Diterpenoids from Siegesbeckia pubescens and their PPARγ agonist activities

International Conference and Exhibition on Marine Drugs and Natural Products

July 25-27, 2016 Melbourne, Australia

Yiping Ye

Zhejiang Academy of Medical Sciences, China

Posters & Accepted Abstracts: J Pharmacogn Nat Prod

Abstract :

We previously reported ameliorative effects of the aqueous extract of Siegesbeckia pubescens on experimental colitis in rats by activation of PPAR�³ and inhibition of NF-�ºB pathway, consequently suppressing the release of multiple pro-inflammatory cytokines. Here, activity-guided fractionation was isolated to obtain 8 ditepenoids by using reporter gene assays. The aqueous extract of Siegesbeckia pubescens was applied to resin column chromatography to get five fractions, and the activity-guided fractionation was further isolated by silica gel and Rp-18 column chromatography to obtain 8 compounds. HEK293 cells were transiently transfected by Lipofectamine�®3000 with the expression plasmid of pCDNA-PPAR�³, the reporter plasmid PPRE-tk-luc, and pRL-tk as internal reference plasmid and were incubated for 24h. Then, the cells were treated with above 8 compounds respectively and were incubated for 48h. Luciferase activity and fluorescence intensity were measured. The structures of 8 compounds were elucidated as diterpenoids, including two new diterpenoids. 7 of these diterpenoids except compound 5 displayed PPAR�³ agonist activities at the maximum concentration of no toxicity against HEK293T cells. These active diterpenoids may be potent natural PPAR�³ agonists for antiinflammatory agents, anti-diabetics.

Biography :

Yiping Ye has completed his PhD from Zhejiang University department of Chemistry. She is the Professor of Institute of Materia Medica, Zhejiang Academy of Medical Sciences. She has published more than 50 papers in reputed journals.

Email: yeyiping2005@163.com