PRECLINICAL STUDY OF EUCALYMINUM – DRUG OF ANTIMICROBIAL ACTION

Presents Рurpose. Еxperimental study of antimicrobial properties of eucalimin, obtained from medicinal plants and preclinical assessment of its security. Methods. Eucalyptus leaves and shoots are obtained from eucalyptus (Eucalyptus viminalis Labill).) family (Myrtaceae). Substance eucalimin is a standardized purified amount of terpenoid fenolaldegidov phloroglucinol number (euglobals) and triterpenoids. The antimicrobial spectrum of the substance of eucalamin was studied in experiments in vitro by the method of double serial dilutions in liquid nutrient media corresponding to each micro-organism. The study of the potential development of resistance of microorganisms to eucalimin was carried out by the method of continuous action and by the method of serial passages using laboratory and clinical strains of Staphylococcus aureus. The chemotherapeutic efficacy of the finished dosage forms of eucalimin (1% alcohol solution, suppositories 0.05 g and 0.03 g) was studied in experiments in vivo on experimental models of localized infectious process of white rats caused by Staphylococcus aureus (infected wound, purulent ulcer and staphylococcal vaginitis). Preclinical study of the safety evkalimina conducted at single and long-term administration of laboratory animals. Cumulative properties evkalimina was studied by Lima. General toxic effect eucalimin was studied at 30 and 90 day introduction into the stomach of rats-males in doses of 5, 50, 250 and 500 mg/kg was determined hematological and biochemical parameters, enzyme activity of blood serum. Allergizing, immunomodulatory, embryotoxic and teratogenic, mutagenic properties were studied. Results. The results of experimental studies indicate that eucalimin has a broad spectrum of antimicrobial activity, including against clinical strains of antibiotic-resistant Staphylococcus genus, Streptococcus, spore-forming bacteria, causative agents of diphtheria and tuberculosis. In animal experiments on various models of localized infectious process, high chemotherapeutic efficacy of eucalimin in two dosage forms (1% alcohol solution and suppositories) was established. Preclinical toxicological study suggests that eucalimin low toxicity at single and long-term administration in laboratory animals and is well tolerated. The drug has no cumulative, embryotoxic, teratogenic, mutagenic, allergenic and irritant properties. Eucalimin in doses of 5-250 mg/kg stimulated the formation of antibodies to thymusdependent antigen. Eucalimin increased nonspecific resistance of rats, increasing 2 times opsono-phagocytic index. Conclusions. In vitro experiments revealed a high antimicrobial activity of eucalamine against a wide range of pathogenic microorganisms, the absence of the potential for the development of resistance of Staphylococcus strains to the drug. In experiments in vivo on different experimental models of localized infections found expressed chemotherapeutic action of dosage forms eucalimin. Eucalimin showed no systemic toxicity, allergenicity, mutagenicity, embryotoxicity, teratogenicity. Stimulated humoral immunity.