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DOI: 10.1055/s-0032-1327876
In vitro Metabolism of Grandisin, a Lignan with Anti-chagasic Activity
Publication History
received 29 June 2012
revised 27 September 2012
accepted 01 October 2012
Publication Date:
13 November 2012 (online)
![](https://www.thieme-connect.de/media/plantamedica/201218/lookinside/thumbnails/10.1055-s-0032-1327876-1.jpg)
Abstract
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.
Key words
tetrahydrofuran lignans - grandisin - in vitro metabolism - Piper solmsianum - Piperaceae - Jacobsen catalyst-
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