KR20210151477A - Composition for Improving Degenerative Arthritis Using an Extract of Pine Leaf, etc. - Google Patents

Abstract

The present invention discloses a composition for alleviating degenerative arthritis using a pine needle extract and the like having an activity to promote differentiation of cartilage progenitor cells. As described above, according to the present invention, it is possible to provide a composition for alleviating degenerative arthritis using a pine needle extract having an activity to promote differentiation of cartilage progenitor cells.

Description

Composition for Improving Degenerative Arthritis Using an Extract of Pine Leaf, etc.}

The present invention relates to a composition for improving osteoarthritis using a pine needle extract and the like.

Arthritis is a representative cartilage-related disease, and is broadly divided into rheumatoid arthritis and degenerative arthritis. Degenerative arthritis is a disease in which local degenerative changes occur as joint cartilage is worn away, and is also referred to as osteoarthritis. .

Osteoarthritis is a representative degenerative disease closely related to aging, and is a common disease with a high prevalence of about 14.5% of the total population in Korea and about 80% of the elderly over 60 years of age.

Although the pathological mechanism of osteoarthritis is not yet precisely identified, it is known that one cause is an absolute decrease in the number of chondrocytes and damage to the articular cartilage caused by inflammatory factors such as NO, TNF-α, IL-1β, and PGE2.

Therefore, a substance having an activity to promote proliferation of chondrocytes may be a candidate substance for a therapeutic agent for osteoarthritis.

Currently, drugs clinically used for the treatment of degenerative arthritis are painkillers, steroids, nonsteroidal anti-inflammatory drugs, or chondroprotectors such as hyaluronic acid, glucosamine, and chondroitin.

The present invention discloses osteoarthritis improvement activity based on chondrocyte proliferation promoting activity, such as pine needle extract.

It is an object of the present invention to provide a composition for improving osteoarthritis using a pine needle extract and the like.

Other objects or specific objects of the present invention will be set forth below.

As can be seen in the Examples and Experimental Examples below, the present invention has been completed by confirming that the hot water extract of pine needles and the mixed extract of Goji fruit, Schisandra fruit, and Baeknyeoncho fruit have differentiation promoting activity of cartilage progenitor cells.

Therefore, the composition for improving osteoarthritis of the present invention is characterized in that it contains a hot water extract of pine needles, a mixed hot water extract of Goji fruit, Schisandra fruit, and Baeknyeoncho fruit, or a mixture thereof as an active ingredient.

As used herein, the term “active ingredient” refers to a component capable of exhibiting the desired activity by itself or in combination with a carrier that has no activity by itself.

In the composition of the present invention, the active ingredient may be included in any amount (effective amount) depending on the use, formulation, purpose of formulation, etc., as long as it can exhibit degenerative arthritis improving activity, and a typical effective amount may be based on the total weight of the composition. when determined within the range of 0.001 wt % to 20.0 wt %. As used herein, the term "effective amount" refers to the intended medical and pharmacological effects, such as the improvement of degenerative arthritis, when the composition of the present invention is administered to a mammal, preferably a human, to which it is applied during the administration period as suggested by a medical professional. It refers to the amount of the active ingredient included in the composition of the present invention. Such an effective amount can be determined empirically within the ordinary ability of one of ordinary skill in the art.

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

The food composition of the present invention may be prepared in any form, for example, beverages such as tea, juice, carbonated beverages, and ion beverages, processed oils such as milk and yogurt, gums, rice cakes, Korean sweets, bread, confectionery, noodles, etc. of foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jellies, bars, and the like health functional food preparations. In addition, the food composition of the present invention may have any product classification in terms of legal and functional classification as long as it conforms to the enforcement laws at the time of manufacture and distribution. For example, it may be a health functional food according to the Health Functional Food Act, or soy milk, fermented beverages, special purpose food, etc. according to each food type in the Food Code of Food Sanitation Act (Ministry of Food and Drug Safety Announcement, Food Standards and Specifications).

The food composition of the present invention may contain food additives in addition to the active ingredients thereof. Food additives are generally understood as substances that are added to, mixed or infiltrated with food in manufacturing, processing, or preserving food. The Food Additives Ordinance (Ministry of Food and Drug Safety Notice, Food Additive Standards and Specifications) according to the Food Sanitation Act restricts food additives with guaranteed safety by classifying them into chemical synthetic products, natural additives, and mixed preparations.

These food additives may be divided into sweeteners, flavoring agents, preservatives, emulsifiers, acidulants, thickeners, and the like in terms of functionality.

The sweetener may be used in an amount to give the food a suitable sweetness, and may be natural or synthetic. Preferably, a natural sweetener is used. Examples of the natural sweetener include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.

Flavoring agents may be used to improve taste or aroma, and both natural and synthetic ones may be used. Preferably, it is a case where a natural thing is used. In the case of using a natural product, the purpose of nutritional enhancement in addition to flavor may be concurrently used. The natural flavoring agent may be obtained from apples, lemons, tangerines, grapes, strawberries, peaches, or the like, or obtained from green tea leaves, horseradish leaves, bamboo leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. In addition, one obtained from ginseng (red ginseng), bamboo shoots, aloe vera, ginkgo biloba, etc. may be used. The natural flavoring agent may be a liquid concentrate or a solid extract. Optionally, a synthetic flavoring agent may be used, and the synthetic flavoring agent may be an ester, an alcohol, an aldehyde, a terpene, or the like.

As a preservative, sodium calcium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate, EDTA (ethylenediaminetetraacetic acid), etc. can be used, and as an emulsifier, acacia gum, carboxymethylcellulose, xanthan gum, Pectin, etc. are mentioned, and acidulant, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid, etc. can be used as an acidulant. The acidulant may be added so that the food composition has an appropriate acidity for the purpose of inhibiting the growth of microorganisms in addition to the purpose of enhancing the taste.

As a thickening agent, a suspending agent, a settling agent, a gel-forming agent, a bulking agent, etc. can be used.

The food composition of the present invention may contain, in addition to the food additives described above, physiologically active substances or minerals known in the art for the purpose of supplementing and reinforcing functionality and nutrition and guaranteed stability as food additives.

Examples of such physiologically active substances include catechins contained in green tea and the like, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoylthiamine, and the like. Minerals include calcium preparations such as calcium citrate, magnesium stearate Magnesium preparations, such as iron preparations, such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, zinc, etc. are mentioned.

In the food composition of the present invention, the food additives as described above may be included in an appropriate amount to achieve the purpose of the addition according to the product type.

In relation to other food additives that may be included in the food composition of the present invention, reference may be made to the Food Codex or the Food Additives Codex.

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

The pharmaceutical composition of the present invention may be prepared as an oral dosage form or a parenteral dosage form according to the route of administration by a conventional method known in the art, including a pharmaceutically acceptable carrier in addition to the active ingredient. Here, "pharmaceutically acceptable" means that it does not inhibit the activity of the active ingredient and does not have toxicity beyond what the application (prescription) target can adapt.

When the pharmaceutical composition of the present invention is prepared as an oral dosage form, powder, granules, tablets, pills, dragees, capsules, liquids, gels, syrups, suspensions, wafers according to methods known in the art together with a suitable carrier It can be prepared in a formulation such as Examples of suitable pharmaceutically acceptable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, Cellulose such as sodium carboxymethylcellulose and hydroxypropylmethylcellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable and oil. In the case of formulation activity, the formulation may be formulated by including a diluent and/or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, and a surfactant, if necessary.

When the pharmaceutical composition of the present invention is prepared for parenteral use, it may be formulated in the form of injections, transdermal administrations, nasal inhalants and suppositories together with suitable carriers according to methods known in the art. In the case of formulation for injection, suitable carriers include sterile water, ethanol, polyols such as glycerol or propylene glycol, or mixtures thereof, preferably Ringer's solution, PBS (phosphate buffered saline) containing triethanolamine, or sterile water for injection. , an isotonic solution such as 5% dextrose may be used. When formulated for transdermal administration, it may be formulated in the form of an ointment, a cream, a lotion, a gel, an external solution, a pasta agent, a liniment agent, an air roll, and the like. In the case of nasal inhalants, it can be formulated in the form of an aerosol spray using a suitable propellant such as dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, etc. (tween) 61, polyethylene glycols, cacao fat, laurin fat, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearate, sorbitan fatty acid esters, etc. may be used.

Formulation of pharmaceutical compositions is known in the art, and specifically, reference may be made to the literature [Remington's Pharmaceutical Sciences (19th ed., 1995)] and the like. This document is considered a part of this specification.

A preferred dosage of the pharmaceutical composition of the present invention is in the range of 0.001 mg/kg to 10 g/kg per day, preferably 0.001 mg/kg to 1 g, depending on the patient's condition, weight, sex, age, severity of the patient, and the route of administration. It can be in the range /kg. Administration may be performed once or divided into several times a day. Such dosages should not be construed as limiting the scope of the invention in any respect.

As described above, according to the present invention, it is possible to provide a composition for improving degenerative arthritis using a pine needle extract having an activity to promote differentiation of cartilage progenitor cells.

The composition of the present invention may be commercialized as a food or drug.

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 samples

The hot water extract of pine needles was prepared in powder form by adding 10 times the weight of water to the pulverized pine needles, extracting at 80-100° C. for 24 hours, filtering, and concentrating the filtrate under reduced pressure and freeze-drying.

Goji berry (fruit), omija (fruit), and baeknyeoncho (fruit) are mixed with the same weight and pulverized, then 10 times the weight of water is added thereto, extracted at 80-100° C. for 24 hours, filtered, and the filtrate is concentrated under reduced pressure. It was prepared in a powder form by freeze-drying.

<Experimental Example> Osteoarthritis improvement activity test - Chondrocyte differentiation promotion activity test

For ATDC5 cells, which are precursors of chondrocytes, DMEM medium (Dulbecco's Modified Eagle Medium) (Gibco, NY, USA) and F-12 medium (Gibco, NY, USA) are mixed 1:1, and penicillin/streptomycin 100units/ml and 10% fetal bovine serum was added, and cultured at _{37° C. and 5% CO 2 conditions.}

When the cells were filled to about 75% in the culture vessel, the cells were dissociated by treatment with trypsin, and the cells were aliquoted to contain ^{2×10 4 cells per well in a 48-well plate.} After 24 hours, cell differentiation was induced with a medium containing 10 μg/ml transferrin and 30 nM sodium selenite, and treated with 100 μg/mL of the sample of Example. After 14 days, the medium of the cells was removed for Alcian-blue staining, washed with 1×PBS (phosphate buffer saline), the cells were fixed with 95% methanol, and 1% Alcian-blue 8GS stained for 16 hours. After removing the staining solution, it was washed three times for 30 seconds with 3% acetic acid, and after dissolving the dye with 10% acetic acid, absorbance was measured at 650 nm. The average absorbance value for each sample group was obtained according to three repeated experiments, and the cell proliferation rate was measured by comparing it with the absorbance value of the control group, which was cultured with only a medium without adding a sample, and the percentage was shown in Table 1 below. .

Change in proliferation rate of osteoblasts (%) division Osteoblast proliferation rate (%) control 100 Sample A 132.27±3.42* Mixed Sample 1 (A:B=8:2) 154.53±5.44* Mixed Sample 2 (A:B=6:4) 146.73±5.26* Mixed Sample 3 (A:B=5:5) 132.54±5.47* Mixed Sample 4 (A:B=4:6) 124.62±4.55* Mixed Sample 5 (A:B=2:8) 123.43±2.74* B sample 127.64±2.74* Sample A: pine needle hot water extract
Sample B: Mixed hot water extract of Goji berry (fruit), Schisandra (fruit) and Baeknyeoncho (fruit)
Mixed sample: weight ratio
* p<0.05

Referring to the results of [Table 1], the mixed sample 1 had the highest chondrocyte differentiation promoting effect, followed by the mixed sample 2 the highest. In addition, these mixed samples showed higher effects than single samples.

Statistical processing

For statistical processing, ANOVA analysis was used, and statistical significance was verified using Student't test ( *P<0.05 ).

Claims (4)

A composition for improving degenerative arthritis, comprising, as an active ingredient, a hot water extract of pine needles, a mixed hot water extract of Goji fruit, Schisandra fruit, and Baeknyeoncho fruit, or a mixture thereof.
According to claim 1,
The mixture is a composition, characterized in that the hot water extract of pine needles, goji fruit, omija fruit, and mixed hot water extract of baeknyeoncho fruit is 8:2 to 6:4 by weight.
3. The method of claim 1 or 2,
The composition is a food composition, characterized in that the composition.
3. The method of claim 1 or 2,
The composition is a pharmaceutical composition, characterized in that the composition.