Synthesis and Biological Activity of Piperine Derivatives as Potential PPARγ Agonists.

ABSTRACT:

Introduction

Peroxisome proliferator-activated receptor γ (PPARγ) plays a key role in glucose, which is a ligand-mediated transcription factor. The lipid homeostasis often serves as a pharmacological target for new drug discovery and development.

Materials and methods

In the research, we synthesized a series of piperine derivatives and then used a fluorescence polarization-based PPARγ ligand screening assay to evaluate the agonistic activity of PPARγ. Then, we cultured human normal hepatocytes, which were treated with 100μM compounds 2a, 2t or 3d. Then, the levels of PPARγ gene were determined so as to show whether the compounds could activate or inhibit the expression of PPARγ.

Results

A total of 30 piperine der

SUBMITTER: Wang Y 

PROVIDER: S-EPMC7266110 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature