Singh Neetu, Wadhawan Mohit, Tiwari Savitri, Kumar Ranjeet, Rathaur Sushma
Department of Biochemistry, Institute of Science, Banaras Hindu University, Varanasi 221005, India.
Department of Biochemistry, Institute of Science, Banaras Hindu University, Varanasi 221005, India.
Acta Trop. 2016 Jul;159:20-8. doi: 10.1016/j.actatropica.2016.03.004. Epub 2016 Mar 8.
Phenylarsine oxide (PAO), a specific protein tyrosine phosphatase (PTP) inhibitor significantly decreased the motility and viability of Setaria cervi ultimately leading to its death. The PTP activity present in the cytosolic and detergent soluble fractions as well as on surface of these parasites was significantly inhibited by PAO. A marked alteration in protein spots abundance after proteomic analysis showed 14 down-regulated and 9 upregulated spots in the treated parasites as compared to the control. The PTP inhibition led to increase in the cytosolic and mitochondrial calpain activity in these parasites. PAO also blocked the ATP generation in the parasite depicted by reduced activity of phosphoglycerate kinase and expression of enolase. An increased ROS level, induced lipid peroxidation/protein carbonyl formation and decreased activity of different antioxidant enzymes like thioredoxin reductase, glutathione reductase and glutathione transferases was also observed in the PAO treated parasites. PAO, thus disturbs the overall homeostasis of the filarial parasite by inhibiting PTPs. Thereby suggesting that these molecules could be used as a good chemotherapeutic target for lymphatic filariasis.
苯胂化氧(PAO)是一种特异性蛋白酪氨酸磷酸酶(PTP)抑制剂,可显著降低牛带绦虫的活力和生存能力,最终导致其死亡。PAO可显著抑制这些寄生虫胞质和去污剂可溶部分以及其表面的PTP活性。蛋白质组学分析后蛋白质斑点丰度的显著变化显示,与对照相比,处理后的寄生虫中有14个斑点下调,9个斑点上调。PTP抑制导致这些寄生虫胞质和线粒体钙蛋白酶活性增加。PAO还通过磷酸甘油酸激酶活性降低和烯醇化酶表达减少,表明寄生虫中的ATP生成受阻。在PAO处理的寄生虫中还观察到活性氧水平升高、脂质过氧化/蛋白质羰基形成增加以及硫氧还蛋白还原酶、谷胱甘肽还原酶和谷胱甘肽转移酶等不同抗氧化酶的活性降低。因此,PAO通过抑制PTPs扰乱了丝虫寄生虫的整体稳态。从而表明这些分子可作为淋巴丝虫病的良好化疗靶点。