KR102184670B1 - Anti-inflammatory composition comprising Ginsenoside Rg3 - Google Patents

Abstract

An example of the present invention provides an anti-inflammatory composition comprising ginsenoside Rg3 as an active ingredient. In addition, an example of the present invention is a composition comprising a ginsenoside Rg3-containing material or a ginsenoside Rg3-containing material as an active ingredient, wherein the ginsenoside Rg3 content in the ginsenoside Rg3-containing material is ginsenoside Rg3 It provides an anti-inflammatory composition, characterized in that 1.0 to 6.0% by weight based on the total weight of the contained material. The anti-inflammatory composition according to the present invention has no side effects on the human body or human skin and has excellent anti-inflammatory effect because it contains as an active ingredient a natural substance that is derived from ginsenoside Rg3 itself or from plants and has a very high content of ginsenoside Rg3. Represents. Accordingly, the composition according to the present invention may be embodied as pharmaceuticals, cosmetics, personal care products, etc. for preventing, improving or treating various inflammatory diseases.

Description

Anti-inflammatory composition comprising Ginsenoside Rg3}

The present invention relates to an anti-inflammatory composition, and more particularly, to a composition comprising a material containing a high ginsenoside Rg3 or ginsenoside Rg3 as an active ingredient and is harmless to the human body and has excellent anti-inflammatory efficacy.

Human skin is the primary barrier of the human body, and it not only protects the internal organs from stimuli of the external environment such as changes in temperature and humidity, ultraviolet rays, and pollutants, but also protects the body from infection by external pathogens such as bacteria and viruses. Play a role.

Inflammation is a phenomenon that appears as a series of defense purposes to minimize the response and restore the damaged area when cells or tissues are damaged by any cause.A reaction occurs in nerves, blood vessels, lymphatic vessels, body fluids, cells and tissues, resulting in a reaction. It causes local or systemic dysfunction such as pain, swelling, redness, and fever. The causes of inflammation include physical factors and chemical factors caused by chemical substances, and immunological factors caused by antibody reactions. In addition, inflammation is caused by blood vessel or hormonal imbalance or acute infection. Cells damaged by external stimuli secrete pro-inflammatory cytokines and various biological mediators such as chemokine, interleukine, and interferon to dilate blood vessels, thereby making them permeable. As it rises, antibodies, complement, plasma, and phagocytic cells flock to the site of inflammation. This phenomenon causes erythema or exothermic reaction. In order to eliminate inflammation, there is a method of injecting drugs that remove inflammatory sources or reduce biological reactions and symptoms. Drugs that have been used for anti-inflammatory purposes to date include ibuprofen and indomethacin as a non-steroidal system, and dexamethasone as a steroid system, but have large side effects and have problems in terms of safety. It is held and its use is limited. In this respect, development of a safe anti-inflammatory material with few side effects is required.

On the other hand, Ginsenoside is a kind of saponin in ginseng and has a glycoside structure in which sugar is added to the parent body composed of triterpene chemically. The ginsenoside is a name given to the meaning of a glycoside isolated from ginseng in order to distinguish it from saponins of other plants. Until now, ginseng saponin has been known to exert various effects in regulating body functions by affecting not only the central nervous system, the endocrine system, the immune system, and the metabolic system, but also skin whitening and homeostasis. Until now, more than 30 species of ginsenosides have been isolated and identified from ginseng (including red ginseng), and the pharmacological action of each ginsenoside has been revealed one after another. Representative ginseng saponins are Panaxadiol-type Ginsenosides: Ra1, Ra2, Ra3, Rb1, Rb2, Rb3, Rc, Rd, Rg3) and Panaxatriol-based ginsenosides according to the structure of aglycon. It is divided into side (Panaxatriol-type Ginsenosides: Re, Rf, Rgl, Rg2). Ginsenoside Rg3, a type of minor ginsenoside, is not included in ginseng roots, but is included in steamed processed products such as red ginseng. The pharmacological action of ginsenoside Rg3 has been reported to inhibit cancer cell metastasis, inhibit platelet aggregation and antithrombosis, relax blood vessels, inhibit experimental liver injury, and inhibit anticancer drug resistance. In addition, with regard to the efficacy of ginsenoside Rg3, Korean Patent Publication No. 10-1756790 discloses 20(S)-ginsenoside Rg3 and 20(R)-ginsenoside Rg3 in weight ratio 7: Containing a mixture of 3 as an active ingredient, obesity, diabetes, hyperinsulinemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hypertension, arteriosclerosis, coronary heart disease, stroke and fatty liver A pharmaceutical composition for preventing or treating any one disease selected from the group consisting of is disclosed. In addition, Korean Patent Publication No. 10-1733665 discloses a pharmaceutical composition for preventing or treating Gleevec-resistant leukemia, comprising ginsenoside F1 or Rg3 as an active ingredient. In addition, Korean Patent Registration No. 10-1863739 discloses that as a topical preparation for preventing and/or treating dementia, 20(R)-ginsenoside Rg3 as an active ingredient; And ginseng (Radix Ginseng) volatile oil, Moschus volatile oil, Iris (Rhizoma Acori Tatarinowii) volatile oil, Turmeric (Radix Curcumae) volatile oil, or a topical formulation comprising one of Rhizoma Chuanxiong volatile oil It is disclosed. In addition, Korean Patent Application Publication No. 10-2015-0110908 discloses a composition for preventing or treating hepatotoxic diseases containing ginsenoside Rg3. In addition, Korean Patent Laid-Open Publication No. 10-2014-0126892 contains ginsenoside Rg3 as an active ingredient, and has anti-aging, skin wrinkle improvement, whitening, moisturizing improvement, acne improvement, skin trouble improvement effect, etc. Is disclosed. In addition, Korean Patent Publication No. 10-1416140 discloses a composition for external application for skin for promoting lipid biosynthesis containing ginsenoside Rg3 as an active ingredient. In addition, Korean Patent Publication No. 10-1355320 discloses a pharmaceutical composition for the prevention and treatment of hepatitis C containing ginsenoside Rg3 or a pharmaceutically acceptable salt thereof as an active ingredient. In addition, Korean Patent Publication No. 10-1155695 discloses a composition for skin whitening comprising ginsennoside Rg3 as an active ingredient. In addition, Republic of Korea Patent Publication No. 10-1655256 discloses a skin external composition for itching relief comprising 0.00001 to 40.0% by weight of ginsenoside Rg3 and 0.00001 to 40.0% by weight of Taeji-like lipid complex based on the total weight of the composition for external application for skin. have. The prior art discloses various effects of ginsenoside Rg3, but does not disclose a direct correlation between ginsenoside Rg3 and anti-inflammatory.

The present invention is derived from the conventional technical background, and an object of the present invention is to provide a composition that is harmless to the human body and has excellent anti-inflammatory efficacy.

The inventors of the present invention extract red ginseng and the like with alcohol to obtain red ginseng extract, etc., and then react the red ginseng extract with beta-glucosidase to obtain enzyme bioconversion products such as red ginseng extract, and then compare their anti-inflammatory efficacy. As a result, it was confirmed that the enzyme bioconversion product such as red ginseng extract has remarkably excellent anti-inflammatory efficacy compared to the corresponding red ginseng extract, and the present invention was completed. The enzyme bioconversion product such as the red ginseng extract is characterized in that the total ginsenoid content is about 1/2 to 3/5 level compared to the corresponding red ginseng extract, but the ginsenoside Rg3 content is about 10 to 15 times higher, and this feature From this, it was confirmed that the high anti-inflammatory efficacy of enzyme bioconversion products such as red ginseng extract is mainly determined by ginsenoside Rg3, and the present invention was completed.

In order to solve the above object, an example of the present invention provides an anti-inflammatory composition comprising ginsenoside Rg3 as an active ingredient.

In order to solve the above object, an example of the present invention is a composition consisting of a substance containing ginsenoside Rg3 or containing a substance containing ginsenoside Rg3 as an active ingredient, wherein the ginsenoside Rg3 content in the substance containing ginsenoside Rg3 Provides an anti-inflammatory composition, characterized in that 1.0 to 6.0% by weight based on the total weight of the ginsenoside Rg3-containing material.

The anti-inflammatory composition according to the present invention has no side effects on the human body or human skin and has excellent anti-inflammatory effect because it contains as an active ingredient a natural substance that is derived from ginsenoside Rg3 itself or from plants and has a very high content of ginsenoside Rg3. Represents. Accordingly, the composition according to the present invention may be embodied as pharmaceuticals, cosmetics, personal care products, etc. for preventing, improving or treating various inflammatory diseases.

1 is a photograph of an ear condition of a mouse for each TPA treatment day in an in-vivo experiment on the anti-inflammatory effect of red ginseng extract and its enzyme conversion reaction product.
FIG. 2 is a photograph (400 times magnification) showing the results of biological histologic analysis of mouse ears 3 days after treatment with TPA in an in-vivo experiment on the anti-inflammatory efficacy of red ginseng extract and its enzyme conversion reaction product.
3 is a graph showing the results of measuring the average concentration of IL-6 in mouse ears when 3 days elapsed after TPA treatment in an in-vivo experiment on the anti-inflammatory efficacy of red ginseng extract and its enzyme conversion reaction product.

The term "composition" used in the present invention refers to a material in which two or more components are uniformly mixed, and is a concept including an intermediate material for manufacturing a finished product as well as a finished product.

The term "pharmaceutically acceptable" as used herein means that it does not significantly irritate the organism and does not inhibit the biological activity and properties of the administered active substance.

The term "prevention" as used in the present invention refers to any action that suppresses or delays the progression of symptoms of a specific disease (eg, inflammatory disease) by administration of the composition of the present invention.

The term "improvement" as used herein refers to any action that at least reduces the severity of a parameter related to the condition being treated, for example a symptom.

The term "treatment" used in the present invention refers to any action that improves or beneficially alters the symptoms of a specific disease (eg, thrombotic disease) by administration of the composition of the present invention.

As used herein, the term "administering" means providing a given composition of the present invention to a subject by any suitable method. At this time, the individual refers to all animals, such as humans, monkeys, dogs, goats, pigs, mice, etc., having diseases in which symptoms of a specific disease can be improved by administering the composition of the present invention.

The term "pharmaceutically effective amount" as used herein refers to an amount sufficient to treat a disease at a reasonable benefit or risk ratio applicable to medical treatment, which is the type, severity, activity of the drug, drug Sensitivity to, administration time, route of administration and rate of excretion, duration of treatment, factors including drugs used simultaneously, and other factors well known in the medical field.

Hereinafter, the present invention will be described in detail.

The anti-inflammatory composition according to an embodiment of the present invention includes ginsenoside Rg3 as an active ingredient. In addition, the anti-inflammatory composition according to an embodiment of the present invention is composed of a ginsenoside Rg3-containing material or includes a ginsenoside Rg3-containing material as an active ingredient.

The ginsenoside Rg3-containing material is characterized in that the content of ginsenoside Rg3 is about 5 to 30 times, preferably 10 to 20 times higher than that of conventional red ginseng extract extracted from red ginseng. The ginsenoside Rg3 content in the ginsenoside Rg3-containing material is 1.0 to 6.0% by weight based on the total weight of the ginsenoside Rg3-containing material when considering the anti-inflammatory effect of the composition or the manufacturing economy of the ginsenoside Rg3-containing material. It is preferable that it is, and it is more preferable that it is 2.0-5.0 weight%, and it is most preferable that it is 2.5-4.5 weight%. In addition, the total ginsenoside content in the ginsenoside Rg3-containing material is 5-30 based on the total weight of the ginsenoside Rg3-containing material when considering the anti-inflammatory efficacy of the composition or the manufacturing economy of the ginsenoside Rg3-containing material. It is preferable that it is weight%, it is more preferable that it is 8-25 weight%, and it is most preferable that it is 10-15 weight%.

The ginsenoside Rg3-containing material is preferably a bioconversion product obtained by reacting an extract of a raw material selected from ginseng, ginseng fruit, white ginseng or red ginseng with beta-glucosidase. The ginseng is a concept including fresh ginseng, white ginseng, white ginseng, and the like, and the red ginseng is a concept including red ginseng. The fresh ginseng refers to the undried ginseng, the white ginseng refers to the ginseng dried in the sun after removing the epidermis using fresh ginseng as a raw material, and the white ginseng refers to the ginseng dried in the sun from the fine roots excluding the body of fresh ginseng. Red ginseng refers to red ginseng processed by steaming fine roots excluding the body of fresh ginseng with a jeungsam and drying to 15% or less moisture. In the present invention, ginseng is not particularly limited in varieties and places of origin, and may be ginseng selected from various origins, such as Korean ginseng, Samchil ginseng, Jeonchil ginseng, American ginseng, Chinese ginseng, Vietnamese ginseng, and jukjeol ginseng. Considering the side content and type, Korean ginseng is preferable. In addition, the Korean ginseng may be selected from various varieties such as Cheonggyeong, Yeonpung, Seonpung, Cheongseon, Cheonryang, Gopung, Geumpung, Seonwon, and Seonhyang. The substance containing ginsenoside Rg3 of the present invention can be obtained using various known methods. For example, the substance containing ginsenoside Rg3 of the present invention can be obtained by using the method disclosed in Korean Patent Publication No. 10-1908659. The Republic of Korea Patent Publication No. 10-1908659 discloses that ginseng fruit juice, ginseng fruit extract, ginseng fruit juice juice, ginseng fruit fruit extract, or a concentrated solution thereof are used as beta-glucosidase and hemicellulase. A method of increasing the content of rare ginsenosides such as ginsenoside Rg3 by reacting with a mixed enzyme of) is disclosed. In addition, the extract of the raw material selected from ginseng, ginseng fruit, white ginseng or red ginseng can be obtained using a variety of known methods. For example, red ginseng extract can be obtained using a known solvent extraction method. At this time, the extraction solvent is water, a lower alcohol having 1 to 4 carbon atoms (e.g., methanol, ethanol, propanol, and butanol) or a mixture thereof such as a hydrated lower alcohol, propylene glycol, 1,3-butylene glycol, glycerin, and acetone. , Diethyl ether, ethyl acetate, butyl acetate, dichloromethane, chloroform, hexane, and mixtures thereof. When using water as the extraction solvent, it is preferable that water is hot water. In addition, when using alcohol as the extraction solvent, the alcohol is preferably a lower alcohol having 1 to 4 carbon atoms, and the lower alcohol is more preferably selected from methanol or ethanol. In addition, when a hydrous alcohol is used as the extraction solvent, the alcohol content is preferably 50 to 90%. In the present invention, the extract is preferably an alcohol extract of red ginseng in consideration of the ginsenoside content and type. In addition, when using alcohol as the extraction solvent, the alcohol is preferably 60 to 95% by weight of hydrated ethanol, and more preferably 70 to 90% by weight of hydrated ethanol when considering extraction efficiency. In the present invention, the ginsenoside Rg3-containing material most preferably uses 70-90% ethanol from red ginseng as an extraction solvent to obtain a red ginseng extract, and a red ginseng extract is added to a liquid reaction medium such as a buffer solution to determine the volume of the liquid reaction medium. It is added in an amount of about 0.5 to 5% (w/v), preferably 0.5 to 2% (w/v), and beta-glucosidase is added to about 1 based on the weight of the substrate (red ginseng extract). After adding in an amount of ~8 times, preferably 2~6 times, organisms by enzymes for about 12~20 hr, preferably 14~18 hr at about 40~60℃, preferably about 45~55℃ After the conversion reaction proceeds, impurities are removed through centrifugation or filtration, and the remaining bioconversion product-containing solution (corresponding to the supernatant after centrifugation or the filtrate after filtration) is concentrated and dried (e.g., freeze-dried) to solidify. It can be manufactured by a method or the like. In addition, it is possible to obtain a ginsenoside Rg3 containing material or ginsenoside Rg3 itself having an increased purity through chromatography or the like from the bioconversion product-containing solution, a concentrate thereof, or a solid thereof.

Ginsenoside Rg3 used as an active ingredient of the composition in the present invention or ginsenoside Rg3 contained in the enzyme bioconversion product of red ginseng extract is preferably composed of the isomers S-type and R-type, ginsenoside in the present invention The weight ratio of the isomer S-form to R-form constituting the side Rg3 is preferably 2:1 to 10:1, more preferably 3:1 to 9:1, and 5:1 to 10 when considering the anti-inflammatory effect of the composition. Most preferably, it is 8:1.

Since the composition of the present invention has excellent anti-inflammatory effect, it can be used to prevent, ameliorate or treat various inflammatory diseases. The inflammatory diseases include atopy, psoriasis, dermatitis, allergies, arthritis, rhinitis, otitis media, sore throat, tonsillitis, cystitis. , Nephritis, pelvicitis, Crohn's disease, ulcerative colitis, ankylosing spondylitis, systemic lupus erythematodes (SLE), atherosclerosis, asthma, arteriosclerosis, edema, rheumatoid arthritis, delayed allergy (type IV allergy), Graft rejection, graft versus host disease, autoimmune encephalomyelitis, multiple sclerosis, inflammatory bowel disease, arthritis, cystic fibrosis, diabetic retinopathy, rhinitis, ischemic-reperfusion injury, vascular restenosis, glomerulonephritis, gastrointestinal allergy, etc. In view of the fact that the composition of the present invention is mainly implemented as a pharmaceutical composition or cosmetic composition in the form of an external preparation for skin, it is preferable that it is an inflammatory skin disease. The above inflammatory diseases are known to be caused by various inflammatory cytokines. Typically, IL-6 (Interleukin-6) is secreted from macrophages as an important mediator in acute inflammatory reactions, and muscles, bones, ovaries, systemic lupus erythematosus Involved in the back. A substance containing ginsenoside Rg3 or ginsenoside Rg3 (preferably a substance high in ginsenoside Rg3) used as an active ingredient of the composition in the present invention decreases the expression level of IL-6 (Interleukin-6) to the corresponding site Inhibits the inflammatory response of

The composition of the present invention may be embodied as a pharmaceutical composition, a cosmetic composition, a personal care product, etc., depending on the purpose or aspect of use, and may preferably be embodied as a pharmaceutical composition or a cosmetic composition in the form of an external preparation for skin. In addition, the content of a substance containing ginsenoside Rg3 or ginsenoside Rg3 (preferably a substance containing high ginsenoside Rg3), which is an active ingredient in the composition of the present invention, is also in various ranges depending on the specific form of the composition and the purpose of use or aspect. Can be adjusted in.

The content of the active ingredient in the pharmaceutical composition according to the present invention is not largely limited, for example, 0.01 to 99% by weight, preferably 0.5 to 50% by weight, more preferably 1 to 30% by weight based on the total weight of the composition. Can be In addition, the pharmaceutical composition according to the present invention may further include additives such as a pharmaceutically acceptable carrier, excipient, or diluent in addition to the active ingredient. Carriers, excipients and diluents that can be included in the pharmaceutical composition of the present invention include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate. , Cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oils. In addition, the pharmaceutical composition of the present invention may further contain one or more active ingredients known to have anti-inflammatory effects in addition to a substance containing ginsenoside Rg3 or ginsenoside Rg3 (preferably a substance containing high ginsenoside Rg3). The pharmaceutical composition of the present invention can be formulated into a dosage form for oral administration or a dosage form for parenteral administration by a conventional method. When formulated, such as fillers, extenders, binders, wetting agents, disintegrants, surfactants, etc. It can be formulated using diluents or excipients. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and these solid preparations include at least one excipient in the active ingredient, such as starch, calcium carbonate, and sucrose. ), lactose, or gelatin. In addition, in addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral administration include suspensions, liquid solutions, emulsions, and syrups.In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, fragrances, and preservatives may be included. have. Formulations for parenteral administration may include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, lyophilized formulations, and suppositories. As the non-aqueous solvent and the suspension solvent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate may be used. As a base for suppositories, witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin, and the like may be used. Furthermore, it can be preferably formulated according to each disease or component by an appropriate method in the art or by using a method disclosed in Remington's Pharmaceutical Science (latest edition), Mack Publishing Company, Easton PA. The pharmaceutical composition of the present invention may be orally or parenterally administered to mammals including humans according to a desired method, and parenteral administration methods include skin external use, intraperitoneal injection, rectal injection, subcutaneous injection, intravenous injection, muscle These include intra- or intrathoracic injection. The dosage of the pharmaceutical composition of the present invention is not largely limited as long as it is a pharmaceutically effective amount, and the range varies according to the patient's weight, age, sex, health condition, diet, administration time, administration method, excretion rate, and disease severity. Varies. In addition, the pharmaceutical composition of the present invention may be administered once or several times a day. The pharmaceutical composition according to the present invention is preferably prepared in the form of an external preparation for skin such as a cream, gel, patch, spray, research agent, warning agent, lotion agent, liniment agent, pasta agent, or cataplasma agent when considering the aspect to be used. Do.

The cosmetic composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing , Oil, powder foundation, emulsion foundation, wax foundation, spray, etc. may be formulated, but is not limited thereto. Specifically, the cosmetic composition of the present invention may be prepared in the form of a flexible lotion, nutritional lotion, nutritional cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder. When the formulation of the cosmetic composition of the present invention is a paste, cream, or gel, as a carrier component, animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide, etc. Can be used. When the formulation of the cosmetic composition of the present invention is a solution or emulsion, a solvent, solubilizing agent or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene Glycol, 1,3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or fatty acid ester of sorbitan. When the formulation of the cosmetic composition of the present invention is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, an ethoxylated isostearyl alcohol, a suspending agent such as polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester , Microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or tracant, and the like may be used. When the formulation of the cosmetic composition of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. In particular, in the case of a spray, additionally chlorofluorohydro Propellants such as carbon, propane/butane or dimethyl ether may be included. When the formulation of the cosmetic composition of the present invention is a surfactant containing cleansing, as carrier components, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, Fatty acid amide ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters may be used. When considering the aspect to be used, the cosmetic composition according to the present invention is preferably prepared in the form of a lotion, tonic, conditioner, essence, lotion, cream, aerosol, pack, soap, moisturizer, and spray.

Hereinafter, the present invention will be described in more detail through examples. However, the following examples are only intended to clearly illustrate the technical features of the present invention, and do not limit the scope of the present invention.

1. Ginsenoside Rg3 Enzymatic production

Red rice ginseng, red ginseng, white rice ginseng, and fresh ginseng were purchased from Geumsan, Chungnam, respectively, then ground with a grinder, powdered, and dried. Thereafter, about 10 times of 80% fermented alcohol was added to 10 kg of dry weight of each sample, mixed uniformly, extracted three times for about 24 hr at room temperature, and filtered. Thereafter, the filtered extract was concentrated under reduced pressure and lyophilized to obtain an extract sample. Thereafter, 5 g of the extract sample was added to 500 ml of 100 mM acetate buffer (pH=5.0), and 20 g of a commercially available beta-glucosidase product (manufacturer: Novozyme) was added thereto. A total of 500 ml of a reaction solution was prepared by addition. Then, the enzyme conversion reaction was performed at about 50° C. for about 16 hr. After completion of the enzyme conversion reaction, the enzyme conversion reaction product solution was centrifuged to obtain a supernatant, and the supernatant was concentrated under reduced pressure conditions and lyophilized to obtain a sample of the enzyme conversion reaction product. Thereafter, the extract and its enzyme conversion product were quantitatively analyzed by high performance liquid chromatography (HPLC), and the results are shown in Table 1 below.

Raw material for extraction Ginsenoside content of extract (mg/g) Ginsenoside content of enzyme conversion reaction product (mg/g) Total Ginsenoside Ginsenoside Rg3 Total Ginsenoside Ginsenoside Rg3 Red ginseng 222.93 2.13 108.80 27.08 Red ginseng 230.59 2.82 145.14 36.11 White ginseng 190.78 0 112.21 15.02 Fresh ginseng 205.54 0 130.89 17.44

As shown in Table 1 above, the ginsenoside Rg3 content in the red ginseng extract was 2.82 mg/g, and the ginsenoside Rg3 content in the enzyme conversion reaction product of the red ginseng extract was 36.11 mg/g. The Rg3 content increased by about 33.29 mg/g. In addition, the contents of S-form and R-form were 30.85 mg/g and 5.25 mg/g, respectively, of the total ginsenoside Rg3 content of 36.11 mg/g in the enzyme conversion reaction product of red ginseng extract. . The weight ratio of S-form and R-form in ginsenoside Rg3 in the enzyme conversion reaction product of red ginseng extract was 5.87:1.

2. Anti-inflammatory effect of red ginseng extract and its enzyme conversion reaction product in- vivo Experiment

(1) Experiment method

Seven-week-old female BALB/c mice were reared for 5 days in an environment of 20±2° C., 68±5% relative humidity, and 12-hour light-dark cycle, and were adapted to the laboratory environment. In addition, water and feed were freely ingested during the experiment.

An inflammation inducing agent solution was prepared by dissolving 1 mg of TPA (12-O-tetradecanoylphorbol-13-acetate), an inflammation inducing agent, in 20 μl of acetone. In addition, 600 µg of the red ginseng extract sample obtained above was dissolved in 20 µl of acetone to prepare a red ginseng extract solution. In addition, 600 μg of a sample of the enzyme conversion reaction product of the red ginseng extract obtained above was dissolved in 20 μl of acetone to prepare a solution of the enzyme conversion reaction product. Thereafter, 7-week-old female BALB/c mice were divided into four groups: the Control group (no treatment), the TPA group, the RG group, and the RG3 group. Mice belonging to the control group (no treatment) were not treated separately. In addition, to mice belonging to the TPA group, an inflammation inducing agent solution was applied to the inner and outer sides of the ear once a day for 4 days, and left to stand for 30 minutes to induce inflammation. In addition, the RG group mice were applied with an inflammation inducing agent solution once a day for 4 days on the inner and outer sides of the ear and left for 30 minutes to induce inflammation, and then the red ginseng extract solution was treated on the same site and left for 4 hr. In addition, to RG3 group mice, once a day for 4 days, an inflammation inducing agent solution was applied to the inner and outer sides of the ear, left for 30 minutes to induce inflammation, and then treated with a solution of the enzyme conversion reaction product of red ginseng extract on the same site for 4 hr. Left for a while.

The ear condition of the mouse was observed for each drug treatment day and the change in ear thickness was measured. In addition, 3 days after the drug treatment, the mice were sacrificed by cervical dislocation, and the ear tissue was separated and fixed. Thereafter, H&E staining was performed on the ear tissue for bio-histochemical analysis. Specifically, the fixed mouse ear tissue was cut to a thickness of about 2.0 μm using a microtome (LEICA RM2125RT, Nussloch, Germany) to make a section, stained with Harry's hematoxylin-eosin, and then analyzed with a light microscope and images. Volume changes in epithelial and dermal tissues were observed using an image analysis program (i-Solution, Nikon). In addition, IL-6 (Interleukin-6) ELISA Kit was used to quantify the concentration of IL-6 generated in the ear tissue.

(2) Experiment result

1 is a photograph of an ear condition of a mouse for each TPA treatment day in an in-vivo experiment on the anti-inflammatory effect of red ginseng extract and its enzyme conversion reaction product. In addition, Table 2 below shows the results of measuring the ear thickness of mice for each TPA treatment day in an in-vivo experiment on the anti-inflammatory efficacy of red ginseng extract and its enzyme conversion reaction product.

Drug treatment day Average ear thickness for each mouse in the experimental group (㎜) Control group
(No treatment group) TPA group RG group RG3 group Day 1 0.327 0.287 0.317 0.293 Day 2 0.333 0.747 0.707 0.667 Day 4 0.340 0.870 0.737 0.587

As shown in Fig. 1 and Table 2, mice of the experimental group (TPA group) treated with only TPA (12-O-tetradecanoylphorbol-13-acetate) had thickened ears from the second day of treatment and showed skin necrosis. However, after treatment with TPA (12-O-tetradecanoylphorbol-13-acetate), the experimental group treated with red ginseng extract (RG group) and TPA (12-O-tetradecanoylphorbol-13-acetate) treated with the enzyme bioconversion product of red ginseng extract. It was confirmed that the mice of the experimental group (RG3 group) significantly alleviated the thickness of the ear and skin necrosis compared to the mice of the experimental group treated with only TPA. In particular, it was confirmed that the enzyme bioconversion product of red ginseng extract has more than twice the anti-inflammatory effect compared to red ginseng extract. Specifically, the RG group treated with red ginseng extract showed an effect of reducing the thickness of the ear by about 15% on the 4th day of drug treatment compared to the TPA group treated with only TPA, whereas RG3 treated with the enzyme bioconversion product of the red ginseng extract. In the group, the ear thickness decreased by about 33% on the 4th day of drug treatment when compared to the TPA group treated with TPA alone.

FIG. 2 is a photograph (400 times magnification) showing the results of biological histologic analysis of mouse ears 3 days after treatment with TPA in an in-vivo experiment on the anti-inflammatory efficacy of red ginseng extract and its enzyme conversion reaction product. In addition, Table 3 below shows the results of measuring the average concentration of IL-6 in the mouse ear when 3 days elapsed after TPA treatment in an in-vivo experiment on the anti-inflammatory efficacy of red ginseng extract and its enzyme conversion reaction product. It is shown as a graph.

Classification of experimental group IL-6 average concentration (pg/ml) Control (no treatment group) 9.708 TPA group 377.094 RG group 111.931 RG3 group 26.155

As shown in FIG. 2, the ear cross section of the experimental group (TPA group) mice treated with only TPA (12-O-tetradecanoylphorbol-13-acetate) was confirmed to increase the inflammatory cells in the dermal layer with a distinct increase in thickness of the epithelium and dermis. The thinner the dermal layer means that the wound scar is smaller. On the other hand, it can be seen that the RG3 group treated with the enzyme bioconversion product of the red ginseng extract had a very thin dermal layer thickness of the mouse ear when compared to the TPA group treated with only TPA.

In addition, as shown in Table 3 and Figure 3, both the RG group treated with red ginseng extract and the RG3 group treated with the enzyme bioconversion product of the red ginseng extract showed remarkable IL-6 concentration compared to the TPA group treated with only TPA. Decreased. Specifically, the RG group treated with red ginseng extract decreased the IL-6 concentration by about 70% when compared to the TPA group treated with only TPA, whereas the RG3 group treated with the enzyme bioconversion product of red ginseng extract treated only TPA. Compared with the group, the IL-6 concentration decreased by about 93%. From these results, it can be seen that the increased ginsenoside Rg3 in the enzymatic bioconversion product of red ginseng extract significantly reduced IL-6, an acute inflammation index, in experimental animal models in which inflammation was induced by TPA treatment, thereby exerting excellent anti-inflammatory effects have.

As described above, the present invention has been described through the above embodiments, but the present invention is not necessarily limited thereto, and various modifications may be possible without departing from the scope and spirit of the present invention. Accordingly, the scope of protection of the present invention should be construed as including all embodiments falling within the scope of the claims appended to the present invention.

Claims (8)

As a composition consisting of a substance containing ginsenoside Rg3 or containing a substance containing ginsenoside Rg3 as an active ingredient,
The ginsenoside Rg3-containing material is added with an alcohol extract of red ginseng to the liquid reaction medium in an amount of 0.5 to 2% (w/v) based on the volume of the liquid reaction medium, and beta-glucosidase is added. After adding the red ginseng extract in an amount of 2 to 6 times the weight of the red ginseng extract, the bioconversion reaction by enzymes was carried out at 45 to 55°C for 14 to 18 hours, and impurities were removed through centrifugation or filtration, and the remaining bioconversion product-containing solution was added. It is a bioconversion product obtained by concentration and drying,
The alcohol is hydrated ethanol at a concentration of 70 to 90% by weight,
The total ginsenoside content in the ginsenoside Rg3-containing material is 10 to 15% by weight based on the total weight of the ginsenoside Rg3-containing material,
The ginsenoside Rg3 content in the ginsenoside Rg3-containing material is 2.5-4.5% by weight based on the total weight of the ginsenoside Rg3-containing material,
The ginsenoside Rg3 is composed of S-type and R-type, and the weight ratio of the S-type to R-type is 5:1 to 8:1.
delete delete delete delete The anti-inflammatory composition of claim 1, wherein the composition is used for preventing, improving or treating inflammatory diseases.
The anti-inflammatory composition of claim 6, wherein the inflammatory disease is an inflammatory skin disease.
The anti-inflammatory composition according to any one of claims 1, 6, or 7, wherein the composition is a pharmaceutical composition or a cosmetic composition in the form of an external preparation for skin.

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