厚皮香酚性成分及其镇痛活性

Phenolic constituents from Ternstroemia gymnanthera and their analgesic activities

目的研究厚皮香Ternstroemia gymnanthera(Wight et Arn.) Beddome酚类成分及其镇痛活性。方法厚皮香95%乙醇提取物的乙酸乙酯部位采用硅胶、RP18、Sephadex LH-20进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。然后,小鼠醋酸扭体实验测定镇痛活性。结果从中分离得到8个酚类化合物,分别鉴定为东莨菪内酯(1)、4-hydroxy-3-(methoxycarbonyl)benzoic acid(2)、原儿茶醛(3)、methyl 2-(3,4-dihydroxyphenyl)-2-methoxyacetate(4)、3,4-二羟基苯乙醇(5)、3,4-二羟基苯乙酸甲酯(6)、对羟基苯甲醛(7)、3,4-二羟基苯乙酸(8)。化合物1~4、7均能有效地抑制小鼠扭体次数。结论化合物1~3、5~8均为首次从该植物中分离得到,1、3、5、7~8为首次从该属植物中分离得到。化合物1、4、7具有显著的镇痛活性。

AIM To study the phenolic constituents from Ternstroemia gymnanthera(Wight et Arn.) Beddome and their analgesic activities.METHODS The ethyl acetate fraction of 95% ethanol extract from T. gymnanthera was isolated and purified by silica, RP18 and Sephadex LH-20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The analgesic activities were tested based on mice acetic acid writhing experiment.RESULTS Eight phenolic compounds were isolated and identified as scopoletin(1), 4-hydroxy-3-(methoxycarbonyl)benzoic acid(2), protocatechualdehyde(3), methyl 2-(3,4-dihydroxyphenyl)-2-methoxyacetate(4), 3,4-dihydroxyphenylethanol(5), methyl 2-(3,4-dihydroxyphenyl)acetate(6), 4-hydroxybenzaldehyde(7) and 3,4-dihydroxyphenylaceticacid(8). Compounds 1-4 and 7 could effectively reduce the number of writhing in mice.CONCLUSION Compounds 1-3 and 5-8 are isolated from this plant for the first time, and compounds 1, 3, 5, 7 and 8 are isolated from genus Ternstroemia for the first time. Compounds 1, 4 and 7 have significant analgesic activities.