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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Effect of fluorescent dyes on in vitro-differentiated, late-stage plasmodium falciparum gametocytes
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Effect of fluorescent dyes on in vitro-differentiated, late-stage plasmodium falciparum gametocytes

机译：荧光染料对体外分化的晚期恶性疟原虫配子细胞的影响

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Plasmodium falciparum gametocytes are not associated with clinical symptoms, but they are responsible for transmitting the pathogen to mosquitoes. Therefore, gametocytocidal interventions are important for malaria control and resistance containment. Currently available drugs and vaccines are not well suited for that purpose. Several dyes have potent antimicrobial activity, but their use against gametocytes has not been investigated systematically. The gametocytocidal activity of nine synthetic dyes and four control compounds was tested against stage V gametocytes of the laboratory strain 3D7 and three clinical isolates of P. falciparum with a bioluminescence assay. Five of the fluorescent dyes had submicromolar 50% inhibitory concentration (IC50) values against mature gametocytes. Three mitochondrial dyes, MitoRed, dihexyloxacarbocyanine iodide (DiOC6), and rhodamine B, were highly active (IC50s 200 nM). MitoRed showed the highest activity against gametocytes, with IC50s of 70 nM against 3D7 and 120 to 210 nM against clinical isolates. All compounds were more active against the laboratory strain 3D7 than against clinical isolates. In particular, the endoperoxides artesunate and dihydroartemisinin showed a 10-fold higher activity against 3D7 than against clinical isolates. In contrast to all clinically used antimalarials, several fluorescent dyes had surprisingly high in vitro activity against late-stage gametocytes. Since they also act against asexual blood stages, they shall be considered starting points for the development of new antimalarial lead compounds.
机译：恶性疟原虫配子体细胞与临床症状无关，但它们负责将病原体传播给蚊子。因此，杀细胞杀灭干预对控制疟疾和控制耐药性很重要。当前可用的药物和疫苗不适用于该目的。几种染料具有有效的抗菌活性，但尚未对它们对配子体细胞的用途进行系统的研究。使用生物发光测定法测试了9种合成染料和4种对照化合物对实验室菌株3D7的V期配子细胞和恶性疟原虫的3种临床分离株的杀细胞活性。五种荧光染料对成熟配子细胞具有亚微摩尔浓度的50％抑制浓度（IC50）值。三种线粒体染料MitoRed，碘化二己基氧杂碳菁氰（DiOC6）和若丹明B具有很高的活性（IC50 <200 nM）。 MitoRed对配子细胞表现出最高的活性，对3D7的IC50为70 nM，对临床分离株的IC50为120至210 nM。与实验室分离株相比，所有化合物对实验室菌株3D7的活性都更高。特别是，青蒿琥酯和二氢青蒿素的内过氧化物对3D7的活性比对临床分离株的活性高10倍。与所有临床使用的抗疟疾药物相比，几种荧光染料对后期配子细胞具有出乎意料的高体外活性。由于它们还可以对抗无性血液阶段，因此应将其视为开发新的抗疟铅化合物的起点。

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