Toxicological assessment of synthesized and characterized transition metal(II) complexes of eflornithine hydrochloride hydrate on albino rats

W A Osunniran,A T Bale,J A Obaleye,A C Tella,Y O Ayipo,A O Rajee

doi:10.4314/bcse.v34i3.6

Abstract

Transition metal complexes of Cu(II), Co(II) and Ni(II) with eflornithine hydrochloride hydrate (EFN), an antitrypanosomiasis drug, as ligand have been synthesized and characterized by melting point, elemental analysis, Fourier transform infrared (FTIR), electronic spectra, magnetic susceptibility and electrospray ionization mass spectrometry (ESI-MS). The FTIR spectral data suggested the coordination modes of the ligand to be bidentate, coordinated to the metal ions through its carboxylate oxygen atom and an amino nitrogen atom. From the microanalytical data, the stoichiometry of the metal complexes is 1:2 (metal to ligand). The electronic absorption and magnetic susceptibility studies generally suggested octahedral geometry for the metal complexes. Toxicological evaluation of the ligand (EFN) and complexes were carried out using albino rats. Twenty-five albino rats that were used for the experiment were randomly divided into five groups and animals in group 1 served as a control. All the animals were sacrificed twenty-four hours after completion of their doses. The results revealed a high level of toxicity of EFN than the synthesized metal complexes.  KEY WORDS: Eflornithine hydrochloride hydrate, Carboxylate moiety, Antitrypanosomiasis drug, Toxicological evaluation, Albino rats  Bull. Chem. Soc. Ethiop. 2020, 34(3), 489-500. DOI: https://dx.doi.org/10.4314/bcse.v34i3.6

Highlights

Parasitic diseases represent a major world health problem with very limited therapeutic options, most of the available treatments being decades old and suffering from limited efficacy and/or undesirable collateral effects [1]
This study is aimed at synthesizing eflornithine hydrochloride hydrate (EFN)-transition metal complexes, carried out characterization using various physicochemical and spectroscopic techniques like melting point, elemental analysis, UV, Fourier transform infrared (FTIR), magnetic susceptibility and electrospray ionization mass spectrometry (ESI-MS) and in vivo toxicity of the ligand (Figure 1) and its metal complexes evaluated using albino rats
The preparation of EFN-metal complexes can be represented by the general formula : c

Summary

Introduction

Parasitic diseases represent a major world health problem with very limited therapeutic options, most of the available treatments being decades old and suffering from limited efficacy and/or undesirable collateral effects [1]. Human African trypanosomiasis (HAT) or sleeping sickness is a fatal disease, caused by infection with haemoflagellates of the Trypanosome brucei subspecies, the parasite lives and multiply extracellularly in the blood and tissue fluids in the human host and are transmitted by the bite of infected tsetse flies of the genus glossina in a salivarian mode of transmission. Eflornithine hydrochloride hydrate (EFN) is an ornithine derivative with an activity that is specific against Trypanosoma brucei gambiense [4]. Not many works have been reported on the antitrypanosomiasis activity of eflornithine hydrochloride hydrate, as a complex drug

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