Plasmepsin II inhibitory activity of alkoxylated and hydroxylated chalcones.
Sixteen antimalarial alkoxylated and hydroxylated chalcones were tested for their ability to inhibit recombinant plasmepsin II in vitro. The best inhibitory compounds had either a chloro or dimethylamino group at the 4-position of phenyl ring A in the chalcone template. Combination of the chalcones with chloroquine showed additivity or mild antagonism of Plasmodium falciparum K1 growth in culture.
Sriwilaijaroen
Nongluk
N
Department of Biochemistry, Faculty of Science, Mahidol University, Bangkok, Thailand.
Liu
Mei
M
Go
Mei-Lin
ML
Wilairat
Prapon
P
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002738:Chloroquine / Q000633:toxicity*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D015800:Protozoan Proteins
D000962:Antimalarials; D047188:Chalcones; D015800:Protozoan Proteins; D002738:Chloroquine; D016282:Aspartic Acid Endopeptidases; C100637:plasmepsin II