Mandlik Vineetha, Patil Sohan, Bopanna Ramanamurthy, Basu Sudipta, Singh Shailza
National Centre for Cell Science, NCCS Complex, SP Pune University Campus, Ganeshkhind, Pune, India.
Department of Chemistry, Indian Institute of Science Education and Research (IISER), Pune, Pashan, Pune, India.
PLoS One. 2016 Oct 21;11(10):e0164585. doi: 10.1371/journal.pone.0164585. eCollection 2016.
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.
皮肤利什曼病每年影响近70万至130万人。由于缺乏合适的药物以及耐药性问题日益严重，这种疾病的治疗很困难。除了目前的治疗方式外，香豆素等天然化合物可作为辅助治疗剂。在本研究中，我们对香豆素衍生物进行了计算机模拟筛选，并在体外和体内探索了它们的抗利什曼原虫特性。其中一种化合物（化合物2）表现出杀利什曼原虫活性，为进一步研究其特性，开发了该化合物的纳米脂质体制剂。与未治疗的小鼠相比，用化合物2治疗BALB/c小鼠的皮肤损伤显示损伤大小显著减小（p<0.05），这表明化合物2可能具有抗利什曼原虫特性。
