新型奥克梯隆型皂苷元荧光探针的设计、合成与活性评价

发布时间：2018-03-26 09:17

本文选题：人参皂苷　切入点：荧光探针　出处：《有机化学》2017年08期

【摘要】：24R-奥克梯隆型皂苷元(Pyxinol),化学名称(20S,24R)-环氧达玛-3β,12β,25-三醇,是20(S)-原人参二醇的主要代谢产物,具有抗心肌缺血再灌注损伤(myocardial ischemia-reperfusion injury,MIRI)的活性.为了构建有活性的Pyxinol荧光探针,设计应用不同物理特性的连接臂连接Pyxinol与荧光基团异硫氰酸荧光素(FITC,常用荧光基团),以降低荧光大基团对Pyxinol的空间位阻干扰.合成的荧光探针用H9C2心肌细胞进行了体外抗MIRI活性评价.结果显示,具有亲水柔性乙氧基链的荧光探针保留了Pyxinol的抗MIRI活性.该活性小分子荧光探针的首次合成,为Pyxinol等人参皂苷的生物活性机制研究提供了重要的分子工具.
[Abstract]:Pyxinolus saponins of the type of 24R- Oxythyleneuron, the chemical name of which is "20Sn 24R" -Epoxy Dama -3 尾 -12 尾 -butadiol, is the main metabolite of 20 ~ (-) -protopaxadiol, and has the activity of resisting myocardial ischemia-reperfusion injuryMIRI. in order to construct the active Pyxinol fluorescent probe, a new fluorescent probe was developed for myocardial ischemia and reperfusion injury in order to construct the active Pyxinol fluorescent probe, which is the main metabolite of 20 ~ (-4) -protopanaxadiol. In order to reduce the steric interference of large fluorescent groups to Pyxinol, the Pyxinol and FITC with different physical characteristics were designed. The synthesized fluorescent probes were carried out by H9C2 cardiomyocytes. The in vitro evaluation of MIRI activity showed that, The fluorescence probe with hydrophilic flexible ethoxy chain retains the anti-#en1# activity of Pyxinol. The first synthesis of the small molecule fluorescence probe provides an important molecular tool for the study of the bioactivity mechanism of Pyxinol and other ginsenosides.
【作者单位】：烟台大学新型制剂与生物技术药物研究山东省高校协同创新中心分子药理和药物评价教育部重点实验室;
【基金】：国家自然科学基金(No.21502164) 山东省优秀中青年科学家科研奖励基金(No.BS2015YY039) 烟台大学博士科研基金(No.YX14B17)资助项目~~
【分类号】：O657.3;R914;R96

【相似文献】