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Bile Acids As Drug Candidates

Date:
March 19, 2008
Source:
American Society for Biochemistry and Molecular Biology
Summary:
Bile acid derivatives can turn on the vitamin D receptor without causing excess calcium buildup, a finding that could lead to vitamin D therapies for conditions beyond just bone and skin disorders.
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Derivatives of lithocholic acid can activate the same receptor as calcitriol, the active form of vitamin D, without affecting blood calcium levels.
Credit: Journal of Lipid Research

Bile acid derivatives can turn on the vitamin D receptor (VDR) without causing excess calcium buildup, researchers report, a finding that could lead to vitamin D therapies for conditions beyond just bone and skin disorders.

While calcium balance may be the most well-known role of vitamin D, this molecule --through VDR binding-- regulates many functions including immunity and cell growth and thus has diverse therapeutic potential.

However, while vitamin D-based drugs are effective against some cancers and microbial infections, the risk of excess blood calcium has limited their clinical use.

Bile acids, compounds secreted from the liver that aid in digestion, can also bind to the VDR, though not as strongly.

However, Makoto Makishima and colleagues found that derivates of the bile acid LCA (lithocolic acid) are very potent VDR activators. Interestingly, though, these acids did not induce the expression of calcium channels in various cell types.

The researchers then compared the effects of orally-fed vitamin D or LCA derivatives on mice; they found that LCA could promote VDR activation in mice without causing calcium buildup and weight loss that was observed in vitamin D animals. This study suggests bile acid derivates might have solid clinical potential.

This research was recently published in The Journal Of Lipid Research.


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The above post is reprinted from materials provided by American Society for Biochemistry and Molecular Biology. Note: Materials may be edited for content and length.


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American Society for Biochemistry and Molecular Biology. "Bile Acids As Drug Candidates." ScienceDaily. ScienceDaily, 19 March 2008. <www.sciencedaily.com/releases/2008/03/080314165355.htm>.
American Society for Biochemistry and Molecular Biology. (2008, March 19). Bile Acids As Drug Candidates. ScienceDaily. Retrieved July 31, 2015 from www.sciencedaily.com/releases/2008/03/080314165355.htm
American Society for Biochemistry and Molecular Biology. "Bile Acids As Drug Candidates." ScienceDaily. www.sciencedaily.com/releases/2008/03/080314165355.htm (accessed July 31, 2015).

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