我们报道了合成和表征一种红光活化的金纳米粒子，它被功能化为生物素化铜（II）配合物，并具有通用分子式[Cu（L3）（L6）] - AuNPs（生物素-Cu @AuNP）。其中L3 =N-（3-（（E）-3,5-二叔丁基-2-羟基苯甲醛亚胺）-4-羟基苯基）-5-（（3aS，4S，6aR）-2-氧代己螺（3,4-d）咪唑- 4-基）戊酰胺，L6 = 5-（1,2-二硫杂环戊烷-3-基）-N-（1,10-邻菲啰啉-5-基）戊酰胺。我们研究了其光物理，理论和光细胞毒潜力。纳米共轭物在生物素阳性和生物素阴性的癌细胞以及正常细胞中的摄取不同。纳米共轭物还在红光下（600-720 nm，30 Jcm-2）照射下表现出对生物素阳性的A549（IC50：13 μg / mL；黑暗中> 150 μg / mL）和HaCaT（IC50：23 μg / mL；黑暗中> 150 μg / mL）细胞的显着光动力活性，具有显著的高光学指数（PI> 15）。纳米共轭物对HEK293T（生物素阴性）和HPL1D（正常）细胞的毒性较小。共聚焦显微镜证实生物素-Cu @AuNP在A549细胞中有选择性的线粒体和部分细胞质定位。几项光物理和理论研究揭示了红光辅助产生单线态氧（1O2）（Ф（1O2）= 0.68）作为反应性氧化物质（ROS），从而导致明显的氧化应激和线粒体膜损伤，并导致A549细胞的caspase 3/7依赖性凋亡。总体而言，展示出红光辅助靶向光动力学活性的纳米复合物（生物素-Cu @AuNP）成为理想的下一代PDT药剂。版权所有 © 2023 Elsevier Inc. 保留所有权利。

We report the synthesis and characterization of red-light activable gold nanoparticle functionalized with biotinylated copper(II) complex of general molecular formula, [Cu(L3)(L6)]-AuNPs (Biotin-Cu@AuNP), where L3 = N-(3-((E)-3,5-di-tert-butyl-2-hydroxybenzylideneamino)-4-hydroxyphenyl)-5-((3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, L6 = 5-(1,2-dithiolan-3-yl)-N-(1,10-phenanthrolin-5-yl)pentanamide, which was explored for their photophysical, theoretical and photo-cytotoxic potentials. The nanoconjugate exhibits differential uptake in biotin positive and biotin negative cancer cells as well as normal cells. The nanoconjugate also shows remarkable photodynamic activity against biotin positive A549 (IC50: 13 μg/mL in red light; >150 μg/mL in dark) and HaCaT (IC50: 23 μg/mL in red light; >150 μg/mL in dark) cells under red light (600-720 nm, 30 Jcm-2) irradiation, with significantly high photo-indices (PI>15). The nanoconjugate is less toxic to HEK293T (biotin negative) and HPL1D (normal) cells. Confocal microscopy confirms preferential mitochondrial and partly cytoplasmic localization of Biotin-Cu@AuNP in A549 cells. Several photo-physical and theoretical studies reveal the red light-assisted generation of singlet oxygen (1O2) (Ф (1O2) =0.68) as a reactive oxygen species (ROS) which results in remarkable oxidative stress and mitochondrial membrane damage, leading to caspase 3/7-dependent apoptosis of A549 cells. Overall, the nanocomposite (Biotin-Cu@AuNP) exhibiting red light-assisted targeted photodynamic activity has emerged as the ideal next generation PDT agents.Copyright © 2023 Elsevier Inc. All rights reserved.