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Molecules ; 23(2)2018 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-29419735

RESUMO

The Latin American plant Tabernaemontana longipes was studied in this work as a potential source of antiparasitic agents. The chloroform extract of T. longipes leaves was separated into several fractions, and tested for antitrypanosomal activity. One of the fractions displayed significant growth inhibitory activity against Trypanosoma brucei. The active principle in the fraction was isolated, purified, and characterized by NMR and mass spectrometry. The antitrypanosomal agent in the CHCl3 extract of T. longipes leaves is the pentacyclic triterpenoid bauerenol acetate. A metabolite profiling assay suggest that the triterpenoid influences cholesterol metabolism. The molecular target(s) of bauerenol and its acetate, like many other antiparasitic pentacyclic triterpenoids is/are unknown, but they present privileged structural scaffolds that can be explored for structure-based activity optimization studies using phenotypic assays.


Assuntos
Extratos Vegetais/química , Extratos Vegetais/farmacologia , Tabernaemontana/química , Triterpenos/química , Triterpenos/farmacologia , Tripanossomicidas/química , Tripanossomicidas/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Testes de Sensibilidade Parasitária , Trypanosoma brucei brucei/efeitos dos fármacos
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