Abstract
TGR5 is a member of the G protein-coupled receptor family and is activated by bile acids. TGR5 is thought to be a promising food factor target for preventing metabolic diseases because the activation of TGR5 prevents obesity and hyperglycemia in mice fed a high-fat diet. In the present study, we established an evaluation system for the TGR5 ligand activity, and identified a limonoid nomilin as an activator of TGR5 from among approximate 150 purified food compounds. Unlike bile acids, nomilin did not exhibit the farnesoid X receptor ligand activity. Although the nomilin derivative obacunone was capable of activating TGR5, limonin (the most abundant limonoid in citrus seeds) was not a TGR5 activator. When male C57BL/6J mice fed a high-fat diet for 9 weeks were further fed a high-fat diet either alone or supplemented with 0.2% w/w nomilin for 77 days, nomilin-treated mice had lower body weight, serum glucose, serum insulin, and enhanced glucose tolerance. Our results suggest a novel biological function of nomilin as an agent having anti-obesity and anti-hyperglycemic effects that are likely to be mediated through the activation of TGR5.
Recommended Citation
Sato, R.
(2012)
"Food factors that mimic bile acid functions,"
Journal of Food and Drug Analysis: Vol. 20
:
Iss.
1
, Article 24.
Available at: https://doi.org/10.38212/2224-6614.2090