Simultaneous administration of 2-aminoethyl diphenylborinate and chloroquine reverses chloroquine resistance in malaria parasites
Simultaneous administration of 2-aminoethyl diphenylborinate and chloroquine reverses chloroquine resistance in malaria parasites
复制标题
同时服用 2-氨基乙基二苯硼酸酯和氯喹可逆转疟原虫对氯喹的耐药性
DOI：
10.1128/aac.04805-14
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Kawazu S
中科院分区：
文献类型：
--
作者：
Mossaad E;Furuyama W;Enomoto M;Kawai S;Mikoshiba K;Kawazu S
通过同时给予二苯硼酸 2-氨基乙酯，在体外几乎完全逆转了耐 CQ 的恶性疟原虫 K-1 菌株中的氯喹 (CQ) 耐药性，平均±标准差 (SD) 50% 抑制浓度 (IC50) 从 1,050 ± 95 nM 显着降低至 14 ± 2 nM (2-APB)。 2-APB 的 CQ 抗性逆转活性与维拉帕米具有相同的功效，在 CQ 抗性 Plasmodium chabaudi AS(30CQ) 菌株的体内小鼠感染模型中也观察到了这一活性。
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 achievedin vitroby 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 anin vivomouse infection model with the CQ-resistant Plasmodium chabaudi AS(30CQ) strain.