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Ðanić M, Stanimirov B, Pavlović N, et al. Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome. Front Pharmacol. 2018;9:1382doi: 10.3389/fphar.2018.01382.
Ðanić, M., Stanimirov, B., Pavlović, N., Goločorbin-Kon, S., Al-Salami, H., Stankov, K., & Mikov, M. (2018). Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome. Frontiers in pharmacology, 91382. https://doi.org/10.3389/fphar.2018.01382
Ðanić, Maja, et al. "Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome." Frontiers in pharmacology vol. 9 (2018): 1382. doi: https://doi.org/10.3389/fphar.2018.01382
Ðanić M, Stanimirov B, Pavlović N, Goločorbin-Kon S, Al-Salami H, Stankov K, Mikov M. Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome. Front Pharmacol. 2018 Dec 03;9:1382. doi: 10.3389/fphar.2018.01382. eCollection 2018. PMID: 30559664; PMCID: PMC6287190.
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Front Pharmacol. 2018 Dec 03;9:1382. doi: 10.3389/fphar.2018.01382. eCollection 2018.

Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome.

Frontiers in pharmacology

Maja Ðanić, Bojan Stanimirov, Nebojša Pavlović, Svetlana Goločorbin-Kon, Hani Al-Salami, Karmen Stankov, Momir Mikov

Affiliations

  1. Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia.
  2. Department of Biochemistry, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia.
  3. Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia.
  4. Biotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Biosciences Research Precinct, Curtin Health Innovation Research Institute, Curtin University, Perth, WA, Australia.

PMID: 30559664 PMCID: PMC6287190 DOI: 10.3389/fphar.2018.01382

Abstract

Apart from well-known functions of bile acids in digestion and solubilization of lipophilic nutrients and drugs in the small intestine, the emerging evidence from the past two decades identified the role of bile acids as signaling, endocrine molecules that regulate the glucose, lipid, and energy metabolism through complex and intertwined pathways that are largely mediated by activation of nuclear receptor farnesoid X receptor (FXR) and cell surface G protein-coupled receptor 1, TGR5 (also known as GPBAR1). Interactions of bile acids with the gut microbiota that result in the altered composition of circulating and intestinal bile acids pool, gut microbiota composition and modified signaling pathways, are further extending the complexity of biological functions of these steroid derivatives. Thus, bile acids signaling pathways have become attractive targets for the treatment of various metabolic diseases and metabolic syndrome opening the new potential avenue in their treatment. In addition, there is a significant effort to unveil some specific properties of bile acids relevant to their intrinsic potency and selectivity for particular receptors and to design novel modulators of these receptors with improved pharmacokinetic and pharmacodynamic profiles. This resulted in synthesis of few semi-synthetic bile acids derivatives such as 6α-ethyl-chenodeoxycholic acid (obeticholic acid, OCA), norursodeoxycholic acid (norUDCA), and 12-monoketocholic acid (12-MKC) that are proven to have positive effect in metabolic and hepato-biliary disorders. This review presents an overview of the current knowledge related to bile acids implications in glucose, lipid and energy metabolism, as well as a potential application of bile acids in metabolic syndrome treatment with future perspectives.

Keywords: atherosclerosis; bile acids; diabetes; farnesoid X receptor; gut microbiota; lipoprotein; metabolic syndrome; transmembrane G protein coupled receptor 5

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