| ID | JOS-ijms23052601 |
| 著者：名前 | 内藤, 琴音/ 折原, 悠太/ 坂上, 宏/ 三浦, 拓瑞/ 佐藤, 慶太郎/ 天野, 滋/ 坂東, 健二郎/ 飯島, 洋介/ 黒﨑, 宏太/ 植沢, 芳広/ 橋本, 雅司/ 若林, 英嗣 |
| 著者：別形式 | Naitoh, Kotone / Orihara, Yuta / Sakagami, Hiroshi / Miura, Takumi / Satoh, Keitaro / Amano, Shigeru / Bandow, Kenjiro / Iijima, Yosuke / Kurosaki, Kota / Uesawa, Yoshihiro / Hashimoto, Masashi / Wakabayashi, Hidetsugu |
| 著者：カナ | ナイトウ, コトネ/ オリハラ, ユウタ/ サカガミ, ヒロシ/ ミウラ, タクミ/ サトウ, ケイタロウ/ アマノ, シゲル/ バンドウ, ケンジロウ/ イイジマ, ヨウスケ/ クロサキ, コウタ/ ウエサワ, ヨシヒロ/ ハシモト, マサシ/ ワカバヤシ, ヒデツグ |
| 著者：所属 | 城西大学理学部 / 城西大学理学部 / 明海大学歯科医学総合研究所 / 城西大学理学部 / 明海大学歯学部 / 明海大学歯科医学総合研究所 / 明海大学歯学部 / 埼玉医科大学総合医療センター歯科口腔外科 / 明治薬科大学 医療分子解析学研究室 / 明治薬科大学 医療分子解析学研究室 / 城西大学理学部 / 城西大学理学部 |
| 著者：所属(別形式） | Josai University, Faculty of Science / Josai University, Faculty of Science / Meikai University, Research Institute of Odontology / Josai University, Faculty of Science / Meikai University School of Dentistry, Department of Diagnostics and Therapeutics Sciences, Division of Pharmacology / Meikai University, Research Institute of Odontology / Meikai University School of Dentistry, Department of Oral Biology and Tissue Engineering, Division of Biochemistry / Saitama Medical University, Saitama Medical Center, Department of Oral and Maxillofacial Surgery / Meiji Pharmaceutical University, Department of Medical Molecular Informatics / Meiji Pharmaceutical University, Department of Medical Molecular Informatics / Josai University, Faculty of Science / Josai University, Faculty of Science |
| 著者版フラグ | publisher |
| 出版者 | MDPI |
| 冊子ISSN | 16616596 |
| 電子ISSN | 14220067 |
| 掲載誌名 | |
| 巻 | 23 |
| 号 | 5 |
| 刊行年月 | 2022-03 |
| 開始ページ | 1 |
| 終了ページ | 13 |
| コンテンツ作成日 | 2022-02-06 |
| コンテンツ修正日 | 2022-02-21 |
| コンテンツ登録日 | 2022-05-31 |
| 識別番号：DOI | info:doi/10.3390/ijms23052601 |
| 識別番号：DOI（リンク） | |
| PubMed番号 | 35269748 |
| 抄録 | Background: Very few papers covering the anticancer activity of azulenes have been reported, as compared with those of antibacterial and anti-inflammatory activity. This led us to investigate the antitumor potential of fifteen 4,6,8-trimethyl azulene amide derivatives against oral malignant cells. Methods: 4,6,8-Trimethyl azulene amide derivatives were newly synthesized. Anticancer activity was evaluated by tumor-specificity against four human oral squamous cell carcinoma (OSCC) cell lines over three normal oral cells. Neurotoxicity was evaluated by cytotoxicity against three neuronal cell lines over normal oral cells. Apoptosis induction was evaluated by Western blot and cell cycle analyses. Results: Among fifteen derivatives, compounds 7, 9, and 15 showed the highest anticancer activity, and relatively lower neurotoxicity than doxorubicin, 5-fluorouracil (5-FU), and melphalan. They induced the accumulation of a comparable amount of a subG1 population, but slightly lower extent of caspase activation, as compared with actinomycin D, used as an apoptosis inducer. The quantitative structure–activity relationship analysis suggests the significant correlation of tumor-specificity with a 3D shape of molecules, and possible involvement of inflammation and hormone receptor response pathways. Conclusions: Compounds 7 and 15 can be potential candidates of a lead compound for developing novel anticancer drugs. |
| キーワード | |
| 注記 | Licensee MDPI, Basel, Switzerland.This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
| 言語 | eng |
| 資源タイプ | text |
| ジャンル | |
| フォーマット | application/pdf |
| 権利 | Copyright © 2022 by the authors. |
| このアイテムを表示する：本文(pdf) |  ( 3.7MB) ダウンロード回数： 回 |
| このアイテムを表示する：URI | |
