在体外和体内,来自Aglaia odorata的天然抗神经炎症抑制剂
Qianqian Yin1, Gang Chen1, Danyang Mu2
1School of Traditional Chinese Materia Medica, Key Laboratory of Innovative Traditional Chinese Medicine for Major Chronic Diseases of Liaoning province, Key Laboratory for TCM Material Basis Study and Innovative Drug Development of Shenyang City, Shenyang Pharmaceutical University, Shenyang 110016, China.
芳香菌的化合物,特别是环[b]衍生物,通过抑制氧化的产生,表现出强大的抗神经炎症活性. 洛卡格拉醇通过通过NF-κB通路减少微质激活和炎症标志物,在体内证明了有效性.
科学领域:
- 自然产品化学 自然产品化学
- 神经药理学神经药理学
- 药用化学 医学化学
背景情况:
- 神经炎症与各种神经系统疾病有关.
- 芳香草是生物活性化合物的植物来源.
- 识别新型抗神经炎症剂对于治疗开发至关重要.
研究的目的:
- 为了分离和描述来自Aglaia odorata的化合物.
- 在体外和体外评估它们的抗神经炎症活性.
- 阐明有前途的化合物的作用机制.
主要方法:
- 使用光谱分析 (ECD,NMR) 和量子化学计算,分离和阐明化合物的结构.
- 在体外生物活性查使用脂聚糖诱导的BV-2细胞来测量氧化抑制.
- 在 lipopolysaccharide 治疗的小鼠模型中的体内研究,使用免疫光学,qRT-PCR 和西方斑点.
主要成果:
- 从Aglaia odorata中分离出50种化合物,其中包括7种新化合物.
- 环[b]衍生物表现出强烈的氧化抑制 (IC50 2-100 nM),显著优于米诺环素.
- 洛卡格拉 (12) 减弱了微质激活和减少了体内炎症基因表达,表明NF-κB通路的抑制.
结论:
- 香味是一种丰富的抗神经炎症化合物的来源.
- 环[b]富兰衍生物显示出作为神经炎症疾病治疗剂的显著潜力.
- 洛卡格拉醇的机制涉及抑制NF-κB信号通路.
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