Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-kappaB activation and PPAR transcriptional activity.

Article Details

Citation

Copy to clipboard

Quang TH, Ngan NT, Minh CV, Kiem PV, Yen PH, Tai BH, Nhiem NX, Thao NP, Anh Hle T, Luyen BT, Yang SY, Choi CW, Kim YH

Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-kappaB activation and PPAR transcriptional activity.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6681-7. doi: 10.1016/j.bmcl.2012.08.099. Epub 2012 Sep 13.

PubMed ID

23031596 [ View in PubMed

]

Abstract

In the screening search for NF-kappaB inhibitory and PPAR transactivational agents from medicinal plants, a methanol extract of the whole plant of Tacca plantaginea and its aqueous fraction showed the significant activities. Bioassay-guided fractionation combined with repeated chromatographic separation of the aqueous fraction of the methanol extract of T. plantaginea resulted in the isolation of two new diarylheptanoid glycosides, plantagineosides A (1) and B (2), an unusual new cyclic diarylheptanoid glycoside, plantagineoside C (3), and three known compounds (4-6). Their structures were determined by extensive spectroscopic and chemical methods. Compounds 3-6 significantly inhibited TNFalpha-induced NF-kappaB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values ranging from 0.9 to 9.4 muM. Compounds 1-6 significantly activated the transcriptional activity of PPARs in a dose-dependent manner, with EC(50) values ranging from 0.30 to 10.4 muM. In addition, the transactivational effects of compounds 1-6 were evaluated on three individual PPAR subtypes, including PPARalpha, gamma, and beta(delta). Compounds 1-6 significantly enhanced the transcriptional activity of PPARbeta(delta), with EC(50) values in a range of 11.0-30.1 muM. These data provide the rationale for using T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
{4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy}acetic acid	Peroxisome proliferator-activated receptor delta	EC 50 (nM)	650	N/A	N/A	Details
Troglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	720	N/A	N/A	Details