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

Eun-Rhan Woo,Chi-Su Yoon,Hwan Lee,Wonmin Ko,Zhiming Liu,Linsha Dong,Dong-Sung Lee

doi:10.3390/ijms22147482

Eun-Rhan Woo, Chi-Su Yoon + Show 5 more

Open Access

https://doi.org/10.3390/ijms22147482

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

Highlights

As the average life span of humans is increasing, aging societies are rapidly developing in many countries, and the attitude towards prevention of aging is actively changing worldwide
The results revealed that compound 1 upregulated the expression of HO-1 (Figure 7a,b)
When macrophages are stimulated by lipopolysaccharides (LPS), known as endotoxins, an inflammatory response occurs, and inflammatory cytokines such as interleukin (IL)-6 and IL-1β are released

Summary

Introduction

As the average life span of humans is increasing, aging societies are rapidly developing in many countries, and the attitude towards prevention of aging is actively changing worldwide. Aging has been linked to immune disregulation, oxidative stress, and free radical generation [1]. It is accompanied by a decrease in organ function and loss of regenerative ability [2]. Among these dysfunctions, oxidative stress contributes to an aging-related chronic inflammatory process, called “inflammatory aging” [3]. Chronic inflammation is a condition in which inflammatory cytokines and chemokines are increased in response to physiological and environmental factors, allowing the immune system to continue functioning at low levels [5]. Oxidative stress contributes to the development of age-related diseases, causes imbalance in the body, and directly causes oxidative damage to cells, resulting in an inflammatory response in which local tissues resist the invasion

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