Boyle R W, Paquette B, van Lier J E
MRC Group in the Radiation Sciences, Faculty of Medicine, University of Sherbrooke, Québec, Canada.
Br J Cancer. 1992 Jun;65(6):813-7. doi: 10.1038/bjc.1992.174.
Aluminium phthalocyanines substituted to different degrees with hydrophilic sulphonic acid and hydrophobic phthalimidomethyl groups were investigated in vivo as new agents for the photodynamic therapy of malignant tumours. Parameters studied included the photodynamic action on EMT-6 mammary tumours in BALB/c mice, the therapeutic window and the potential for direct cell killing, assayed via an in vivo/in vitro test. Although the efficiency of photoinactivation of the EMT-6 tumour increases by a factor of ten with reduction of the number of sulphonic acid groups from four to two, no further effect was seen with the addition of the hydrophobic phthalimidomethyl groups. Addition of the latter groups however increased the potential for direct cell killing by a factor of two and expanded the therapeutic window by a factor of four, thus improving the usefulness of the dye as a photosensitiser for the photodynamic therapy of cancer.
研究了用亲水性磺酸和疏水性邻苯二甲酰亚胺甲基基团不同程度取代的铝酞菁作为恶性肿瘤光动力治疗的新型药物在体内的情况。研究的参数包括对BALB/c小鼠EMT-6乳腺肿瘤的光动力作用、治疗窗口以及直接细胞杀伤潜力，通过体内/体外试验进行测定。尽管随着磺酸基团数量从四个减少到两个，EMT-6肿瘤的光灭活效率提高了十倍，但添加疏水性邻苯二甲酰亚胺甲基基团后未观察到进一步的效果。然而，添加后一组基团使直接细胞杀伤潜力提高了两倍，并使治疗窗口扩大了四倍，从而提高了该染料作为癌症光动力治疗光敏剂的实用性。
