Inhibitory Effect of Acyl-CoA : Cholesterol Acyltransferase Inhibitor-Low Density Lipoprotein Complex on Experimental Atherosclerosis(Biopharmacy)
スポンサーリンク
概要
- 論文の詳細を見る
KV-2920 is a novel acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor. To confirm the efficacy of KV-2920-low density lipoprotein (LDL) complex (KV-LDL complex) as a drug-carrier complex on experimental atherosclerosis, we examined its inhibitory effects in vitro and in vivo. LDL was isolated from human plasma and the KV-LDL complex was prepared by incubation in the presence of Celite 545. The complex contained about 800 mol KV-2920 in 1 mol LDL. The cholesterol levels in the serum and aorta of atherogenic mice after 14 weeks of feeding were significantly higher than those of nonatherogenic mice. With the intravenous injection of KV-LDL complex, although the cholesterol levels in the serum were not influenced, the level of cholesterol ester in the aorta of atherogenic mice was significantly reduced. The concentration of cholesterol ester in the macrophages derived from ICR mice was predominantly increased by incubation with LDL for 48 h, this increase was significantly inhibited by incubation with KV-LDL complex. Moreover, the complex also inhibited the increase of cholesterol ester in macrophages following incubation with oxidized LDL. These findings suggest that KV-LDL complex inhibits the foam cell formation of macrophages though action of KV-2920 as an ACAT inhibitor, and prevents the accumulation of cholesterol ester in the aorta of atherogenic mice. Therefore, KV-LDL complex may be useful as a drug-carrier complex in antiatherosclerotic therapy.
- 公益社団法人日本薬学会の論文
- 2003-01-01
著者
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Sato Juichi
Department of General Medicine, Nagoya University Hospital
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Sato J
Hokkaido Pharmaceutical University School Of Pharmacy
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Sato J
Department Of General Medicine Nagoya University Hospital
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Sato J
Hokkaido Coll. Of Pharmacy Hokkaido Jpn
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Sato Juichi
Department Of General Medicine Nagoya University Hospital
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Sato Juichi
Hokkaido College Of Pharmacy
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MORIMOTO Kazuhiro
Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical Uni
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Morimoto Kazuhiro
Hokkaido Pharmaceutical University School of Pharmacy
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Shirahase Hiroaki
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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Sato Juichi
Hokkaido Institute Of Pharmaceutical Sciences
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Morimoto Kazuhiro
Department Of Pharmaceutics Graduate School Of Pharmaceutical Sciences Hokkaido Pharmaceutical Unive
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Morimoto Kazuhiro
Department Of Applied Chemistry Faculty Of Engineering Doshisha University
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Shirahase Hiroaki
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Shirahase Hiroaki
Research Laboratories Kyoto Pharmaceutical Company Ltd.
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Morimoto K
Hokkaido Pharmaceutical University School Of Pharmacy
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YOSHIMI Akihisa
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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Ito Keiji
Department Of Pharmaceutics Hokkaido College Of Pharmacy
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Yoshimi A
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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TAUCHI Yoshihiko
Department of Pharmaceutics, Hokkaido College of Pharmacy
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Shirahase H
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Ito Keiji
Department Of Pediatrics Hokkaido Children's Hospital And Medical Center
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Yoshimi Akihisa
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Tauchi Y
Department Of Pharmaceutics Hokkaido College Of Pharmacy
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Tauchi Yoshihiko
Department Of Pharmaceutics Hokkaido College Of Pharmacy
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Ito Keiji
Department Of Internal Medicine Keio University
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ITO Keiji
Department of Internal Medicine , Keio University
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