摘要
天然产物由于其化学结构的丰富多样性及其独特的药理活性,倍受全球生物制药研发人员的关注。然而,天然产物大多存在溶解性差、生物利用度低等缺点。研究表明,糖类结构在细胞表面有许多结合位点,具有较好的细胞靶向性,且具有良好的水溶性,是先导药物的良好载体。对天然产物进行糖基修饰可有效改善先导药物的生物利用度低、溶解性差、药理活性差等问题。本文简要综述了近年来以糖类为主要糖基修饰的供体及在天然产物改造中的应用,以期为相关药物开发提供参考。
Due to the rich diversity of chemical structures and unique pharmacological activities,natural products have attracted much attention from researchers of biopharmaceutical research and development all over the world.However,most of the natural products have disadvantages such as poor solubility and low bioavailability.Studies have shown that the carbohydrate structure has many binding sites on the cell surface,good cell targeting ability,and good water solubility,which is a good carrier of lead drugs.Glycosylated modification of natural products can effectively improve the problems of lead drugs such as low bioavailability,poor solubility and poor pharmacological activity.In this paper,we briefly reviewed the application of saccharide as the main saccharide donor in the modification of natural products in recent years,to provide reference for the development of related drugs.
作者
兰青
孙成新
王先恒
彭君轲
何芋岐
王玉和
赵长阔
LAN Qing;SUN Cheng-xin;WANG Xian-heng;PENG Jun-ke;HE Yu-qi;WANG Yu-he;ZHAO Chang-kuo(Key Laboratory of Basic Pharmacology of Ministry of Education/Joint International Research Laboratory of Ethnomedicine of Ministry of Education,Zunyi Medical University,Zunyi 563099,China;School of Pharmacy,Zunyi Medical University,Zunyi 563099,China;Pharmacy Department,The Affiliated Hospital of Zunyi Medical University,Zunyi 563000,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2022年第16期1595-1601,共7页
Chinese Journal of New Drugs
基金
贵州省优秀青年科技人才项目(黔科合平台人才[2019]5657)
贵州省中医药管理局重点项目(QZYY-2021-086)
贵州省科技支撑项目(黔科合支撑2019[2829])
遵义医科大学校招标课题资助项目([2013]F-680)
遵义市校联合基金资助项目(CK-1187-041)。
关键词
糖基化修饰
天然产物
活性
应用
glycosylation
natural product
activity
application
