具有优异光诱导抗癌活性的水溶性金属卟啉盐，其源于高肿瘤蓄积性。
Water-soluble metalloporphyrinates with excellent photo-induced anticancer activity resulting from high tumor accumulation.
作者信息
Hu Xiaojun, Ogawa Kazuma, Kiwada Tatsuto, Odani Akira
机构信息
Division of Pharmaceutical Sciences, Graduate School of Medical Science, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa 920-1192, Japan.
Institute for Frontier Science Initiative, Kanazawa University, Kanazawa 920-1192, Japan.
出版信息
J Inorg Biochem. 2017 May;170:1-7. doi: 10.1016/j.jinorgbio.2017.02.001. Epub 2017 Feb 4.
To develop a water-soluble and tumor-targeted photosensitizer for photodynamic therapy (PDT), a porphyrin framework containing the metal ion gallium(III) was combined with platinum(II)-based groups to produce two new pentacationic metalloporphyrinates, Ga-4cisPtTPyP (5,10,15,20-tetrakis{cis-diammine-chloro-platinum(II)}(4-pyridyl)-porphyrinato gallium(III) hydroxide tetranitrate) and Ga-4transPtTPyP (5,10,15,20-tetrakis{trans-diammine-chloro-platinum(II)} (4-pyridyl)-porphyrinato gallium(III) hydroxide tetranitrate). Both complexes exhibited high singlet oxygen quantum yields (Φ) and remarkable photocytotoxicity with appreciable phototoxic indexes (PIs). In particular, Ga-4cisPtTPyP showed a low IC value (Colon 26: 0.12μM; Sarcoma 180: 0.08μM) under illumination and its PI up to 1000. With outstanding tumor accumulation (tumor/muscle ratio>9), Ga-4cisPtTPyP almost completely inhibited tumor growth over two weeks in an in vivo PDT assay. These results imply that Ga-4cisPtTPyP could be a promising anticancer agent for use in PDT.
为开发一种用于光动力疗法（PDT）的水溶性且肿瘤靶向的光敏剂，将含有金属离子镓（III）的卟啉框架与铂（II）基基团结合，制备了两种新的五价金属卟啉盐，即Ga-4cisPtTPyP（5,10,15,20-四{顺式二胺氯铂（II）}（4-吡啶基）卟啉合镓（III）氢氧化物四硝酸盐）和Ga-4transPtTPyP（5,10,15,20-四{反式二胺氯铂（II）}（4-吡啶基）卟啉合镓（III）氢氧化物四硝酸盐）。两种配合物均表现出高的单线态氧量子产率（Φ）以及具有可观光毒性指数（PI）的显著光细胞毒性。特别地，Ga-4cisPtTPyP在光照下显示出低的IC值（结肠26：0.12μM；肉瘤180：0.08μM），其PI高达1000。凭借出色的肿瘤蓄积（肿瘤/肌肉比率>9），在体内PDT试验中，Ga-4cisPtTPyP在两周内几乎完全抑制了肿瘤生长。这些结果表明，Ga-4cisPtTPyP可能是一种用于PDT的有前景的抗癌剂。
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