In vitro evaluation of dual agonists for PPARγ/β from the flower of Edgeworthia gardneri (wall.) Meisn.

ETHNOPHARMACOLOGICAL RELEVANCE

In Tibet, the flower of Edgeworthia gardneri (Wall.) Meisn., locally named "Lvluohua, [symbols: see text]", has been traditionally used to treat diabetes mellitus for many years.

AIM OF THIS STUDY

To evaluate the activity of dual agonists for PPARγ/β from the flower of E.gardneri in vitro.

MATERIALS AND METHODS

HeLa cells were transiently co-transfected with the re-constructed plasmids of pBIND-PPARγ-LBD or pBIND-PPARβ-LBD and rL4.35. The activities of crude extracts, secondary fractions and compounds from the flower of E.gardneri were evaluated with the transfected cells. Rosiglitazone (at 0.5 μg/mL) and L-165041 (at 0.5 μg/mL) were used as the positive controls for PPARγ and PPARβ respectively.

RESULTS

The results demonstrated that n-hexane, ethyl acetate and n-butanol extracts from the flower of E.gardneri were able to significantly activate PPARγ and PPARβ respectively, and the activity of ethyl acetate extract was much better. We further observed that, among the 11 secondary fractions of ethyl acetate extract, the fr. 9 could activate PPARγ and PPARβ significantly. Moreover, umbelliferone (from fr.9) and pentadecanoic acid could activate PPARγ and PPARβ at the same time.

CONCLUSIONS

The extracts from the flower of E.gardneri could significantly activate PPARγ and PPARβ. Besides, umbelliferone and pentadecanoic acid isolated from the flower of E.gardneri were the new agonists for PPARγ and PPARβ.