Asymmetrically substituted Cationic Indole- and Fluorene Porphyrins inhibit Tumor Proliferation in small Intestinal Neuroendocrine Tumors and Medullary Thyroid Carcinomas
Sprache des Titels:
Englisch
Original Kurzfassung:
In this study we demonstrate anticancer activity of novel fully water soluble cationicporphyrins. The two cationic porphyrins 5,10,15-tris(N-methylpyridinium-4-yl)-20-[1-phenyl4-(3-N-phenylsulfonylindolyl)]-21H,23H-porphyrin chloride (TMPy3PhenIndolprot1P-Cl3) and 5-{5-[2-(9,9-Dimethyl)fluorenyl]-N-methylpyridinium-3-yl}-10,15,20-tris(N-methyl-pyridinium-4-yl)-21H,23Hporphyrin chloride (TMPy3PyFluorenyl1P-Cl4) were prepared and their antiproliferative effects
were studied in two human tumor cell lines and a normal human fibroblast cell line. Effects of the
novel porphyrin compounds were evaluated in the small intestinal neuroendocrine tumor cell line KRJ-I, the medullary thyroid carcinoma cell line MTC-SK and the normal human fibroblast cell line HF-SAR by cell counting, mitochondrial activity assays and cell cytotoxicity analyses. TMPy3PhenIndolprot1P-Cl3 and TMPy3PyFluorenyl1P-Cl4 showed antiproliferative effects in the tumor cell lines MTC-SK and KRJ-I; mitochondrial activity was decreased and cytotoxic effects
were observed, while no significant alterations of the human fibroblasts were noted. With the
advantage of full water solubility and antiproliferative effects in tumor cell lines, the novel porphyrin
compounds TMPy3PhenIndolprot1P-Cl3 and TMPy3PyFluorenyl1P-Cl4 could be a new therapeutic
option in anticancer treatment.