膜輸送系を標的とする光線力学的治療の効果増強剤の新薬シーズ開発

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Author: 遠藤, 良夫ほか

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Publication date: 2017-04-28

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Note (General)：: 金沢大学がん進展制御研究所5-アミノレブリン酸（ALA）は従来の光線力学的治療で用いられてきたポルフィリン関連化合物とは異なり、がん細胞内でプロトポルフィリンIXに変換され、光感受性物質として活性化し、殺細胞効果を発揮する。本研究ではALAとの同時処理により細胞内PpIX量を増加させてPDT効果を増...

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Material Type: 文書・図像類
Title: 膜輸送系を標的とする光線力学的治療の効果増強剤の新薬シーズ開発
Author/Editor: 遠藤, 良夫
Endo, Yoshio
Author Heading: 遠藤, 良夫
Endo, Yoshio
Publication Date: 2017-04-28
Publication Date (W3CDTF): 2017-04-28
Alternative Title: Development of novel Schiff base derivative for enhancing the anticancer potential of 5-aminolevulinic acid-based photodynamic therapy
Periodical title: 平成28(2016)年度科学研究費補助金基盤研究(C) 研究成果報告書 = 2016 Fiscal Year Final Research Report
No. or year of volume/issue: 2014-04-01 - 2017-03-31
Volume: 2014-04-01 - 2017-03-31
Pages: 4p.-
Text Language Code: jpn
Subject Heading: 光線力学的治療
5-アミノレブリン酸
効果増強
Target Audience: 一般
Note (General): 金沢大学がん進展制御研究所
5-アミノレブリン酸（ALA）は従来の光線力学的治療で用いられてきたポルフィリン関連化合物とは異なり、がん細胞内でプロトポルフィリンIXに変換され、光感受性物質として活性化し、殺細胞効果を発揮する。本研究ではALAとの同時処理により細胞内PpIX量を増加させてPDT効果を増強する低分子化合物TX-816の誘導体開発を実施し、TX-816のアルキルベンゼン型誘導体が有用なリード化合物になることを見出した。
5-Aminolevulinic acid (ALA) is now widely used for photodynamic diagnosis and photodynamic therapy (ALA-PDT) of various cancers. In the heme biosynthesis pathway, ALA is converted to protoporphyrin IX (PpIX). Following excitation with blue light (405 nm), the accumulated PpIX emits a red fluorescence (635 nm). Thus, cancer tissue can be effectively visualized by the PpIX fluorescence. Furthermore, absorption of light beyond 630 nm by PpIX leads to the production of reactive oxygen species that can induce cell death in various cancer cells. Previously, we found that the Schiff base derivative TX-816 can significantly increase the effect of ALA-PDT by accelerating the intracellular PpIX accumulation. In this study, we synthesized TX-816 derivatives in which 2-chloro-4-nitroaniline was substituted with 4-alkyl aniline. These derivatives were chemically more stable than TX-816 was. The derivatives may become a potent lead compounds for the development of prodrug-type ALA-PDT sensitizers.
研究課題/領域番号:26430160, 研究期間(年度):2014-04-01 - 2017-03-31
DOI: 10.24517/00055481
Source: https://kanazawa-u.repo.nii.ac.jp/?action=repository_action_common_download&item_id=49168&item_no=1&attribute_id=26&file_no=1
https://kanazawa-u.repo.nii.ac.jp/?action=repository_action_common_download&item_id=49168&item_no=1&attribute_id=26&file_no=1
Access Restrictions: 限定公開
Rights (production): CC BY-NC-ND
Related Material: https://kaken.nii.ac.jp/search/?qm=30211783
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-26430160/
https://kaken.nii.ac.jp/report/KAKENHI-PROJECT-26430160/26430160seika/
Data Provider (Database): 国立情報学研究所 : 学術機関リポジトリデータベース（IRDB）（機関リポジトリ）
https://irdb.nii.ac.jp
Original Data Provider (Database): 金沢大学 : 金沢大学学術情報リポジトリKURA