KR20190113144A - Composition for preventing or improving hypertension and manufacturing mehtod thereof - Google Patents

Abstract

The present invention relates to a composition for preventing or alleviating hypertension and a manufacturing method thereof and, more specifically, to a food composition or a pharmaceutical composition comprising a persimmon stalk end extract and garlic as an active ingredient. According to the present invention, the prevention or the alleviation of hypertension is effective by showing excellent angiotensin converting enzyme (ACE) inhibitory activity, and the human safety as a natural material is very excellent.

Description

Composition for preventing or improving hypertension and its manufacturing method {COMPOSITION FOR PREVENTING OR IMPROVING HYPERTENSION AND MANUFACTURING MEHTOD THEREOF}

The present invention relates to a composition for preventing or improving hypertension and a method for producing the same, and more particularly, to a composition for preventing or improving hypertension and a method for producing the same, including the extract and garlic as an active ingredient.

Hypertension is one of the representative diseases of modern adult diseases, and the cause of intrinsic hypertension, which accounts for the majority of hypertension, has not yet been precisely identified, but it is estimated to be mainly caused by the following two mechanisms.

 The first mechanism is the mechanism by which the sympathetic nervous system is activated to increase blood pressure by causing a change in the pressure-diuresis, which is known to be involved in the activity of the renin-angiotensin system. (Genest, JE and Koiw, OK, Physiopathology and Treatment, McGraw-Hill, 1977). The second mechanism is reported to be caused by abnormal release of Na-releasing hormone and Na-transporter, leading to inadequate release of Na, resulting in an increase in the concentration of catecholamine or angiotensin II and constriction of the renal centrifugal arteries. (Kurtz, TW et al., N. Engl. J. Med., 317: 1043, 1987). In addition to these, it is known that the symptoms of hypertension are caused by a mechanism in which Na and Ca concentrations increase due to abnormalities of the cell membrane and arterial pressure is increased.

On the other hand, angiotensin converting enzyme (Kininase II, peptidyldipeptide hydrolase, EC 34151, hereinafter referred to as 'ACE' for convenience) hydrolyzes C-terminal dipeptides (His-Leu) of inactive angiotensin I, thereby smoothing vascular wall smooth muscle. It also converts to angiotensin II, which has contracting action, and inhibits the release of water and Na by promoting aldosterone secretion in the adrenal cortex. Bradykinin also has vascular relaxation. Decompose and deactivate (Manjusri, D and Richard, LS, J Biol Chem, 250: 6162, 1975); Davis, JO, Fed Proc, 36: 1753, 1977). This activity of ACE is a cause of hypertension.

For this reason, in vitro inhibition of ACE has been used to screen antihypertensive drugs because ACE specific inhibitors are useful for regulating blood pressure in the human body and ACE activity is closely related to the development of hypertension. Therapeutic vascular decompressants, such as captopril, enalapril, ramipril, have been synthesized as ACE inhibitors, but side effects due to the use of these drugs have been reported to affect taste, reduce white blood cells, angioedema, and liver dysfunction. There is a continuing need for the search for a substance having an antihypertensive effect.

KR 10-2015-0132988 A KR 10-1154044 B1

 Genest, J.E. and Koiw, O.K., Physiopathology and Treatment, McGraw-Hill, 1977  Kurtz, T.W. et al., N. Engl. J. Med., 317: 1043, 1987  Manjusri, D and Richard, LS, J Biol Chem, 250: 6162, 1975; Davis, JO, Fed Proc, 36: 1753, 1977

Accordingly, an object of the present invention is to provide a composition for preventing or improving hypertension and a method for producing the same, which are useful for the prevention or improvement of hypertension, have no side effects, etc., including natural products.

The composition for preventing or improving hypertension of the present invention for the above object and a method for producing the same are characterized in that the food composition or pharmaceutical composition comprising the extract and garlic as an active ingredient.

The fertilized egg further includes a yolk, and the extract of the teat is characterized in that the teat is extracted using water as a solvent.

To 100 parts by weight of the extract, characterized in that it comprises 50 to 100 parts by weight of garlic and 5 to 30 parts by weight of fertilized egg yolk.

And a method for producing a composition for preventing or improving hypertension according to the present invention comprises the steps of extracting hot water from the tapper, heating by adding garlic to the tapper extract, and cooling the heated heating material. Characterized in that.

After the heating step, further comprising the step of reheating by adding the yolk of the fertilized egg to the cooled cooling water, 50-100 parts by weight of garlic and 5-30 parts by weight of fertilized egg yolk It is characterized by the addition.

After the reheating step, the step of removing the 50 ~ 60% of the moisture of the reheated heating material, and further comprising the step of molding the heated water is removed in a ring.

According to the present invention, it shows an excellent ACE inhibitory activity and is effective in the improvement or prevention of hypertension, and also has the advantage of very excellent human safety as a natural material.

1 is a graph showing the results of Test Example 1 according to the present invention.

Hereinafter, the present invention will be described in detail.

As used herein, the term "hypertension" refers to a disease in which a systolic blood pressure is 140 mmHg or more or a diastolic blood pressure is 90 mmHg or more in an adult 18 years or older. The hypertension is classified into primary hypertension (essential hypertension) and secondary hypertension according to the cause of the onset, and the hypertension that is not identified by the onset is classified as primary hypertension, and the hypertension with the onset of the cause is classified as secondary hypertension. 95% of the identified hypertension patients are classified as primary hypertension. For the purposes of the present invention, the hypertension is not particularly limited, but may be interpreted as a target disease that can be prevented, alleviated or improved by administration of the composition of the present invention. have.

The composition for preventing or improving hypertension according to the present invention is to have the effect of inhibiting the activity of an ACE (angiotension converting enzyme), characterized in that it comprises the extract and garlic as an active ingredient.

The extract of the tap means that the extract of the persimmon, which is calyx of the persimmon fruit, using a solvent, the tap is dried or used as it is. Here, the drying method of the nipple may be natural drying or hot air drying, but is not limited thereto.

In addition, the pacifier extract refers to a resultant such as a solid component obtained by removing the solvent from the liquid component, as well as the liquid component extracted for a predetermined time in a warm state after immersing the pacifier in the solvent. In addition, it can be comprehensively interpreted to include all of the diluents of these products, their concentrates, their modifiers, and purified products in addition to the results.

More specifically, the extract of the tap water may be extracted by adding water to the tap and heating it to 40 to 100 ° C., and the extract may be filtered or removed to carry out a concentration or drying process to remove the solvent. , Filtration, concentration and drying can all be performed. Specifically, the filtration may be performed using a filter paper or a reduced pressure filter, the concentration may be concentrated under reduced pressure using a reduced pressure concentrator, for example, a rotary evaporator, and the drying may be performed by, for example, a lyophilization method.

The garlic is a beneficial component of the body contains a large amount of allicin, activating the cells, and promotes blood circulation is excellent. In the present invention, the garlic may be used as it is raw garlic, may be used in a dried form, may be used by grinding it, without limiting its form.

In addition, the composition of the present invention may further comprise yolks of fertilized eggs. The yolk of the fertilized egg is a component that helps to promote health when ingested, as well as enhances the effect of inhibiting the ACE activity through interaction with the extract of persimmon, garlic.

Here, the blending ratio of the sieve extract, garlic and fertilized egg yolk is not limited, but preferably 50 to 100 parts by weight of garlic and 5 to 30 parts by weight of fertilized egg yolk with respect to 100 parts by weight of the extract.

The composition as described above is composed of natural products and excellent in stability to the human body, and also excellent in inhibiting ACE activity can effectively prevent or improve hypertension.

The composition of the present invention may be provided as a food composition, the food composition is added to food materials, such as beverages, teas, confectionery, or a food prepared by tablets, pills, capsules, powders, suspensions, etc. Ingestion means that it has a specific effect on health, but unlike general medicine, it has the advantage that there is no side effect that can occur when taking long-term use of the drug as a raw material.

At this time, there is no particular limitation on the type of food, it is natural that it may further contain various additives according to the type of food.

In addition, the composition of the present invention may be provided as a pharmaceutical composition, more specifically, may be provided as a solid preparation for the purpose of oral administration. The solid preparations include tablets, pills, powders, granules, capsules, and the like, and such solid preparations may further include excipients.

In addition, it is obvious that in addition to the excipient, it may further include various types of pharmaceutically acceptable additives.

On the other hand, the composition according to the present invention does not limit the intake or its dosage, for example, 60kg adult weight of about 1 to 30g each can be taken three times a day before meals.

Hereinafter, a method for preparing a composition for preventing or improving hypertension according to the present invention will be described in detail.

The manufacturing method according to the present invention includes the steps of extracting hot water from the tap, and adding garlic to the tap extract to heat it. And after the step of heating, further comprising the step of reheating by adding the yolk of the fertilized egg to the heated heating water.

Faucet Hydrothermal  step.

First, prepare the nipple and wash it thoroughly. The nipple may be dried or may not be dried, but is not limited thereto. In addition, the nipple may be used as it is without grinding, or may be used by grinding about 50 ~ 200mesh.

Next, 1-3 weight times of water which is a solvent is added to the said nipple, and it heats at 40-100 degreeC. At this time, the heating time is not limited, but water is enough to reduce the evaporation by 30 ~ 50%.

Then, the extracted tap extract is filtered with filter paper to remove the tap.

remind Faucet  Heating by adding garlic to the extract.

Next, remove the husks and prepare freshly washed garlic. And by adding garlic to the extract of the faucet and heated to 40 ~ 90 ℃ 100 ~ 200 minutes.

Here, the garlic may be undried, but may be dried, and may be cut or crushed into pieces, and the form is not limited thereto.

And the amount of the garlic used is preferably 50 to 100 parts by weight based on 100 parts by weight of the extract, because such a compounding ratio shows an excellent effect on the activity of ACE.

The heated Heating water  Cooling step.

And the heated heating is cooled. At this time, the cooling method is not limited, it is sufficient if the cooling to 15 ~ 30 ℃.

The cooled On coolant  Reheating by adding yolks of fertilized eggs.

Next, only the yolk of the fertilized egg is added to the cooled coolant, and it is then reheated at 40 to 90 ° C. for 150 to 200 minutes.

At this time, the amount of the fertilized egg yolk is about 5 to 30 parts by weight based on 100 parts by weight of the extract.

The composition prepared as described above may additionally be processed into a solid preparation for oral administration as well as food.

As an example, it may be prepared as a pill. After the reheating step, the method may further include removing 50 to 60% of moisture of the reheated heating material, and molding the heated water having been removed into a ring.

That is, the reheated heating material is further heated to 100 ° C. or 100 ° C. or more, or concentrated under reduced pressure at 40 to 80 ° C. to remove water by 50 to 60%. And it is put into the refilling machine is molded into a ring and dried. At this time, the size of the ring is not limited, for example, the size of the diameter may be about 3 ~ 10mm, the molding and drying method according to the machine according to the method known in the art.

Hereinafter, specific embodiments according to the present invention will be described.

(Example 1)

The washed nappa was pulverized to about 100 mesh, and 1.86 kg of water was added to 1 kg of the pulverized nappa powder and heated to 80 ° C. for 5 hours. Then, the heated heating water was filtered through a filter cloth to obtain 1.06 kg of the extract of persimmon.

Next, 800 g of garlic which had been removed by washing the shell was added to 1.06 kg of the extract, and then heated at 60 to 80 ° C. for 150 minutes, and then allowed to stand at room temperature and cooled to 25 ° C.

The concentrated product was concentrated under reduced pressure to evaporate about 50% of moisture, and then a ring having a diameter of 4 mm was prepared using a dehydrator.

(Example 2)

The same as in Example 1,

200 g of fertilized egg yolk was added to the cooled product which was left to cool to room temperature, and heated again at 60 to 80 ° C. for 180 minutes, and then left at room temperature to cool to 25 ° C.

(Test Example 1)

Cytotoxicity Assessment

DMEM (Dulbecco's) with human hepatocytes Hep G2 (Korean Cell Line Bank, Korea) purchased with 10% fetal bovine serum (FBS) and 1% antibiotic (antibiotics; 100 U / ml of penicillin and 01 mg / ml of stereptomycin) The modified eagle medium was incubated at 37 ° C. under 5% CO 2 (95% air).

The cultured Hep G2 cells were treated with 10, 50 and 100 μM samples, respectively, and MTT (3- (4,5-Dimethylthiazol-2-yl) -2,5-Diphenyltetrazolium Bromide) solution was added to each cell. After 4 hours of reaction at 37 ° C, DMSO was added to dissolve formazan produced in the cells, and cell viability was measured by measuring absorbance at 570 nm. In this case, cells which were not treated with the compound were used as a control.

As the sample, the pills of Example 1 and Example 2 were ground and used as powder.

And the results are shown in Figure 1 attached.

As can be seen in the accompanying Figure 1, it was confirmed that the compositions of Examples 1 and 2 do not show particular cytotoxicity to human hepatocytes.

(Test Example 2)

Inhibitory effect of ACE

ACE inhibitory activity was analyzed by spectroscopic analysis according to Chang et al. In other words. 20 mM sodium borate buffer (containing 0.3 M NaCl, pH 8.3) was used to prepare a sample (EA), captopril (CP), an ACE solution and a substrate HHL solution.

ACE-catalyzed reaction was carried out by reaction at 37 ° C. for 30 minutes with the following composition: 100 μl EA or CP solution + 100 μl ACE solution (40 mM / ml) + 100 μl HHL (15 mM) solution (A1); 100 μl EA or CP solution + 200 μl borate buffer (A2); 100 μl borate buffer + 100 μl ACE solution + 100 μl HHL solution (A3); 300 μl borate buffer (A4). The enzymatic reaction was stopped by adding 3 ml of OPA solution (pH 12.0). After the reaction, the mixture was allowed to stand at 25 ° C. for 20 minutes, and the absorbance was measured at 390 nm using a spectrometer (Beckman DU-640, Brea, CA, USA). ACE inhibition rate of EA and CP was calculated by the following formula.

[Equation 1]

% Inhibition = [1-(A1-A2) / (A3-A4)] × 100

And IC ₅₀ (μM) for the ACE activity was obtained and the results are shown in Table 1 below.

Test Example 2 Results division IC ₅₀ (μM) Example 1 47.3 ± 0.4 Example 2 41.5 ± 0.2 Positive control group (captopril) 55.2 ± 0.2

As can be seen in Table 1, it was confirmed that the compositions of Examples 1 and 2 of the present invention exhibited superior ACE inhibitory activity than the control.

Therefore, it was confirmed through the above experimental example that the composition according to the present invention shows excellent ACE inhibitory activity, which is effective for the improvement or prevention of hypertension, and the human safety is also very excellent.

As mentioned above, although this invention was demonstrated in detail using the preferable embodiment, the scope of the present invention is not limited to a specific embodiment, Comprising: It should be interpreted by the attached Claim. In addition, those skilled in the art should understand that many modifications and variations are possible without departing from the scope of the present invention.

Claims (7)

Food composition for preventing or improving hypertension, characterized in that it comprises a extract and garlic as an active ingredient.
The method of claim 1,
The active ingredient further comprises a fertilized egg yolk,
The teat extract is a food composition for preventing or improving hypertension, characterized in that the extract is extracted with a solvent as a solvent.
The method of claim 2,
The food composition for preventing or improving high blood pressure, characterized in that it comprises 50 to 100 parts by weight of garlic and 5 to 30 parts by weight of fertilized egg yolk, based on 100 parts by weight of the extract.
A pharmaceutical composition for preventing or improving hypertension, comprising: extract of persimmon and garlic as an active ingredient.
Hydrothermal extraction of the nipple,
Adding garlic to the faucet extract and heating it;
Method for producing a composition for preventing or improving hypertension, characterized in that it comprises the step of cooling the heated heating.
The method of claim 5,
After the cooling step,
Reheating by adding the yolk of the fertilized egg to the cooled coolant,
The method of producing a composition for preventing or improving hypertension, characterized in that 50 to 100 parts by weight of garlic and 5 to 30 parts by weight of fertilized egg yolk is added to 100 parts by weight of the extract.
The method of claim 6,
After the reheating step,
Removing 50 to 60% of moisture of the reheated heating material;
Method for producing a composition for preventing or improving hypertension, characterized in that it further comprises the step of molding the heated water is removed in a ring.

Images