KR20160075902A - COMPOSITION COMPRISING ALCOHOL EXTRACTS FROM Fomitopsis sp. FOR TREATING OR PREVENTING HYPERLIPIDEMIA - Google Patents
COMPOSITION COMPRISING ALCOHOL EXTRACTS FROM Fomitopsis sp. FOR TREATING OR PREVENTING HYPERLIPIDEMIA Download PDFInfo
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- KR20160075902A KR20160075902A KR1020140184317A KR20140184317A KR20160075902A KR 20160075902 A KR20160075902 A KR 20160075902A KR 1020140184317 A KR1020140184317 A KR 1020140184317A KR 20140184317 A KR20140184317 A KR 20140184317A KR 20160075902 A KR20160075902 A KR 20160075902A
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- A—HUMAN NECESSITIES
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
Description
More particularly, the present invention relates to a composition for treating or preventing hyperlipidemia, which comprises an alcoholic extract of a topical antioxidant effective in the treatment and prevention of hyperlipidemia.
Hyperlipidemia refers to a disease of high blood fat content. Generally, when total cholesterol is over 240 ㎎ / dl or triglycerides are over 200 ㎎ / dl, it is called hyperlipidemia. Hyperlipidemia is known to be a major cause of hypertension, myocardial infarction, and stroke due to cholesterol blocks the blood vessels and inhibits blood circulation.
BACKGROUND ART In order to prevent or treat hyperlipidemia due to cholesterol, studies have been made on substances that inhibit the absorption of cholesterol. Currently, statin drugs are widely used for the treatment of hyperlipidemia due to inhibition of cholesterol absorption. The drug in this series is an inhibitor of Hmg-CoA reductase and has the effect of inhibiting cholesterol synthesis and lowering blood LDL-cholesterol. In addition, ezetimibe, niacin and fibrate preparations are mainly used. However, there is a possibility that side effects such as myalgia, constipation or digestive disorder and hepatic dysfunction are rarely observed when the drug is administered.
In PCT / KR2012 / 10604, it has been disclosed that the alcohol extract of Pseudomonas aeruginosa can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipidemia.
In PCT / KR2012 / 10612, it has been disclosed that the water extract of red mulberry can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipemia.
In PCT / KR2012 / 10550, it has been disclosed that the alcohol extract of the flower shield mushroom can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipidemia.
On the other hand, in order to treat and prevent hyperlipidemia due to triglyceride, studies have been made on drugs having a mechanism of action that acts on digestive enzymes and inhibits the absorption of fat.
Xenical TM (orlistat) is well known as a typical drug. It inhibits the activity of TGL by covalent bonding with serine, which is the active site of triglyceride lipase (TGL), and prevents the fat from being degraded and absorbed .
Development of a Specific Egg Yolk Antibody to the Pancreatic Lipase Domain for the Prevention of Obesity ", Kor J. Microbiol . Biotechnol . Vol. 36, No. 4, 299-306 (2008) Suggesting a method to prevent the absorption of fat by inhibiting the activity.
In PCT / KR2012 / 10558, it has been disclosed that the alcohol extract of yellow vanda mushroom can be used as a composition for treating and preventing obesity by inhibiting the activity of pancreatic lipase.
In PCT / KR2012 / 10602, it has been disclosed that water extract of Chrysanthemum morbus Mushroom can be used as a composition for treating and preventing obesity by inhibiting the activity of pancreatic lipase.
On the other hand, in PCT / KR2012 / 10621, water extract of acacia mushroom suppresses the activity of pancreatic lipase and the activity of raising pancreatic cholesterol ester, and it is known that it can inhibit fat absorption.
However, there is a continuing need for a new mushroom extract which can inhibit the absorption of fat and cholesterol and effectively prevent hyperlipidemia and obesity.
A problem to be solved by the present invention is to provide a novel mushroom extract which can inhibit the absorption of fat and cholesterol without showing any side effects in vivo.
Another object of the present invention is to provide a novel mushroom extract which can inhibit the activity of raising pancreatic cholesterol ester and the activity of pancreatic lipase.
A problem to be solved by the present invention is to provide a composition capable of inhibiting the absorption of fat and cholesterol and treating or preventing hyperlipidemia.
In order to accomplish the above object, the present invention provides a composition for treating or preventing hyperlipidemia comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a medicament for the treatment or prevention of hyperlipemia, which comprises an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a method for treating or preventing hyperlipidemia comprising administering to an animal an alcoholic extract of 1 to 10 carbon atoms in a topical topical sispy.
The present invention provides a health functional food for improving or preventing hyperlipidemia comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention also provides a composition for inhibiting the activity of raising pancreatic cholesterol ester comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a medicament for inhibiting the activity of raising pancreatic cholesterol ester comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a method for inhibiting the activity of a pancreatic cholesterol ester raise comprising administering to an animal an alcoholic extract of 1 to 10 carbon atoms in a formic topoisose.
The present invention provides a health-functional food for inhibiting the activity of raising pancreatic cholesterol ester comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention also provides a composition for inhibiting the activity of pancreatic lipase comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a medicament for inhibiting the activity of pancreatic lipase comprising an alcohol extract of 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
The present invention provides a method for inhibiting the activity of pancreatic lipase comprising administering to an animal an alcoholic extract of 1 to 10 carbon atoms in a topical topical sisffi.
The present invention provides a health functional food for inhibiting the activity of pancreatic lipase comprising an alcohol extract having 1 to 10 carbon atoms in the formic topoisose as an active ingredient.
In addition, the present invention can be used as a composition for prevention and treatment of obesity by inhibiting the activity of pancreatic lipase and inhibiting the absorption of fat by the alcoholic extract having 1 to 10 carbon atoms in the formic topoisose.
In the present invention, the extract of the above-mentioned topical topoisomerase, in particular, the alcoholic extract of the topical topical syste, lowers the activity of the pancreatic cholesterol ester raise and effectively inhibits the activity of the pancreatic lipase, which is triglyceride lipase (TGL) To replace drugs that treat or prevent hyperlipidemia.
In the present invention, the alcoholic extract having 1 to 10 carbon atoms in the formic topoisose may be one obtained by extracting a lower alcohol having 1 to 5 carbon atoms as an extraction solvent. When the formic top system is extracted with a low-alcohol having 1 to 5 carbon atoms, it exerts excellent digestion and absorption inhibitory effects on the body fat.
Particularly, as such an alcohol extracting solvent, a lower alcohol having 1 to 5 carbon atoms, more preferably ethanol, and most preferably 90 to 99.99% (v / v) ethanol can be used.
In the present invention, the weight or weight of the mushroom is understood to refer to the weight or weight of the dried mushroom unless otherwise noted.
On the other hand, the alcoholic extract of the above-mentioned topical topical sisue may be one prepared by a conventional method for producing a plant extract. Preferably, the former is dried and ground, and then the residue is removed. Then, 0.1 to 20 g of the pulverized product is added per 100 ml of the alcohol having 1 to 10 carbon atoms, more preferably, 1 to 20 g of the pulverized product per 100 ml of the extraction solvent, 5 g may be added to the solution. When the content of the powdery topoisosity product is too small as compared with that of the extraction solvent, the effect of the topisisispie is not sufficient, and when the amount of the solvent is excessively large relative to the amount of the extraction solvent, the increase in the effect is not significant It is not preferable from the viewpoint of productivity because the production cost is increased.
In this case, the extraction conditions are not limited, but it is preferable that the mixture is mixed with an alcohol having 1 to 10 carbon atoms, which is an extraction solvent, at a temperature of 20 to 60 ° C for 12 to 36 hours, more preferably 30 To 40 < 0 > C for 20 to 24 hours.
Extraction at an excessively low temperature condition requires a long time for extracting an active ingredient, and extraction at an excessively high temperature may deteriorate the activity, which is undesirable.
When the extraction time is too short, the concentration of the effective component to be extracted is low, and when the extraction is performed for an excessively long time, the concentration of the extraction effective ingredient increases with the increase of the extraction time.
Then, the alcohol extract of the foamy topical sisphyl extracted by the above method is filtered through a filter cloth, and the filtrate is centrifuged to remove the precipitate, and the filtrate can be concentrated or concentrated under reduced pressure, followed by freeze-drying.
On the other hand, the content of the alcoholic extract of the topical antioxidant, which is an active ingredient of the above-described embodiment of the composition for treating or preventing obesity and hyperlipidemia, is not limited, but may be preferably 0.001 to 50% by weight. When the content of the alcoholic extract of the topical herbicide is less than 0.001% by weight, digestion and absorption of the fat in the body are insignificant. When the content is more than 50% by weight, the effect of increasing the inhibitory activity is insignificant It is not economical. More preferably, the content of the alcoholic extract of Formicotissis in the composition may be from 0.01 to 50% by weight, most preferably from 0.1 to 30% by weight.
The present invention provides a medicament for the treatment or prevention of hyperlipidemia or obesity, which comprises an alcohol extract of the formidoxis espei contained in the composition according to the embodiment as an active ingredient. The medicament containing such alcoholic extract of the topical topical sisu as an active ingredient may further contain suitable carriers, excipients and diluents conventionally used for the production thereof.
Examples of the carrier, excipient and diluent which can be contained in the pharmaceutical preparation containing the alcoholic extract of the present invention include the lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, , Alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil have.
The medicines containing the alcohol extract of the present invention as an active ingredient can be used as oral formulations such as powders, granules, tablets, suspensions, emulsions and syrups according to conventional methods.
The oral formulations are meant to include solid and liquid formulations for oral administration and solid formulations for oral administration may include tablets, pills, powders, granules, capsules and the like, For example, starch, calcium carbonate, sucrose or lactose, gelatin and the like in combination with at least one excipient. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral use include suspensions, solutions, emulsions, and syrups. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, have.
The preferred dosage of the composition containing the alcoholic extract of the present topical cosmetic composition of the present invention varies depending on the condition and body weight, the degree of disease, the drug form, the administration route and the period, but can be appropriately selected by those skilled in the art. Preferably, the medicinal product containing the alcohol extract of the present invention as an active ingredient is 0.0001 to 100 mg / kg per day based on the amount of the alcoholic extract of the topical topical agent, preferably 0.01 to 10 mg / Mg / kg < / RTI > The administration may be carried out once a day or divided into several doses. The dose and the number of administrations do not limit the scope of the present invention in any aspect.
According to another embodiment of the present invention, there is provided a health functional food for improving or preventing hyperlipidemia or obesity, which comprises an alcoholic extract of Formicotissis as an active ingredient. Herein, the term "health functional food" means a natural product or a processed product containing one or more nutrients, preferably a state of being able to be directly eaten through a certain processing step.
Examples of the health functional food to which the alcohol extract of the present invention is added include various foods, beverages, gums, tea, vitamin complex, and the like. In addition, in the present invention, the food may contain special nutritional foods (eg, crude oil, infant formula, etc.), meat products, fish products, tofu, mackerel, noodles (eg, (Such as soy sauce, soybean paste, hot pepper paste, mixed sauce), sauces, confectionery (eg snacks), dairy products (eg fermented milk, cheese), other processed foods, kimchi, pickled foods (For example, fruits and vegetables, beverages, fermented beverages, etc.), natural seasonings (eg, ramen soup, etc.). The food, beverage or food additive may be prepared by a conventional production method.
In the present specification, the functional food refers to a food group which is imparted with added value to function and express the function of the food by using physical, biochemical, biotechnological techniques, etc., Means a food which is processed and designed so that the body control function related to restoration and the like is sufficiently expressed to the living body. The functional food may include a food-acceptable food-aid additive, and may further comprise suitable carriers, excipients and diluents conventionally used in the production of functional foods.
In the present specification, beverage means a generic term for drinking or enjoying a taste and is intended to include a functional beverage. The beverage is not particularly limited as long as it contains the alcohol extract of the formic topoisose as an active ingredient as an essential ingredient at the indicated ratio, and there is no particular limitation to other ingredients, and various flavors or natural carbohydrates, ≪ / RTI > Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and Xylitol, sorbitol, and erythritol. Natural flavors (tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate may be generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the composition of the present invention. In addition, the composition of the present invention may be used for natural fruit juice, fruit juice drink, And may further contain flesh for manufacture.
In addition to the above, the health functional food of the present invention may contain various kinds of nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, colorants and heavies (cheese, chocolate etc.), pectic acid and its salts, And salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like. These components can be used independently or in combination. The proportion of such additives is not critical, but may be selected in the range of 0 to 20 parts by weight per 100 parts by weight of alcohol extract of the present invention.
In the present specification, functional beverages are used to control the bio-defense rhythm of the beverage group or beverage composition to which the added value is imparted so that the function of the beverage functions for a specific purpose by using physical, biochemical, biotechnological techniques, Means a beverage which has been designed so that the body control function related to restoration and the like is sufficiently expressed in the living body.
The above-mentioned functional beverage is not particularly limited to the other components other than the alcoholic extract of the present invention of the present invention as an essential ingredient in the indicated ratio, and may contain various flavors or natural carbohydrates as an additional ingredient can do. Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and xylitol , Sorbitol, and erythritol. Natural flavors (tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate is generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the composition of the present invention.
In addition, in a health functional food for the purpose of improving or preventing hyperlipidemia or obesity, the amount of the extract may be 0.01 to 15% by weight of the total food, and the beverage composition may contain 0.02 to 5 g , Preferably 0.3 to 1 g.
According to another embodiment of the present invention, there is provided a method for preparing an alcoholic extract of a topical topical sisue.
According to an embodiment of the present invention, there is provided a method for preparing an alcoholic extract of a topical topical sispy comprising the steps of: preparing a topical topical sispy; mixing the topical topical sispy with an alcohol having from 1 to 10 carbon atoms; At a temperature of 20 to 60 DEG C for 12 to 36 hours.
Meanwhile, in the method for producing an alcohol extract having 1 to 10 carbon atoms in the formic topoisose according to the above-mentioned embodiment, the alcohol is an alcohol having 1 to 5 carbon atoms, more preferably ethanol, most preferably 90 to 99.9 % (v / v) ethanol. When extracted with such an extraction solvent, it was found that cholesterol from the digestive tract and the effect of reducing the amount of fat absorption from the digestive tract were remarkably exhibited in addition to the effect of inhibiting digestion and absorption of cholesterol and inhibiting digestion and absorption of fat in the extracted extract. The specific extraction time, the extraction temperature, and the mixing ratio of the formic acid and the extraction solvent are different from those described above.
The composition comprising the alcohol extract of the present invention as an active ingredient inhibits the activity of pancreatic cholesterol esterase and pancreatic lipase to inhibit the digestion and absorption of cholesterol, fat, or both to treat or prevent hyperlipidemia Can be usefully used for the prophylactic use and the therapeutic or prophylactic use of obesity.
Fig. 1 is a graph showing the inhibitory activity of pancreatic cholesterol ester raise of the alcohol extract of the topical topical sispy in comparison with the control.
FIG. 2 is a graph showing the inhibitory activity of pancreatic lipase in alcohol extract of common topoisomerase compared to a control. FIG.
Figure 3 shows the results of Fomitopsis sp. Ethanol extract of the present invention in comparison with a control.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, the structure and effects of the present invention will be described in detail with reference to specific embodiments of the present invention. It should be understood, however, that the following examples are provided for a better understanding of the invention and are not to be construed as limiting the scope of the invention.
Hereinafter, the present invention will be described in detail with reference to examples.
Example : Formic top sheath Espie Preparation of alcohol extract
The dried Fomitopsis sp. Ethanol (50 ml) was mixed with 2 g of the powder as an extraction solvent, and the mixture was placed in a shaking incubator at 37 캜 for 24 hours. The supernatant of the shaking incubator was centrifuged at 2500 rpm for 10 minutes and then the Fomitopsis sp. Alcohol extracts were collected and stored at -20 ° C
Experimental Example
:
One.
Fomitopsis
sp
. Pancreatic cholesterol by alcohol extract
Esther Reyes
Active measurements and results
Pancreatic cholesterol esterase plays a role in recognizing acyl chain-bearing substrates as non-specific and isolating acyl chains. The Fomitopsis sp. In order to measure the activity of pancreatic cholesterol esterase raising by the alcohol extract, a poison flinic acid cholesterol ester raise made in Sigma chemical was used as an enzyme. Pancreatic cholesterol esterase cleaved the chromo-genic substrate (p-nirophenylbutyrate), and the activity of the enzyme was confirmed by color reaction. The inhibitory effect of enzyme was measured by the change of absorbance at 405 nm using a microplate reader, and Fomitopsis sp. Calculated as% based on absorbance at 405 nm of alcohol-treated untreated group.
The Fomitopsis sp. The effect of alcohol extracts on the enzyme activity was measured. As a result, Fomitopsis sp. Alcohol extract decreased the pancreatic cholesterol ester raising activity. The results are briefly shown in Fig.
2. Fomitopsis sp . Measurement and Results of Pancreatic Lipase Activity by Alcohol Extract
Pancreatic lipase plays a role in recognizing acyl chain-bearing substrates nonspecifically and isolating acyl chains. Fomitopsis sp. To measure pancreatic lipase activity by alcohol extract, porcine pancreatic lipase type 2 (Sigma chemical, Type II, manufactured by Sigma Chemical Co., Ltd.) was used as an enzyme. Using pancreatic lipase's ability to decompose chromo-genic substrate (p-nirophenylbutyrate), the activity of the enzyme was confirmed through color development. The inhibitory effect of the enzyme was measured by the change of absorbance at 405 nm using a microplate reader and expressed as% based on the absorbance at 405 nm of the extract-untreated group. Fomitopsis sp. The activity of the enzyme was measured by alcohol extracts. As a result, the activity of Fomitopsis sp. Alcohol extract decreased the pancreatic lipase activity. The results are briefly shown in Fig.
3. Fomitopsis sp. Measurement of Neutral Fat Absorption by Ethanol Extract
Fomitopsis sp. ≪ / RTI > of the Example showing the inhibitory effect of pancreatic lipase activity. Serum triglyceride levels were measured to determine whether ethanol extracts were also effective at the individual level. A 0.5 ml oral fat suspension was orally administered to 8-week-old Balb / c mice (male, body weight ~ 25 g) fasted for 16 hours. The fat suspension consisted of 30% olive oil, 0.5% (w / v) carboxymethylcellulose sodium (CMC-Na) and 1% (v / v)
Preparation Example: Formulation with Formicolaisispialcohol Extract
Production Example 1. Preparation of powder
20 mg of powdered topoisopropyl alcohol extract, 100 mg of lactose, 10 mg of talc.
The above ingredients were mixed and filled in an airtight container to prepare powders.
Production Example 2. Preparation of tablets
100 mg of corn starch, 100 mg of lactose, and 2 mg of magnesium stearate.
After mixing the above components, tablets were prepared by tableting according to the usual preparation method of tablets.
Production Example 3. Preparation of capsules
10 mg of Formitol, 2 mg of crystalline cellulose, 14.8 mg of lactose, and 0.2 mg of magnesium stearate.
The above components were mixed according to a conventional capsule preparation method and filled in gelatin capsules to prepare capsules.
Production Example 4. Production of liquid agent
20 mg of Formitol, 20 mg of isopropyl alcohol, 10 g of isomerized sugar, 5 g of mannitol, and purified water.
Each component was added to purified water in accordance with the usual liquid preparation method and dissolved, and the lemon flavor was added in an appropriate amount. Then, the above components were mixed, and purified water was added thereto. The whole was adjusted to 100 ml with purified water, And sterilized to prepare a liquid preparation.
Production Example 5. Production of Health Food
Vitamin B 12, vitamin C 12, vitamin C 12, vitamin C 12, vitamin C 10, vitamin C 12, vitamin C 12, vitamin C 12, 10 ㎍ of biotin, 1.7 ㎎ of nicotinic acid amide, 50 ㎍ of folate, 0.5 mg of calcium pantothenate, 1.75 mg of ferrous sulfate, 0.82 mg of zinc oxide, 25.3 mg of magnesium carbonate, 15 mg of potassium phosphate, 55 mg of potassium citrate, 90 mg of potassium citrate, 100 mg of calcium carbonate, and 24.8 mg of magnesium chloride.
Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.
Claims (20)
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