International Journal of Oncology 2005-12-01

Cytotoxicity of the polyamine oxidase inactivator MDL 72527 to cancer cells: comparison with a saturated structural analogue.

Nikolaus Seiler, Jacques Renault, Francine Gossé, Stamatiki Roussi, Francis Raul

Index: Int. J. Oncol. 27(6) , 1669-76, (2005)

Full Text: HTML

Abstract

MDL 72527 (N1,N4-di-2,3-butadienyl-1,4-butanediamine) is a selective inactivator of polyamine oxidase with therapeutic potential. However, the development of lethal toxic effects due to prevention of spermine degradation is a considerable disadvantage of the compound. Since the cytotoxicity of MDL 72527 was postulated to be independent of its anti-polyamine oxidase activity, its cytotoxicity to cancer cells was compared with that of a close analogue that is devoid of structural features enabling mechanism-based inactivation of polyamine oxidase. N1,N4-di-n-butyl-1,4-butanediamine proved to be a cytotoxic agent of considerable potency, which induces mainly non-apoptotic cell death, whereas MDL 72527 causes under identical conditions both, apoptotic and non-apoptotic cell death. The sensitivity of cells to both compounds is presumably dependent of their glutathione content.

Related Compounds

  • MDL 72527

Related Articles:

How important is the oxidative degradation of spermine?: minireview article.

2004-07-01

[Amino Acids 26(4) , 317-9, (2004)]

Polyamine metabolism is involved in adipogenesis of 3T3-L1 cells.

2012-02-01

[Amino Acids 42(2-3) , 619-26, (2012)]

Synergism between apple procyanidins and lysosomotropic drugs: potential in chemoprevention.

2006-01-01

[Anticancer Res. 26(5A) , 3381-5, (2006)]

Perturbation of polyamine metabolism and its relation to cell death in human colon cancer cells treated by 7beta-hydroxycholesterol and 7beta-hydroxysitosterol.

2006-12-01

[Int. J. Oncol. 29(6) , 1549-54, (2006)]

MDL 72527 and spermine oxidation products induce a lysosomotropic effect and mitochondrial alterations in tumour cells.

2007-04-01

[Biochem. Soc. Trans. 35(Pt 2) , 343-8, (2007)]

More Articles...