| Item type |
文献 / Documents(1) |
| 公開日 |
2022-08-22 |
| アクセス権 |
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|
アクセス権 |
open access |
| 資源タイプ |
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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 |
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|
関連識別子 |
https://doi.org/10.1016/j.bbrep.2022.101329 |
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関連名称 |
10.1016/j.bbrep.2022.101329 |
| 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 |
Development of a novel tocopheryl ester for suppression of lipid accumulation without cytotoxicity by optimization of dicarboxylic ester moiety |
| 著者 |
ヤマサキ, ミサキ
セト, ユイカ
大園, 瑞音
中尾, 允泰
重永, 章
大髙, 章
佐野, 茂樹
小暮, 健太朗
|
| 抄録 |
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内容記述 |
Tocopheryl succinate (Tsuc) is a succinic acid ester of the well-known antioxidant α-tocopherol (T). Tsuc exhibits various biological activities, including tumor growth suppression via activation of cell signaling and prevention of lipid accumulation in mouse adipocyte 3T3-L1 cells. The latter findings suggest that Tsuc may be a drug candidate for the treatment of obesity. However, Tsuc was found to induce apoptosis of normal cells (in addition to cancer cells), demonstrating the need to reduce the cytotoxicity of Tsuc without losing the suppression effect on lipid accumulation. Based on our previous findings, we focused on the ester structure of Tsuc for controlling cytotoxicity. Herein, we examined the cytotoxicity and lipid accumulation suppression effect of various T ester derivatives. We found that the terminal carboxylic group is necessary for suppression of lipid accumulation. We synthesized tocopheryl glutarate (Tglu) and tocopheryl adipate (Tadi) by elongation of carbon atoms 1 and 2 of the dicarboxylic moiety, respectively. Tglu and Tadi did not show any cytotoxicity, and both esters suppressed lipid accumulation, although their suppression activities were weaker than that of Tsuc. Tadi showed a more potent lipid accumulation inhibitory effect than Tglu. Although Tadi inhibited lipogenesis and promoted lipolysis, lipolysis was induced at lower concentrations than inhibition of lipogenesis, suggesting that Tadi mainly affects lipolysis. Taken together, we succeeded in the reduction of cytotoxicity, without loss of the suppression effect on lipid accumulation, by elongation of the dicarboxylic moiety of Tsuc. Tadi may be a promising candidate as an anti-obesity drug. |
| キーワード |
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|
主題 |
Tocopheryl ester |
| キーワード |
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|
主題 |
Cytotoxicity |
| キーワード |
|
|
主題 |
Lipid accumulation suppression |
| キーワード |
|
|
主題 |
Anti-obesity |
| 書誌情報 |
en : Biochemistry and Biophysics Reports
巻 31,
p. 101329,
発行日 2022-08-16
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| 収録物ID |
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収録物識別子タイプ |
ISSN |
|
収録物識別子 |
24055808 |
| 出版者 |
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|
出版者 |
Elsevier |
| 権利情報 |
|
|
権利情報 |
This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
| EID |
|
|
識別子 |
390033 |
| 言語 |
|
|
言語 |
eng |
bbrep_31_101329.pdf (2.41 MB)
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