From Structural Modification to Diverse Pharmacological Activities: Recent Advances and Future Perspectives of Bile Acids

ABSTRACT Bile acids (BAs) are amphiphilic steroid acids that exert a broad range of physiological effects—including the regulation of metabolism, immune responses, and inflammatory processes—through activation of specific receptors such as the farnesoid X receptor (FXR) and the G protein‐coupled bile acid receptor 1 (TGR5). The gut microbiota plays a critical role in BA metabolism, and alterations in the BA pool have been closely linked to various metabolic disorders, including nonalcoholic fatty liver disease and type 2 diabetes. Consequently, targeting BA signaling pathways offers a novel mechanistic perspective for the prevention and treatment of these metabolic and inflammatory diseases. With growing insight into the biological functions of BAs, the development of BA‐based therapeutics and their structural derivatives is emerging as a promising strategy for the management of metabolic diseases.