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确定一个裂-[2]rotaxane的细胞内运输机制
Xiaofeng Bao1, Idit Isaacsohn, Angela F Drew
1Department of Chemistry, University of Cincinnati, Cincinnati, Ohio 45221, USA.
Journal of the American Chemical Society
|September 14, 2006
概括
罗塔克桑,机械分子机器,促进细胞物质运输. 它们的形状灵活性,特别是轮子的滑动运动,对于治疗剂的高效跨膜输送至关重要.
科学领域:
- 超分子化学 超分子化学
- 纳米技术纳米技术
- 细胞生物学 细胞生物学
背景情况:
- 罗塔克桑是相互锁定的分子架构,具有作为开关和传感器的潜在应用.
- 最近的发现强调了罗塔克桑作为细胞内物质运输的代理物的实用性.
- 需要阐明罗他森介导的跨膜传输机制.
研究的目的:
- 为了研究罗他素介导的跨膜传输的机制.
- 确定形状灵活性在客结合和细胞传递中的作用.
- 评估罗塔克桑在向药物输送方面的治疗潜力.
主要方法:
- 两维NMR光谱分析轮素形状.
- 化学修饰以创建一个形状锁定的罗塔xane.
- 在各种溶剂 (水性,DMSO,) 中进行客结合亲和力研究.
- 使用化和流细胞计的细胞吸收研究.
- 温度和ATP依赖性测定用于探测运输机制.
主要成果:
- 一种含有裂的轮素存在于"封闭"和"开放"的形状.
- 规格的灵活性提高了水溶液和DMSO溶液中的客体结合.
- 与灵活的罗塔桑相比,锁定型罗塔桑的转运效率降低.
- 实现了的高细胞吸收 (89-98%),这取决于罗他素度.
- 运输在很大程度上是温度和ATP独立的,这表明被动膜通道.
结论:
- 罗塔克桑轮的滑动运动对于细胞物质的传递至关重要.
- 罗塔克桑可以作为机械装置,增强客人协会和细胞吸收.
- 罗塔克桑代表了一个有前途的新类纳米设备,用于将治疗剂送入细胞.
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