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Review
. 2017 Jul;7(4):427-438.
doi: 10.1016/j.apsb.2017.05.005. Epub 2017 Jun 16.

The potential of natural products for targeting PPAR α

Daniela Rigano  1 , Carmina Sirignano  1 , Orazio Taglialatela-Scafati  1
Affiliations
Review

The potential of natural products for targeting PPAR α

Daniela Rigano et al. Acta Pharm Sin B. 2017 Jul.

Abstract

Peroxisome proliferator activated receptors (PPARs) α, -γ and -β/δ are ligand-activated transcription factors and members of the superfamily of nuclear hormone receptor. These receptors play key roles in maintaining glucose and lipid homeostasis by modulating gene expression. PPARs constitute a recognized druggable target and indeed several classes of drugs used in the treatment of metabolic disease symptoms, such as dyslipidemia (fibrates, e.g. fenofibrate and gemfibrozil) and diabetes (thiazolidinediones, e.g. rosiglitazone and pioglitazone) are ligands for the various PPAR isoforms. More precisely, antidiabetic thiazolidinediones act on PPARγ, while PPARα is the main molecular target of antidyslipidemic fibrates. Over the past few years, our understanding of the mechanism underlying the PPAR modulation of gene expression has greatly increased. This review presents a survey on terrestrial and marine natural products modulating the PPARα system with the objective of highlighting how the incredible chemodiversity of natural products can provide innovative leads for this "hot" target.

Keywords: Dyslipidemia; Mechanism of action; Metabolic syndrome; Natural product; PPARα.

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Figures

fx1
Graphical abstract
Fig. 1
Figure 1
PPAR transcriptional activation in the cell nucleus. (A) Binding of PPAR/RXR ligands; (B) Changes in the associated transcriptional cofactors; (C) Activation of the transcriptional complex.
Fig. 2
Figure 2
Representative members of the fibrate family.
Fig. 3
Figure 3
PPARα-modulating mono- and sesquiterpenes.
Fig. 4
Figure 4
PPARα-modulating diterpenes.
Fig. 5
Figure 5
PPARα-modulating triterpenes.
Fig. 6
Figure 6
PPARα-modulating carotenoids.
Fig. 7
Figure 7
PPARα-modulating polyketides.
Fig. 8
Figure 8
PPARα-modulating phenylpropanoids and tannins.
Fig. 9
Figure 9
PPARα-modulating chalcones, stilbenes and flavonoids.
Fig. 10
Figure 10
PPARα-modulating isoflavonoids and biflavonoids.
Fig. 11
Figure 11
PPARα-modulating alkaloids.
See this image and copyright information in PMC

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