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CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines
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- Authors
- Issue Date
- 2009
- Publisher
- Spandidos Publications
- Citation
- Oncol Rep 21:1413-1419,2009
- Keywords
- belotecan ; camptothecin analogue ; CKD-602 ; malignant glioma ; topoisomerase 1 inhibitor
- Abstract
- CKD-602 7-[2-(N-isopropylamino)ethyl]-(20S)-
camptothecin, belotecan) is a synthetic water-soluble camptothecin
derivative and topoisomerase inhibitor that has been
shown to have clinical anticancer effect against ovarian and
lung cancer. We studied its anticancer effects on four human
glioma cell lines, U87 MG, U343 MG, U251 MG and
LN229. Cell viability was quantified by a modified 2-(2-
methoxy-4-nitropheyl)-3-(4-nitropheyl)-5-(2,4-disulfophenyl)
-2H-tetrazolium, monosodium salt and significant time- and
dose-dependent cytotoxicity was observed in all cell lines.
Susceptibility to CKD-602 at 48 h after treatment varied
among the four cell lines and their IC50 value was as follows:
9.07 nM (95% CI 0.18-37.42) for LN229, 14.57 nM (95% CI
0.86-47.33) for U251 MG, 29.13 nM (95% CI 0.35-101.23)
for U343 MG, and 84.66 nM (95% CI 34.63-148.25) for U87
MG. CKD-602 induced cell cycle arrest at G2 phase and
produced antiproliferative activity and apoptosis in all cell
lines. Thus, CKD-602 showed a significant anticancer effect
on glioma cells in vitro and is a promising candidate for further
studies on malignant gliomas.
- ISSN
- 1021-335X
- Language
- English
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