橙皮苷和橙皮素衍生物的合成及生物活性研究进展  

Research Progress of Synthesis and Biological Activity of Hesperidin and Hesperitin Derivatives

作　　者：黄爱玲 张义龙[1] 黄成[1] 李俊[1] HUANG Ailing;ZHANG Yilong;HUANG Cheng;LI Jun(School of Pharmacy,Anhui Medical University,Anhui Province Key Laboratory of Major Autoimmune Disease;Anhui Institute of Innovative Drugs,Hefei 230032,China)

机构地区：[1]安徽医科大学药学院,重大自身免疫性疾病安徽省重点实验室,安徽省创新药物产业共性技术研究院,安徽合肥230032

出　　处：《药学进展》2018年第7期527-536,共10页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.81473268);安徽省高校自然科学研究项目(No.KJ2016A364)

摘　　要：橙皮苷和橙皮素主要存在于芸香科柑橘属植物果实中,属于二氢黄酮类化合物,已证实橙皮苷具有多种生物活性,日益引起重视。橙皮苷生物活性确切、药理作用广泛,在医药学上有广泛的用途,因此具有广阔的开发和利用前景,但由于橙皮苷溶解度低而影响其吸收,生物利用度低,橙皮素在体内易代谢,难以维持血药浓度,因而对两者的化学修饰成为新药设计和开发的热点。为了更好地开发、利用橙皮苷和橙皮素,结合国内外研究现状,总结前人研究成果和探寻知识空白,综述橙皮素及橙皮苷衍生物的最新合成情况及其生物活性研究进展,以期为橙皮苷和橙皮素的结构改造与创新药物研究提供参考。Hesperidin and hesperitin are mainly found in citrus fruits of Rutaceae and belong to dihydroflavones. A variety of biological activities of hesperidin have been approved, drawing increasing scientific attention. With established biological activities and a wide range of pharmacological effects, hesperidin has been widely used in medicine and shows broad prospects for development and utilization. However, the bioavailability of hesperidin is low due to its poor solubility and absorption. Moreover, hesperitin is easy to be metabolized, so it＇s hard to maintain a high blood concentration.Therefore, the chemical modification of hesperidin and hesperitin becomes a hot spot of new drug design and development. In order to optimize the development and utilization of hesperidin and hesperitin, previous researches were summarized and knowledge gaps were explored based on studies at home and abroad, the latest progress in the synthesis of hesperitin and hesperidin derivatives and their pharmacological activities were also reviewed, so as to provide reference for structural modification and innovative drug research of hesperidin and hesperetin.

关 键 词：橙皮苷 橙皮素 新药设计 药物合成 

分 类 号：R914.5[医药卫生—药物化学]