KR101696342B1 - Composition for Anti-Diabetes - Google Patents

Abstract

The present invention discloses an antidiabetic composition. More specifically, the present invention is when high-fat and be administered in the diabetes-induced experimental animal induced by dietary carbohydrate has a hypoglycemic effect, such as (i) sweetbrier (Rosa rugosa Thunberg extract, (ii) Momordica charantia L. ) leaf, Guidia ( Psidium guajava L. ) leaves and mulberry leaves ( Morus alba L. ), (iii) a mixture of Sasa borealis ( Hack .) Makino ) Leaf, Curcuma longa L. ), Saururus chinensis Baill and a mixture of the same, (iv) an extract of mixture of Yeoju leaf, guava leaf, mulberry leaf, Sasae leaf,

Description

Composition for Anti-Diabetes < RTI ID = 0.0 >

The present invention relates to an anti-diabetic composition.

Diabetes is a condition in which insulin in the pancreas is secreted from the β-cells of the pancreas and insufficiency or insufficiency is caused and blood glucose in the blood is not used as energy but accumulated in the blood to cause hyperglycemia and urinary glucose is detected.

Diabetes is usually divided into insulin-dependent diabetes (type I diabetes) and non-insulin dependent diabetes (type II diabetes). Insulin-dependent diabetes mellitus is caused by viral infection, resulting in the disruption of the beta cells of the pancreas, resulting in insulin secretion, which is mainly caused by a young age group of 10 to 20 years. Therefore, it is called pediatric diabetes, It is a name given because it is difficult to maintain life. Non-insulin dependent diabetes mellitus is a cause of obesity, such as insulin secretion in the beta cells of the pancreas, but the amount is lacking, its ability to reduce the onset, and usually after the onset of 30 years or older is also called adult diabetes. It is not called insulin non-dependent diabetes because it is not necessary to supply insulin from the outside in order to maintain life, but this does not mean that insulin treatment is not necessary for the treatment of hyperglycemia.

For the treatment of diabetes, biguanides, thiazolidinediones, sulfonylureas, benzoic acid derivatives, and? -Glucosidase inhibitors are used. Drug-induced diabetes treatment has many side effects, and the World Health Organization (WHO) strongly recommends the use of natural products with less side effects on diabetes (Grover JK, Vats V., Rathi SS, Journal of Ethnopharmacology, 73 , pp 461-470, 2000).

As the natural products proposed to be effective for the treatment of diabetes, there have been reported the extracts of Cucurbitaceae (Korean Patent No. 464815), the phthalic acid derivatives (Korean Patent No. 457690) and the extracts of Hovenia japonica (Korean Patent No. 417287) , Polysaccharides isolated from Angelica gigas Nakai (International Publication No. 2001-60386), and ruminant bile (US Patent No. 6451355).

The present invention also discloses an anti-diabetic activity, such as a natural extract, which is a kind of natural product.

It is an object of the present invention to provide an anti-diabetic composition using an extract of Allium cepaensis.

Other and further objects of the present invention will be described below.

The present invention, as shown in the following Examples and Experimental Examples, (i) Rosa rugosa Thunberg leaf and stem extract, (ii) Momordica charantia L. ) fruit, Guidia ( Psidium guajava L. ) leaves, and Morus alba L. ) mixture of leaf and skin, (iii) Sasa borealis ( Hack .) Makino ) Leaf, Curcuma longa L. ) Tuber, Saururus chinensis Baill ), (iv) mixture extracts of Leaf fruit, Guava leaf, Mulberry leaf and stem, Sasa leaf, Ueruga tuber, Saururus chinensis, and leaf and stems of leaves showed antidiabetic activity and anti - obesity activity In the first place.

In view of the foregoing, the present invention provides, in one aspect, an antidiabetic composition comprising an extract selected from the group consisting of the following (I) to (IV) as an active ingredient. In another aspect, And an extract selected from the group consisting of (I) to (IV) as an active ingredient.

(Ⅰ) Leaf and stem extract,

(Ⅱ) extract of mixture of Leaf fruit, guava leaf and mulberry leaf and skin,

(Ⅲ) Extract of Saurus leaves, Ulgus tuber,

(Ⅳ) Extracts of Leaf Berries, Guava Leaf, Mulberry Leaf and Stalks, Sasa Leaf, Ulmus Tuber, Saururus chinensis, and Composite Leaf and Stem

In the present specification, "anti-diabetic" means the prevention, treatment, improvement or delay of the onset of diabetes, specifically, prevention of pathological symptoms such as hyperglycemia caused by lack of insulin or lack of insulin, , Treatment, improvement, or delayed onset of such pathological symptoms.

As used herein, the term "extract" means an extract obtained by extracting a subject to be extracted with an alcohol having 1 to 4 carbon atoms such as methanol or ethanol, acetone, ethyl acetate, chloroform, methylene chloride, water, or a mixed solvent thereof, Is understood to mean a fraction further purified with the recited solvent. Here, the extraction method includes both a method of immersing the object to be extracted in an extraction solvent and a method of distilling the object to be extracted into an extraction solvent. In addition, any method such as cold-pressing, heating, ultrasonic wave, and reflux may be applied to the extraction method through immersion. However, the above-mentioned "extract" preferably means that the object to be extracted is extracted (immersed or distilled) with water, ethanol or a mixed solvent thereof, more preferably an ethanol aqueous solution having an ethanol content of 70% to 90% it means. Where% is the concentration (v / v) by volume percentage and refers to a volume of solute dissolved in a volume of solution as is known in the art. For example, 30% (v / v) means that 30 ml of the solute is dissolved in 100 ml of the solution. As used herein, the term "extract" means an extract of purified form through filtration, a liquid concentrated extract from which the extraction solvent is removed, and a powdery extract from which the extraction solvent has been removed.

In the present specification, the term "diabetes " includes insulin-dependent diabetes mellitus (type 1 diabetes) and non-insulin dependent diabetes mellitus (type 2 diabetes mellitus) as described above. Further, Diabetes mellitus such as hyperthyroidism, hypercortisolism, hyperglycemia or diabetes due to catecholamine hypertrophy, gestational diabetes mellitus.

The term "active ingredient" as used herein alone means an ingredient which exhibits the desired activity or which can exhibit activity together with a carrier which is itself inactive.

In the present specification, "anti-obesity" means a decrease in body fat and / or a decrease in body weight. Therefore, it includes prevention of obesity, treatment of obesity, and further includes reducing weight / body fat for beauty or health purposes, although the weight is not classified as obesity or overweight.

In the present specification, the term "obesity" means an abnormally increased state of adipose tissue, whether it is obesity due to genetic factors or obesity due to environmental factors. When the body mass index (BMI) It is meant to include obesity (for BMI> 30.0), obesity (for BMI 25-30), and overweight (for BMI> 23-25).

On the other hand, in the following Examples and Experimental Examples, the active ingredient of the antidiabetic composition of the present invention is characterized in that the active ingredient of the above-mentioned (IV) is an extract of Leptospira, guava leaf, mulberry leaf, stem, sage leaf, Is fermented by yeast or the like, its antidiabetic activity is increased.

Therefore, the active ingredient of the antidiabetic composition of the present invention is a mixture of Saccharomyces cerevisiae ( Saccharomyces cerevisiae), a mixture of Leaf fruit, Guava leaf, Mulberry leaf and stem, Sasa leaf, cerevisiae), Fitch's your self (Pichia jagini), Bacillus interference Tiller's (Bacillus subtilis ) and Lactobacillus casei may be preferable.

In the present specification, the term "fermented product" means a culture obtained by adding and mixing a carbon source to the fermentation subject and inoculating the lactic acid bacteria. The culture may be used as it is, or it may be used in a purified form through filtration or the like, or may be used in liquid or powder form by concentration under reduced pressure and / or lyophilization, or may be used in the form of an alcohol having 1 to 4 carbon atoms such as methanol, ethanol, Chloroform, methylene chloride, water or a mixed solvent thereof. When extracted and used, there is no particular limitation on the extraction method. Specifically, the extraction method includes both a method of immersing the object to be extracted (that is, a fermented product) in an extraction solvent and a method of distilling the object to be extracted with an extraction solvent. In addition, any method such as cold-pressing, heating, ultrasonic wave, and reflux may be applied to the extraction method through immersion. Herein, the meaning of the extract includes the purified form of the extract through filtration, and the liquid or powdery extract in which the extraction solvent is partially or completely removed.

The carbon source of the microorganism inoculated in the above is well known in the art, and thus any of those known in the art can be used. Usually, oligosaccharides, lactose, glucose, fructose, sugar, molasses, dextrose, will be. These carbon sources can be added in an arbitrary range in consideration of the intended fermentation time, degree of fermentation, and the like. It is usually added in the range of 1 to 20 parts by weight based on 100 parts by weight of the ginseng or red ginseng powder to be fermented.

In addition, the cultivation after inoculation of the microorganisms can be carried out at a temperature of 15 ° C to 45 ° C, particularly at a temperature of 25 ° C to 40 ° C, in consideration of the inoculated microorganisms. If the incubation temperature is lower than the above range, the fermentation rate may be slowed and unwanted fermentation products may be produced. Even if the incubation temperature is higher than the above range, the fermentation rate may be similarly slowed down due to the death of the fermentation microorganisms, . In the case of the incubation time, it is preferable to continue until the growth of the inoculated microorganism reaches a maximum. The time at which the inoculated microorganism reaches its maximum growth will depend on the incubation temperature, the amount of fermentation material, the amount of microorganisms inoculated, and so on. Those skilled in the art will be able to determine at what point in time the maximum growth of the inoculated microorganisms takes into account, in consideration of the culture temperature, the amount of the fermentation raw material, the amount of the microorganism to be inoculated,

The antidiabetic composition and the anti-obesity composition (hereinafter, the composition of the present invention) of the present invention may be contained in an arbitrary amount (effective amount) depending on the purpose of use, formulation, compounding or the like as long as the active ingredient can exhibit antidiabetic activity or anti- , A typical effective amount will be determined within the range of from 0.001 wt% to 99.990 wt% based on the total weight of the composition. Here, "effective amount" refers to the amount of active ingredient capable of inducing an anti-diabetic effect or an anti-obesity effect. Such effective amounts can be determined experimentally within the ordinary skill of those skilled in the art. The subject to which the composition of the present invention can be applied (prescription) is preferably a mammal and a person, particularly a human.

The anti-obesity composition of the present invention can be identified as a food composition in a specific embodiment.

When the composition of the present invention is identified as a food composition, the form of the food is not particularly limited as far as it is a beverage such as tea, juice, carbonated beverage, ionic drink, processed oil such as milk and request route, gum, rice cake, Food preparations such as foods, powders, tablets, capsules and the like.

The food composition of the present invention may contain sweetening agents, flavoring agents, physiologically active ingredients, minerals and the like in addition to the active ingredients thereof.

Sweetening agents may be used in an amount that sweetens the food in a suitable manner, and may be natural or synthetic. Preferably, natural sweeteners are used. Examples of natural sweeteners include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose and maltose.

Flavors may be used to enhance taste or flavor, both natural and synthetic. Preferably, a natural one is used. When using natural ones, the purpose of nutritional fortification can be performed in addition to the flavor. Examples of natural flavoring agents include those obtained from apples, lemons, citrus fruits, grapes, strawberries, peaches, and the like, or those obtained from green tea leaves, Asiatica, Daegu, Cinnamon, Chrysanthemum leaves and Jasmine. Also, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, banks and the like can be used. The natural flavoring agent may be a liquid concentrate or a solid form of extract. Synthetic flavors may be used depending on the case, and synthetic flavors such as esters, alcohols, aldehydes, terpenes and the like may be used.

Examples of the physiologically active substance include catechins such as catechin, epicatechin, gallocatechin and epigallocatechin, and vitamins such as retinol, ascorbic acid, tocopherol, calciferol, thiamine and riboflavin.

As the mineral, calcium, magnesium, chromium, cobalt, copper, fluoride, germanium, iodine, iron, lithium, magnesium, manganese, molybdenum, phosphorus, potassium, selenium, silicon, sodium, sulfur, vanadium and zinc can be used.

In addition, the food composition of the present invention may contain preservatives, emulsifiers, acidifiers, thickeners and the like as needed in addition to the above sweeteners.

It is preferable that such preservatives, emulsifiers and the like are added in a minimum amount as long as they can attain an application to which they are added. And will generally be used in the range of from 0.0005% to about 0.5% by weight based on the total weight of the food composition.

Examples of the preservative which can be used include calcium sodium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate and EDTA (ethylenediaminetetraacetic acid).

Examples of the emulsifier which can be used include acacia gum, carboxymethyl cellulose, xanthan gum, pectin and the like.

Examples of the acidulant that can be used include acid, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, and phosphoric acid. Such an acidulant may be added so that the food composition has a proper acidity for the purpose of inhibiting the growth of microorganisms other than the purpose of enhancing the taste.

Agents that may be used include suspending agents, sedimentation agents, gel formers, bulking agents and the like.

In addition, the food composition of the present invention may contain a powder or extract derived from a natural product in order to improve flavor or palatability and to impart other functionalities, and may be a pregelatinized powder or extract, a soybean powder or extract, a shell powder or extract, Extracts, juice or extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng juice or extracts, extracts of ginseng juice or extracts, extracts of ginseng juice or extracts, extracts of spinach juice or extracts, lotus juice or extracts, Powder or extract, licorice powder or extract, granular powder or extract, granular powder or extract, sine powder or extract, pistachio powder or extract, ginger powder or extract, jujube powder or extract, Water-based powder or extract, dried powder or extract, Or extract, dermis (crustacea bark) powder or extract, ginger powder or extract, green tea powder or extract, omija powder or extract, hinoki powder or extract, dirt powder or extract, egg yolk powder or extract, cinnamon powder or extract, Cyano and the like can be exemplified. Such an extract may be obtained by mixing the object to be extracted.

In another specific embodiment, the composition of the present invention can be identified as a pharmaceutical composition.

The pharmaceutical composition of the present invention may be in a form suitable for oral use (tablets, suspensions, granules, emulsions, capsules, syrups, etc.), parenteral formulations (sterile injectable aqueous or non- Ointments, ointments, solutions, creams, ointments, gels, lotions, patches, and the like).

The term "pharmaceutically acceptable" as used herein means that the application (subject) does not have an adaptive or higher toxicity (sufficiently low toxicity) without inhibiting the activity of the active ingredient.

Examples of pharmaceutically acceptable carriers include lactose, glucose, sucrose, starch (e.g., corn starch, potato starch and the like), cellulose, derivatives thereof (e.g. sodium carboxymethylcellulose, ethylcellulose, etc.), malt, gelatin, talc, (E.g., peanut oil, cottonseed oil, sesame oil, olive oil, etc.), polyols (e.g., propylene glycol, glycerin, etc.), alginic acid, emulsifiers (e.g., TWEENS), wetting agents (For example, sodium lauryl sulfate), a coloring agent, a flavoring agent, a tableting agent, a stabilizer, an antioxidant, a preservative, water, a saline solution and a phosphate buffer solution. The carrier may be selected from one or more of suitable pharmaceutical formulations according to the formulation of the pharmaceutical composition of the present invention.

The excipient may be selected according to the formulation of the pharmaceutical composition of the present invention. For example, when the pharmaceutical composition of the present invention is prepared by an aqueous suspension, suitable excipients include sodium carboxymethylcellulose, methylcellulose, hydropropylmethylcellulose , Sodium alginate, polyvinylpyrrolidone, and the like can be used. As a suitable excipient when prepared by injection, Ringer's solution, isotonic sodium chloride and the like can be used.

The pharmaceutical composition of the present invention may be administered orally or parenterally.

The daily dose of the pharmaceutical composition of the present invention is usually 0.001 to 150 mg / kg body weight, and may be administered once or several times. However, since the dosage of the pharmaceutical composition of the present invention is determined in view of various related factors such as route of administration, age, sex, weight, and patient's severity of the patient, the dose is limited in any aspect to the scope of the present invention Should not be understood to be.

INDUSTRIAL APPLICABILITY As described above, the present invention can provide a composition for anti-diabetic and an anti-obesity composition. The composition of the present invention can be commercialized as a medicine or food.

Figure 1 shows the feed intake for 8 weeks.
FIG. 2 shows the result of blood glucose change of an experimental animal when the sample was administered for 8 weeks.
3 shows the results of blood glucose lowering measurement.
FIG. 4 shows the result of measuring the body weight change of the experimental animals when the sample was administered for 8 weeks.

Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these examples and experimental examples.

< Example > Preparation of sample

&Lt; Example 1 >

1 kg of the crushed leaf and stem were dried and crushed, and 2 kg of 80% ethanol was added and the mixture was heated for 6 hours. The filtrate was filtered through a Whatman No.2 filter. The filtrate was concentrated under reduced pressure and dried in a freeze dryer (Samwon Engineering Co., Ltd., Korea)

&Lt; Example 2 > Preparation of mixed extract

The following medicinal plants obtained by drying and crushing were mixed at the same weight, and the same method as in <Example 1> was carried out to prepare a complex extract.

T1: Yeast fruit + Guava leaf + Mulberry leaf and stem

T2: Saury leaves + Ulug tuber + Saururus chrysanthemum + Leaf and stem

T3: Yeoju fruit + Guava leaf + Mulberry leaf and stem + Sasa leaf + Ulk tuber + Three hundred milliseconds outpost + Japanese leaf and stem

&Lt; Example 3 > T3 Preparation of Fermented Products

200 parts by weight of water was added to 100 parts by weight of T3 (lupus fruit + guava leaf + mulberry leaf and stem + sagittal leaf + elliptical tuber + And then sterilized at 121 DEG C for 20 minutes using a sterilizer. Herein, microorganisms F1 to F3 below the seed culture in the MRS liquid medium 3.0% (v / v) inoculated and fermented at 30 ° C for 7 days to prepare a fermented product. The fermented product was sterilized at 100 ° C for 10 minutes, concentrated under reduced pressure, and lyophilized to be used in the experiment.

F1: Saccharomyces access to the serenity of Mai Ke Vichy (Saccharomyces cerevisiae) and Fitch's your self (Pichia jagini )

F2: Bacillus subtilis and Lactobacillus &lt; RTI ID = 0.0 & gt; casei )

F3: F1 + F2

< Experimental Example > Anti-diabetic  And Anti-obesity  Active experiment

<Experimental Example 1> Antidiabetic activity test

<Experimental Example 1-1> Experiment of blood glucose measurement changes

All animal experiments were conducted by the Animal Experimental Ethics Committee of the Dong-Shin University College of Oriental Medicine. High-fat, high-carbohydrate diets were purchased from foreign countries for the production of obese type 2 diabetes-inducing animals (Surwit's high fat, high sucrose diet (HFD), Research Diets, D12331). Male ICR mice (Central laboratory animals, Korea) weighing 23-25g were purchased and kept at 40-60% humidity and maintained in a stainless-steel cage for one week and undergone adaptation. After that, high fat, high carbohydrate diets were fed to induce obesity type diabetes and used in the experiment.

Experimental groups were divided into three groups: normal (general feed), control (high fat high carbohydrate feed only), metformin treatment (metformin feed with high fat high carbohydrate feed), sample treatments (T1 to T3 and RRT, (W / w) and 0.5% (w / w) of metformin were added to high-fat, high-carbohydrate diets, respectively. The experiment was carried out for 8 weeks and the feed intake for 8 weeks is shown in FIG.

Blood glucose was measured in the tail vein before and two weeks after the test using a test machine measurement kit.

The results are shown in Fig. 2 for Example 1 and Example 2, and in Table 1 below for the fermentation of Example 3.

Referring to FIG. 2, it can be seen that the extract obtained from the corresponding extract is also active, but the complex extract, especially T3, is most active.

Table 1 also shows that all T3 fermentations exhibit activity above the T3 extract.

<Experimental Example 1-2> hypoglycemic measurement experiment

OGTT (Oral Glucose Tolerance Test) test was used for blood glucose lowering test, and Han S. et al . (2012, JK Oriental Med.). After 7 hours of fasting, mice were fasted for more than 8 hours and blood glucose was measured. Fasting glucose (1 g / kg body weight) was dissolved in distilled water for oral administration. After 30 minutes, 60 minutes and 90 minutes, And blood glucose was measured.

The results are shown in Fig.

As shown in FIG. 3, similar to the results shown in [FIG. 2], the extracts of the seedlings exhibited activity, but the complex extracts, especially T3, showed the highest activity.

<Experimental Example 2> Anti-obesity activity test

The body weight was measured before the experiment (Experimental Example 1) and once a week. When weighing, the mouse was confined in a limited space so as not to move, and the weight was measured accurately.

The results are shown in Fig.

Referring to the results of FIG. 4, it can be seen that all of the samples of the Examples had lowered body weight in contrast to Control.

Statistical processing

All data were analyzed using CoStat software (CoHort Software, Monterey, USA), a statistical program. Significant difference test for each treatment and sample group was performed with least significant difference (LSD) at p <0.05 level after analysis of variance.

Claims (8)

Consisting of Saccharomyces cerevisiae and Pichia jagini , of a mixture of lily of the valley , guava leaf, mulberry leaf and stem, boleberry leaf, elliptical tuber, A composition for anti-diabetes comprising a fermented product of a mixed microorganism as an active ingredient.
delete delete The method according to claim 1,
Wherein the composition is a pharmaceutical composition.
The method according to claim 1,
Wherein the composition is a food composition. delete delete delete

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