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Comparison of the antiproliferative properties of
antiestrogenic drugs (nafoxidine and clomiphene) on glioma cells in vitro
Yaz G, Kabadere S, Oztopcu P, Durmaz R, Uyar R
Osmangazi University, Medical Faculty, Department of Physiology, Eskisehir,
Turkey.
The antitumoral activity of nonsteroidal antiestrogens on C6 and low passage of
human glioma cells was investigated.
Tamoxifen and its metabolite,
4-hydroxytamoxifen, did not influence viability of the human cells, but
tamoxifen had a limited antiproliferative effect on C6 cells (IC50: 49
micromol/l).
The derivatives of tamoxifen, nafoxidine and clomiphene, caused
reduction of living cell number in a dose-dependent manner.
These two drugs
showed differences in their potency following 24-hour incubation in a humidified
atmosphere with 37 degrees C and 5% CO2.
Obtained from a tetrazolium-formazan
growth rate assay, IC50 of nafoxidine for C6 cells was calculated as 44
micromol/l and for the human cells as 16.5 micromol/l.
The calculated IC50 dose
of clomiphene for C6 is 16 micromol/l and for the human cells 13 micromol/l.
Compared to the other drugs we used, it is clear that clomiphene is the most
efficient inhibitor of C6 and the human glioma cells.
These preliminary results
suggest that nafoxidine and clomiphene possess antiproliferative effect on two
different sources of glioma cells and therefore, instead of tamoxifen, multiple
activities of these drugs may enable their use in combination therapy of
glioblastoma malignancies.
PMID: 15289732 [PubMed - in process]
Source: http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15289732
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