| ID | JOS-02507005-34-4877 |
| 著者：名前 | 島田, 智哉子/ 植沢, 芳広/ 石原, 真理子/ Kagaya, Hajime/ 金本, 大成/ 寺久保, 繁美/ 中島, 秀喜/ 高尾, 浩一/ 宮城, 昂幹/ 杉田, 義昭/ 坂上, 宏 |
| 著者：別形式 | Shimada, Chiyako / Uesawa, Yoshihiro / Ishihara, Mariko / Kagaya, Hajime / Kanamoto, Taisei / Terakubo, shigemi / Nakashima, hideki / Takao, Koichi / Miyashiro, Takaki / Sugita, Yoshiaki / Sakagami, Hiroshi |
| 著者：カナ | シマダ, チヤコ/ ウエサワ, ヨシヒロ/ イシハラ, マリコ/ カガヤ, ハジメ/ カナモト, タイセイ/ テラクボ, シゲミ/ ナカシマ, ヒデキ/ タカオ, コウイチ/ ミヤシロ, タカキ/ スギタ, ヨシアキ/ サカガミ, ヒロシ |
| 著者：所属 | 明海大学歯学部 / 明治薬科大学 / 明海大学歯学部 / 明治薬科大学 / 聖マリアンナ医科大学 / 聖マリアンナ医科大学 / 聖マリアンナ医科大学 / 城西大学薬学部 / 城西大学薬学部 / 城西大学薬学部 / 明海大学歯学部 |
| 著者：所属(別形式） | Meikai University School of Dentistry, Department of Diagnostic and Therapeutic Sciences, Division of Pharmacology / Meiji Pharmaceutical University, Department of Clinical Pharmaceutics / Meikai University School of Dentistry, Department of Diagnostic and Therapeutic Sciences, Basic Chemistry / Meiji Pharmaceutical University, Department of Clinical Pharmaceutics / St. Marianna University School of Medicine / St. Marianna University School of Medicine / St. Marianna University School of Medicine / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Meikai University School of Dentistry, Department of Diagnostic and Therapeutic Sciences, Division of Pharmacology |
| 著者版フラグ | publisher |
| 出版地 | Athens |
| 出版者 | International Institute of Anticancer Research |
| NCID | AA12440673 |
| 冊子ISSN | 02507005 |
| 電子ISSN | 17917530 |
| 掲載誌名 | |
| 巻 | 34 |
| 号 | 9 |
| 刊行年月 | 2014-09 |
| 開始ページ | 4877 |
| 終了ページ | 4884 |
| コンテンツ作成日 | 2014-07-01 |
| コンテンツ登録日 | 2014-11-07 |
| 抄録 | Background: A total of 12 piperic acid amides, including piperine, were subjected to quantitative structure?activity relationship (QSAR) analysis, based on their cytotoxicity, tumor selectivity and anti-HIV activity, in order to find new biological activities. Materials and Methods: Cytotoxicity against four human oral squamous cell carcinoma (OSCC) cell lines and three human oral normal cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Tumor selectivity was evaluated by the ratio of the mean 50% cytotoxic concentration (CC50) against normal oral cells to that against OSCC cell lines. Anti-HIV activity was evaluated by the ratio of the CC50 to 50% HIV infection-cytoprotective concentration (EC50). Physicochemical, structural, and quantum-chemical parameters were calculated based on the conformations optimized by LowModeMD method followed by density functional theory method. Results: All compounds showed low-to-moderate tumor selectivity, but no anti-HIV activity. N-Piperoyldopamine (8) which has a catechol moiety, showed the highest tumor selectivity, possibly due to its unique molecular shape and electrostatic interaction, especially its largest partial equalization of orbital electronegativities and vsurf descriptors. Conclusion: The present study suggests that molecular shape and ability for electrostatic interaction are useful parameters for estimating the tumor selectivity of piperic acid amides. |
| 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 c2014 International Institute of Anticancer Research |
| このアイテムを表示する：本文(pdf) |  ( 418.0KB) ダウンロード回数： 回 |
| このアイテムを表示する：URI | |
