Kim Ha-Rim, Noh Eun-Mi, Kim Seon-Young
Jeonju AgroBio-Materials Institute, Jeonju, 54810, Republic of Korea.
Heliyon. 2023 Jan 5;9(1):e12778. doi: 10.1016/j.heliyon.2022.e12778. eCollection 2023 Jan.
Ginger ( Roscoe) has been used for food and applied in Ayurvedic medicine in India for thousands of years. With a reputation for strong anti-inflammatory properties, it has been used for to treat colds, migraines, nausea, arthritis, and high blood pressure in China and Southeast Asia. The physiological activity of ginger is attributed to its functional components, including gingerol and shogaol, and their derivatives.
We aimed to investigate the effects of 8- and 10-shogaol and their bioactive signaling mechanisms in a dextran sodium sulfate (DSS)-induced colitis mouse model. The anti-colitis efficacy of 6-, 8-, and 10-derivatives of gingerol and shogaol was comparatively analyzed.
Colitis was induced by providing mice with drinking water containing 5% DSS (w/v) for 8 days. The 6-, 8-, and 10-derivatives of gingerol and shogaol were orally administered for two weeks at a dose of 30 mg/kg. Changes in body weight and disease activity index were measured. The levels of pro-inflammatory cytokines, iNOS and COX-2, as well as the phosphorylation of NF-κB were analyzed using ELISA, PCR, or western blotting. Mucin expression and mRNA levels were measured using alcian blue staining and PCR, respectively. The tight-junction-associated proteins occludin and ZO-1 were assessed using immunohistological staining.
The 6-, 8-, and 10-derivatives of gingerol and shogaol exhibited anti-inflammatory effects by regulating NF-κB signaling. Among the compounds administered, 10-shogaol was the most effective against DSS-induced inflammation. Comparative analysis of the chemical structure showed that shogaol, a dehydrated analog of gingerol, was more effective. 6- and 10-shogaol showed similar effects on DSS-induced morphological changes in the colonic mucus layer, mucin expression, and tight junction proteins.
6-, 8-, and 10-Gingerol and 6-, 8-, and 10-shogaol significantly improved the clinical symptoms and intestinal epithelial barrier damage in DSS-induced colitis in mice. The derivatives effectively inhibited DSS-induced inflammation through the regulation of NF-κB signaling. Moreover, 10-shogaol showed the most potent anti-inflammatory effect among the six compounds used in this study. The results indicate that 8- and 10-shogaol, both main ingredients in ginger, may serve as therapeutic candidates for the treatment of colitis.
姜（Roscoe）数千年来一直被用于食品，并在印度阿育吠陀医学中应用。因其强大的抗炎特性而闻名，在中国和东南亚，它已被用于治疗感冒、偏头痛、恶心、关节炎和高血压。姜的生理活性归因于其功能成分，包括姜辣素和姜烯酚及其衍生物。
我们旨在研究8-姜烯酚和10-姜烯酚及其生物活性信号传导机制在葡聚糖硫酸钠（DSS）诱导的结肠炎小鼠模型中的作用。对姜辣素和姜烯酚的6-、8-和10-衍生物的抗结肠炎疗效进行了比较分析。
通过给小鼠提供含5% DSS（w/v）的饮用水8天来诱导结肠炎。姜辣素和姜烯酚的6-、8-和10-衍生物以30mg/kg的剂量口服给药两周。测量体重和疾病活动指数的变化。使用酶联免疫吸附测定（ELISA）、聚合酶链反应（PCR）或蛋白质免疫印迹法分析促炎细胞因子、诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）的水平以及核因子κB（NF-κB）的磷酸化。分别使用阿尔辛蓝染色和PCR测量粘蛋白表达和mRNA水平。使用免疫组织化学染色评估紧密连接相关蛋白闭合蛋白和紧密连接蛋白1（ZO-1）。
姜辣素和姜烯酚的6-、8-和10-衍生物通过调节NF-κB信号传导发挥抗炎作用。在所给药的化合物中，10-姜烯酚对DSS诱导的炎症最有效。化学结构的比较分析表明，姜烯酚的脱水类似物姜烯酚更有效。6-姜烯酚和10-姜烯酚对DSS诱导的结肠黏液层形态变化、粘蛋白表达和紧密连接蛋白显示出相似的作用。
6-、8-和10-姜辣素以及6-、8-和10-姜烯酚显著改善了DSS诱导的小鼠结肠炎的临床症状和肠上皮屏障损伤。这些衍生物通过调节NF-κB信号传导有效抑制了DSS诱导的炎症。此外，10-姜烯酚在本研究使用的六种化合物中显示出最有效的抗炎作用。结果表明，姜中的两种主要成分8-姜烯酚和10-姜烯酚可能作为治疗结肠炎的候选药物。
