Synthesis, cellular uptake and animal toxicity of a tetra(carboranylphenyl)-tetrabenzoporphyrin
Synthesis, cellular uptake and animal toxicity of a tetra(carboranylphenyl)-tetrabenzoporphyrin
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DOI：
10.1016/j.bmc.2005.10.037
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发表时间：
2006-03-15
影响因子：
3.5
通讯作者：
Vicente, MGH
中科院分区：
文献类型：
--
作者：
Gottumukkala, V;Ongayi, O;Vicente, MGH
以丁吡咯和碳硼烷基苯甲醛为原料，经缩合、金属插入、氧化、脱金属、脱硼等反应，合成了一种水溶性巢状碳硼烷基四苯并卟啉，总收率43%。该化合物在人胶质母细胞瘤T98 G细胞内的累积程度显著高于结构相关的巢式碳硼烷基卟啉，并优先定位于细胞溶酶体中。使用雄性和雌性BALB/c小鼠进行的动物毒性研究表明，即使以160 mg/kg的剂量，以4 mg/mL的浓度单次腹腔内注射给药，两种化合物也是无毒的。结果表明，四（碳硼烷苯基）四苯并卟啉是一种很有前途的新型肿瘤增敏剂。(c)2005爱思唯尔有限公司保留所有权利。
A water-soluble nido-carboranyl-tetrabenzoporphyrin has been synthesized in 43% overall yield, by condensation of butanopyrrole with a carboranylbenzaldehyde, followed by metal insertion, oxidation, demetallation and deboronation reactions. This Compound accumulated within human glioblastoma T98G cells to a significant higher extent than a structurally related nido-carboranylporphyrin, and localized preferentially in the cell lysosomes. Animal toxicity studies using male and female BALB/c mice revealed that both compounds are non-toxic even at a dose of 160 mg/kg, administered intraperitoneally as a single injection at a concentration of 4 mg/mL. It is concluded that the tetra(carboranylphenyl)-tetrabenzoporphyrin is a promising new sensitizer for the treatment of malignant tumors. (c) 2005 Elsevier Ltd. All rights reserved.