Chen Nanhua, LaCrue Alexis N, Teuscher Franka, Waters Norman C, Gatton Michelle L, Kyle Dennis E, Cheng Qin
Drug Resistance and Diagnostics, Australian Army Malaria Institute, Brisbane, Australia.
Department of Global Health, University of South Florida, Tampa, Florida, USA.
Antimicrob Agents Chemother. 2014 Aug;58(8):4773-81. doi: 10.1128/AAC.02647-14. Epub 2014 Jun 9.
Artemisinin (ART)-based combination therapy (ACT) is used as the first-line treatment of uncomplicated falciparum malaria worldwide. However, despite high potency and rapid action, there is a high rate of recrudescence associated with ART monotherapy or ACT long before the recent emergence of ART resistance. ART-induced ring-stage dormancy and recovery have been implicated as possible causes of recrudescence; however, little is known about the characteristics of dormant parasites, including whether dormant parasites are metabolically active. We investigated the transcription of 12 genes encoding key enzymes in various metabolic pathways in P. falciparum during dihydroartemisinin (DHA)-induced dormancy and recovery. Transcription analysis showed an immediate downregulation for 10 genes following exposure to DHA but continued transcription of 2 genes encoding apicoplast and mitochondrial proteins. Transcription of several additional genes encoding apicoplast and mitochondrial proteins, particularly of genes encoding enzymes in pyruvate metabolism and fatty acid synthesis pathways, was also maintained. Additions of inhibitors for biotin acetyl-coenzyme A (CoA) carboxylase and enoyl-acyl carrier reductase of the fatty acid synthesis pathways delayed the recovery of dormant parasites by 6 and 4 days, respectively, following DHA treatment. Our results demonstrate that most metabolic pathways are downregulated in DHA-induced dormant parasites. In contrast, fatty acid and pyruvate metabolic pathways remain active. These findings highlight new targets to interrupt recovery of parasites from ART-induced dormancy and to reduce the rate of recrudescence following ART treatment.
以青蒿素(ART)为基础的联合疗法(ACT)被用作全球非复杂性恶性疟原虫疟疾的一线治疗方法。然而,尽管其效力高且起效迅速,但在最近出现ART耐药性之前很久,ART单药治疗或ACT就存在较高的复发率。ART诱导的环状体休眠和复苏被认为是复发的可能原因;然而,关于休眠寄生虫的特征,包括休眠寄生虫是否具有代谢活性,人们知之甚少。我们研究了双氢青蒿素(DHA)诱导的休眠和复苏过程中恶性疟原虫各种代谢途径中12种关键酶编码基因的转录情况。转录分析表明,暴露于DHA后,10个基因立即下调,但编码质体和线粒体蛋白的2个基因持续转录。几个额外的编码质体和线粒体蛋白的基因,特别是编码丙酮酸代谢和脂肪酸合成途径中酶的基因的转录也得以维持。添加脂肪酸合成途径中生物素乙酰辅酶A(CoA)羧化酶和烯酰-酰基载体还原酶的抑制剂,分别使DHA处理后休眠寄生虫的复苏延迟了6天和4天。我们的结果表明,在DHA诱导的休眠寄生虫中,大多数代谢途径下调。相比之下,脂肪酸和丙酮酸代谢途径仍然活跃。这些发现突出了新的靶点,可用于阻断寄生虫从ART诱导的休眠中复苏,并降低ART治疗后的复发率。