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Goyazensolide Induces Apoptosis in Cancer Cells in vitro and in vivo.
| Content Provider | PubMed Central |
|---|---|
| Author | Acuña, Ulyana Muñoz Shen, Qi Ren, Yulin Lantvit, Daniel D. Wittwer, Jennifer A. Kinghorn, A. Douglas Swanson, Steven M. Blanco, Esperanza J. Carcache De |
| Abstract | As part of the screening program for anticancer agents from natural sources, the sesquiterpene lactone goyazensolide (GZL) was identified as a potent NF-κB inhibitor. The hollow-fiber assay was used to evaluate the anti-tumor efficacy of GZL in vivo. The mechanistic effects of GZL were evaluated in the HT-29 colonic cell line to reveal the pathway through which GZL exerts its effects. NF-κB subunits p65 and p50 were inhibited, and the upstream mediator IκB kinase (IKKβ) was downregulated in a dose-dependent manner. Apoptosis was mediated by caspase-3, and cell cycle arrest was detected in G1-phase. Consequently, 96% of the cell population was in sub G1-phase after treatment with GZL (10 μM).The antitumor effect of GZL was observed at a dose of 12.5 mg/kg. Cell adhesion was affected as a result of NF-κB inhibition. GZL appears to selectively target the transcription factor NF-κB. In summary, GZL sensitizes HT-29 colon cancer cells to apoptosis and cell death in a dose-dependent manner both in vivo and in vitro, through NF-κB inhibition (IC50 = 3.8 μM). Thus, it is a new potent lead compound for further development into a new effective chemotherapeutic agent. |
| Related Links | http://dx.doi.org/10.3923/ijcr.2013.36.53 |
| Ending Page | 53 |
| Page Count | 18 |
| Starting Page | 36 |
| File Format | |
| ISSN | 18119727 |
| e-ISSN | 18119735 |
| Journal | International journal of cancer research |
| Issue Number | 2 |
| Volume Number | 9 |
| Language | English |
| Publisher Date | 2013-02-01 |
| Access Restriction | Open |
| Subject Keyword | Cancer Research Oncology Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cancer Research Oncology |