Lee Gi Baek, Kim Yohan, Lee Kyung Eun, Vinayagam Ramachandran, Singh Mahendra, Kang Sang Gu
Department of Biotechnology, Institute of Biotechnology, College of Life and Applied Sciences, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk, 38541, Republic of Korea.
Stemforce, 313 Institute of Industrial Technology, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk, 38541, Republic of Korea.
Appl Biochem Biotechnol. 2024 Dec;196(12):8431-8452. doi: 10.1007/s12010-024-05003-4. Epub 2024 Aug 3.
Flavonols effectively scavenge the reactive nitrogen species (RNS) and reactive oxygen species (ROS) and act as immune-enhancing, anti-inflammatory, anti-diabetic, and anti-carcinogenic agents. Here, we explored the comparative antioxidant and anti-inflammatory properties of plant-originating flavonols, like quercetin, rutin, and troxerutin against acetylsalicylic acid. Quercetin and rutin showed a high ability to remove active ROS, but troxerutin and acetylsalicylic acid exhibited little such function. In RAW 264.7 cells, quercetin, rutin, and troxerutin did not exhibit cellular toxicity at low concentrations. In addition, quercetin, rutin, and troxerutin considerably (p < 0.05) lowered the protein expression of cyclooxygenase 2 (COX-2) as compared to acetylsalicylic acid in cells inflamed with lipopolysaccharides (LPS). Additionally, in inflamed cells, quercetin and rutin significantly down-regulated the nitrogen oxide (NO) level (p < 0.05) at higher concentrations, whereas Troxerutin did not reduce the NO level. In addition, Troxerutin down-regulated the pro-inflammatory protein markers, such as TNF-α, COX-2, NF-κB, and IL-1β better than quercetin, rutin, and acetylsalicylic acid. We observed that troxerutin exhibited a significantly greater anti-inflammatory effect than acetylsalicylic acid did. Acetylsalicylic acid did not significantly down-regulated the expression of COX-2 and TNF-α (p < 0.05) compared to troxerutin. Hence, it can be concluded that the down-regulation of NO levels and the expression of COX-2 and TNF-α proteins could be mechanisms of action for the natural compounds quercetin, rutin, and troxerutin in preventing inflammation.
黄酮醇能有效清除活性氮物种（RNS）和活性氧物种（ROS），并具有免疫增强、抗炎、抗糖尿病和抗癌作用。在此，我们探讨了植物来源的黄酮醇，如槲皮素、芦丁和曲克芦丁与乙酰水杨酸相比的抗氧化和抗炎特性。槲皮素和芦丁具有较高的清除活性ROS的能力，但曲克芦丁和乙酰水杨酸的这种功能较弱。在RAW 264.7细胞中，槲皮素、芦丁和曲克芦丁在低浓度时未表现出细胞毒性。此外，与用脂多糖（LPS）诱导炎症的细胞中的乙酰水杨酸相比，槲皮素、芦丁和曲克芦丁显著（p < 0.05）降低了环氧化酶2（COX-2）的蛋白表达。此外，在炎症细胞中，槲皮素和芦丁在较高浓度时显著下调了一氧化氮（NO）水平（p < 0.05），而曲克芦丁未降低NO水平。此外，曲克芦丁比槲皮素、芦丁和乙酰水杨酸更好地下调了促炎蛋白标志物，如肿瘤坏死因子-α（TNF-α）、COX-2、核因子-κB（NF-κB）和白细胞介素-1β（IL-1β）。我们观察到曲克芦丁表现出比乙酰水杨酸显著更强的抗炎作用。与曲克芦丁相比，乙酰水杨酸未显著下调COX-2和TNF-α的表达（p < 0.05）。因此，可以得出结论，下调NO水平以及COX-2和TNF-α蛋白的表达可能是天然化合物槲皮素、芦丁和曲克芦丁预防炎症的作用机制。
