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Int J Parasitol Drugs Drug Resist ; 7(1): 83-89, 2017 04.
Artigo em Inglês | MEDLINE | ID: mdl-28171818

RESUMO

Giardia duodenalis is an intestinal parasite that causes giardiasis, a widespread human gastrointestinal disease. Treatment of giardiasis relies on a small arsenal of compounds that can suffer from limitations including side-effects, variable treatment efficacy and parasite drug resistance. Thus new anti-Giardia drug leads are required. The search for new compounds with anti-Giardia activity currently depends on assays that can be labour-intensive, expensive and restricted to measuring activity at a single time-point. Here we describe a new in vitro assay to assess anti-Giardia activity. This image-based assay utilizes the Perkin-Elmer Operetta® and permits automated assessment of parasite growth at multiple time points without cell-staining. Using this new approach, we assessed the "Malaria Box" compound set for anti-Giardia activity. Three compounds with sub-µM activity (IC50 0.6-0.9 µM) were identified as potential starting points for giardiasis drug discovery.


Assuntos
Antiprotozoários/isolamento & purificação , Antiprotozoários/farmacologia , Descoberta de Drogas , Giardia lamblia/efeitos dos fármacos , Antiprotozoários/química , Automação , Resistência a Medicamentos , Giardia lamblia/crescimento & desenvolvimento , Processamento de Imagem Assistida por Computador , Estágios do Ciclo de Vida/efeitos dos fármacos , Testes de Sensibilidade Parasitária
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