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Volume 11
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10.3390/nu11081820
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Article

The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions

by
Michele Biagioli
1,
Adriana Carino
1,
Chiara Fiorucci
1,
Giannamaria Annunziato
2,
Silvia Marchianò
1,
Martina Bordoni
1,
Rosalinda Roselli
3,
Cristina Di Giorgio
1,
Federica Castiglione
1,
Patrizia Ricci
1,
Agostino Bruno
2,
Andrea Faccini
4,
Eleonora Distrutti
5,
Monia Baldoni
1,
Gabriele Costantino
2 and
Stefano Fiorucci
1,*
1
Dipartimento di Scienze Biomediche e Chirurgiche, Università di Perugia, 06100 Perugia, Italy
2
Department of Food and Drugs, University of Parma, 43100 Parma, Italy
3
Department of Pharmacy, University of Naples Federico II, 80100 Naples, Italy
4
Centro Interdipartimentale Misure ‘G. Casnati’—University of Parma, 43100 Parma, Italy
5
Azienda Ospedaliera di Perugia, 06100 Perugia, Italy
*
Author to whom correspondence should be addressed.
Nutrients 2019, 11(8), 1820; https://doi.org/10.3390/nu11081820
Submission received: 25 June 2019 / Revised: 2 August 2019 / Accepted: 5 August 2019 / Published: 7 August 2019
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Abstract

Pelargonidins are anthocyanidins thought to be beneficial for the human health, although controversies exist over the doses needed and the unclear mechanism of action, along with poor systemic bioavailability. One putative target of pelargonidins is the aryl hydrocarbon receptor (AhR). A synthetic pelargonidin (Mt-P) was synthesized by the methylation of the pelargonidin (the natural compound indicated as P). Mt-P transactivated the AhR with an EC50 of 1.97 µM and was ~2-fold more potent than the natural compound. In vitro Mt-P attenuated pro-inflammatory activities of Raw264.7 macrophage cells in an AhR-dependent manner. In vivo, administration of the Mt-P in Balb/c mice resulted in a dose-dependent attenuation of signs and symptoms of colitis induced by TNBS. A dose of 5 mg/kg Mt-P, but not the natural compound P, reversed intestinal inflammation and increased expression of Tnf-α, Ifn-ƴ, and Il-6, while promoted the expansion of regulatory T cells and M2 macrophages. In C57BL/6J mice fed a high fat diet (HFD), Mt-P attenuated body weight gain, intestinal and liver inflammation, and ameliorated insulin sensitivity, while worsened liver steatosis by up-regulating the liver expression of Cd36 and Apo100b. These effects were abrogated by AhR gene ablation. Mt-P is a synthetic pelargonidin endowed with robust AhR agonist activity that exerts beneficial effects in murine models of inflammation and metabolic dysfunction.
Keywords: pelargonidins; aryl hydrocarbon receptor; colitis; hepatic steatosis; inflammation pelargonidins; aryl hydrocarbon receptor; colitis; hepatic steatosis; inflammation

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MDPI and ACS Style

Biagioli, M.; Carino, A.; Fiorucci, C.; Annunziato, G.; Marchianò, S.; Bordoni, M.; Roselli, R.; Giorgio, C.D.; Castiglione, F.; Ricci, P.; et al. The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions. Nutrients 2019, 11, 1820. https://doi.org/10.3390/nu11081820

AMA Style

Biagioli M, Carino A, Fiorucci C, Annunziato G, Marchianò S, Bordoni M, Roselli R, Giorgio CD, Castiglione F, Ricci P, et al. The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions. Nutrients. 2019; 11(8):1820. https://doi.org/10.3390/nu11081820

Chicago/Turabian Style

Biagioli, Michele, Adriana Carino, Chiara Fiorucci, Giannamaria Annunziato, Silvia Marchianò, Martina Bordoni, Rosalinda Roselli, Cristina Di Giorgio, Federica Castiglione, Patrizia Ricci, and et al. 2019. "The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions" Nutrients 11, no. 8: 1820. https://doi.org/10.3390/nu11081820

APA Style

Biagioli, M., Carino, A., Fiorucci, C., Annunziato, G., Marchianò, S., Bordoni, M., Roselli, R., Giorgio, C. D., Castiglione, F., Ricci, P., Bruno, A., Faccini, A., Distrutti, E., Baldoni, M., Costantino, G., & Fiorucci, S. (2019). The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions. Nutrients, 11(8), 1820. https://doi.org/10.3390/nu11081820

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