Abstract
Extracts from Holostylis reniformis were tested in vivo against Plasmodium berghei and in vitro against a chloroquine-resistant strain of Plasmodium falciparum. The hexane extract of the roots was the most active, causing 67% reduction of parasitemia in vivo. From this extract, six lignans, including a new (7'R,8S,8'S)-3',4'-methylenedioxy-4,5-dimethoxy-2,7'-cyclolignan-7-one, were isolated and tested in vitro against P. falciparum. The three most active lignans showed 50% inhibitor concentrations of < or =0.32 microM. An evaluation of minimum lethal dose (30%) values showed low toxicity for these lignans in a hepatic cell line (Hep G2A16). Therefore, these compounds are potential candidates for the development of antimalarial drugs.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials / isolation & purification
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Antimalarials / pharmacology*
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Aristolochiaceae / chemistry*
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Cell Line, Tumor
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Chromatography, High Pressure Liquid
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Circular Dichroism
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Formazans / metabolism
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Humans
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Inhibitory Concentration 50
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Lignans / chemistry
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Lignans / pharmacology*
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Mice
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Molecular Conformation
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Parasitemia / drug therapy
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology
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Plant Roots / chemistry
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Plasmodium berghei / drug effects
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Plasmodium falciparum / drug effects
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Spectrophotometry, Ultraviolet
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Tetralones / chemistry
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Tetralones / pharmacology*
Substances
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Antimalarials
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Formazans
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Lignans
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Plant Extracts
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Tetralones