African Journal of
Pharmacy and Pharmacology

  • Abbreviation: Afr. J. Pharm. Pharmacol.
  • Language: English
  • ISSN: 1996-0816
  • DOI: 10.5897/AJPP
  • Start Year: 2007
  • Published Articles: 2298

Full Length Research Paper

Novel antimalarial agent (Cinnamic 3β-hydroxyolean-12-en-28-carboxylic anhydride): Synthesis, characterization and in vivo studies

J. D. Habila1,2*, F. O. Shode1,  G. I. Ndukwe2, J. O. Amupitan2 and A. J. Nok3
1School of Chemistry, University of KwaZulu-Natal, Durban, South Africa. 2Department of Chemistry, Ahmadu Bello University, Zaria, Nigeria. 3Department of Biochemistry, Ahmadu Bello University, Zaria, Nigeria.
Email: [email protected] or [email protected]

  •  Accepted: 11 December 2011
  •  Published: 29 December 2011

Abstract

The search for potent antimalarial agent has led to the synthesis of a novel hybrid molecule, cinnamic 3β-hydroxyolean-12-en-28-carboxylic anhydride (JH26). The structure was confirmed using 1D and 2D nuclear magnetic resonance (NMR) spectroscopy. The in vivo antimalarial evaluation of the compound JH26 in mice inoculated with the malaria parasite (Plasmodium berghei berghei) was studied after 5 days (D5) of treatment. The results showed a dose dependent decrease in parasitamia at D30 of 44.86 ± 1.0, 65.05 ± 4.0 and 79.33 ± 2.0% recorded on mice at 25, 50 and 100 mgkg-1 body weight dosages, respectively, as compared to the curative rate obtained for artemisinin (97.04 ± 2.0%) and chloroquine (94.40 ± 1.0%), standard drugs used as positive control. 100% mortality was recorded for the parent nucleus oleanolic acid (JH16) at D30 which indicates suppressive action rather than curative ability shown by 3β-hydroxyolean-12-en-28-cinnamic anhydride.

 

Key words: Oleanolic acid, cinnamic 3β-hydroxyolean-12-en-28-carboxylic anhydride, antiplasmodial activity, nuclear magnetic resonance (NMR) spectroscopy.