Hypolipidemic phytoagent

FIELD: chemistry.

SUBSTANCE: invention relates to application of dry extract of aronia melanocarpa as hypolipidemic agent. Claimed extract is obtained by double extraction with 95% ethanol, acidified with hydrochloric acid, at heating on water bath.

EFFECT: claimed invention ensures obtaining agent with expressed ability to reduce level of triacylglycerols, total cholesterol and cholesterol in atherogenic lipoproteins of low density in blood serum.

3 tbl, 3 ex

 

The invention relates to medicine, specifically to pharmacology, and relates to vegetable drugs affecting lipid metabolism, which can be used to normalize cholesterol metabolism, prevention and treatment of atherosclerosis.

Known synthetic means (Lovastatin, Simvastatin, Cerivastatin, Clofibrate, Fenofibrate), affecting lipid metabolism - reduce the content of atherogenic lipoproteins (LDL and VLDL) in patients, while increasing the content of high density lipoprotein (HDL) [2, 4]. These drugs directly intervene in the different stages of lipid metabolism in the liver cells, but also can influence the metabolism of these substances in the cells of other organs and systems of the muscle cells of the cortical layer of kidneys, the nervous fibers. The purpose of these drugs should be undertaken only after a thorough examination of the patient and treatment must be accompanied by the control of the laboratory of lipid metabolism. Such tools include nicotinic acid is a drug traditionally prescribed for patients with atherosclerotic vascular lesion, regardless of the localization.

Also known hypolipidemic agents based on vegetable raw materials, for example, the drug "Tribusponin" containing the amount of steroid saponi�s of the herb Tribulus terrestris [2], product containing a concentrate of triterpenic acids obtained from the meal of sea-buckthorn berries (patent RU №2394587, publication date 20.07.2010), a means of having anorexicas, hypoglycemic, hypolipidemic action, which is an aqueous extract of black and brown leaf bergenia Bergenia crassifolia (patent RU 2409379, publication date 20.01.2011), means "melon oil" (application for invention No. 2002101439, publication date 27.09.2003), medium containing dry beet juice and dry extracts of corn silk, peppermint, rosehip cinnamon and horsetail (patent RU №97114385, publication date 27.02.2009), camelina oil (patent RU №2246964, publication date 27.02.2005), a tool based on the medicinal plants of clover, lovage and alfalfa (patent RU №2242986, publication date 27.12.2004), syrup, containing ethanolic extract of the leaves of plantain (patent RU №2144830, publication date 27.01.2000), "Petromin" - extract triterpene glycosides-patrimonito D, b and C, obtained from the roots of patrinia average (patent RU №2189241, publication date 20.09.2002). Also known biologically active food supplements: the herbal collection crushed for medicinal plant materials, comprising: the root of Dioscorea Caucasian, herb of Tribulus terrestris, the flowers of red clover, mistletoe shoots, BlackBerry leaves, black currant leaves, grass soul�s, caraway fruits (patent RU №2472360, publication date 20.01.2013 G.); the powder of the leaves of the walnut (patent RU №2399316, publication date 20.09.2010), crushed grape seeds (patent RU №2302137, publication date 10.07.2007), the powder from the husks pumpkin (patent RU №2302132, publication date 10.07.2007), powder of tomato pomace (patent RU №2360449, publication date 10.07.2009), collection of medicinal plants containing Senna leaves, bearberry leaves, mint leaves, grass motherwort, grass series and rosehips (patent RU №2150287, publication date 10.06.2000).

The list of lipid-lowering drugs of vegetable origin is limited, while they are the most promising in the treatment and prevention of diseases associated with atherosclerosis. Herbal medicines have a lower toxicity compared to synthetic drugs and long-term use, often without significant side effects [5].

The closest to the proposed is the drug "Polisponin", dry extract of rhizomes and roots of Dioscorea nipponskoy [2]. Hypocholesterolemic effect which is due to the inhibition of cholesterol absorption in the intestine. Hypocholesterolemic effect "Polisponina" small, in addition, binding bile acids in the intestine and preventing their suction�Oia, "Polisponin" violates the absorption of lipids and fat-soluble vitamins, especially vitamin K, and folic acid, which limits its use for prevention of cardiovascular diseases. While the extract of chokeberry has the ability to reduce the levels of triacylglycerols, total cholesterol and cholesterol in atherogenic LDL in the serum, allowing it to be used for prevention and complex treatment of such cardiovascular diseases as coronary heart disease, myocardial infarction, the risk of which is largely determined by a high content of cholesterol, low-density lipoprotein and low - high density lipoproteins and to a lesser extent, increased total cholesterol and triglycerides.

A new technical task is to expand the Arsenal of lipid-lowering agents of plant origin.

To solve this problem as gipolipedimecescoe means use dry extract of chokeberry (Aronia melanocarpa), obtained by the method of twofold extraction with 95% ethanol, acidified with hydrochloric acid.

Fruits chokeberry Aronia (black chokeberry) (Aronia melanocarpa (Mich.) Elliot), SEM. Rosaceae are officinal medicinal raw materials. Pills "Aronia+C, sleeper�GIEZ fruits and Aronia juice, providing adaptogenic, antispasmodic, hypotensive, diuretic, choleretic, C - and P-vitamin activity, prescribed for the prevention of P-vitamin deficiency, treatment of hypertension stage I and II and other diseases associated with increased blood pressure [2, 7].

Chokeberry juice can be a potential cardioprotective and anti-diabetic agent, it has strong antioxidant properties [10], bioactivating powder of chokeberry has hepatoprotective activity [8], the leaves of chokeberry have pronounced antioxidant activity [1].

New in the present invention is that the dry extract of chokeberry (Aronia melanocarpa), obtained by the method of twofold extraction with 95% ethanol, was first proposed as lipid-lowering drugs.

The use of plants of the genus Aronia Aronia, specifically of chokeberry (A. melanocarpa), as hypolipidemic agents in the known sources of information are not described. Application for a new appointment was made possible thanks to the discovery of his new properties, namely the ability to reduce the levels of triacylglycerols, total cholesterol and cholesterol in atherogenic LDL. This property is not explicitly derives to a person skilled in the art. Ethanolic extract and�Onias chokeberry (A. melanocarpa) can be used for the normalization of lipid metabolism, prevention and treatment of atherosclerosis. Thus, the proposed technical solution meets the criteria of "novelty" and "inventive step", "industrial applicability".

New properties of alcoholic extract of chokeberry (A. melanocarpa) were detected due to recent experimental studies.

For research was used the extract from the fruits of chokeberry (A. melanocarpa), obtained using as the extractant of 95% ethyl alcohol, acidified with hydrochloric acid.

To extract plant material was subjected twice to extraction with 95% ethanol, acidified with hydrochloric acid by heating on a water bath, the extract was combined.

The liquid extract was evaporated under vacuum (30-40 mm Hg.CT.) at temperatures above 45°C on a rotary evaporator type IR-LT to a moisture content of not more than 40%. Bring the moisture up to the standard value (25%) carried out in a vacuum drying Cabinet type "MSS-45K" at a temperature not exceeding 45°C.

To establish the hypolipidemic properties of the extract of chokeberry conducted three series of experiments. To evaluate the hypolipidemic effect of the extract of chokeberry, we used a model of�Troy Moyle, reproduced in experimental animals by injection of Triton WR 1339, a non-ionic detergent. This model is characterized by ease of play, low toxicity of Triton and the dependence of the effect on the concentration of detergent allows you to play hyperlipidemia varying severity [3].

The experiments were performed on 24 albino male rats weighing 280-320 g, obtained from the kennel "Dawn" (Tomsk).

The animals were housed under standard conditions in a natural light mode, with free access to water and food (the temperature in the vivarium of 20±2°C, humidity - less than 80%). Feeding the animals was carried out by the special granules with mineral and vitamin additives "Feed for laboratory rats of closed joint stock company "Biopro" (Novosibirsk).

The content and all manipulations inflicted on animals during the quarantine and study was in accordance with the rules of laboratory practice, approved by the decree of the Minister of health and social development dated 23 August 2010 no n "On approval of rules of laboratory practice, as well as with the observance of the Convention for the protection of vertebrate animals used for experimental and other scientific purposes, adopted by the European Union in 1986, and Directive 86/609 EEC, based on the text of the agreement�of "Dr. Robert Hubrecht, Current EU LegislationControllingAnimalExperiments".

To reproduce a model of acute hyperlipidemia rats were intraperitoneally injected with the detergent Triton WR 1339 at a dose of 200 mg/kg, dissolved in 0.9% NaCl solution. After 24 hours the rats were killed CO2-asphyxia using a standard camera. The obtained blood was centrifuged at 1500 g for 15 min in a centrifuge CM-6M and the serum was determined the content of triacylglycerols (TAG), total cholesterol (LDL) and cholesterol in the lipoproteins (LDL-cholesterol) and high (HDL-cholesterol) density by using enzymatic kits.

The triacylglycerols and cholesterol were determined using enzymatic kits "Triglycerides" (code 101-0052) and "Cholesterol" (code 101-0051) company Chronolab (Spain) according to the protocols supplied with the kits. Cholesterol in lipoproteins of low and high density was determined by direct enzymatic colorimetric method using kits "LDLCholesterol" (code 101-0516) and HDLCholesterol" (code 101-0597) company Chronolab (Spain). Based on the obtained experimental data was computed atherogenic index (AI) according to the formula: IA=(XC-HDL-XC/HDL-cholesterol [9].

The research results presented in examples 1-3.

Example 1. Injection of Triton WR 1339 at a dose of 200 mg/kg to rats helps increase the level of TAG in the serum of animals after 24 hours at 29 times (p<0.01), total cholesterol 3 times (p<0.01) and cholesterol in the atherosclerotic�the military low-density lipoprotein 9-fold (p< 0,01) (tab.1). While the atherogenic index (AI) was increased from 0.99±0,1 to 2.86±0,36 (p<0.01). Sharp increase in the level TAG and cholesterol after a single dose of Triton illustrates the marked hyperlipidemia. It is known that detergent WR 1339 inhibits the activity of lipoprotein lipase, which prevents the utilization of lipoproteins and promotes the accumulation of TAG and cholesterol in the serum of experimental animals [6]. (Table 1 - Effect of Triton WR 1339 (200 mg/kg) on the content of triacylglycerols (TAG), total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m)

Example 2. Pre-course administration of the drug comparison of phenofibrate ("Tricor, France) at a dose of 100 mg/kg as a solution in 0.5% starch mucus within 7 days significantly reduced the level TAG by 83.6% (p<0.01), HDL by 65.1% (p<0.01) and cholesterol in atherogenic LDL by 82.1% (p<0.01) in the serum of experimental animals on the background of the development of acute hyperlipidemia induced by administration of Triton WR 1339. Atherogenic index compared to a drug of phenofibrate with hyperlipidemia induced by detergent WR 1339, decreased significantly with 2,86±0,36 to 0.84±0,1 (p<0.01) (table.2).

Thus, the reference drug fenofibrate ("Tricor, France) at a dose of 100 mg/kg in a model of acute hyperlipidemia, inducere�the auditors injection of Triton WR 1339, has a strong lipid-lowering effect. (Table 2 - effects of exchange rate of drug administration comparison of phenofibrate (100 mg/kg for 7 days) on the content of triacylglycerols (TAG total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m) * - the difference is significant in comparison with the control group, p<0.01)

Example 3. Preliminary course the introduction of the extract of chokeberry (150 mg/kg) as a solution in 0.5% starch mucus within 7 days significantly reduced the level of the TAG to 50.8% (p<0.01), HDL 24.1% (p<0.01) and cholesterol in atherogenic LDL 79.8% (p<0.01) in the serum of experimental animals on the background of the development of acute hyperlipidemia induced by administration of Triton WR 1339. Atherogenic index for extract of chokeberry with hyperlipidemia induced by detergent WR 1339, decreased significantly with 2,86±0,36 to 2.0±0,27 (p<0,05) (tab.3).

Thus, the extract of chokeberry in the dose of 150 mg/kg in a model of acute hyperlipidemia induced by injection of Triton WR 1339, like the comparison drug has hypolipidemic effect, has the ability to reduce the levels of triacylglycerols, total cholesterol and cholesterol in atherogenic LDL in the serum, allowing it to be used for the prevention and composed.�eautiful treatment of such cardiovascular diseases, as coronary heart disease, myocardial infarction, the risk of which is largely determined by a high content of cholesterol, low-density lipoprotein and low - high density lipoproteins and to a lesser extent, increased total cholesterol and triglycerides. (Table 3 - Impact of foreign exchange administration of an extract of chokeberry (150 mg/kg for 7 days) on the content of triacylglycerols (TAG total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m), * - the difference is significant in comparison with the control group, p<0.01; ** - difference is significant in comparison with the control group, p<0,05).

Thus, the extract of chokeberry has the ability to reduce the levels of triacylglycerols, total cholesterol and cholesterol in atherogenic LDL in serum, which makes the perspective of its use for the prevention and complex treatment of such cardiovascular diseases as coronary heart disease, myocardial infarction; risk of development of which is largely determined by a high content of cholesterol, low-density lipoprotein and low - high density lipoproteins and to a lesser extent, increased total cholesterol and triglycerides.

Sources of information

1. �patova O. M., The Prozorovsky N. N., Rusina I. F., Prozorovsky V. N. The antioxidant properties of leaf extract of chokeberry (Aronia melanocarpa) containing proanthocyanidins. // Biomedical chemistry. 2003. - No. 2. Pp. 165-176.

2. The state register of medicines. Official edition in 2 vols: the Medical Council, 2009. - Vol. 2, part 1 - with 568; part 2 - 560C.

3. Korolenko T. A. Changes in the fractional composition of lipoproteins of serum in mice and rats when lipemia caused by Triton WR 1339 / T. A. Korolenko, V. F. tuzi, E. D. Vasil'eva, M. S. Cherkasova, N. And. Tuzikov // Bulletin of experimental biology and medicine. - 2010. - T. 149. - No. 5. - Pp. 499-502.

4. Mashkovsky M. D. Medicines: a guide for physicians: in 2 volumes / M. D. Mashkovsky. - Kharkov: Torsing, 1997. - 560 p.

5. Pashinsky V. G. Plants in the treatment and prevention of diseases / Pashinsky V. G.; Institute of pharmacology, Tomsk scientific centre SB RAMS (Tomsk). - Tomsk: Publishing house of Tomsk University, 1989. - 206 p.

6. Manual on experimental (preclinical) study of new pharmacological substances / under the editorship of R. W. overall mechanism. - M.: Medicine, 2005-832 S.

7. Drug reference "VIDAL" [Electronic resource]: a Description of the medicinal product "Tanakan" URL: http://www.vidal.ru/poisk_preparatov/tanakan.htm.

8. L. V. Savchenkova, Rokitansky V. V. Evaluation of hepatoprotective activity bioactivating powder of chokeberry. // Actual PR�problems of science pharmaceutical and medical universities: materials of scientific-practical conference. Perm. - 2011. - P. 145-149.

9. Haglund o, Luostarinen, R., Wallin, R. The effects of fish oil on triglycerides, cholesterol, fibrinogen and malondialdehyde in humans supplemented with vitamin E. // J. Nutr . - 1991. - V. 121. - P. 165-169.

10. Mayer-Miebach, E., Adamiuk, M., Behsnilian D. Stability of Chokeberry Bioactive Polyphenols during Juice Processing and Stabilization of a Polyphenol-Rich Material from the By-Product / Agriculture. - 2012. - No. 2. - C. 244-258.

Application

Table 1 - Effect of Triton WR 1339 (200 mg/kg) on the content of triacylglycerols (TAG), total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m) * - the difference is significant in comparison with the control group, p<0.01.

Table 2 - effects of exchange rate of drug administration comparison of phenofibrate (100 mg/kg for 7 days) on the content of triacylglycerols (TAG total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m) * - the difference is significant in comparison with the control group, p<0.01.

Table 3 - Impact of foreign exchange administration of an extract of chokeberry (150 mg/kg for 7 days) on the content of triacylglycerols (TAG total cholesterol (LDL), cholesterol in lipoproteins of high (HDL-cholesterol), low (LDL-cholesterol) density and atherogenic index (IA), (X±m) * - the difference is significant in comparison with the control group, p<0.01; ** - difference is significant in comparison with the control group, p<0,05.

Table 1
The determined parametersThe study group
Control (n=8)Triton WR 1339 (n=8)
TAG, mmol/l0,84±0,1324,27±2,96*
Cholesterol, mmol/l2,13±0,196,35±0,67*
HDL-cholesterol, mmol/l1,08±0,071,76±0,24*
LDL-cholesterol, mmol/l0,21±0,021,9±0,29*
IA0,99±0,12,86±0,36*

Table 2
The determined parametersThe study group
Triton WR 1339 (n=8)Fenofibrate (Tricor) (n=8)
TAG, mmol/l24,27±2,963,98±0,32*
Cholesterol, mmol/l 6,35±0,672,21±0,14*
HDL-cholesterol, mmol/l1,76±0,241,21±0,06*
LDL-cholesterol, mmol/l1,9±0,290,34±0,01*
IA2,86±0,360,84±0,1*

Table 3
The determined parametersThe study group
Triton WR 1339 (n=8)Extract + Triton WR 1339 (n=8)
TAG, mmol/l24,27±2,9611,94±1,93*
Cholesterol, mmol/l6,35±0,674,82±0,5**
HDL-cholesterol, mmol/l1,76±0,241,6±0,11
LDL-cholesterol, mmol/l1,9±0,290,76±0,03*
IA2,86±0,362,0±0,27**

The use of a dry extract of chokeberry (Arona melanocarpa), obtained twofold extraction with 95% ethanol, acidified with hydrochloric acid, when heated in a water bath, as lipid-lowering drugs.



 

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2 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to nanoparticles for encapsulating biologically active compounds. The nanoparticle contains a casein matrix, a basic amino acid and a metal selected from a group including a divalent metal, a trivalent metal and combinations thereof. Disclosed is a method of producing nanoparticles, which includes preparing an aqueous solution of a casein source and a basic amino acid and adding to the prepared solution an aqueous solution of a metal selected from a group including a divalent metal, a trivalent metal and combinations thereof to obtain a suspension containing formed nanoparticles. Another version of the method of producing nanoparticles includes mixing an aqueous solution of a casein source and a basic amino acid with a solution of a biologically active compound and adding to the obtained mixture an aqueous solution of a metal selected from the group to obtain a suspension containing formed nanoparticles. Nanoparticles obtained using said methods are used in combination with a carrier to prepare food products, as well as in pharmaceutics and cosmetics.

EFFECT: invention enables to obtain nanoparticles with high stability and low polydispersity.

40 cl, 17 dwg, 13 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to a two-phase mouth wash liquid and a method for use thereof. The disclosed two-phase mouth wash liquid contains a hydrophilic phase, a hydrophobic phase, a hydrotrope and a preservative, wherein the preservative contains (i) sodium benzoate and (ii) potassium sorbate and/or methylisothiazolinone (MIT), and the hydrotrope component contains glycerine and/or propylene glycol. The mouth wash liquid contains (a) 0.05-0.11 wt % sodium benzoate and (b) 0.05-0.2 wt % potassium sorbate and/or 0.0005-0.01 wt % MIT. The hydrophilic phase of the mouth wash liquid can additionally contain cetylpyridinium chloride in amount of 0.01-0.1 wt %, wherein the disclosed method of improving oral health includes using an effective amount of said liquid in the mouth of a subject to reduce the level of cariogenic bacteria.

EFFECT: use of said combination of preservatives coupled with said hydrotrope provides good resistance to microbial contamination without any adverse effect on taste properties or appearance of the mouth was liquid.

12 cl, 1 ex

FIELD: medicine.

SUBSTANCE: combined phyto- and physiotherapy is conducted. The phytotherapy involves administering Prolit Super 2 capsules two times a day (at 8 and 14 o'clock) for one month; the physiotherapy provides rectal electrical stimulation by means of AndroGyn for 8 minutes a day, 15 procedures in the therapeutic course.

EFFECT: invention enables improving the sexual function and prostatic microcirculation, and can be used in ambulance situation.

1 dwg, 1 ex

FIELD: veterinary science.

SUBSTANCE: method includes the complex application of systemic antimycotic agents, surface antifungal agents, additionally the preparation Forvet is injected in a dose of 0.2 ml per 1 kg of mass subcutaneously, for 7 days.

EFFECT: increased efficiency of treatment, no side effects and reduced remission time.

2 tbl

FIELD: chemistry.

SUBSTANCE: method includes treating crushed Echinacea purpurea (L.) Moench roots and rhizome with steam, extraction with ethyl alcohol, then steeping, stirring, steeping, draining a portion of the extract which is equal to the amount of the loaded Echinacea purpurea (L.) Moench roots and rhizome, after draining a portion of the extract, adding ethyl alcohol to the treated material, draining the whole extract; extracting crushed Echinacea purpurea (L.) Moench herbs with ethyl alcohol, steeping, then stirring, steeping, draining a portion of the extract which is equal to the amount of the loaded Echinacea purpurea (L.) Moench herbs, after draining a portion of the extract, adding ethyl alcohol to the treated herbs, draining the whole extract; all obtained extracts are mixed, cooled and filtered under certain conditions. An Echinacea purpurea (L.) Moench tincture. Use of the method to obtain an Echinacea purpurea (L.) Moench tincture.

EFFECT: method preserves the biological activity of components of the tincture and medicinal properties.

3 cl

FIELD: medicine.

SUBSTANCE: burn-treating composition for local application based on Vaseline lanolin, or carbopol, or hydrogel; as an active substance, the composition contains 5% dry extract of the herbal raw material big-flowered self and self-heal containing 60% rosmarinic acid.

EFFECT: above composition is effective for treating burns; it is non-toxic.

7 tbl, 10 ex, 12 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to synthesis of N-mono fluoroalkyl tropanes with application of fluoroalkyliodides, as well as to application of such method for obtaining non-radioactive tropane intermediate compound of formula and its further conversion into 123I-labelled radiopharmaceutical substance DaTSCAN (123I-ioflupane). Method consists in alkylation in presence of base of formula compound with alkylating agent of formula F-(CH2)mX, where m equals 2, 3 or 4, X represents I. .

EFFECT: obtaining non-radioactive tropane intermediate compound of formula and its further conversion into 123I-labelled radiopharmaceutical substance DaTSCAN (123I-ioflupane).

10 cl, 1 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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