Design and synthesis of theranostic antibiotic nanodrugs that display enhanced antibacterial activity and luminescence.

Autor:	Xie S; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Manuguri S; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Proietti G; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Romson J; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Fu Y; Department of Applied Physics, Science for Life Laboratory, KTH Royal Institute of Technology, SE-171 21, Solna, Sweden., Inge AK; Department of Materials and Environmental Chemistry, Stockholm University, S-10691, Stockholm, Sweden., Wu B; Department of Chemistry, University of Massachusetts, Lowell, MA 01854., Zhang Y; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Häll D; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden., Ramström O; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden; ramstrom@kth.se mingdi@kth.se., Yan M; Department of Chemistry, KTH Royal Institute of Technology, Teknikringen 30, S-10044, Stockholm, Sweden; ramstrom@kth.se mingdi@kth.se.; Department of Chemistry, University of Massachusetts, Lowell, MA 01854.
Jazyk:	angličtina
Zdroj:	Proceedings of the National Academy of Sciences of the United States of America [Proc Natl Acad Sci U S A] 2017 Aug 08; Vol. 114 (32), pp. 8464-8469. Date of Electronic Publication: 2017 Jul 25.
DOI:	10.1073/pnas.1708556114
Abstrakt:	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 Escherichia coli The study represents a strategy in the design and development of pure theranostic nanodrugs for combating drug-resistant bacterial infections. Competing Interests: The authors declare no conflict of interest.
Databáze:	MEDLINE
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