Plantagiolides I and J, two new withanolide glucosides from Tacca plantaginea with nuclear factor-kappaB inhibitory and peroxisome proliferator-activated receptor transactivational activities

Abstract

A novel withanolide glucoside, plantagiolide I (1), a new withanolide glucoside, plantagiolide J (2), and six known compounds (3-8) were isolated from the whole plant of Tacca plantaginea . Their structures were determined by spectroscopic and chemical methods. Compound 3 significantly inhibited tumor necrosis factor alpha (TNFα)-induced nuclear factor-kappaB (NF-κB) transcriptional activity in HepG2 cells in a dose-dependent manner, with IC 50 values of 9.0 μM . Compounds 1-8 enhanced the transcriptional activity of peroxisome proliferator-activated receptors (PPARs) in a dose-dependent manner, with EC50 values ranging from 1.6 to 49.7 μM. In addition, the transactivational effects of compounds 1-8 on three individual PPAR subtypes, including PPARα, β(δ), and γ were evaluated. Compounds 1-8 significantly activated the transcriptional activity of PPARβ(δ), with EC50 values in a ranging from 4.1 to 29.6 μM. These results provide scientific support for the use of T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases. © 2012 The Pharmaceutical Society of Japan.