In silico and in vivo study of the antidiabetic properties of some natural biologically active substances

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Abstract

Relevance. According to the Federal Register of Diabetes Mellitus, the number of patients diagnosed with diabetes is 4.9 million people, which is 3.31% of the population of the Russian Federation. The search for new antidiabetic drugs today is still an urgent task of pharmacy. Currently, doctors have a fairly wide range of synthetic drugs in their arsenal, but the issue of rational pharmacotherapy is still open. And in this regard, medicinal products of natural origin look promising.

The aim of the study was to evaluate the theoretical possibility of intermolecular interaction of a number of biologically active substances of plant origin with the active site of non-receptor type 1 tyrosine-protein phosphatase (PTP1B) and the active site of the intestinal maltase-glucoamylase (MGA) enzyme by molecular docking, as well as pharmacological confirmation of specific activity in the experiment.

Material and methods. Male Wistar rats weighing 200–220 grams were used in the study. Modeling of diabetes mellitus was performed by a single intraperitoneal injection of alloxan (150 mg/kg) with a preliminary injection of nicotinamide (250 mg/kg). Animals with a model of diabetes mellitus (n=21) were introduced daily with the original combined substance of plant extracts of Galega officinalis L., Glycyrrhiza glabra L. and Mentha piperita L. at a dose of 500 mg/kg, reference drug - substance gliclazide – 60 mg/kg. The determination of the hypoglycemic effect was carried out after a single introductions and on the 14th day.

Results. The hypoglycemic effect of the phytosubstance was established and the possibility of the influence of biologically active substances on PTP1B and MGA was evaluated. The results of molecular docking indicate a possible interaction of the studied objects with PTP1B and MGA; the highest values of docking are typical for kaempferol, caffeic and ellagic acids. In an in vivo study, a statistically significant decrease in the concentration of glucose in the blood of animals by 49.3% was found.

Conclusions. The possibility of interaction of biologically active substances that are part of plant extracts with specific targets PTP1B and MGA was established by molecular docking, and the hypoglycemic effect of the proposed combined substance of plant extracts of goat's rue, licorice and peppermint was confirmed in the experiment.

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About the authors

A. Sh. Giyoszoda

Medical College of M.S. Khamadoni

Author for correspondence.
Email: asom_giysov@mail.ru

Ph.D. (Biol.)

Tajikistan, Khatlon region, r. M.C.A. Hamadoni

F. S. Sharopov

Institute of Chemistry named after V.I. Nikitin of the National Academy of Sciences of Tajikistan; Research Institution «Chinese-Tajik Innovation Center for Natural Products», National Academy of Sciences of the Republic of Tajikistan

Email: shfarukh@mail.ru

Ph.D.

Tajikistan, Dushanbe; Dushanbe

E. F. Stepanova

Pyatigorsk Medical and Pharmaceutical Institute Branch of Volgograd State Medical University

Email: efstepanova@yandex.ru

Dr.Sc. (Pharm.), Professor, Department of Pharmaceutical Technology with a Course in Medical Biotechnology

Russian Federation, Pyatigorsk

S. S. Saidakhmadov

Medical College of M.S. Khamadoni

Email: s.saidvali@mail.ru

Department of Pharmacy

Tajikistan, Khatlon region, r. M.C.A. Hamadoni

S. E. Storozhenko

Krasnoyarsk State Medical University after Professor V.F. Voyno-Yasenetsky

Email: s.e.storozhenko@yandex.ru

Ph.D. (Pharm.), Department of Pharmacy with a Postgraduate Course

Russian Federation, Krasnoyarsk

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