A water soluble tri-cationic porphyrin-EDTA conjugate induces apoptosis in human neuroendocrine tumor cell lines

Gert Schwach; Patchanita Thamyongkit; Lorenz Michael Reith; Bernhard Svejda; Günther Knör; Roswitha Pfragner; Wolfgang Schoefberger

doi:10.1016/j.bioorg.2011.09.006

A water soluble tri-cationic porphyrin-EDTA conjugate induces apoptosis in human neuroendocrine tumor cell lines

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

Authors

Gert Schwach¹, Patchanita Thamyongkit², Lorenz Michael Reith³, Bernhard Svejda¹, Günther Knör³, Roswitha Pfragner⁴, Wolfgang Schoefberger⁵

Affiliations

¹ Department of Pathophysiology and Immunology, Center of Molecular Medicine, Medical University of Graz, A-8010 Graz, Austria.
² Department of Chemistry, Faculty of Science, Chulalongkorn University, Phayathai Road, Patumwan, Bangkok 10330, Thailand.
³ Institute of Inorganic Chemistry, Johannes Kepler University Linz (JKU), Altenberger Straße 69, 4040 Linz, Austria.
⁴ Department of Pathophysiology and Immunology, Center of Molecular Medicine, Medical University of Graz, A-8010 Graz, Austria. Electronic address: roswitha.pfragner@medunigraz.at.
⁵ Institute of Inorganic Chemistry, Johannes Kepler University Linz (JKU), Altenberger Straße 69, 4040 Linz, Austria. Electronic address: wolfgang.schoefberger@jku.at.

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / pharmacology*
Apoptosis / drug effects*
Caspase 3 / metabolism
Caspase 7 / metabolism
Cell Line, Tumor
Edetic Acid / analogs & derivatives*
Edetic Acid / chemistry*
Edetic Acid / pharmacology
Edetic Acid / therapeutic use
Humans
Neuroendocrine Tumors / pathology
Porphyrins / chemistry
Porphyrins / pharmacology*
Porphyrins / therapeutic use
Water / chemistry

Substances

5,10,15-tris(N-methylpyridinium-4-yl)-20-(1-phenyl-2-(ethylene diamine-tetraacetic acid))-21H,23H-porphyrin
Antineoplastic Agents
Porphyrins
Water
Edetic Acid
Caspase 3
Caspase 7