Journal
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 60, Issue 15, Pages 3853-3860Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jf204514a
Keywords
Piper nigrum Linne; black pepper; piperine; adipogenesis; adipocytes; peroxisome proliferator-activated receptor-gamma
Funding
- NRF
- MEST [2012-0000655]
- Ministry of Health, Welfare, and Family Affairs, Republic of Korea [A090282]
- Korea Health Promotion Institute [A090282] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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 gamma, SREBP-1c, and C/EBP beta, was markedly decreased. Intriguingly, mRNA levels of PPAR gamma target genes were also down-regulated. Moreover, a luciferase reporter assay indicated that pipierine significantly represses the rosiglitazone-induced PPAR gamma transcriptional activity. Finally, GST-pull down assays demonstrated that piperine disrupts the rosiglitazone-dependent interaction between PPAR gamma and coactivator GBP. 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 gamma activity as well as suppressing PPAR gamma expression, thus leading to potential treatment for obesity-related diseases.
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