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.

译文

使用NF-κ b-荧光素酶,逆转录酶聚合酶链反应,过氧化物酶体增殖物反应元件 (PPRE)-荧光素酶评估了苦参根中的9种化合物 (1  -  9) 的抗炎和过氧化物酶增殖物激活受体 (ppar) 反式激活作用。GAL-4-PPAR嵌合体分析。化合物4和8以剂量依赖的方式显着抑制了tnf α 诱导的HepG2细胞中的NF-κ b转录活性,其ic of值分别为4.0和4.4  μ m。此外,这些化合物的转录抑制功能被HepG2细胞中环氧合酶2和诱导型一氧化氮合酶基因表达水平的降低所证实。化合物1、3、5、6、8和9以剂量依赖性方式显着激活ppar的转录,其值范围为1.1至13.0  μ m。化合物1、3、5、6、8和9表现出剂量依赖性ppar α 反式激活活性,其值在0.9  -  16.0  μ m的范围内。化合物1、3、8和9也以剂量依赖的方式显着上调ppar γ 活性,其e of value为10.5、6.6、15.7和1.6  μ m,而化合物1、8和9表现出反式激活ppar β(δ) 效应,其e of value为11.4、10.3,和1.5  μ m,分别。这些结果为使用S. flavescens的根提供了科学依据,并需要进一步研究以开发用于预防和治疗炎症和代谢疾病的新药物。

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