title: Anti-inflammatory and PPAR transactivational properties of flavonoids from the roots of Sophora flavescens.
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-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.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
authors.forename: Tran Hong
authors.initials: TH
authors.lastname: Quang
authors.forename: Nguyen Thi Thanh
authors.initials: NT
authors.lastname: Ngan
authors.forename: Chau Van
authors.initials: CV
authors.lastname: Minh
authors.forename: Phan Van
authors.initials: PV
authors.lastname: Kiem
authors.forename: Bui Huu
authors.initials: BH
authors.lastname: Tai
authors.forename: Nguyen Xuan
authors.initials: NX
authors.lastname: Nhiem
authors.forename: Nguyen Phuong
authors.initials: NP
authors.lastname: Thao
authors.forename: Bui Thi Thuy
authors.initials: BT
authors.lastname: Luyen
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Yang
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D051546:Cyclooxygenase 2 / Q000378:metabolism; D005419:Flavonoids / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000145:classification; D010936:Plant Extracts / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry*; D029909:Sophora / Q000737:chemistry*; D015533:Transcriptional Activation / Q000187:drug effects*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D005419:Flavonoids; D016328:NF-kappa B; D047492:Peroxisome Proliferator-Activated Receptors; D010936:Plant Extracts; D014409:Tumor Necrosis Factor-alpha; C496319:NOS2 protein, human; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human
keywords: Flavonoid, NF-κB-luciferase assay; Leguminosae; PPRE-luciferase assay; RT-PCR; Sophora flavescens