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Recombinant C-Terminal Domains from Scorpine-like Peptides Inhibit the Plasmodium berghei Ookinete Development In Vitro
International Journal of Peptide Research and Therapeutics ( IF 2.5 ) Pub Date : 2020-10-30 , DOI: 10.1007/s10989-020-10130-7
Leonel Vargas-Jaimes , María Carmen Rodriguez , Rocío Argotte-Ramos , Víctor Rivelino Juárez-González , Nina Pastor , Catherine Cesa-Luna , Lourival D. Possani , Verónica Quintero-Hernández

Malaria is a parasitic disease, caused by protozoa of the genus Plasmodium, and is transmitted to humans through the bites of infected Anopheles mosquitoes. More than 200 million cases of malaria are reported annually and about 400,000 deaths worldwide. Currently, the use of antimalarial drugs has been efficient in most cases, however, resistance to these drugs is increasing, making it necessary and essential to have a new range of possible drugs or medicines to combat this disease. Scorpion venom contains peptides whose functions are now intensively studied. Some of these peptides are known as Scorpine-like, which have anti-bacterial and antiplasmodial properties as they have been described to inhibit the development of parasites responsible for malaria. Scorpine-like peptides are composed of two structural domains: one α-helical N-terminal domain, and a C-terminal domain with the cysteine-stabilized α/β motif, which confers the peptide the function of blocking potassium channels and/or anti-bacteria activity. In this work, two C-terminal domains from Scorpine-like peptides were constructed and expressed in Escherichia coli, and their function was analyzed. We were able to demonstrate that the recombinant C-terminal domains rCterVm and rCterHg showed antiplasmodial activity producing 60% and 90% inhibition, respectively, of Plasmodium berghei development at 1 µM and 0.15 µM concentration, which makes these peptides promising candidates against Malaria.



中文翻译:

来自蝎子样肽的重组C末端域抑制伯氏疟原虫Ookinete体外发展。

疟疾是由疟原虫属的原生动物引起的寄生虫病,并通过被感染的按蚊叮咬传播给人类。蚊子。每年报告超过2亿例疟疾病例,全世界范围内约有40万人死亡。当前,在大多数情况下抗疟药的使用是有效的,但是,对这些药物的抗药性正在增加,这使得有必要并且必不可少的是要有新的可能的药物或药物来对抗这种疾病。蝎毒含有肽,其功能现已得到深入研究。这些肽中的某些被称为Scorpine-like,具有抗菌和抗血浆特性,因为它们已被描述为抑制引起疟疾的寄生虫的发展。蝎子样肽由两个结构域组成:一个α螺旋N末端结构域和一个具有半胱氨酸稳定的α/β基序的C末端结构域,赋予肽阻断钾通道和/或抗菌活性的功能。在这项工作中,构建了两个来自Scorpine样肽的C末端结构域,并在其中表达大肠杆菌,及其功能进行了分析。我们能够证明重组C末端结构域rCterVm和rCterHg表现出抗疟原虫活性,分别在1 µM和0.15 µM浓度下对伯氏疟原虫的发育产生60%和90%的抑制作用,这使这些肽有望成为抗疟疾的候选药物。

更新日期:2020-10-30
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