Abstract |
Kahweol, the coffee-specific deterpene, has been shown to have potential anti- cancer effects against several cancers. However, the molecular mechanisms underlying the anti- cancer activity of kahweol have not yet established. In this study, we investigated whether kahweol could show anti- cancer effects on oral squamous cell lines (OSCCs), HN22 and HSC4. We conducted an 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay, 4'-6-diamidino2-phenylindole ( DAPI) staining, propidium iodide staining, immunocytochemistry, and Western blot analysis for the characterization of kahweol and the underlying signaling pathway. We determined that kahweol-treated cells showed significantly decreased cell viability and increased nuclear condensation and an increased sub-G1 population in OSCCs. Interestingly, suppression of the transcription factor specificity protein 1 (Sp1) was followed by induced apoptosis by kahweol in a dose-dependent manner. In addition, kahweol modulated the protein expression level of the Sp1 regulatory genes including cell cycle regulatory proteins and anti-apoptotic proteins, resulting in apoptosis. Taken together, results from these findings suggest that kahweol may be a potential anti- cancer drug candidate to induce apoptotic cell death through downregulation of Sp1 in OSCCs.
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Authors | Jung-Il Chae, Young-Joo Jeon, Jung-Hyun Shim |
Journal | Phytotherapy research : PTR
(Phytother Res)
Vol. 28
Issue 12
Pg. 1879-86
(Dec 2014)
ISSN: 1099-1573 [Electronic] England |
PMID | 25196544
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2014 John Wiley & Sons, Ltd. |
Chemical References |
- Antineoplastic Agents, Phytogenic
- Diterpenes
- Sp1 Transcription Factor
- Sp1 protein, human
- kahweol
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Topics |
- Antineoplastic Agents, Phytogenic
(pharmacology)
- Apoptosis
(drug effects)
- Carcinoma, Squamous Cell
(pathology)
- Cell Line, Tumor
(drug effects)
- Cell Proliferation
(drug effects)
- Cell Survival
(drug effects)
- Diterpenes
(pharmacology)
- Down-Regulation
- Humans
- Mouth Neoplasms
(pathology)
- Signal Transduction
(drug effects)
- Sp1 Transcription Factor
(metabolism)
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