目的研究甘草次酸3位酯类衍生物的合成及其抗炎活性。方法以甘草次酸为原料,结合甘草次酸的构效关系,采用化学方法合成了氨基酸类化合物或咪唑杂环类化合物与甘草次酸结构单元构筑的Ⅳ-乙酰氨基乙酸甘草次酸酯、Ⅳ-乙酰-DL-α-氨基丙酸甘草次酸酯、Ⅳ-乙酰-DL-蛋氨酸甘草次酸酯、咪唑-4-羧酸-5-甘草次酸酯和咪唑-4-羧酸-5-(11-脱氧甘草次酸)酯等5种甘草次酸3位酯类衍生物,并经IR、^1H NMR、MS等确证其结构。以二甲苯引起的小鼠耳肿胀模型评价其抗炎活性。结果所合成的衍生物对二甲苯致小鼠耳肿胀具有明显的抑制作用。结论甘草次酸3位酯类衍生物具有明显的抗炎活性,抗炎活性接近于氢化可的松,部分化合物的抗炎活性高于氢化可的松。
OBJECTIVE To study the synthesis and anti - inflammatory activities of 3 - esterified derivatives of glycyrrhetinic acid. METHODS On the basis of construction related medical effect of glycyrrhetinic acid ,five new 3 - esterified derivatives of glycyrrhetinic acid were synthesised with glycyrrhetinic acid, amino acid and imidazole heterocyclic compounds. Their structures were all confirmed by IR, ^1HNMR and MS, and their anti - inflammatory activities were also evaluated with the model xylene - induced ear edema in mice. RESULTS The 5 target compounds had the inhibitory effect on xylene - induced ear edema in mice, and some compounds had higher inhibition rates than Hydrocortisone. CONCLUSION All of the 5 target compounds have anti - inflammatory activities, and the anti - inflammatory activities are comparable to Hydrocortisone, and some have higher anti - inflammatory activities than Hydrocortisone.