楤木单体的结构改造及抗炎活性研究  

Structural modification and anti-inflammatory biological evaluation of monomeric compounds from Aralia elata

作　　者：季宇彬[1] 邓迪 王宝琪 许旭东[2] 田瑜[2] 尚海[2] JI Yu-bin;DENG Di;WANG Bao-qil,;XU Xu-dong;TIAN Yu;SHANGHai(Center of Research and Development on Life Sciences and Environment Sciences, Harbin University of Commerce, Harbin 150076, China;Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine （Natural Medicine） and Translational Medicine, Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Key Laboratory of Efficacy Evaluation of Chinese Medicine against Glycolipid Metabolic Disorders, State Administration of Traditional Chinese Medicine, Zhong Guan Cnn Open Laboratory of the Research and Development of Natural Medicine and Health Products, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China)

机构地区：[1]哈尔滨商业大学生命科学与环境研究中心,黑龙江哈尔滨150076 [2]中国医学科学院,北京协和医学院药用植物研究所,中药(天然药物)创新药物研发北京市重点实验室,中草药物质基础与资源利用教育部重点实验室,天然药物、健康产品的研究与开发中关村开放实验室,中药干预糖脂代谢紊乱性疾病药效评价重点研究室,北京100193

出　　处：《中草药》2018年第7期1525-1532,共8页Chinese Traditional and Herbal Drugs

基　　金：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)

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。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.

关 键 词：楤木 金盏花苷E 结构改造 抗炎活性 RAW264.7细胞 

分 类 号：R284.3[医药卫生—中药学]