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A more recent version of this article appeared on April 1, 2008

Papers In Press, published online ahead of print January 7, 2008
J. Lipid Res., doi:10.1194/jlr.M700293-JLR200
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Submitted on June 25, 2007
Revised on January 7, 2008
Accepted on January 7, 2008

Lithocholic acid derivatives act as selective vitamin D receptor modulators without inducing hypercalcemia

Michiyasu Ishizawa, Manabu Matsunawa, Ryutaro Adachi, Shigeyuki Uno, Kazumasa Ikeda, Hiroyuki Masuno, Masato Shimizu, Ken-ichi Iwasaki, Sachiko Yamada, and Makoto Makishima

Division of Biochemistry, Department of Biomedical Sciences, Nihon University School of Medicine, Itabashi-ku, Tokyo 173-8610

Corresponding Author: maxima{at}med.nihon-u.ac.jp

1alpha ,25-Dihydroxyvitamin D3 [1,25(OH)2D3], a vitamin D receptor (VDR) ligand, regulates calcium homeostasis and also exhibits noncalcemic actions on immunity and cell differentiation. In addition to disorders of bone and calcium metabolism, VDR ligands are potential therapeutic agents in the treatment of immune disorders, microbial infections, and malignancies. Hypercalcemia, the major adverse effect of vitamin D3 derivatives, limits their clinical application. The secondary bile acid lithocholic acid (LCA) is an additional physiological ligand for VDR, and its synthetic derivative, LCA acetate, is a potent VDR agonist. In this study, we found an additional derivative, LCA propionate, is a more selective VDR activator than LCA acetate. LCA acetate and LCA propionate induced expression of the calcium channel transient receptor potential vanilloid type 6 (TRPV6) as effectively as that of CYP24A1, while 1,25(OH)2D3 was more effective on TRPV6 than on CYP24A1 in intestinal cells. In vivo experiments showed that LCA acetate and LCA propionate effectively induced tissue VDR activation without causing hypercalcemia. These bile acid derivatives have the ability to function as selective VDR modulators.


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