Division of Applied Biosciences, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan.
Life Sci. 2010 Feb 27;86(9-10):337-43. doi: 10.1016/j.lfs.2010.01.001. Epub 2010 Jan 20.
Glucosamine has been used safely to relieve osteoarthritis in humans, but the precise mechanism underlying its efficacy is still unclear. In this study, we investigated the direct effects of glucosamine and related compounds on mast cell mediated inflammation using cultured mast cells and an animal model.
Dinitrophenyl (DNP)-IgE-sensitized rat basophilic leukemia RBL-2H3 cells were treated with glucosamine-HCl (GlcN-HCl), N-acetylglucosamine (GlcNAc), chitin oligomer or chitosan oligomer. Cells were stimulated by DNP-BSA to induce degranulation and released beta-hexosaminedase was determined colorimetrically to measure the degree of degranulation. Dinitrofluorobenzene (DNFB) sensitized BALB/c mice were administrated orally with 1 or 0.1mg GlcN-HCl or GlcNAc for 6 days. One hour after the final administration, mice were challenged by DNFB to induce ear swelling.
GlcN-HCl significantly inhibited the antigen-induced degranulation of RBL-2H3 cells at higher than 0.01 mg/mL for 24h-treatment while GlcNAc, a chitin oligomer and a chitosan oligomer had no effect. GlcN-HCl also suppressed intracellular calcium mobilization. GlcN-HCl and GlcNAc significantly suppressed the antigen-induced up-regulation of TNF-alpha and IL-6 mRNA. Ear swelling and histamine levels of plasma and ear in DNFB-treated mice were significantly suppressed by oral administration of GlcN-HCl or GlcNAc (0.1 and 1mg) for 6 days.
Our results strongly suggest that GlcN-HCl and GlcNAc have anti-inflammatory effects in vivo by suppressing the activation of mast cells.
氨基葡萄糖已被安全地用于缓解人类骨关节炎，但它的确切疗效机制仍不清楚。在这项研究中，我们使用培养的肥大细胞和动物模型研究了氨基葡萄糖及其相关化合物对肥大细胞介导的炎症的直接影响。
用二硝基苯（DNP）-IgE 致敏的大鼠嗜碱性白血病 RBL-2H3 细胞处理氨基葡萄糖盐酸盐（GlcN-HCl）、N-乙酰氨基葡萄糖（GlcNAc）、几丁寡糖或壳寡糖。用 DNP-BSA 刺激细胞诱导脱颗粒，比色法测定β-己糖胺酶的释放来衡量脱颗粒的程度。用二硝基氟苯（DNFB）致敏 BALB/c 小鼠，连续 6 天每天口服 1 或 0.1mg GlcN-HCl 或 GlcNAc。末次给药后 1 小时，用 DNFB 对小鼠进行攻毒，诱导耳部肿胀。
GlcN-HCl 在高于 0.01mg/ml 时对 RBL-2H3 细胞的抗原诱导脱颗粒有显著抑制作用，作用时间为 24 小时，而 GlcNAc、几丁寡糖和壳寡糖则没有作用。GlcN-HCl 还抑制细胞内钙动员。GlcN-HCl 和 GlcNAc 显著抑制抗原诱导的 TNF-α和 IL-6mRNA 的上调。连续 6 天口服 GlcN-HCl 或 GlcNAc（0.1 和 1mg）可显著抑制 DNFB 处理小鼠的耳部肿胀和血浆及耳部组织中的组胺水平。
我们的研究结果强烈表明，GlcN-HCl 和 GlcNAc 通过抑制肥大细胞的激活，具有体内抗炎作用。
