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The Cardenolides Strophanthidin, Digoxigenin and Dihydroouabain Act as Activators of the Human RORγ/RORγT Receptors

The Cardenolides Strophanthidin, Digoxigenin and Dihydroouabain Act as Activators of the Human RORγ/RORγT Receptors

Kaja Karaś, Anna Sałkowska, Aurelia Walczak-Drzewiecka, Katarzyna Ryba, Jarosław Dastych, Rafał A Bachorz, Marcin Ratajewski

Toxicol Lett. 2018 Oct 1;295:314-324.

PMID: 29981919

Abstract:

Two isoforms of a ligand-activated nuclear receptor, RORγ and RORγT, have been implicated in various physiological functions, including energy metabolism, circadian rhythm and immune system development. Using a stably transfected reporter cell line, we screened two chemical libraries and identified three cardenolides (natural, plant-derived pesticides) as activators of RORγ-dependent transcription. These compounds increased G6PC and NPAS2 expression in HepG2 cells, accompanied by increased occupancy of RORγ within the promoters of these genes. Further, strophanthidin, digoxigenin and dihydroouabain upregulated IL17A and IL17F expression and enhanced IL17 secretion in Th17 human lymphocytes. Molecular docking analyses of these compounds to the RORγ LBD showed favorable docking scores, suggesting that cardenolides may act as agonists of the receptor. Thus, our results provide new chemical structures for further development of RORγ-selective modulators with virtual therapeutic potential.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP66284-A	Strophanthidin		66-28-4	Price

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