Research Article

Anti-Inflammatory and PPAR Transactivational Properties of Flavonoids from the Roots of Sophora flavescens

  1. Tran Hong Quang1,2,†,
  2. Nguyen Thi Thanh Ngan1,†,
  3. Chau Van Minh2,
  4. Phan Van Kiem2,
  5. Bui Huu Tai1,2,
  6. Nguyen Xuan Nhiem1,2,
  7. Nguyen Phuong Thao1,2,
  8. Bui Thi Thuy Luyen1,
  9. Seo Young Yang1,
  10. Young Ho Kim1,*

Article first published online: 30 OCT 2012

DOI: 10.1002/ptr.4871

Additional Information

How to Cite

Quang, T. H., Ngan, N. T. T., Minh, C. V., Kiem, P. V., Tai, B. H., Nhiem, N. X., Thao, N. P., Luyen, B. T. T., Yang, S. Y. and Kim, Y. H. (2012), Anti-Inflammatory and PPAR Transactivational Properties of Flavonoids from the Roots of Sophora flavescens. Phytother. Res.. doi: 10.1002/ptr.4871

Author Information

  1. 1

    College of Pharmacy, Chungnam National University, Daejeon, Korea

  2. 2

    Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), Caugiay, Hanoi, Viet Nam

  1. †

    The authors contributed equally to this research

* Young Ho Kim, College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
E-mail: yhk@cnu.ac.kr

  • †

    The authors contributed equally to this research

Publication History

  1. Article first published online: 30 OCT 2012
  2. Manuscript Accepted: 3 OCT 2012
  3. Manuscript Revised: 5 SEP 2012
  4. Manuscript Received: 31 MAY 2012

Funded by

  • Ministry of Education, Science and Technology. Grant Number: 2009-0093815

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Keywords:

  • Sophora flavescens;
  • Leguminosae;
  • Flavonoid, NF-κB-luciferase assay;
  • RT-PCR;
  • PPRE-luciferase assay

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-κB-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-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 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 EC50 values ranging from 1.1 to 13.0 μM. Compounds 1, 3, 5, 6, 8, and 9 exhibited dose-dependent PPARα transactivational activity, with EC50 values in a range of 0.9 − 16.0 μM. Compounds 1, 3, 8, and 9 also significantly upregulated PPARγ activity in a dose-dependent manner, with EC50 values of 10.5, 6.6, 15.7, and 1.6 μM, whereas compounds 1, 8, and 9 demonstrated transactivational PPARβ(δ) effects with EC50 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.

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