高等学校化学学报 ›› 2013, Vol. 34 ›› Issue (10): 2308.doi: 10.7503/cjcu20130124

• 有机化学 • 上一篇    下一篇

阿糖胞苷金属卟啉衍生物的合成及光动力抗肿瘤活性

何洁, 刘文洪, 何利民, 陈丽园   

  1. 浙江中医药大学生物工程学院, 杭州 310053
  • 收稿日期:2013-02-04 出版日期:2013-10-10 发布日期:2013-10-10
  • 作者简介:何洁,女,讲师,主要从事卟啉方面的研究.E-mail:xuejianzi@aliyun.com
  • 基金资助:

    浙江省自然科学基金项目(批准号:LQ12H28006)和浙江省医药卫生科学研究基金计划(批准号:2009B115)资助.

Synthesis and Photodynamic Antitumor Activity of New Metalloporphyrin-Ara-C Compounds

HE Jie, LIU Wen-Hong, HE Li-Min, CHEN Li-Yuan   

  1. College of Bioengineering, Zhejiang Chinese Medical University, Hangzhou 310053, China
  • Received:2013-02-04 Online:2013-10-10 Published:2013-10-10

摘要:

设计并合成了阿糖胞苷卟啉衍生物(AHP), 并通过金属插入反应获得了4种金属卟啉衍生物, 采用核磁共振、红外光谱、紫外-可见光谱和质谱等手段对化合物的结构进行了表征.光动力抗肿瘤活性实验结果表明, 含药浓度为25 μmol/L的ZnAHP经光照30 min后对人乳腺癌MCF-7细胞的光动力杀伤率平均达(45.86±8.20)%.

关键词: 阿糖胞苷, 金属卟啉, 光动力抗肿瘤活性

Abstract:

Photodynamic therapy(PDT) is a promising modality with minimally invasive approach to the clinical treatment of oncology generally based on photosensitizers, as they can utilize the administration and selective accumulation in cancer tissues to cause tissue injury and cell death by exposure to suitable visible light. Porphyrins can be used as efficient photosensitizers with their unique characteristic π-system and coordinating metals. To develop new porphyrin photosensitizers of PDT, porphyrin-Ara-C compound was designed and synthesized, then four metalloporphyrin-Ara-C compounds were synthesized through metal insertion reaction. Their structures were characterized by 1H NMR, IR, UV-Vis and MS. The photodynamic antitumor activity experimental results showed that the killing rate of PDT with 25μmol/L ZnAHP reacted for 30 min to MCF-7 cell could reach (45.86±8.20)%.

Key words: Ara-C, Metalloporphyrin, Photodynamic antitumor activity

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