Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome
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...
| Main Authors: | , , , , , , |
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| Format: | Journal Article |
| Published: |
2018
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| Online Access: | http://hdl.handle.net/20.500.11937/74354 |
| _version_ | 1848763251557400576 |
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| author | Danic, M. Stanimirov, B. Pavlovic, N. Golocorbin-Kon, S. Al-Salami, Hani Stankov, K. Mikov, M. |
| author_facet | Danic, M. Stanimirov, B. Pavlovic, N. Golocorbin-Kon, S. Al-Salami, Hani Stankov, K. Mikov, M. |
| author_sort | Danic, M. |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | 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 6a-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. |
| first_indexed | 2025-11-14T11:00:30Z |
| format | Journal Article |
| id | curtin-20.500.11937-74354 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T11:00:30Z |
| publishDate | 2018 |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-743542019-06-25T00:48:53Z Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome Danic, M. Stanimirov, B. Pavlovic, N. Golocorbin-Kon, S. Al-Salami, Hani Stankov, K. Mikov, M. 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 6a-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. 2018 Journal Article http://hdl.handle.net/20.500.11937/74354 10.3389/fphar.2018.01382 http://creativecommons.org/licenses/by/4.0/ fulltext |
| spellingShingle | Danic, M. Stanimirov, B. Pavlovic, N. Golocorbin-Kon, S. Al-Salami, Hani Stankov, K. Mikov, M. Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title_full | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title_fullStr | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title_full_unstemmed | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title_short | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome |
| title_sort | pharmacological applications of bile acids and their derivatives in the treatment of metabolic syndrome |
| url | http://hdl.handle.net/20.500.11937/74354 |