新型四酰胺基铝酞菁的制备及其在体光动力抗癌活性研究

为寻求在红光区具有良好光动力治疗（PDT）抗癌活性的新型四取代铝酞菁光敏剂，以4-硝基邻苯二甲酸为原料，用苯酐尿素法合成了四氨基铝酞菁（TAAIPc）、四乙酰胺基铝酞菁（TAcAAIPc）、四丙酰胺基铝酞菁（TPrAAIPc）和四丁酰胺基铝酞菁（TBuAAIPc）。表征了所得产物的结构，测试了其荧光光谱和急性毒性；并在输出波长532nm下测定了其光动力抗癌活性。结果表明，所得的酰胺基取代系列铝酞菁对小鼠无明显毒性。当注射剂量为20mg／kg时，上述四种铝酞菁光敏剂对小鼠S180实体瘤的抑瘤率分别为44．96％，45．87％．45．62％和48．65％，差别不明显。加大剂量至40mg／kg时，抑瘤率依次为39．16％，42．81％，40．56％和51．82％。在此剂量下，四丁酰胺基铝酞菁表现出较高的光动力治疗抗癌活性。

Preparation and Photodynamic Anticancer Activities of New Tetraamido-Subsitituted Aluminum Phthalocyanines

For the development of novel tetra-substituted aluminum phthalocyanine used as photodynamic therapy (PDT) photosensitizer with good photodynamic anticancer activity, tetraamino-, tetraacetamido-, tetrapropanamido- and tetrabutanamido-aluminum phthalocyanines are synthesized by phthalic anhydride-urea method with 4-nitro phthalic acid as preactant. The structures of these aluminum phthalocyanines are characterized. Their fluorescent spectra and acute toxicity are also measured. Meanwhile, their photodynamic anticancer activities are determined. As a result,the aluminum phthalocyanines are innoxious to mice. When 20 mg/kg aluminum phthalocyanines are injected to S_(180) sarcoma-bearing mice, the sensitizers show that the rates of inhibitory to S_(180) sarcoma are 44.96%, 45.87%, 45.62% and 48.65% respectively,which are in little difference according to the order of tetraamino-, tetraacetamido-, tetrapropanamido- and tetrabutanamido-phthalocyanine aluminum, respectively. While the concentration of injecton is raised to 40 mg/kg, the rates of inhibitory are 39.16%, 42.81%, 40.56% and 51.82% respectively for the same order. In this condition, tetrabutanamidophthalocyanine aluminum shows the highst PDT anticancer activitiy.