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Bile Acids in Gastroenterology pp 61–90Cite as

Bile Acid as Therapeutic Agents

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Abstract

Bile acids are the amphipathic compounds produced as the end products of cholesterol metabolism in the liver. Due to their detergent properties, bile acids play important roles in micelle formation and in intestinal lipid absorption. Besides such classical functions, bile acids modulate a number of intracellular signaling cascades involved in apoptosis, immune response, and carcinogenesis. In addition, recent findings showed that bile acids are endogenous ligands of the farnesoid X receptor (FXR; nuclear receptor (NR) subfamily 1 group H member 4 (NR1H4)) and the membrane-bound G-protein-coupled bile acid receptor 1 (GP-BAR1, commonly known as TGR5), indicating that bile acids themselves are signaling molecules. Taken together with the fact that both FXR and TGR5 regulate various physiological processes, including lipid metabolism, glucose metabolism, and energy expenditure, these findings suggest that modulation of bile acid metabolism and/or signaling would be a potential therapeutic strategy for the treatment of several diseases. In this context, bile acid-related drugs (agents) such as ursodeoxycholic acid, bile acid mimetics, and bile acid sequestrants have garnered the attention as therapeutic agents with pleiotropic properties. This chapter aims to provide an overview of the clinical efficacy and limitations of pharmacotherapies with bile acid-related drugs and to discuss molecular mechanisms underlying their pharmacological activities.

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  1. Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, The University of Tokyo, 7-3-1 Hongo, Bukyoku, Tokyo, 113-8655, Japan

    Yoshihide Yamanashi, Tappei Takada & Hiroshi Suzuki

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    Susumu Tazuma

  2. Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan

    Hajime Takikawa

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Yamanashi, Y., Takada, T., Suzuki, H. (2017). Bile Acid as Therapeutic Agents. In: Tazuma, S., Takikawa, H. (eds) Bile Acids in Gastroenterology. Springer, Tokyo. https://doi.org/10.1007/978-4-431-56062-3_5

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