Glycyrrhizic Acid Conjugates with Amino-Acid Alkyl Esters with Anti-Inflammatory and Antiulcer Activity
摘要
The anti-inflammatory and antiulcer activity of several glycyrrhizic acid (GA) conjugates with amino-acid methyl/ethyl esters at a dose of 50 mg/kg was studied in a carrageenan-induced paw edema model in mice as compared with voltaren and in an indomethacin-induced gastric ulcer model in rats as compared with omeprazole. The GA conjugate with L-alanine ethyl ester (V) exerted a pronounced anti-inflammatory effect comparable to voltaren, reducing paw edema by 1.8 times (p < 0.01) as compared with the control group and by 1.5 times (p < 0.01) as compared with GA. The highest antiulcer activity, comparable to that of omeprazole, was demonstrated by the GA conjugate containing three residues of L-methionine methyl ester III and the GA conjugate with two residues of aminoenanthic acid methyl ester VII, reducing the number of ulcers as compared to the control by 3.9 times (p < 0.001) and 3.7 times (p < 00.001), respectively. These conjugates reduced the number of ulcers by an average of 3.1 times (p < 0.01) as compared to starting GA.