against gliceraldehyde 3-phosphate dehydrogenase enzyme from Trypanosoma cruzi. Its inhibitory constant (Ki) is in the low micromolar concentration and it was determined by isothermal titration calorimetry to be 27.3 ± 2.47 µmol L-1. The non-competitive mechanism is asserted to be putative of the mode of action martianine displays against T. cruzi GAPDH. Results show that martianine has a great potential to become new lead molecule by inhibiting this key enzyme and for the development of new drugs against Chagas disease.
【 授权许可】
CC BY
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