In Vitro Activity of wALADin Benzimidazoles against Different Life Cycle Stages of Plasmodium Parasites

被引：4

作者：

Lentz, Christian S. ^{[1
]}

Sattler, Julia M. ^{[2
]}

Fendler, Martina ^{[1
]}

Gottwalt, Simon ^{[2
]}

Halls, Victoria S. ^{[3
]}

Strassel, Silke ^{[1
]}

Arriens, Sandra ^{[1
]}

Hannam, Jeffrey S. ^{[3
]}

Specht, Sabine ^{[1
]}

Famulok, Michael ^{[3
]}

Mueller, Ann-Kristin ^{[2
]}

Hoerauf, Achim ^{[1
]}

Pfarr, Kenneth M. ^{[1
]}

机构：

[1] Univ Hosp Bonn, Inst Med Microbiol Immunol & Parasitol, Bonn, Germany

[2] Univ Heidelberg Hosp, Dept Infect Dis, Parasitol Unit, Heidelberg, Germany

[3] Univ Bonn, LIMES Inst, Chem Biol & Med Chem Unit, Bonn, Germany

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2015年 / 59卷 / 01期

关键词：

AMINOLEVULINIC-ACID DEHYDRATASE; HEME-BIOSYNTHESIS; MALARIAL PARASITE; FALCIPARUM; MOTILITY; SURFACE; CELL;

D O I：

10.1128/AAC.02383-14

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

wALADin1 benzimidazoles are specific inhibitors of delta-aminolevulinic acid dehydratase from Wolbachia endobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stage Plasmodium falciparum in vitro (50% inhibitory concentrations, 39, 7.7, and 12.8 mu M, respectively). One of these derivatives inhibited gliding motility of Plasmodium berghei ANKA infectious sporozoites with nanomolar affinity and blocked invasion into hepatocytes but did not affect intrahepatocytic replication. Hence, wALADin1 benzimidazoles are tools to study gliding motility and potential antiplasmodial drug candidates.

引用

页码：654 / 658

页数：5

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