Xu Shangjie, Chen Shen, Zhang Manhua, Shen Tao
Center for Photochemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100080, China.
J Photochem Photobiol B. 2003 Dec 5;72(1-3):61-7. doi: 10.1016/j.jphotobiol.2003.09.001.
Two phenmethylamino hypocrellin B derivatives are novel photodynamic agents synthesized by a mild reaction between hypocrellin B and phenmethylamine. The red absorption of the photosensitizers is enlarged distinctly and the peri-hydroxylated perylenequinone structure of the parent HB is preserved. 9,10-diphenyl-anthracene (DPA) bleaching and electron paramagnetic resonance (EPR) spin trapping techniques were used to study the photodynamic activities of the phenmethylamino hypocrellin B derivatives in the presence of oxygen. Singlet oxygen (1O2) and superoxide anion radical (O2*-) generated in the process of illumination of the phenmethylamino hypocrellin B in aerobic solution were observed. The photodamage of PMAHBs to MGC803 cancer cells was investigated in vitro. The results in vitro reveal that the phenmethylamino hypocrellin B derivatives show a much less significant decrease in cytotoxicity than that of their parent HB. It exhibits higher selectivity of light-orientation, which can decrease the damage to normal tissues by irradiating the tumor tissues, and so increases the drug safety.
两种苯甲胺基竹红菌素B衍生物是通过竹红菌素B与苯甲胺之间的温和反应合成的新型光动力剂。光敏剂的红光吸收明显增大，并且母体竹红菌素B的周环羟基化苝醌结构得以保留。采用9,10-二苯基蒽（DPA）漂白和电子顺磁共振（EPR）自旋捕获技术研究了苯甲胺基竹红菌素B衍生物在有氧条件下的光动力活性。观察到在有氧溶液中光照苯甲胺基竹红菌素B过程中产生的单线态氧（1O2）和超氧阴离子自由基（O2*-）。体外研究了苯甲胺基竹红菌素B衍生物对MGC803癌细胞的光损伤。体外实验结果表明，苯甲胺基竹红菌素B衍生物的细胞毒性下降程度远低于其母体竹红菌素B。它表现出更高的光定位选择性，通过照射肿瘤组织可减少对正常组织的损伤，从而提高了药物安全性。
