Anti-inflammatory and PPAR Subtypes Transactivational Activities of Phenolics and Lignans from the Stem Bark of Kalopanax pictus

Bulletin of the Korean chemical society

Bui Thi Thuy Luyen¹  Chau Van Minh¹  Phan Van Kiem¹  Nguyen Phuong Thao¹  Nguyen Thi Thanh Ngan¹  Tran Hong Quang¹  Bui Huu Tai¹  Nguyen Xuan Nhiem¹  Seok Bean Song¹ 

关键词: Kalopanax pictus;    Araliaceae;    Phenolic;    Anti-inflammatory;    PPAR transactivational activity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A new compound, kalopanaxin F (3), and 11 known compounds (1, 2, 4-12), were isolated from the stem bark of Kalopanax pictus. Their structures were elucidated on the basis of chemical and spectroscopic methods. Five of the compounds (2, 3, 5, 6, and 12) significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 values ranging from 6.2 to 9.1 μM. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 3-7, 9, and 12 significantly activated the transcriptional activity of PPARs dose-dependently, with EC50 values ranging from 4.1-12.7 μM. Compounds 4 and 5 exhibited PPARα, PPARγ, and PPARβ(δ) transactivational activities in a dose-dependent manner, with EC50 values of 16.0 and 17.0, 8.7 and 16.5, 26.2 and 26.3 μM, respectively.

【 授权许可】

Unknown