Molecular Target of Piperine in the Inhibition of Lipid Droplet Accumulation in Macrophages
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- Matsuda Daisuke
- Graduate School of Pharmacy, Kitasato University
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- Ohte Satoshi
- 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, Chinese Academy of Medical Science
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- Rudel Lawrence
- Department of Pathology, Arteriosclerosis Research Program, Wake Forest University School of Medicine
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- Hong Bin
- 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 Pharmacy, Kitasato University
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Description
An alkaloid piperine isolated from the Piper Nigrum was found to inhibit lipid droplet accumulation in mouse macrophages, and especially inhibited cholesteryl ester (CE) synthesis (IC50: 25 μM). The metabolism of cholesterol from lysosome to lipid droplet was inhibited with a similar IC50 (18 μM), indicating that the site of inhibition is one of the steps between the lysosomes and the endoplasmic reticulum. Therefore, effects of piperine on acyl-CoA:cholesterol acyltransferase (ACAT) activity in the microsomes prepared from mouse macrophage and liver were studied, to show that the compounds inhibited the activity in both cases (IC50: 9.1, 7.0 μM, respectively). Furthermore, piperine was found to inhibit both ACAT1 and ACAT2 isozymes to a similar extent (IC50: 16, 18 μM, respectively) in cell-based assays using ACAT1- or ACAT2-expressing cells. Thus, it was suggested that piperine inhibited macrophage ACAT to decrease CE synthesis, leading to a reduction of lipid droplets.
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 31 (6), 1063-1066, 2008
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390001204627017728
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- NII Article ID
- 110006684316
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- NII Book ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- NDL BIB ID
- 9508966
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- CiNii Articles
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- Abstract License Flag
- Disallowed