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Hyodeoxycholic Acid Derivatives as Liver X Receptor α and G-protein-coupled Bile Acid Receptor Agonists

Hyodeoxycholic Acid Derivatives as Liver X Receptor α and G-protein-coupled Bile Acid Receptor Agonists

Simona De Marino, Adriana Carino, Dario Masullo, Claudia Finamore, Silvia Marchianò, Sabrina Cipriani, Francesco Saverio Di Leva, Bruno Catalanotti, Ettore Novellino, Vittorio Limongelli, Stefano Fiorucci, etc.

Sci Rep. 2017 Feb 24;7:43290.

PMID: 28233865

Abstract:

Bile acids are extensively investigated for their potential in the treatment of human disorders. The liver X receptors (LXRs), activated by oxysterols and by a secondary bile acid named hyodeoxycholic acid (HDCA), have been found essential in the regulation of lipid homeostasis in mammals. Unfortunately, LXRα activates lipogenic enzymes causing accumulation of lipid in the liver. In addition to LXRs, HDCA has been also shown to function as ligand for GPBAR1, a G protein coupled receptor for secondary bile acids whose activation represents a promising approach to liver steatosis. In the present study, we report a library of HDCA derivatives endowed with modulatory activity on the two receptors. The lead optimization of HDCA moiety was rationally driven by the structural information on the binding site of the two targets and results from pharmacological characterization allowed the identification of hyodeoxycholane derivatives with selective agonistic activity toward LXRα and GPBAR1 and notably to the identification of the first example of potent dual LXRα/GPBAR1 agonists. The new chemical entities might hold utility in the treatment of dyslipidemic disorders.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP83498	Hyodeoxycholic acid		83-49-8	Price

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