PPAR Ligands Containing Stilbene Scaffold

Area of Science:

• Molecular Biology
• Pharmacology
• Medicinal Chemistry

Background:

• Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors crucial for lipid and glucose metabolism.
• PPARs also play roles in regulating tumors, inflammation, cardiovascular diseases, and infertility.
• Synthetic PPAR ligands are used to treat dyslipidemia and diabetes, with new dual agonists showing broader benefits.

Purpose of the Study:

• To review ligands of PPARs that incorporate a stilbene scaffold.
• To summarize different types of stilbene-based PPAR ligands based on their chemical structures.
• To highlight the pharmacological potential of stilbene derivatives as PPAR modulators.

Main Methods:

• Literature review of scientific publications on PPAR ligands and stilbene derivatives.
• Chemical structure-based classification of identified stilbene-PPAR ligands.
• Analysis of reported biological activities and therapeutic implications.

Main Results:

• Identified various stilbene-containing compounds as modulators of PPARs.
• Categorized these compounds based on their chemical structures and scaffold variations.
• Highlighted the diverse pharmacological activities, including antioxidant and anti-inflammatory properties.

Conclusions:

• Stilbene-based compounds represent a promising class of PPAR ligands.
• Medicinal chemistry efforts in stilbene derivatives have expanded research into PPAR modulation.
• These compounds hold significant potential for developing novel therapeutics targeting metabolic and inflammatory diseases.