3
RUDN University chemist synthesized a new compound with strong anti-diabetic properties

RUDN University chemist synthesized a new compound with strong anti-diabetic properties

RUDN University chemist synthesized new derivatives of 1,2,4-triazole, which have pronounced antidiabetic properties. Experiments have shown that these molecules “work” better than acarbose — an existing hypoglycemic drug — and have antioxidant properties. In the future, they can be used to develop drugs against type 2 diabetes.

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.

Student's Scientific Initiatives View all
03 Nov 2017
June 22 - 26, 2017 in Barnaul, Altai State University, took place the Summer Academy of the BRICS Youth Assembly, an international event that brought together representatives of different countries
1230
Main Publications View all
15 Nov 2017
RUDN University scientists publish results of their scientific researches in highly-recognized in whole world and indexed in international databases journals (Web of Science, Scopus ect.). That, of course, corresponds to the high status of the University and its international recognition. Publications of June-September 2017 ( In Journals of categories Q1-Q3)
1357
Similar newsletter View all
21 Oct
RUDN University mathematician determined the conditions for the coexistence of three species in the wild

RUDN University mathematician together with colleagues from India and France for the first time studied in detail the system of coexistence of three species of living creatures in the wild. The results help to understand what parameters determine the extinction andли survivalof species, and how the number of species changes in space and time.

27
21 Oct
RUDN University Chemist Created Coordination Polymers Films with up to 99.99% antibacterial efficiency

RUDN University chemist with his colleagues from Portugal has developed two types of coating based on new coordination polymers with silver. Both compounds were successfully tested against four common pathogens.

24
21 Oct
RUDN scientists have improved titanium dental implants with graphene nanosloyers

RUDN researchers have created and tested a method for processing titanium dental implants. It turned out that theanoslos of graphene on the surface of titanium improve its interaction with stem cells,which are placed on the implant so that it better "takes root".Thanks to this method ofprocessing, stem cells are better kept on the surface, multiply and turn into the desired cells.

26
Similar newsletter View all