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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。
In order to seek a new tetra-substituted aluminum phthalocyanine photosensitizer with good photodynamic therapy (PDT) anticancer activity in the red region, 4-nitro phthalic acid was used as a starting material to synthesize tetraamino aluminum phthalocyanine (TAAlPc), tetraacetamido aluminum phthalocyanine (TAcAAlPc), tetrapropionamide aluminum phthalocyanine (TPrAAlPc) and tetrabutylamido aluminum phthalocyanine (TBuAAlPc). The structure of the obtained product was characterized and its fluorescence spectrum and acute toxicity were tested. Its photodynamic anticancer activity was measured at the output wavelength of 532 nm. The results show that the resulting amide-substituted series of aluminum phthalocyanine has no obvious toxicity on mice. When the injection dose was 20mg / kg, the inhibition rates of the four kinds of aluminum phthalocyanine photosensitizers to the solid tumor of S180 mice were 44.96%, 45.87%, 45.62% and 48.65% respectively, with no obvious difference. When the dosage was increased to 40mg / kg, the tumor inhibition rates were 39.16%, 42.81%, 40.56% and 51.82%, respectively. At this dose, tetrabutylamido aluminum phthalocyanine showed higher photodynamic therapy for anticancer activity.