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Effects of K-877, a novel selective PPARα modulator, on small intestine contribute to the amelioration of hyperlipidemia in low-density lipoprotein receptor knockout mice
http://hdl.handle.net/2241/00146710
http://hdl.handle.net/2241/0014671095c3e102-81f1-44f7-a189-043c0f8a4f8c
名前 / ファイル | ライセンス | アクション |
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JPS_133-4 (509.0 kB)
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Item type | Journal Article(1) | |||||
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公開日 | 2017-07-04 | |||||
タイトル | ||||||
タイトル | Effects of K-877, a novel selective PPARα modulator, on small intestine contribute to the amelioration of hyperlipidemia in low-density lipoprotein receptor knockout mice | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源 | http://purl.org/coar/resource_type/c_6501 | |||||
タイプ | journal article | |||||
著者 |
Takei, Kenta
× Takei, Kenta× Nakagawa, Yoshimi× Wang, Yunong× Han, Song-iee× Satoh, Aoi× Sekiya, Motohiro× Matsuzaka, Takashi× Shimano, Hitoshi |
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著者別名 |
中川, 嘉
× 中川, 嘉× 関谷, 元博× 松坂, 賢× 島野, 仁 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Peroxisome proliferator-activated receptor α (PPARα) is a well-known therapeutic target for treating hyperlipidemia. K-877 is a novel selective PPARα modulator (SPPARMα) that enhances PPARα transcriptional activity with high selectivity and potency, resulting in reduced plasma lipid levels. This study aimed to evaluate the effects of K-877 on hyperlipidemia in low-density lipoprotein receptor knockout (Ldlr−/−) mice, a mouse model of atherosclerosis. We revealed that K-877 administration significantly decreased plasma triglyceride (TG) and total cholesterol (TC) levels and increased plasma high-density lipoprotein cholesterol (HDL-C) levels in Ldlr−/− mice. K-877 administration to Ldlr−/− mice efficiently increased the gene expression of PPARα and its target genes related to fatty acid oxidation in the liver and small intestine. The same treatment significantly increased ATP-binding cassette a1 gene expression in the liver and small intestine and reduced Niemann Pick C1-like 1 gene expression in the small intestine, suggesting that K-877 administration induced HDL-C production in the liver and small intestine and reduced cholesterol absorption in the small intestine. In conclusion, K-877 administration had pronounced effects on the liver and small intestine in Ldlr−/− mice. K-877 is an attractive PPARα-modulating drug for treating hyperlipidemia that works equally well in both the liver and small intestine. | |||||
書誌情報 |
Journal of pharmacological sciences 巻 133, 号 4, p. 214-222, 発行日 2017-04 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 1347-8613 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA11806667 | |||||
PubMed番号 | ||||||
識別子タイプ | PMID | |||||
関連識別子 | 28366492 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.jphs.2017.02.003 | |||||
権利 | ||||||
権利情報 | © 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/). | |||||
著者版フラグ | ||||||
値 | publisher | |||||
出版者 | ||||||
出版者 | Elsevier | |||||
出版者 | ||||||
出版者 | Japanese Pharmacological Society |