In:
Phytotherapy Research, Wiley, Vol. 27, No. 9 ( 2013-09), p. 1300-1307
Abstract:
Anti‐inflammatory and peroxisome proliferator‐activated receptors (PPARs) transactivational effects of nine compounds (1 − 9) from the roots of Sophora flavescens were evaluated using NF‐ κ B‐luciferase, reverse transcriptase polymerase chain reaction, peroxisome proliferator response element (PPRE)‐luciferase, and GAL‐4‐PPAR chimera assays. Compounds 4 and 8 significantly inhibited TNFα‐induced NF‐ κ B transcriptional activity in HepG2 cells in a dose‐dependent manner, with IC 50 values of 4.0 and 4.4 μM, respectively. Furthermore, the transcriptional inhibitory function of these compounds was confirmed by a decrease in cyclooxgenase 2 and inducible nitric oxide synthase gene expression levels in HepG2 cells. Compounds 1, 3, 5, 6, 8, and 9 significantly activated the transcription of PPARs in a dose‐dependent manner, with EC 50 values ranging from 1.1 to 13.0 μM. Compounds 1, 3, 5, 6, 8, and 9 exhibited dose‐dependent PPARα transactivational activity, with EC 50 values in a range of 0.9 − 16.0 μM. Compounds 1, 3, 8, and 9 also significantly upregulated PPAR γ activity in a dose‐dependent manner, with EC 50 values of 10.5, 6.6, 15.7, and 1.6 μM, whereas compounds 1, 8, and 9 demonstrated transactivational PPAR β(δ) effects with EC 50 values of 11.4, 10.3, and 1.5 μM, respectively. These results provide a scientific rationale for the use of the roots of S. flavescens and warrant further studies to develop new agents for the prevention and treatment of inflammatory and metabolic diseases. Copyright © 2012 John Wiley & Sons, Ltd.
Type of Medium:
Online Resource
ISSN:
0951-418X
,
1099-1573
Language:
English
Publisher:
Wiley
Publication Date:
2013
detail.hit.zdb_id:
1493490-5
detail.hit.zdb_id:
639136-9
SSG:
15,3
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