天然甜味抑制衍生物分子改性和构效关系的研究

探索具有超高强度甜味抑制作用的新型食品添加剂，对改善高能食品、运动食品、传统高糖食品的食用品质，具有重要的社会效益和经济价值。本项目的核心是如何通过分子结构改性等方法，使天然母分子向甜味抑制强度更高、综合特性更优的衍生物转变。以天然存在的2-（4-甲氧基苯氧基）丙酸为母分子，通过羧基酯化、在苯环上选择性引入羟基、烷基、烷氧基、卤取代衍生以及旋光活性拆分等方法，分析其对衍生物甜味抑制强度大小、是否影响其他风味、是否带有苦涩异味等特性的影响和影响规律，研究影响衍生物甜味抑制作用强度大小的结构特点和结构优先性，建立系统的2-（4-甲氧基苯氧基）丙酸衍生物的甜味抑制机理和构效关系理论，并进行实验表征。在试验中，将发现一些全新的具有超高强度甜味抑制作用的新型衍生物，筛选1~2种进行毒理学评价，作为潜在的新型食品添加剂加以开发。本研究工作量大，难度大，意义重大。

Exploring new food additives with high-potency sweetness inhibition has important economic value and social benefits for improving the edible quality of high-energy food, sports food and traditional high-sugar food. The core of this project is to explore how to convert natural parent molecule into its derivatives with stronger inhibitory effect on sweetness and better overall characteristics by esterification of a carboxyl group, selective introduction of hydroxyl, alkoxy and halogen atoms on benzene rings, and optical active resolution. The effects of 2-(4-methoxyphenoxy) propionic acid derivatives on sweetness inhibition, other flavors, bitterness and astringency are analyzed, and the structural characteristics and the structural priority affecting sweetness inhibition are investigated. The sweetness inhibition mechanism and the structure-activity relationship of 2-(4-methoxyphenoxy) propionic acid derivatives can be systematically established and experimentally characterized. Some new high-potency sweetness inhibitors will be discovered from this research, one or two of which will be chosen to conduct toxicological experiments and developed as potential food additives. This research has heavy workload and great difficulty but with remarkable significance.