The Molecular Target of Rubimaillin in the Inhibition of Lipid Droplet Accumulation in Macrophages
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概要
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The naphthohydroquinone rubimaillin, which has an angular-type three cyclic skeleton and was isolated from the Chinese medical plant Rubia cordifola, was found to inhibit lipid droplet accumulation in mouse macrophages and to selectively inhibit cholesteryl ester synthesis (IC50: 18 μM). The metabolism of cholesterol from lysosomes to lipid droplets was inhibited by the compound with a similar IC50 (45 μM). Moreover, rubimaillin inhibited acyl-CoA:cholesterol acyltransferase (ACAT1) activity in ACAT1-expressing cells (IC50: 80 μM). Thus, these data strongly suggest that rubimaillin inhibits macrophage ACAT activity in order to decrease cholesteryl ester (CE) synthesis, leading to a reduction in the number of lipid droplets. Furthermore, rubimaillin was found to inhibit the ACAT2 isozyme in ACAT2-expressing cells (IC50: 22 μM). We concluded that rubimaillin is a dual inhibitor of ACAT1 and ACAT2, but is more selective for the ACAT2 isozyme.
著者
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MATSUDA Daisuke
Graduate School of Pharmacy, Kitasato University
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OHSHIRO Taichi
Graduate School of Pharmacy, Kitasato University
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JIANG Wei
National Key Laboratory for Screening of New Microbial Drugs, Institute of Medical Biotechnology, Ch
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HONG Bin
National Key Laboratory for Screening of New Microbial Drugs, Institute of Medical Biotechnology, Ch
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SI Shuyi
National Key Laboratory for Screening of New Microbial Drugs, Institute of Medical Biotechnology, Ch
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TOMODA Hiroshi
Graduate School of Pharmacy, Kitasato University
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Ohshiro Taichi
Graduate School Of Pharmaceutical Sciences Kitasato University:(present Office)department Of Medhici
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Hong Bin
National Key Laboratory For Screening Of New Microbial Drugs Institute Of Medical Biotechnology Chin
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Si Shuyi
National Key Laboratory For Screening Of New Microbial Drugs Institute Of Medical Biotechnology Chin
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Ohba Mio
Graduate School of Pharmaceutical Sciences, Kitasato University
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Matsuda Daisuke
Graduate School Of Pharmaceutical Sciences Kitasato University
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Jiang Wei
National Key Laboratory For Screening Of New Microbial Drugs Institute Of Medical Biotechnology Chin
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Tomoda Hiroshi
Graduate School Of Pharmaceutical Sciences Kitasato University
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Ohshiro Taichi
Graduate School Of Pharmaceutical Sciences Kitasato University
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Tomoda Hiroshi
Graduate School Of Pharmaceutical Sciences Kitasato Univ.
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Jiang Wei
National Key Laboratory for Screening of New Microbial Drugs, Institute of Medical Biotechnology, Chinese Academy of Medical Science
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Si Shuyi
National Key Laboratory for Screening of New Microbial Drugs, Institute of Medical Biotechnology, Chinese Academy of Medical Science
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Tomoda Hiroshi
Graduate School of Pharmaceutical Science, Kitasato University
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