摘要
目的研究银杏内酯B衍生物对神经细胞的保护作用。方法以银杏内酯B为原料,对其结构进行修饰,通过酯化反应在银杏内酯B的C-10位羟基分别引入肉桂酰基、4-羟基肉桂酰基、4-甲氧基肉桂酰基、3,4-二甲氧基肉桂酰基合成银杏内酯B的衍生物。并对银杏内酯B和4种衍生物对诱导型SH-SY5Y细胞活力的影响进行了研究。结果与结论合成了4种银杏内酯B衍生物,其结构经ESI-MS、1H-NMR和13C-NMR谱确证,其中目标物GBHC-2、GBHC-3和GBHC-4为未见报道的新化合物。细胞活力实验结果表明,银杏内酯B及其4种衍生物均能显著提高6-OHDA诱导的SH-SY5Y细胞的活力,化合物GBHC-4的活性稍好于其他化合物,但5种化合物之间并无显著差异。
In order to study the protective effect of ginkgolide B derivatives on nerve cells,the structure of ginkgolide B was modified with ginkgolide B as raw material.Cinnamic acid,4-hydroxycinnamic acid,4-methoxycinnamic acid and 3,4-dimethoxycinnamic acid were introduced into the C-10 hydroxyl group of ginkgolide B via esterification.The structures of target compounds were characterized by 1H-NMR,13C-NMR and ESI-MS.The effects of ginkgolide B and its four derivatives on the viability of induced SH-SY5 Y cells were also studied.Among them GBHC-2,GBHC-3 and GBHC-4 were new compounds.The results showed that ginkgolide B and its derivatives could significantly increase the viability of SH-SY5 Y cells induced by 6-OHDA.The activity of GBHC-4 was slightly better than that of other compounds,but there was no significant difference among the five compounds.
作者
冯自立
徐佳元
朱志斌
陈旺
赵正栋
胡代花
白瑜
FENG Zi⁃li;XU Jia⁃yuan;ZHU Zhi⁃bin;CHEN Wang;ZHAO Zheng⁃dong;HU Dai⁃hua;BAI Yu(Shaanxi University of Technology,Hanzhong 723001,China;Shaanxi Cuicheng Biomedical Technology Co.,Ltd.,Hanzhong 723007,China)
出处
《中国药物化学杂志》
CAS
CSCD
北大核心
2020年第4期199-203,共5页
Chinese Journal of Medicinal Chemistry
基金
陕西省重点研发计划项目(2018ZDXM-SF-083)
陕西省教育厅服务地方专项计划项目(18JC008)
陕秦巴山区生物资源综合开发协同创新中心产业化培育项目(QBXT-18-1)
关键词
银杏内酯
衍生物
结构修饰
细胞活力
ginkgolides
derivatives
structural modification
cell viability
作者简介
通信作者:冯自立(1979-),男(汉族),陕西汉中人,副教授,博士,主要从事天然药物制备工艺和构效关系研究,Tel:13891697269,E⁃mail:fengzili2008@163.com。
