Abstract
Organic extracts of the leaves of Azadirachta indica A. Juss. yielded ten antitrypanosomal terpenoids. Three of these (1-3), are novel and are derivatives of nimbolide and nimbin. They were extracted from chloroform fraction of methanol extract. These compounds were found to exhibit strong antitrypanosomal activities against Trypanosoma brucei rhodesiense with MIC values ranging of 6.9, 15.6 and 7.8 µg/ml respectively and were more active than Cymerlarsan (a standard drug), which had an MIC value of 187.5 µg/ml when tested against T. b. rhodesiense. The structures were elucidated by spectroscopic methods including; NMR, MS, UV and IR.
Highlights
Azadirachta indica (Meliaceae) is a large tree growing in tropical/subtropical regions
A tea prepared from the leaves and bark is used to treat fever (Kokwaro, 1993); a decoction of fresh leaves is used as a favorite wash to cure old ulcers of long standing and the aqueous extract of the leaves in particular is used as remedy for malaria, similar to the practice in Nigeria
The methanol extract of A. indica exerts a pronounced antiinflammatory and a fairly good antipyretic effect in rabbits, and may justify its use in the treatment of fever resulting from malaria (Okpanyi and Ezeukwu, 1981)
Summary
Azadirachta indica (Meliaceae) is a large tree growing in tropical/subtropical regions. Extracts from different parts of A. indica have shown activity against several diseases and their vectors that affect human and animals (Nagui, 1987; Mackinnon et al, 1997). The methanol extract of A. indica exerts a pronounced antiinflammatory (rat paw oedema) and a fairly good antipyretic effect (pyrogen induced hyperpyrexia) in rabbits, and may justify its use in the treatment of fever resulting from malaria (Okpanyi and Ezeukwu, 1981). Crude extracts of some of the limonoids constituents of the A. indica have been shown to exhibit antimalarial activities against chloroquine resistant K1 strain of Plasmodium falciparum (Bray et al, 1990). We report the structures of three new limonoids that were isolated from the leaves of A. indica and their activities against T. b. We report the structures of three new limonoids that were isolated from the leaves of A. indica and their activities against T. b. rhodesiense
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