摘要
本文报道了7种中介-四(取代苯基)卟吩衍生物的合成和4种化合物在非细胞体系内的光敏化效应和肿瘤光生物活性。在D_2中对NADPH光氧化作用的敏化效应测定结果表明,4种卟吩衍生物产~1O_2等活性氧物质的能力远高于HpD及癌光啉。但这些化合物对体外培养人舌鳞状细胞癌细胞TCA-8113系的光灭活作用却很弱,而对小鼠S_(180)肉瘤则又有一定的荧光定位和光动力治疗效果。但其迟发光毒作用严重。此外,含卤素的卟吩衍生物(Ⅱ_(1-3))未能激发出荧光,提示卤素对荧光的可能淬灭作用。
The preparation of 7 meso-tetrasubstituted phenyl porphines and the photosensitizing effects and tumor-photobiological activities of 4 of these compounds in cell-free system are presented here.It has been shown by the data in determination of the ability of compounds Ⅰ1_4 to sensitize photooxidation of NADPH in D2O under the illumination _of He-Ne laser that the ability to generate active oxygen species of them was much higher than those of YHpD and PsD-007.But they were weak in photoinactivation for the cultured human tongue squamocell cancer cells TCA-8113 in vitro.However, they were effective, in some degree, in the photo-localization and photodynamic therapy of sarcoma Si80 in mice.Severe delayed phototoxic reaction occurred in the mice administered these compounds.Porphines with halogen atoms in their molecules (compounds Ⅱ1_3) could not be excited and were non-fluorescent.This suggests that there was possibly a quenching effect of ha'ogen atoms on porphine fluorescence.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
1989年第2期110-114,共5页
Academic Journal of Second Military Medical University
基金
国家自然科学基金
关键词
肿瘤
光化学
卟吩
诊断
tumor photochemodiagnosis and photochemotherapy
porphines
