In vitro Metabolism of Grandisin, a Lignan with Anti-chagasic Activity
| Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
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| Data(s) |
26/09/2013
26/09/2013
01/12/2012
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| Resumo |
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. FINEP FINEP FAPESP FAPESP CAPES CAPES CNPq CNPq |
| Identificador |
PLANTA MEDICA, STUTTGART, v. 78, n. 18, pp. 1939-1941, DEC, 2012 0032-0943 http://www.producao.usp.br/handle/BDPI/33742 10.1055/s-0032-1327876 |
| Idioma(s) |
eng |
| Publicador |
GEORG THIEME VERLAG KG STUTTGART |
| Relação |
PLANTA MEDICA |
| Direitos |
openAccess Copyright GEORG THIEME VERLAG KG |
| Palavras-Chave | #TETRAHYDROFURAN LIGNANS #GRANDISIN #IN VITRO METABOLISM #PIPER SOLMSIANUM #PIPERACEAE #JACOBSEN CATALYST #INTESTINAL MICROBIOTA #VIROLA-SURINAMENSIS #PIPER-SOLMSIANUM #DEGRADATION #(-)-GRANDISIN #MODEL #FLAVONOIDS #MICROFLORA #OXIDATION #PLANT SCIENCES #CHEMISTRY, MEDICINAL #PHARMACOLOGY & PHARMACY |
| Tipo |
article original article publishedVersion |
