Peroxisome proliferator-activated receptor gamma agonist action of 3-methyl-1,2-cyclopentanedione.
Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor superfamily that plays a pivotal role in regulating inflammatory gene expression. The purpose of this study was to investigate the effects of coffee extract, 3-methyl-1,2-cyclopentanedione (3-MCP) on PPARs in vitro. Western blotting and luciferase assays using the PPAR response element (PPRE) construct revealed that 3-MCP induced PPARgamma-selective activation in YPEN-1 cells and that treatment with the PPARgamma selective antagonist, GW9662, was associated with a decrease in 3-MCP-induced PPARgamma activity. The 3-MCP also was shown to suppress reactive species generation and pro-inflammatory transcription factor NF-kappaB activity through PPARgamma activation. Theses results indicate that 3-MCP is a novel PPARgamma agonist and suggests that this agent may have a potential to minimize inflammation.
Choi
Seo Young
SY
Department of Pharmacy, College of Pharmacy, Pusan National University, San 30, Jang-jun-dong, Geomjung-gu, Geomjung-ku, Busan, Korea.
Chung
Jae Heun
JH
Kim
Dae Hyun
DH
Chung
Sang Woon
SW
Kim
Ji Young
JY
Yu
Byung Pal
BP
Chung
Hae Young
HY
D000813:Anilides / Q000494:pharmacology; D000818:Animals; D015153:Blotting, Western; D002460:Cell Line; D003517:Cyclopentanes / Q000494:pharmacology*; D015536:Down-Regulation / Q000187:drug effects; D016328:NF-kappa B / Q000378:metabolism; D047495:PPAR gamma / Q000819:agonists*; D051381:Rats
C457499:2-chloro-5-nitrobenzanilide; D000813:Anilides; D003517:Cyclopentanes; D016328:NF-kappa B; D047495:PPAR gamma; C471838:3-methyl-1,2-cyclopentanedione