灯盏花乙素苷元结构修饰的研究进展  

Research Progress on Structural Modification of Scutellarin

作　　者：韩官甫 李润涛[3] 张伟 HAN Guanfu;LI Runtao;ZHANG Wei(School of Pharmaceutical Science&Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming Medical University,Kunming 650500,China;Kunming Longjin Pharmaceutical CO.,LTD,Kunming 650503,China;Beijing Peking University school of pharmaceutical sciences,Beijing 100191,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 [2]昆明龙津药业股份有限公司,云南昆明650503 [3]北京大学药学院,北京100191

出　　处：《中国民族民间医药》2020年第14期60-63,共4页Chinese Journal of Ethnomedicine and Ethnopharmacy

摘　　要：灯盏花乙素是从灯盏细辛中提取的有药理活性的化合物,目前主要用于治疗缺血性心脑血管疾病。灯盏花乙素苷元是灯盏花乙素在人体内的主要吸收形式,但是灯盏花乙素苷元存在溶解度和稳定性差,生物利用度低、脑分布低、活性弱等缺陷。基于已有的灯盏花乙素苷元的构效关系发现,灯盏花乙素苷元A环的6、7、8位和B环的4’位对活性影响较小。对灯盏花乙素苷元在A环和B环上的结构优化进行总结,为进一步开发以灯盏花乙素苷元为先导化合物的新药提供参考。Scutellarin,which is extracted from Erigeron breviscapine,is a definitely pharmacologically active nature product.It is widely used in the treatment of ischemic cardiovascular and cerebrovascular diseases.The scutellarein is the main form of absorption of scutellarin in the human body,however,there are some defects such as poor solubility and stability,low bioavailability,low brain distribution and weak activity.Based on the existing structure-activity relationship of scutellarein,we found that 6,7,8 positions in A ring and 4’ positions in B ring of scutellarein had little effect on activity.In this paper,the structure optimization of scutellarein in A and B rings is summarized,which provides a reference for the further development of new drugs with scutellarein as the leading compound.

关 键 词：灯盏花乙素苷元 溶解度 结构修饰 合成 

分 类 号：R914.5[医药卫生—药物化学]