Galium aparine L., family Rubiaceae, is a widely spread species in the Galium genus. The herb of G. aparine is part of folk remedies and dietary supplements. In this study, we analyzed the chemical composition and immunomodulatory activities of G. aparine herb ethanolic extracts obtained from the plant material by maceration with 20%, 60% or 96% ethanol. The contents of hydroxycinnamic acid derivatives, flavonoids and polyphenols were determined spectrophotometrically, with extractives and polysaccharides quantified gravimetrically. The qualitative composition was studied using UHPLC-DAD-MS/MS analysis; isolation not previously described in G. aparine quercetin rhamnoglucoside was carried out through column chromatography, and the immunomodulatory activity of extracts was determined in the reaction of lymphocyte blast transformation. Major constitutes of extracts were iridoids, i.e., monotropein, 10-desacetylasperulosidic acid and asperulosidic acid; p-hydroxybenzoic acid; hydroxycinnamic acid derivatives, i.e., 3-O-caffeoylquinic, 5-O-caffeoylquinic, 3,4-O-dicaffeoylquinic, 3,5-O-dicaffeoylquinic, 4,5-O-dicaffeoylquinic acids and caffeic acid derivatives; flavonoids, i.e., rutin, quercetin 3-O-rhamnoglucoside-7-O-glucoside, and isorhamnetin 3-O-glucorhamnoside. Significantly, quercetin 3-O-rhamnoglucoside-7-O-glucoside was first isolated and identified in Galium species so far investigated. All G. aparine herb ethanolic extracts stimulate the transformational activity of immunocompetent blood cells, with 96% ethanolic extract being the most active. The data obtained necessitate further research into the mechanisms of immunomodulatory activity of extracts from G. aparine herb.

Extracts from aerial parts of G. aparine (cleavers) constitute a herbal remedy with monography in British Herbal Pharmacopeia. On the European market, there are several drugs and food supplements consisting of Galium extracts. In folk medicine, cleavers was used topically in Europe, Asia, and the Americas to treat skin diseases. In several remedies, cleavers is also listed as an immunomodulatory active herb influencing the defense response of the human body. The aim of this study was to investigate the immunostimulatory activity and antioxidant potential in vitro of a raw infusion of cleavers and bioactive fractions. The functional activity of lymphocytes in the reaction of the lymphocyte blast transformation (RLBT) method was used for immunomodulatory activity assays and direct scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), and hydrogen peroxide (H₂O₂) was chosen for the examination of antioxidant activity. It was shown that both the raw extract and fractions show significant immunostimulatory and scavenging activities. The obtained data partially justify the traditional use of cleavers as topical remedy for skin infections and for wounds.

Diabetes mellitus is a global medical and social issue. In the developed countries of the world, from 5 to 12% of the population are diagnosed with diabetes mellitus and, according to WHO prognosis, the level of this disease may increase to 30-35%. Type 2 diabetes is a disease that progresses over time, but the rational and systematic use of hypoglycemic synthetic drugs and phytopreparations can significantly delay the onset of insulin therapy. A promising source of BAS with a hypoglycemic effect is the raw material of plants of the Heather family, namely, bearberry leaves. However, on the Ukrainian market there are no domestic galenic and novo-galenic preparations based on biologically active substances of this raw material, which indicates the prospects for the development of new drugs, including those with hypoglycemic action. The aim. The aim of the study was to study the phytochemical composition and to carry out a screening of the hypoglycemic activity of dry extracts from bearberry leaves modified with various amino acids to identify promising substances with hypoglycemic action. Materials and methods. The objects of the study were 11 dry extracts from bearberry leaves, 10 of which were modified with various amino acids. The study of the phenolic compounds of the extracts was carried out by TLC, HPLC, and spectrophotometry. To assess the hypoglycemic activity of the extracts, two experiments were carried out - primary screening and oral glucose tolerance test. Results. Using TLC and HPLC, in the extracts obtained arbutin, gallic acid, 5 flavonoids were identified, among which hyperoside was dominant, 4 hydroxycinnamic acids, among which chlorogenic and caffeic acids were dominant, and their content was established. In the extracts obtained, main groups of phenolic compounds were quantified using a spectrophotometric method. Dry extracts from bearberry leaves, modified with cysteine, arginine and glutamic acid, showed the strongest hypoglycemic activity. Conclusions. The chemical composition of phenolic compounds and the hypoglycemic activity of dry extracts from bearberry leaves modified with 10 different amino acids were determined. The most promising substances turned out to be extracts modified with cysteine, arginine and glutamic acid; therefore, they are promising agents for the development of new drugs.