期刊
PLOS ONE
卷 11, 期 3, 页码 -出版社
PUBLIC LIBRARY SCIENCE
DOI: 10.1371/journal.pone.0149832
关键词
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资金
- EU [HEALH-F2-2008-20166]
- Pfizer Hungary Award [TAMOP-4.2.2.A-11/1/KONV-2012-0035]
- OTKA grant [K82039, TAMOP -4.2.2.A-11/1/KONV-2012-0035]
- Hungarian Brain Research Program [KTIA-NAP_13-2014-0007]
- AVIDIN Ltd.
- AVICOR Ltd.
- [GOP-1.1.1-11-2011-0003]
C-150 a Mannich-type curcumin derivative, exhibited pronounced cytotoxic effects against eight glioma cell lines at micromolar concentrations. Inhibition of cell proliferation by C-150 was mediated by affecting multiple targets as confirmed at transcription and protein level. C-150 effectively reduced the transcription activation of NFkB, inhibited PKC-alpha which are constitutively over-expressed in glioblastoma. The effects of C-150 on the Akt/Notch signaling were also demonstrated in a Drosophila tumorigenesis model. C-150 reduced the number of tumors in Drosophila with similar efficacy to mitoxantrone. In an in vivo orthotopic glioma model, C-150 significantly increased the median survival of treated nude rats compared to control animals. The multi-target action of C-150, and its preliminary in vivo efficacy would render this curcumin analogue as a potent clinical candidate against glioblastoma.
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