Effects of NTE-122, a Novel Acyl-CoA:Cholesterol Acyltransferase Inhibitor, on Cholesterol Esterification and High-Density Lipoprotein-Induced Cholesterol Efflux in Macrophages

スポンサーリンク

概要

• 論文の詳細を見る

• We investigated the effects of a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, NTE-122 (trans-1, 4-bis[[1-cyclohexyl-3-(4-dimethylamino phenyl)ureido]methyl]cyclohexane), on ACAT activities in macrophages originating from several species and high-density lipoprotein (HDL)-induced cholesterol efflux in phorbol 12-myristate 13-acetate (PMA)-treated THP-1 cells. NTE-122 inhibited cell-free ACAT activities in human PMA-treated THP-1 cells and mouse J774.1 cells with IC50 values of 0.88 and 360 nM, respectively. NTE-122 competively inhibited the ACAT activity in PMA-treated THP-1 cells. NTE-122 also inhibited cellular ACAT activities in PMA-treated THP-1 cells, rat peritoneal macrophages and J774.1 cells with IC50 values of 3.5, 84 and 6800 nM, respectively. Furthermore, NTE-122 prevented cholesterol accumulation in PMA-treated THP-1 cells incubated with acetylated low density lipoprotein, simultaneously with HDL, while it caused accumulation of a significant amount of free cholesterol in the absence and even in the presence of HDL. NTE-122 also enhanced HDL-induced cholesterol efflux from established foam cells converted from PMA-treated THP-1 cells. These results suggest that NTE-122, capable of inhibiting macrophage ACAT activity in humans more strongly than those in the other species, exhibits anti-atherogenic effects by preventing the foam cell formation and enhancing the foam cell regression in humans.

• 社団法人 日本薬理学会の論文
• 1999-02-01

著者

• 田中 東

  日清食品ホールディングス株式会社食品安全研究所

• 東 幸雅

  日清食品(株)食品安全研究所

• Yamasaki Masahiro

  Central Research Institute Nissin Food Products Co. Ltd.

• Yamasaki M

  Kumamoto Univ. Kumamoto Jpn

• Tanaka Azuma

  Food Safety Research Institute Nissin Food Products Co. Ltd.

• Azuma Yukimasa

  Food Safety Research Institute Nissin Food Products Co. Ltd.

• Azuma Yukimasa

  Central Research Institute Nissin Food Products Co. Ltd.

• OHNO Katsutoshi

  Central Research Institute, Nissin Food Products Co., Ltd.,

• YAMADA Toshihiro

  Central Research Institute, Nissin Food Products Co., Ltd.,

• NOBUHARA Yoichi

  Central Research Institute, Nissin Food Products Co., Ltd.,

• KAWASAKI Takashi

  Central Research Institute, Nissin Food Products Co., Ltd.

• IKEMOTO Kiyohito

  Central Research Institute, Nissin Food Products Co., Ltd.

• Nobuhara Yoichi

  Central Research Institute Nissin Food Products Co. Ltd.

• Nobuhara Yoichi

  Central Research Institute Nissin Food Products Co. Ltd

• Kawasaki Tomihisa

  Central Research Institute Nissin Food Products Co. Ltd.

• Ikemoto Kiyohito

  Central Research Institute Nissin Food Products Co. Ltd.

• Yamada Toshihiro

  The Food Safety Research Institute Nissin Foods Holdings Co. Ltd.

• Nobuhara Youichi

  Central Research Institute Nissin Food Products Co. Ltd.

• Yamada Toshihiro

  Food Safety Research Institute Nissin Foods Holdings Co. Ltd.

関連論文

• スチレンオリゴマーの内分泌撹乱作用に関する生物学的評価(第2報)
• ふなずし由来乳酸菌NLB163のヒトに対するコレステロール低下作用
• ふなずしからのコレステロール低下作用を有する乳酸菌の分離
• P-098 p53R2遺伝子発現機構に基づくヒト細胞遺伝毒性試験法(ポスターセッション)
• ポリスチレン容器中に存在する新規スチレントリマーの同定, 定量及び生物学的評価
• スチレンオリゴマーの内分泌撹乱作用に関する生物学的評価
• Identification of tumor promotion marker genes for predicting tumor promoting potential of chemicals in BALB/c 3T3 cells
• A Genotoxicity test system based on p53R2 gene expression in human cells
• Lactobacillus gasseri NY0509 およびLactobacillus casei NY1301 発酵乳酸菌飲料の健常成人の糞便内菌叢に及ぼす影響
• Lactobacillus gasseri NY0509 および Lactobacillus casei NY1301 のビフィズス菌増殖促進効果
• Lactobacillus gasseri NY0509 および Lactobacillus casei NY1301 の人工消化液耐性並びに腸内有害菌抑制効果
• Lactobacillus gasseri NY0509およびLactobacillus casei NY1301含有乳酸菌飲料の健常成人の排便および糞便内菌叢に及ぼす影響
• Effects of Heat Stress on Temperature Regulation in Initial Exercise
• Cytoprotective Effects of 4,6-Bis(1H-pyrazol-1-yl)pyrimidine and Related Compounds on HCl・Ethanol-Induced Gastric Lesions in Rats
• Synthesis and Cytoprotective Antiulcer Activity of 2- or 4-(1H-Pyrazol-1-yl)pyrimidine Derivatives Related to Mepirizole and Dulcerozine
• Effects of NTE-122, an Acyl-CoA : Cholesterol Acyltransferase Inhibitor, on Cholesterol Esterification and Lipid Secretion From CaCo-2 Cells, and Cholesterol Absorption in Rats
• Effects of NTE-122, a Novel Acyl-CoA:Cholesterol Acyltransferase Inhibitor, on Cholesterol Esterification and High-Density Lipoprotein-Induced Cholesterol Efflux in Macrophages
• Effects of NTE-122, a Novel Acyl-CoA:Cholesterol Acyltransferase Inhibitor, on Cholesterol Esterification and Secretions of Apolipoprotein B-Containing Lipoprotein and Bile Acids in HepG2
• Cholesterol : Lowering Effects of NTE : 122, a Novel Acyl : CoA:Cholesterol Acyltransferase (ACAT) Inhibitor, on Cholesterol Diet : Fed Rats and Rabbits
• O-18 Development of genotoxicity test system based on a p53R2 gene expression in human cells(MUTAGENICITY)(GENERAL SESSION BY ORAL PRESENTATION)(Proceedings of the 31st Annual Meeting)
• Comparison of the Anticoagulant and Antithrombotic Effects of YM-75466, a Novel Orally-Active Factor Xa Inhibitor,and Warfarin in Mice
• Problems with Methods used to Screen Estrogenic Chemicals by Yeast Two-Hybrid Assays
• NTE-122, an Acyl-CoA:Cholesterol Acyltransferase Inhibitor, Prevents the Progression of Atherogenesis in Cholesterol-Fed Rabbits
• Detection of Walnut Residues in Processed Foods by Polymerase Chain Reaction
• CHARACTERISTICS OF MILD IRRITANTS AND ADAPTIVE CYTOPROTECTION ; ROLE OF ENDOGENOUS PROSTAGLANDINS IN SELF-DEFENSIVE MECHANISMS
• CHANGES IN TRANSMUCOSAL POTENTIAL DIFFERENCE AND LUMINAL PH IN ANESTHETIZED RAT STOMACH AFTER EXPOSURE TO ETHANOL
• Mossbauer Study on the Crystallization Process of α-Fe/Nd_2Fe_B type Nanocomposite Magnet Alloy
• Validation of an in vitro screening test for predicting the tumor promoting potential of chemicals based on gene expression
• Changes in the two-dimensional protein patterns of ribosomal and cytosol fractions during transitionary growth phase in an adenine-requiring mutant atrain of Kluyveromyces lactis
• Lactobacillus casei NY1301 Increases the Adhesion of Lactobacillus gasseri NY0509 to Human Intestinal Caco-2 Cells(Microbiology & Fermentation Technology)
• A Genotoxicity test system based on p53R2 gene expression in normal human skin cells
• Specific Detection by the Polymerase Chain Reaction of Potentially Allergenic Salmonid Fish Residues in Processed Foods

もっと見る 閉じる

スポンサーリンク