Artículos de revistas
In vitro Metabolism of Grandisin, a Lignan with Anti-chagasic Activity
Fecha
2012-12Registro en:
PLANTA MEDICA, STUTTGART, v. 78, n. 18, pp. 1939-1941, DEC, 2012
0032-0943
10.1055/s-0032-1327876
Autor
Ferreira, Leandro De Santis
Callejon, Daniel Roberto
Engemann, Anna
Cramer, Benedikt
Humpf, Hans-Ulrich
Barros, Valeria Priscila de
Assis, Marilda das Dores
Silva, Denise Brentan da
Albuquerque, Sérgio de
Okano, Laura Tiemi
Kato, Massuo Jorge
Lopes, Norberto Peporine
Institución
Resumen
Tetrahydrofuran lignans represent a well-known group of phenolic compounds capable of acting as antiparasitic agents. In the search for new medicines for the treatment of Chagas disease, one promising compound is grandisin which has shown significant activity on trypomastigote forms of Trypanosoma cruzi. In this work, the in vitro metabolism of grandisin was studied in the pig cecum model and by biomimetic phase I reactions, aiming at an ensuing a preclinical pharmacokinetic investigation. Although grandisin exhibited no metabolization by the pig microbiota, one putative metabolite was formed in a biomimetic model using Jacobsen catalyst. The putative metabolite was tested against T. cruzi revealing loss of activity in comparison to grandisin.