Synthesis and Evaluation of Fatty Acid Amides on the N-Oleoylethanolamide-Like Activation of Peroxisome Proliferator Activated Receptor α
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- Takao Koichi
- Faculty of Pharmaceutical Sciences, Josai University
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- Noguchi Kaori
- Faculty of Pharmaceutical Sciences, Josai University
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- Hashimoto Yosuke
- Faculty of Pharmaceutical Sciences, Josai University
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- Shirahata Akira
- Faculty of Pharmaceutical Sciences, Josai University
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- Sugita Yoshiaki
- Faculty of Pharmaceutical Sciences, Josai University
書誌事項
- タイトル別名
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- Synthesis and Evaluation of Fatty Acid Amides on the <i>N</i>-Oleoylethanolamide-Like Activation of Peroxisome Proliferator Activated Receptor α
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A series of fatty acid amides were synthesized and their peroxisome proliferator-activated receptor α (PPAR-α) agonistic activities were evaluated in a normal rat liver cell line, clone 9. The mRNAs of the PPAR-α downstream genes, carnitine-palmitoyltransferase-1 and mitochondrial 3-hydroxy-3-methylglutaryl-CoA synthase, were determined by real-time reverse transcription-polymerase chain reaction (RT-PCR) as PPAR-α agonistic activities. We prepared nine oleic acid amides. Their PPAR-α agonistic activities were, in decreasing order, N-oleoylhistamine (OLHA), N-oleoylglycine, Oleamide, N-oleoyltyramine, N-oleoylsertonin, and Olvanil. The highest activity was found with OLHA. We prepared and evaluated nine N-acylhistamines (N-acyl-HAs). Of these, OLHA, C16:0-HA, and C18:1Δ9-trans-HA showed similar activity. Activity due to the different chain length of the saturated fatty acid peaked at C16:0-HA. The PPAR-α antagonist, GW6471, inhibited the induction of the PPAR-α downstream genes by OLHA and N-oleoylethanolamide (OEA). These data suggest that N-acyl-HAs could be considered new PPAR-α agonists.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 63 (4), 278-285, 2015
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204176581504
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- NII論文ID
- 130005061431
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 026283592
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- PubMed
- 25832022
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可