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Abstract

The aim of this work was to study the effect of glikverin based on voglibose and quercetin on lipid metabolism in experimental metabolic syndrome. Materials. The metabolic syndrome model was reproduced by keeping rats on a hypercaloric diet (containing 20 % fatty food and fructose ad libitum (1 g per day per 100 g of body weight as a 10 % aqueous solution) for 8 weeks. The content of complex carbohydrates in the daily diet of animals was 60 %. The following groups of rats were used: group 1 — intact control; group 2 — rats receiving a hypercaloric diet; group 3 — animals that were administered glikverin at a dose of 50 mg/kg on the background of hypercaloric diet, groups 4–6 — animals that were administered comparison drugs on the background of hypercalorie diet: quercetin substance at a dose of 50 mg/kg, the voglibose substance at a dose of 0.06 mg/kg and standard drug — metformin at a dose of 60 mg/kg. The study drugs were administered simultaneously with the hypercaloric diet intragastrically for 8 weeks. Lipid metabolism was assessed by body weight gain, total cholesterol, triacylglycerols, low- and highdensity lipoprotein cholesterol, and serum TNF-α levels. Results. It was found that the combined product glikverin reduces body weight gain by 66%, which is probably specified by the action of its component component voglibose, which slows down the breakdown and absorption of carbohydrates in the intestine. The results of the study of lipid metabolism in blood serum showed that the combination of voglibose and quercetin in the combined agent leads to the summation of their pharmacological effects. Under the influence of glikverin, the content of total cholesterol decreased by 1.7 times, LDL-C and TAG - by 1.6 and 2.2 times, respectively, the level of HDL-C increased by 46%. Comparative analysis showed that the pronounced antiatherogenic effect of the combined agent is due to the effect of both components, with a predominant effect on the lipid metabolism of quercetin. The revealed hypocholesterolemic and hypolipidemic action provide an antiatherogenic effect. The severity of this effect, which provided glikverin, significantly exceeded the comparison agents quercetin, voglibose and metformin. The combination of voglibose and quercetin also reduced by 38% the content of TNF-α - an inductor of insulin resistance in obesity. The obtained results substantiate the expediency of further pharmacological study of the antidiabetic properties of glikverin as a promising tool for the treatment of metabolic syndrome and type 2 diabetes.

Screening study of the antihyperglycemic action of new solid quercetin dispersions

“…At present, a standardized solid dispersion of quercetin with polyethylene oxide and neusilin has already been obtained at the National University of Pharmacy, which, together with voglibose, is included in the composition of a new combined antidiabetic agent under the code name "Glikverin". The pronounced antihyperglycemic and antidiabetic effect of "Glikverin" has been experimentally proven in models of insulin resistance, type 2 diabetes mellitus and metabolic syndrome [11].…”

“…The experimental dose of the investigated solid dispersions of quercetin was selected on the basis of previously obtained results in the study of solid dispersions of quercetin with polyethylene oxide and neusilin and amounted to 50 mg/kg [11].…”