Bile acids: Trying to understand their chemistry and biology with the hope of helping patients


  • Alan F. Hofmann

    Corresponding author
    1. Division of Gastroenterology, Department of Medicine, University of California, San Diego, San Diego, CA
    • Division of Gastroenterology, Department of Medicine, University of California, San Diego 92093-0063
    Search for more papers by this author
    • fax: (858) 459-1754.

  • Potential conflict of interest: Dr. Hofmann received grants from and holds intellectual property rights for Falk Pharma. He is a consultant for Daiichi Sankyo, Sorbent Technologies, Relypsa, and Chiasma.


An informal review of the author's five decades of research on the chemistry and biology of bile acids in health and disease is presented. The review begins with a discussion of bile acid structure and its remarkable diversity in vertebrates. Methods for tagging bile acids with tritium for metabolic or transport studies are summarized. Bile acids solubilize polar lipids in mixed micelles; progress in elucidating the structure of the mixed micelle is discussed. Extensive studies on bile acid metabolism in humans have permitted the development of physiological pharmacokinetic models that can be used to simulate bile acid metabolism. Consequences of defective bile acid biosynthesis and transport have been clarified, and therapy has been developed. Methods for measuring bile acids have been improved. The rise and fall of medical and contact dissolution of cholesterol gallstones is chronicled. Finally, principles of therapy with bile acid agonists and antagonists are given. Advances in understanding bile acid biology and chemistry have helped to improve the lives of patients with hepatobiliary or digestive disease. (HEPATOLOGY 2009.)