Targeted Ultrasound-Assisted Cancer-Selective Chemical Labeling and Subsequent Cancer Imaging using Click Chemistry.

ABSTRACT: Metabolic sugar labeling followed by the use of reagent-free click chemistry is an established technique for in?vitro cell targeting. However, selective metabolic labeling of the target tissues in?vivo remains a challenge to overcome, which has prohibited the use of this technique for targeted in?vivo applications. Herein, we report the use of targeted ultrasound pulses to induce the release of tetraacetyl N-azidoacetylmannosamine (Ac4 ManAz) from microbubbles (MBs) and its metabolic expression in the cancer area. Ac4 ManAz-loaded MBs showed great stability under physiological conditions, but rapidly collapsed in the presence of tumor-localized ultrasound pulses. The released Ac4 ManAz from MBs was able to label 4T1 tumor cells with azido groups and significantly improved the tumor accumulation of dibenzocyclooctyne (DBCO)-Cy5 by subsequent click chemistry. We demonstrated for the first time that Ac4 ManAz-loaded MBs coupled with the use of targeted ultrasound could be a simple but powerful tool for in?vivo cancer-selective labeling and targeted cancer therapies.

SUBMITTER: Wang H 

PROVIDER: S-EPMC4918225 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature