In vitro cytotoxic effect of difluoromethylornithine increased nonspecifically by peptide coupling

H. Süli-Vargha, R. Morandini, J. Bódi, L. Nagy, H. Medzihradszky-Schweiger, G. Ghanem

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Abstract

Difluoromethylomithine (DFMO)-peptide conjugates were syntesized as prodrugs to improve the cytotoxic efficacy of DFMO. All conjugates inhibited cell growth n different cell lines more effectively than DFMO itself. The best cytotoxic effect was achieved in all cell lines by DFMO-Glu-His-Phe- Arg-Trp-Gly-OMe, where the carrier peptide is a melanotropin hormone fragment. Although this conjugate is capable of displacing labeled melanotropin from its receptor, its cytotoxic effect on the receptor-positive human melanoma cell line has not been proven to be receptor-mediated. The differences in the cytotoxicities of the congeners seem to be influenced, at least in part, by the nature of the carrier molecule.

Original languageEnglish
Pages (from-to)997-1000
Number of pages4
JournalJournal of pharmaceutical sciences
Volume86
Issue number9
DOIs
Publication statusPublished - Sep 1997

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ASJC Scopus subject areas

  • Pharmaceutical Science

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