Pharmacological geroprotective composition and method of obtaining thereof

FIELD: chemistry.

SUBSTANCE: invention represents a pharmacological geroprotective composition, which includes a polyphenol component, vitamins and microelements, humic acids, containing polyphenol components, vitamin C, vitamin A, iron (II) chloride and selenium (IV) dioxide, with the composition components being in a specified ratio in wt %.

EFFECT: increased life expectancy and retardation of tumour development.

2 cl, 3 dwg, 2 tbl, 4 ex

 

The invention relates to medicine, namely to the pharmaceutical industry, and concerns of geroprotective compositions based polyphenolic components, vitamins and minerals and how it was received.

Epidemiological data and the results of experimental studies indicate that a variety of polyphenolic components (flavonoids) play an important role in the prevention of such age-related diseases like cancer and cardiovascular disease (Graf V., Milbury R.E, Blumberg J.B. Flavonols, flavones, flavanones, and human health: epidemiological evidents // J.Med. Food. - 2005. - Fall; V.8, N 3. - P.281-290).

There is evidence that high levels of flavonoids directly associated with a reduced risk of myocardial infarction (Hernandez-Diaz S., Marinez-Losa E., Fernandez-Jame E., Serrano-Martinaz M., Martines-Gonzalez M. Dietary folate and the risk of nonfatal myocardial infarction // Epidemiology. - 2002. - V.13. - P.700-706) and other cardiovascular diseases (Kondo K., Matsumoto, A., Kurata N., Tanahashi H., Koda, H., Amachi T., Itakura H. Inhibition of oxidation of low-density lipoprotein with red wine // Lancet. - 1994. - V.344. - P.1152).

In addition, it was found that resveratrol (a flavonoid found in red wine has anti-carcinogenic effects: inhibits the growth of induced skin tumors in mice (Jang M, Cai L., Udeani G.O., Slowing K.V., Thomas CF, Beecher CW, Fong H.H., Farnsworth NR, Kinghorn A.D., Mehta, R.G., Moon R.C., J.M. Pezzuto, Cancer chemopreventive activity of resveratrol, a natural product derived from grapes // Science. - 1997. - V.275. - P.218-220)

There is evidence that other polyphenolic components (catechins contained in green tea), not only reduce the level of lipids in the body and prevent the development of cardiovascular diseases (Arts, I.C., Hollman P.Ch., Feskens E. J.M., De Mesquita H.B.B., Kromhout D. Catechin intake might explain the inverse relation between tea consumption and ischemic heart disease; the Zutphen elderly study // Am. J. Clin. Nutr. - 001. - V.74. - P.227-232), but also can reduce the risk of cancer (Zheng W., Doyle TJ, L.H. Kushi, T.A. Sellers, Hong C-p, Folsom A.R. Tea consumption and cancer incidence in a prospective cohort study of postmenopausal women // Am. J. Epidemiol. - 1996. - V.144. - P.175-182).

In medicine describes the components are mainly used in plant extracts.

Known hepatoprotective agent-based polyphenols artichoke (EN 2281112, publ. 10.08.2006), antioxidant-based tools polyphenols chagi (EN 2339390, publ. 10.08.2006) and grass psellus (EN 2390347, publ. 27.05.2010), a drug for the treatment of precancerous skin lesions (EN 2366447, 27.11.2007), health SUPPLEMENTS on the basis of grape seed extract (EN 2350125, publ. 27.03.2009) and other

Known pharmaceutical compositions on the basis of polyphenols, additionally comprising ascorbic acid (RU 2229303, publ. 27.05.2004; EN 2301666, publ. 27.06.2007), which has a strong antioxidant effect. Also known compositions, including retinol (beta-carotene - vitamin a-retinol), participating in Antioch identiy protection of the organism (EN 2350125, publ. 27.03.2009).

In addition, there are politieacademie composition for the prevention of iron deficiency anemia on the basis of iron compounds (RU 2005130673, publ. 10.04.2007) and means for slowing down the aging containing selenium (EN 2433819, publ. 20.11.2012). It is known that a lack of selenium can affect the development of cardiovascular diseases, atherosclerosis (Alissa E.M. et al., 2003), cancer, and immunity disorders (Seiler W.O., 2001), and the use of its drugs significantly reduces the risk of developing lung cancer (Reid M.E. Ter-Minassian, 2002).

Renowned pharmaceutical composition on the basis of polyphenols, blocking cancer cell proliferation and metastasis, used in the treatment of cancer (RU 2301666, publ. 27.06.2007). In the composition included at least one polyphenolic compound selected from the group consisting of Galata epigallocatechin, Galata epicatechin, epigallocatechin, epicatechin and catechin. Are polyphenolic compounds in green tea extract. Compositions also include ascorbic acid, lysine, Proline, salt, selenium, copper, magnesium. This song was adopted by the authors for the prototype.

The technical result of the invention is to provide a stable pharmacological geroprotective compositions based on polyphenolic component of humic substances that contain both low-solubility reorga the practical selenium compounds and iron, and hydrophobic organic substances (vitamin A).

This technical result is achieved by the fact that pharmacological geroprotective composition according to the invention contains humic acid containing polyphenolic components, vitamin C, vitamin a, iron chloride(II) and selenium dioxide(IV) in the following ratio, wt.%:

humic acid containing
polyphenolic components0,45-0,55
vitamin C0,009-0,011
vitamin A0,0045-0,0055
chloride iron(II)0,02-0,025
dioxide selenium(IV)0,0012-0,0015
restwater

The proposed composition differs from the prototype in that the sources of polyphenols are used humic acid derived from wood lignin (PA 2012 7059). This feedstock has a high cost of obtaining and high reproducibility of the chemical composition.

One of the most pronounced effects from the use of g is minovich acids, is to strengthen the overall immune response due to the presence of polyphenolic groups in their structure (Filov VA, Berkovich A.M. Humic substances: the use of their biological effects. Veterinary science. 2007. No. 8. P.14-17).

It is known that vitamin A (its precursor, beta-carotene and retinol) is a strong antioxidant, is involved in the metabolism of the organism.

It should be noted that the study of geroprotective effect in mice when introduced animals only one drug, in particular beta-carotene had no significant effect on life expectancy (H.R. Massie, J.R. Ferreira Jr., DeWolfe L.K. Effect of dietary beta-carotene on the survival of young and old mice // Gerontology. - 1986. - V.32, N.4. - P.189-195), however, in the experiments, when they were used so-called diet antioxidant mixture consisting of beta-carotene, alpha-tocopherol, ascorbic acid, rutin, selenium, and zinc - in hybrid mice when introduced with food, starting with a two-month age - effect was statistically significant compared with control mice, there was an increase mud (Bezlepkin V.G. et al., 1996).

Thus, studies on the evaluation of geroprotective properties of beta-carotene in mice indicate that beta-carotene has a certain gain other applicable supplements or components of the diet, there is General geroprotective properties.

There is also evidence of the ability of vitamin a and beta-carotene to increase the survival rate of mice CBA after gamma irradiation, if the drugs were injected 2 days after irradiation (Seifter E., Rettura, G., J. Padawer et al. Morbidity and mortality reduction by supplemental vitamin A or beta-carotene in CBA mice given total-body gamma-radiation // J. Natl. Cancer Inst. - 1984. - V.73, N.5. - P.1167-1177).

These results confirm the presence of vitamin A and beta-carotene antioxidant properties as well as evidence of ability to influence immune processes.

It is known that selenium is required for some of the biochemical mechanisms in the body and lowering its level in the blood can lead to the development of diseases such as cancer, cardiovascular diseases, and immunity (Seiler W.O. Clinical pictures of malnutrition in ill elderly subjects // Nutrition. - 2001. - V.17. - P.496-498).

Some animal studies have shown that selenium deficiency leads to death due to acute cardiovascular insufficiency, and impaired lymphocyte proliferation (Alissa EM, Bahijri S.M., Ferns GA The controversy surrounding selenium and cardiovascular disease: a review of the evidence // Med. Sci. Monit. - 2003. - V.9. - P. RA9-RA18). There are epidemiological data (although according to the authors still insufficient for a complete conclusion about the role of selenium), suggesting that the lack of selenium plays an important role in etiology the cardiovascular diseases, as well as in the development of atherosclerosis (Alissa E.M. et al., 2003).

A randomized clinical study on the effect of selenium have demonstrated a statistically significant reduction in the risk of lung cancer (Reid M.E. Ter-Minassian, Duffield-Lillico AJ, Garland L., B.W. Turnbull, L.C. Clark, J.R. Marshall Selenium supplementation and lung cancer incidence: an update of the nutritional prevention of cancer trial // Cancer Epidemiol biomarkers are Prev. - 2002. - V.11. - P.1285-1291).

It is known that iron is the main trace elements necessary to sustain the human body.

There is epidemiological evidence suggesting that age at assessment age level over 70 years of age) there was a decrease of iron content in the body in both men and women, leading to an increased risk of mortality, mainly from cardiovascular disease (Corti M. R., et al., 1997).

Also known to occur in the elderly trace element deficiency disease (reduced levels of iron in the body) cause the development of immunosupressed, as well as increase the likelihood of tumors, in particular multiple myeloma (Kudrin A.V., Rock AV, and other Immunopharmacology trace elements. M.: Izd-vo KMC. 2000. 537 S.).

Provides information about the interaction of dietary polyphenols and iron - as it turned out, polyphenols inhibit the absorption of heme iron is mainly due to the achieve the level basolateral yield of ions (Qianyi M Et al., 2010).

Research has helped to create pharmacological geroprotective composition on the basis of humic acids containing polyphenolic component, vitamin C, vitamin A, iron chloride(II), and selenium dioxide(IV) taking into account the properties and characteristics of the components described above.

The proposed composition contains both soluble inorganic compounds of iron and selenium, as well as hydrophobic organic substances (vitamin A).

To obtain the stability of the proposed composition method of its receipt by ultrasonic treatment to the components.

A method of obtaining anti-cancer drugs (EN 2102083, publ. 20.01.98), in which ultrasonic treatment is applied as pre-treatment medical lignin, part of the funds, and ultrasonic treatment is carried out with a radiation power 40±0.5 W, the oscillation frequency 22±0,5 kHz for 20-25 minutes.

A method of obtaining anti-cancer remedies based on coordination compounds of bivalent platinum and humic substances (EN 2368379, publ. 27.09.2009). According to this invention an aqueous solution containing humic substances, process coordination compound of platinum under the influence of ultrasonic radiation in the range is astot from 18 to 66 kHz with a power of 0.5 to 5 W/cm 3. When the output power 5 watts/cm3with a frequency of 22 kHz, the treatment is carried out within 5-20 minutes Method provides a more homogeneous and more stable during storage of the product. This method is chosen as a prototype.

However, all the methods described are not applicable to obtain a stable composition containing both soluble inorganic compounds and hydrophobic organic substances (vitamin A).

This technical result is also achieved by the fact that in the method of obtaining the proposed pharmacological geroprotective composition comprising processing the aqueous solution source of humic substances-compounds of metals with ultrasonic radiation, according to the invention an aqueous solution of the original humic acid containing polyphenolic components, is treated with iron chloride(II) and selenium dioxide(IV) the ultrasonic radiation power of 0.1-2 W/cm3with a frequency of 15 kHz for 5 minutes, then vitamin a at ultrasonic radiation power of 0.1-2 W/cm3with a frequency of 45 kHz for 2 minutes, and then vitamin C with ultrasound radiation power of 0.1-2 W/cm3with a frequency of 35 kHz for 0.5 minutes.

The invention is illustrated in the drawings, where:

figure 1 presents the dependence built in the coordinates: X - the life of animals in months, Y is the number of mice with regular astral cycles, % of total; curve 2 shows the results for the treated group geroprotective tool, curve 1 represents the results for the control group;

figure 2 presents the dependence built in the coordinates: X - the life of animals in months, Y is the number of individuals killed mice, in pieces; curve 2 shows the results for the treated group geroprotective tool, curve 1 represents the results for the control group;

figure 3 presents a diagram in which the value along the Y-axis represents the number of tumors in animals at the end of the experience; column 1 reflects the results for the control group, column 2 - the results for the group of animals treated geroprotective tool, the upper part of the column shows the number of breast tumors, and the lower - tumors at other sites.

The achievement of the technical result of the invention the following examples.

Example 1. Getting geroprotective products containing polyphenols, vitamins and mineral components in a single sonication.

Humic acid, 40% presents polyphenolic components in an amount of 5 g was dissolved in 1000 ml of distilled water at periodic stirring and constant heating to 50°C is for 0.5 hours. Next, to the solution was added iron chloride(II) in an amount of 225 mg, selenium dioxide(IV) in an amount of 1.4 mg, vitamin C (L-ascorbic acid) 100 mg vitamin a (oil solution of retinol)containing 50 mg of active ingredient, after which the solution was treated with ultrasound as described in the prototype (EN 2368379): if the radiation power 5000 watts with a frequency of 22 kHz for 10 minutes.

Further we investigated the chemical composition and stability obtained geroprotective tools (example 3).

Example 2. Getting geroprotective products containing polyphenols, vitamins and mineral components with three times sonication.

Humic acid, 40% presents polyphenolic components in an amount of 5 g was dissolved in 1000 ml of distilled water at periodic stirring and constant heating to 50°C for 0.5 hours. Next, to the solution was added iron chloride(II) in an amount of 225 mg and selenium dioxide(IV) in an amount of 1.4 mg, after which the solution was treated with ultrasonic radiation with a frequency of 15 kHz with a power of 2000 watts for 5 minutes. Then the solution was injected into vitamin A (oil solution of retinol)containing 50 mg of active substance under conditions of simultaneous processing of ultrasound with a frequency of 45 kHz at a power of 1000 watts for 2 minutes, and then centuries the Dili vitamin C (L-ascorbic acid) 100 mg and continued processing with a frequency of 35 kHz with a power of 2000 watts for 0.5 minutes.

Further we investigated the chemical composition and stability obtained geroprotective tools (example 3), and its specific activity (example 4).

Example 3. Studies of the chemical composition and the stability of the obtained geroprotective tools.

In the original humic substances by the method of mass spectrometry, ion cyclotron resonance Fourier transform (DDI FC MS) were identified following oligo - and polyphenolic components:

3 Benzoyloxy-4,5-dihydroxy-benzoic acid;

5-(furan-2-carbonyloxy)-2-methyl-benzofuran-3-carboxylic acid;

2,6-dimethyl-benzo(1,2-b,4,5-b')difuran-3,7-dicarboxylic acid;

5-(furan-2-carbonyloxy)-2-methyl-benzofuran-3-carboxylic acid;

Rhamnetin;

Methyl ((4-methyl-6-oxo-6-benzo(C)chromen-3-yl)oxy) acetic acid;

Sulogin;

2,6-Diacetyl-7,9-dihydroxy-8,9b-dimethylbenzofuran-1,3(2H,9bH)-dione;

Methyl 5-hyroxy-7,8-dimethoxy-1,3-dioxo-1,3,10,11-tetrahydrobenzo[5,6]cycloocta[1,2-c]furan-4-carboxylate;

(1-methoxy, carbonyloxy-6-oxo-6h-benzo(c)chromen-3-yloxy)-acetic acid;

Adrenalin;

Phenylpropanoid-substituted epicatechin and other

Obtained according to examples 1 and 2 geroprotective composition was characterized by the following composition (table 1).

That is person 1
IndexThe composition according to example 1The composition according to example 2
Humic acid containing polyphenolic components0,48%0,47%
0,2%0,2%
Vitamin C0,009%0,008%
Vitamin A0,004%0,005%

Iron0,01%0,009%
Selenium0,0001%0,0001%

The solutions obtained geroprotective compositions were placed in conditions of accelerated storage at 40°C to establish their stability. The results of the control of pH and the appearance of solutions in different periods of the study are presented below (table 2).

Table 2
PeriodThe composition according to example 1The precipitatepHThe precipitatepH
Day 0No7,0No7,2
Day 46Yes6,2No7,0
Day 91Yes5,9No7,1
Day 137Yes5,2No6,7
Day 183Yes4,8Yes6,1

It is revealed that geroprotective the composition according to example 2 has a higher stability.

Example 4. Study of specific actions geroprotective composition.

Geroprotective composition obtained in example 2, was tested in experiments in vivo to determine its toxicity and impact on life expectancy.

When breeding drugs is and soldering animals used tap water (2.5 ml of the original solution were added to 250 ml of water).

In the experiment 100 outbred female mice of line SHR 3 months of age (50 experimental and 50 control) with an average weight of 27 grams with fixed dates of birth. Mice constantly received drinking water geroprotective composition at a dose of 15 mg/kg daily. Control mice received tap water.

During the whole experience has not identified significant geroprotective effect of composition on the General condition of the animals, the dynamics of body weight and feed consumption. The data obtained indicate that in the studied dose of the drug did not produce any toxic effect.

Starting from 13.5 months of life in control mice was observed age-related disorders of the estrous function, expressed in the decrease in the relative frequency of regular cycles (Figure 1). At the same time, the experimental mice treated geroprotective composition, similar changes were noted. The differences (decrease in the frequency of regular cycles in the control group compared with experimental 20-25%) of 13.5 and 16.5-month-old mice was statistically reliable in nature. Thus, geroprotective tool helps to normalize the astral cycle.

For the whole observation period in the control and experimental groups fell by 50 animals (100% of the original quantity). The average lifespan of mice amounted to:in control - 578,0±13,85 days; in the experimental group 621,0±17,21 day (compared with control, p<0,05) (Figure 2). Thus, geroprotective composition significantly increases the lifespan of mice.

Tumors in the control group were found in 33 of mice and experience - 19 mice. Primary tumors in animals of both groups were neoplasms of the mammary glands. In control they are found in 23 mice in the experimental group in 13 animals (p<0,05) (Figure 3). All the tumors were isolated, with the exception of two mice in the control group, which emerged from the two neoplasms of the breast. The first tumor in mice detected later than in control - at the age of 338 days. The average latent period in the detection of breast tumors was in control - 461±21,97 day, and in the experimental group was 510±27,15 day. Thus, in mice treated geroprotective composition, neoplasms of the mammary gland were found later and less frequently than in the control.

The proposed pharmacological geroprotective the composition has a stability thanks to its preparation and can be used as a means of increasing life expectancy and slow down the development of tumors.

1. Pharmacological geroprotective composition comprising polyphenolic component, vitamins and trace elements, characterized in that the composition is I contains humic acid, containing polyphenolic components, vitamin C, vitamin a, iron chloride(II) and selenium dioxide(IV) in the following ratio, wt. %:

humic acid containing
polyphenolic components0,45-0,55
vitamin C0,009-0,011
vitamin A0,0045-0,0055
chloride iron(II)0,02-0,025
dioxide selenium(IV)0,0012-0,0015
restwater

2. The method of obtaining pharmacological geroprotective composition according to claim 1, comprising processing the aqueous solution source of humic substances-compounds of metals with ultrasonic radiation, characterized in that the aqueous solution source of humic acids containing polyphenolic components, is treated with iron chloride(II) and selenium dioxide(IV) the ultrasonic radiation power of 0.1-2 W/cm3with a frequency of 15 kHz for 5 minutes, then vitamin a at ultrasonic radiation power of 0.1-2 W/cm3with a frequency of 45 kHz for 2 mine is, and then vitamin C with ultrasound radiation power of 0.1-2 W/cm3with a frequency of 35 kHz for 0.5 minutes.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of general formula (I) or pharmaceutically acceptable salts thereof, where Alk is an C1-C6alkyl group; G is C=O and Q is CR51R52 or NR51, where R51 and R52, being identical or different, independently denote H, C1-C6alkyl, optionally substituted with a substitute selected from a group comprising carboxy, phenoxy, benzyloxy, C1-C6alkoxy or hydroxy; C3-C6cycloalkylC1-C6alkyl; phenylC1-C6alkyl, optionally substituted with a halogen; phenylamidoC1-C6alkyl; phenylC1-C6alkylamidoC1-C6alkyl, optionally substituted with a C1-C6alkoxy group; or R51 and R52, together with a carbon atom with which they are bonded form a C=O or C2-C6alkenyl group, optionally substituted with a phenyl; M1 is CR49, where R49 is H; M2 is CR50, where R50 is H; R38 is H, C1-C6alkyl, substituted with a phenoxy group; C3-C6cycloalkylC1-C6alkyl; arylC1-C6alkyl, optionally substituted with 1 or 2 substitutes selected from a group comprising C1-C6alkyl, C1-C6alkoxy, C1-C6alkoxycarbonyl, carboxyl, N-methylamido, hydroxy, C1-C6alkoxyC1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulphanyl, cyano, halogen, perfluoroC1-C6alkyl, nitro, formyl, hydroxyC1-C6alkyl and amino, wherein the aryl moiety is a phenyl or naphthyl; and heteroarylC1-C6alkyl, where the heteroaryl moiety is pyridinyl, optionally substituted with 1 or 2 groups selected from C1-C6alkoxy or hydroxyC1-C6alkyl, pyrazolyl or isoxazolyl, substitute with 1 or 2 C1-C6alkyl groups; R47 and R48 is C1-C6alkyl. The invention also relates to specific compounds, a method of reducing or weakening bitter taste, a composition of a food/non-food product or beverage or drug for reducing or lightening bitter taste and a method of producing a compound of formula (I).

EFFECT: obtaining novel compounds which are useful as bitter taste inhibitors or taste modulators.

37 cl, 6 dwg, 12 tbl, 186 ex

FIELD: medicine.

SUBSTANCE: halogen-containing hydrocarbonate chloride sodium, alkaline, boron high-magnesium, iodine and fluorine natural mineral water 'Lazarevskaya Tselebnaya' No. 84-E of the Volokonskoye deposite in Sochi is taken according to the following procedure: 30-35 minutes before meals in small sips, six times a day daily in a dose of 200-250 ml at t°=(23-24)°C, for 45 days every 2-3 days with taking the above natural halogen-containing mineral water in the same volumes for the following 45 days. The therapeutic course makes 3 years.

EFFECT: method enables improving the health status in the individuals subject to the hazardous effect of radionuclides taken with water or food.

2 cl, 6 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: food ration is added with multi-component natural concentrated food products (NCFP) with high concentrations of biologically active substances (BAS) of herbal (HNCFP) and (or) protein-herbal (PHNCFP) raw material, for the purpose of nutritional support of sportsmen doing various sports, their individual physiological requirements; that results in recovering a set of characteristics of physiological functions and qualities determining a degree of activity of morphofunctional body systems, activities of daily living and professional performance, with providing preventing donozological and pathological conditions, achieving high sport scores. The above food products can be presented by NCFP Antitox and NCFP SportAtiv-2.

EFFECT: invention provides easier exercise tolerance and recovery thereafter, improving health in sportsmen.

5 cl

FIELD: medicine.

SUBSTANCE: method involves preliminary intraperitoneal single administration of 5% aqueous alloxan in a dose of 15 mg/kg of body weight into a rat's body on an empty stomach. That is followed by administering afobazol under conditions of oxidative stress after observing the rat's blood glucose gain at least twice. Afobazol is administered subcutaneously in a dose of 10 mg/kg of body weight once a day for 30 days with underlying administration of L-arginine in a dose of 10 mg/kg of body weight or with underlying NG-nitroarginine methyl ester (L-NAME)-inhibitor of NOS-3 enzyme in a dose of 25 mg/kg of animal's weight.

EFFECT: method enables correcting the oxidative stress and NO-producing endothelial dysfunction accompanying vascular complications of diabetes mellitus.

1 dwg, 6 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to rehabilitation medicine and concerns prevention of meteopathic reactions. That is ensured by administering an adaptogene agent presented by a phytococktail containing mixed 70% tinctures of eleuterococcus, common licorice and rhodiola rosea in the ratio of 2:1:1. The cocktail is introduced in a dose of 10-15 drops for two weeks once a day, taking into account an individual's chronotype. That is followed by a magnetic-infrared-laser exposure covering the acupuncture points Tr(X)5 - Wai Guan, E(III)36 - Zuo San Li, Tr(X)15 - Tian Liao and MC(IX)5 - Jian Shi through an applicator wetted in the phytococktail containing 70% alcoholates of rhodiola rosea, common licorice, yellow starwort and spiny eleuterococcus in the ratio of 2:2:1:1, in a combination with an aromatherapy with Atlas cedar oil.

EFFECT: integrated exposure in the developed mode provides higher non-specific body resistance to meteorological factors.

2 ex, 3 tbl, 8 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented: using a compound of formula (1) or its salt for preparing a drug for increasing HIF-1α stabilisation in a cell, as well as for preparing a drug enhancing the immune response in an individual, for preventive management of a wound to avoid an infection, for treatment of the microbial infection, for improvement of efficacy of a vaccine for management of the wound in the individual. What is presented is a pharmaceutical composition containing the above HIF-1α prolyl hydroxylase inhibitor and one or more additives. What is shown is achieving the declared applications by using the new compound of formula (1) with the HIF-1α prolyl hydroxylase (HIFPH2 (EGLN1)) inhibitor. It makes it applicable for treating HIF-1 alpha activity related diseases, conditions and/or syndromes.

EFFECT: preparing the drug for increasing HIF-1α stabilisation in a cell.

26 cl, 20 dwg, 8 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: what is used is a 20% alcoholic tincture (1:10) of medicinal herbs in the following weight proportions: Rhaponticum carthamoides roots and rhizomes - 2, tormentil roots - 1, peppermint leaves - 3. A mouthwash is prescribed before a dentist's appointment for 3-4 days 3 times a day, as well as 10-15 minutes before an impression manipulation.

EFFECT: method provides reducing intensity a gag reflex accompanying dental manipulations.

FIELD: medicine.

SUBSTANCE: what is presented is a method for stimulating the post-traumatic spinal cord regeneration consisting in a single-stage transplantation of human umbilical cord blood mononuclear cells pre-transduced with recombinant adenovirus with a cloned gene of glial derived neurotrophic factor (gdnf), in the damage area.

EFFECT: using the invention enables providing a better outcome of the post-traumatic spinal cord regeneration, reduced length of staying in hospital of patients suffering from a spinal cord injury and improving the patients' quality of life.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a pharmaceutical composition for dehydration, atrophy and removal of abnormal tissues, and to using it. The pharmaceutical composition for dehydration, atrophy and removal of abnormal tissues contains a composite of an inorganic polymer iron salt as an active ingredient; the composite of the inorganic polymer iron salt is polymer ferrous sulphate silicate (PFSS), or polyferrous silicate chloride (PFSC), or polyphosphate ferrous sulphate (PPFS). Using the pharmaceutical composition consists in preparing the drug for dehydration, atrophy and removal of abnormal tissues.

EFFECT: pharmaceutical composition is effective for dehydration, atrophy and removal of abnormal tissues in treating haemorrhoids, haemangiomas, varicose veins, burns, bleeding traumatic wounds, local wounds caused by chemicals or microorganisms.

9 cl, 12 dwg, 2 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine and can be used for modification of eating behaviour in a subject. For this purpose peripheral introduction of PYY in an amount, efficient for achieving physiological levels of PYY3-36 in blood, plasma and serum, determined after food intake, is performed; or performed is peripheral introduction of PYY agonist in an amount, efficient for imitation of physiological levels of PYY3-36 in blood, plasma or serum, determined after food intake with modification of eating behaviour, by reducing intake of calories, food consumption or appetite reduction or increase of energy consumption in the subject. Also claimed is application of PYY or its agonist as an active ingredient in production of medication.

EFFECT: group of inventions provides weight reduction in the subject due to reduction of intake of calories, appetite reduction or increase of energy consumption in the subject.

50 cl, 9 dwg, 6 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, genetic engineering and molecular biology. What is presented is a method for monitoring breast cancer in an individual. The method involves determining an expression ratio of the paired box 2 gene to beta defensin-1 gene (PAX2-to-DEFB1) in the cells produced from the individual's breast with the PAX2-to-DEFB1 expression ratio correlating with the breast conditions. What is also presented is a kit for monitoring breast cancer.

EFFECT: invention can be used in medicine in treating and monitoring cancer.

10 cl, 40 dwg, 8 tbl, 17 ex

FIELD: medicine.

SUBSTANCE: invention refers to a new agent representing rhodanine derivatives of formula (I), wherein X=N or CH for treating malignant diseases of varying sites.

EFFECT: agent is antiproloferative and antimetastatic action for treating malignant diseases.

3 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of organic chemistry, namely to compounds of the general formula I , and its pharmaceutically acceptable salts, where R1, R2 and R3 represent hydrogen, D, E, G, J and L represent CH; n equals to an integer number 1 or 2; W represents oxygen; R4 represents C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkenyl, where the said C1-6alkyl is possibly substituted with one substituent, independently selected from a group, consisting of hydrogen, C1-4alkyl, C3-6cycloalkyl and C3-6cycloalkenyl; Y represents carbonyl; R5 represents C1-6alkyl, C1-6alkoxy or C3-4heteroaryl, which represents a heterocyclic aromatic ring, containing 1-2 heteroatoms, selected from nitrogen and oxygen. The invention also relates to a pharmaceutical composition based on a formula I compound, application of the formula I compound and a method of prevention, treatment of alleviation of a disease, associated with abnormal angiogenesis.

EFFECT: obtained are novel compounds useful in treatment of diseases associated with unregulated angiogenesis, such as cancer, as well as skin and eye diseases.

13 cl, 3 tbl, 11 ex

FIELD: biotechnology.

SUBSTANCE: method comprises isolation of mononuclear cells (MNC) from peripheral blood of a patient, separation of cells to adherent and non-adherent fractions, addition of the adherent fraction to the MNC of growth factors, loading of the dendritic cell with antigens of tumour lysate in vitro, the stimulation of maturation of dendritic cells for the next day. At that, the obtained immature DCs are added to lysate-autologous tumour cells at a dose of 100 mcg/ml, and after 48 hours within the subsequent 24 hours the rf-tumour necrosis factor-alpha is applied at a dose of 25 ng/ml. Then, the co-culture is carried out of mature dendritic cells activated with lysate and the non-adherent fraction of MNC at a ratio of 1:10 in the presence of recombinant human interleukin-12 at a dose of 10 ng/ml and the recombinant human interleukin-18 at a dose of 100 ng/ml.

EFFECT: invention enables to improve the level of cytotoxic and interferon-producing activity of antigen-activated dendritic cells while reducing the duration of their culture.

4 tbl

FIELD: medicine.

SUBSTANCE: invention concerns an agent for preventing malignant diseases representing rhodanine derivatives of general formula (1) .

EFFECT: high efficacy.

1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a solid pharmaceutical product for oral administration which contains a photosensitiser representing a compound of general formula I:

wherein R1 represents a substituted or unsubstituted unbranched, branched or cyclic alkyl group, and each R2 independently represents a hydrogen atom or optionally a substituted alkyl group or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable carrier or excipient. The above pharmaceutical product is presented in the form of a tablet, a pill or a capsule having an enteric and gastroresistant coating, or in the form of the tablet or the capsule containing a number of balls, drops, granules or mini-pills with an enteric and gastroresistant coating. The above coating disintegrates in the lower gastrointestinal tract. The invention also refers to using the above photosensitiser in preparing the solid pharmaceutical product applicable in photodynamic treatment or diagnostics of a cancer condition in the lower gastrointestinal tract. What is also described is a photodynamic method of treating or diagnosing the cancer condition in the lower gastrointestinal tract by administering the solid pharmaceutical product containing the photosensitiser.

EFFECT: invention provides photosensitiser delivery to the lower gastrointestinal tract, and homogenous distribution of the photosensitiser in the target region, thereby improving the response to photodynamic treatment or diagnostics.

20 cl, 2 dwg, 2 tbl, 54 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a method for preparing an anticancer vaccine agent for treating solid tumours. The method for preparing the anticancer vaccine agent for treating solid tumours consisting in sampling of a raw tumour material, mixing and homogenisation in a buffer solution, multiple centrifugation with residue sampled; the residue is suspended in an acid buffer, mixed, neutralised, centrifuged; the supernatant is collected, enriched and purified with a combination of salt deposition and chromatography on an immobilised protein A or G; the prepared solution is passed through columns with immobilised human immunoglobulins IgG and human placental immobilised proteins; the prepared antibodies are subject to enzymatic treatment to prepare Fab- or F(ab)2-fragments used to immunise animals; immune antibodies are prepared and used to recover the total immunoglobulin fraction to be passed through the columns with the immobilised human immunoglobulins IgG and immobilised human placental proteins; the solution passed through the columns is subject to immunoaffinity chromatography on the columns with immobilised immunoglobulins prepared earlier at the stage of purification and enrichment; the end products specifically bound by the latter types of the columns are eluted with a solution dissociating antigen-antibody complexes, concentrated, filtered through antimicrobial filters, mixed with an adjuvant.

EFFECT: preparation prepared by the method described above enables providing higher clinical effectiveness in solid tumours treatment.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide and its salts, such as hydrobromide, hydrochloride, methane sulfonate, ethane-1,2-disulfonate. The invention also relates to a medication and a pharmaceutical composition based on the said compound and its salts for inhibition of ATP-ase activity of HSP90.

EFFECT: novel compound and its salts, which can be applied in medicine for cancer treatment, are obtained.

23 cl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to biotechnology and represents an oncolytic adenoviral vector, a cell and a pharmaceutical composition containing the above vector, as well as applications of the above vectors in preparing a drug for treating cancer in an individual, and to a method of treating cancer in the individual. The presented invention may be used for treating cancer. The oncolytic adenoviral vector contains a nucleic acid skeleton of serotype 5 adenovirus (Ad5), deletion in 24 nucleotides related to amino acids 122-129 in E1A constant region 2, and a nucleic acid sequence coding the human granulocyte-macrophage colony-stimulating factor (GM-CSF) in a site of deleted gp19k/6.7K in the region E3, and capside modification if needed.

EFFECT: invention provides improving the tumour-specific immune response in the individual.

40 cl, 36 dwg, 10 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a pharmaceutical composition for dehydration, atrophy and removal of abnormal tissues, and to using it. The pharmaceutical composition for dehydration, atrophy and removal of abnormal tissues contains a composite of an inorganic polymer iron salt as an active ingredient; the composite of the inorganic polymer iron salt is polymer ferrous sulphate silicate (PFSS), or polyferrous silicate chloride (PFSC), or polyphosphate ferrous sulphate (PPFS). Using the pharmaceutical composition consists in preparing the drug for dehydration, atrophy and removal of abnormal tissues.

EFFECT: pharmaceutical composition is effective for dehydration, atrophy and removal of abnormal tissues in treating haemorrhoids, haemangiomas, varicose veins, burns, bleeding traumatic wounds, local wounds caused by chemicals or microorganisms.

9 cl, 12 dwg, 2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: method of obtaining a reagent for preparation of a radiopharmaceutical based on technetium-99m-labelled ciprofloxacin consists in preparation of a hydrochloric acid solution of tin (II) chloride dehydratate with tin concentration 7 mg/ml by careful mixing of 0.07 mg of tin (II) chloride dehydratate and 0.2 ml of 1M hydrochloric acid and carrying out dissolution in an inert gas (argon) medium with further bringing the volume to 10 ml with distilled water after completion of dissolution, sampling 0.015-0.025 ml of the prepared solution and its mixing with 5-6 mg of a ciprofloxacin hydrochloride substance, the obtained solution is frozen at a temperature of liquid nitrogen, placed in a sublimator chamber and subjected to freeze drying at specified parameters of lyophiliser: T=-50°C, vacuum - 0.0015 Torr, for 20.5 hours, with further placement in the upper lyophilic chamber and after-drying for 5.5 hours at a temperature of+15°C.

EFFECT: increased term of the reagent application time due to increase of its stability.

1 dwg, 1 tbl, 1 ex

Up!