Application of a cybLuc Aminoluciferin for Deep Tissue Bioluminescence Imaging in Rodent Models

Bioluminescent imaging (BLI) technology has been extensively applied due to various advantages such as noninvasiveness, high sensitivity and selectivity, excellent biocompatibility and real-time visualization and monitoring. The firefly luciferase (Fluc)/luciferin system, one of the principal bioluminescent systems, has been developed as a sensor for imaging biological processes. However, a limited number of Fluc substrates hamper the further application of firefly luciferase/luciferin systems for biomedical purposes. Here we describe an approach to synthesize a series of novel luciferin substrates (cyaLucs) that produced elevated bioluminescent signals in vitro. Furthermore, we demonstrate the high efficiency of N-cyclobutylaminoluciferin (cybLuc) with high light emission and long duration in deep tissue imaging by diagnosis of cerebral tumors in vivo in a rodent model.