张光辉，张拴，龙旭，郭惠，孟庆华，左振宇

（陕西中医药大学 药学院, 陕西 咸阳 712046）

异甘草素合成工艺优化及其清除自由基活性研究

张光辉，张拴＊，龙旭，郭惠，孟庆华，左振宇

（陕西中医药大学 药学院, 陕西 咸阳 712046）

对异甘草素的合成工艺进行优化和体外清除自由基活性进行研究。通过间苯二酚、冰醋酸、对羟基苯甲酸合成异甘草素，考察物料比、温度、反应时间对产率的影响，通过紫外分光度法对其清除自由基活性进行研究。酚与酸物料比1∶2.5，240 W微波辐射3 min，2,4-二羟基苯乙酮产率最高为65.75%；当醛酮物质的量比为3∶1，温度控制在120～130 ℃，回流6 h，异甘草素产率最高为28.10%；反应时间控制20 min，异甘草素加入量为1.00 mL清除DPPH自由基能力最强，为66.4%。异甘草素具有一定的抗自由基活性。

异甘草素；合成；抗自由基

Abstract:The synthesis process of isoliquiritigenin was optimized and its activity of scavenging free radicals in vitro was studied. Firstly, isoliquiritigenin was prepared from resorcinol, acetic acid and p-hydroxybenzoic acid. The influence of molar ratio of reactants, reaction temperature and reaction time on the yield of isoliquiritigenin product was investigated. The results showed that, when the molar ratio of resorcinol and acetic acid was 1:2.5, microwave radiation was 240 W for 3 min, the product yield of 2, 4-dihydroxyacetophenone reached the maximum value, 65.75%;When the molar ratio of aldehyde and ketone was 3:1, the temperature was about 120～ 130 ºC with reflux time of 6 h,the yield of isoliquiritigenin product was as high as 28.10%. Then, the activity of scavenging DPPH free radicals was the highest, about 66.4 when 1.00 mL isoliquiritigenin was added to the solution with the reaction time of about 20 min.The results indicated that isoliquiritigenin has good anti-free radicals ability.

Key words:Isoliquiritigenin; Synthesis; Anti-free radicals

甘草为豆科植物甘草，胀果甘草和光果甘草的根及根茎[1]，又名拉乌尔草，早在《神农本草经》上就列为上品中药，其性味甘平，传统中医药认为它具有补脾益气、清热解毒、通淋利尿、祛痰止咳、缓急止痛、调和诸药的功效等作用，在我国主要分布于新疆、甘肃、西藏等地区。异甘草素是甘草中黄酮中的主要成份之一，结构如图1示，属于二氢黄酮类化合物，分子式为C15H12O4，熔点198～200℃，黄色针状结晶[2]。异甘草素有抗溃疡、抗炎[3]、解痉、抗菌、抗肿瘤[4]、美白、抗氧化[5]、预防动脉粥样硬化、保护肝脏[6]等广泛的药理作用，但是甘草中的异甘草素的含量低，价格昂贵，提取过程繁琐，限制了它的应用。

为此，本实验拟对化学方法合成异甘草素条件进行优化，并对其体外清除自由基活性进行研究，旨在为进一步开发利用异甘草素提供实验基础。……