Antiplasmodial activity of aryltetralone lignans from Holostylis reniformis.
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.
de Andrade-Neto
Valter F
VF
Laboratório de Malaria, Centro de Pesquisas René Rachou/FIOCRUZ, 30190-002, Belo Horizonte, MG, Brazil.
da Silva
Tito
T
Lopes
Lucia M Xavier
LM
do Rosário
Virgílio E
VE
de Pilla Varotti
Fernando
F
Krettli
Antoniana U
AU
D000818:Animals; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology*; D029065:Aristolochiaceae / Q000737:chemistry*; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D002942:Circular Dichroism; D005562:Formazans / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D017705:Lignans / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008968:Molecular Conformation; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D018512:Parasitemia / Q000188:drug therapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D013056:Spectrophotometry, Ultraviolet; D044024:Tetralones / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D005562:Formazans; D017705:Lignans; D010936:Plant Extracts; D044024:Tetralones