| ID | JOS-02507005-34-1743 |
| 著者：名前 | |
| 著者：別形式 | Sekine, Shota / Shimodaira, Chisato / Uesawa, Yoshihiro / Kagaya, Hajime / Kanda, Yumiko / Ishihara, Mariko / Amano, Osamu / Sakagami, Hiroshi / Wakabayashi, Hidetsugu |
| 著者：カナ | |
| 著者：所属 | 城西大学理学部 / 城西大学理学部 / 明治薬科大学 / 明治薬科大学 / 明海大学歯学部 / 明海大学歯学部 / 明海大学歯学部 / 明海大学歯学部 / 城西大学理学部 |
| 著者：所属(別形式） | Josai University, Faculty of Science / Josai University, Faculty of Science / Meiji Pharmaceutical University, Department of Clinical Pharmaceutice / Meiji Pharmaceutical University, Department of Clinical Pharmaceutice / Meikai University School of Dentistry / Meikai University School of Dentistry / Meikai University School of Dentistry / Meikai University School of Dentistry / Josai University, Faculty of Science |
| 著者版フラグ | publisher |
| 出版地 | Athens |
| 出版者 | Potamitis Press |
| NCID | AA12440673 |
| 冊子ISSN | 02507005 |
| 電子ISSN | 17917530 |
| 掲載誌名 | |
| 巻 | 34 |
| 号 | 4 |
| 刊行年月 | 2014-04 |
| 開始ページ | 1743 |
| 終了ページ | 1750 |
| コンテンツ作成日 | 2014-01-10 |
| コンテンツ登録日 | 2014-07-09 |
| 抄録 | Background: We newly synthesized twenty 2-aminotropones with different lengths of methylene units, with or without introduction of isopropyl group at C-4 position of the cycloheptatriene ring, which were then subjected to quantitative structure?activity relationship (QSAR) analysis. Materials and Methods: Viable cell number was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The tumor specificity was determined by the ratio of the mean CC50 (50% cytotoxic concentration) for the normal cells (human gingival fibroblast, HGF) to that of the human oral squamous cell carcinoma (OSCC) cell line (Ca9-22) derived from gingival tissue. Anti-UV activity (SI) was determined by the ratio of CC50 to EC50 (the concentration that increased the viability of UV-irradiated cells to 50%) using HSC-2 OSCC cells. Physico-chemical, structural, and quantum-chemical parameters were calculated based on conformations optimized by the LowModeMD method followed by the Discrete Fourier Transform (DFT) method. Fine-cell structure was observed by transmission electron microscopy. Results: 2-Aminotropones induced cytotoxicity, accompanied by the production of many rough endoplasmic reticula with enlarged lacuna and vacuolated mitochondria. Their cytotoxicity was a positive function of the number of methylene units and hydrophobicity. Anti-UV activity showed a good correlation with lowest unoccupied molecular orbital (LUMO) energy, but not with the length of methylene units. All twenty 2-aminotropones induced a very low level of hormetic growth stimulation at lower concentrations. Conclusion: Different types of chemical descriptors may be applicable to estimating the cytotoxicity and anti-UV activity of 2-aminotropones. |
| キーワード | |
| 言語 | eng |
| 資源タイプ | text |
| ジャンル | |
| フォーマット | application/pdf |
| 権利 | Copyright c 2014 International Institute of Anticancer Research |
| このアイテムを表示する：本文(pdf) |  ( 1.4MB) ダウンロード回数： 回 |
| このアイテムを表示する：URI | |
