In-vivo antimalarial activity of some oxygenated xanthones.
A series of oxygenated xanthones was prepared so that the antimalarial activity of each compound could be evaluated in vivo, using 4-day suppressive assays against Plasmodium berghei ANKA in BALB/c mice. When given in a dose of 20 mg/kg.day for 4 days, most of the compounds produced significant chemosuppression of parasitaemia. The most active compound was 1,3,6,8-tetrahydroxyxanthone, which reduced the percentage of erythrocytes infected by 70.5%, followed by norlichexanthone (44.3%) and its isomer, 1,3,8-trihydroxy-6-methylxanthone (37.0%). Whereas di-C-allyl-dihydroxyxanthone showed lower but still notable activity (33.4%), 1,3-dihydroxyxanthone was much less active (15.1%). This appears to be the first demonstration of the antimalarial activity of some hydroxyxanthones in vivo.
Fotie
J
J
Department of Organic Chemistry, Faculty of Science, University of Yaounde I, PO Box 812, Yaounde, Cameroon. fotie@uycdc.uninet.cm
Nkengfack
A E
AE
Rukunga
G
G
Tolo
F
F
Peter
M G
MG
Heydenreich
M
M
Fomum
Z T
ZT
D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D004353:Drug Evaluation, Preclinical; D004912:Erythrocytes / Q000187:drug effects; D005260:Female; D008288:Malaria / Q000097:blood / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D008807:Mice, Inbred BALB C; D000069463:Olive Oil; D010084:Oxidation-Reduction; D010938:Plant Oils / Q000627:therapeutic use; D010962:Plasmodium berghei; D011803:Quinine / Q000627:therapeutic use; D016896:Treatment Outcome; D044004:Xanthones / Q000737:chemistry / Q000627:therapeutic use*
D000962:Antimalarials; D000069463:Olive Oil; D010938:Plant Oils; D044004:Xanthones; D011803:Quinine