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首页> 外文期刊>Chemistry: A European journal >Synthesis,Aggregation and Cellular Investigations of Porphyrin-Cobaltacarborane Conjugates
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Synthesis,Aggregation and Cellular Investigations of Porphyrin-Cobaltacarborane Conjugates

机译：卟啉-钴碳硼烷共轭物的合成，聚集和细胞研究

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A new series of porphyrin-cobaltacarborane conjugates(1-5)that contain four to sixteen carborane clusters per porphyrin macrocycle,were prepared in excellent yields(90-97%)by means of a ring-opening reaction of the zwitterionic cobaltacarborane [3,3'-Co(8-C4H8O2)-1,2-C2B9H_(10))(1',2'-C2B9H_(11))].The X-ray structure of one conjugate(3)is presented.The aggregation properties of these conjugates were investigated by using absorption and fluorescence spectrophotometry,and the stages of microcrystal formation were captured by using atomic force microscopy.All conjugates were found to aggregate in aqueous solutions,to form a broad dispersity of particle sizes.The cellular uptake,cytotoxicity,and preferential sites of subcellular localization of this series of conjugates were evaluated in human carcinoma HEp2 cells.The extent of conjugate cellular uptake depends on the number of cobaltacarborane units at the porphyrin periphery,their distri- bution,and the conjugate aggregation behavior.Conjugates 2 and 4,bearing either two adjacent or three 3,5-dico-baltacarboranephenyl groups,accumulated the most within HEp2 cells and are,therefore,the most promising boron neutron capture therapy agents.All conjugates showed very low dark-and photo-toxicity,probably due to their strong tendency for aggregation in aqueous solutions,and localized sub-cellularly within vesicles that correlated,to some extent,with the cell lyso-somes.
机译：通过两性离子型钴碳硼烷的开环反应，制备了一系列新的卟啉-钴碳硼烷共轭物（1-5），每个卟啉大环含有四到十六个碳硼烷簇，产率极高（90-97％）。 3'-Co（8-C4H8O2）-1,2-C2B9H_（10））（1'，2'-C2B9H _（（11））]。给出了一种共轭物（3）的X射线结构。聚集性质通过吸收和荧光分光光度法研究了这些结合物，并通过原子力显微镜捕获了微晶形成的阶段。发现所有结合物都在水溶液中聚集，形成了粒径分散的宽细胞吸收，细胞毒性，并在人癌HEp2细胞中评估了这一系列结合物的亚细胞定位的优先位点。结合物细胞摄取的程度取决于卟啉外围的钴碳硼烷单元的数量，其分布以及结合物的聚集行为。结合2和4，带有两个相邻的或三个3,5-二ico基碳硼烷苯基，在HEp2细胞中积累最多，因此是最有希望的硼中子俘获治疗剂。所有结合物都显示出非常低的暗和光-毒性，可能是由于它们在水溶液中很强的聚集趋势，并且定位在与细胞溶酶体在某种程度上相关的囊泡内的亚细胞内。

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