Selenocosmiinae organic substance having bioactive properties

 

The invention relates to biochemical pharmacology and can be used in clinical medicine as an anti-inflammatory, wound healing, hemostatic, anti-cancer, deworming and cardiac tonic. A substance with a wide spectrum of biological actions selenocarbonates. It contains selenoprotein, selenium and sesquiterpene lactone and obtained under the action of electromagnetic high-frequency fields power 510-3W/cm at a frequency of 20-30 MHz. Selenocarbonates additionally contains the ketone thujone - selenocosmiinae; or the anion of the bromine - bromide-selenocarbonates; or terpyridyl - selecteddirectory or alpha-pinene - selenaencarnation; or azulene - solenoidoperated. Proposed substances that ensure their use for stimulating the immune system and for the regulation of various metabolic processes. 5 C.p. f-crystals, 13 ill.

The invention relates to biochemical pharmacology and pharmacodynamics, biochemical medicine, cellular and molecular biology, immunopharmacology and applied medicine and can be used is, antihelminth and cardiac tonic. This substance can be used to stimulate the immune system and for the regulation of various metabolic processes.

Currently in clinical medicine for the correction of immune and metabolic processes, as well as for the regulation of the cardiovascular mechanisms are organic substances of natural origin. It is, as a rule, preparations of extracts of thymus, lymph nodes, connective tissue and spleen. Such drugs are well known in clinical practice substance - timogen, T-activin, mielopid, timoptic etc. (Mashkovsky M. D. Drugs, corrective processes of immunity. In kN. Medicines, Kharkov, Torching”, so 2, 1997, p 199-207).

In recent years the attention of many researchers attracted selenium and its compounds, the so-called selenesetestcase proteins, because the biochemical functions of selenium are determined not by the trace, and selenoproteome organic substances. The lack of this mineral can lead to disruption of cellular integrity, changes in the metabolism of thyroid hormones, activity biotransformed is. the characteristic feature of selenium-containing proteins in mammals is that they are associated with redox processes occurring inside the cell and outside it. Characterized to date twelve of selenium-containing proteins, including enzymes - glutathione peroxidase, iodernization, thioredoxine, selectstatement and others. Isotopic data analysis and the results of theoretical studies suggest that in mammals may be from 20 to 100 selenium-containing proteins (C. A. tutelian, etc. in the book. Selenium in humans, M., 2002, S. 18-34).

By now fairly well understood biological functions of selenium, including the mechanism of action of glutathione peroxidase, the recovery process peroxynitrite under the action of selenium-containing proteins, the mechanism of interaction of selenium with antioxidants, especially vitamins C, E and A. we have also Studied the role of selenium in the emergence and development of cardiac diseases, the influence of selenium on the biosynthesis of prostaglandins, the effect of selenium on reproduction, and the role of selenium in the metabolism of xenobiotics (C. A. tutelian, etc. in the book. Selenium in the human body. M, 2002 the ideological components and regulators in the implementation of complex metabolic processes, including oxidation-reduction, vascular, neuro-humoral and others. In this regard, a particularly relevant issue receipt of such biologically active compounds of selenium, which could take a direct part in normalizing and restoring a number of homeostatic processes. However received to date medicinal substance selenium series are either the trace element or its compounds with vitamins, including amino acids, such as cysteine or methionine. In this regard, the generated medicinal substance of the new class should to some extent according to their structure and mechanism of action to meet the selenium-containing proteins directly involved in diverse physiological processes and metabolic, immune, reproductive, genoprotective and others.

To solve this task offers medicinal substances with the effect of selenium-containing proteins. They include low-molecular weight component - protein, obtained by extraction of the protein-containing vegetable raw materials with organic solvents, selenium, sesquiterpene lactone, thujone, anions bromide, terpyridyl, PI is. The invention is illustrated in Fig.1-13.

Getting celestechenping organic matter - STP

As the original products use green mass of protein-enriched plants, such as cereals, legumes, leaves of corn. Extraction from plant tissue extract protein. The extraction was carried out with ether, ethyl alcohol, Dimexidum. The extract obtained is evaporated and produce lyophilic drying. The powder is dissolved in 60-90% ethanol solution. The solution is injected selenium obtained by thermolysis of Selenomethionine (6-12 μg per 1 ml of solution). Then to the mixture add a certain amount of sesquiterpene lactone and put it in a high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz).

1. Substance selenocarbonates - STP

The substance includes a molecule of selenoprotein (Fig.1), which is attached with the sesquiterpene lactone - STL (Fig.2) to the carboxyl groups of the side chain residues of glutamic and/or aspartic acid and/or C-terminal carboxyl groups through difficult-the ester linkage (Fig.3). Molecule selenocarbonates represents two polypeptide alpha - and beta-chain connection of the slot). Selenium is obtained by thermolysis of Selenomethionine, included in the side alkyl radicals of amino acids, connecting some links of alpha and/or beta-chains of one or two neighboring protein molecules, thereby further “stitching” them.

When all the physiological pH the molecule selenocarbonates ionized. Charged are P - and N-terminal group and associated withcarbon atoms of the side chain containing a carboxyl or amino group (-COO-, -NH+3).

2. Substance selenocosmiinae (Fig.6)

The substance includes an ionized molecule selenocarbonates (Fig.3) to which is attached the ketone thujone - T (Fig.4) through the amino group of the side chains of residues of arginine and/or terminal amino groups (Fig.5).

3. Substance bromide-selenocarbonates (Fig.7)

The substance includes an ionized molecule selenocarbonates to which the amino groups of the side chains of residues of arginine and/or histidine and/or terminal amino groups attached anions bromine (Br-).

4. Substance selenitireducens (Fig.9)

The substance includes an ionized molecule selenocarbonates, to which is attached terpyridyl - TN (Fig.8) Amoxiline groups through hard-essential communication.

5. Substance selenaencarnation (Fig.11)

The substance includes an ionized molecule selenocarbonates (Fig.3) to which is attached alpha-pinene (P), pre-oxidized to verbenol (Fig.10) to the carboxyl groups of the side chains of residues of glutamic and/or aspartic acid and/or C-terminal carboxyl groups through hard-essential communication.

6. Substance solenoidoperated (Fig.13)

The substance includes an ionized molecule selenocarbonates (Fig.3) to which is attached azulene (AZ), largely polarized (Fig.12) on the terminal carboxyl (-) and amino-(+) groups and/or side chains of arginine (+), and/or histidine (+), and/or glutamic acid(-), and/or aspartic acid(-) (Fig.13).

Examples get selenocosmiinae organic substances

Example 1

The method of producing selenocarbonates

To ionized molecule selenoprotein add the required amount of sesquiterpene lactone. The mixture was kept in the high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz). The molar ratio STL:selenoprotein 4:1.

Example 2

The method of receiving selenation thujone. The mixture was kept in the high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz). The molar ratio of T:selenocarbonates 4:1.

Example 3

The method of obtaining bromide-selenocarbonates

To ionized molecule selenocarbonates add the required amount of bromine anions obtained by electrolysis of NaBr. The mixture was kept in the high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz). The molar ratio VG:selenocarbonates 4:1.

Example 4

The method of producing selecteddirectory

To ionized molecule selenocarbonates add the required amount of terpingidrata. The mixture was kept in the high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz). The molar ratio of TN:selenocarbonates 4:1.

Example 5

The method of producing sleepinginairports.net

To ionized molecule selenocarbonates add the required amount of pinene, pre-oxidized to verbenol. The mixture was kept in the high-frequency electromagnetic field (capacity 510what I solenoidoperated

To ionized molecule selenocarbonates add the required amount of azulene. The mixture was kept in the high-frequency electromagnetic field (capacity 510-3W/cm, the frequency of 20-30 MHz). The molar ratio of Al:selenocarbonates 4:1.

Acute toxicity of the preparation was studied intraperitoneal injection Se-TP at a dose of 250 mg/kg to mice (age 6 weeks, weight 28-30 g). The value of LD was 700 mg/kg

In the study the overall toxicity mice were injected Se-TP at a dose of 100 mg/kg / day intraperitoneally continuously for 10 days. Weight loss and any other violations not mentioned, in the future, under the observation of these mice within three months of abnormalities not detected.

As a result of the research showed that Se-TA is an organic compound that has a strong biological effect, non-toxic, completely soluble in water and biological fluids - blood, lymph and cerebrospinal fluid. In 1 ml of Se-TA contains, depending on the number of amino acids in the ligand from 20 to 30 mg of the substance and 8-10 mcg of selenium.

The dose of an administered drug depends on the clinical condition of the patient, his age, weight, and method of administration. Effective techno or fractionally.

The method of activation and stimulation of metabolic and immune processes is as follows.

The resulting preparation Se-TA is a solution of the active substance in 60-90% ethyl alcohol, 1 ml of which contains 20-30 mg of the drug substance. Se-TA be administered orally, intramuscularly, intravenously, intraarterially, as well as externally in the form of a suspension in an oil solution or in the form of ointment with oil-alcohol filler.

When oral administration is necessary, the dose is calculated as follows:

20 drops of solution containing 20-30 mg of the drug substance;

10 drops (1/2 ml) contains 10-15 mg drug;

5 drops (1/4 ml) contains 5 -7,5 mg drug;

3 drops (1/7 ml) contains 3,3 mg of the drug.

Intramuscular, intravenous or intraarterial administration of drug dissolved in physiological solution for best of dissociation in the ratio of 1:10-1:20 using the 60% alcohol or 1:15 with 90% alcohol.

For example, when clinical pathology moderate the drug is administered once in the form of injections from 0.1 to 0.5 ml / day, severe pathology of the specified dose is administered twice a day. In the intensive drug therapy introduced the practical solution. In the case of oral administration, depending on the age, weight and extent of injury from 0.5 to 3.0 ml, and the drug is dissolved in 1/3 Cup boiled lukewarm water (36-38C). The duration of treatment can vary from 1 to 3 months, in the case of a seriously leaking pathology the course of treatment, repeat with an interval of 1-2 months prior to the expressed clinical effect. During treatment control effect treatment study of biochemical parameters and immune status.

Claims

1. Selenocosmiinae organic matter with a wide spectrum of biological activity, characterized in that it contains selenoprotein which consists of two polypeptideand- chain protein in lateral alkyl radicals which entered selenium, connecting some linksor-chains of one or two adjacent molecules of the protein, polypeptide chain also connected by a disulfide bridge at cysteine residues, with selenoprotein connected with the sesquiterpene lactone through the carboxyl groups of the side chains and octatetraene field capacity 510-3W/cm at a frequency of 20-30 MHz.

2. Substance under item 1 further comprises the ketone thujone and is selenocosmiinae (Fig.6), while the thujone with selenocarbonates is connected via the amino group of the side chains of residues of arginine and/or terminal amino groups.

3. Substance under item 1 further comprises anions bromide and represents a bromide-selenocarbonates (Fig.7), while the bromine with selenocarbonates is connected via the amino group of the side chains of residues of arginine and/or histidine and/or terminal amino groups.

4. Substance under item 1, further comprises terpyridyl and represents selenitireducens (Fig.9), while terpyridyl with selenocarbonates connected via carboxyl groups of the side chains of residues of glutamic and/or aspartic acid and/or C-terminal carboxyl group.

5. Substance under item 1 additionally contains alpha-pinene, pre-oxidized to verbenol, and represents selenaencarnation (Fig.11), while pinene with selenocarbonates connected via carboxyl groups of the side chains of residues of glutamic and/or aspartic acid and/or C-terminal carboxyl group.

6. Substance p is connected with selenocarbonates on the terminal carboxyl (-) and amino (+) groups and/or side chains of arginine (+) and/or histidine (+), and/or glutamic acid (-) and/or aspartic acid (-).

 

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