The health benefits of botanicals is linked to their phytochemicals that often exert pleiotropic effects via targeting multiple molecular signaling pathways such as the peroxisome proliferator-activated receptors (PPARs) and the nuclear factor kappaB (NFκB). The PPARs are transcription factors that control metabolic homeostasis and inflammation while the NF-κB is a master regulator of inflammatory genes such as the inducible nitric-oxide synthase that result in nitric oxide (NO) overproduction. Extracts of Maerua subcordata (MS) and selected candidate constituents thereof, identified by liquid chromatography coupled to mass spectroscopy, were tested for their ability to induce PPARγ mediated gene expression in U2OS-PPARγ cells using luciferase reporter gene assay and also for their ability to inhibit lipopolysaccharide (LPS) induced NO production in RAW264.7 macrophages. While measuring the effect of test samples on PPARγ mediated gene expression, a counter assay that used U2OS-Cytotox cells was performed to monitor cytotoxicity or any non-specific changes in luciferase activity. The results revealed that the fruit, root, and seed extracts were non-cytotoxic up to a concentration of 30 g dry weight per litre (gDW/L) and induced PPARγ mediated gene expression but the leaf extract showed some cytotoxicity and exhibited minimal induction. Instead, all extracts showed concentration (1–15 gDW/L) dependent inhibition of LPS induced NO production. The root extract showed weaker inhibition. Among the candidate constituents, agmatine, stachydrine, trigonelline, indole-3-carboxyaldehyde, plus ethyl-, isobutyl-, isopropyl, and methyl-isothiocyanates showed similar inhibition, and most showed increased inhibition with increasing concentration (1–100 μM) although to a lesser potency than the positive control, aminoguanidine. The present study demonstrated for the first time the induction of PPARγ mediated gene expression by MS fruit, root, and seed extracts and the inhibition of LPS induced NO production by MS fruit, leaf, root, and seed extracts and some candidate constituents thereof.

中文翻译：

---

过氧化物酶体增殖物激活的受体γ（PPARγ）介导的基因表达的诱导和黑皮夜蛾（Maerua subcordata（Gilg）DeWolf）诱导的一氧化氮生成的抑制。

植物药的健康益处与其通常通过靶向多种分子信号传导途径（例如过氧化物酶体增殖物激活受体（PPAR）和核因子κB（NFκB））发挥多效作用的植物化学物质有关。PPAR是控制新陈代谢稳态和炎症的转录因子，而NF-κB是炎症基因（如可诱导的一氧化氮合酶）的主要调节剂，可导致一氧化氮（NO）过量产生。液相色谱-质谱联用技术鉴定的马氏Ma提取物及其选定的候选成分，使用萤光素酶报告基因测试了它们在U2OS-PPARγ细胞中诱导PPARγ介导的基因表达的能力，以及在RAW264.7巨噬细胞中抑制脂多糖（LPS）诱导的NO产生的能力。在测量测试样品对PPARγ介导的基因表达的影响时，进行了使用U2OS-Cytotox细胞的对抗测定，以监测细胞毒性或荧光素酶活性的任何非特异性变化。结果表明，果实，根和种子提取物在达到30 g干重/升（gDW / L）的浓度下均无细胞毒性，并能诱导PPARγ介导的基因表达，但叶提取物却显示出一定的细胞毒性，并且诱导程度最低。取而代之的是，所有提取物对LPS诱导的NO产生均表现出浓度（1-15 gDW / L）依赖性抑制。根提取物显示出较弱的抑制作用。在候选成分中，胍丁胺，水苏碱，松果碱，吲哚-3-羧醛以及乙基，异丁基，异丙基和异硫氰酸甲酯显示出相似的抑制作用，并且大多数显示出随着浓度增加（1-100μM）而增加的抑制作用。比阳性对照氨基胍的效力低。本研究首次证明了MS果实，根和种子提取物对PPARγ介导的基因表达的诱导和对LPS诱导的MS果实，叶，根和种子提取物及其一些候选成分的NO生成的抑制。尽管浓度比阳性对照氨基胍低，但大多数浓度（1-100μM）随浓度增加而增加。本研究首次证明了MS果实，根和种子提取物对PPARγ介导的基因表达的诱导和对LPS诱导的MS果实，叶，根和种子提取物及其一些候选成分的NO生成的抑制。尽管浓度比阳性对照氨基胍低，但大多数浓度（1-100μM）随浓度增加而增加。本研究首次证明了MS果实，根和种子提取物对PPARγ介导的基因表达的诱导和对LPS诱导的MS果实，叶，根和种子提取物及其一些候选成分的NO生成的抑制。