Journal Article Synthesis and Evaluation of Fatty Acid Amides on the N-Oleoylethanolamide-Like Activation of Peroxisome Proliferator Activated Receptor α

高尾, 浩一  ,  野口, 香織  ,  橋本, 陽介  ,  白幡, 晶  ,  杉田, 義昭

63 ( 4 )  , pp.278 - 285 , 2015-04 , 日本薬学会
ISSN:0009-23631347-5223
NCID:AA00602100
Description
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.
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http://libir.josai.ac.jp/il/user_contents/02/G0000284repository/pdf/JOS-cpb.c14-00881.pdf

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