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Design and synthesis of theranostic antibiotic nanodrugs that display enhanced antibacterial activity and luminescence
KTH, School of Chemical Science and Engineering (CHE), Chemistry.
KTH, School of Chemical Science and Engineering (CHE), Chemistry.
KTH, School of Chemical Science and Engineering (CHE), Chemistry, Organic Chemistry.
KTH, School of Chemical Science and Engineering (CHE), Chemistry, Organic Chemistry.
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2017 (English)In: Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, E-ISSN 1091-6490, Vol. 114, no 32, p. 8464-8469Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
National Academy of Sciences , 2017. Vol. 114, no 32, p. 8464-8469
Keywords [en]
Aggregation-induced emission, Fluoroquinolones, Nanodrugs
National Category
Organic Chemistry
Identifiers
URN: urn:nbn:se:kth:diva-212259DOI: 10.1073/pnas.1708556114Scopus ID: 2-s2.0-85026889484OAI: oai:DiVA.org:kth-212259DiVA, id: diva2:1134978
Funder
Science for Life Laboratory - a national resource center for high-throughput molecular bioscience
Note

QC 20170822

Available from: 2017-08-22 Created: 2017-08-22 Last updated: 2017-08-22Bibliographically approved

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Xie, ShengManuguri, SeshaProietti, GiampieroRomson, JoakimFu, YingZhang, YangHäll, DanielRamström, OlofYan, Mingdi
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