Bifunctional aggregation-induced emission luminogen for monitoring and killing of multidrug-resistant bacteria
View Patent ↗Antibiotic compounds having both antibiotic and aggregation-induced emission (AIE) characteristics. The compounds comprise an azole antibiotic unit, for example naphthalimide triazole (NT), and an AIE unit, for example triphenylethylene (TriPE). The compounds act as an effective AIEgen with ROS generating capabilities. The present combinations of an azole antibiotic unit and an AIE unit do not negatively affect the antibacterial properties of the azole. Accordingly, the present compounds exterminate bacteria with both the antibacterial mechanism of the azole along with the ROS produced when the AIE unit is exposed to light. In addition, the intrinsic imagining ability of the present compounds enables them to be used as imaging tools to monitor the drug-bacteria interaction. Collectively, the present compounds provide multiple functions including imaging, monitoring, and bacterial infection inhibition for integrated diagnosis and treatment in clinical practices.
1 . An antibiotic compound capable of staining and killing Gram-positive and Gram-negative bacteria, comprising a compound that exhibit aggregation induced emission properties, wherein the compound comprises:
2 . A pharmaceutical composition comprising the antibiotic compound of claim 1 and a pharmaceutically acceptable carrier.
3 . The pharmaceutical composition of claim 2 , wherein the pharmaceutically acceptable carrier is a topical carrier.
4 . A method of treating a bacterial infection in a patient, comprising:
administering the compound of claim 1 to a site of an infection in a patient; and
illuminating the site of the infection to generate reactive oxygen species from the compound of claim 1 .
5 . The method of treating a bacterial infection in a patient according to claim 4 , wherein the site of the infection is illuminated with light for a duration of time in the range of 2 minutes to 30 minutes.
6 . The method of treating a bacterial infection in a patient according to claim 4 , wherein the illuminating comprises illuminating with white light.
7 . A method of generating reactive oxygen species, comprising:
administering the compound of claim 1 to a portion of an object; and
illuminating the portion of the object.
8 . The method of generating reactive oxygen species according to claim 7 , wherein the portion of the object is illuminated with white light for a duration of time in the range of 2 minutes to 30 minutes.
9 . A method of imaging antibiotic interaction with bacteria, comprising:
administering the compound of claim 1 to a bacterial infection; and
imaging the bacterial infection to view fluorescence produced from aggregation of the compound of claim 1 .