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首页> 外文期刊>The American Journal of Tropical Medicine and Hygiene >Antileishmanial Activity of Compounds Derived from the Medicines for Malaria Venture Open Access Box against Intracellular Leishmania major Amastigotes
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Antileishmanial Activity of Compounds Derived from the Medicines for Malaria Venture Open Access Box against Intracellular Leishmania major Amastigotes

机译：疟疾风险开放存取盒药物衍生的化合物对细胞内利什曼原虫主要变形虫的抗leishmanial活性。

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摘要

Leishmaniasis is a complex tropical disease caused by kinetoplastid parasitic protozoa of the genus Leishmania and is transmitted by the sand fly insect vector. Cutaneous leishmaniasis (CL) is the most common form of this disease, and CL infections often result in serious skin lesions and scars. CL remains a public health problem in many endemic countries worldwide because of the absence of effective, safe, and cost-effective drugs for treatment. One of the strategies we chose to use to find novel chemical entities worthy of further development as antileishmanials involved screening synthetic and natural products libraries. In our study, we developed a Leishmania major intracellular amastigote assay that uses the activity of luciferase as a measure of parasite proliferation and used this assay to screen a collection of 400 compounds obtained from Medicines for Malaria Venture (MMV) for their antileishmanial activity. Our results showed that 14 compounds identified by MMV as antimalarial drugs have antileishmanial activity and can potentially be optimized for CL drug development.
机译：利什曼病是一种由利什曼原虫属的运动质体寄生原生动物引起的复杂热带病，由沙蝇昆虫媒介传播。皮肤利什曼病（CL）是该疾病的最常见形式，CL感染通常会导致严重的皮肤损伤和疤痕。由于缺乏有效，安全和合算的治疗药物，CL在全球许多流行国家仍然是公共卫生问题。我们选择使用的一种策略来寻找值得进一步发展的新型化学实体，因为抗污药涉及筛选合成和天然产物库。在我们的研究中，我们开发了一种利什曼原虫主要的胞内鞭毛虫测定方法，该方法利用萤光素酶的活性作为寄生虫增殖的量度，并使用该方法筛选了从疟疾药物公司（MMV）获得的400种化合物的抗疟疾活性。我们的结果表明，由MMV鉴定为抗疟药的14种化合物具有抗疟疾活性，可以针对CL药物开发进行优化。

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