瑞香科木脂素类化合物及其对脂多糖诱导的肿瘤坏死因子和一氧化氮产生的抑制作用。
Secoiridoids from the Seed of and Their Inhibitory Potential on LPS-Induced Tumor Necrosis Factor and Nitric Oxide Production.
机构信息
Taiwan Sugar Research Institute, Tainan 70176, Taiwan.
Department of Biological Science and Technology, National Pingtung University of Science and Technology, Pingtung 91201, Taiwan.
出版信息
Molecules. 2018 Jul 4;23(7):1633. doi: 10.3390/molecules23071633.
Three new secoiridoid constituents, goncarin A−C (⁻), and a new derivative, goncarin A monoacetate (), along with two known lignins, pinoresinol () and paulownin (), were isolated from the seed of (Baill.) Becc. The structures of the new metabolites were determined on the basis of extensive spectroscopic analysis, particularly mass spectroscopy and 2D NMR (¹H⁻¹H COSY, HMQC, HMBC, and NOESY) spectroscopy. The aim of this study was to identify the anti-inflammatory effects of compounds ⁻ on lipopolysaccharide (LPS)-stimulated murine macrophage cell lines (RAW 264.7). Following stimulation with LPS, elevated levels of nitric oxide (NO) production were detected in RAW 264.7 cells; however, pretreatment with compounds ⁻ significantly inhibited the production of NO (around 40⁻80%, < 0.01⁻0.05), by suppressing the expression of inducible NO synthase (iNOS). In addition, LPS-stimulated tumor necrosis factor-α (TNF-α) production was significantly reduced by compounds ⁻ (25⁻40%, < 0.01⁻0.05). These results suggested that compounds ⁻ may exert anti-inflammatory activity, and that compounds ⁻ may be considered a potential therapeutic for the treatment of inflammatory diseases associated with macrophage activation.
从 （Baill.）Becc 的种子中分离得到了三种新的环烯醚萜类成分，即 goncarin A−C（⁻）和 goncarin A 单乙酸酯（），以及两种已知的木脂素，pinoresinol（）和 paulownin（）。新代谢产物的结构是基于广泛的光谱分析确定的，特别是质谱和 2D NMR（¹H-¹H COSY、HMQC、HMBC 和 NOESY）光谱。本研究的目的是鉴定化合物 ⁻ 对脂多糖（LPS）刺激的小鼠巨噬细胞系（RAW 264.7）的抗炎作用。在 LPS 刺激后，RAW 264.7 细胞中检测到一氧化氮（NO）生成水平升高；然而，化合物 ⁻ 的预处理通过抑制诱导型一氧化氮合酶（iNOS）的表达，显著抑制了 NO 的产生（约 40⁻80%，<0.01⁻0.05）。此外，化合物 ⁻ 还显著降低了 LPS 刺激的肿瘤坏死因子-α（TNF-α）的产生（25⁻40%，<0.01⁻0.05）。这些结果表明，化合物 ⁻ 可能具有抗炎活性，并且化合物 ⁻ 可被视为治疗与巨噬细胞激活相关的炎症性疾病的潜在治疗药物。
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