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Peroxisome proliferator-activated receptor gamma agonist action of 3-methyl-1,2-cyclopentanedione
Seo Young Choi1, Jae Heun Chung, Dae Hyun Kim
1Department of Pharmacy, College of Pharmacy, Pusan National University, San 30, Jang-jun-dong, Geomjung-gu, Geomjung-ku, Busan, Korea.
Abstract:
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.
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