PPAR Ligands Containing Stilbene Scaffold

(E-pub Ahead of Print)

Author(s): Marialuigia Fantacuzzi, Barbara De Filippis*, Rosa Amoroso, Letizia Giampietro.

Journal Name: Mini-Reviews in Medicinal Chemistry

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Peroxisome proliferator-activated receptors (PPARs) are transcriptional factors which belong to the ligand-activated nuclear receptor superfamily. They are ubiquitously expressed throughout the body. So far, three major subtypes have been identified, PPARα, PPARβ/δ and PPARγ. They are crucial for lipid and glucose metabolism and are also involved in the regulation of several types of tumors, inflammation, cardiovascular diseases and infertility. The importance of these transcription factors in physiology and pathophysiology has been largely investigated.

Synthetic PPAR ligands are widely used in the treatment of dyslipidemia (e.g. fibrates - PPARα activators) or in diabetes mellitus (e.g. thiazolidinediones - PPARγ agonists) while a new generation of dual agonists reveals hypolipemic, hypotensive, antiatherogenic, anti-inflammatory and anticoagulant action. Many natural ligands, including polyphenolic compounds, influence the expression of these receptors. They have several health-promoting properties, including antioxidant, anti-inflammatory, and antineoplastic activities. Resveratrol, a stilbene polyphenol, is a biological active modulator of several signaling proteins, including PPARs. Given the enormous pharmacological potential of resveratrol, stilbene-based medicinal chemistry has had a rapid increase covering various areas of research.

The present review discusses ligands of PPARs that contain stilbene scaffold and summarizes the different types of compounds on the basis of chemical structure.

Keywords: PPAR, stilbene, resveratrol, hybrid, fibrates, thiazolidindiones.

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Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1389557519666190603085026
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