title: Simultaneous administration of 2-aminoethyl diphenylborinate and chloroquine reverses chloroquine resistance in malaria parasites.
abstract: A nearly complete reversal of chloroquine (CQ) resistance in the CQ-resistant Plasmodium falciparum K-1 strain, with a significant decrease in the mean ± standard deviation (SD) 50% inhibitory concentration (IC50) from 1,050 ± 95 nM to 14 ± 2 nM, was achieved in vitro by the simultaneous administration of 2-aminoethyl diphenylborinate (2-APB). The CQ resistance-reversing activity of 2-APB, which showed the same efficacy as verapamil, was also observed in an in vivo mouse infection model with the CQ-resistant Plasmodium chabaudi AS(30CQ) strain.
authors.affiliation: National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Hokkaido, Japan The United Graduate School of Veterinary Sciences, Gifu University, Gifu, Japan College of Veterinary Medicine, Sudan University of Science and Technology, Khartoum, Sudan.
authors.forename: Ehab
authors.initials: E
authors.lastname: Mossaad
authors.affiliation: National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Hokkaido, Japan.
authors.forename: Wakako
authors.initials: W
authors.lastname: Furuyama
authors.affiliation: Princess Margaret Cancer Centre, Toronto, Canada.
authors.forename: Masahiro
authors.initials: M
authors.lastname: Enomoto
authors.affiliation: Laboratory of Tropical Medicine and Parasitology, Dokkyo Medical University, Tochigi, Japan.
authors.forename: Satoru
authors.initials: S
authors.lastname: Kawai
authors.affiliation: Laboratory for Developmental Neurobiology, RIKEN Brain Science Institute, Saitama, Japan.
authors.forename: Katsuhiko
authors.initials: K
authors.lastname: Mikoshiba
authors.affiliation: National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Hokkaido, Japan skawazu@obihiro.ac.jp.
authors.forename: Shin-ichiro
authors.initials: S
authors.lastname: Kawazu
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D002738:Chloroquine / Q000627:therapeutic use*; D005260:Female; D020128:Inhibitory Concentration 50; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D008813:Mice, Inbred ICR; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000472:pathogenicity*; D014700:Verapamil / Q000627:therapeutic use
chemical_list: D000962:Antimalarials; D002738:Chloroquine; D014700:Verapamil