Исследование антиэкссудативной активности производных эризимина и цимарина

Abstract

Comparative investigation of antiexudative activity-chemical structure dependence in a series of erysimine and cymarine derivatives was conducted on the model of carrageenan edema in white Wistar rats. The test substances were administered intragastrically at a dose of 5.0 mg/kg 30 minutes before introduction of the phlogogenic agent. Edema was caused by injection of 0.1 ml of 1% aqueous suspension of carrageenan. Antiexudative activity was determined by the degree of edema reduction in experimental animals as compared to control ones and expressed as a percentage. Diclofenac sodium was used as a comparative drug. The highest antiexudative activity among the erysimine derivatives was shown by 3’,4’-О-propylidene-erysimine that reduced the carrageenan edema by 39.4% (p < 0.05) and provided an anti-inflammatory effect comparable with the effect of diclofenac sodium. Replacing ethyl radical with propyl, phenyl, methyl, phenylpropenoic and 3-methoxy-4-hydroxyphenyl radicals decreased the antiexudative activity from 39.4 % to 13.5 %. Derivatives of cymarine have a less pronounced antiexudative activity: ethanoliminocymarine reduced the volume of edema in rats by 29.9% (p < 0.05). Replacing ethanol with pyridine-para-methylene and urea reduced the antiexudative activity from 29.9% to 9.0%. Erysimine and cymarine derivatives are a promising group of organic compounds for further synthesis and pharmacological screening to be used as a basis for development of medicines with antiexudative activity.