title: Piperine, a component of black pepper, inhibits adipogenesis by antagonizing PPARγ activity in 3T3-L1 cells.
abstract: 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, PPARγ, SREBP-1c, and C/EBPβ, was markedly decreased. Intriguingly, mRNA levels of PPARγ target genes were also down-regulated. Moreover, a luciferase reporter assay indicated that pipierine significantly represses the rosiglitazone-induced PPARγ transcriptional activity. Finally, GST-pull down assays demonstrated that piperine disrupts the rosiglitazone-dependent interaction between PPARγ 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 PPARγ activity as well as suppressing PPARγ expression, thus leading to potential treatment for obesity-related diseases.
authors.affiliation: Department of Bioscience and Biotechnology, BK21 Graduate Program, Sejong University, Seoul, Korea.
authors.forename: Ui-Hyun
authors.initials: UH
authors.lastname: Park
authors.forename: Hong-Suk
authors.initials: HS
authors.lastname: Jeong
authors.forename: Eun-Young
authors.initials: EY
authors.lastname: Jo
authors.forename: Taesun
authors.initials: T
authors.lastname: Park
authors.forename: Seung Kew
authors.initials: SK
authors.lastname: Yoon
authors.forename: Eun-Joo
authors.initials: EJ
authors.lastname: Kim
authors.forename: Ji-Cheon
authors.initials: JC
authors.lastname: Jeong
authors.forename: Soo-Jong
authors.initials: SJ
authors.lastname: Um
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D050156:Adipogenesis / Q000187:drug effects*; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D052117:Benzodioxoles / Q000494:pharmacology*; D002454:Cell Differentiation / Q000187:drug effects; D015536:Down-Regulation / Q000187:drug effects*; D051379:Mice; D047495:PPAR gamma / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*; D029222:Piper nigrum / Q000737:chemistry*; D010880:Piperidines / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D053284:Polyunsaturated Alkamides / Q000494:pharmacology*
chemical_list: D000470:Alkaloids; D052117:Benzodioxoles; D047495:PPAR gamma; D010880:Piperidines; D010936:Plant Extracts; D053284:Polyunsaturated Alkamides; C008922:piperine