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

• Main Authors: Hwan Lee, Zhiming Liu, Chi-Su Yoon, Linsha Dong, Wonmin Ko, Eun-Rhan Woo, Dong-Sung Lee
• Format: Article
• Language: English
• Published: MDPI AG 2021-07-01
• Series: International Journal of Molecular Sciences
• Subjects: <i>Coreopsis lanceolata</i> L.; flower; mouse macrophage RAW 264.7; mouse microglia BV2; anti-inflammation
• Online Access: https://www.mdpi.com/1422-0067/22/14/7482

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 <i>Coreopsis lanceolata</i> L. The dried flowers of <i>C. lanceolata</i> were extracted with 70% EtOH, and the obtained extract was divided into CH₂Cl₂, EtOAc, <i>n</i>-BuOH, and H₂O fractions. The CH₂Cl₂ fraction was separated using silica gel and C-18 column chromatography to yield phenylheptatriyne (<b>1</b>), 2′-hydroxy-3,4,4′-trimethoxychalcone (<b>2</b>), and 4′,7-dimethoxyflavanone (<b>3</b>). Additionally, the EtOAc fraction was subjected to silica gel, C-18, and Sephadex LH-20 column chromatography to yield 8-methoxybutin (<b>4</b>) and leptosidin (<b>5</b>). All the compounds isolated from <i>C. lanceolata</i> 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 <i>C. lanceolata</i> was confirmed, which may exert a therapeutic effect in treatment of neuroinflammation-related diseases.