A Platinum Functional Porphyrin Conjugate: An Excellent Cancer Killer for Photodynamic Therapy

被引:20
作者
Hu, Xiaojun [1 ,2 ]
Ogawa, Kazuma [3 ]
Li, Siqiaozhi [2 ]
Kiwada, Tatsuto [4 ]
Odani, Akira [4 ]
机构
[1] Shanghai Univ, Sch Life Sci, Lab Biosensing Technol, Shanghai 200444, Peoples R China
[2] Kanazawa Univ, Grad Sch Med Sci Pharmaceut & Hlth Sci, Div Pharmaceut Sci, Kanazawa, Ishikawa 9201192, Japan
[3] Kanazawa Univ, Inst Frontier Sci Initiat, Kanazawa, Ishikawa 9201192, Japan
[4] Kanazawa Univ, Coll Med Pharmaceut & Hlth Sci, Kanazawa, Ishikawa 9201192, Japan
关键词
Photodynamic therapy; Anticancer agent; Porphyrin; ANTICANCER ACTIVITY; TUMOR-CELLS; PHOTOSENSITIZER; OXALIPLATIN; DERIVATIVES; MECHANISMS; BIODISTRIBUTION; PHTHALOCYANINE; MITOCHONDRIA; CISPLATIN;
D O I
10.1246/bcsj.20180382
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A novel tetracationic porphyrin-platinum(II) conjugate was synthesized and characterized. This complex, 4Pt(dach)ClTPyP, showed reasonable water solubility, lack of aggregation, and high singlet oxygen quantum yield. It also exhibited low dark cytotoxicity and excellent photocytotoxicity (Colon26: 0.17 mu M; Sarcoma180: 0.25 mu M). The mechanisms of cell death have been investigated and are attributed to high singlet oxygen generation, internalization into nucleus, and a caspase-3 induced apoptosis pathway. In the in vivo photodynamic therapy (PDT) assay, 4Pt(dach) ClTPyP completely killed tumor tissue, not simply displaying inhibition of tumor growth, and no recurrence was seen 18 days later after a single administration. All these findings of 4Pt(dach)ClTPyP shed light on a potential clinical use for cancer PDT in the future.
引用
收藏
页码:790 / 796
页数:7
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