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目的研究桂枝的化学成分及其神经保护作用。方法运用多种色谱方法对桂枝体积分数90%乙醇提取物的化学成分进行分离纯化,并根据波谱数据和理化性质确定其化学结构。采用建立体外脂多糖(lipopolysaccharide,LPS)激活N9小胶质细胞异常活化的筛选模型对所分离化合物的活性进行评价。结果分离得到了10个化合物,分别鉴定为桂皮醛(cinnamaldehyde,1)、肉桂酸(cinnamic acid,2)、肉桂醇(cinnamyl alcohol,3)、原儿茶醛(protocatechuic aldehyde,4)、原儿茶酸(protocatechuic acid,5)、香豆素(coumarin,6)、钩果草苷(harpagoside,7)、二氢肉桂苷(dihydrocinnacasside,8)、3,4,5-三甲氧基-1-β-D-吡喃葡萄糖苷(3,4,5-trimethoxypheny-1-β-Dglucopyranoside,9)和邻香豆酸葡萄糖苷(O-coumaric acid glucoside,10)。抑制活性试验表明,化合物3能够较好地抑制LPS刺激的N9小胶质细胞NO释放,在其发挥抑制作用的浓度范围内不影响小胶质细胞的存活率。结论从桂枝乙醇提取物中分离得到10个化合物,其中化合物7、9和10为首次从樟科植物中分离得到。化合物3具有较好的抑制活性。
Objective To study the chemical constituents of Guizhi and its neuroprotective effects. Methods The chemical constituents of 90% ethanol extract of Cassia twig were separated and purified by a variety of chromatographic methods. The chemical structure of the extracts was determined according to spectral data and physicochemical properties. The activity of isolated compounds was evaluated using a screening model that established in vitro activation of N9 microglial cells by lipopolysaccharide (LPS). Results Ten compounds were isolated and identified as cinnamaldehyde (1), cinnamic acid (2), cinnamyl alcohol (3), protocatechuic aldehyde (4) Protocatechuic acid (5), coumarin (6), harpagoside (7), dihydrocinnacasside (8), 3,4,5-trimethoxy-1- 3,4-trimethoxypheny-1-β-D-glucopyranoside (9) and O-coumaric acid glucoside (10). Inhibitory activity test showed that Compound 3 could inhibit NO release from LPS-stimulated N9 microglial cells, and did not affect the survival rate of microglial cells in the concentration range that exerted its inhibitory effect. Conclusion Ten compounds were isolated from the ethanol extract of Cassia twig, among which compounds 7, 9 and 10 were isolated from Lauraceae for the first time. Compound 3 has better inhibitory activity.