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从 L. 的花中分离出的苯庚三炔对 BV2 和 RAW264.7 细胞中 NF-κB 的抑制和 HO-1 表达的抗神经炎症和抗炎活性。

Anti-Neuroinflammatory and Anti-Inflammatory Activities of Phenylheptatriyne Isolated from the Flowers of L. via NF-κB Inhibition and HO-1 Expression in BV2 and RAW264.7 Cells.

机构信息

College of Pharmacy, Chosun University, Dong-gu, Gwangju 61452, Korea.

College of Pharmacy, Wonkwang University, Iksan 54538, Korea.

出版信息

Int J Mol Sci. 2021 Jul 13;22(14):7482. doi: 10.3390/ijms22147482.

Abstract

Aging is associated with immune disregulation and oxidative stress which lead to inflammation and neurodegenerative diseases. We have tried to identify the anti-neuroinflammatory and anti-inflammatory components of L. The dried flowers of were extracted with 70% EtOH, and the obtained extract was divided into CHCl, EtOAc, -BuOH, and HO fractions. The CHCl fraction was separated using silica gel and C-18 column chromatography to yield phenylheptatriyne (), 2'-hydroxy-3,4,4'-trimethoxychalcone (), and 4',7-dimethoxyflavanone (). Additionally, the EtOAc fraction was subjected to silica gel, C-18, and Sephadex LH-20 column chromatography to yield 8-methoxybutin () and leptosidin (). All the compounds isolated from inhibited the production of nitric oxide (NO) in LPS-induced BV2 and RAW264.7 cells. In addition, phenylheptatriyne and 4',7-dimethoxyflavanone reduced the secretion of inflammatory cytokines, tumor necrosis factor alpha (TNF-α), and interleukin (IL)-6. Among them, phenylheptatriyne was significantly downregulated in the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). Subsequently, phenylheptatriyne also effectively inhibited nuclear factor-kappa B (NF-κB) activation in LPS-stimulated BV2 and RAW264.7 cells. Based on these results, the anti-neuroinflammatory effect of phenylheptatriyne isolated from was confirmed, which may exert a therapeutic effect in treatment of neuroinflammation-related diseases.

摘要

衰老是与免疫失调和氧化应激相关的,这些会导致炎症和神经退行性疾病。我们试图确定 L 的抗炎和神经保护成分。 用 70%EtOH 提取 的干燥花,得到的提取物分为 CHCl、EtOAc、-BuOH 和 HO 馏分。CHCl 馏分用硅胶和 C-18 柱色谱分离,得到苯庚三炔()、2'-羟基-3,4,4'-三甲氧基查尔酮()和 4',7-二甲氧基黄烷酮()。此外,EtOAc 馏分经硅胶、C-18 和 Sephadex LH-20 柱色谱分离得到 8-甲氧基丁烷()和 leptosidin()。从 中分离得到的所有化合物均抑制 LPS 诱导的 BV2 和 RAW264.7 细胞中一氧化氮 (NO) 的产生。此外,苯庚三炔和 4',7-二甲氧基黄烷酮减少炎症细胞因子肿瘤坏死因子-α (TNF-α) 和白细胞介素 (IL)-6 的分泌。其中,苯庚三炔显著下调诱导型一氧化氮合酶 (iNOS) 和环加氧酶-2 (COX-2) 的表达。随后,苯庚三炔还能有效抑制 LPS 刺激的 BV2 和 RAW264.7 细胞中核因子-κB (NF-κB) 的激活。基于这些结果,证实了从 中分离出的苯庚三炔具有神经保护作用,这可能对治疗与神经炎症相关的疾病有治疗作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e34/8303746/ec597b5291ae/ijms-22-07482-g001.jpg

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