Synthesis and cellular studies of a carboranylchlorin for the PDT and BNCT of tumors.
Synthesis and cellular studies of a carboranylchlorin for the PDT and BNCT of tumors.
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用于肿瘤 PDT 和 BNCT 的碳硼酰二氯的合成和细胞研究。
DOI：
10.1016/j.bmc.2006.05.026
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发表时间：
2006
期刊：
影响因子：
--
通讯作者：
Vicente,MGracaH
中科院分区：
文献类型：
--
作者：
Luguya,Raymond;Jensen,TimothyJ;Smith,KevinM;Vicente,MGracaH
本文叙述了由已知的碳硼烷卟啉合成闭-和巢-碳硼烷二氢卟啉4和5的方法。发现水溶性巢式碳硼烷卟啉5具有非常低的暗细胞毒性（使用基于MTT的测定法，IC 50>500μM），但在红光存在下具有毒性（在0.55J/cm 2光剂量下，IC 50 =80μM）。在相同的实验条件下，碳硼烷二氢卟酚5被人胶质瘤T98 G细胞吸收的程度显著高于叶绿素降解产物二氢卟酚e6。碳硼烷二氢卟酚5的亚细胞定位的首选网站被发现是细胞溶酶体。我们的研究结果表明，碳硼烷二氢卟酚5是一个有前途的新的双重敏化剂的PDT和BNCT治疗肿瘤。
The syntheses of closo- and nido-carboranylchlorins 4 and 5 from a known carboranylporphyrin are described. Water-soluble nido-carboranylporphyrin 5 was found to have very low dark cytotoxicity (IC50>500μM using a MTT-based assay) but to be toxic in the presence of red light (IC50=80μM at 0.55J/cm2light dose). Under the same experimental conditions, carboranylchlorin 5 was taken up by human glioma T98G cells to a significantly higher extent than chlorin e6, a chlorophyll degradation product. The preferred sites of subcellular localization of carboranylchlorin 5 were found to be the cell lysosomes. Our results suggest that carboranylchlorin 5 is a promising new dual sensitizer for the PDT and BNCT treatment of tumors.