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Potential Antitumor Activity of 2-O-α-D-Glucopyranosyl-6-O-(2-Pentylheptanoyl)-L-Ascorbic Acid
https://tokushima-u.repo.nii.ac.jp/records/2007507
https://tokushima-u.repo.nii.ac.jp/records/2007507d02505cd-9f09-42fc-bbce-83465f89d8f7
| 名前 / ファイル | ライセンス | アクション |
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ijms_19_2_535.pdf (3.18 MB)
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| Item type | 文献 / Documents(1) | |||||||||||||||||||||||||||||
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| 公開日 | 2020-12-09 | |||||||||||||||||||||||||||||
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| アクセス権 | open access | |||||||||||||||||||||||||||||
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| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||||||||||||||||||||||
| 資源タイプ | journal article | |||||||||||||||||||||||||||||
| 出版社版DOI | ||||||||||||||||||||||||||||||
| 関連識別子 | https://doi.org/10.3390/ijms19020535 | |||||||||||||||||||||||||||||
| 関連名称 | 10.3390/ijms19020535 | |||||||||||||||||||||||||||||
| 出版タイプ | ||||||||||||||||||||||||||||||
| 出版タイプ | VoR | |||||||||||||||||||||||||||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||||||||||||||||||||
| タイトル | ||||||||||||||||||||||||||||||
| タイトル | Potential Antitumor Activity of 2-O-α-D-Glucopyranosyl-6-O-(2-Pentylheptanoyl)-L-Ascorbic Acid | |||||||||||||||||||||||||||||
| 著者 |
ミウラ, カオリ
× ミウラ, カオリ
× ハラグチ, ミサキ
× イトウ, ヒデユキ
× 田井, 章博
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| 内容記述 | Intravenous administration of high-dose ascorbic acid (AA) has been reported as a treatment for cancer patients. However, cancer patients with renal failure cannot receive this therapy because high-dose AA infusion can have side effects. To solve this problem, we evaluated the antitumor activity of a lipophilic stable AA derivative, 2-O-α-D-glucopyranosyl-6-O-(2-pentylheptanoyl)-L-ascorbic acid (6-bOcta-AA-2G). Intravenous administration of 6-bOcta-AA-2G suppressed tumor growth in colon-26 tumor-bearing mice more strongly than did AA, even at 1/10 of the molar amount of AA. Experiments on the biodistribution and clearance of 6-bOcta-AA-2G and its metabolites in tumor-bearing mice showed that 6-bOcta-AA-2G was hydrolyzed to 6-O-(2-propylpentanoyl)-L-ascorbic acid (6-bOcta-AA) slowly to yield AA, and the results suggested that this characteristic metabolic pattern is responsible for making the antitumor activity of 6-bOcta-AA-2G stronger than that of AA and that the active form of 6-bOcta-AA-2G showing antitumor activity is 6-bOcta-AA. In in vitro experiments, the oxidized form of 6-bOcta-AA as well as 6-bOcta-AA showed significant cytotoxicity, while the oxidized forms of ascorbic acid showed no cytotoxicity at all, suggesting that the antitumor activity mechanism of 6-bOcta-AA-2G is different from that of AA and that the antitumor activity is due to the reduced and oxidized form of 6-bOcta-AA. The findings suggest that 6-bOcta-AA-2G is a potent candidate as an alternative drug to intravenous high-dose AA. | |||||||||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||||||||
| 主題 | ascorbic acid | |||||||||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||||||||
| 主題 | stable ascorbic acid derivatives | |||||||||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||||||||
| 主題 | acyl ascorbic acid | |||||||||||||||||||||||||||||
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| 主題 | antitumor activity | |||||||||||||||||||||||||||||
| 書誌情報 |
en : International Journal of Molecular Sciences 巻 19, 号 2, p. 535, 発行日 2018-02-10 |
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| 収録物識別子タイプ | ISSN | |||||||||||||||||||||||||||||
| 収録物識別子 | 14220067 | |||||||||||||||||||||||||||||
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| 収録物識別子タイプ | ISSN | |||||||||||||||||||||||||||||
| 収録物識別子 | 16616596 | |||||||||||||||||||||||||||||
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| 収録物識別子タイプ | NCID | |||||||||||||||||||||||||||||
| 収録物識別子 | AA12038549 | |||||||||||||||||||||||||||||
| 出版者 | ||||||||||||||||||||||||||||||
| 出版者 | MDPI | |||||||||||||||||||||||||||||
| 権利情報 | ||||||||||||||||||||||||||||||
| 権利情報 | © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). | |||||||||||||||||||||||||||||
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| 識別子 | 359255 | |||||||||||||||||||||||||||||
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| 言語 | eng | |||||||||||||||||||||||||||||
