[关键词]
[摘要]
目的 对楤木Aralia elata中的单体成分金盏花苷E进行结构改造,并对其结构改造后的类似物进行体外抗炎活性研究。方法 以天然易得的齐墩果酸为起始原料,经苷元28位羧基保护、3位糖苷化、28位羧基脱保护、28位羧基酰胺化、胺基侧链酰胺化、糖基苯甲酰基脱保护、甲叉基脱保护共7步反应制得目标化合物,利用巨噬细胞RAW264.7模型评价化合物的抗炎活性。结果 设计并合成了10个金盏花苷E的结构类似物G1~G5和H1~H5,均经谱学技术确证结构。生物活性实验结果表明,10个化合物对RAW264.7细胞呈现不同程度的抗炎活性,其中化合物G1~G4、H1~H3的抗炎活性优于先导物。结论 化合物G1~G5和H1~H5均为未见文献报道的新化合物,具有潜在的抗炎活性,值得深入研究。
[Key word]
[Abstract]
Objective Based on structural modification of monomeric compound calenduloside E from Aralia elata, to evaluate anti-inflammatory activity of the analogues. Methods Applying oleanolic acid as starting material, the target compounds were prepared by seven steps reactions and evaluated for anti-inflammatory effects by RAW264.7 cells in vitro. Results Ten analogues G1-G5 and H1-H5 were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that all of the compounds had different levels potency of anti-inflammatory effects in cells. In particular, compounds G1-G4 and H1-H3 showed significant anti-inflammatory activity comparing wiht lead compounds. Conclusion The new compounds G1-G5 and H1-H5 which showed potential of anti-inflammatory biological activity, had not been reported in any literatures and deserved further research.
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[基金项目]
国家自然科学基金资助项目(81302656);北京市自然科学基金资助项目(7144225);中国医学科学院医学与健康科技创新工程项目(2016-I2M-1-012)