論文 - 詳細
| RRC ID | 52686 |
|---|---|
| 著者 | Wada T, Maruyama R, Irie Y, Hashimoto M, Wakabayashi H, Okudaira N, Uesawa Y, Kagaya H, Sakagami H. |
| タイトル | In Vitro Anti-tumor Activity of Azulene Amide Derivatives. |
| ジャーナル | In Vivo |
| Abstract |
BACKGROUND/AIM:There exist few research articles regarding the anticancer activity of azulene-related compounds. We investigated here the relative cytotoxicity of 10 azulene amide derivatives against cancer and normal cells. MATERIALS AND METHODS:Cytotoxicity against four human oral squamous cell carcinoma (OSCC) cell lines and three human oral normal cells (gingival fibroblasts, periodontal ligament fibroblasts and pulp cells) was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetra-zolium bromide method. Antitumor activity was evaluated by tumor-specificity (TS) (ratio of mean 50% cytotoxic concentration (CC50) against normal cells to that against OSCC cell lines) and potency-selectivity expression (PSE) (ratio of TS to CC50 against tumor cells). Apoptosis-inducing activity was evaluated by cleavage of poly ADP-ribose polymerase and caspase-3 with western blot analysis. RESULTS:N-Propylguaiazulenecarboxamide [1] showed the highest TS and PSE values, compared to that of doxorubicin, and induced apoptosis in two OSCC cell lines. QSAR analysis demonstrated that their tumor-specificity of azulene amide derivatives was correlated with hydrophobicity and molecular shape. CONCLUSION:Compound [1] can be considered as a lead compound for manufacturing new anticancer drug candidates. |
| 巻・号 | 32(3) |
| ページ | 479-486 |
| 公開日 | 2018-1-1 |
| DOI | 10.21873/invivo.11264 |
| PII | 32/3/479 |
| PMID | 29695549 |
| PMC | PMC6000805 |
| MeSH | Amides / chemistry Amides / pharmacology* Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Apoptosis / drug effects Azulenes* / chemistry Cell Line, Tumor Cell Proliferation / drug effects Cell Survival / drug effects Dose-Response Relationship, Drug Doxorubicin / pharmacology Fibroblasts / drug effects Humans Molecular Structure |
| IF | 1.541 |
| 引用数 | 5 |
| リソース情報 | |
| ヒト・動物細胞 | Ca9-22(RCB1976) HSC-2(RCB1945) HSC-3(RCB1975) HSC-4(RCB1902) |