UDC 615.322:615.451.1

Actuality. The widespread use of herbal drugs with anti-inflammatory and nephroprotective properties stimulates the search for new active biological substances. Of particular interest are plants from the Ranunculaceae family, especially Anemone nemorosa, which contains a range of potentially bioactive components such as anemonin, protoanemonin, and others. Understanding the acute toxicity, anti-inflammatory, and hypoazotemic activity of Anemone nemorosa extracts opens possibilities for the development of new therapeutic agents based on this plant. Materials and methods. Ethanol extracts were obtained from the aerial parts of Anemone nemorosa harvested during the flowering period. The study included the examination of oral acute toxicity conducted on Wistar rats over 14 days, anti-inflammatory activity using the carrageenan-induced paw edema method in Wistar rats, and hypoazotemic activity on models of healthy and acute renal failure in Wistar rats. Results. The extracts showed no acute toxicity at the administered dose. It was established that the oral administration of the extracts is non-toxic up to a dose of 200 mg/kg body weight. The anti-inflammatory tests did not reveal significant therapeutic effects. However, the hypoazotemic tests demonstrated a reduction in blood urea and creatinine levels, and an increase in these indicators in urine, especially under conditions of acute renal failure, indicating a strong diuretic effect of the extracts. Conclusions. The Anemone nemorosa extracts exhibited strong hypoazotemic and diuretic activity, which may be beneficial for the treatment of kidney diseases. The absence of anti-inflammatory activity requires further analysis and possible modification of extraction methods. The study results support the potential use of this plant in developing new nephroprotective phytopreparations. © O. Khropot, Yu. Konechnyi, G. Lavryk, I. Tymchuk, O. Pinyazhko, V. Lubenets, R. Konechna.

Author keywords

Acute toxicity; Anemone nemorosa; Anti-inflammatory activity; Extracts; Hypoazotemic activity; Ranunculacea

New 4-aryl-3-(morpholin-4-yl)-2-arylimino-2,3-dihydrothiazole derivatives 1.1-1.16 were obtained using the Hantzsch reaction by condensation of N-(morpholin-4-yl)-N'-arylthioureas with the corresponding α bromoacetophenones in alcohols. Synthesized hydrobromides 1.1-1.8 were formed as crystalline precipitates during the boiling of the reaction mixture. Bases 1.9-1.16 were obtained by neutralizing the corresponding hydrobromides with NH4OH solution. It has been proposed a possible mechanism of the reaction that is based on the study of the structure of the synthesized compounds. The structures of the synthesized compounds were confirmed by 1H NMR spectroscopy with its special techniques (NOESY and ROESY experiments). It has been shown the formation of the isomer 4-(4'-chlorophenyl)-3-(morpholin-4-yl)-2-(4'-chlorophenylamino)-2.3-dihydrothiazole on the basis of compound 1.14. Pharmacological screening of synthesized derivatives of 4-aryl-2-arylimino-2,3-dihydrothiazole compounds revealed the analgesic effect in the model of visceral pain caused by the introduction of acetic acid to white mice. The anti-inflammatory effect of the synthesized compounds was evaluated in vivo by reducing limb edema in rats with carrageenan-induced inflammation. Thus, the synthesized compounds have analgesic and anti-inflammatory activity.