个人信息Personal Information
副教授
硕士生导师
性别:男
毕业院校:中科院大连化学物理研究所
学位:博士
所在单位:化工学院
学科:药物化学. 药物工程
办公地点:大连理工大学西部校区
联系方式:Office telephone:84986200
电子邮箱:wangss@dlut.edu.cn
齐墩果酸的结构修饰和α-葡萄糖苷酶抑制活性
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论文类型:期刊论文
发表时间:2022-06-26
发表刊物:高等学校化学学报
卷号:33
期号:4
页面范围:744-749
ISSN号:0251-0790
摘要:The natural pentacyclic triterpene compound, oleanolic acid, has a series of biological activities, such as antitumor, anti-HIV, hypoglycemic and liver protective activities, but its relatively weak activities and low bioavailability limit its clinical applications. In order to investigate the hypoglycemic activity of oleanolic acid derivaties, sixteen derivatives were synthesized by modification of oleanolic acid at C2, C3 and C28 positions via oxidation, esterification, cyclization, Mannich reaction and so on. Their structures were determined by physicochemical properties, MS and NMR data. Their in vitro inhibitory activities against alpha-glucosidase were tested. The results show that all the tested compounds exhibit alpha-glucosidase inhibitory activities in various degrees at the concentration of 200 mu g/mL. Among then, 3-oxo and 29-ester derivatives (2, 5-7) show lower inhibitory activity than oleanolic acid. The preliminary analysis of structure-activity relationship revealed that the free carboxyl group at C28 was indispensable and hydroxyl or other hydrogen-based donor groups at C3 contributed to increase inhibitory activity.
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