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 soil scientists have revealed a direct correlation between the rate of soil formation of carbon dioxide, called CO2 emissions, and the content of microbial biomass in it. It is known that CO2 emission from soil is mainly conditioned by respiration of soil microorganisms and plant roots. The more CO2 soil emits, the more microbial biomass it usually contains. It was shown that CO2 emission by chernozem of different ecosystems (or different types of land use) correlates with the content of microbial biomass, and most closely with the rate of its microbial respiration. And the soil with good microbial properties has the “best quality”, is more fertile, provides the highest yield of crops and other plant biomass.
RUDN University chemists and their colleagues from the Russian Academy of Sciences have proposed new catalysts that allow to reduce the temperature of the oxidation reaction of alkanes three times — from 150 to 50 degrees. This significantly reduces the cost of synthesizing alcohols, aldehydes and other compounds needed, in particular, for the production of nylon and capron.
A chemist from RUDN University has developed a catalyst for the production of eugenol acetate, a substance that destroys the larvae of mosquitoes transmitting dangerous diseases, being a safe chemical for human health.
RUDN soil scientists have revealed a direct correlation between the rate of soil formation of carbon dioxide, called CO2 emissions, and the content of microbial biomass in it. It is known that CO2 emission from soil is mainly conditioned by respiration of soil microorganisms and plant roots. The more CO2 soil emits, the more microbial biomass it usually contains. It was shown that CO2 emission by chernozem of different ecosystems (or different types of land use) correlates with the content of microbial biomass, and most closely with the rate of its microbial respiration. And the soil with good microbial properties has the “best quality”, is more fertile, provides the highest yield of crops and other plant biomass.
RUDN University chemists and their colleagues from the Russian Academy of Sciences have proposed new catalysts that allow to reduce the temperature of the oxidation reaction of alkanes three times — from 150 to 50 degrees. This significantly reduces the cost of synthesizing alcohols, aldehydes and other compounds needed, in particular, for the production of nylon and capron.