Biological Activity of Coumarin Derivatives as Anti-Leishmanial Agents.
Biological Activity of Coumarin Derivatives as Anti-Leishmanial Agents.
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DOI：
10.1371/journal.pone.0164585
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发表时间：
2016
期刊：
影响因子：
3.7
通讯作者：
Singh S
中科院分区：
文献类型：
--
作者：
Mandlik V;Patil S;Bopanna R;Basu S;Singh S
皮肤利什曼病每年影响近70万至130万人。由于缺乏适当的药物和日益严重的耐药性问题，这种疾病的治疗很困难。天然化合物，如香豆素作为补充治疗剂，除了目前的治疗方式。在这项研究中，我们已经进行了计算机筛选的香豆素衍生物和它们的抗利什曼原虫性能已被探索在体外和体内。其中一种化合物（化合物2）表现出杀利什曼活性，为了进一步研究其性质，开发了该化合物的纳米脂质体制剂。与未处理的小鼠相比，用化合物2处理BALB/c小鼠的皮肤损伤显示出显著减小的损伤尺寸（p<0.05），表明化合物2可能具有抗利什曼原虫的性质。
Cutaneous leishmaniasis affects nearly 0.7 to 1.3 million people annually. Treatment of this disease is difficult due to lack of appropriate medication and the growing problem of drug resistance. Natural compounds such as coumarins serve as complementary therapeutic agents in addition to the current treatment modalities. In this study, we have performed an in-silico screening of the coumarin derivatives and their anti-leishmanial properties has been explored both in-vitro and in-vivo. One of the compounds (compound 2) exhibited leishmanicidal activity and to further study its properties, nanoliposomal formulation of the compound was developed. Treatment of cutaneous lesions in BALB/c mice with compound 2 showed significantly reduced lesion size as compared to the untreated mice (p<0.05) suggesting that compound 2 may possess anti-leishmanial properties.
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