Antimalarial evaluation of copper(II) nanohybrid solids: inhibition of plasmepsin II, a hemoglobin-degrading malarial aspartic protease from Plasmodium falciparum.

Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry
Subash Chandra MohapatraShyam Singh Chauhan

Abstract

A new class of copper(II) nanohybrid solids, LCu(CH(3)COO)(2) and LCuCl(2), have been synthesized and characterized by transmission electron microscopy, dynamic light scattering, and IR spectroscopy, and have been found to be capped by a bis(benzimidazole) diamide ligand (L). The particle sizes of these nanohybrid solids were found to be in the ranges 5-10 and 60-70 nm, respectively. These nanohybrid solids were evaluated for their in vitro antimalarial activity against a chloroquine-sensitive isolate of Plasmodium falciparum (MRC 2). The interactions between these nanohybrid solids and plasmepsin II (an aspartic protease and a plausible novel target for antimalarial drug development), which is believed to be essential for hemoglobin degradation by the parasite, have been assayed by UV-vis spectroscopy and inhibition kinetics using Lineweaver-Burk plots. Our results suggest that these two compounds have antimalarial activities, and the IC(50) values (0.025-0.032 microg/ml) are similar to the IC(50) value of the standard drug chloroquine used in the bioassay. Lineweaver-Burk plots for inhibition of plasmepsin II by LCu(CH(3)COO)(2) and LCuCl(2) show that the inhibition is competitive with respect to the substrate. The inhibition...Continue Reading

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Citations

Apr 10, 2013·Asian Pacific Journal of Tropical Biomedicine·S PonarulselvamS Thangamani
Aug 1, 2010·Expert Opinion on Drug Discovery·Kunal Roy, Probir Kumar Ojha
Sep 4, 2015·Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences·Clarence S Yah, Geoffrey S Simate
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Dec 22, 2011·Metallomics : Integrated Biometal Science·Clare Duncan, Anthony R White
Dec 2, 2020·Journal of Functional Biomaterials·Ekaterina O Mikhailova

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