Die Gao1, Yong-lan Zhang1, Pan Xu1, Ye-xin Lin1, Feng-qing Yang1, Jian-hui Liu2, Hai-wen Zhu1, Zhi-ning Xia3. 1. College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China. 2. College of Pharmacy and Bioengineering, Chongqing University of Technology, Chongqing 400054, China. 3. College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China. Electronic address: tcm_anal_cqu@163.com.
Abstract
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.
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.