title: Antimalarial pharmacodynamics of chalcone derivatives in combination with artemisinin against Plasmodium falciparum in vitro.
abstract: Use of artemisinin based combination therapies (ACTs) is increasing in treatment of malaria. Their extensive and indiscriminate deployment will ultimately lead to selection of resistance. Thus, alternate ACTs are needed. We reported in vitro antimalarial potential of chalcone derivatives. A few potent chalcones were selected for their antimalarial interaction in combination with artemisinin in vitro. Combinations evaluated show synergistic or additive interactions. Chalcones act on broad range of asexual stages of the parasite. The synergistic combinations decrease hemozoin formation in parasitized erythrocytes. These combinations do not affect new permeation pathways induced in the host cells. This is the first report showing antiplasmodial interactions between artemisinin and synthetic chalcone azole derivatives. Thus, chalcones and artemisinin combinations open the possibility of novel ACTs.
authors.affiliation: Department of Zoology, North Campus, University of Delhi, New Delhi 110007, India.
authors.forename: Amit
authors.initials: A
authors.lastname: Bhattacharya
authors.forename: Lokesh C
authors.initials: LC
authors.lastname: Mishra
authors.forename: Manish
authors.initials: M
authors.lastname: Sharma
authors.forename: Satish K
authors.initials: SK
authors.lastname: Awasthi
authors.forename: Virendra K
authors.initials: VK
authors.lastname: Bhasin
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004338:Drug Combinations; D004357:Drug Synergism; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D006420:Hemeproteins / Q000378:metabolism; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D004338:Drug Combinations; D006420:Hemeproteins; C020753:hemozoin; D002599:Chalcone; C031327:artemisinin