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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 evaluate the anti-inflammatory activity and sodium-retention effect of the synthesized glycyrrhetic acid derivatives. Methods Acute and chronic inflammation models were constructed to evaluate the anti-inflammatory activity and sodium-retention effect of the synthesized 6 glycyrrhetic acid derivatives. Results Deoxy glycyrrhetinic acid, methyl glyoxylic acid methyl ester, glycyrrhetinic acid methyl ester -3-O-acetate and glycyrrhetinic acid methyl ester showed better acute inflammatory antagonistic activity. Glycyrrhetinic acid ethyl ester-3 -O-acetate and glycyrrhetinic acid also have some activity. Deoxy glycyrrhetinic acid, deoxy glycyrrhetinic acid methyl ester, glycyrrhetinic acid methyl ester -3-O-acetate and glycyrrhetinic acid methyl ester of cotton ball granuloma model rats 24h urinary output, urinary potassium content, serum Sodium ion content and potassium ion content were not significantly affected. Conclusions Deoxy glycyrrhetinic acid, methyl glyoxylic acid methyl ester, glycyrrhetinic acid methyl ester -3-O-acetate and glycyrrhetinic acid methyl ester have obvious antagonistic effects on acute inflammation (exudative reaction mainly) Ethyl acetate -3-O-acetate and glycyrrhetinic acid also have some inhibition of acute inflammation. The four derivatives with significant acute inflammation antagonism did not show significant sodium and water retention.