KR102777268B1 - Cosmethic composition for skin whitening containing essential oil of Siegesbeckia glabrescens Makino flower - Google Patents

Abstract

The present invention relates to a skin whitening cosmetic composition comprising an essential oil extracted from a jindeukchal flower. The essential oil extracted from a jindeukchal flower according to the present invention has an excellent skin whitening effect by inhibiting the proliferation of melanocytes at the skin cell level and inhibiting the activity of tyrosinase and melanin biosynthesis in melanocytes. Therefore, the jindeukchal flower essential oil according to the present invention can be usefully used as a cosmetic composition, a food composition, a quasi-drug composition, a pharmaceutical composition, or a food composition.

Description

{Cosmethic composition for skin whitening containing essential oil of Siegesbeckia glabrescens Makino flower}

The present invention relates to a skin whitening cosmetic composition comprising essential oil extracted from the flower of Jindeukchal.

The skin covers the outer surface of the human body and protects the inside of the body from external environmental stimuli. The skin is divided into the epidermis, dermis, and subcutaneous fat. The epidermis, which constitutes the outermost layer of the skin, is composed of the stratum corneum, stratum lucidum, stratum granulosum, stratum spinosum, and stratum basale, and contains various cells including keratinocytes, melanocytes, Langerhans cells, and Merkel cells. The homeostasis of the epidermis is maintained by the proliferation, differentiation, and exfoliation of keratinocytes, the immune response of the entire skin is regulated by Langerhans cells, and the tactile function exists by Merkel cells.

Melanin-forming cells exist in the basal layer, the lowest part of the epidermis, and when stimulated by ultraviolet rays, tyrosine and tyrosinase in the melanin-forming cells react to oxidize Dopa into Dopaquinone, thereby synthesizing melanin. Melanin is transferred to keratinocytes through melanosomes and distributed throughout the epidermis.

Melanin determines the color of skin and hair and is expressed as eumelanin or pheomelanin depending on the ability to produce melanosomes, the number of melanosomes (melanin) that have moved to the epidermis, and the degree of maturity. Melanin protects cells by suppressing damage to DNA caused by photobiological reactions of ultraviolet rays, damage to cells caused by photosynthetic substances or reactive oxygen species inside and outside the cell, and inflammatory reactions.

However, if melanin is not properly removed due to overproduction of melanin or abnormal exfoliation process of the skin, it causes skin pigmentation such as freckles, liver spots, and melasma.

The subcutaneous fat, which is the innermost layer of the skin, protects the body from stimulation by temperature changes such as heat and cold, and has fat in fat cells connected by fibrous tissue, and this fat layer has different thicknesses in each body part. The dermis, a thick layer of cells, maintains and protects the tissues within the skin. The dermis has a thick skin layer and protects the body from external pressure, and the nerves in the dermis act as receptors for pain and touch, such as detecting touch and heat, and blood vessels supply nutrients to cells. In addition, the dermis maintains its structure by fibroblasts, maintaining the elasticity and physical condition of the skin.

Meanwhile, essential oils are substances characterized by strong volatility that are obtained from plants with unique fragrances produced by a single plant or plant species through physical methods such as steam distillation, organic solvent extraction, and pressing. Essential oils are produced from various parts of plants such as flowers, leaves, roots, stems, and fruits, and the fragrance, physiological activity, and components may differ depending on each part.

Even if it is the same plant species, the chemical composition of the essential oil varies depending on the cultivation area, soil environment, and climate conditions, so it has a high degree of regional specificity. In addition, since the essential oil has a molecular weight of about 200 Da, it has a relatively high absorption capacity into skin cells and tissues, and thus exhibits physiological activity and therapeutic efficacy.

Jindeukchal ( Siegesbeckia glabrescens Makino) is an annual plant of the Asteraceae family that grows along roadsides and in fields. From August to September, yellow flowers bloom in corymb form at the ends of stems and branches. The involucre has five lobes, with the lanceolate flower having three tips and the tubular flower having five tips. The involucre surrounds the fruit and has hairs that secrete a sticky liquid, allowing it to stick to other objects. Jindeukchal is also called Heeryum, Heecheom, and Jindungchal, and there are three types: Hairy Jindeukchal, Jindeukchal, and Jeju Jindeukchal.

In oriental medicine, the efficacy of Jindeokchal is known to be effective in treating high blood pressure, diabetes, stroke, paralysis, and strengthening physical strength. The chirenol component of Jindeokchal whole plant inhibits the formation of fat cells and helps prevent obesity, and also helps prevent heart disease caused by diabetes by increasing the viability of myocardial cells. The herperidin component of Jindeokchal inhibits the proliferation of inflammatory cells that cause pain, and is effective in anti-inflammation and analgesia. However, the characteristics and efficacy of the volatile components and essential oil of Jindeokchal flowers are not known.

The purpose of the present invention is to provide a skin whitening cosmetic composition containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

In addition, another object of the present invention is to provide a skin whitening food composition containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

In addition, another object of the present invention is to provide a pharmaceutical composition for skin whitening containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

In addition, another object of the present invention is to provide a pharmaceutical composition for preventing or treating melanin hyperpigmentation disease, which comprises essential oil extracted from Siegesbeckia glabrescens Makino as an active ingredient.

In addition, another object of the present invention is to provide a method for producing Jindeukchal flower essential oil with enhanced skin whitening efficacy.

To achieve the above purpose, the present invention provides a skin whitening cosmetic composition containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

Next, another object of the present invention is to provide a skin whitening food composition containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

Furthermore, another object of the present invention is to provide a pharmaceutical composition for skin whitening containing essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

In addition, another object of the present invention is to provide a pharmaceutical composition for preventing or treating melanin hyperpigmentation disease, which comprises essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

Finally, the present invention provides a method for producing Jindeukchal flower essential oil with enhanced skin whitening efficacy, comprising the steps of: 1) washing Jindeukchal flowers; 2) precipitating the Jindeukchal flowers in hexane, an organic solvent; 3) evaporating the precipitate in a rotary evaporator to concentrate it, thereby obtaining a solid concrete; 4) dissolving the concrete with ethyl alcohol and then removing insoluble wax through vacuum cooling filtration; and 5) producing Jindeukchal flower absolute type essential oil by concentrating, separating, and refining it using a rotary evaporation.

The essential oil extracted from the Jindeukchal flower according to the present invention has an excellent skin whitening effect by inhibiting the proliferation of melanocytes at the skin cell level, inhibiting the activity of tyrosinase in melanocytes, and inhibiting melanin biosynthesis. Therefore, the Jindeukchal flower essential oil according to the present invention can be usefully used as a cosmetic composition, a food composition, a quasi-drug composition, a pharmaceutical composition, or a food composition.

Figure 1 is a flow chart showing a process for extracting absolute type essential oil from Jin Deuk Chal flowers in one embodiment of the present invention.
Figure 2 is a graph showing the cell survival rate of melanin-forming cells in essential oil separated from the flower of Jin Deuk Chal according to one embodiment of the present invention.
FIG. 3 is a graph showing the proliferation inhibitory effect of essential oil isolated from the flower of Jin Deuk Chal on melanin-forming cells in one embodiment of the present invention.
FIG. 4 is a graph showing the inhibitory effect of essential oil isolated from the flower of Jin Deuk Chal on the activity of tyrosinase in melanin-forming cells in one embodiment of the present invention.
FIG. 5 is a graph showing the inhibitory effect of essential oil isolated from the flower of Jin Deuk Chal on melanin biosynthesis in melanin-forming cells according to one embodiment of the present invention.

Hereinafter, the present invention will be described in detail with reference to the attached drawings as implementation examples of the present invention. However, the following implementation examples are presented as examples of the present invention, and if it is judged that a detailed description of a technology or configuration well known to those skilled in the art may unnecessarily obscure the gist of the present invention, the detailed description thereof may be omitted, and the present invention is not limited thereby. The present invention is capable of various modifications and applications within the scope of the following claims and equivalents interpreted therefrom.

In addition, the terms used in this specification are terms used to appropriately express preferred embodiments of the present invention, and may vary depending on the intention of the user or operator, or the customs of the field to which the present invention belongs. Therefore, the definitions of these terms should be made based on the contents throughout this specification. Throughout the specification, when a part is said to “include” a certain component, this does not mean that other components are excluded, but rather that other components can be further included, unless specifically stated otherwise.

Throughout this specification, '%' used to indicate the concentration of a particular substance, unless otherwise stated, is (w/w) % for solid/solid, (w/v) % for solid/liquid, and (v/v) % for liquid/liquid.

Hereinafter, the present invention will be described in more detail.

The present inventors have confirmed that essential oil derived from the flower of Jindeukchal, extracted using an organic solvent extraction method, can be used as a composition for skin whitening by inhibiting the activity of tyrosinase in melanin-forming cells and inhibiting melanin biosynthesis, and have completed the present invention.

In one aspect, the present invention relates to a cosmetic composition for skin whitening comprising essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

In one embodiment, the essential oil extracted from Siegesbeckia glabrescens Makino may be extracted from any one or more parts selected from the group consisting of Siegesbeckia leaves, stems, fruits, flowers, and roots, and preferably may be extracted from Siegesbeckia flowers, but is not limited thereto.

In one embodiment, the Siegesbeckia glabrescens Makino flower may be a flower bud just before flowering and may be an undried flower.

In one embodiment, the essential oil extracted from Siegesbeckia glabrescens Makino may be manufactured by including, but not limited to, a step of extracting Siegesbeckia glabrescens Makino with hexane (n-hexane) and then concentrating under reduced pressure to obtain a solid concrete; a step of dissolving the solid concrete in ethyl alcohol to remove insoluble wax; and a step of obtaining an essential oil by concentrating the same under reduced pressure to remove the solvent.

In one embodiment, the method for obtaining the concrete of the present invention and the method for obtaining the essential oil may include any method that can be modified by a person having ordinary knowledge in this technical field.

The term "essential oil" used in the present invention is a general term for aromatic oils (volatile substances) extracted and separated from plants (plant leaves, stems, fruits, flowers, roots, etc.), and is classified in various ways depending on the extract, extraction method, use, and purpose. Essential oils derived from natural products are classified as essential oils, absolutes, or concretes depending on the extraction method.

The term "extract" used in the present invention means an active ingredient separated from a natural product, i.e., a substance exhibiting the desired activity. The extract can be obtained by an extraction process using water, an organic solvent, or a mixed solvent thereof, and includes a dried powder of the extract or all forms formulated using the same. In addition, the extract also includes a fraction of an extract that has undergone the extraction process. The extraction method of the extract is not particularly limited, and may be extracted by, for example, stirring extraction, shaking extraction, hot water extraction, cold extraction, reflux cooling extraction, or ultrasonic extraction. As the extraction solvent, a polar solvent such as water, a C1-C4 lower alcohol, a nonpolar solvent such as hexane, chloroform, dichloromethane, or ethyl acetate, or a mixture of two or more thereof can be used.

In one embodiment, the essential oil extracted from Siegesbeckia glabrescens Makino comprises P-Cymene, 2-Isopropyl-5-methylanisole, Thymoquinone, Caryophyllene, Undecanoic acid, Bicyclogermacrene, α-Bisabolene, Lauric acid, Tridecanoic acid, Myristic acid, Linolenic acid, Ethyl linoleate, Ethyl linolenate, It may include at least one volatile organic compound selected from the group consisting of, but is not limited to, 2,2'-Methylenebis(4-methyl-6-tert-butylphenol), 1-Octadecene, Cyclotetracosane, 1-Nonadecene, Tocopherols, Aristolone, and α-Amyrin.

In one embodiment, the essential oil extracted from Siegesbeckia glabrescens Makino may be included in a concentration of 0.1 to 20 μg/mL, but is not limited thereto. However, if included in a concentration of 20 μg/mL or more, it may be toxic to skin cells, so it is preferable to use it in the concentration provided in the present invention.

In one embodiment, the composition may inhibit, but is not limited to, proliferation of melanocytes.

In one embodiment, the composition may inhibit, but is not limited to, the activity of tyrosinase in melanocytes.

In one embodiment, the composition may inhibit melanin biosynthesis within melanocytes, but is not limited thereto.

The “cosmetic composition” of the present invention can be manufactured by including a cosmetically effective amount of the essential oil extracted from the Jindeukchal of the present invention described above and a cosmetically acceptable carrier.

In this specification, “cosmetically effective amount” means an amount sufficient to achieve the skin whitening effect of the composition of the present invention described above.

The external form of the cosmetic composition contains a cosmetically or dermatologically acceptable medium or base. It may be provided in any formulation suitable for topical application, for example in the form of a solution, a gel, a solid, a pasty anhydrous product, an emulsion obtained by dispersing an oil phase in an aqueous phase, a suspension, a microemulsion, a microcapsule, a microgranule or a vesicular dispersion of ionic (liposomes) and nonionic type, or in the form of a cream, a skin, a lotion, a powder, an ointment, a spray or a concealer stick. These compositions can be prepared according to methods conventional in the art. The composition according to the invention can also be used in the form of a foam or in the form of an aerosol composition further containing a compressed propellant.

The cosmetic composition according to one embodiment of the present invention is not particularly limited in its formulation, and may be formulated as cosmetics such as, for example, a softening toner, an astringent toner, a nourishing toner, a nourishing cream, a massage cream, an essence, an eye cream, an eye essence, a cleansing cream, a cleansing foam, a cleansing water, a pack, a powder, a body lotion, a body cream, a body oil, and a body essence.

When the cosmetic composition of the present invention is in the form of a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tragacanth, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as a carrier component.

When the cosmetic composition of the present invention is in the form of a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and particularly in the case of a spray, a propellant such as chlorofluorohydrocarbon, propane/butane or dimethyl ether may be additionally included.

When the formulation of the cosmetic composition of the present invention is a solution or emulsion, a solvent, a solvating agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol 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, liquid diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or tragacanth, etc. can be used as carrier components.

When the formulation of the cosmetic composition of the present invention is a surfactant-containing cleansing, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyl taurate, sarcosinate, fatty acid amide ether sulfate, alkyl amidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, linolenic derivative, or ethoxylated glycerol fatty acid ester may be used as a carrier component.

The cosmetic composition of the present invention can be applied to cosmetics such as skin, lotion, cream, essence, pack, foundation, color cosmetics, sunscreen, two-way cake, face powder, compact, makeup base, skin cover, eye shadow, lipstick, lip gloss, lip fix, eyebrow pencil, toner, and cleansing agents such as shampoo and soap.

A cosmetic composition according to one embodiment of the present invention may further include, in addition to the essential oil extracted from the above-described Jin Deuk Chal, a functional additive and an ingredient included in a general cosmetic composition. The functional additive may include an ingredient selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, high molecular peptides, high molecular polysaccharides, sphingolipids, and seaweed extracts.

In addition to the functional additives, the cosmetic composition of the present invention may also contain ingredients included in general cosmetic compositions, if necessary. In addition, examples of the contained ingredients include fat components, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, bactericides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, fragrances, blood circulation promoters, cooling agents, antiperspirants, purified water, and the like.

In one aspect, the present invention relates to a skin whitening food composition comprising essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

Since the food composition of the present invention includes the essential oil extracted from the aforementioned Jindeukchal, descriptions of the same content as the essential oil extracted from the aforementioned Jindeukchal of the present invention are omitted in order to avoid excessive complexity of the present specification due to descriptions of the same content.

The food composition of the present invention can be formulated into various forms such as tablets, pills, granules, capsules, liquid preparations, and beverages, and added to foods. There is no particular limitation on the type of food. Examples of foods to which the essential oil extracted from the jindeukchal of the present invention can be added include drinks, meat, sausages, bread, biscuits, rice cakes, chocolate, candies, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, alcoholic beverages, and vitamin complexes, dairy products, and dairy products, and include all health foods and health functional foods in the conventional sense.

The health food and health functional food composition containing the essential oil extracted from Jindeukchal according to the present invention can be added to food as it is or used together with other foods or food ingredients, and can be used appropriately according to a conventional method. The mixing amount of the essential oil extracted from Jindeukchal can be appropriately determined depending on its purpose of use (prevention or improvement). In general, the amount of the composition in the health food and health functional food can be added in an amount of 0.1 to 90 parts by weight of the total food weight. However, in the case of long-term intake for the purpose of maintaining health or regulating health, the amount can be below the above range, and since there is no problem in terms of safety, the active ingredient can also be used in an amount above the above range.

The health food and health functional food composition of the present invention contains the essential oil extracted from the jindeukchal of the present invention as an essential ingredient in the indicated ratio, and has no particular limitations on other ingredients, and may contain various flavoring agents or natural carbohydrates as additional ingredients like a conventional beverage. Examples of the above-mentioned natural carbohydrates are conventional sugars such as monosaccharides, for example, glucose, fructose, etc.; disaccharides, for example, maltose, sucrose, etc.; and polysaccharides, for example, dextrin, cyclodextrin, etc., and sugar alcohols such as xylitol, sorbitol, and erythritol. As flavoring agents other than those described above, natural flavoring agents (thaumatin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used. The proportion of the natural carbohydrate is generally about 1 to 20 g, preferably about 5 to 12 g, per 100 g of the health functional food composition of the present invention.

In addition to the above, the health food and health functional food composition containing the essential oil extracted from the Jin Deuk Chal of the present invention may contain various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic flavoring agents and natural flavoring agents, coloring agents and thickeners (cheese, chocolate, etc.), pectic acid and its salts, alginic acid and its salts, organic acids, protective colloid thickeners, pH regulators, stabilizers, preservatives, glycerin, alcohol, carbonating agents used in carbonated beverages, etc. In addition, the health food and health functional food composition of the present invention may contain fruit pulp for the production of natural fruit juice and fruit juice drinks and vegetable drinks.

These ingredients can be used independently or in combination. The proportion of these additives is not so important, but is generally selected in the range of 0.1 to about 20 parts by weight per 100 parts by weight of the health food and health functional food composition containing the essential oil extracted from the Jindeukchal of the present invention.

In one aspect, the present invention relates to a pharmaceutical composition for skin whitening comprising essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.

Since the pharmaceutical composition of the present invention includes the essential oil extracted from the aforementioned Jindeukchal, descriptions of the overlapping contents with the essential oil extracted from the aforementioned Jindeukchal of the present invention are omitted in order to avoid excessive complexity of the present specification due to descriptions of overlapping contents.

The term "quasi-drug" in the present invention refers to products that are used for the purpose of diagnosing, treating, improving, alleviating, managing or preventing diseases of humans or animals, and have a milder effect than a pharmaceutical product. For example, according to the Pharmaceutical Affairs Act of the Republic of Korea, quasi-drugs are products other than those used for the purpose of pharmaceutical products, and include products used for the treatment or prevention of diseases of humans or animals, products that have a mild effect on the human body or do not act directly, etc.

The pharmaceutical composition of the present invention can be manufactured in the form of an ointment, lotion, spray, patch, cream, powder, suspension, gel, gel, or filter filler, but is not limited thereto.

When the essential oil extracted from the Jindeukchal of the present invention is used as an over-the-counter drug additive, the essential oil extracted from the Jindeukchal may be added as is or used together with other over-the-counter drugs or over-the-counter drug ingredients, and may be used appropriately according to a conventional method. The mixing amount of the effective ingredient may be appropriately determined depending on the intended use.

In one aspect, the present invention relates to a pharmaceutical composition for preventing or treating melanin hyperpigmentation disease, comprising an essential oil extracted from Siegesbeckia glabrescens Makino as an active ingredient.

Since the pharmaceutical composition of the present invention includes the essential oil extracted from the aforementioned Jindeukchal, descriptions of the same content as the essential oil extracted from the aforementioned Jindeukchal of the present invention are omitted in order to avoid excessive complexity of the present specification due to descriptions of the same content.

In one embodiment, the melanin hyperpigmentation disorder can be, but is not limited to, melasma, freckles, senile pigmentation, or solar lentigines.

The above "prevention" means any action that reduces the frequency or degree of occurrence of a pathological phenomenon. Prevention may be complete or partial. In this case, it may mean a phenomenon in which the symptoms of melanin hyperpigmentation disease in an individual are reduced compared to when the composition is not used.

The above "treatment" means any act of clinical intervention to change the natural process of the target or cell to be treated, and may be performed during the progression of a clinical pathological condition or to prevent it. The desired therapeutic effect may include preventing the occurrence or recurrence of a disease, alleviating symptoms, reducing all direct or indirect pathological consequences of the disease, preventing metastasis, reducing the rate of disease progression, alleviating or temporarily alleviating the disease condition, or improving the prognosis.

The pharmaceutical composition of the present invention is administered in a pharmaceutically effective amount. The term "pharmaceutically effective amount" as used in the present invention means an amount sufficient to treat a disease at a reasonable benefit/risk ratio applicable to medical treatment and not causing side effects, and the effective dosage level can be determined according to factors including the patient's health condition, the type and severity of the disease, the activity of the drug, the sensitivity to the drug, the administration method, the administration time, the administration route and the excretion rate, the treatment period, the drug used in combination or simultaneously, and other factors well known in the medical field. The composition of the present invention can be administered as an individual therapeutic agent or in combination with other therapeutic agents, can be administered sequentially or simultaneously with conventional therapeutic agents, and can be administered singly or in multiple doses. Considering all of the above factors, it is important to administer an amount that can obtain the maximum effect with the minimum amount without side effects, and this can be easily determined by those skilled in the art.

In the present invention, the "subject" is not particularly limited to an entity for the purpose of preventing or treating a melanin hyperpigmentation disease, and refers to an animal including a human, for example, a mammal including a non-primate (e.g., a cow, a pig, a horse, a cat, a dog, a rat, and a mouse) and a primate (e.g., a monkey, for example, a cynomolgous monkey and a chimpanzee). In some cases, it may be an entity excluding a human.

The composition according to the present invention may contain only a pharmaceutically effective amount of essential oil extracted from Jin Deuk Chal, or may contain one or more pharmaceutically acceptable carriers, excipients or diluents. The pharmaceutically effective amount as mentioned above means an amount sufficient to prevent, improve and treat the symptoms of melanin hyperpigmentation disease. The term "pharmaceutically acceptable" as mentioned above means a composition that is physiologically acceptable and does not typically cause allergic reactions such as gastrointestinal disorders, dizziness or similar reactions when administered to humans.

In addition, the composition containing a pharmaceutically acceptable carrier can be in various oral or parenteral dosage forms. When formulated, it can be prepared using diluents or excipients such as fillers, bulking agents, binders, wetting agents, disintegrating agents, and surfactants that are commonly used. The above carrier, excipient and diluent may be at least one selected from the group consisting of lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia gum, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, saline solution, methyl hydroxybenzoate, propyl hydroxy benzoate, talc, magnesium stearate, and mineral oil, dextrin, calcium carbonate, propylene glycol and liquid paraffin, but is not limited thereto, and all conventional carriers, excipients or diluents can be used. The above components may be added independently or in combination to the essential oil extracted from the effective ingredient, Jindeukchal.

In addition, the pharmaceutical composition of the present invention may have any one dosage form selected from the group consisting of tablets, pills, powders, granules, capsules, suspensions, oral solutions, emulsions, syrups, sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, and suppositories. As a base for the suppository, witepsol, macrogol, Tween 61, cacao butter, laurin butter, glycerol, gelatin, and the like can be used.

The essential oil extracted from the present invention can be administered in various oral and parenteral formulations for clinical administration, and when formulated, it is manufactured using diluents or excipients such as commonly used fillers, bulking agents, binders, wetting agents, disintegrants, and surfactants.

Solid preparations for oral administration include tablets, pastes, powders, granules, capsules, troches, etc., and these solid preparations are prepared by mixing essential oils extracted from one or more of the present invention's ginsengs with at least one excipient, such as starch, calcium carbonate, sucrose, lactose, or gelatin. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral administration include suspensions, oral solutions, emulsions, or syrups, and in addition to commonly used simple diluents such as water and liquid paraffin, various excipients such as wetting agents, sweeteners, flavoring agents, and preservatives may be included.

Preparations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, lyophilized preparations, suppositories, etc. Non-aqueous solutions and suspensions can be used, such as propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate. Suppository bases can be used, such as witepsol, macrogol, Tween 61, cacao butter, laurin butter, glycerol, and gelatin.

In addition, the effective dosage for the human body of the essential oil extracted from the Jin Deuk Chal of the present invention may vary depending on the patient's age, body weight, sex, dosage form, health condition, and disease severity, and is generally about 0.001-100 mg/kg/day, and preferably 0.01-35 mg/kg/day. When based on an adult patient weighing 70 kg, it is generally 0.07-7000 mg/day, and preferably 0.7-2500 mg/day, and may be administered once or several times a day at regular intervals depending on the judgment of a doctor or pharmacist.

The pharmaceutical composition of the present invention can be used alone or in combination with methods using surgery, radiation therapy, hormone therapy, chemotherapy, or biological response modifiers.

The pharmaceutical composition of the present invention can also be provided in the form of an external preparation containing essential oil extracted from Jindeukchal as an active ingredient.

When the pharmaceutical composition of the present invention is used as a skin external preparation, it may additionally contain adjuvants commonly used in the field of dermatology, such as any other ingredients commonly used in skin external preparations, such as fatty substances, organic solvents, solubilizers, thickening and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic emulsifiers, nonionic emulsifiers, fillers, metal ion sequestering agents, chelating agents, preservatives, vitamins, blocking agents, humectants, essential oils, dyes, pigments, hydrophilic activators, lipophilic activators or lipid vesicles. In addition, the above ingredients may be introduced in amounts commonly used in the field of dermatology. When the pharmaceutical composition of the present invention is provided as a skin external preparation, it may be in the form of, but is not limited to, an ointment, a patch, a gel, a cream or a spray.

In one aspect, the present invention provides a method for producing Jindeukchal flower essential oil having skin whitening efficacy.

In one embodiment, the method may include: a 1st step of washing a jindeukchal flower; a 2nd step of precipitating the jindeukchal flower in hexane, which is an organic solvent; a 3rd step of evaporating the precipitate in a rotary evaporator to concentrate it, thereby obtaining a solid concrete; a 4th step of dissolving the concrete with ethyl alcohol and then removing insoluble wax through a vacuum cooling filtration; and a 5th step of producing a jindeukchal flower absolute type essential oil by concentrating, separating, and refining it using a rotary evaporation.

Hereinafter, embodiments of the present invention will be described in more detail with reference to the attached drawings. However, the following embodiments are only intended to concretize the contents of the present invention, and the present invention is not limited thereby.

<Example 1> Production of absolute type essential oil extracted from Jindeukchal flower

Figure 1 is a flow chart showing a process for extracting essential oil from a Siegesbeckia glabrescens Makino flower according to one embodiment of the present invention. The Siegesbeckia glabrescens Makino flower was collected in August from a wild flower growing at Hoseo University (Asan, Korea).

Referring to Fig. 1, the Jin Deuk Chal flower was extracted through a volatile organic solvent extraction method. First, the Jin Deuk Chal flower was extracted with hexane (n-hexane), and then precipitated to obtain a precipitate. Thereafter, the precipitate was evaporated and concentrated using a rotary evaporation to obtain a solid concrete. Thereafter, the concrete was dissolved in ethyl alcohol, and then vacuum cooling filtration was used to remove insoluble wax, and again, a rotary evaporation was used to remove the solvent, and concentration, separation, and purification were performed to finally obtain an absolute type of Jin Deuk Chal flower essential oil. The Jin Deuk Chal flower essential oil manufactured by the above method was stored in a -80 ℃ freezer until used in the experiment.

<Example 2> Analysis of the components of absolute type Jin Deuk Chal flower essential oil

The component analysis of the essential oil of Jin Deuk Chal flower was requested to KBSI (Korea Basic Science Institute, Seoul Center). A gas chromatography/mass spectrometer (6890N GC/5975i MS, Agilent, USA) was used, and the column of GC/MS was DB5-MS (30 m×50 μm, 0.25 μm). The carrier gas was helium and flowed at 1 mL/min for analysis. The oven temperature was maintained at 40℃ - 2℃/min - 230℃ - 5℃/min - 300℃ (5 min), and the injection temperature was analyzed at 280℃. In addition, the interface temperature was 300℃, the ion source temperature was 230℃, and the analyzer temperature was 150℃, and the mass range was analyzed at 40~800 m/z.

The essential oil components of Jin Deuk Chal flower were identified by comparing the retention indices (RI) of volatile components with the retention times of standard substances or by comparing the mass spectrum of volatile components with the mass spectrum of the Wiley 7Nist 05 library. RI was determined under the same conditions as the sample using C ₆ ~ C ₂₄ (n-alkane).

As a result, it was confirmed that it consists of a total of 20 components as shown in Table 1 below, and the main components are Dodecanoic acid 32.34%, Linolenic acid 10.19%, Bicyclogermacrene (24703-35-3) 8.22%, Undecanoic acid 8.13%, Caryophyllene 5.99%, Benzene, 2-methoxy-4-methyl-1-(1-methylethyl)- 5.50%, α-Amyrin 5.07%, 1-Octadecene 4.03%, Aristolone 4.00%, Tridecanoic acid 2.78%, cis-α-Bisabolene 2.37%, Cyclotetracosane 2.14%, Antioxidant BKF 1.64%, γ-Tocopherol 1.63%, p-Cymene. It was confirmed that the contents were high in the following order: 1.44%, 1-Nonadecene 1.12%, Ethyl linolenate 0.94%, Thymoquinon 0.91%, Linoleic acid ethyl ester 0.85%, and Tetradecanoic acid 0.72%.

No Component name Retention time Area (%) 1 p-Cymene 15.673 1.44 2 Benzene, 2-methoxy-4-methyl-1-(1-methylethyl)- 29.485 5.50 3 Thymoquinone 30.800 0.91 4 Caryophyllene 41.373 5.99 5 Undecanoic acid 45.747 8.13 6 Bicyclogermacrene(24703-35-3) 46.076 8.22 7 cis-α-Bisabolene 49.019 2.37 8 Dodecanoic acid 51.880 32.34 9 Tridecanoic acid 56.879 2.78 10 Tetradecanoic acid 61.894 0.72 11 Linolenic acid 79.998 10.19 12 Linoleic acid ethyl ester 80.507 0.85 13 Ethyl linolenate 80.754 0.94 14 Antioxidant BKF 90.455 1.64 15 1-Octadecene 94.270 4.03 16 Cyclotetracosane 100.321 2.14 17 1-Nonadecene 104.301 1.12 18 γ-Tocopherol 106.487 1.63 19 Aristolone 110.680 4.00 20 α-Amyrin 111.453 5.07 Total Identified(%) 100.00

<Example 3> Measurement of the effect of absolute type Jin Deuk Chal flower essential oil on the survival rate (toxicity) of melanin-forming cells

The cell viability (toxicity) of the absolute type Jin Deuk Chal flower essential oil obtained in the above Example 1 on melanocytes was investigated. Specifically, mouse melanocyte B16BL6 cells were placed in a 96-well plate at 2 × 10 ³ cells/100 μL/well, cultured in an incubator at 37°C and 5% CO ² , and then treated with the Jin Deuk Chal flower essential oil of Example 1 at a concentration of 0.1, 1, 5, 10, or 20 μg/mL and cultured for 48 hours. After that, EZ-cytox was treated, and the absorbance was measured at 450 nm.

As a result, as shown in Fig. 2, the Jindeukchal flower essential oil did not show any cytotoxicity at concentrations of 0.1 to 20 μg/mL, and rather showed a tendency for cell viability to increase. However, since the cell viability that had increased at a concentration of 20 μg/mL decreased somewhat, it was confirmed that the Jindeukchal flower essential oil manufactured in Example 1 was preferable at a concentration of 20 μg/mL or less, and was applied to subsequent experiments.

<Example 4> Measurement of the effect of absolute type Jin Deuk Chal flower essential oil on the proliferation rate of melanin-forming cells

The cell proliferation rate of the Jin Deuk Chal flower essential oil manufactured in the above Example 1 on mouse-derived melanocytes was investigated. Specifically, mouse melanocyte B16BL6 cells were placed at a concentration of 2 × 10 ³ cells/100 μL/well in a 96-well plate coated with 0.1 mg/mL collagen (type I), cultured in an incubator containing 5% CO ² at 37°C, and treated with Jin Deuk Chal flower essential oil containing 2% FBS at a concentration of 0.1, 1, 5, 10, or 20 μg/mL and cultured for 36 hours. At this time, a group treated only with 2% FBS was used as a positive control group. After that, the cells were cultured for 12 hours after treating with a BrdU labeling solution, treated with a BrdU antibody, and treated with a chemiluminescence solution to measure the cell proliferation rate.

As a result, as shown in Figure 3, the essential oil of the Jindeukchal flower showed the highest cell proliferation rate at a concentration of 1 μg/mL, and the cell proliferation rate decreased in a concentration-dependent manner starting from a concentration of 10 μg/mL.

Through these results, it was confirmed that the absolute type Jin Deuk Chal flower essential oil of the present invention effectively inhibits the proliferation of melanin-forming cells.

<Example 5> Measurement of the effect of absolute type Jin Deuk Chal flower essential oil on the activity of Tyrosinase in melanin-forming cells

The effect of the essential oil of the Chinensis chinensis flower prepared in Example 1 on the activity of tyrosinase in mouse-derived melanocytes was investigated. Specifically, mouse melanocyte B16BL6 cells were injected at 5 × 10 ⁵ cells in a 60 mm culture dish and cultured in a 5% CO ² incubator at 37°C. As a positive control, 200 nM α-MSH treated with 2% FBS was used, and the essential oil of the Chinensis chinensis flower containing 2% FBS and 200 nM α-MSH was treated at a concentration of 0.1, 1, 5, 10, or 20 μg/mL and cultured for 48 hours. After cell lysis and centrifugation, the supernatant was collected and treated with L-DOPA (2 mg/mL) at 37°C for 1 hour, and the level of tyrosinase activity was evaluated by measuring the absorbance at 490 nm.

As a result, as shown in Fig. 4, the essential oil of the Jindeukchal flower exhibited the highest tyrosinase inhibitory activity at a concentration of 1 μg/mL, and tyrosinase activity decreased in a concentration-dependent manner starting from a concentration of 10 μg/mL.

<Example 6> Measurement of the effect of Jin Deuk Chal flower absolute type essential oil on melanin biosynthesis in melanin-forming cells

The effect of the essential oil of the Chrysanthemum indicum obtained in Example 1 on melanin biosynthesis in mouse-derived melanocytes was investigated. Melanocyte-forming cells B16BL6 were injected at 5 × 10 ⁵ cells in a 60 mm culture dish and cultured in a 5% CO ² incubator at 37°C. As a positive control, 200 nM α-MSH treated with 2% FBS was used, and the essential oil of the Chrysanthemum indicum containing 2% FBS and 200 nM α-MSH was treated at a concentration of 0.1, 1, 5, 10, or 20 μg/mL and cultured for 48 hours. After that, the cells were lysed, centrifuged, and the pellet was treated with 1 N sodium hydroxide reagent at 80°C for 1 hour, and the effect on melanin pigment reduction was confirmed by measuring the absorbance at 405 nm.

As a result, as shown in Fig. 5, the absolute type of Jin Deuk Chal flower essential oil exhibited the highest melanin biosynthesis inhibitory activity at a concentration of 1 μg/mL, and it was confirmed that melanin biosynthesis in melanin-forming cells was inhibited in a concentration-dependent manner starting from a concentration of 5 μg/mL.

As described above, specific embodiments of the present invention have been described in detail; however, those skilled in the art who understand the spirit of the present invention will be able to easily suggest other backward inventions or other embodiments included within the scope of the spirit of the present invention by adding, changing, deleting, etc. other components within the scope of the same spirit. Therefore, it should be understood that the embodiments described above are exemplary in all aspects and not restrictive. The scope of the present invention is indicated by the scope of the claims described below rather than the detailed description described above, and all changes or modifications derived from the meaning and scope of the claims and the equivalent concept should be interpreted as being included in the scope of the present invention.

Claims (14)

A cosmetic composition for skin whitening, comprising essential oil extracted from Siegesbeckia glabrescens Makino as an active ingredient.
In the first paragraph,
A cosmetic composition for skin whitening, characterized in that the essential oil is extracted from the flower of Jindeukchal.
In the first paragraph,
A cosmetic composition for skin whitening, which is manufactured by including the steps of extracting the essential oil from the root of the plant with n-hexane and then concentrating under reduced pressure to obtain a solid concrete; dissolving the solid concrete in ethyl alcohol to remove insoluble wax; and concentrating the same under reduced pressure to obtain an essential oil from which the solvent has been removed.
In the first paragraph,
A cosmetic composition for skin whitening, wherein the essential oil contains a volatile organic compound.
In paragraph 4,
The above volatile organic compounds are P-Cymene, 2-Isopropyl-5-methylanisole, Thymoquinone, Caryophyllene, Undecanoic acid, Bicyclogermacrene, α-Bisabolene, Lauric acid, Tridecanoic acid, Myristic acid, Linolenic acid, Ethyl linoleate, Ethyl linolenate, 2,2'-Methylenebis(4-methyl-6-tert-butylphenol), A cosmetic composition for skin whitening, comprising at least one selected from the group consisting of 1-octadecene, cyclotetracosane, 1-nonadecene, tocopherols, aristolone, and α-amyrin.
In the first paragraph,
A cosmetic composition for skin whitening, characterized in that the essential oil is contained in a concentration of 0.1 to 20 ㎍/mL.
In the first paragraph,
The composition is a cosmetic composition for skin whitening, characterized in that it inhibits the proliferation of melanin-forming cells.
In the first paragraph,
The composition is a cosmetic composition for skin whitening, characterized in that it inhibits the activity of tyrosinase in melanin-forming cells.
In the first paragraph,
The composition is a cosmetic composition for skin whitening, characterized in that it inhibits melanin biosynthesis in melanin-forming cells.
A food composition for skin whitening, comprising essential oil extracted from Siegesbeckia glabrescens Makino as an effective ingredient.
A pharmaceutical composition for skin whitening, comprising essential oil extracted from Siegesbeckia glabrescens Makino as an active ingredient.
delete delete Step 1: Washing the Jindeukchal Flowers;
Step 2: precipitating the above Jin Deuk Chal flower in hexane (n-hexane), an organic solvent;
Step 3: obtaining solid concrete by evaporating and concentrating the above sediment in a rotary evaporator;
Step 4: Dissolving the above concrete with ethyl alcohol and then removing the insoluble wax through vacuum cooling filtration; and
A method for producing Jindeukchal flower essential oil with enhanced skin whitening efficacy, comprising the steps of producing Jindeukchal flower absolute type essential oil by concentrating, separating, and refining using a rotary evaporation.