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

Xie S, Manuguri S, Proietti G, Romson J, Fu Y, Inge AK, Wu B, Zhang Y, Häll D, Ramström O, Yan M

Proc. Natl. Acad. Sci. U.S.A. 114 (32) 8464-8469 [2017-08-08; online 2017-07-25]

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

Affiliated researcher

PubMed 28743748

DOI 10.1073/pnas.1708556114

Crossref 10.1073/pnas.1708556114

pii: 1708556114
pmc: PMC5559051

Publications 9.5.0