Taquet Jean-Philippe, Frochot Céline, Manneville Vincent, Barberi-Heyob Muriel
DCPR, UMR 7630 CNRS-INPL, Groupe ENSIC, Nancy University, 1 Rue Grandville, F-54001 Nancy, France.
Curr Med Chem. 2007;14(15):1673-87. doi: 10.2174/092986707780830970.
Photodynamic therapy (PDT) is a relatively new cytotoxic treatment, predominantly used in anticancer approaches, that depends on the retention of photosensitizers in tumor and their activation after light exposure. This technology is based on the light excitation of a photosensitizer which induces very localized oxidative damages within the cells by formation of highly reactive oxygen species, the most important being singlet oxygen. Many photo-activable molecules have been synthesized such as porphyrins, chlorins and more recently phthalocyanines which present a strong light absorption at wavelengths around 670 nm and are therefore well-adapted to the optical window required for PDT application. However, the lack of selective accumulation of these photo-activable molecules within tumor tissue is a major problem in PDT, and one research area of importance is developing targeted photosensitizers. Indeed, targeted photodynamic therapy offers the advantage to enhance photodynamic efficiency by directly targeting diseased cells or tissues. Many attempts have been made to either increase the uptake of the dye by the target cells and tissues or to improve subcellular localization so as to deliver the dye to photosensitive sites within the cells. The aim of this review is to present the actual state of the development of phthalocyanines covalently conjugated with biomolecules that possess a marked selectivity towards cancer cells; for some of them their photophysical properties and photodynamic activity will be presented.
光动力疗法（PDT）是一种相对较新的细胞毒性治疗方法，主要用于抗癌治疗，它依赖于光敏剂在肿瘤中的潴留以及光照后其激活。该技术基于光敏剂的光激发，通过形成高活性氧物种（其中最重要的是单线态氧）在细胞内诱导非常局部的氧化损伤。已经合成了许多可光激活的分子，如卟啉、二氢卟酚，最近还有酞菁，它们在670nm左右的波长处有强烈的光吸收，因此非常适合PDT应用所需的光学窗口。然而，这些可光激活分子在肿瘤组织中缺乏选择性积累是PDT中的一个主要问题，一个重要的研究领域是开发靶向光敏剂。事实上，靶向光动力疗法具有通过直接靶向病变细胞或组织来提高光动力效率的优势。人们已经进行了许多尝试，要么增加染料在靶细胞和组织中的摄取，要么改善亚细胞定位，以便将染料递送至细胞内的光敏位点。本综述的目的是介绍与对癌细胞具有显著选择性的生物分子共价缀合的酞菁的实际发展状况；对于其中一些，将介绍它们的光物理性质和光动力活性。
