Planta Med 2015; 81 - PX42
DOI: 10.1055/s-0035-1556486

Antimalarial metabolites from Buxus sempervirens

S Cai 1, 2, AL Risinger 3, S Nair 4, DR Powell 2, TJC Anderson 4, SL Mooberry 3, RH Cichewicz 1, 2
  • 1Natural Products Discovery Group, Institute for Natural Products Applications and Research Technologies
  • 2Department of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019
  • 3Department of Pharmacology, The University of Texas Health Science Center at San Antonio, San Antonio, TX 78229
  • 4Department of Genetics, Texas Biomedical Research Institute, San Antonio, TX 78227

Some malaria parasites (Plasmodium falciparum) have developed resistance to all currently available antimalarial drugs including artemisinin derivatives, so there is an urgent need to discover new chemicals with antimalarial activity. Eight new lupinane derivatives (1 – 8) were isolated from the extract of the English boxwood (Buxus sempervirens) using bioassay guided fractionation and examined for activity against malarial parasites Plasmodium falciparum. The lupinane derivatives range in potency from 0.49 – 3.36 µM against the drug sensitive HB3 parasite and retain efficacy in an artemisinin and multidrug resistant parasite recently isolated in Southeast Asia. Compounds 2 and 3 in particular exhibited greater than 30-fold selectivity for malaria parasites as compared to human cancer cell lines.