𝔖 Bobbio Scriptorium
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In vitro and In vivo evaluation of betulinic acid as an antimalarial

✍ Scribed by J. C. P. Steele; D. C. Warhurst; G. C. Kirby; M. S. J. Simmonds

Publisher
John Wiley and Sons
Year
1999
Tongue
English
Weight
67 KB
Volume
13
Category
Article
ISSN
0951-418X

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✦ Synopsis

The lupane-type triterpene betulinic acid was isolated from an ethanol extract of the root bark of the Tanzanian tree Uapaca nitida Mu Β¨ll-Arg. (Euphorbiaceae). The in vitro antiplasmodial IC 50 values of betulinic acid against chloroquine resistant (K1) and sensitive (T9-96) Plasmodium falciparum were found to be 19.6 mg/mL and 25.9 mg/mL, respectively. The in vitro activities of several related triterpenes were also evaluated. Betulin was found to be inactive at 500 mg/mL for both K1 and T9-96. Ursolic acid exhibited IC 50 values of 36.5 mg/mL and 28 mg/mL, and oleanolic acid exhibited IC 50 values of 88.8 mg/mL and 70.6 mg/mL against K1 and T9-96, respectively. When betulinic acid was tested for in vivo activity in a murine malaria model (P. berghei) the top dosage employed of 250 mg/kg/day was ineffective at reducing parasitaemia and exhibited some toxicity. Betulinic acid has not previously been evaluated for in vivo activity. This is believed to be the first compound to be isolated from U. nitida.

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