4,5-二咖啡酰奎宁酸对 RAW264.7 细胞和炎症大鼠模型的抗炎作用,Nutrients

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4,5-二咖啡酰奎宁酸对 RAW264.7 细胞和炎症大鼠模型的抗炎作用
Nutrients ( IF 4.546 ) Pub Date : 2021-10-09 , DOI: 10.3390/nu13103537
Goeun Jang ₁ , Seulah Lee ₁ , Joonho Hong ₂ , Boram Park ₃ , Dokyung Kim ₄ , Chunsung Kim ₁

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迫切需要比目前使用的非甾体抗炎药更安全、更有效的抗炎药。二咖啡酰奎宁酸 (diCQA) 异构体 4,5-diCQA 具有抗氧化活性和各种其他促进健康的益处；然而，其抗炎特性需要进一步研究。本研究旨在分别使用 RAW264.7 细胞和角叉菜胶诱导的炎症模型在体外和体内评估 4,5-diCQA 的抗炎特性。在 RAW264.7 细胞中，4,5-diCQA 预处理显着抑制脂多糖诱导的一氧化氮、前列腺素 E _{2 的}表达、一氧化氮合酶、环氧合酶-2、肿瘤坏死因子-α、白细胞介素-1β和白细胞介素-6，不诱导细胞毒性。4,5-diCQA 的抑制作用是通过抑制核因子-κB 核易位和丝裂原活化蛋白激酶 (MAPK) 磷酸化来介导的。以 5、10 和 20 mg/kg 体重的剂量口服 4,5-diCQA 可抑制角叉菜胶诱导的水肿和一氧化氮合酶、环氧合酶-2 和肿瘤坏死因子-α 的表达-依赖方式。总的来说，我们的结果表明 4,5-diCQA 通过在体外抑制核因子-κB 和 MAPK 通路的激活并在体内减少角叉菜胶诱导的水肿来发挥抗炎作用。因此，4,5-diCQA 显示出作为非甾体抗炎药的天然替代品的潜力。

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Anti-Inflammatory Effect of 4,5-Dicaffeoylquinic Acid on RAW264.7 Cells and a Rat Model of Inflammation

Anti-inflammatory agents that are safer and more effective than the currently used non-steroidal anti-inflammatory drugs are urgently needed. The dicaffeoylquinic acid (diCQA) isomer 4,5-diCQA exhibits antioxidant activity and various other health-promoting benefits; however, its anti-inflammatory properties require further investigation. This study was conducted to evaluate the anti-inflammatory properties of 4,5-diCQA in vitro and in vivo using RAW264.7 cells and a carrageenan-induced inflammation model, respectively. In RAW264.7 cells, 4,5-diCQA pretreatment significantly inhibited lipopolysaccharide-induced expression of nitric oxide, prostaglandin E₂, nitric oxide synthase, cyclooxygenase-2, tumor necrosis factor-α, interleukin-1β, and interleukin-6, without inducing cytotoxicity. The inhibitory effects of 4,5-diCQA were mediated by the suppression of nuclear factor-κB nuclear translocation and mitogen-activated protein kinase (MAPK) phosphorylation. Oral administration of 4,5-diCQA at doses of 5, 10, and 20 mg/kg of the body weight suppressed carrageenan-induced edema and the expression of nitric oxide synthase, cyclooxygenase-2, and tumor necrosis factor-α in a dose-dependent manner. Collectively, our results suggest that 4,5-diCQA exerts anti-inflammatory effects by suppressing activation of the nuclear factor-κB and MAPK pathways in vitro and reducing carrageenan-induced edema in vivo. Therefore, 4,5-diCQA shows potential as a natural alternative to non-steroidal anti-inflammatory drugs.

更新日期：2021-10-09

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