KR20190023904A - Novel extract and Use of the same - Google Patents

Abstract

The present invention provides novel extracts and uses thereof. The present invention has the advantage of being able to effectively treat, ameliorate, inhibit and / or prevent enlargement of the prostate gland.

Description

Novel extract and Use of the same < RTI ID = 0.0 >

The present invention relates to a novel extract, and more particularly to a novel extract of Aronia and a use thereof.

Black chokeberry, a fruit of Aronia, contains a high content of anthocyanin. Black chalkberry anthocyanin contained in black chokeberry is known to be effective for urinary diseases and hyperplasia of the prostate. Publication No. 10-2013-0101381)

An example of applying the supercritical extraction method to efficiently extract useful anthocyanins from fruits and beans is disclosed in Korean Patent Publication No. 10-2013-0060606, and anthocyanin- An example is known (refer to Korean Patent Laid-Open Publication No. 10-2017-0060737)

Studies on Aronia have been conducted, but since Aronia has not yet been sufficiently known, related research is needed.

On the other hand, palmitic acid is a kind of fatty acid, and its relation with Aronia is not known.

Korean Patent Laid-Open Publication No. 10-2013-0101381, (March 13, 2013), specification Korean Patent Laid-Open Publication No. 10-2013-0060606, (June 3, 2013), specification Korean Patent Laid-Open Publication No. 10-2017-0060737, (June 27, 201), specification

A problem to be solved by the present invention is to provide a novel extract of Aronia.

In addition, a problem to be solved by the present invention is to provide a use of a novel extract of Aronia.

The object of the present invention is not limited to the above-mentioned problems, and other matters not mentioned can be clearly understood by those skilled in the art from the following description.

The present invention provides an Aronia extract comprising palmitic acid.

The palmitic acid may be extracted from Aronia fruit.

The palmitic acid may be an active ingredient.

The palmitic acid may be enriched.

The above-mentioned astaxanthin extract may contain 0.7% by weight or 1.44% by weight or more of the palmitic acid in the total weight.

In addition, the above-mentioned Aronia extract may contain 13 ug / ml or 6.1 ug / ml or less of methyl 3-O-caffeoylquinic acid.

The above-mentioned Aronia extract may be one extracted by a solvent extraction method in which the Aronia fruit is extracted only as a solvent.

The solvent extraction method may include extracting the Aronia fruit with a solvent at an extraction temperature of 10 to 100 degrees Celsius.

The extraction may be performed in an accelerated solvent extractor.

The solvent may be ethanol.

The ethanol may be 80 to 100% by volume ethanol.

The extraction temperature may be 10 to 100 degrees Celsius.

The extraction temperature may be 30 degrees Celsius.

The Aromania extract may be for the treatment, improvement, inhibition or prevention of benign prostatic hyperplasia.

The treatment, improvement, inhibition or prevention may be by inhibition of one or more selected from 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue.

The Aronia is a shrub native to North America and belongs to Rosaceae, and contains anthocyanins and the like.

The aronia can be all or part of, and can be, for example, a fruit.

The present invention also provides medicinal and / or food uses for the treatment, amelioration, inhibition and / or prevention of prostate enlargement of the prostate gland extract of the present invention. Treatment is meant to include improvement or relief of symptoms associated with enlarged prostate, and prevention is meant to include inhibition of developing into a disease at a pre-disease stage.

In one embodiment, the present invention provides a pharmaceutical composition for treating or preventing enlargement of the prostate gland comprising the Aronia extract of the present invention as an active ingredient.

The treatment or prophylaxis may be by inhibition of one or more of 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue.

The composition of the present invention may contain the active ingredient in an amount of 0.01 to 99% by weight based on the total weight of the composition.

In another embodiment, the present invention provides a food composition for improving or inhibiting enlargement of the prostate gland comprising the Aronia extract of the present invention as an active ingredient.

The improvement or inhibition may be due to one or more inhibition selected from 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue.

Unless otherwise indicated, the food composition is equally applied to the pharmaceutical composition of the present invention, unless otherwise stated. This " improvement " is included in the " treatment " and means that the condition or symptom is improved. The term " inhibition " means inhibiting the occurrence of a condition or symptom, and may be included in prevention.

The food composition may be variously contained in foods containing beverages, and may be in the form of beverages, gums, tea, health functional foods, etc. The health functional foods may be formulated into tablets, capsules and the like. The term "functional food" as used herein refers to foods prepared (processed) by using raw materials or ingredients having useful functions in accordance with the Korean Health Function Food Act, and the term "functional" To the nutritional control of the structure and function of the body, and to obtain a beneficial effect for health use such as physiological action. The food composition may comprise conventional food additives, and the food additives may be selected from natural compounds such as ketones, chemical compounds such as glycine, sodium citrate, nicotinic acid, cinnamic acid, etc., Additives, L-sodium glutamate preparations, noodle-added alkalies, preservative preparations, tar coloring preparations and the like. In addition, the food composition includes food additives and the like.

The present invention also provides a method of treating or preventing prostate enlargement comprising the step of administering to a mammal, including a human, in need of the Aromania extract of the present invention. The present invention also provides the use of the Aromania extract of the present invention for the manufacture of a preparation for the treatment or prophylaxis of benign prostatic hyperplasia. The administered Aronia extract may be an effective amount of an Aronia extract.

Unless otherwise indicated, the phrases referred to in the pharmaceutical compositions, food compositions, methods, and uses of the invention are each the same unless otherwise indicated.

The extract or the composition of the present invention can be administered orally or parenterally to mammals including humans, and the active ingredient can be formulated together with a pharmaceutically acceptable carrier to be formulated and administered. In the case of formulation, diluents or excipients such as fillers, extenders, binders, humectants, disintegrants and surfactants which are usually used can be used. Solid form preparations for oral administration include tablets, pills, powders, granules, capsules and the like, which may contain at least one excipient such as starch, calcium carbonate, sucrose, lactose and And / or gelatin. In addition, lubricants such as magnesium and talc are also used. Liquid preparations for oral administration include suspensions, solutions, emulsions and syrups. Various excipients such as wetting agents, sweetening agents, fragrances and / or preservatives, and the like are used in addition to commonly used simple diluents such as water and liquid paraffin. . Formulations for parenteral administration include injectable solutions, suspensions, emulsions, lyophilisers, nasal cleansers, and suppositories. Injectable solutions, suspensions and emulsions may be prepared by mixing water, non-aqueous or suspensions, and active ingredients. Examples of non-aqueous and suspensions include vegetable oils such as propylene glycol, polyethylene glycol and olive oil, ethyl oleate , And the like. As a base for suppositories, witepsol, macrogol, tween 61, cacao paper, laurin, glycerol and / or gelatin can be used. For parenteral administration, it can be administered by subcutaneous injection, intravenous injection, or intramuscular injection.

The extract of Aronia contained in the composition of the present invention or used in the use or method can be used in a dose of 0.01 to 1000 mg / kg, preferably 1 to 500 mg / kg per day on an adult basis. The administration can be administered once or several times a day. However, the scope of the present invention is not limited by the dose and the number of administrations.

The above-mentioned astaxanthin extract can be formulated by adding additives such as pharmaceutically or pharmacologically acceptable carrier, excipient or diluent. Remington's Pharmaceutical Science (recent edition), Mack Publishing Company, Easton PA , Which is incorporated herein by reference.

Accordingly, the composition of the present invention may further comprise a pharmaceutically acceptable additive or a pharmaceutically acceptable additive, and may be composed of the active ingredient and the pharmaceutically acceptable excipient or the pharmaceutically acceptable excipient.

The present invention can effectively treat, ameliorate, inhibit and / or prevent enlargement of the prostate gland.

FIG. 1 is a photograph showing the prostate tissue images taken to confirm the difference in prostate size according to the administration of astaxanthin extract and the graph showing the weight of the prostate (upper arm) and the PI index It is a graph (Howe).
FIG. 2 is a graph showing the amount of DHT produced in the prostate tissue (left) and a graph showing the amount of 5AR expression (right) according to experimental groups.
FIG. 3 is a graph showing the amount of marker expression in the prostate tissue in each test group. FIG. 3 is a graph showing the amount of AR expression, a graph showing the amount of PSA expression, and a graph showing the amount of PCNA expression (lower left).
FIG. 4 is a graph showing the MS spectrum of the Aroma extract (T1). FIG.
FIG. 5 is a graph showing the MS spectrum of the Aroma extract (T2). FIG.
FIG. 6 is a graph showing the MS spectrum of the extract of Aronia (T3). FIG.
FIG. 7 is a graph showing the MS spectrum of the extract of T4.
FIG. 8 is a graph showing the structural formula of palmitic acid in the MS analysis result that the peak indicated by Palmitic acid in the peak of FIG. 4 is attributed to a component showing the molecular structure of palmitic acid.

BRIEF DESCRIPTION OF THE DRAWINGS The advantages and features of the present invention and the manner of achieving them will be more apparent from the following detailed description taken in conjunction with the accompanying drawings. The present invention may, however, be embodied in many different forms and should not be construed as being limited to the embodiments set forth herein. Rather, these embodiments are provided so that this disclosure will be thorough and complete, and will fully convey the scope of the invention to those skilled in the art. But is only provided to fully inform the owner of the scope of the invention, and the present invention is only defined by the scope of the claims.

Throughout the specification, "and / or" include each and every combination of one or more of the components mentioned.

The terminology used herein is for the purpose of illustrating embodiments and is not intended to be limiting of the present invention. In the present specification, the singular form includes plural forms unless otherwise specified in the specification. It is noted that the terms " comprises "and / or" comprising ", as used herein, do not exclude the presence or addition of one or more other elements and / or steps.

In the present specification, 'Aronia' means all or part of the Aronia tree (eg, fruit) that has not been subjected to a separate drying process after being harvested or has been subjected to a drying process.

Hereinafter, the results of the experiment confirmed that the novel extract of the present invention is very effective for the benign prostatic hyperplasia.

The reagents and the like used in the examples were the highest available from the market, and those purchased from Sigma Co. were used.

≪ Example 1 >

1-1. Manufacture of Aromania extract

Aronia fruit (obtained from Samhung, an agricultural company) was stored frozen until harvest. Aronia fruit was lyophilized, pulverized and pulverized, and extracted with an accelerated solvent extraction apparatus (SpeedExtractor E-916) at an extraction pressure of 100 bar. Four kinds of extracts (T1 to T4) were prepared by extracting 60 v / v% ethanol alcohol or 100 v / v% ethanol alcohol as extraction solvent at low temperature (30 ° C.) or high temperature (100 ° C.) for 10 minutes . The extract was concentrated under reduced pressure in the shade state and then lyophilized and powdered. The extraction solvent and extraction temperature for each extract are summarized in Table 1.

Aromania extract Extraction solvent Extraction temperature T1 100 v / v% ethanol 30 degrees Celsius T2 100 v / v% ethanol 100 degrees Celsius T3 60 v / v% ethanol 30 degrees Celsius T4 60 v / v% ethanol 100 degrees Celsius

1-2. Animal experiment

1-2-1. Preparation of experimental animals

Experimental animals were male Wistar rats aged 6 weeks. The experimental animals were kept at 23 ± 2 ℃, 55 ± 5% relative humidity and 12 hours for light and dark. The experimental animals were housed 2 per cage, and the weighing and changing of the bedding were carried out once every 5 days.

1-2-2. Preparing Animal Model for Greater Prostate

The experimental animals prepared in 1-2-1. Were subjected to castration in order to exclude the effect of intrinsic testosterone after a week of purifying period. The test animals were anesthetized with isoflurane and the back surface was laid facing to the operator and the skin at the end of the scrotum was incised, and the left and right testes and epididymis were cut out and the incision surface was sutured. In the vehicle control group, only skin incision and repair were performed. All the experimental animals were treated with antibiotics (cefazolin) and carprofen to alleviate inflammation and pain. After stabilization for 10 days after castration, the wound was healed and the testosterone propionate (TP) was intraperitoneally administered. The animals at the time of initiation were weighed 200-250 g on average per group, and were placed so that they were not in a cage between the other groups during the experiment, and water and feed were fed freely. All experimental animals except the control group were intraperitoneally injected with 3 mg / kg body weight / day of testosterone propionate (TP) to induce enlargement of the prostate gland. In order to minimize the error of the experiment, , The total injection volume was dissolved in corn oil so as to have a volume of 100 μl. The control group was intraperitoneally injected with 100 μl of corn oil without testosterone propionate (TP).

1-2-3. Experiment group configuration and processing

TP was administered once a day for 6 weeks after the start of administration, and the test substance (physiological saline, soap palmetto, or Ahnia extract) was administered together with TP but administered orally. Each experimental group was constructed as shown in Table 2 below, and 8 animals were per group. TP was administered to each experimental group according to the body weight of the experimental animals, so that the total volume did not exceed 100 袖 l, and care was made so as not to cause inflammation at the injection site. In order to reduce the administration error of the hormone and the sample, the weight of the experimental animals was measured every 7 days, and the concentration corresponding to each individual was calculated and administered. The extracts of Aronia were weighed and weighed to the concentration of 0.5% -CMC and then administered orally.

group Treatment condition Negative control group
(Negative control) TP (3 mg / kg body weight, i.p.) + physiological saline (10 mg / kg body weight, p.o.) Positive control group
(Positive control) TP (3 mg / kg body weight, i.p.) + saw palmetto (100 mg / kg body weight, p.o.) T1 treated group TP (3 mg / kg body weight, i.p.) + Aronia extract T1 (100 mg / kg body weight, p.o.) T2 treated group TP (3 mg / kg body weight, i.p.) + Aronia extract T2 (100 mg / kg body weight, p.o.) T3-administered group TP (3 mg / kg body weight, i.p.) + Aronia extract T3 (100 mg / kg body weight, p.o.) T4-administered group TP (3 mg / kg body weight, i.p.) + Aronia extract T4 (100 mg / kg body weight, p.o.)

1-2-4. Autopsy and sampling

After anesthetizing the animals, arterial blood was collected from the abdominal artery using an SST tube, left at room temperature for 1 hour, centrifuged at 3000 rpm, and serum was isolated at 3 ml or more. Immediately after the blood collection, the cervical dislocation was euthanized. The prostate and bladder were removed, carefully separated, washed once with PBS, and lightly removed. Some of the extracted prostates were fixed in 10% neutral buffered formalin solution for histopathological examination and some were stored at -80 ° C for gene and protein analysis.

1-2-5. Prostate shots and weighing results

The prostate and bladder removed from 1-2-4 were photographed, and some of the results are shown in FIG. In addition, the prostate weight was measured and converted to PI (Prostate index) index. The PI index, which represents the degree of hypertrophy of the prostate, was calculated as the percentage of prostate weight per body weight. The prostate weight and PI index are also shown in FIG. FIG. 1 is a graph showing a photograph of a prostate tissue specimen taken to confirm the prostate size difference due to the administration of an extract of Aronia in an asymptomatic animal model of prostate hyperplasia, a graph showing the weight of the prostate (upper arm) (Howe). As a result, prostate size was found to be smaller in the astronomic extract group (T1 to T4) than in the negative control group (NC), and the positive control group (PC) was not significantly different from the negative control group (NC). In addition, the PI index was the lowest in T2 treated group with Aronia extract, but the difference between the groups treated with Aronia extract (T1 to T4) did not seem to be large.

These results suggest that the Ahnonia extract of the present invention has an effect on the enlargement of the prostate gland and does not show a significant difference between the extracts in terms of prostate size.

Therefore, further experiments were conducted to further investigate the difference in efficacy between the extracts in relation to the enlargement of the prostate gland.

Specifically, experiments were carried out to examine the effect of Aronia extract on 5AR expression, DHT production, AR expression, PSA expression and PCNA expression in prostate tissue.

Testosterone produced in testis is transferred into prostate cells and converted to DHT (dihydrotestosterone) by 5AR (5-alpha reductase). Converted DHT binds to androgen receptors (AR) (5AR, AR, PSA, and DHT) on prostate glandular hyperplasia by inducing PSA (prostate specific antigen) expression by acting as a transcription factor. In order to confirm it in more detail. We also investigated the effects of Ahniae extract on prostate hyperplasia induced by prostate cell proliferation by confirming the effect of Ahniae extract on proliferating cell nuclear antigen (PCNA).

1-2-6. 5AR expression in prostate tissue, confirmation of inhibition of DHT production

For some of the prostate tissues collected at 1-2-4, 5AR and DHT production were measured. Specifically, the following method was used.

To 100 mg of prostate tissue, 1 ml of cold PBS was added, followed by pulverization using a homogenizer, followed by centrifugation at 1000 g for 15 minutes to obtain a supernatant. The amount of 5AR expression in tissues (# CSB-EL022654RA, Cusabio Biotech Co., Ltd., China) and the amount of DHT produced (# CSB-E07878h, Cusabio Biotech Co., Ltd., China) were measured using an ELISA kit, Experiments were conducted according to the kit instructions. 50 μl of supernatant was subjected to shaking incubation at room temperature for 1 hour with HRP-conjugate and antibody in a 96-well microplate coated with goat-anti-rabbit antibody. After incubation, the substrate solution was added, and after 15 minutes, the reaction was stopped with sulfuric acid solution, and the difference between samples was measured at 450 nm within 10 minutes. Calculation of the measured values is performed using a standard graph and the unit is expressed in pg / mL.

The experimental results are shown in Fig. FIG. 2 is a graph showing the amount of DHAR produced in the prostate tissue by the experimental group (left) and a graph showing the amount of 5AR expression in the prostate tissue by the experimental group (right).

As shown in FIG. 2, the amount of 5AR expression and DHT production in the tissues treated with astaxanthin extract (T1-T3) were significantly lower than those in the experimental group (NC) that induced prostate enlargement. Especially, in the T1 treated group, the decrease of the DHT production was remarkable, which is more effective than the positive control (PC). There was no significant difference in the amount of DHT produced in the T4 administration group.

1-2-7. Confirmation of inhibition of AR, PSA, PCNA expression in prostate tissue

The mRNA expression levels of the markers (AR, PSA, PCNA) were measured by PCR analysis on some of the prostate tissues collected in 1-2-4. Specifically, the following method was used.

To extract the RNA from the prostate tissue, 1 ml of QIAzol lysis reagent was added to 10-20 mg of tissue extracted, homogenized with a homogenizer, and extracted according to the manufacturer's protocol (Qiagen). The total RNA extracted was quantified by ds-11 plus spectrophotometer (Denovix). For cDNA synthesis, 1 μg of total RNA was reacted in a thermocycler (Biorad) with a total volume of 20 μl according to the protocol of QuantiTect reverse transcription kit (Qiagen), and cDNA synthesized through ds-11 plus spectrophotometer (Denovix) was quantified .

The real-time PCR reaction was performed using Gotaq qPCR Master mix (promega) using the principle that SYBR Green I fluorescent reagent binds to DNA and emits light. For the reaction, 100 ng of cDNA, 25 μl of Gotaq qPCR Master mix , forward primer (10 pmole) and reverse primer (10 pmole) were added to a final volume of 50 μl. The primer base sequence used in the composition is as follows.

AR: forward-caaagggttggaaggtgaga (SEQ ID NO: 1),

    reverse-cccagagctacctgcttcac (SEQ ID NO: 2)

PSA: forward-gggggcaaagatatatcaa (SEQ ID NO: 3),

     reverse-gcacaccatcacaaatgagg (SEQ ID NO: 4)

PCNA: forward-ttggaatcccagaacaggag (SEQ ID NO: 5),

      reverse-agaaaacttcaccccgtcct (SEQ ID NO: 6)

GAPDH: forward-agacagccgcatcttcttgt (SEQ ID NO: 7),

       reverse-tgatggcaacaatgtccact (SEQ ID NO: 8)

PCR was carried out using a Mx 3000P QPCR system (Agilent) at a denaturation temperature of 95 ° C for 2 min, a denaturation temperature of 95 ° C for 15 sec, and an annealing temperature of 60 ° C for 1 min. For the analysis of the results, comparative quantification method using Ct value was used and the amount of each expression was presented based on the amount of GAPDH expression.

The experimental results are shown in Fig. FIG. 3 is a graph showing the expression level of the marker in the prostate tissue according to the experimental group, and graphs (upper left) showing the AR expression amount, upper left graph showing the PSA expression amount, and graph showing the PCNA expression amount (lower left) will be.

As shown in FIG. 3, PCNA expression levels were significantly decreased in the astronomic extract-treated groups (T1 to T4) as compared with the negative control group (NC), and it was found to be particularly effective in the T1-treated group and the T2-treated group. In addition, the expression of AR was decreased in T1 and T2 treated group, and PSA was also decreased in T1 treated group, but no significant change was observed in T4 treated group.

From the above results, it can be concluded that the extracts of T1 and T2 are more effective than the extracts of T3 and T4. Especially, in the inhibition of AR expression, T1 and T2 extracts showed significant effects, but T3 and T4 extracts did not show such effects.

To determine the cause of these differences, the components of each extract were analyzed as follows.

1-3. Analysis of components of Aromaniae extract

1-3-1. Preparation of test solution and standard solution

A standard stock solution of 100 ug / ml was prepared by dissolving the compounds isolated from Aronia using HPLC beforehand in methanol. Using this, five working standard solutions ranging from 200 ug / ml to 12.5 ug / ml were prepared and used in the experiments. Each of the extracts (T1 to T4) was dissolved in the same volume of methanol and filtered through a membrane filter (44513-NP PTFE, diameter 17mm, pore size 0.45um) to be used as the sample solution for HPLC analysis.

1-3-2. HPLC analysis

In order to select the most suitable conditions for separating the main components of the Aromaniae extract, the sensitivity and the separation ability were examined by changing the type of the column and the composition ratio of the solvent with reference to the literature. Water containing 0.1% TFA and cyanomethyl (MeCN) were monitored at UV 280, 360, and 520 nm under the concentration gradient of Table 3 as developing solvent. The HPLC column used for the analysis was phenomenex gemini (4.6 × 250 mm, 5 μm), flow rate was 1.0 ml / min, column temperature was 30 ° C., and sample injection amount was 20 μl.

Final time (min) Flow rate (ml / min) 0.1% TFA-Water (%) MeCN (%) 0 1.0 90 10 5 1.0 85 15 15 1.0 85 15 45 1.0 70 30

1-3-3. MS analysis

The Q-TOF MS (Agilent 6530) was used to measure the MS chromatogram of the extract of Aronia. The total ion chromatogram (TIC) was monitored in the negative mode, and the analysis conditions are shown in Table 4 below.

Parameter Value Gas temperature (캜) 300 Gas flow rate (L / min) 9 Nebulizer (psig) 45 Sheath gas temperature (° C) 350 Sheath gas flow rate (L / min) 11

1-3-4. Analysis of anthocyanin and phenolic compounds in extracts

Since it is known that Aronia is rich in polyphenol components, especially anthocyanins, and anthocyanin components are known to have an effect on male urinary system-related diseases, in order to determine whether the difference in the effect between extracts is due to anthocyanin, For the extracts (T1 to T4), HPLC analysis was carried out and the content of major anthocyanin and phenolic compounds contained in the extract was analyzed. HPLC analysis was carried out in the manner described in 1-3-2. The compound to be analyzed is a compound of the following formulas (1) to (4): 1- (3,4-dihydroxycinnamoyl) cyclopenta-2,3-diol (compound of formula 1), Methyl 3-O- caffeoylquinic acid 3-bD-glucopyranose (compound of formula 3) and Cyanidin-3-bD-arabinopyranose (compound of formula 4). The compounds of the formulas (1) to (4) were isolated from aronia and used as standard compounds.

[Chemical Formula 1]

(2)

(3)

[Chemical Formula 4]

The results of the analysis are shown in Table 5 below.

Aromania extract Compound (1)
(mg / ml) Compound (2)
(ug / ml) Compound (3)
(mg / ml) Compound (4)
(mg / ml) T1 0.200 6.019 0.702 1.307 T2 0.216 12.833 0.462 1.191 T3 0.196 15.958 0.471 1.147 T4 0.222 31.558 0.523 1.289

As shown in Table 5, the compounds of formula (I) and the compound of formula (IV) do not show a significant difference in the content of the four extracts, but the compound of formula (II) and the compound of formula (III) show a significant difference in content. The compound of formula 2 showed a relatively high concentration in the extract (T4), which has the least effect on the enlargement of the prostate. In addition, the compound of formula (3) is an anthocyanin component, which is contained at a relatively high concentration in one extract (T1), and the remaining extracts (T2 to T3) contain an amount within an error range (0.462-0.523 mg / ml) appear. However, such results were contrary to expectations. Since the compound of formula (III) was previously known as an ingredient containing aronia that is effective for male urinary system-related diseases, the compound of formula (III) is more effective for the extract (T2) As well as the fact that it can be included.

In order to find out the reason for such a result, MS analysis was used to analyze the components of the extract which are highly correlated with the effect on the enlarged prostate. Specifically, the same method as in 1-3-5.

1-3-5. MS analysis of extract components

The components of the extract were analyzed by the method of 1-3-3. The results are shown in FIGS. 4 to 8. FIG. FIG. 4 is a graph showing the MS spectrum of the extract of Aronia (T1), FIG. 5 is a graph showing the MS spectrum of the Aronia extract (T2), and FIG. 6 is a graph showing the MS spectrum of the Aronia extract (T3) , And FIG. 7 is a graph showing the MS spectrum of the extract of T4. FIG. 8 is a graph showing the structural formula of palmitic acid in the MS analysis result that the peak indicated by Palmitic acid in the peak of FIG. 4 is attributed to a component showing the molecular structure of palmitic acid. From these results, as shown in FIG. 4 to FIG. 7, the ion peak showing a significant correlation with the effect of each extract was revealed by MS analysis, and the component corresponding to the peak was found to be palmitate as MS Analysis. In addition, the content of palmitic acid contained in each extract was calculated from the corresponding peak value. As a result, it was found that the palmitic acid contained 1.441 wt% of T1, 0.707 wt% of T2, 0.245 wt% of T3, and 0.548 wt% of T4. Considering that T1 and T2, which exert more excellent effects on benign prostatic hyperplasia, are both 0.7% by weight or more of palmitic acid, the extract of Aronia containing 0.7% by weight or more of palmitic acid Is more effective for the benign prostatic hyperplasia.

1-4. Analysis of experimental results

Compared with the other extracts (T3 and T4), the Aroma extract (T1, T2) containing palmitic acid in an amount of 0.7 wt% or more contained palmitic acid in a high content. Indicating a high correlation. Thus, it can be seen that the Aroma extract of the present invention has an effect on the enlargement of the prostate gland depending on the content of palmitic acid contained therein.

Since the extract of the present invention has an effect on the enlargement of the prostate gland depending on the contained palmitic acid, the effect can be easily controlled by controlling the concentration of palmitic acid contained therein. As described above, the extract of the present invention, which not only exerts an effect on the enlargement of the prostate gland but also can easily control its effect, can be more effectively used depending on the state of the enlarged prostate gland. As a result, the extract of Aronia containing palmitic acid, like the Aronia extract of the present invention, has not been known before, so it is not only novel but also remarkable.

Considering that the extract (T2) containing palmitic acid in an amount of not less than 0.7% by weight and the extract (T1) containing not less than 1.44% by weight are effective in treating enlargement of the prostate in reference to Table 5 and the like, It is understood that a composition comprising an extract of Aronia containing an acid in an amount of preferably 0.7 wt% or more, more preferably 1.44 wt% or more, and a composition thereof is more effective for improving, treating, inhibiting, and / or preventing prostatic hyperplasia .

In addition, the extract (T2) containing methyl 3-O-caffeoyl-quinic acid in an equivalent amount of 13 ug / ml or less and the extract (T1) containing 6.1 ug / ml or less in terms of equivalent amount are effective on the enlargement of the prostate When considered, the extract of Aronia may contain methyl 3-O-caffeoyl-quinic acid in an amount of preferably not more than 13 ug / ml, more preferably not more than 6.1 ug / ml.

As a result, it can be seen that the extract or composition of the present invention is particularly effective in improving, treating, inhibiting, and / or preventing prostatic hyperplasia.

≪ Preparation Example 1 > Preparation of pharmaceutical composition

100 mg of corn starch, 100 mg of lactose, and 2 mg of magnesium stearate prepared in the same manner as in Example 1-1 were packed in gelatin capsules to prepare capsules.

≪ Preparation Example 2 > Preparation of food composition

(10% by weight), liquid fructose (0.5% by weight), oligosaccharides (2% by weight), sugar (2% by weight), and the like were prepared in the same manner as in Example 1-1, Water was added to the salt (0.5% by weight) to adjust the remaining amount, and homogeneously mixed and instant sterilized to prepare a health drink.

<110> Gyeongnam National University of Science and Technology Industry-Academic Cooperation Foundation          KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY <120> Novel extract and Use of the same <130> GP17048 <160> 8 <170> Kopatentin 2.0 <210> 1 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Forward primer for AR <400> 1 caaagggttg gaaggtgaga 20 <210> 2 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Reverse primer for AR <400> 2 cccagagcta cctgcttcac 20 <210> 3 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Forward primer for PSA <400> 3 gggggcaaag atatatgcaa 20 <210> 4 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Reverse primer for PSA <400> 4 gcacaccatc acaaatgagg 20 <210> 5 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Forward primer for PCNA <400> 5 ttggaatccc agaacaggag 20 <210> 6 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Reverse primer for PCNA <400> 6 agaaaacttc accccgtcct 20 <210> 7 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Forward primer for GAPDH <400> 7 agacagccgc atcttcttgt 20 <210> 8 <211> 20 <212> DNA <213> Artificial Sequence <220> <223> Reverse primer for GAPDH <400> 8 tgatggcaac aatgtccact 20

Claims (9)

Aromania extract containing palmitic acid. The extract of claim 1, wherein the palmitic acid is present in an amount of at least 0.7 wt% of the total weight. The extract of claim 1, wherein the atorvastatin extract is extracted by a solvent extraction method in which the arhnia fruit is extracted only as a solvent. The extract of claim 1, wherein the atorvastatin extract is for treating, improving, inhibiting or preventing prostatic hyperplasia. 5. The extract of claim 4, wherein said treatment, improvement, inhibition or prevention is by at least one inhibitor selected from 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue. A pharmaceutical composition for treating or preventing prostatic hyperplasia comprising an extract of Aronia as an active ingredient. 7. The pharmaceutical composition according to claim 6, wherein said treatment or prevention is by inhibition of at least one selected from 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue. A food composition for improving or inhibiting prostatic hyperplasia comprising an extract of Aronia as an active ingredient. 9. The food composition of claim 8, wherein the improvement or inhibition is by inhibition of at least one selected from 5AR expression, DHT production, AR expression, PSA expression, or PCNA expression in prostate tissue.

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