RUDN University chemist synthesized a new compound with strong anti-diabetic properties
In the small intestine, the complex structure of starch is broken down into simpler oligosaccharides by the action of the enzyme α-amylase. Then, under the action of the enzyme α-glucosidase, the resulting oligosaccharides pass into glucose and other monosaccharides. If you inhibit — that is, “turn off” — one or both of these enzymes, the rate of carbohydrate absorption will decrease, and, consequently, the concentration of glucose in the blood will decrease. This antidiabetic effect makes researchers pay more and more attention to the search and synthesis of α-amylase and α-glucosidase inhibitors.
Yuness El Bakri from the RUDN University in collaboration with colleagues 17 have synthesized new derivatives of 1,2,4-triazole. They belong to the class of heterocycles — organic compounds that contain “rings” of carbon atoms and atoms of other elements. Due to their structure, which resembles that of natural products, heterocyclic compounds have interesting biologically active properties.
RUDN chemists studied the structure of new heterocyclic compounds using x-ray diffraction analysis and spectral methods. They then evaluated in vitro the inhibitory activity of all 1,2,4-triazole derivatives and compared them with acarbose, a hypoglycemic drug that inhibits α-glucosidase. All of the new compounds proved to be potent inhibitors of α-glucosidase, and three of them also demonstrated the ability to inhibit α-amylase.
Using molecular docking, a method for modeling the properties of molecules, the researchers showed that three triazole derivatives — 6 — methyl-7H,8H,9H-[1,2,4]triazolo[4,3-b][1,2,4]triazepine-8-one and 6-methyl-7H-[1,2,4]triazolo[4,3-b][1,2,4]triazepine-8(9H)-thion-surpass acarbose in inhibitory activity relative to α — glucosidase.
Based on the results of experiments, RUDN biochemists selected the best conformation of 6-methyl-7H-[1,2,4]triazolo[4,3-b][1,2,4]triazepine-8(9H)-thion in complex with α-glucosidase and performed its molecular dynamic modeling.
Calculations have shown that the degree of inhibition of α-glucosidase is mainly due to the number and strength of bonds between the compound and the active residues of the enzyme. The results obtained allow us to conclude that the synthesized compound is stable.
Younes El Bakri and his colleagues also showed the antioxidant properties of the new compounds. Chemists used a spectrophotometer to measure changes in the optical density of solutions containing specifically colored free radicals (ABTS cation-radical (2,2’-azinobis3-ethylbenzothiazoline-6-sulfonate) and DPPH radical (2,2-diphenyl-1-picrylhydrazyl)), to which antioxidants were added. Using these methods, they determined the ability of the antioxidant to interact with ABTS and DPPH radicals. Also, the antioxidant activity of 1,2,4-triazole derivatives was evaluated by evaluating the ability of antioxidant iron reduction.
The chemists concluded that the 1,2,4-triazole derivatives they obtained are promising for use as antidiabetic drugs. They expect that the properties of these substances will soon become the subject of Toxicological and pharmacological studies in vivo.
Article in the journal Bioorganic Chemistry.
RUDN summarized the results of the scientific competition "Project Start: work of the science club ". Students of the Faculty of Physics, Mathematics and Natural Sciences have created a project for a managed queuing system using a neural network to redistribute resources between 5G segments. How to increase flexibility, make the network fast and inexpensive and reach more users — tell Gebrial Ibram Esam Zekri ("Fundamental Computer Science and Information Technology", Master's degree, II course) and Ksenia Leontieva ("Applied Mathematics and Computer Science", Master's degree, I course).
The National Demographic Report, 2023 Demographic Well-Being of Russian Regions (hereinafter - the National Demographic Report) was prepared by the scientific team of the Institute of Demographic Studies of the Federal Research Center of the Russian Academy of Sciences, the Vologda Scientific Center of the Russian Academy of Sciences, Peoples' Friendship University of Russia, the Center for Family and Demography of the Academy of Sciences of the Republic of Tatarstan, as well as with the participation of leading scientists from the Republic of Bashkortostan, Stavropol Krai, Volgograd, Ivanovo, Kaliningrad, Nizhny Novgorod, Sverdlovsk Oblasts and Khanty-Mansi Autonomous Okrug–Yugra.
RUDN summarized the results of the scientific competition "Project Start: work of the science club ". Students of the Faculty of Physics, Mathematics and Natural Sciences have created a project for a managed queuing system using a neural network to redistribute resources between 5G segments. How to increase flexibility, make the network fast and inexpensive and reach more users — tell Gebrial Ibram Esam Zekri ("Fundamental Computer Science and Information Technology", Master's degree, II course) and Ksenia Leontieva ("Applied Mathematics and Computer Science", Master's degree, I course).
What is your first association with the word “laboratory”? Flasks and beakers? Microscopes and centrifuges? Yes, many of us would answer the same way.
The National Demographic Report, 2023 Demographic Well-Being of Russian Regions (hereinafter - the National Demographic Report) was prepared by the scientific team of the Institute of Demographic Studies of the Federal Research Center of the Russian Academy of Sciences, the Vologda Scientific Center of the Russian Academy of Sciences, Peoples' Friendship University of Russia, the Center for Family and Demography of the Academy of Sciences of the Republic of Tatarstan, as well as with the participation of leading scientists from the Republic of Bashkortostan, Stavropol Krai, Volgograd, Ivanovo, Kaliningrad, Nizhny Novgorod, Sverdlovsk Oblasts and Khanty-Mansi Autonomous Okrug–Yugra.