KR102376521B1 - Composition for preventing, improving or treating prostate disease comprising extract of Ainsliaea acerifolia as effective component - Google Patents

Abstract

The present invention relates to a composition for preventing, improving, or treating prostate disease, comprising an extract of maple leaf as an active ingredient. The present invention is a pharmaceutical composition for preventing or treating prostate disease, comprising an extract of maple leaf ( Ainsliaea acerifolia ) as an active ingredient.

Description

Composition for preventing, improving or treating prostate disease comprising extract of Ainsliaea acerifolia as effective component

The present invention relates to a composition for preventing, improving, or treating prostate disease, comprising an extract of maple leaf as an active ingredient.

The prostate is an organ that produces various secretions to prevent the urethra from drying out, and is closely related to androgens, the male hormone. As the secretion increases, it gets bigger, and the prostate in the 20s and 30s is maintained until the 50s, and then it becomes enlarged. This is called benign prostatic hyperplasia, and even if the size is returned to normal with hormone treatment, there is a high risk of side effects, and it is difficult to cure because it will return to its original state as soon as the hormone treatment is stopped.

Representative diseases occurring in the prostate include an enlarged prostate, chronic prostatitis, and prostate cancer. Although prostatitis has various causes, it is mainly caused by bacterial infection, inflammation of unknown cause, and chronic pain. Prostate cancer is a malignant tumor in the relatively outer part of the prostate. It accounts for about 35% of all male cancer patients, and it is said to be increasing by 2-3% every year. The incidence in Korea is three per 100,000 people, which is not yet at a level of concern, but the rate is gradually increasing due to the westernized diet and the rapidly increasing elderly population.

On the other hand, Benign prostatic hyperplasia (BPH) is a disease in which the prostate gland tissue around the urethra grows and compresses the urethra due to aging and imbalance of sex hormones. It is a male disease. Recently, in Korea, the rate of increase in the number of patients with BPH has been increasing rapidly, exceeding 20% every year, and it is caused by excessive proliferation of smooth cells and epithelial cells in the prostate transition zone. It is known that this is due to anatomical occlusion by an enlarged prostate and functional occlusion by α1-receptor that contracts prostate smooth muscle. The main symptoms of obstruction include thin and weak urine stream or weak urine, delayed urine that has to wait for a long time to start urinating, interruption of urination unintentionally while urinating, drip-like drips at the end of urination, and a feeling of residual urination, etc. This is an example. Among the various mechanisms of prostate enlargement, the representative mechanisms are known to be related to the male hormones testosterone (T) and dihydrotestosterone (DHT).

On the other hand, maple leaf (Ainsliaea acerifolia ) is commonly grown in the mountains. The underground stem is stretched, the stem stands upright, does not branch, and the height is 35-80cm. Long brown hairs all over. Leaves with long petioles are turned in the middle of the stem. Leaves are 6-12.5cm long and 6.5-19cm wide, palm-shaped and shallowly split into 7-11 pieces, and the split pieces are again shallowly split into 3 pieces. The cracked piece is triangular, with a sharp tip and serrated edges. There are some hairs on both sides of the leaf and petiole, and the length of petiole is 5~13cm. The white flowers bloom from July to September, and several capillary flowers are formed at the ends of stems in raceme inflorescences. The head flower consists of 3 tubular flowers, 1-1.5cm in diameter, and the involucre is cylindrical and has a slightly red color, and many pieces of egg-shaped or long oval-shaped bracts are arranged in several rows. The fruit is aqueous, 9mm long, has a wide oval shape, has vertical ridges, and ripens from October to November. The tubular hairs are white, and the length is 10-11 mm. Eat young shoots It is distributed in Korea, China and Japan. A similar type of leaf with a thin dented part is called Gaya maple leaf (var. subapoda), and it is mainly grown in Mt. Gaya.

Korean Patent No. 1522273 and Korean Patent No. 1793379 disclose turmeric extract and turmeric thorn extract, which show androgen receptor reduction and prostate weight reduction effects as a prevention and effect of benign prostatic hyperplasia, but the maple extract of the present invention is effective There is no disclosure of a composition for preventing, improving or treating prostate disease, including as a component.

Korean Patent Registration No. 10-1522273 Korean Patent No. 10-1793379

The problem to be solved by the present invention is to provide a composition for preventing, improving or treating prostate disease, which includes an extract of maple leaf as an active ingredient.

The present invention provides a pharmaceutical composition for preventing or treating prostate disease comprising an extract of maple leaf ( Ainsliaea acerifolia ) as an active ingredient.

The extraction solvent of the maple odor extract may be water, a C1-C4 lower alcohol, or a mixture thereof.

The prostate disease may be prostatitis, an enlarged prostate, or lower urinary tract due to an enlarged prostate.

The maple leaf extract can reduce the content of DHT (dihydrotestosterone) or testosterone (testosterone) in tissue or serum.

In addition, the present invention provides an agent for improving dysuria caused by prostate disease comprising a pharmaceutical composition as an active ingredient.

In addition, the present invention provides a health functional food composition for preventing or improving prostate disease comprising an extract of maple leaf ( Ainsliaea acerifolia ) as an active ingredient.

The maple odor ( Ainsliaea acerifolia ) extract may be prepared in any one formulation selected from beverages, pills, tablets, capsules, and powders.

The present invention reduces the weight of the prostate thickened by prostatic hyperplasia (BPH) and significantly reduces the content of testosterone and DHT in serum and prostate, so it can be effectively applied to prostate diseases such as benign prostatic hyperplasia, prostatitis or prostate cancer. can

1 is a result confirming the weight change of the prostate according to the administration of the extract of the present invention. NC is negative control; BPH is an enlarged prostate; BPH+AA inducing benign prostatic hyperplasia and treated with maple extract; BPH+Finasteride is a group treated with finasteride as a benign control and inducing enlargement of the prostate.
Figure 2 is the result of confirming the change in the DHT content in the protein extracted from the ionizing gland tissue according to the administration of the maple leaf extract of the present invention. NC is negative control; BPH is an enlarged prostate; BPH+AA inducing benign prostatic hyperplasia and treated with maple extract; BPH+Finasteride is a group treated with finasteride as a benign control and inducing enlargement of the prostate.
3 is a result confirming the change in the content of testosterone in serum according to the administration of the extract of the present invention. NC is negative control; BPH is an enlarged prostate; BPH+AA inducing benign prostatic hyperplasia and treated with maple extract; BPH+Finasteride is a group treated with finasteride as a benign control and inducing enlargement of the prostate.
4 is a result of H&E staining of prostate tissue according to the administration of a maple extract of the present invention. NC is negative control; BPH is an enlarged prostate; BPH+AA inducing benign prostatic hyperplasia and treated with maple extract; BPH+Finasteride is a group treated with finasteride as a benign control and inducing enlargement of the prostate.
5 is a result confirming the thickness change of the prostate epithelial tissue according to the administration of the extract of the present invention. NC is negative control; BPH is an enlarged prostate; BPH+AM induces prostatic hyperplasia and is treated with Maple odor extract; BPH+Finasteride is a group treated with finasteride as a benign control and inducing enlargement of the prostate.

Hereinafter, preferred embodiments of the present invention will be described in detail. Throughout the specification, when a part "includes" a certain component, it means that other components may be further included, rather than excluding other components, unless otherwise stated.

The present invention relates to a pharmaceutical composition for preventing or treating prostate disease, comprising an extract of maple leaf ( Ainsliaea acerifolia ) as an active ingredient.

The prostate disease is preferably, but not limited to, benign prostatic hyperplasia, prostate cancer or prostatitis, and more preferably prostatic hyperplasia, which may include hair loss or urination disorder due to benign prostatic hyperplasia.

The maple odor extract may be prepared by a method comprising the following steps, but is not limited thereto:

(1) extracting by adding an extraction solvent to the odor of autumn leaves;

(2) filtering the extract of step (1); and

(3) Concentrating the filtered extract of step (2) under reduced pressure and drying to prepare an extract.

In step (1), the extraction solvent is preferably selected from water, C1-C4 lower alcohol or a mixture thereof, more preferably C1-C4 lower alcohol, even more preferably 95% (v/ v) Pretanol (Alcohol, Prethanol), but not limited thereto.

In the above production method, the extraction method may use all conventional methods known in the art, such as filtration, hot water extraction, immersion extraction, reflux cooling extraction, and ultrasonic extraction. The extraction solvent is preferably added by adding 1 to 20 times the weight of the dried maple odor, more preferably 5 to 15 times. The extraction temperature is preferably 4 to 50 ℃, but is not limited thereto. In addition, the extraction time is preferably 0.5 to 10 hours, more preferably 0.5 to 5 hours, but is not limited thereto. In the above method, it is preferable to use a vacuum vacuum concentrator or a vacuum rotary evaporator for the concentration under reduced pressure in step (3), but is not limited thereto. In addition, drying under reduced pressure, vacuum drying, boiling drying, spray drying or freeze drying is preferable, but is not limited thereto.

The maple leaf extract may reduce the content of dihydrotestosterone (DHT) or testosterone in tissue or serum, and the tissue may be prostate tissue.

The pharmaceutical composition of the present invention may further include a carrier, excipient, or diluent in addition to the maple odor extract.

The pharmaceutical composition of the present invention may be administered orally or parenterally, and when administered parenterally, it is preferable to select an external skin or intraperitoneal, rectal, intravenous, muscle, subcutaneous, intrauterine dural or intracerebrovascular injection method.

The pharmaceutical composition of the present invention may be prepared using a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, and a surfactant. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations include at least one excipient in one or more compounds, for example, starch, calcium carbonate, sucrose or lactose ( lactose), gelatin, etc. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid formulations for oral administration include suspensions, solutions, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, fragrances, and preservatives may be included. there is. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. As the non-aqueous solvent and the suspending solvent, propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate may be used. As the base of the suppository, witepsol, macrogol, tween) 61, cacao butter, laurin, glycero gelatin, and the like can be used.

The composition according to the present invention is administered in a pharmaceutically effective amount. In the present invention, "pharmaceutically effective amount" means an amount sufficient to treat a disease at a reasonable benefit/risk ratio applicable to medical treatment, and the effective dose level is the type, severity, and drug activity of the patient. , can be determined according to factors including sensitivity to drug, administration time, administration route and excretion rate, duration of treatment, concurrent drugs, and other factors well known in the medical field. The composition of the present invention may be administered as an individual therapeutic agent or in combination with other therapeutic agents, may be administered sequentially or simultaneously with conventional therapeutic agents, and may be administered singly or multiple times. In consideration of all of the above factors, it is important to administer an amount that can obtain the maximum effect with a minimum amount without side effects, which can be easily determined by a person skilled in the art.

The dosage of the composition of the present invention can be used in various ranges depending on the weight, age, sex, health status, diet, administration time, administration method, excretion rate and severity of the disease of the patient.

In addition, the present invention relates to an agent for improving dysuria caused by prostate disease comprising the pharmaceutical composition as an active ingredient.

In addition, the present invention relates to a health functional food composition for the prevention or improvement of prostate disease comprising the extract of maple leaf as an active ingredient.

The health functional food composition for the prevention or improvement of prostate disease comprising the maple odor extract as an active ingredient is prepared from any one selected from beverages, pills, tablets, capsules, and powders, or added as a component of food. may be prepared, and may be appropriately prepared according to a conventional method.

Examples of foods to which the maple odor extract of the present invention can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, It may be in any one form selected from tea, drinks, alcoholic beverages, and vitamin complexes, and includes all health functional foods in a conventional sense.

The health functional food includes various nutrients, vitamins, minerals (electrolytes), synthetic and natural flavorants, colorants and enhancers (cheese, chocolate, etc.), pectic acid and its salts, alkynic acid and its salts, organic acids, protective colloidal thickeners , a pH adjuster, a stabilizer, a preservative, glycerin, alcohol, a carbonation agent used in carbonated beverages, and the like. In addition, it may contain the pulp for the production of natural fruit juices and vegetable beverages. These components may be used independently or in combination.

The health functional food composition of the present invention may contain various flavoring agents or natural carbohydrates as additional ingredients. The natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As the sweetener, natural sweeteners such as taumartin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like can be used.

Hereinafter, the present invention will be described in more detail using examples. These examples are only for illustrating the present invention in more detail, and it will be apparent to those of ordinary skill in the art that the scope of the present invention is not limited thereto.

Example 1: Preparation of Maple Leaf Extract

From Korea Plant Extract Bank, 10 g of maple odor extract extracted in large quantities with an extraction yield of 13.77% using 95% (v/v) pretanol (HPLC grade) as an extraction solvent was sold. received and used in animal experiments (in vivo).

Example 2: Construction of Animal Models and Statistical Analysis

After acclimatizing 10-week-old male Wister rats (central laboratory animal) for 1 week, the prostate hypertrophy-inducing group (BPH) was subcutaneously injected with 3 mg/kg of testosterone propionate (TP) for 4 weeks to establish a model. did Maple odor extract-administered group was orally administered 100mg/kg maple leaf extract one hour before TP injection for 4 weeks, and positive control group was administered 10mg/kg of finasteride, a 5α-reductase inhibitor, used as a treatment for benign prostatic hyperplasia. did

Statistical analysis was performed by ANOVA, where # indicates a statistically significant difference compared to the normal group (NC), meaning P < 0.05; * indicates that there is a statistically significant difference compared to the BPH inducing group, and P < 0.05.

Example 3: Prostate Weighing

Prostate hyperplasia was induced by subcutaneously injecting testosterone propionate (TP) into rats for 4 weeks, and the extract of maple leaf and Finasteride, which is being used as a treatment for enlarged prostate, were orally administered together for 4 weeks. After the end of drug administration, prostate glands from sacrificed mice were collected and weights were compared.

As a result, as shown in FIG. 1 , each experimental group (normal group: NC, prostatic hyperplasia induced group: BPH, prostatic hypertrophy induced group + maple extract administration group: BPH+AA, prostatic hypertrophy induced group + finasteride administration group: BPH + Finasteride), the weight of the prostate in the TP-induced group increased compared to the normal group. confirmed that it did.

Example 4: DHT changes in the prostate

After the end of the experiment to determine the content of DHT (dihydrotestosterone) in the protein in the prostate tissue in an enlarged prostate animal model, the protein was extracted from the isolated prostate tissue, and the content of DHT (dihydrotestosterone) using an ELISA kit (ALPCO, Salem) was measured.

As a result, as shown in FIG. 2 , it was confirmed that the content of dihydrotestosterone (DHT) in the serum was statistically significantly decreased in the group to which the maple extract was administered.

Example 5: Analysis of changes in the content of testosterone in serum

In order to check the change in the content of testosterone in an enlarged prostate animal model, after the end of the experiment, the separated blood was centrifuged at 12,000 rpm for 20 minutes, and the supernatant was taken from the serum using an ELISA kit (Cayman, USA) to testosterone (testosterone). ) was measured.

As a result, as shown in FIG. 3 , the content of testosterone in the serum was statistically significantly decreased in the group administered with the extract of maple leaf.

Example 6: Histopathological changes in the prostate

After the end of the experiment, the extracted prostate was fixed with 10% neutral buffered formalin for 24 hours and then embedded with paraffin. The embedded tissue was sectioned to a thickness of 4 μm to make a section, and then stained with H&E [hematoxylin (Sigma-Aldrich, USA) and eosin Y (eosin Y, Sigma-Aldrich)], and encapsulated with an inclusion solution. Thus, the microscopic examination was carried out with an optical microscope.

As a result, as shown in FIGS. 4 and 5 , it was confirmed that the height and number of epithelial cells were overproliferated in the BPH-induced group, but such epithelial cell overgrowth was inhibited in the group administered with the Maple Leaf extract.

As described above, the composition for preventing or treating prostate disease comprising the extract of maple leaf according to the present invention as an active ingredient reduces the weight of the prostate thickened by prostatic hypertrophy (BPH), and reduces the amount of testosterone or DHT in prostate tissue or serum. Since the content is significantly reduced, it can be effectively applied to prostate diseases such as enlarged prostate, prostatitis or prostate cancer.

The preferred embodiment of the present invention has been described in detail above. The description of the present invention is for illustrative purposes, and those of ordinary skill in the art to which the present invention pertains will understand that other specific forms can be easily modified without changing the technical spirit or essential features of the present invention.

Accordingly, the scope of the present invention is indicated by the claims described below rather than the above detailed description, and all changes or modifications derived from the meaning, scope, and equivalent concept of the claims are included in the scope of the present invention. should be interpreted

Claims (7)

Maple extract ( Ainsliaea acerifolia ) A pharmaceutical composition for preventing or treating benign prostatic hyperplasia comprising an extract as an active ingredient. According to claim 1,
The extraction solvent of the maple odor extract is water, C1-C4 lower alcohol, or a pharmaceutical composition for the prevention or treatment of benign prostatic hyperplasia, characterized in that a mixture thereof. delete According to claim 1,
The extract of maple leaf extract is a pharmaceutical composition for the prevention or treatment of benign prostatic hyperplasia, characterized in that it reduces the content of DHT (dihydrotestosterone) or testosterone (testosterone) in tissue or serum. [Claim 5] An agent for improving urination disorders caused by benign prostatic hyperplasia comprising the pharmaceutical composition of any one of claims 1, 2 or 4 as an active ingredient. A health functional food composition for preventing or improving prostatic hyperplasia comprising an extract of maple leaf ( Ainsliaea acerifolia ) as an active ingredient. 7. The method of claim 6,
The maple odor ( Ainsliaea acerifolia ) extract is a health functional food composition for the prevention or improvement of enlarged prostate, characterized in that it is prepared in any one formulation selected from beverages, pills, tablets, capsules and powders.

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