Studies On Synthesis And Preliminary Photodynamic Anti-Tumor Effects Of Chlorophyll Derivatives

Photodynamic therapy (PDT) is a non-invaoive or minimally invasive, non-thermogenesis treatment by destroying the target tissues and cells with photochem reaction. It has many advantages such as good treatment efficiency, little side effect, simple conditions for treatment compared with traditional treatment. Choosing a suitable photosensitizer is crucial for PDT, which will directly affect the effect of PDT.Different kinds of photosensitizers have different absorptions in visible light region. And our main synthesis work is to get photosensitizers which have long wavelength absorption. Photosensitizer is transfered into the focus through the blood, so it must be water-solubility. And photosensitizer must penetrate through the cell membranes and has a high selectivity absorption in the cancer cells, it must be fat-solubility. In this dissertation the main work is about the structure modification of chlorophyll derivatives. We have made some modifications in E-ring and propanic acid side chain in chlorophyll derivatives.Chlorophyll is a kind of green pigment existed in the nature. Its degradation products and derivatives have amplitude applications in many aspects such as tumor, anaemia, cancer, liver injury, antimicrobial. In recent years, there are many reports about new photodynamic medicines for tumor by developing from the stabile derivatives of the chlorophyll degradation products. Preparation of purpurin-18 and pyropheophorbide a using silkworm excrement crude chlorophylls extract as starting material respectively under different reaction condition and the synthesis of purpurin-18-imide and pyropheophorbide a-amide by the reaction of purpurin-18, pyropheophorbide a with amines were presented.In this dissertation, eight new compounds were synthesized including three of purpurin-18-imides and five of pyropheophorbide a-amides in one year and two months. They were all characterized by ~1H-NMR and MS. And the preliminary photodynamic anti-tumor effect of purpurin-18-N-hexamethylene-imide was determined by MTT method. The result of experiment shows that purpurin-18-N-hexamethylene-imide has an obvious inhibition effect to tumor. The studies on photodynamic anti-tumor effect of other new compounds are now in progress.