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Antimicrobial Agents and Chemotherapy, January 2005, p. 264-268, Vol. 49, No. 1
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.1.264-268.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.

Effects of Root Extracts of Fagara zanthoxyloides on the In Vitro Growth and Stage Distribution of Plasmodium falciparum

Olakunle O. Kassim,1* Mark Loyevsky,1,3 Biaffra Elliott,1 Andrew Geall,4 Henrietta Amonoo,3 and Victor R. Gordeuk2,3

Department of Microbiology,1 Department of Medicine,2 Center for Sickle Cell Disease, Howard University College of Medicine, Washington, D.C.,3 Biocal, Inc., San Diego, California4

Received 26 April 2004/ Returned for modification 21 June 2004/ Accepted 15 September 2004

The development of resistance by Plasmodium falciparum to conventional drugs poses a threat to malaria control. There is therefore a need to find new, effective, and affordable remedies for malaria, including those derived from plants. This study demonstrates that crude, reverse-phase high-pressure liquid chromatography (RP-HPLC)-semipurified, and RP-HPLC-purified root extracts of Fagara zanthoxyloides inhibit the growth of P. falciparum in vitro, with 50% inhibitory concentrations (IC50s) of 4.90, 1.00, and 0.13 µg/ml, respectively. Roots of F. zanthoxyloides, known as chewing sticks, are widely used for tooth cleaning in West Africa. Microscopic examination of Giemsa-stained slides showed a virtual absence of schizonts in ring-stage synchronized cultures treated with crude extracts at concentrations of 30 to 60 µg/ml during 36 to 48 h of incubation. These observations suggest that the active constituent in the extract may be cytotoxic for P. falciparum trophozoites, thereby inhibiting their development to the schizont stage. A pure bioreactive fraction was subsequently obtained from the chromatographic separations. When this fraction was mixed with pure fagaronine, the mixture coeluted as a single peak on the analytical RP-HPLC column, suggesting that fagaronine may be the active antimalarial constituent of Fagara root extracts. Additional experiments showed that fagaronine also inhibited P. falciparum growth, with an IC50 of 0.018 µg/ml. The results of this study suggest that the antimalarial activity of fagaronine deserves further investigation.

* Corresponding author. Mailing address: Department of Microbiology, Howard University College of Medicine, 520 W St., NW, Washington, DC 20059. Phone: (202) 806-4319. Fax: (202) 806-4508. E-mail: kkassim{at}howard.edu.

Antimicrobial Agents and Chemotherapy, January 2005, p. 264-268, Vol. 49, No. 1
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.1.264-268.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.





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