Antiplasmodial activity of short peptide-based compounds

作者：Mahindra Amit; Gangwal Rahul P; Bansal Sunil; Goldfarb Nathan E; Dunn Ben M; Sangamwar Abhay T; Jain Rahul^*

来源：RSC Advances, 2015, 5(29): 22674-22684.

DOI：10.1039/c5ra00779h

Three series of short peptide-based compounds were synthesized, which upon evaluation against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum in vitro, produced IC50 values ranging between 1.4-4.7 mu g mL(-1). Importantly, higher antimalarial activity against the drug-resistant strain of P. falciparum (W2) was observed for the tested peptides, indicating their potential in the treatment of drug-resistant malaria parasites. The lack of cytotoxicity in all tested peptides provides evidence of their safety profile. The selected peptides were evaluated in an enzymatic inhibitory assay against plasmepsin II, a potential target for antiplasmodial activity, also indicated from the results of the molecular docking studies.

• 出版日期2015