Isolation and Antitrypanosomal Characterization of Furoquinoline and Oxylipin from .

In the absence of vaccines, there is a need for alternative sources of effective chemotherapy for African trypanosomiasis (AT). The increasing rate of resistance and toxicity of commercially available antitrypanosomal drugs also necessitates an investigation into the mode of action of new antitrypanosomals for AT In this study, furoquinoline 4, 7, 8-trimethoxyfuro (2, 3-b) quinoline (compound ) and oxylipin 9-oxo-10, 12-octadecadienoic acid (compound ) were isolated from the plant species (Lam) Zepern and Timler (root), and their in vitro efficacy and mechanisms of action investigated in () the species responsible for AT. Both compounds resulted in a selectively significant growth inhibition of (compound , half-maximal effective concentration EC = 1.7 μM, selectivity indices SI = 74.9; compound , EC = 1.2 μM, SI = 107.3). With regards to effect on the cell cycle phases of , only compound significantly arrested the second growth-mitotic (G2-M) phase progression even though G2-M and DNA replication (S) phase arrest resulted in the overall reduction of cells in G0-G1 for both compounds. Moreover, both compounds resulted in the aggregation and distortion of the elongated slender morphology of . Analysis of antioxidant potential revealed that at their minimum and maximum concentrations, the compounds exhibited significant oxidative activities in (compound , 22.7 μM Trolox equivalent (TE), 221.2 μM TE; compound , 15.0 μM TE, 297.7 μM TE). Analysis of growth kinetics also showed that compound exhibited a relatively consistent growth inhibition of at different concentrations as compared to compound . The results suggest that compounds and are promising antitrypanosomals with the potential for further development into novel AT chemotherapy.