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作为细胞运输剂的宿主-[2] 转素
Vadims Dvornikovs1, Brian E House, Marcia Kaetzel
1Department of Chemistry, University of Cincinnati, Cincinnati, Ohio 45221, USA.
Journal of the American Chemical Society
|July 3, 2003
概括
宿主-[2]rotaxanes,具有双-24-皇冠-8以太环,作为有效的细胞运输剂. 它们有效地结合氨基酸和光体,促进细胞吸收,包括核运输.
科学领域:
- 超分子化学 超分子化学
- 化学生物学 化学生物学
- 材料科学 材料科学 材料科学
背景情况:
- 宿主[2] 罗塔克桑是设计的超分子结构,在分子运输中具有潜在的应用.
- 迪本佐-24-皇冠-8 (DB24C8) 乙烯和旋部分是影响宿主-客人相互作用的关键组成部分.
- 了解这些罗塔克桑的结合亲缘关系和运输能力对于它们的发展至关重要.
研究的目的:
- 在不同的溶剂系统中,研究宿主-[2]rotaxanes与各种客体的结合亲缘关系.
- 为了评估这些罗塔克桑对生物相关分子的细胞运输效率.
- 为了比较不同轮素架构的运输能力.
主要方法:
- 宿主-[2]rotaxanes与环法或芳香裂阻断组的合成和表征.
- 在水性缓冲体,DMSO和混合溶剂系统中测定异常结合常数 (K(A)) 的光谱测定.
- 细胞吸收研究使用光标记客人和COS-7细胞来评估运输效率.
主要成果:
- 宿主-[2]罗塔克桑在测试溶剂中表现出强烈的关联常数 (10^4到10^5M^-1) 对于性客体和光体.
- 与单独的旋风组件相比,罗塔xane架构增强了客人结合.
- 旋风-[2] 罗他森1有效地将光素和光素-PKC抑制剂运输到COS-7细胞中,包括细胞核.
- 裂-[2]rotaxane 2尽管具有相似的结合亲和力,但其光素运输效率较低,这表明细胞传递依赖于结构.
结论:
- 宿主-[2] 转素是有效的分子转运体,能够与高亲和力结合多样化的客体.
- 罗他素结构有利于分子识别和结合.
- 特定的罗塔xane 架构显著影响细胞吸收效率,突出了结构设计对于有针对性的传递的重要性.
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