Raj Shweta, Sasidharan Santanu, Tripathi Timir, Saudagar Prakash
Department of Biotechnology, National Institute of Technology-Warangal, Warangal 506004, India.
Molecular and Structural Biophysics Laboratory, Department of Biochemistry, North-Eastern Hill University, Shillong 793022, India.
Int J Biol Macromol. 2022 Apr 30;205:211-219. doi: 10.1016/j.ijbiomac.2022.02.047. Epub 2022 Feb 17.
Current treatments for leishmaniasis involve various drugs, including miltefosine and amphotericin B, which are associated with several side effects and high costs. Long-term use of these drugs may lead to the development of resistance, thereby reducing their efficiency. Chrysin (CHY) is a well-known, non-toxic flavonoid with antioxidant, antiviral, anti-inflammatory, anti-cancer, hepatoprotective, and neuroprotective properties. Recently we have shown that CHY targets the MAP kinase 3 enzyme of Leishmania and neutralizes the parasite rapidly. However, CHY is associated with low bioavailability, poor absorption, and rapid excretion issues, limiting its usage. In this study, we developed and tested a novel CHY-gold nanoformulation with improved efficacy against the parasites. The reducing power of CHY was utilized to reduce and conjugate with gold nanoparticles. Gold nanoparticles, which are already known for their anti-leishmanial properties, along with conjugated CHY, exhibited a decreased parasite burden in mammalian macrophages. Our findings showed that this biofunctionalized nanoformulation could be used as a potential therapeutic tool against leishmaniasis.
目前治疗利什曼病的方法包括使用多种药物，如米替福新和两性霉素B，这些药物会带来多种副作用且成本高昂。长期使用这些药物可能会导致耐药性的产生，从而降低其疗效。白杨素（CHY）是一种著名的无毒类黄酮，具有抗氧化、抗病毒、抗炎、抗癌、肝脏保护和神经保护特性。最近我们发现CHY作用于利什曼原虫的丝裂原活化蛋白激酶3酶，并能迅速消灭该寄生虫。然而，CHY存在生物利用度低、吸收差和排泄快等问题，限制了其应用。在本研究中，我们开发并测试了一种新型的CHY-金纳米制剂，其对寄生虫的疗效有所提高。利用CHY的还原能力来还原金纳米颗粒并与之结合。金纳米颗粒本身就因其抗利什曼原虫特性而闻名，与结合的CHY一起，在哺乳动物巨噬细胞中显示出寄生虫负荷降低。我们的研究结果表明，这种生物功能化的纳米制剂可作为治疗利什曼病的潜在治疗工具。
