Ecology- and bioassay-guided drug discovery for treatments of tropical parasitic disease: 5alpha,8alpha-epidioxycholest-6-en-3beta-ol isolated from the mollusk Dolabrifera dolabrifera shows significant activity against Leishmania donovani.
作者： Kathryn E. Clark , Angela Capper , Gina Della Togna , Valerie J. Paul , Luz I. Romero
DOI: 10.1177/1934578X1300801109
关键词: Dolabrifera 、 Dolabrifera dolabrifera 、 Vero cell 、 Biology 、 Plasmodium falciparum 、 Bioassay 、 Trypanosoma cruzi 、 Leishmania donovani 、 Ecology 、 Amastigote
摘要: An ecology- and bioassay-guided search employed to discover compounds with activity against tropical parasitic diseases cancer from the opisthobranch mollusk, Dolabrifera dolabrifera, led discovery of antileishmanial properties in known compound, 5α,8α-epidioxycholest-6-en-3β-ol (1). Compound 1 was identified through nuclear magnetic resonance spectroscopy (1H, 13C) mass spectrometry. The compound concentrated digestive gland D. but not detected other body parts, fecal matter or mucus. showed an IC50 4.9 µM towards amastigote form Leishmania donovani compared 281 control Vero cell line, a 57.3-fold difference, demonstrated no measurable Plasmodium falciparum, Trypanosoma cruzi, breast MCF-7.
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