Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden.
Department of Applied Physics, Science for Life Laboratory, KTH Royal Institute of Technology, SE-171 21, Solna, Sweden.
Proc Natl Acad Sci U S A. 2017 Aug 8;114(32):8464-8469. doi: 10.1073/pnas.1708556114. Epub 2017 Jul 25.
We report the modular formulation of ciprofloxacin-based pure theranostic nanodrugs that display enhanced antibacterial activities, as well as aggregation-induced emission (AIE) enhancement that was successfully used to image bacteria. The drug derivatives, consisting of ciprofloxacin, a perfluoroaryl ring, and a phenyl ring linked by an amidine bond, were efficiently synthesized by a straightforward protocol from a perfluoroaryl azide, ciprofloxacin, and an aldehyde in acetone at room temperature. These compounds are propeller-shaped, and upon precipitation into water, readily assembled into stable nanoaggregates that transformed ciprofloxacin derivatives into AIE-active luminogens. The nanoaggregates displayed increased luminescence and were successfully used to image bacteria. In addition, these nanodrugs showed enhanced antibacterial activities, lowering the minimum inhibitory concentration (MIC) by more than one order of magnitude against both sensitive and resistant The study represents a strategy in the design and development of pure theranostic nanodrugs for combating drug-resistant bacterial infections.
我们报告了基于环丙沙星的纯治疗性纳米药物的模块化制剂，该药物显示出增强的抗菌活性，以及聚集诱导发射（AIE）增强，成功用于细菌成像。这些药物衍生物由环丙沙星、全氟芳基环和通过亚胺键连接的苯基环组成，通过从全氟芳基叠氮化物、环丙沙星和醛在丙酮中的直接方案在室温下高效合成。这些化合物呈推进器形状，在沉淀到水中时，很容易组装成稳定的纳米聚集体，将环丙沙星衍生物转化为 AIE 活性发光体。纳米聚集体显示出增强的发光性，并成功用于细菌成像。此外，这些纳米药物显示出增强的抗菌活性，使最低抑菌浓度（MIC）降低了一个数量级以上，对敏感和耐药的细菌均有效。该研究代表了设计和开发用于对抗耐药性细菌感染的纯治疗性纳米药物的一种策略。
