In Vitro Cytotoxic Effect of Difluoromethylornithine Increased Nonspecifically by Peptide Coupling

Difluoromethylornithine (DFMO)-peptide conjugates were synthesized as prodrugs to improve the cytotoxic efficacy of DFMO. All conjugates inhibited cell growth in different cell lines more effectively than DFMO itself. The best cytotoxic effect was achieved in all cell lines by DFMO-Glu-His-Phe-Arg-T...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1997-09, Vol.86 (9), p.997-1000
Main Authors: Süli-Vargha, H., Morandini, R., Bódi, J., Nagy, L., Medzihradszky-Schweiger, H., Ghanei, G.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
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Summary:Difluoromethylornithine (DFMO)-peptide conjugates were synthesized as prodrugs to improve the cytotoxic efficacy of DFMO. All conjugates inhibited cell growth in 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.
ISSN:0022-3549
1520-6017
DOI:10.1021/js970080d