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The analysis presented in this article is a continuation of a broader qualitative study examining the composition of the chloroform fraction of Caltha palustris. The study discovered 29 compounds, and 26 of them have been identified:paraffinic hydrocarbons, esters, fatty aldehydes, morphine derivatives, thiazole derivatives, benzodiazepines, naphthalene, and a small amount of terpene. It was figured out that the investigated lipophilic extract has an antioxidant impact. For the investigation, there were used such assays as the DPPH radical and the ABTS radical cation assays. Moreover the investigated lipophilic extract has an antimicrobial activity both in terms of gram-positive (Staphylococcus aureus (ATCC 25923 (F-49)), Bacillus cereus 34 (non-MDR), Enterococcus faecalis 26(MDR) and gram-negative, (Raoultella terrigena (ATCC 33257), Escherichia coli (ATCC 25922), Escherichia coli 168) microorganisms and yeast Candida spp. In addition, the significant content of biologically active substances in the lipophilic volatile fraction of Caltha palustris indicates the prospects for further study. © 2023, Research Journal of Pharmacy and Technology. All rights reserved.

Author keywords

Antimicrobial activity; Antioxidant effect; Caltha palustris; Gas chromatography; Lipophilic extract; Сhloroform fraction

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

UDC 547.551.552

New S-(ω-fluoralkyl) 4-amino- and 4-acetamidobenzenesulfonothioates were synthesized by the reaction of sodium salts of the substituted thiosulfonic acids and correspondingω-fluoralkylbromides. The study of their antimicrobial activity against thirteen referenceand clinical bacterial and fungal strains using agar diffusion method was conducted. All compounds showed significant antimicrobial activity, two of them showed higher activity against Candida albicans than known antifungal compound of sulfonothioate class, S-ethyl ester of 4-aminobenzenethiosulfonic acid.

Abstract

In the literature, the chemical composition of Rhododendron tomentosum is mainly represented by the study of isoprenoid compounds of essential oil. In contrast, the study of the content of flavonoids will contribute to the expansion of pharmacological action and the use of the medicinal plant for medical purposes. The paper deals with the technology of extracts from Rh. tomentosum shoots using ethanol of various concentrations and purified water as an extractant. Extracts from Rh. tomentosum were obtained by a modified method that combined the effects of ultrasound and temperature to maximize the extraction of biologically active substances from the raw material. Using the method of high-performance thin-layer chromatography in a system with solvents ethyl acetate/formic acid/water (15:1:1), the following substances have been separated and identified in all the extracts obtained: rutin, hyperoside, quercetin, and chlorogenic acid. The total polyphenol content (TPC) and total flavonoid content (TFC) were estimated using spectrophotometric methods involving the Folin-Ciocalteu (F-C) reagent and the complexation reaction with aluminum chloride, respectively. A correlation analysis was conducted between antioxidant activity and the polyphenolic substance content. Following the DPPH assay, regression analysis shows that phenolic compounds contribute to about 80% (r2 = 0.8028, p < 0.05) of radical scavenging properties in the extract of Rh. tomentosum. The extract of Rh. tomentosum obtained by ethanol 30% inhibits the growth of test cultures of microorganisms in 1:1 and 1:2 dilutions of the clinical strains #211 Staphylococcus aureus and #222 Enterococcus spp. and the reference strain Pseudomonas aeruginosa ATCC 10145. © 2024 by the authors.

Author keywords

aluminum chloride; antimicrobial activity; antioxidant activity; chlorogenic acid; DPPH assay; Folin-Ciocalteu reagent; HPTL; hyperoside; Ledum palustre; quercetin; Rhododendron tomentosum; rutin; UV–Vis

УДК 615.276:547.789:542.91

The aim of the work.To predict the mechanisms of antiсancer activity using modern web tools for the compound Les-6489.

Materials and Methods. Molecular docking of EGFR and HER2 tyrosine kinases was performed for compound Les-6489. To evaluate the stability of complexes with Les-6489, molecular dynamics (MD) simulations were performed using GROMACS 13, which is accessed through the SiBioLead server.

Results and Discussion. As a result of in silico studies, a mechanism of antitumor activity was predicted for the studied compound Les-6489, which is implemented by inhibiting EGFR and HER2 tyrosine kinases.

Conclusions.The obtained results may become a platform for further structural optimization of the identified thiazole-isoindole hybrid molecule in the development of modern anticancer agents