Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.

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Citation

Quang TH, Ngan NT, Minh CV, Kiem PV, Tai BH, Thao NP, Song SB, Kim YH

Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2527-33. doi: 10.1016/j.bmcl.2012.01.136. Epub 2012 Feb 8.

PubMed ID
22381047 [ View in PubMed
]
Abstract

Phytochemical study on the roots of Asarum sieboldii resulted in the isolation of one new compound, (1R,2S,5R,6R)-5'-O-methylpluviatilol (1) and 12 known compounds (2-13). Their structures were determined by extensive spectroscopic methods, including 1D and 2D NMR, and MS spectra. The absolute configuration of compound 1 was established using CD spectrum. Compounds 4, 5, and 12/13 significantly inhibited TNFalpha-induced NF-kappaB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values ranging from 6.4 to 9.4 muM. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 1-3, 6,7, 10, and 11 significantly activated the transcriptional activity of PPARs in a dose-dependent manner, with EC(50) values ranging from 1.7 to 20.9 muM. Compounds 7, 10, and 11 exhibited significant dose-dependent PPARalpha transactivational activity, with EC(50) values of 19.5, 15.7, and 4.0 muM, respectively. Compounds 1, 6, 7, 10, and 11 activated PPARgamma transcriptional activity, with EC(50) values ranging from 3.6 to 22.6 muM, whereas compounds 10 and 11 significantly increased PPARbeta(delta) transactivational activity, with EC(50) values of 22.6 and 4.9 muM, respectively. These results provide a scientific support for the use of the roots of A. sieboldii and warrant further studies to develop new agents for the prevention and treatment of the inflammatory and metabolic diseases.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
{4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy}acetic acidPeroxisome proliferator-activated receptor deltaEC 50 (nM)640N/AN/ADetails
TroglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)730N/AN/ADetails