Department of Medical Parasitology and Mycology, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran.
Exp Parasitol. 2013 Oct;135(2):344-9. doi: 10.1016/j.exppara.2013.07.018. Epub 2013 Aug 6.
Pentavalent antimonial compounds have been the first line therapy for leishmaniasis; unfortunately the rate of treatment failure of anthroponotic cutaneous leishmaniasis (ACL) is increasing due to emerging of drug resistance. Elucidation of the molecular mechanisms operating in antimony resistance is critical for development of new strategies for treatment. Here, we used a cDNA-AFLP approach to identify gene(s) which are differentially expressed in resistant and sensitive Leishmania tropica field isolates. We identified five genes, aquaglyceroporin (AQP1) acts in drug uptake, ATP-binding cassette (ABC) transporter (MRPA) involved in sequestration of drug, phosphoglycerate kinase (PGK) implicated in glycolysis metabolism, mitogen activated protein kinase (MAPK) and protein tyrosine phosphatase (PTP) responsible for phosphorylation pathway. The results were confirmed using real time RT-PCR which revealed an upregulation of MRPA, PTP and PGK genes and downregulation of AQP1 and MAPK genes in resistant isolate. To our knowledge, this is the first report of identification of PTP and PGK genes potentially implicated in resistance to antimonials. Our findings support the idea that distinct biomolecules might be involved in antimony resistance in L. tropica field isolates.
五价锑化合物一直是治疗利什曼病的一线药物;不幸的是,由于耐药性的出现,人源皮肤利什曼病(ACL)的治疗失败率正在增加。阐明在锑耐药中起作用的分子机制对于开发新的治疗策略至关重要。在这里,我们使用 cDNA-AFLP 方法来鉴定在耐药和敏感的利什曼热带田间分离株中差异表达的基因。我们鉴定了五个基因,水甘油通道蛋白(AQP1)在药物摄取中起作用,ATP 结合盒(ABC)转运蛋白(MRPA)参与药物隔离,磷酸甘油激酶(PGK)参与糖酵解代谢,丝裂原激活蛋白激酶(MAPK)和蛋白酪氨酸磷酸酶(PTP)负责磷酸化途径。使用实时 RT-PCR 对结果进行了验证,结果显示耐药分离株中 MRPA、PTP 和 PGK 基因上调,AQP1 和 MAPK 基因下调。据我们所知,这是首次报道 PTP 和 PGK 基因可能与抗锑耐药有关。我们的研究结果支持这样一种观点,即不同的生物分子可能参与利什曼热带田间分离株的锑耐药。