論文 - 詳細
| RRC ID | 42695 |
|---|---|
| 著者 | Akatsu Y, Ohshima N, Yamagishi Y, Nishishiro M, Wakabayashi H, Kurihara T, Kikuchi H, Katayama T, Motohashi N, Shoji Y, Nakashima H, Sakagami H. |
| タイトル | Apoptosis-inducing activity of trihaloacetylazulenes against human oral tumor cell lines. |
| ジャーナル | Anticancer Res |
| Abstract |
Twenty-six trihaloacetylazulene derivatives were investigated for their tumor-specific cytotoxicity and apoptosis-inducing activity against three human normal cells (HGF, HPC, HPLF) and four human tumor cell lines (HSC-2, HSC-3, HSC-4, HL-60). The trichloroacetylazulenes [1b-13b] generally showed higher cytotoxicity as compared to the corresponding trifluoroacetylazulenes [1a-13a]. The trichloroacetylazulenes [1b-13b] also showed higher tumor-specific cytotoxicity (expressed as TS value) than the corresponding trifluoroacetylazulenes [1a-13a]. Especially, 2,3-dimethyl-1-trichloroacetylazulene [5b] and 1,3-ditrichloroacetyl-4,6,8-trimethylazulene [11b] showed the highest cytotoxicity and tumor specificity (TS > 35.6 and > 44.1, respectively). These compounds induced internucleosomal DNA fragmentation in HL-60 cells, but not in HSC-2 and HSC-3 cells, but activated caspase-3, -8 and -9 in all of these cells, suggesting the activation of both mitochondria-independent (extrinsic) and dependent (intrinsic) pathways. Western blot analysis showed that two compounds [5b, 11b] slightly increased the intracellular concentration of pro-apoptotic proteins (Bad, Bax) in HSC-2 cells. None of the 26 compounds showed anti-HIV activity. These results suggest [5b] and [11b] as possible candidates for future cancer chemotherapy. |
| 巻・号 | 26(3A) |
| ページ | 1917-23 |
| 公開日 | 2006-1-1 |
| PMID | 16827125 |
| MeSH | Apoptosis / drug effects Azulenes / chemistry Azulenes / pharmacology* Carcinoma, Squamous Cell / drug therapy* Carcinoma, Squamous Cell / pathology Cell Line Cell Line, Tumor Drug Screening Assays, Antitumor Fibroblasts / cytology Fibroblasts / drug effects HL-60 Cells Humans Hydrocarbons, Halogenated / chemistry Hydrocarbons, Halogenated / pharmacology Mouth Neoplasms / drug therapy* Mouth Neoplasms / pathology Structure-Activity Relationship |
| IF | 1.994 |
| 引用数 | 18 |
| WOS 分野 | ONCOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | HSC-2(RCB1945) HSC-3(RCB1975) HSC-4(RCB1902) |