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Picrasidine N Is a Subtype-Selective PPARβ/δ Agonist
Shuai Zhao1, Yuichiro Kanno2, Wei Li3
1College of Life Science, Northeast Forestry University , Harbin 150040, People's Republic of China.
Journal of Natural Products
|March 31, 2016
Summary
A natural compound, picrasidine N, acts as a selective agonist for peroxisome proliferator-activated receptor (PPAR) β/δ. This selective activation of PPARβ/δ offers potential for drug development and understanding its biological roles.
Area of Science:
- Pharmacology
- Molecular Biology
- Natural Products Chemistry
Background:
- Peroxisome proliferator-activated receptor (PPAR) β/δ is implicated in lipid homeostasis, cancer, and inflammation.
- Understanding PPARβ/δ's diverse physiological roles requires selective modulators.
Purpose of the Study:
- To identify novel PPARβ/δ agonists from natural compounds.
- To characterize the subtype and gene selectivity of identified agonists.
Main Methods:
- Screening of plant extracts and natural compounds using a mammalian one-hybrid assay.
- Luciferase reporter gene assay to assess transcriptional activity.
- Quantitative PCR to measure target gene mRNA expression (ANGPTL4).
Main Results:
- Picrasidine N (1) was identified as a novel PPARβ/δ agonist.
- Compound 1 selectively activated PPARβ/δ with minimal activity on PPARα and PPARγ.
- 1 enhanced PPARβ/δ transcriptional activity and selectively induced ANGPTL4 mRNA expression.
Conclusions:
- Picrasidine N is a potent, subtype-selective, and gene-selective PPARβ/δ agonist.
- This compound shows potential as a lead for drug development.
- It serves as a valuable chemical tool for studying PPARβ/δ function.
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