七甲川花菁染料作为肿瘤靶向和光动力治疗载体的研究进展

Novel Heptamethine Cyanine Dye as a Delivery Carrier for Tumor Targeting and Photodynamic Therapy

七甲川花菁近红外荧光染料(NIRF)可直接被肿瘤细胞特异性吸收,具有肿瘤靶向性。与化疗药物偶联后,该类染料可通过血脑屏障将药物转运至肿瘤部位,不仅可以减少化疗药物使用剂量,降低药物的毒副作用,也可通过近红外荧光成像实现对肿瘤治疗的实时监控。七甲川花菁染料所展示的线粒体毒性和光敏特性,可直接杀死肿瘤细胞,抑制肿瘤新生血管的形成。通过纳米包裹,能够显著增强该类染料的肿瘤靶向能力,实现实时跟踪药物释放情况。七甲川花菁染料特异性识别肿瘤细胞的能力与有机阴离子转运肽的作用密切相关,缺氧和线粒体膜电位也参与了染料吸收的调控。这些发现有利于将近红外荧光染料应用于肿瘤的靶向治疗。

Heptamethine cyanine near infrared fluorescence（NIRF） dyes can be taken up directly and accumulated specifically in the cancer cells and character with tumors target. By conjugated these dye with drug as carriers for the safe delivery of chemotherapies to tumor site through blood-brain barrier（BBB）,not only reduce the side effects and doses of drug but also allow the real-time monitoring of therapeutic effect. Moreover theses dyes can be utilized as effective agent for photodynamic therapy. Some these dyes even reveal remarkable tumoricidal activity with mitochondrial toxicity to directly kill tumor cells and inhibit tumor growth by destroying neovascularization. Encapsulated nanoparticle significantly enhanced NIRF dyes tumor-targeting ability and tracking drug release. The different uptake of the dyes into cancer but not normal cells is possible due to the presence of specific organic anion-transporting peptides（OATPs）,and regulated by hypoxia and mitochondrial membrane potentials. These advances have widely extended current application of cancer target therapy by NIRF delivery carrier.