甘草次酸衍生物的抗炎活性及水钠潴留作用的研究

Study on the anti-inflammatory activity and water-sodium retention effect of different glycyrrhetic acid derivatives

目的对合成的系列甘草次酸衍生物进行抗炎活性,水钠潴留作用的评价。方法构建了急性及慢性炎症模型,评价合成的6个甘草次酸衍生物的抗炎活性及水钠潴留作用。结果脱氧甘草次酸、脱氧甘草次酸甲酯、甘草次酸甲酯-3-O-乙酸酯及甘草次酸甲酯均表现出较好的急性炎症拮抗活性,甘草次酸乙酯-3-O-乙酸酯及甘草次酸也具有一定的活性。脱氧甘草次酸、脱氧甘草次酸甲酯、甘草次酸甲酯-3-O-乙酸酯及甘草次酸甲酯对棉球肉芽肿模型大鼠24 h尿量、尿钾离子含量、血清钠离子含量和钾离子含量均未见明显影响。结论脱氧甘草次酸、脱氧甘草次酸甲酯、甘草次酸甲酯-3-O-乙酸酯及甘草次酸甲酯对急性炎症(渗出反应为主)有明显的拮抗作用,甘草次酸乙酯-3-O-乙酸酯及甘草次酸对急性炎症也有一定抑制作用。4种具有显著急性炎症拮抗作用的衍生物未表现出明显水钠潴留作用。

OBJECTIVE To make evaluation of anti-inflammatory activity and water-sodium retention effects of the six synthetic glycyrrhetinic acid derivatives.METHODS The anti-inflammatory activity and water-sodium retention effects of the derivatives were evaluated on acute and chronic inflammation models.RESULTS Oxygen glycyrrhetinic acid,deoxy glycyrrhetinic acid methyl ester,glycyrrhetinic acid methyl ester-3-O-acetate and glycyrrhetinic acid methyl ester showed acute inflammation antagonistic activity,in addition glycyrrhetinic acid ethyl ester-3-O-acetate and glycyrrhetinic acid also have a certain activity.Deoxy glycyrrhetinic acid,deoxy glycyrrhetinic acid methyl ester,the glycyrrhetinic Methyl-3-O-acetate,and glycyrrhetinic acid methyl ester had no obvious effect on 24 hour urine output,urine potassium content,serum sodium levels or potassium levels of rats with granuloma model.CONCLUSION The deoxy glycyrrhetinic acid,deoxy licorice acid methyl ester,glycyrrhetinic methyl-3-O-acetate and glycyrrhetinic acid methyl ester had significant antagonism on acute inflammation（exudative reaction-based）,licorice sub-ethyl-3-O-acetate and glycyrrhetinic acid also have some inhibition effect on acute inflammation.The four derivatives which have significant antagonism of the acute inflammatory didn′t show obvious water-sodium retention effect.