Antioxidant

 

(57) Abstract:

The invention relates to preparations containing organic active compound, which can be used as a medicine and food additives, prevent the development of free radical processes and impaired antioxidant system of living organisms. The inventive use allantoin as an antioxidant. The technical result consists in the expansion of the means of possessing antioxidant properties. Exogenous introduction of allantoin increases additional pool of antioxidants in living cells and blood plasma and increases the body's resistance to oxidative stress. table 2.

The invention relates to preparations containing organic active compound, which can be used as a medicine and food additives, prevent the development of free radical processes and impaired antioxidant system of living organisms in various biological processes such as aging, stress and diseases associated with disorders of free radical processes (inflammation, cancer, ischemia).

Antioxidants are westwooddame access components oxidative reactions to each other or modifying the oxidation of the substrate (tocopherol, cholesterol, chelators of metals of variable valence), and the true antioxidants, capable of reacting with active forms of oxygen, to form or molecular products, or radicals with lower reactivity (SOD, catalase, glutathione peroxidase).

Currently there are a large number of antioxidants, used in medical, pharmaceutical, cosmetic and food industries. Using both natural and synthetic antioxidants, such as superoxide dismutase (patent US 5498434, A 23 D 7/00) [1]. Glutathione is antioxidant properties during ischemia. Protective agents against oxidative stress and chronic diseases are some of the vitamins (vitamin C - ascorbic acid, carotenoids, vitamin E, vitamin A) (VanPoppel G. , VandenBerg N. Vitamins and cacer // Cancer Letters., 1997.- V. 114.- N 1-2.-P. 195-202) [2].

Natural antioxidants include compounds such as para-aminobenzoic acid (Akberova S. I., Musayev, P. I., Magomedov N. M., Babayev H. F., qahramanov H. M., Stroeva O., Paraaminobenzoic acid as an antioxidant. / / Dokl. Academy of Sciences, 1998, I. 361, No. 3, S. 419 - 421) [3], urea, uric acid (Kenya M. C., Shkurat, Etc., Lukasz A. I., Guskov E. P. Changing UB is the Qing.in 1993.-So 27, N 3.-S. 37-43) [4], glutathione (Loft S, now NOT. Markers of oxidative damage to DNA: Antioxidants and molecular damage //Oxidants and antioxidants., 1999.- V. 300.- P. 166-184) [5], lecithin (patent US 5498434, A 23 D 7/00, 1996-03-12) [6].

The disadvantage is used as antioxidants substances is their instability: enzymes - jirorastvorimogo, tocopherol and carotene - high molecular weight, which complicates their permeability through cell membranes.

The technical result of the invention consists in the expansion of the means of possessing antioxidant activity. This is achieved by using as an antioxidant allantoin.

Know the use of allantoin for the regeneration of skin cells (patent RU, 2137462, C1, 6 a 61 K 7/00, 7/48) [7], in the pharmaceutical industry for the treatment and mitigation of the symptoms of weliwita and vulvovaginitis (patent RU, 02117479, C1, 6 a 61 K 31/195) [8], in medicine as a wound-healing and epitheliomatous tool (patent RU, 2011376, C1, 5 a 61 K 7/16) [9].

It is known that allantoin is involved in metabolic processes as an intermediate product of the metabolism of purines in living cells lower primates and other mammals. In these animals the catabolism of purines ends with the formation of allantoin as a result of hydrolysis and urinary purine is uric acid, which can accumulate in the body in the form of lithate and its sodium salt (R. Marri, etc. Biochemistry man. - M.: Mir, 1993, so 2, S. 24-25) [10].

New found our property allantoin is its ability to increase the body's resistance to oxidative stress, reduce the intensity of the processes of lipid peroxidation in various tissues and increase additional pool of antioxidants in the cell and blood plasma by increasing the concentration of allantoin in the body when it is exogenous introduction.

These provisions proved by us experimentally. The results are shown in table. 1 and 2.

Table. 1. The effect of allantoin on the content of products of lipid peroxidation in various tissues of rats treated with high pressure oxygen.

Table. 2. The effect of allantoin on the activity of antioxidant enzymes in various tissues of rats treated with high pressure oxygen.

Example usage:

1 ml of a freshly prepared aqueous solution of allantoin (Serva) at a concentration of 2x10-4M/ml was injected intraperitoneally 1 h, 12 h and 24 h before treatment increased oxygen pressure (0.3 MPa -2 h) at a rate of 1 ml of a mixture of 200 g of weight of the animal.

In conditions of oxidative stress induced by hyperbaric oxygenation (HBO), the observed increase in the intensity of GENDER in all tissues: the MDA level increased by 43-90% (table. 1, examples A4, B4, D4, g, S4), the content of SB is increased by 50-103% (table. 1, examples B4, G4, E4, S4, K4).

While there has been a violation of coordination in the work conjugate of the antioxidant enzymes SOD and catalase. In terms of GCE observed inhibition of SOD activity on 53-60% in various tissues of rats (table.4, examples B4, D4, g, S4), whereas catalase activity increases by 24-77% in the tissues (table. 4, examples G4, E4, 34, K4) and in erythrocytes is reduced by 38% from the th stress, we used as experimental models, accompanied by a significant intensification of GENDER, tension and a violation of the synergistic functioning of the components of the antioxidant enzyme system in rat tissues.

Studies have shown that pretreatment of allantoin leads to a significant decrease in the intensity FLOOR in erythrocytes, brain, lungs, liver and kidneys of rats in conditions of HBO-induced oxidative stress. The use of allantoin leads to the decrease in MDA level in GCE in tissues that are 40-57% relative to the intact control and 60-72% relative giperatsidnogo control (table. 1, examples A5, B5, D5, g, I5), SB level with the introduction of allantoin is reduced in the brain of 31% (table. 1, an example G5), lung 36% (table. 1 E5) compared with the intact control. Compared to hyperoxidized control there has been a significant decrease in the level of SHO in all tissues at 26-62% (table. 1, examples B5, G5, E5, 5, K5). In General, allantoin leads to normalization of the SB level in various tissues with HBO, and in the brain and lungs their content on 31 - 36% lower than in control. It should be emphasized that the level of the FLOOR when using allantoin not just normal, and falls neither the compulsory introduction of allantoin leads to normalization of SOD activity in tissues at HBO compared with the inhibition of the activity of antioxidant enzymes in unprotected animals (PL.2). The use of allantoin normalizes the activity and significantly activates SOD on 77-165% in tissues relative to giperatsidnogo control (table.2, examples A5, B5, D5, g, K5).

Thus, we can conclude that the use of allantoin helps to normalize the functioning of the most important antioxidant enzymes - SOD in tissues with HBO-induced oxidative stress.

Preliminary introduction of allantoin leads to normalization of catalase activity in the brain, lungs, liver and kidneys when HBO (PL. 2, examples G5, E5, 5, K5).

The advantage of allantoin compared with known antioxidants is that it is well soluble in water compared with vitamins a and E, is characterized by a stable molecular structure and ability to prevent oxidative damage from all known types of active oxygen metabolites, in contrast to the antioxidant enzymes SOD and catalase.

The analysis of the conducted research allows to draw the conclusion that allantoin has a high antioxidant capacity and power. It is you who WNA products FLOOR - MDA and SHO - in terms of HBO-induced oxidative stress following values for the intact control. The introduction of allantoin has a normalizing effect on the activity of SOD and catalase, restoring optimal ratio of paired activity of antioxidant enzymes and the consistency of their actions, relieves tension and imbalance of antioxidant enzymes under oxidative stress.

Sources of information

1. Patent US 6015548 And 61 To 7/42. Roberts R. L. et al. High efficiency skin protection formulation with sunscreen agents and antioxidats.

2. VanPoppel G., H. VandenBerg Vitamins and cancer // Cancer Letters., 1997.- V. 114.-N 1-2.- P. 195-202.

3. Akberova S. I., Musayev, P. I., Magomedov N. M., Babayev H. F., qahramanov H. M., Stroeva O., Paraaminobenzoic acid as an antioxidant. / / Dokl. Academy of Sciences, 1998, I. 361, No. 3, S. 419-421.

4. Kenya M. C., Shkurat, Etc., Lukasz A. I., Guskov E. P. changes in the level of uric acid in the tissues of rats as a systemic response to hyperoxia// the Aerospace and environmental medicine.in 1993.- So 27, N 3. -S. 37-43.

5. Loft S, now HE. Markers of oxidative damage to DNA: Antioxidants and molecular damage //Oxidants and antioxidants., 1999.- V. 300.-P. 166-184.

6. Patent US 54998434, A 23 D 7/00. Jonston J. D. Synergistic compositions for extending animal feed shelf life.

7. Patent RU 2137462, C1, 6 A 61 K 7/00 "Cosmetic cream>9. Patent RU 2011376, C1, 5 A 61 K 7/16 "Dental elixir" from 30.04.1994.

10. P. Murray, etc. Biochemistry man. - M.: Mir, 1993, so 2, S. 24 - 25.

Use allantoin as an antioxidant.

 

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