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论文类型：期刊论文

发表时间：2021-01-10

发表刊物：JOURNAL OF PORPHYRINS AND PHTHALOCYANINES

卷号：24

期号：9

页面范围：1093-1098

ISSN号：1088-4246

关键字：chlorin e6; glutathione; maleimide; singlet oxygen; oxidative stress; photodynamic therapy

摘要：Three derivatives of chlorin e6 (1-3) were synthesized by introduction of maleimide, cysteine and glutathione at C-13 carboxyl of the chlorin scaffold. The evaluation of their PDT effects showed that compound 1, the derivative with a maleimide group, exhibited more potent photocytotoxicity against HepG2 cells (IC50 3.2 mu M) than 2 (IC50 6.7 mu M) and 3 (IC50 10.2 mu M), although the cellular uptake of 1 was slightly lower than that of 2 and 3. The high PDT effect of 1 was found to be in agreement with the high level of intracellular singlet oxygen. Further investigation of the mechanism revealed that 1 can significantly lower the GSH level in HepG2 cells due to the addiction reaction of maleimide and GSH, thus resulting in the reduction of ROS scavenging and the enhancement of cellular oxidative stress. This approach to improve PDT effects of photosensitizers by means of interfering with the cellular redox system and enhancing cellular oxidative stress offers a new strategy for development of photosensitizers in cancer therapy.