Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea.

Hiroyuki Sato (1, 2, 3) , Cédric Genet , Axelle Strehle , Charles Thomas (4) , Annelise Lobstein (5) , Alain Wagner (5) , Charles Mioskowski (5) , Johan Auwerx (4, 6) , Régis Saladin

1 Department of Physics - Department of Physics
2 Department of Physics
3 MCC - Science and Technology Research Center
4 IGBMC - Institut de génétique et biologie moléculaire et cellulaire
5 Institut Gilbert-Laustriat : Biomolécules, Biotechnologie, Innovation Thérapeutique
6 ICS - Institut Clinique de la Souris

Olive tree (Olea europeaea) leaves are well known for their effect on metabolism in particular as a traditional anti-diabetic and anti-hypertensive herbal drug. These properties are until now only attributed to oleuropein, the major secoiridoid of olive leaves. Here we describe the isolation and the identification of another constituent implicated in the anti-diabetic effect of this plant, i.e. oleanolic acid. We show that this triterpene is an agonist for TGR5, a member of G-protein coupled receptor activated by bile acids and which mediates some of their various cellular and physiological effect. Oleanolic acid lowers serum glucose and insulin levels in mice fed with a high fat diet and it enhances glucose tolerance. Our data suggest that both oleuropein and oleanolic acid are involved in the anti-diabetic effect of olive leaves and further emphasize the potential role of TGR5 agonists to improve metabolic disorders.

Domaines: Biologie moléculaire

Hiroyuki Sato, Cédric Genet, Axelle Strehle, Charles Thomas, Annelise Lobstein, et al.. Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea.. Biochemical and Biophysical Research Communications, 2007, 362 (4), pp.793-8. ⟨10.1016/j.bbrc.2007.06.130⟩. ⟨hal-00188900⟩