AIE-based gold nanostar-berberine dimer nanocomposites for PDT and PTT combination therapy toward breast cancer

作者：Li, Rong-Tian; Chen, Ming; Yang, Zi-Chuan; Chen, Yong-Jian; Huang, Nai-Han; Chen, Wen-Hua^*; Chen, Jun; Chen, Jin-Xiang^*

来源：Nanoscale, 2022, 14(27): 9818-9831.

DOI：10.1039/d2nr03408e

• NANOPARTICLES
• MEMBRANE
• CELLS

We designed and synthesized three new berberine-based compounds, namely, pyridine-2,6-dimethyl-/2,2'-bipyridine-3,3'-dimethyl-tethered berberine dimers BD1 and BD2, and a tetrakis(4-benzyl)ethylene linked berberine tetramer BD4. We identified that the dimer BD2 and tetramer BD4, as well as 1,10-phenanthroline-2,9-dimethyl-linked berberine dimer BD3 previously reported by us, showed remarkable aggregation-induced emission (AIE) properties which endowed them with higher singlet oxygen (O-1(2)) production ability than berberine. Of the four compounds, BD3 exhibits the lowest Delta E-ST energy with the highest O-1(2) generation ability and thus was selected for further construction of AuNSs-BD3@HA (denoted as ABH, AuNSs = gold nanostars; HA = hyaluronic acid). The nanosystem of ABH shows a remarkable therapeutic effect toward breast cancer by combining photodynamic therapy (PDT) from BD3, photothermal therapy (PTT) from AuNSs, and the CD44-targeting capability of HA. The synergistically enhanced PDT and PTT induce superior cancer cell apoptosis/necrosis in vitro and anti-breast cancer activity in vivo. This study provides a new concept for PDT using natural product derivatives and their combination with PTT for efficient treatment of tumors.

• 单位
  南方医科大学