Synthesis, Microcharacterization, and Antileishmanial Activity of Novel Artesunate Transition Metal Complexes

International Journal of Chemistry | Vol. 6, No. 5, May 2015 | pp. 33–40

DOI: 10.46882/2015/IJC/000080

Article Type: Original Research Paper

Title: Synthesis, Microcharacterization, and Antileishmanial Activity of Novel Artesunate Transition Metal Complexes

Names of Authors: A. A. Yusuf¹, S. K. Das²*

Authors’ Affiliations:
¹Department of Chemistry, Ahmadu Bello University, Zaria, Nigeria.
²Department of Pharmaceutical Sciences, Jadavpur University, Kolkata, India.

Abstract: The systemic spread of drug-resistant protozoal vectors requires the structural modification of classic sesquiterpene lactone frameworks via coordination to transition metal ions to enhance lethal cellular targeting. This study reports the synthesis, microcharacterization, and in vitro biological evaluation of novel copper(II), zinc(II), and iron(II) complexes coordinated with artesunate ligands. The newly synthesized structures were characterized using elemental analysis, molar conductance, magnetic susceptibility, and FT-IR spectroscopy. Analytical metrics established a 1:2 metal-to-ligand ratio, corresponding to the molecular formula [M(ART)₂Cl₂], where ART represents the deprotonated artesunate drug. Molar conductance values in DMF confirmed non-electrolytic properties. FT-IR spectra established that the drug coordinates in a bidentate manner, binding to the metal cores via the lactone carbonyl and the deprotonated carboxylate oxygen atoms. In vitro antileishmanial susceptibility testing was executed against Leishmania donovani promastigotes using the Alamar Blue assay. The iron(II)-artesunate complex demonstrated high lethal potency, yielding an IC50 value of 1.42 μM compared to standalone uncoordinated artesunate (6.84 μM). This enhanced performance is driven by metal-induced homolytic cleavage of the peroxide bridge, accelerating free radical generation inside the parasite cells.

Keywords: Artesunate; Metal complexes; Coordination chemistry; Antileishmanial activity; Leishmania donovani; Free radicals

Manuscript Timeline: Received: June 05, 2014; Revised: July 18, 2014; Accepted: August 20, 2014; Published: May 04, 2015.

Citation: Yusuf, A. A., & Das, S. K. (2015). Synthesis, Microcharacterization, and Antileishmanial Activity of Novel Artesunate Transition Metal Complexes. International Journal of Chemistry, 6(5), 33–40.

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