Promising anti-growth effects of palladium(II) saccharinate complex of terpyridine by inducing apoptosis on transformed fibroblasts in vitro


Coskun M. D. , ARI F. , ORAL A. Y. , SARIMAHMUT M. , KUTLU H. M. , YILMAZ V. T. , ...More

BIOORGANIC & MEDICINAL CHEMISTRY, vol.21, no.15, pp.4698-4705, 2013 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 21 Issue: 15
  • Publication Date: 2013
  • Doi Number: 10.1016/j.bmc.2013.05.023
  • Title of Journal : BIOORGANIC & MEDICINAL CHEMISTRY
  • Page Numbers: pp.4698-4705
  • Keywords: Palladium(II) complexes, Fibrosarcoma, Cytotoxicity, Apoptosis, PLATINUM(II) COMPLEXES, BIOLOGICAL EVALUATION, CYTOTOXIC ACTIVITY, BETA-LACTOGLOBULIN, ANTITUMOR, ANTICANCER, IFOSFAMIDE, DESIGN, PD(II), PT(II)

Abstract

Fibrosarcoma is one of the fatal cancer types and there is still not satisfactory success in its treatment despite new drugs. Therefore, the search for a new compound has been going on. It is currently known that some palladium-based anti-cancer compounds seem to have powerful apoptosis-inducing effects in cancer cells. For this purpose, a palladium(II)-saccharinate complex containing terpyridine which was synthesized by our research group was investigated in terms of its anti-tumor effects against mouse embryonic fibroblast NIH/3T3 (normal cell line) and rat embryonic fibroblast 5RP7 (H-ras transformed cell line) in vitro. The MTT and ATP viability assays were used to determine anti-growth/cytotoxic effects. Cytotoxic activity was confirmed by real time cytotoxicity analysis system. Flow cytometry analysis was further used to determine the mode of cell death (apoptosis/necrosis). Apoptosis was confirmed by triple-staining the cells with Hoechst 33342/PI/Calcein-AM triple and evaluated with fluorescence microscopy. It was found that the compound showed significant anti-growth activity by inducing apoptosis in a dose dependent manner. In conclusion, taking into account the cytotoxic activity of the compound at even relatively lower doses, in vivo experiments to elucidate its potential use for the treatment of fibrosarcoma are warranted. (C) 2013 Elsevier Ltd. All rights reserved.