作为一种强大的UVA化疗剂的2,4-二二甲基胺
Marvin Pollum1, Steffen Jockusch, Carlos E Crespo-Hernández
1Department of Chemistry and Center for Chemical Dynamics, Case Western Reserve University , Cleveland, Ohio 44106, United States.
Journal of the American Chemical Society
|December 16, 2014
概括
在胺衍生物中替代硫会产生强大的光敏剂. 2,4-Dithiothymine 呈现出超快的三倍体状态和高单元氧生成,表明其作为有效的UVA化疗剂的潜力.
科学领域:
- 摄影化学的使用.
- 生物物理化学 生物物理化学
- 药用化学 医学化学
背景情况:
- 胺衍生物在DNA和光生物学中至关重要.
- 了解修改核基的光物理性质是开发新治疗剂的关键.
- 核基中硫的替代可以显著改变其电子和光物理特性.
研究的目的:
- 研究硫替代的胺衍生物的光物理性质,特别是2-thiothymine,4-thiothymidine和2,4-dithiothymine.
- 为了比较这些化合物的光敏化能力与天然的提米丁.
- 评估2,4-二二二二胺作为UVA化疗剂的潜力.
主要方法:
- 紫外线-Vis吸收光谱法用于确定光谱变化.
- 五秒短暂吸收光谱用于研究超快速兴奋状态动态和系统间交叉 (ISC).
- 纳米秒时间分辨率的发光光谱测量单点氧气生成.
主要成果:
- 硫的替代导致了吸收光谱的显著红色变化,2,4-二二二胺在363nm显示最大值.
- 2,4-Dithiothymine表现出180 ± 40 fs的超快速系统间交叉寿命,这是DNA基衍生物中记录的最短寿命.
- 胺衍生物显示显著增加了系统间交叉率和接近单元的三倍产量,导致强烈的光敏化.
- 4 - 硫胺胺和2,4-二硫胺是高效的单片氧气生成器,具有高量子产量 (0.42-0.46).
结论:
- 硫的替代大大提高了胺的光物理性质,将其转化为一个高效的光敏感剂.
- 2,4-dithiothymine的近单位的三倍产量和高效的单一氧气生成表明它在UVA化疗中优于4-thiothymidine.
- 2,4-Dithiothymine作为一种更有效的化疗剂具有前景,特别是在更深层组织应用中.
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