一种水溶性三阳离子卟啉-EDTA 缀合物诱导人神经内分泌肿瘤细胞系凋亡。

Department of Pathophysiology and Immunology, Center of Molecular Medicine, Medical University of Graz, A-8010 Graz, Austria.

Department of Chemistry, Faculty of Science, Chulalongkorn University, Phayathai Road, Patumwan, Bangkok 10330, Thailand.

Bioorg Chem. 2012 Feb;40(1):108-113. doi: 10.1016/j.bioorg.2011.09.006. Epub 2011 Oct 6.

In this study, a completely water soluble tri-cationic porphyrin-EDTA conjugate was synthesized. We present data demonstrating the tumoristatic effects of the novel fully water soluble cationic porphyrin TMPy(3)PhenEDTA-P-Cl(4) in the dark, in the medullary thyroid carcinoma cell lines MTC-SK and SHER-I and weaker effects in the small intestinal neuroendocrine tumor cell line KRJ-I. In addition, cytotoxic effects were also studied in normal human fibroblasts that represent normal tissue and the results are compared to the tumor cell lines.

在这项研究中，合成了一种完全水溶性的三阳离子卟啉-EDTA 缀合物。我们提供的数据表明，新型全水溶性阳离子卟啉 TMPy（3）PhenEDTA-P-Cl（4）在黑暗中具有肿瘤抑制作用，在甲状腺髓样癌细胞系 MTC-SK 和 SHER-I 中表现出更强的作用，而在小肠神经内分泌肿瘤细胞系 KRJ-I 中作用较弱。此外，还研究了正常人类成纤维细胞（代表正常组织）中的细胞毒性作用，并将结果与肿瘤细胞系进行了比较。