Immunostimulating and antioxidant composition

FIELD: medicine.

SUBSTANCE: invention refers to pharmacology and can be used in veterinary science and medicine for chemotherapy. There is disclosed immunostimulating and antioxidant lithium composition containing lithium ascorbate and lithium aspartate in percentage ratio 50:50.

EFFECT: expansion of the list of low-toxicity immunomodulators applicable for manufacture of drugs.

1 dwg, 2 tbl

 

The invention relates to chemical compositions based on salts of lithium, possessing biological activity, in particular antioxidant and immunostimulating properties, and can be used in medical and veterinary practice for treatment.

The level of technology

Known bioactive drug ascorbate lithium used as a means for increasing the activity of neutrophils [1] and has, in addition, antioxidant activity [2]. The composition and the achieved result the tool closest to the claimed and selected as a prototype.

Known from the patent No. 2226391 the drug has a low immunostimulatory activity.

The technical problem of the invention is the extension of the list of therapeutic agents and the development of effective immunostimulating drug based on lithium salts, namely, obtaining a new composition having immunostimulating properties in combination with antioxidant activity.

The invention

The problem is solved by the use of lithium ascorbate together with lithium aspartate in the following ratio, wt.%:

ascorbate lithium - 50

aspartate lithium - 50.

Used for solving the problem known component aspartate (asparagine) lithium is used in psycho-neurological clinics is in the treatment of Alzheimer's disease [3]. Its immunostimulatory properties we found for the first time, as available in the patent and medical literature such information does not occur. The composition of the mixture 50:50 chosen from considerations of optimal manifestation of biological activity of the components. We tested other options, however, the variation of the mass fraction of ingredient reduces the activity of one of the target parameters and reduces the overall synergistic effect.

Comparison with the prototype shows that the inventive composition contains distinctive characteristics which together are necessary and sufficient to solve the task.

Industrial applicability

The invention is implemented in practice and tested in laboratory conditions. When described in the section "summary of the invention the ratio of the components is provided a positive effect on the achievement of the objectives of the technical research task.

The composition according to the invention is used to test the reaction of blast transformation of human lymphocytes (rbtl). With this purpose, conducted the analysis steps of the claimed composition on immunocompetent cells, stimulated phytohemagglutinin (PHA). Investigated the influence of the drug at various concentrations in the range from 0.01 to 0.2 mg/ml Evaluation of the proliferative activity of lymphocytes is spontaneous and induced PHA test performed in accordance with the methodological recommendations of farmkomiteta of the RF Ministry of health (Vedomosti of the pharmacological Committee, 1999, No. 1). Similar tests conducted with drug-prototype (ascorbate lithium).

The results of the testing of drugs in the reaction rbtl shown in the drawing. The testing found that the inventive composition has a stimulating effect on PHA induced lymphocyte proliferative activity. The drawing shows, along with the test without preparation (first two columns, white and black), four charts, two column for the SP-test, two column for PHA-test, respectively, for control of the prototype and the claimed composition. In the control columns have zero height.

From the graphs it is clear that in the area studied concentrations of the inventive composition has a marked stimulatory effect on lymphocytes and the most convincing test of spontaneous proliferation (without activating the influence of PHA), enhancing the effect of 2.2-2.5 times in comparison with the prototype. An important feature of the claimed compositions is the lack of inhibitory effect on the proliferative activity of cells, while the prototype is marked 10-15%suppression activity of lymphocytes compared with controls (drawing).

Investigated the effect of the claimed composition on the functional activity of polymorphonuclear leukocytes in the peripheral blood of donors in a wide range of concentration is rd. Used are known from the literature, the modeling technique of phagocytosis using Staphylococcus aureus N-209 (D.K. Novikov, V.N. Novikov. Assessment of immune status. Moscow-Vitebsk, 1996, 281 C.). Counts the percentage of active neutrophils (PAN) and the percentage of completed phagocytosis (NRF) in the control test without the influence of drugs. The results are presented in table 1, which shows that after exposure of the claimed compositions in the field of the investigated concentration increases the percentage of active neutrophils and phagocytic activity in comparison with the prototype, which opens up the prospect for rational therapy of immunodeficiency.

The antioxidant activity of the composition according to the invention was determined by the cathodic voltammetry, in particular through the process of oxygen reduction (EV 02) [4]. The antioxidant activity of interest was assessed on a temporary or a so-called kinetic criterion of antioxidant activity, which shows the effectiveness of drug interactions with oxygen radicals and is determined by the formula:

where is the criterion of antioxidant activity, µmol/l min;

the oxygen concentration in the original solution without drug, µmol/l;

Ii- mn is an increase in the current EV O 2in the presence of the drug, MCA;

Ibeg- the current value EV O2without the drug in solution, MCA;

T - time of the process, minutes

Research in this procedure the compositions claimed in the percentage of 50:50 showed good antioxidant properties. Results in comparison with ascorbate lithium presented in table 2, which shows that the claimed composition is not inferior to the activity of the prototype with the same concentration values.

In the literature there is no information about the use of the claimed composition in veterinary or medical practice, indicating the novelty of technical solutions, and non-obviousness peak (resonance) ascending immunostimulatory and antioxidant activity of the composition allows to speak about the technical solutions according to the criterion of "inventive step".

The percentage of active neutrophils (PAN) and the percentage of completed phagocytosis (NRF) when testing the claimed composition
Table 1
Dose, mg/mlPAN,%NRF, %
The placeholderTrackThe placeholderTrack
control without medication27,127,132,232,2
0,0131,240,144,272,1
0,0234,444,5to 49.380,4
0,229,235,341,263,3
The antioxidant activity of the claimed composition

Table 2
MedicationWithslaveTo
Prototype (ascorbate lithium)0,020,89
0,21,20
Declare to notizia 0,021,17
0,21,10
Cslave- working concentration, g/l;
K - kinetic criterion of antioxidant activity, µmol/l min

Sources of information

1. Carpenters V.M.; Chuchalin B.C.; Skorik N.A.; Ulyanov, S.; Balashov P.P.; Ruzaev LN. Means for increasing the activity of neutrophils. RF patent №2226391, MPK7 AC 31/375. Publ. 2004.04.10 (prototype).

2. Abramchik O.A., Korotkova H., carpenters E.V., Kurbanov Y.A. Study of antioxidant activity and toxicity of ascorbate lithium // proc. Dokl. VII all-Russian scientific conference "Analytics of Siberia and the Far East." Novosibirsk. 2004. S.

3. Pharmaceutical compositions. US Patent No. 4810497, 1989.03.07.

4. Dracheva L.V. and other Study of antioxidant activity of biocomposite based probiotics. The food industry, No. 3, 2007, p.14-15.

The composition having immunostimulatory and antioxidant activity, including ascorbate lithium aspartate lithium in the following ratio, wt.%:

ascorbate lithium50
aspartate lithium 50



 

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