Octa-Substituted Anionic Porphyrins: Topoisomerase I Inhibition and Tumor Cell Apoptosis Induction

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• 作者：Baoping Zhai ; Li Shuai ; Li Yang ; Xiaocheng Weng ; Lin Wu ; Shaoru Wang ; Tian Tian ; Xiaojun Wu ; Xiang Zhou ; Congyi Zheng
• 刊名：Bioconjugate Chemistry
• 出版年：2008
• 出版时间：August 2008
• 年：2008
• 卷：19
• 期：8
• 页码：1535-1542
• 全文大小：255K
• 年卷期：v.19,no.8(August 2008)
• ISSN：1520-4812

文摘

β-Octabromo-meso-tetra(4-carboxyl)phenyl porphyrin 6 and β-octaphenyl-meso-tetra(4-carboxyl)phenyl porphyrin 8 were synthesized and fully characterized by ¹H NMR, UV, and HRMS. Their cytotoxicities to tumor cells were tested using MTT assays. One kind of tumor cell apoptosis induced by these anionic porphyrins under irradiation was examined by flow cytometric analysis. The inhibition of Topo I (Topoisomerase I) indicates that Topo I preferentially binds to the synthesized compounds, thus blocking the interaction between Topo I and DNA. The results implied that compounds 4, 6, and 8 are potential inhibitors to Topo I, which might be one of the important factors inducing apoptosis of tumor cells.