Synthesis and Evaluation of Photosensitizeing Dyes for Photodynamic Diagnosis and Therapy.

以天然原卟啉和叶绿素为原料，采用分步合成的方法合成了各种卟啉和氯叶绿衍生物，为早期癌症的光动力学诊断和治疗提供了新的光敏染料。染料在癌细胞中的特异性积累取决于它们的分子结构；极性取代基的高度对称分配表明染料在癌细胞中没有有效的积累；极性和非极性基团的局部取代是进行诊断所必需的。染料与癌细胞相互作用的机制已经阐明，注入血液中的染料分子结合癌细胞膜，穿透细胞膜，与线粒体膜接触。含氟染料有望成为核磁共振技术用于深部癌三维分析的化学探针。

Varous Kinds of Porphyrin and cholorophyll derivatives have been synthesized from naturally occuring protoporphyrins and chloorphyll and stepwise synthetic methods to provide new photosensitizing dyes in photodynamic diagnosis and therapy in early cancer. Specific accumu- lation of dyes in cancer cell depends upon their molecular structure; highly symmetric allocation of polar substituents shows no effective accumulation of dye in cancer cell; localized substitutuion of both polar and non-polar groups is essential to exert diagnosis. Mechanism of interaction between dye and cancer cell has been elucidated; dye molecule injected in blood binds membrene of cancer cell, penetrates the membrene, contact with the membrene of mitochondria. Fluorine containning dyes seem to be promisible chemical probe to three dimensional analysis of deep cancer with nuclear magnetic resonance technique.