Le Quang, Zhang Zhichang, Sun Daniel, Cui Quanjun, Yang Xinlin, Hassan Ameer E
Dept of Orthopaedic Surgery, University of Virginia, 22903, USA.
Dept of Orthopaedic Surgery, The First Affiliated Hospital of Xinxiang Medical University, Wehui, 453100, Henan, China.
Heliyon. 2023 Apr 25;9(5):e15769. doi: 10.1016/j.heliyon.2023.e15769. eCollection 2023 May.
Glucosamine and N-acetyl-glucosamine (NAG) are amino sugars found in human extracellular matrix with previously described anti-inflammatory effects. Despite mixed results from clinical studies, these molecules have been used extensively in supplements.
We investigated the anti-inflammatory properties of two synthesized derivatives of N-acetyl-glucosamine (NAG), bi-deoxy-N-acetyl-glucosamine (BNAG) 1 and 2.
Using mouse macrophage RAW 264.7 cells with lipopolysaccharide (LPS) to induce inflammation, the effects of NAG, BNAG 1, and BNAG 2 on the expression of IL-6, IL-1β, inducible nitric oxide synthase (iNOS) and COX-2 were studied using ELISA, Western blot and quantitative RT-PCR. Cell toxicity and nitric oxide (NO) production were evaluated using WST-1 assay and the Griess reagent, respectively.
Among the three tested compounds, BNAG1 shows the highest inhibition of iNOS, IL-6, TNF α and IL-1β expression and NO production. All three tested compounds show slight inhibition on cell proliferation of RAW 264.7 cells, except that BNAG1 displays a remarkable toxicity at the tested maximum dose of 5 mM.
BNAG 1 and 2 exhibit notable anti-inflammatory effects compared to the parent NAG molecule.
氨基葡萄糖和N-乙酰氨基葡萄糖（NAG）是存在于人体细胞外基质中的氨基糖，具有先前所述的抗炎作用。尽管临床研究结果不一，但这些分子已在补充剂中广泛使用。
我们研究了N-乙酰氨基葡萄糖（NAG）的两种合成衍生物双脱氧-N-乙酰氨基葡萄糖（BNAG）1和2的抗炎特性。
使用脂多糖（LPS）诱导炎症的小鼠巨噬细胞RAW 264.7细胞，采用ELISA、蛋白质免疫印迹法和定量逆转录聚合酶链反应研究NAG、BNAG 1和BNAG 2对白细胞介素-6（IL-6）、白细胞介素-1β（IL-1β）、诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）表达的影响。分别使用WST-1法和格里斯试剂评估细胞毒性和一氧化氮（NO）生成。
在三种测试化合物中，BNAG1对iNOS、IL-6、肿瘤坏死因子α（TNFα）和IL-1β表达及NO生成的抑制作用最强。除BNAG1在5 mM的测试最大剂量下显示出显著毒性外，所有三种测试化合物对RAW 264.7细胞的增殖均有轻微抑制作用。
与母体NAG分子相比，BNAG 1和2表现出显著的抗炎作用。
