Effect of N1,N14-bis(ethyl)homospermine on the growth of U-87 MG and SF-126 human brain tumor cells

The effect of the spermine analogue N1,N14-bis(ethyl)homospermine on the growth, polyamine levels, and survival of U-87 MG and SF-126 human brain tumor cells was examined in tissue culture. At concentrations of 10 mumols and above, N1,N14-bis(ethyl)homospermine inhibited growth significantly, caused...

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Bibliographic Details
Published in:Cancer research (Chicago, Ill.) Ill.), 1990-06, Vol.50 (11), p.3137-3140
Main Authors: BASU, H. S, PELLARIN, M, FEUERSTEIN, B. G, DEEN, D. F, BERGERON, R. J, MARTON, L. J
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
Brain Neoplasms - analysis
Brain Neoplasms - pathology
Cell Division - drug effects
General aspects
Humans
Medical sciences
Pharmacology. Drug treatments
Putrescine - analysis
Spermidine - analysis
Spermine - analogs & derivatives
Spermine - analysis
Spermine - pharmacology
Tumor Cells, Cultured - pathology
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Summary:The effect of the spermine analogue N1,N14-bis(ethyl)homospermine on the growth, polyamine levels, and survival of U-87 MG and SF-126 human brain tumor cells was examined in tissue culture. At concentrations of 10 mumols and above, N1,N14-bis(ethyl)homospermine inhibited growth significantly, caused a marked decrease in intracellular levels of the naturally occurring polyamines putrescine, spermidine, and spermine, and had a considerable cytotoxic effect on both cell lines after more than 96 h of treatment. In earlier studies we showed that the affinity of the analogue for calf thymus DNA was higher than the affinity of spermine, but that it did not aggregate DNA or release bound ethidium bromide from DNA as efficiently as spermine does. Therefore, the growth-inhibitory and cytotoxic effects of N1,N14-bis(ethyl)homospermine support our hypothesis that polyamine analogues that can enter cells, deplete intracellular levels of natural polyamines, and replace the natural polyamines from their binding sites on DNA without replacing function should act as antiproliferative agents.
ISSN:0008-5472
1538-7445