Medicine/ 7. Clinical Medicine.
C.
pharm. s., R. Î. Shcherbyna, d.
pharm. s, professor, O. I. Panasenko, d. pharm. s, professor, E. G. Knysh, c. pharm. s., A. V. Samko
Zaporozhye State Medical University, Ukraine
Antioxidant activity of
1,2,4-triazole derivatives
Antioxidants
are chemicals that prevent oxidation of other chemicals. They protect main cell
components neutralizing the damaging effects of free radicals, which are
natural by-products of cell metabolism.
In
a normal cell there is antioxidant balance, suitable to oxidant. However, this
balance can be shifted. This stage is called oxidative stress. Oxidative stress
causes damage of biopolymers including nucleic acids, proteins, fatty acids and
carbohydrates.
This
molecular mechanism of cell damage leads to the formation of wide range of
cytotoxic products, most of which are aldehydes, such as malonic dialdehyde and
4-hydroxynonenal. Oxidative stress leads to serious cell damage that causes
various human diseases.
Therefore,
the search for substances that could not only prevent but also increase the stability of human body and hinder the process of
oxidative stress is important task of medicine and pharmacy.
The
main aim
of our research was to study the antioxidant activity of (AOA) 1,2,4-triazole
derivatives. In series of screening studies the original compounds of
1,2,4-triazole derivatives of AOA compounds were used in vitro experiments
(table. 1)
Lipoprotein
suspension of yolk eggs, LPO initiative in which was carried out using ferrous
iron ions was used as a model
system to determine the total AOA of 1,2,4-triazole derivatives. Experimental
substances were added to the suspension in concentration of 10-3 mol
/ l.
The
intensity of leading peroxide oxidation of lipids (POL)
processes in a model system was appraised with the concentration of
active products that react with 2-thiobarbituric acid (TBA-AP).
The
results of definition AOA 1,2,4-triazole derivatives have obtained. It was
found that compounds of 1,2,4-triazole derivatives in different stage of
displaying were able
to inhibit the generation of free radicals.
Thus, potassium 2-((4-amino-3-(morpholinomethyl)-4H-1,2,4-triazol-5-yl)thio)acetate
(PKR-173) which depress the formation
of end products POL – TBA-AP on 95,37% (ð˂0,001) has the most expressive
ÀÎÀ.
As
a result of studies some "structure-action" regularity that could be
used in further purposeful search for substances with antioxidant activity.
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