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  

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

作　　者：周锦兰[1] 程红[1] 万福贤[1] 俞开潮[1] 李正佳[2] 

机构地区：[1]华中科技大学化学系,湖北武汉430074 [2]华中科技大学激光技术与工程研究院,湖北武汉430074

出　　处：《中国激光》2005年第8期1155-1160,共6页Chinese Journal of Lasers

基　　金：国家自然科学基金(20275011);湖北省自然科学基金(2002AB051)资助项目。

摘　　要：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(TAAlPc)、四乙酰胺基铝酞菁(TAcAAlPc)、四丙酰胺基铝酞菁(TPrAAlPc)和四丁酰胺基铝酞菁(TBuAAlPc)。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。For the development of novel tetra-substituted aluminum phthalocyanine used as photodynamic therapy （PDT） photosensitizer with good photodynamie antieaneer activity, tetraamino-, tetraaeetamido- . tetrapropanamido- and tetrabutanamido aluminum phthalocyanines are synthesized by phthalic anhydride-urea method with 4-nitro phthalie acid as preaetant. The structures of these aluminum phthaloeyanines are characterized. Their fluorescent spectra and acute toxicity are also measured. Meanwhile, their photodynamie antieaneer activities are determined.As a result, the aluminum phthaloeyanines are innoxious to mice. When 20 mg/kg aluminum phthalocyanines are injected to S180 sarcoma-bearing mice, the sensitizers show that the rates of inhibitory to S180 sarcoma are 44.96%,45.87%, 45.62% and 48.65% respectively, which are in little difference according to the order of tetraamino-，tetraaeetamido-, tetrapropanamido- and tetrabutanamido-phthaloeyanine aluminum, respectively. While the concentration of injeeton 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, tetrabutanamidophthaloeyanine aluminum shows the highst PDT antieaneer aetivitiy。

关 键 词：医用光学和生物技术 光动力治疗 铝酞菁 抗癌活性 合成 表征 

分 类 号：R454.2[医药卫生—治疗学] R312[医药卫生—临床医学]