Piperine, a Component of Black Pepper, Inhibits Adipogenesis by Antagonizing PPAR纬 Activity in 3T3-L1 Cells

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• 作者：Ui-Hyun Park ; Hong-Suk Jeong ; Eun-Young Jo ; Taesun Park ; Seung Kew Yoon ; Eun-Joo Kim ; Ji-Cheon Jeong ; Soo-Jong Um
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2012
• 出版时间：April 18, 2012
• 年：2012
• 卷：60
• 期：15
• 页码：3853-3860
• 全文大小：348K
• 年卷期：v.60,no.15(April 18, 2012)
• ISSN：1520-5118

文摘

This study investigated the antiadipogenic activity of black pepper extract and its constituent piperine in 3T3-L1 preadipocytes as well as the underlying molecular mechanisms. Both black pepper extract and piperine, without affecting cytotoxicity, strongly inhibited the adipocyte differentiation of 3T3-L1 cells. The mRNA expression of the master adipogenic transcription factors, PPAR纬, SREBP-1c, and C/EBP尾, was markedly decreased. Intriguingly, mRNA levels of PPAR纬 target genes were also down-regulated. Moreover, a luciferase reporter assay indicated that pipierine significantly represses the rosiglitazone-induced PPAR纬 transcriptional activity. Finally, GST-pull down assays demonstrated that piperine disrupts the rosiglitazone-dependent interaction between PPAR纬 and coactivator CBP. Genome-wide analysis using microarray further supports the role of piperine in regulating genes associated with lipid metabolism. Overall, these results suggest that piperine, a major component of black pepper, attenuates fat cell differentiation by down-regulating PPAR纬 activity as well as suppressing PPAR纬 expression, thus leading to potential treatment for obesity-related diseases.

Keywords:

Piper nigrum Linne; black pepper; piperine; adipogenesis; adipocytes; peroxisome proliferator-activated receptor-纬