Simultaneous Administration of 2-Aminoethyl Diphenylborinate and Chloroquine Reverses Chloroquine Resistance in Malaria Parasites | Zendy

Ehab Mossaad | Zendy; Wakako Furuyama | Zendy; Masahiro Enomoto | Zendy; Satoru Kawai | Zendy; Katsuhiko Mikoshiba | Zendy; Shinichiro Kawazu | Zendy

Open Access

Simultaneous Administration of 2-Aminoethyl Diphenylborinate and Chloroquine Reverses Chloroquine Resistance in Malaria Parasites

Author(s) -

Ehab Mossaad,

Wakako Furuyama,

Masahiro Enomoto,

Satoru Kawai,

Katsuhiko Mikoshiba,

Shinichiro Kawazu

Publication year - 2015

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.04805-14

Subject(s) - chloroquine , plasmodium chabaudi , plasmodium falciparum , malaria , verapamil , in vivo , pharmacology , strain (injury) , in vitro , ic50 , cross resistance , drug resistance , biology , virology , parasitemia , medicine , microbiology and biotechnology , immunology , biochemistry , calcium

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.

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