儿茶素及其衍生物合成研究进展  

Progress in the Synthesis of Catechin and Its Derivatives

作　　者：陆昌琪[1] 毛世红[1] 童华荣[1] 丁阳平[1] LU Changqi;MAO Shihong;TONG Huarong;DING Yangping(College of Food Science,Southwest University,Chongqing 400715,China)

机构地区：[1]西南大学食品科学学院,重庆400715

出　　处：《食品科学》2018年第11期316-326,共11页Food Science

基　　金：重庆市自然科学基金项目(cstc2014jcyj A80024);中央高校基本科研业务费专项资金项目(XDJK2014C159);西南大学博士基金项目(SWU111040);重庆市特色食品工程技术研究中心能力提升项目(cstc2014pt-gc8001)

摘　　要：儿茶素具有抗肿瘤、抗氧化、抗病菌以及保护心脑器官等多种药理作用,这些药理活性主要由其多羟基结构决定,然而,多羟基结构也使儿茶素在中性和碱性条件下结构不稳定。儿茶素被人体摄入后会很快在生物酶作用下发生甲基化或糖苷化,研究发现,在儿茶素结构中引入其他基团可有效提高其稳定性和生物利用率,并特异性增强儿茶素药理作用。其中,甲基儿茶素抗过敏和逆转肿瘤细胞耐药性表现突出,糖苷儿茶素水溶性显著提高并可有效防止褐变,而酰化儿茶素由于脂溶性明显增强,其抗氧化和抗癌活性也随之明显增强。在不同位置进行取代达到的效果也不相同,通过研究儿茶素及其不同衍生物的合成途径和药理作用,将有助于进一步研究发现儿茶素新的药理功能并加快促进儿茶素药物的临床应用,本文详细介绍了儿茶素生物合成和化学合成途径,重点综述儿茶素不同衍生物的合成途径并简单说明其药理作用。Catechins not only have antitumor, antioxidant, antibacterial and antiviral functions, but also can protect the heart and brain and execute other pharmacological effects. These pharmacological effects are principally dependent on the polyhydroxyl structure of catechins, which, however, makes catechins unstable under neutral and alkaline conditions. Catechins are rapidly methylated or glycosylated by enzymes when ingested into the human body. Researchers have found that introducing new chemical groups into the structure of catechins can significantly improve their stability and bioavailability and specifically enhance their pharmacological effects. Notably, methylated catechins can suppress allergic reaction and tumor cell resistance; glycosylation can increase the water solubility of catechins and effectively prevent browning, while acylated catechins show significantly improved antioxidant and antitumor activity due to their high fat solubility. Moreover, the effects of substitution at different locations are different. Studying the synthesis routes and pharmacological effects of catechin derivatives will help discover new pharmacological effects of catechins and promote the clinical application of catechins. The aim of this article is to outline the the biosynthesis and chemical synthesis pathways of catechins with focus on the synthesis pathways and pharmacological effects of catechin derivatives.

关 键 词：生物合成 化学合成 结构修饰 药理作用 研究展望 

分 类 号：O629.9[理学—有机化学]