In vivo Antimalarial Activity of α-Mangostin and the New Xanthone δ-Mangostin.
Based on the previously reported in vitro antiplasmodial activity of several xanthones from Garcinia mangostana, two xanthones, α-mangostin and a new compound, δ-mangostin, were isolated from mangosteen husk, and the in vitro antiplasmodial and cytotoxic effects were determined. α-Mangostin was more active against the resistant Plasmodium falciparum chloroquine-resistant (FCR3) strain (IC50  = 0.2 ± 0.01 μM) than δ-mangostin (IC50  = 121.2 ± 1.0 μM). Furthermore, the therapeutic response according to the administration route was evaluated in a Plasmodium berghei malarial murine model. The greatest therapeutic response was obtained with intraperitoneal administration; these xanthones reduced parasitemia by approximately 80% with a daily dose of 100 mg/kg administered twice a day for 7 days of treatment. Neither compound was effective by oral administration. Noticeable toxicological effects were not observed. In addition to the antimalarial effect of these xanthones isolated from G. mangostana husk, the availability of larger amounts of husk raw material to purify the bioactive xanthones is advantageous, permitting additional preclinical assays or chemical transformations to enhance the biological activity of these substances.
PECET, Medical Research Institute, School of Medicine, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Yulieth
Y
Upegui
PECET, Medical Research Institute, School of Medicine, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.|Center for Development of Products against Tropical Diseases - CIDEPRO, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Sara M
SM
Robledo
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Juan Fernando
JF
Gil Romero
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Winston
W
Quiñones
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Rosendo
R
Archbold
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Fernando
F
Torres
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Gustavo
G
Escobar
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Bibiana
B
Nariño
Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia, Calle 67 No. 53-108, Medellín, 050010, Colombia.
Fernando
F
Echeverri
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D004195:Disease Models, Animal; D004912:Erythrocytes / Q000187:drug effects; D029762:Garcinia mangostana / Q000737:chemistry*; D006461:Hemolysis; D006801:Humans; D007274:Injections, Intraperitoneal; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D018512:Parasitemia / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects*; D020298:U937 Cells; D044004:Xanthones / Q000494:pharmacology*
D000962:Antimalarials; D044004:Xanthones; C021053:mangostin
Garcinia mangostana; Plasmodium berghei; Plasmodium falciparum; antimalarial activity; xanthones