岩白菜素新颖衍生物合成及其镇咳祛痰活性  

Synthesis of Novel Derivatives of Bergenin and Its Antitussive and Antispasmodic Activity

作　　者：周金娜 张荣平 邹澄 杨为民 何波 陈德云 段文越 ZHOU Jin-Na;ZHANG Rong-ping;ZOU Cheng;YANG Wei-min;HE Bo;CHEN De-yun;DUAN Wen-yue(School of Pharmaceutical Sciences&Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming Medical University,Kunming Yunnan 650500,China)

机构地区：[1]昆明医科大学药学院暨云南省天然药物药理重点实验室,云南昆明650500

出　　处：《昆明医科大学学报》2020年第8期14-17,共4页Journal of Kunming Medical University

基　　金：云南省科技厅-昆明医科大学应用基础研究联合专项重点基金资助项目(2017FE468-001);云南省有毒药用植物研究创新团队基金资助项目(2020HCOO8)。

摘　　要：目的研究岩白菜素衍生物及其镇咳祛痰活性。方法对岩白菜素7位进行结构改造,利用偶氮还原法将岩白菜素偶氮衍生物合成氨基岩白菜素。波谱法进行结构鉴定后,采用氨水引咳法和气管酚红排泌法评价化合物镇咳祛痰活性。结果供试药组镇咳活性显著优于模型组(P<0.01);与岩白菜素组相比,供试药组小鼠3 min内咳嗽次数降低(P<0.01)。同时,供试药组祛痰活性显著优于生理盐水组(P<0.01);与岩白菜素组相比,供试药组小鼠气管酚红排出量同样明显增加(P<0.01)。结论氨基岩白菜素的合成方法简便,且化合物具备镇咳祛痰活性,为岩白菜素的深入研究提供了基础。Objective To study the derivatives of Bergenin and their antitussive and expectorant activities.Methods The bergenin azo derivative was converted to amino bergen by an azo reduction method. After the structure identification by NMR and the antitussive and expectorant activity of the compound was evaluated by ammonia water to induce cough and tracheal phenol red excretion. Results The antitussive activity of the test drug group was significantly better than that of the model group(P < 0.01);Compared with the bergenin group,The number of coughs in the test drug group was reduced within 3 minutes(P < 0.01). The expectorant activity of the test group was significantly better than that of the normal saline group(P < 0.01). Compared with the bergenin group,the tracheal phenol red excretion of the test group was also significantly increased(P < 0.01). Conclusion The synthesis method of the compound is simple, and the compound has the antitussive and expectorant activity.This study provides a foundation for the further study of the compound.

关 键 词：岩白菜素 含氮衍生物 重氮化偶合反应 

分 类 号：R284.3[医药卫生—中药学] R965.1[医药卫生—中医学]