| ID | JOS-j.toxrep.2015.09.009 |
| 著者：名前 | 坂上, 宏/ 島田, 智哉子/ Kanda, Yumiko/ 天野, 修/ Sugimoto, Masahiro/ Ota, Sana/ Soga, Tomoyoshi/ 冨田, 勝/ Sato, Akira/ Tanuma, Sei-ichi/ 高尾, 浩一/ 杉田, 義昭 |
| 著者：別形式 | Sakagami, Hiroshi / Shimada, Chiyako / Kanda, Yumiko / Amano, Osamu / Sugimoto, Masahiro / Ota, Sana / Soga, Tomoyoshi / Tomita, Masaru / Sato, Akira / Tanuma, Sei-ichi / Takao, Koichi / Sugita, Yoshiaki |
| 著者：カナ | サカガミ, ヒロシ/ シマダ, チヤコ/ カンダ, ユミコ/ アマノ, オサム/ スギモト, マサヒロ/ オオタ, サナ/ ソガ, トモヨシ/ トミタ, マサル/ サトウ, アキラ/ タヌマ, セイイチ/ タカオ, コウイチ/ スギタ, ヨシアキ |
| 著者：所属 | 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 / 慶應義塾大学先端生命科学研究所 / 慶應義塾大学先端生命科学研究所 / 慶應義塾大学先端生命科学研究所 / 慶應義塾大学先端生命科学研究所 / 東京理科大学薬学部 / 東京理科大学薬学部 / 城西大学薬学部 / 城西大学薬学部 |
| 著者：所属(別形式） | Meikai University School of Dentistry, Division of Pharmacology / Meikai University School of Dentistry, Division of Pharmacology / Meikai University School of Dentistry, Department of Electron Microscope / Meikai University School of Dentistry, Division of Anatomy / Keio University, Institute for Advanced Bioscience / Keio University, Institute for Advanced Bioscience / Keio University, Institute for Advanced Bioscience / Keio University, Institute for Advanced Bioscience / Tokyo University of Science, Faculty of Pharmaceutical Sciences, Department of Biochemistry / Tokyo University of Science, Faculty of Pharmaceutical Sciences, Department of Biochemistry / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences |
| 著者版フラグ | publisher |
| 出版者 | Elsevier |
| 電子ISSN | 22147500 |
| 掲載誌名 | |
| 巻 | 2 |
| 刊行年月 | 2015 |
| 開始ページ | 1281 |
| 終了ページ | 1290 |
| コンテンツ作成日 | 2015-07-07 |
| コンテンツ修正日 | 2015-09-26 |
| コンテンツ登録日 | 2017-02-06 |
| 識別番号：DOI | info:doi/10.1016/j.toxrep.2015.09.009 |
| 識別番号：DOI（リンク） | |
| 抄録 | 4H-1-benzopyran-4-ones (chromones) are important naturally-distributing compounds. As compared with flavones, isoflavones and 2-styrylchromones, there are only few papers of 3-styrylchromones that have been published. We have previously reported that among fifteen 3-styrylchromone derivatives, three new synthetic compounds that have OCH3 group at the C-6 position of chromone ring, (E)-3-(4-hydroxystyryl)-6-methoxy-4H-chromen-4-one (compound 11), (E)-6-methoxy-3-(4-methoxystyryl)-4H-chromen-4-one (compound 4), (E)-6-methoxy-3-(3,4,5-trimethoxystyryl)-4H-chromen-4-one (compound 6) showed much higher cytotoxicities against four epithelial human oral squamous cell carcinoma (OSCC) lines than human normal oral mesenchymal cells. In order to further confirm the tumor specificities of these compounds, we compared their cytotoxicities against both human epithelial malignant and non-malignant cells, and then investigated their effects on fine cell structures and metabolic profiles and cell death in human OSCC cell line HSC-2. Cytotoxicities of compounds 4, 6, 11 were assayed with MTT method. Fine cell structures were observed under transmission electron microscope. Cellular metabolites were extracted with methanol and subjected to CE-TOFMS analysis. Compounds 4, 6, 11 showed much weaker cytotoxicity against human oral keratinocyte and primary human gingival epithelial cells, as compared with HSC-2, confirming their tumor-specificity, whereas doxorubicin and 5-FU were highly cytotoxic to these normal epithelial cells, giving unexpectedly lower tumor-specificity. The most cytotoxic compound 11, induced the mitochondrial vacuolization, autophagy suppression followed by apoptosis induction, and changes in the metabolites involved in amino acid and glycerophospholipid metabolisms. Chemical modification of lead compound 11 may be a potential choice for designing new type of anticancer drugs. |
| キーワード | |
| 注記 | Open Access |
| 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 2015 The Authors. Published by Elsevier Inc. |
| このアイテムを表示する：本文(pdf) |  ( 2.4MB) ダウンロード回数： 回 |
| このアイテムを表示する：URI | |
