A highly efficient and AIE-active theranostic agent from natural herbs

Fluorescence-based theranostics provides a powerful platform for effective diagnosis and therapy. In particular, luminogens with aggregation-induced emission (AIE) characteristics have triggered state-of-the-art developments in theranostics, thanks to their intrinsic properties, including high signal-to-noise ratios, high photostability and capability as photosensitizing agents. However, the development of AIE luminogens for biological applications mostly stays at rational design and preparation through organic synthesis, which may give rise to high cost, environmental destruction and potential cytotoxicity. Actually, with easy access and good biocompatibility, it would be of great interest to employ AIE-active natural agents from herbs in theranostics and pharmacodynamics studies through fluorescence imaging. In this work, the use of berberine chloride, an AIE-active natural product from herbal plants, as a theranostic agent towards both cancer cells and bacteria is investigated. Through fluorescence bio-imaging, berberine chloride selectively targets cancer cells over normal cells and discriminates Gram-positive against Gram-negative bacteria. Furthermore, light-driven organelle-targeting migration of berberine chloride from mitochondria to the nucleus was discovered. Therapeutic evaluation shows that berberine chloride can efficiently ablate cancer cells over normal cells, and kill Gram-positive bacteria through both in vitro and in vivo photodynamic therapy. This work thus provides a blueprint for the next generation of theranostics using natural AIE luminogens.