天然阿洛糖苷的研究进展  

Research progress in natural allopyranosides

作　　者：王莹莹[1,2] 田雷瑜 杨燕 孙稚颖[1] 王伟 

机构地区：[1]山东中医药大学药学院,山东济南250014 [2]中国医学科学院、北京协和医学院药物研究所,天然药物活性物质与功能国家重点实验室,北京100050

出　　处：《药学学报》2017年第3期378-389,共12页Acta Pharmaceutica Sinica

基　　金：中国医学科学院医学与健康科技创新工程项目(2016-I2M-3-012);北京协和医学院“协和青年基金”项目(3332016057)

摘　　要：天然糖苷类化合物的药理活性与不同糖基之间有着密切的关系,通过糖基化可以改变整个糖苷分子的构象,提高其水溶性,增强其生物活性,甚至改变其药代特性和药理作用机制等。与生物体内常见的D-葡萄糖相比,D-阿洛糖是D-葡萄糖的C-3差向异构体,单糖本身就是一种低能量、不被消化的安全无毒的食糖替代品,已在膳食、保健、医药等领域发挥着重要的生理功能。但自然界中D-阿洛糖绝大部分以稀有的糖苷形式存在,与常见的糖苷如葡萄糖苷、鼠李糖苷等一样,也具有广泛的生物活性。本文主要简述从植物中分离鉴定的不同类型的阿洛糖苷类化合物,还基于文献对其抗肿瘤、抗糖尿病等多种药理活性及其不同糖基取代的构效关系进行综合分析,为基于糖苷类化合物的新药发现和药物设计提供研究思路。The pharmacological activities of natural glycosides are closely related to the polyfunctional sugar moieties. Modification of active natural products by glycosylation can change the stereochemical configuration, improve the solubility, tune up the activities and change pharmacokinetic properties for higher efficacy and better selectivity. Compared with the common D-glucose, D-allose, a C-3 epimer of D-glucose rarely exists in nature, but it plays an important role in food, health, medicine, and so on. It is not easily metabolized in the living organisms, but can be used as a safe and low-calorie sweetener. The natural allopyranosides are absolute conjugation forms which are same as other glucopyranosides and rhamnopyranosides with a broad array of biological activities. This article summarizes the major progresses made in phytochemistry and biological activity studies of these compounds. Structure-activity relationship analyses of partial anti-tumor and anti-diabetic allopyranosides were performed regarding the data reported in the literatures. These insights may provide a theoretical and experimental reference for the discovery of new drug and drug design based on allopyranosides.

关 键 词：糖苷 黄酮阿洛糖苷 阿洛糖酚苷 甾体阿洛糖苷 葫芦烷型阿洛糖苷 D-阿洛糖 

分 类 号：R931[医药卫生—生药学]