Heteroleptic Oxidovanadium(V) Complexes with Activity against Infective and Non-Infective Stages of Trypanosoma cruzi

Abstract

Five heteroleptic compounds, [VVO(IN-2H)(L-H)], where L are 8-hydroxyquinoline derivatives and IN is a Schiff base ligand, were synthesized and characterized in both the solid and solution state. The compounds were evaluated on epimastigotes and trypomastigotes of Trypanosoma cruzi as well as on VERO cells, as a mammalian cell model. Compounds showed activity against trypomastigotes with IC50 values of 0.29–3.02 μM. IN ligand and the new [VVO2(IN-H)] complex showed negligible activity. The most active compound [VVO(IN-2H)(L2-H)], with L2 = 5-chloro-7-iodo-8-hydroxyquinoline, showed good selectivity towards the parasite and was selected to carry out further biological studies. Stability studies suggested a partial decomposition in solution. [VVO(IN-2H)(L2-H)] affects the infection potential of cell-derived trypomastigotes. Low total vanadium uptake by parasites and preferential accumulation in the soluble proteins fraction were determined. A trypanocide effect was observed when incubating epimastigotes with 10 × IC50 values of [VVO(IN-2H)(L2-H)] and the generation of ROS after treatments was suggested. Fluorescence competition measurements with DNA:ethidium bromide adduct showed a moderate DNA interaction of the complexes. In vivo toxicity study on C. elegans model showed no toxicity up to a 100 μM concentration of [VVO(IN-2H)(L2-H)]. This compound could be considered a prospective anti-T. cruzi agent that deserves further research.

Copper(I)‐Thiosemicarbazone Complexes with Dual Anticancer and Antiparasitic Activity

“…Dose‐response curves were recorded and the IC 50 values were determined using GraphPad Prism version 6.00 for Windows (GraphPad Software, La Jolla California USA). The results were presented as mean±SD (standard deviation) of three independent biological replicates [56] …”

“…Plates were kept for 15 min with agitation and absorbance was measured at 570 nm in a Thermo Scientific Varioskan® Flash Multimode instrument. Each assay was performed three times [51–53,56] …”

“…The results were presented as mean � SD (standard deviation) of three independent biological replicates. [56]…”

Multifunctional organometallic compounds for the treatment of Chagas disease: Re(i) tricarbonyl compounds with two different bioactive ligands

“…The results are presented as averages ± SD (standard deviation) of three independent biological replicates. 61 Nifurtimox (Nfx) was used as the reference anti- T. cruzi drug. Dose–response curves were recorded and the IC 50 values were determined using GraphPad Prism version 6.00 for Windows (GraphPad Software, La Jolla California USA).…”

Eco-Friendly Synthesis of an Oxovanadium(IV)-bis(abietate) Complex with Antimicrobial Action

“…For instance, Datta et al [ 19 ] cited the oxovanadium(IV) complex [VO(C 16 H 15 N 4 O 8 S)HSO 4 ] incorporated into the antibiotic cefuroxime as a potential antioxidant and antibacterial agent. Another five compounds encompassing vanadium oxide, 8-hydroxyquinoline derivatives, and the Schiff base ligand, were also reported and studied in vitro against Trypanosoma cruzi , being classified as a potential agent against protozoan [ 20 ]. Vanadium is also related to the treatment of diabetes because they are a potent hypoglycemic agent.…”