20(S)-原人参二醇的荧光示踪及体内活性探析  

Introduction of Fluorescence Tracer and Activity Verification of 20(S)-PPD

作　　者：单艳玲 赵丹丹[1] 吴宿慧[1] 李寒冰[1] 尹光明 李根林[1] SHAN Yanling;ZHAO Dandan;WU Suhui;LI Hanbing;YIN Guangming;LI Genlin(Henan University of Chinese Medicine,Zhengzhou 450046,Henan,China)

机构地区：[1]河南中医药大学,河南郑州450046

出　　处：《中华中医药学刊》2022年第12期186-190,I0058,I0059,共7页Chinese Archives of Traditional Chinese Medicine

基　　金：国家自然科学基金(81503363);河南省中医药科学研究专项(20-21ZY1038)。

摘　　要：目的旨在明确二醇型人参皂苷在肠道菌群作用下的代谢产物20(S)-原人参二醇[20(S)-PPD]是否具有基本的生物活性,为后续研究提供基础数据。方法选择萘酰亚胺作为初级荧光基团,设计荧光探针N-丁基-4-溴-1,8-萘酰亚胺的合成路线,将该荧光探针接入到20(S)-PPD中,制备得到N-丁基-4-溴-1,8-萘酰亚胺标记的20(S)-PPD;然后将其与大肠杆菌混匀作为食物喂给模式生物秀丽隐杆线虫,借助荧光显微技术察线虫的游泳能力及虫体内的荧光强度,检测其在线虫体内的分布及药物活性。结果与空白组相比,PPD给药组线虫体内的荧光强度和分布差异有统计学意义(P=0.036),并随剂量的增加而增强;且给药后的线虫1min内身体摆动次数明显增多,存在显著统计学意义(P<0.01)与显著差异(P<0.05)。结论该20(S)-PPD荧光探针在线虫体内跨细胞膜转运且增强线虫的运动能力,为20(S)-原人参二醇在体内的活性研究与检测提供技术支持。Objective 20(S)-protopanaxadiol[20(S)-PPD]is a metabolite of protopanaxodiol-type ginsenoside under the action of intestinal flora.20(S)-PPD has strong anticancer activity,but its metabolism in vivo is less studied.The study aims to clarify whether 20(S)-PPD has basic biological activity,and provide basic data for further research.Method The synthetic route of the fluorescent probe N-butyl-4-bromo-1,8-naphthalimide was designed by selecting naphthalimide as the primary fluorescent group,and then the fluorescent probe was connected to 20(S)-PPD and 20(S)-PPD labeled with N-butyl-4-bromo-1,8-naphthalimide was prepared.The 20(S)-PPD fluorescent probe was mixed with E.coli as food and fed to the C.elegans,the swimming ability and fluorescence intensity of C.elegans were observed and analyzed by a fluorescence microscope to detect the distribution and pharmaceutical activity of C.elegans in vivo.Result The fluorescence intensity and the number of body swings in one minute of C.elegans treated with 20(S)-PPD fluorescent probe was significantly increased,which showed extremely significant differences compared with that of the control.Conclusion It indicated that the synthesized compound II can transport across the cell membrane in the C.elegans and enhance the motility of the C.elegans,providing technical support for the metabolism and detection of 20(S)-protopanaxadiol in vivo.

关 键 词：20(S)-原人参二醇 化学合成 荧光基团 跨膜转运 

分 类 号：R282.71[医药卫生—中药学]