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一个生物模拟的菌体灵感的超分子系统,基于葡萄糖结合柱[5]与西普罗素化水化合物在一起
Yulia I Aleksandrova1, Dmitriy N Shurpik1, Arina V Pergat1
1Kazan Federal University, A.M. Butlerov Chemistry Institute, Kremlevskaya, 18, Kazan, 420008, Russian Federation. dnshurpik@mail.ru.
新的自我组装的宏环分子,支柱[5]arene,通过增强西普罗素,显示出对抗抗生素耐药性的潜力.
科学领域:
- 超分子化学 超分子化学
- 纳米技术纳米技术
- 抗菌研究 抗菌研究
背景情况:
- 抗生素耐药性是一个日益增长的全球健康威胁.
- 宏循环分子为新型药物递送系统提供了潜力.
- 受菌体启发的载体可以增强抗微生物药物的有效性.
研究的目的:
- 为了合成和表征一种新的水溶性支柱[5]arene与硫糖化物碎片.
- 为了研究支柱[5]arene与西普洛氨酸化物 (Cipro) 的自我组装和复杂化.
- 评估由此产生的高分子纳米结构的生物相容性和增强的抗菌活性.
主要方法:
- 支柱[5]arene的合成和与Cipro的复合.
- 紫外线和光光谱学用于复杂的固体测量和结合常量.
- 动态光散射 (DLS) 和传输电子显微镜 (TEM) 用于纳米结构的表征.
- 在癌症和正常细胞系的体外细胞毒性测定.
- 抗菌分析对抗抗素耐药的 *K.肺炎*.
主要成果:
- 一个新的水溶性支柱[5]arene被成功合成.
- 支柱[5]arene与Cipro (250-300 nm) 形成了稳定的超分子纳米结构.
- 支柱[5]arene/Cipro复合物对哺乳动物细胞的毒性较低.
- 观察到对抗耐药性 *K. pneumoniae* 的抑制作用增加了两倍.
- 分子对接表明,排泄抑制作为一个机制.
结论:
- 支柱[5]arene是开发自组装药物载体的有希望的支架.
- 这些纳米结构可以通过提高药物的疗效来克服抗生素耐药性.
- 该系统显示了下一代抗菌疗法的潜力.
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