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<p>The anti-inflammatory and antiulcer activity of a number of 3-semi- and -thiosemicarbazones of glycyrrhetic acid and its 11-deoxo analog at a dose of 50 mg/kg were studied in the model of carrageenan-induced edema of mouse paws as compared to voltaren and in indomethacin-induced ulcers of the gastric mucosa of rats as compared to omeprazole and a glycyrrhetic acid derivative, carbenoxolone. It was found that the most active compound of the studied glycyrrhetic acid derivatives <b>V</b>-<b>VIII</b> was the 3-semicarbazone of glycyrrhetic acid butyl ester <b>VI</b> and that loss of the 11-oxo group of glycyrrhetic acid led to a decrease in the anti-inflammatory activity of the compounds. Peroral administration of <b>VI</b> decreased paw edema in mice by 36.3% (<i>p</i> &lt; 0.01) and reduced the number of gastric mucosal ulcers in rats by 54.4% (<i>p</i> &lt; 0.002) as compared to the control. Compound <b>VI</b> exhibited antioxidant activity, increasing the catalase level by 63.3% (<i>p</i> &lt; 0.05) and decreasing the malondialdehyde level by 72.2% (<i>p</i> &lt; 0.0001) in the serum of rats as compared to the control. Thus, the anti-inflammatory activity of compound <b>VI</b> was combined with an anti-ulcer effect analogous to the effects of carbenoxolone and omeprazole, which may have been due to its antioxidant properties. This compound is of interest for further studies as an anti-inflammatory and antiulcer agent.</p>

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Anti-Inflammatory and Antiulcer Activity of 3-Semi- and -Thiosemicarbazones of Glycyrrhetic Acid and its 11-Deoxo Analog

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • E. R. Karimova,
  • R. Yu. Khisamutdinova,
  • S. F. Gabdrakhmanova,
  • L. A. Baltina

摘要

The anti-inflammatory and antiulcer activity of a number of 3-semi- and -thiosemicarbazones of glycyrrhetic acid and its 11-deoxo analog at a dose of 50 mg/kg were studied in the model of carrageenan-induced edema of mouse paws as compared to voltaren and in indomethacin-induced ulcers of the gastric mucosa of rats as compared to omeprazole and a glycyrrhetic acid derivative, carbenoxolone. It was found that the most active compound of the studied glycyrrhetic acid derivatives V-VIII was the 3-semicarbazone of glycyrrhetic acid butyl ester VI and that loss of the 11-oxo group of glycyrrhetic acid led to a decrease in the anti-inflammatory activity of the compounds. Peroral administration of VI decreased paw edema in mice by 36.3% (p < 0.01) and reduced the number of gastric mucosal ulcers in rats by 54.4% (p < 0.002) as compared to the control. Compound VI exhibited antioxidant activity, increasing the catalase level by 63.3% (p < 0.05) and decreasing the malondialdehyde level by 72.2% (p < 0.0001) in the serum of rats as compared to the control. Thus, the anti-inflammatory activity of compound VI was combined with an anti-ulcer effect analogous to the effects of carbenoxolone and omeprazole, which may have been due to its antioxidant properties. This compound is of interest for further studies as an anti-inflammatory and antiulcer agent.