KR101429073B1 - Antibacterial composition containg rosa rugosa - Google Patents

Abstract

The present invention relates to an antimicrobial composition comprising a natural extract.

Description

ANTIBACTERIAL COMPOSITION CONTAINING ROSA RUGOSA [0002]

The present invention relates to an antimicrobial composition comprising a natural extract.

Antibiotics are substances with selective toxicity that kill microorganisms and are not toxic to humans or animals and are not inactivated by enzymes in the body. They are mainly DNA replication, transcription and decryption of genetic information, Transport, and biosynthesis of the cell wall, thereby exhibiting an effect through a mechanism of inhibiting the proliferation of microorganisms.

Until now, the main antibiotics could be chemically synthesized with those produced by microorganisms. The first antibiotic produced by this method was penicillin, discovered by Alexander Fleming in 1928, which was then largely liberated from microbial disease. In the United States, about 2-3 million tons a year are produced, of which 50% is used for animal feed and the rest is used as medicines. However, European countries and the United States are strengthening regulations to prohibit antibiotics used for the purpose of promoting the growth of animals and strictly regulate the use of human beings only by a doctor's diagnosis. This is due to the emergence of resistant antibiotics against day-to-day spread of antibiotics, thus requiring safe medicines that can replace conventional antibiotics.

In addition, since antibiotics used in the past have a very complicated structure, they are not only difficult to synthesize, but also have a problem that their synthesis is also less economical than the fermentation method. Thus, discovery of a novel substance or its intermediate product from a natural product or altering its substitution will be useful for obtaining new antibiotics.

Accordingly, the inventors of the present invention have continued to develop an antimicrobial composition having a therapeutic and preventive effect against harmful bacteria that we encounter in everyday life. As a result, they have found that they have excellent antimicrobial activity and are useful for antimicrobial compositions And the present invention was completed.

Published Korean Patent Application No. 2003-0020908

It is an object of the present invention to provide a composition having antibacterial properties and being harmless to an organism.

In order to achieve the above object, the present invention provides an antimicrobial composition comprising an extract of Alabaster leaf as an active ingredient.

The antimicrobial composition of the present invention has an antibacterial activity against bacteria, specifically bacteria on the skin surface. Therefore, it has antimicrobial activity against skin diseases such as atopy, ringworm, or psoriasis, and therefore, it can be used for therapeutic treatment.

Furthermore, the antimicrobial composition of the present invention contains a natural plant-derived component as an active ingredient, and has little side effects and is natural-friendly.

Fig. 1 shows the results of the disk diffusion method of Experimental Example 1. Fig.
C: DMSO (control group)
1: 0.25 mg leaf blade extract
2: 0.5mg leaf extract
3: 1.0 mg leaf leaf extract
4: 2.0 mg leaf leaf extract

In one aspect, the present invention relates to an antimicrobial composition comprising an extract of Rosa rugosa leaf as an active ingredient.

An antimicrobial composition which is one aspect of the present invention may contain Rosa sp. Extract as an active ingredient. The Rosa (Rosa sp.) Is elecampane rose (Rosa Banksiae ), rose ( Rosa Canina , Rosa Chinensis , Rosa Laevigatae ) and Rosa rugosa , and the like, but is not limited thereto.

In addition, the antimicrobial composition which is one aspect of the present invention may be applied to leaves, stems, flowers, and the like of the corresponding plants without limitation, but may specifically include leaf extract of the corresponding plants.

The antimicrobial composition according to one aspect of the present invention may contain an extract or fraction of Rosa rugosa leaf as an active ingredient.

In this specification, the abovementioned adaptation is a deciduous broad-leaved shrub belonging to Rosaceae, which grows at a height of 1 to 1.5 m. It grows in the sandy areas of the beach or at the foot of the mountain. The feather-shaped petals of 7-9 leaves are bloomed from May to July and bear vermilion fruit from August.

For the production of the extract or fraction, Rosa rugosa used in the present specification uses its leaves.

In addition, in the present specification, the Rosa rugosa plant can be used without limitation such as cultivated or commercially available plants.

The extract may contain a C ₁ to C ₆ alcohol extract of Rosa rugosa leaf, and specifically may include an extract of Alabama leaf-methanol or a leaf of Alabama-ethanol.

As used herein, the extract of Rosa rugosa leaf may be a crude extract of a solvent selected from the group consisting of water, C ₁ -C ₆ alcohols, and combinations thereof. The C ₁ -C ₆ alcohol may specifically be methanol or ethanol. When extracting Rosa rugosa leaves with a solvent, it is preferable to extract by adding a solvent corresponding to about 5 to 15 times of the plant, and more preferably about 10 times the amount of the solvent, It is not. The extraction may be performed by heat extraction, cold extraction, reflux cooling extraction, ultrasonic extraction or the like, and there is no limitation as long as it is an extraction method that is obvious to a person skilled in the art. The extraction may be carried out at room temperature, but it may be carried out under heating at a temperature of about 40 to 100 ° C, more preferably about 80 ° C, for a more efficient extraction, It is not. The extraction time is preferably about 2 to 4 hours, more preferably about 3 hours, but it is not limited thereto and may be varied depending on conditions such as extraction solvent and extraction temperature. The extraction may be carried out one or more times several times to obtain a larger amount of the active ingredient, preferably 1 to 5 times, more preferably 3 times of continuous extraction.

In this specification, the Rosa rugosa extract may include a crude extract of Rosa rugosa leaf as described above, and may be included as a soluble fraction of an organic solvent obtained by further extracting the crude extract with an organic solvent having a low polarity It is possible. Examples of the organic solvent include, but are not limited to, hexane, methylene chloride, ethyl acetate, n-butanol, and the like. The extract or the soluble fraction of the extract may be used as it is, or may be used as an extract form by concentration after filtration, and may be used as a form of a lyophilizate by concentration and freeze-drying.

The Rosa rugosa leaf extract of the present invention is preferably, but not limited to, prepared by the following steps:

1) extracting the dried plant by adding an extraction solvent;

2) filtering the extract of step 1);

3) Step of extracting the filtered extract of step 2) by concentration under reduced pressure.

The extraction solvent is preferably a solvent selected from water, an alcohol or a mixture thereof, preferably a C ₁ to C ₄ lower alcohol or a mixed solvent thereof. More preferably, the extraction solvent is methanol or ethanol, But is not limited thereto. The amount of the extraction solvent is preferably 0.5 to 100 times, more preferably 5 to 10 times, the dry weight of the corresponding leaf, but is not limited thereto. The extraction method may be a conventional extraction method such as supercritical extraction, subcritical extraction, high temperature extraction, high pressure extraction, hot water extraction, immersion extraction, reflux cooling extraction and ultrasonic extraction. Preferably, ≪ / RTI > The temperature for extraction is preferably from 10 to 100 ° C, more preferably room temperature, but is not limited thereto. The extraction time is preferably 2 hours to 24 hours, more preferably 3 hours, but is not limited thereto.

In the above method, it is preferable, but not limited, to use a vacuum rotary evaporator for the vacuum concentration in step 3). The drying is preferably, but not exclusively, reduced-pressure drying, vacuum drying, boiling drying, spray drying, room temperature drying or freeze-drying.

The leaf blade extract of the present invention preferably includes but is not limited to the following steps in the step of preparing the extract:

4) Extracting the extract of step 3) with an organic solvent to prepare fractions.

In the above method, the organic solvent in step 4) is preferably n-hexane, dichloromethane and ethyl acetate, more preferably ethyl acetate, but not limited thereto Do not.

In this method, the fraction of step 4) was prepared by suspending a 70% ethanol extract in distilled water, mixing the same amount of n-hexane, separating the hexane layer by adding a separating funnel, The dichloromethane layer was separated and removed, and the remaining water layer was again mixed with an equal volume of ethyl acetate. The ethyl acetate layer was separated, concentrated, lyophilized, and dissolved in ethyl acetate It is preferable to prepare a fraction. The fraction may be obtained by repeating the fractionation process from 1 to 5 times, preferably 3 times, from the extract, followed by fractionation and concentration under reduced pressure. However, the fraction is not limited thereto.

In a specific example of the present invention, the disk diffusion method was performed to confirm the antibacterial activity of the leaf blade extract of the present invention. As a result, it was found that the leaf extract of Toxoplasma gondii exhibits a wide transparent zone or has a high antimicrobial activity with little growth of bacteria.

In the antimicrobial composition which is one aspect of the present invention, the bacteria may specifically include skin pathogenic bacteria, and more specifically, Corynebacterium xerosis .

In a composition according to one aspect of the invention, the bacterium may specifically include a dermatophilic bacterium, and more particularly, a composition comprising Candida albicans , S. cerevisiae , Escherichia coli , B. subtilis , S. mutans , S. aureus , E. hirae , and the like), E. coli , Bacillus subtilis , Streptococcus mutans , Staphylococcus aureus , , M. luteus , methicillin resistant staphylococcus aureus (MRSA), Propionibacterium acnes ( Propionibacterium acnes) acnes ), Epidermophyton floccosum , Microsporum audouinii , Trichophyton, ferrugineum , Trichophyton < RTI ID = 0.0 > mentagrophytes , Trichophyton ruburm , Staphylococcus, aureus , Staphylococcus epidermis , Pityrosporum ovale ), candida albicans ( candida albicans), Corynebacterium zero sheath (Corynebacterium xerosis and Trichomonas Vaginalis ). ≪ / RTI > More specifically, according to one aspect of the compositions of the present invention, the bacteria Corynebacterium zero sheath (Corynebacterium xerosis ) can be uniform.

In the antimicrobial composition according to one aspect of the present invention, the composition may contain 0.02 to 50% by weight of Rosa rugosa leaf extract, based on the total weight of the composition. It is necessary to contain the extract of Rosa rugosa leaf within the above range to have antimicrobial properties. That is, when the extract of Rosa rugosa leaf is contained in an amount of less than 0.02% by weight based on the total weight of the composition, the antimicrobial activity against the bacterium is not observed, and the extract of Rosa rugosa leaf is 50 If it is contained in an amount of more than 1% by weight, it affects the composition ratio of other contained materials. In view of the above, the composition of the present invention may contain 0.02 to 50 wt%, 0.02 to 50 wt%, 0.02 to 50 wt%, 0.02 to 50 wt%, 0.02 to 50 wt% of Rosa rugosa leaf extract, 50% by weight or 0.02 to 50% by weight of Rosa rugosa leaf extract.

In the antimicrobial composition which is one aspect of the present invention, the leaf extract includes Rosa rugosa leaf-C ₁ -C ₆ alcohol extract.

In the antimicrobial composition which is one aspect of the present invention, the alcohol may be methanol or ethanol.

In the antimicrobial composition which is one aspect of the present invention, the composition may be a cosmetic composition.

The formulation of the cosmetic composition is not particularly limited and may be appropriately selected according to the purpose. For example, it can be applied to softeners (skin lotion and milk lotion), nutrition lotion, essence, nutrition cream, massage cream, pack, gel, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing water, A body lotion, a body cream, a body oil, and a body essence, but the present invention is not limited thereto. In addition, the cosmetic composition may be used in the form of an external preparation for skin in the form of ointment, patch, or the like.

The cosmetic composition according to the present invention may contain, in addition to the above-mentioned substances, other ingredients which can give a synergistic effect to the main effect, so long as they do not impair the main effect. The cosmetic composition according to the present invention may further comprise a moisturizing agent, an emollient agent, an ultraviolet absorber, an antiseptic, a bactericide, an antioxidant, a pH adjuster, an organic and inorganic pigment, a fragrance, a cold agent or a limiting agent. The compounding amount of the above components can be easily selected by those skilled in the art within a range not to impair the objects and effects of the present invention. The amount thereof may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, have.

In the antimicrobial composition which is one aspect of the present invention, the composition includes a health food composition.

The health food composition of the present invention provides various forms of food additives or functional foods. The composition may be processed into an extruded tea, a liquid tea, a beverage, a fermented milk, a cheese, a yogurt, a juice, a probiotic agent, a health supplement, and the like, and various other food additives.

In one embodiment, the composition may contain other ingredients or the like that can give synergistic effects to the main effect within a range that does not impair the intended main effect of the present invention. For example, additives such as perfume, coloring agent, bactericide, antioxidant, preservative, moisturizing agent, thickening agent, inorganic salt, emulsifier and synthetic polymer substance may be further added for improvement of physical properties. In addition, it may further contain auxiliary components such as water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymeric polysaccharides and seaweed extract. The above components may be mixed and selected without difficulty by those skilled in the art depending on the purpose of formulation or use, and the amount thereof may be selected within a range that does not impair the objects and effects of the present invention. For example, the addition amount of the above components may be in the range of 0.01 to 5% by weight, more specifically 0.01 to 3% by weight, based on the total weight of the composition.

The composition according to the present invention may be in various forms such as a solution, an emulsion, a viscous mixture, a tablet, a powder, etc., and may be administered by various methods such as simple drinking, injection administration, spraying or squeezing.

In the antimicrobial composition which is one aspect of the present invention, the composition includes a pharmaceutical composition.

The formulation of the pharmaceutical composition according to the present invention may be a solution, a suspension, a milk, a gel, a drip agent, a suppository, a patch or a spray agent, but is not limited thereto. The formulations can be readily prepared according to conventional methods in the art and can be prepared by conventional means such as excipients, wetting agents, emulsifying accelerators, suspending agents, salts or buffers for controlling osmotic pressure, coloring agents, spices, stabilizers, preservatives, Adjuvants may be used as appropriate.

The effective ingredients of the pharmaceutical composition of the present invention will vary depending on the age, sex, weight, pathological condition and severity of the subject to be treated, administration route or judgment of the prescriber. Determination of the amount of application based on these factors is within the level of ordinary skill in the art and its daily dose is, for example, 0.000025 mg / g / day to 0.025 mg / g / day, more specifically 0.00025 mg / g / day. < / RTI >

The pharmaceutical composition of the present invention may be administered orally or transdermally, but is not limited thereto.

In the antimicrobial composition which is one aspect of the present invention, the composition may be a composition for external application to the skin. Specifically, the composition for external application for skin includes a solution, a suspension, a spray, a patch, a pad, a cream, an ointment and a gel.

Hereinafter, the present invention will be described in detail with reference to Examples and Production Examples. However, the following examples and preparative examples are merely illustrative of the present invention and are not intended to limit the scope of the present invention.

< Manufacturing example  1> Preparation of leaf extract

The leaves were dried, pulverized and extracted twice with methanol for 48 hours at room temperature. And concentrated under reduced pressure of 45 degrees.

< Manufacturing example  2> Preparation of strain for antibacterial experiment

Corynebacterium zero sheath (Corynebacterium xerosis , KCTC 9105) were cultured in BHIB (Brain heart infusion broth) (37 g / L) medium at 30 ° C for 24 hours. 200 [mu] l of the above culture was dispensed into a petri dish in which BHI agar was hardened, and the resultant was smoothed with a sterilized smear rod.

< Experimental Example  1> Antibacterial test by disk diffusion method

In order to confirm the antimicrobial activity of the leaf blade extract prepared by the above method, the disk diffusion method was performed as described below.

Sterilized paper disks (8 mm) were adhered to the culture medium with Corynebacterium xerosis by flame sterilized tweezers. The leaf extracts, which were dissolved in DMSO, were absorbed onto the discs at 0.25, 0.5, 1 and 2 mg, respectively. After incubation at 30 ° C for 48 hours, antimicrobial activity inhibition rings were observed around the disc (FIG. 1).

As can be seen from FIG. 1, it was confirmed that the leaf blade extract had antimicrobial properties by forming a transparent ring against the bacteria. Therefore, the leaf blade extract of the present invention is excellent in antibacterial effect and has no side effects, so that it can be effectively used for removing bacteria. Especially, 1mg of leaf extract showed better activity.

Hereinafter, a formulation example of the composition according to the present invention will be described. However, the pharmaceutical composition, the cosmetic composition or the health food composition can be applied to various formulations, and the present invention is not limited thereto but is specifically described.

[Formulation Example 1] Softening lotion (skin lotion)

Compounding ingredient Content (% by weight) Rosa rugosa leaf extract 0.0025 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 Phage-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 2] Nutritional lotion (Milk lotion)

Compounding ingredient Content (% by weight) Rosa rugosa leaf extract 0.0025 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Wax 4.0 Polysorbate 60 1.5 Caprylic / capric triglyceride 5.0 Squalane 5.0 Sorbitacecequioleate 1.5 Liquid paraffin 0.5 Cetearyl alcohol 1.0 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 3] Nourishing cream

Compounding ingredient Content (% by weight) Rosa rugosa leaf extract 0.0025 glycerin 3.0 Butylene glycol 3.0 Liquid paraffin 7.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Squalane 5.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Polysorbate 60 1.2 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 4] Massage cream

Compounding ingredient Content (% by weight) Rosa rugosa extract 0.0025 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 45.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Wax 4.0 Cetearyl glucoside 1.5 Sesquioleic acid sorbitan 0.9 Vaseline 3.0 paraffin 1.5 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 5] Pack

Compounding ingredient Content (% by weight) Rosa rugosa extract 0.0025 glycerin 4.0 Polyvinyl alcohol 15.0 Hyaluronic acid extract 5.0 Beta Glucan 7.0 Allantoin 0.1 Nonyl phenyl ether 0.4 Polysorbate 60 1.2 Ethanol preservative 6.0 Good Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 6] ointment

Compounding ingredient Content (% by weight) Rosa rugosa extract 0.0025 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Squalane 1.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 Wax 4.0 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 1] Soft capsule

400 mg / capsule was mixed with 0.0025 g of Rosa rugosa leaf extract, 50 mg of red ginseng extract, 2 mg of palm oil, 8 mg of palm kernel oil, 4 mg of yellowpearl and 6 mg of lecithin, .

[Formulation Example 2] Tablets

Mixed with 0.0025 g of Rosa rugosa leaf extract, 100 mg of glucose, 50 mg of red ginseng extract, 96 mg of starch and 4 mg of magnesium stearate, 40 mg of 30% ethanol was added to form granules, followed by drying at 60 ° C The tablets were tableted using a tablet machine.

[Formulation Example 3] Granules

Granules were formed by mixing 150 mg of Rosa rugosa leaf extract, 100 mg of glucose, 50 mg of red ginseng extract and 600 mg of starch and 100 mg of 30% ethanol, followed by drying at 60 ° C to form granules, Lt; / RTI &gt; The final weight of the contents was 1 g.

[Formulation Example 4] Drinking agent

0.0025 g of Rosa rugosa leaf extract, 10 g of glucose, 50 mg of red ginseng extract, 2 g of citric acid and 187.8 g of purified water were mixed and filled into bottles. The final volume of the contents was adjusted to 200 ml.

[Formulation Example 5] Preparation of health food

Rosa rugosa leaf extract ............................ 0.0025g

Vitamin mixture

Vitamin A Acetate ....................... 70 ㎍

Vitamin E ............................................ 1.0 mg

Vitamin B1 ........................................... 0.13 mg

Vitamin B2 .......................................... 0.15 mg

Vitamin B6 ........................................... 0.5 mg

Vitamin B12 .............................. 0.2 g

Vitamin C ............................................. 10 mg

Biotin ................................................. 10 [mu] g

Nicotinic acid amide .................................. 1.7 mg

Folic acid ................................................. ..... 50 μg

Calcium pantothenate .................................... 0.5 mg

Mineral mixture

Ferrous sulfate .......................................... 1.75 mg

Zinc oxide ............................................ 0.82 mg

Magnesium carbonate ...................................... 25.3 mg

Potassium Phosphate ......................................... 15 mg

Secondary calcium phosphate ...................................... 55 mg

Potassium citrate ............................................ 90 mg

Calcium carbonate .............................................. 100 mg

Magnesium chloride ..................................... 24.8 mg

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

[Formulation Example 6] Preparation of health drink

Rosa rugosa leaf extract .......................... 0.0025g

Citric acid ................................................. ... 1000 mg

oligosaccharide................................................. .... 100 g

Plum concentrate ................................................ ..... 2 g

Taurine ................................................. ........... 1 g

Purified water was added to the mixture to complete 900 ml

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was heated at 85 DEG C for about 1 hour with stirring, and the solution thus prepared was filtered to obtain a sterilized 2-liter container, which was sealed and sterilized, &Lt; / RTI &gt;

Although the composition ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the blending ratio according to the regional or national preference such as the demand level, the demanding country, the use purpose, and the like. It will be understood by those skilled in the art that various changes in form and details may be made therein without departing from the spirit and scope of the invention as defined by the appended claims.

While the present invention has been particularly shown and described with reference to specific embodiments thereof, those skilled in the art will readily appreciate that many modifications are possible in the exemplary embodiments without materially departing from the novel teachings and advantages of this invention. something to do. Accordingly, the actual scope of the present invention will be defined by the appended claims and their equivalents.

Claims (7)

An antimicrobial composition comprising a C ₁ to C ₆ alcohol extract of Rosa rugosa leaf as an active ingredient,
Wherein the bacterium is Corynebacterium xerosis . delete The method according to claim 1,
Wherein the composition comprises an extract of Rosa rugosa leaf in an amount of 0.02 to 50% by weight based on the total weight of the composition.
delete 4. The composition of claim 1 or 3 wherein the composition is a cosmetic composition.
4. The composition of claim 1 or 3, wherein the composition is a health food composition.
4. The composition of claim 1 or 3, wherein the composition is a pharmaceutical composition.

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