Human Acyl-CoA : Cholesterol Acyltransferase Inhibitory Activities of Aliphatic Acid Amides from Zanthoxylum piperitum DC.(Pharmacognosy)
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概要
- 論文の詳細を見る
Acyl-CoA: cholesterol acyltransferase (ACAT) plays an important role in the esterification of cholesterol with its substrates, cholesterol and fatty acyl coenzyme A, to facilitate both intracellular storage and intercellular transport. ACAT-1 is more involved in macrophage foam cell formation and ACAT-2 plays a critical role in the cholesterol absorption process in intestinal enterocytes. Three aliphatic acid amides, β-sanshool (1), γ-sanshool (2), and hydroxy-β-sanshool (3), were isolated by bioassay-guided fractionation of the ethanolic extracts of Zanthoxylum piperitum DC. Compounds 1 and 2 inhibited human ACAT-1 and -2 activities with IC_<50> values of 39.0 and 79.7μM for 1 and of 12.0 and 82.6μM for 2, respectively. However, the hACAT-1 and -2 inhibitory activities of compound 3 having hydroxyl group were relatively less than those of compounds 1 and 2. A semi-synthetic compound 4, which has acetyl residue at 2'-OH of compound 3, exhibited the increased hACAT-1 and -2 inhibitory activities with ICSO values of 28.1 and 87.5μM, respectively.
- 公益社団法人日本薬学会の論文
- 2007-01-01
著者
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JEONG Tae-Sook
National Research Laboratory of Lipid Metabolism & Atherosclerosis, Korea Research Institute of Bios
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Jeong Tae-sook
National Research Laboratory Of Lipid Metabolism & Atherosclerosis:molecular Science University
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Park Yong-dae
National Research Laboratory Of Lipid Metabolism & Atherosclerosis:molecular Science University
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Lee Woo
National Research Laboratory Of Lipid Metabolism & Atherosclerosis:molecular Science University
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Lee Woo
National Institute Of Toxicological Research Korea Fda
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AN Sojin
National Research Laboratory of Lipid Metabolism & Atherosclerosis
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Jeong Tae-sook
National Research Laboratory Of Lipid Metabolism & Atherosclerosis Korea Research Institute Of B
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An Sojin
National Research Laboratory Of Lipid Metabolism & Atherosclerosis
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Lee Woo
Eco Friendly Biomaterial Research Center Korea Research Institute Of Bioscience And Biotechnology
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