Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing, 100190, PR China.
Org Biomol Chem. 2011 Jun 7;9(11):4168-75. doi: 10.1039/c0ob01278e. Epub 2011 Apr 14.
A series of polyethylene glycol-functionalized benzylidene cyclopentanone dyes with varying lipid/water partition coefficients were synthesized in high yields by a simple process. Detailed characterization and systematic studies of these molecules, including linear and nonlinear photophysical properties, reactive oxygen yields, and in vitro photodynamic therapy (PDT) activities, were conducted. Four of these dyes exhibited good solubility in PBS (>2 mg ml(-1), which is sufficient for clinical venous injection), high reactive oxygen yields, large two-photon absorption and low dark toxicity, under the therapy dosage. Among them, two dyes could be absorbed efficiently by human rectal cancer 1116 cells, and presented strong two-photon excited PDT activity in in vitro cell experiments.
一系列聚乙二醇功能化苯亚甲基环戊酮染料通过简单的过程以高产率合成，具有不同的脂/水分配系数。对这些分子进行了详细的表征和系统研究，包括线性和非线性光物理性质、活性氧产率以及体外光动力疗法（PDT）活性。其中四种染料在 PBS 中具有良好的溶解性（>2mgml(-1)，足以进行临床静脉注射），在治疗剂量下具有高活性氧产率、大双光子吸收和低暗毒性。其中两种染料可以被人直肠癌细胞 1116 有效吸收，并在体外细胞实验中表现出强烈的双光子激发 PDT 活性。
