[关键词]
[摘要]
目的 研究搜山虎(岭南花椒Zanthoxylumau strosinense的根和茎)的化学成分,为双虎肿痛宁酊剂的药效物质基础研究和质量标准提升提供依据。方法 利用AB-8大孔树脂、硅胶、制备色谱进行成分分离,并结合核磁共振氢谱、碳谱和质谱鉴定化合物结构;采用脂多糖(lipopolysaccharide,LPS)刺激小鼠单核巨噬细胞RAW264.7细胞对化合物进行抗炎活性的研究;采用小鼠醋酸扭体法、热板法对分离得到的成分进行镇痛活性的研究。结果 从搜山虎根中共分离得到10个化合物,分别鉴定为胡芦巴碱(1)、甲芬那酸(2)、4-羟基肉桂酸(3)、小檗碱(4)、橙皮苷(5)、新绿原酸(6)、白藜芦醇(7)、芥子酸(8)、脯氨酸(9)和甘草次酸(10)。抗炎活性研究结果表明,化合物2、4~7、10能够显著抑制肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、白细胞介素-6(interleukin-6,IL-6)的释放。镇痛实验结果表明,化合物2、4、7能够显著降低小鼠扭体次数,显著提高痛阈值。结论 所有化合物均为首次从该植物及花椒属植物中分离得到,化合物2、4、7具有很好的抗炎和镇痛作用。
[Key word]
[Abstract]
Objective Identificationthe chemical constituents of Zanthoxyli Austrosinenesis Radix et Caulis is an important work for evaluating the potential pharmacodynamicsubstances and controlling the quality of Shuanghu zhongtong ning tincture. Methods The compounds were isolated by AB-8 macroporous resin, silica gel column chromatography and preparative chromatography. And the structural analysis was performed with NMR and UPLC-Q-TOF and their anti-inflammatory activity and analgesic effects were investigated in vitro. Results Ten compounds were isolated from Zanthoxylum austrosinense Huang and identified as trigonelline (1), mefenamic acid (2), 4-hydroxycinnamic acid (3), berberine (4), hesperidin (5), neochlorogenic acid (6), resveratrol (7), erucic acid (8), proline (9) and glycyrrhetinic acid (10). The anti-inflammatory experiment indicated that compound 2, 4-7, 10 exhibited significant biological activities, which suppressed the release of TNF-α and IL-6. In addition, compound 2, 4, 7 had significant analgesic effects on rats by a reduced writhing and increased the pain threshold. Conclusion All the compounds were isolated from Zanthoxylum austrosinense for the first time. Compounds 2, 4 and 7 exhibited significantly anti-inflammatory activity and analgesic effects.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金资助项目(82060641);中国博士后面上基金资助项目(2019M653814XB);广西科技基地和人才专项(2018AD19035);广西自然科学基金课题(2018JJB140377、2018JJB140325);广西中青年教师提升项目(2019KY0338);广西一流学科建设开放性课题(2019XK127);广西中医药大学校级课题(2018MS003)。