Abstract:
: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 microM). The metabolism of cholesterol from lysosome to lipid droplet was inhibited with a similar IC50 (18 microM), 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 microM, respectively). Furthermore, piperine was found to inhibit both ACAT1 and ACAT2 isozymes to a similar extent (IC50: 16, 18 microM, 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_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Matsuda D,Ohte S,Ohshiro T,Jiang W,Rudel L,Hong B,Si S,Tomoda Hdoi
10.1248/bpb.31.1063subject
Has Abstractpub_date
2008-06-01 00:00:00pages
1063-6issue
6eissn
0918-6158issn
1347-5215pii
JST.JSTAGE/bpb/31.1063journal_volume
31pub_type
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