KR20160020225A - Cosmetic or pharmaceutical composition for skin whitening comprising Astragaloside I or a pharmaceutically acceptable salt thereof - Google Patents

Abstract

Provided in the present invention are: a skin-whitening composition comprising a compound represented by chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient; particularly a cosmetic composition; a pharmaceutical composition; and a health food product. The cosmetic or pharmaceutical composition of the present invention is safe to the human body with reduced side effects, and has excellent effects in whitening the skin or the like.

Description

[0001] Cosmetic or pharmaceutical compositions for skin whitening comprising Astragaloside I or a pharmaceutically acceptable salt thereof,

The present invention relates to a cosmetic composition, a pharmaceutical composition and a health food having an excellent effect on whitening, in particular, an excellent effect relating to the skin. The present invention also relates to a cosmetic composition, a pharmaceutical composition and a health food which can exert such effects even in a small amount.

It is a common desire to have white skin. The color or brightness of the skin is genetically determined by the concentration and distribution of melanin in the human skin, but is also influenced by environmental or physiological conditions such as sun UV, fatigue or stress. Melanin is produced by a nonenzymatic oxidation reaction of tyrosine, which is a kind of amino acid, by the enzyme tyrosinase, which is converted to DOPA and Dopaquinone. The pathway for the formation of melanin is known, but the mechanism by which the melanin synthesis induces tyrosinase is not yet elucidated.

On the other hand, commonly known whitening ingredients include substances inhibiting the activity of tyrosinase enzymes such as kojic acid or arbutin, hydroquinone, vitamin C (L-ascorbic acid) There are plant extracts. By inhibiting the synthesis of melanin pigment, they can brighten the skin tone to realize skin whitening, and it is possible to improve skin hypercholesterolemia such as stain or freckles due to ultraviolet rays, hormones or heredity. However, when applied to skin, there is a problem that the use amount is limited due to safety problems such as irritation and redness, or the effect is insignificant, so that a practical effect can not be expected.

Accordingly, it is urgently required to develop a composition having a skin whitening effect which is safe to the living body, stable in its active ingredient, and more effective than a substance having an effect on existing skin whitening, among other things.

Accordingly, the present invention is to provide such a useful use of a new active ingredient, that is, an active ingredient, which solves the above problems and has few side effects and is safe for human body and has excellent skin whitening effect.

In other words, a problem to be solved by the present invention is to provide a composition comprising the active ingredient having excellent efficacy as an active ingredient.

In order to solve the above problems, the present invention provides a skin whitening composition, preferably a cosmetic composition, a pharmaceutical composition or a health food, comprising Astragaloside I or a pharmaceutically acceptable salt thereof as an active ingredient to provide.

That is, the present invention provides a new use for skin whitening of Astragaloside I or a pharmaceutically acceptable salt thereof.

The inventors of the present invention have confirmed that Astragaloside I inhibits melanin synthesis and exhibits a whitening effect, thereby completing the present invention.

In the present invention, the 'whitening effect' refers to not only brightening the skin tone by inhibiting the synthesis of the melanin pigment but also improving skin hypercholesterolemia due to ultraviolet rays, hormones or heredity, such as spots or freckles.

In order to solve the above-mentioned problems and to achieve the object of the present invention, the present invention provides a composition comprising a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.

[Chemical Formula 1]

The compound represented by the formula (1) has the molecular formula C ₄₃ H ₆₈ O ₁₆ , the molecular weight is 840.99, and Astragaloside I, ASTRAGALOSIDE I (SH); Cyclosiversioside B and so on.

The present invention is not particularly limited to the method for obtaining Astragaloside I, and may be chemically synthesized by a method known in the art, or a commercially available substance may be used.

In the cosmetic composition, the pharmaceutical composition and the health food according to the present invention, the astragaloside I content is preferably 0.00001 to 10% by weight based on the total weight of the cosmetic composition, the pharmaceutical composition and the health food.

"Pharmaceutically acceptable salt" of the present invention preferably includes a base addition salt, wherein the base addition salt includes salts of sodium, potassium, calcium, ammonium, magnesium or organic amino, no.

Astragaloside I of the present invention may exist in solvated as well as unsolvated forms, including forms such as hydrates, ethanolates and the like. Astragaloside I of the present invention may exist in crystalline or amorphous form, and all such physical forms are included within the scope of the present invention.

The cosmetic composition for skin whitening according to the present invention can be used as a skin whitening cosmetic composition in the form of a solution, a ointment for external use, a cream, a foam, a nutrition lotion, a softening water, a pack, But may be formulated as a suspension, emulsion, paste, gel, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation, patch, But is not limited thereto.

In addition, the cosmetic composition of the present invention may further comprise at least one cosmetically acceptable carrier incorporated in a cosmetic composition for general skin, and examples thereof include oil, water, a surfactant, a moisturizer, a lower alcohol, A thickening agent, a chelating agent, a coloring matter, an antiseptic, a perfume, and the like may be appropriately compounded, but the present invention is not limited thereto.

The cosmetically acceptable carrier to be contained in the cosmetic composition of the present invention varies depending on the formulations. When the formulation of the present invention is an ointment, a paste, a cream or a gel, the carrier component may be an animal oil, a vegetable oil, a wax, a paraffin, a starch, a tracer, a cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide Mixtures of these may be used.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder or a mixture thereof may be used as the carrier component, Propellants such as fluorohydrocarbons, propane / butane or dimethyl ether.

When the formulation of the present invention is a solution or an emulsion, a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl benzoate, -Butyl glycol oil, and in particular fatty acid esters of cottonseed oil, peanut oil, corn oil, olive oil, castor oil and sesame oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspension such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Crystalline cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.

When the formulation of the present invention is a soap, alkali metal salts of fatty acids, fatty acid hemiesters, fatty acid protein hydrolizates, isethionates, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugars and the like are used as carrier components .

The present invention also provides a method for skin whitening comprising the step of applying the compound represented by the formula (1) to the skin of an individual. The subject includes, without limitation, mammals including rats, livestock, humans, and the like.

According to another embodiment of the present invention, there is provided a pharmaceutical composition for skin whitening comprising the compound of Chemical Formula 1 as an active ingredient.

The composition comprising the compound of the present invention may be various oral or parenteral formulations, but may preferably be a parenteral agent. In the case of formulation, a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, or a surfactant is usually used. Solid formulations for oral administration include tablets, pills, powders, granules, capsules, and the like, which may contain one or more excipients such as starch, calcium carbonate, sucrose or lactose lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate, talc, and the like are also used. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, and emulsions. Examples of the non-aqueous solvent and the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate.

The present invention can also provide a formulation for external skin preparation for skin whitening effect comprising the compound of Formula 1 as an active ingredient.

When the compound of formula (1) is used as an external preparation for skin, it may further comprise at least one selected from the group consisting of fatty substances, organic solvents, solubilizers, thickeners and gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, , Water, ionic or nonionic emulsifiers, fillers, sequestering agents and chelating agents, preservatives, vitamins, blocking agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or external preparations for skin And any other ingredients used in the skin sciences. The components can also be introduced in amounts commonly used in the field of dermatology.

When the compound of Formula 1 is provided as an external preparation for skin, it may have a formulation such as, but not limited to, ointments, patches, gels, creams or sprays.

The pharmaceutical composition of the present invention is particularly preferably used as a parenteral preparation. For example, the external preparation for skin may be a pharmaceutically acceptable base such as vaseline or stearyl alcohol; Suitable pharmaceutically acceptable surfactants such as polysorbate, sorbitan sesquioleate, and the like; A suitable pharmaceutically acceptable humectant such as glycerin; A suitable pharmaceutically acceptable solvent; And a conventional external preparation for skin preparation in which a flavoring agent, a coloring agent, a stabilizer, a tackifier and the like are homogeneously mixed.

When the compound of Chemical Formula 1 of the present invention is used as a medicine, it may further contain one or more active ingredients showing the same or similar functions. For example, a known skin whitening component may be included. The addition of an additional skin whitening ingredient may further enhance the skin whitening effect of the composition of the present invention. When the above ingredients are added, skin safety, easiness of formulation, and stability of effective ingredients can be considered according to the combined use. In one embodiment of the present invention, the composition is a whitening ingredient known in the art and includes a substance inhibiting tyrosinase enzyme activity such as kojic acid, arbutin, etc., hydroquinone, vitamin C (L-Ascorbic acid); And derivatives thereof, and various plant extracts. ≪ Desc / Clms Page number 2 > The additional component may be included in an amount of 0.0001 to 10% by weight based on the total weight of the composition, and the content range may be adjusted according to requirements such as skin safety, ease of formulation of the compound of Formula 1 .

The pharmaceutical composition of the present invention can provide a desired skin whitening effect when an effective amount of the compound of Formula 1 is included. In the present invention, the term "effective amount" means the amount of a compound capable of exhibiting a skin whitening effect.

An effective amount of the compound of formula (1) contained in the composition of the present invention will vary depending on the form in which the composition is commercialized, how the compound is applied to the skin, and the time on the skin. For example, when the composition is commercialized as a pharmaceutical product, the compound of Formula 1 may be contained at a higher concentration than that of a cosmetic product that is routinely applied to skin. Accordingly, the daily dosage is 0.1 to 100 mg / kg, preferably 30 to 80 mg / kg, more preferably 50 to 60 mg / kg, based on the amount of the compound of formula (1) 6 times a day.

According to another embodiment of the present invention, there is provided a health food for skin whitening effect comprising the compound of formula (1).

The term 'health food' as used herein means a food prepared by adding the compound of formula (1) to food materials such as beverage, tea, spice, gum and confectionery, or by encapsulation, powdering or suspension, But it has the advantage that there are no side effects that can occur when a drug is used for a long period of time using a food as a raw material. Since the health food of the present invention thus obtained can be ingested on a daily basis, a high skin whitening effect can be expected, which is very useful.

When the compound of Chemical Formula 1 is used as a food additive, the compound of Chemical Formula 1 may be added as it is or may be used together with other food or food ingredients, and may be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be suitably determined according to its intended use (prevention, health or therapeutic treatment). Generally, the composition of the present invention is added in an amount of not more than 15 parts by weight, preferably not more than 10 parts by weight, based on the raw material, when the food or beverage is produced. However, in the case of long-term consumption intended for health and hygiene purposes or for health control purposes, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount exceeding the above range . There is no particular limitation on the kind of the food. Examples of the food to which the above substance can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, Alcoholic beverages, and vitamin complexes, all of which include healthy foods in a conventional sense. The health beverage composition of the present invention may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. Such natural carbohydrates are monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, and polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol and erythritol. Examples of sweeteners include natural sweeteners such as tau martin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 mL of the composition of the present invention. In addition to the above, the health food of the present invention may contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acids and salts thereof, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, , A carbonating agent used in carbonated drinks, and the like. In addition, the health food of the present invention may contain flesh for the production of natural fruit juice, fruit juice drink and vegetable drink. These components may be used independently or in combination. The proportion of such additives is not critical, but is generally selected in the range of 0.01 to 0.1 parts by weight per 100 parts by weight of the composition of the present invention.

In one embodiment of the present invention, the composition may contain 0.00001 wt% to 10 wt% of the compound of Formula 1 based on the weight of the entire composition.

Compositions containing Astragaloside I of the present invention or a pharmaceutically acceptable salt thereof exhibit skin whitening effects.

The composition containing Astragaloside I of the present invention or a pharmaceutically acceptable salt thereof can be used as safe and excellent cosmetic ingredients and pharmaceutical ingredients.

Hereinafter, the present invention will be described in more detail with reference to the following examples. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the embodiments described below. The embodiments of the present invention are provided by way of example to facilitate a specific understanding of the present invention.

Reference Example  One: Astragalos seed  I ( Astragaloside  I) Material information

[Chemical Formula 1]

Material name: Astragaloside I

CAS No. : 84680-75-1

Molecular formula: C ₄₃ H ₆₈ O ₁₆

Molecular weight: 840.99

Where to buy: Tauto Biotech (China)

Example  1: whitening effect - melanin total amount reduction effect

The compound of Chemical Formula 1 was added to the culture solution of mouse melanoma cells (B-16 mouse) to determine the whitening effect by measuring the total amount of melanin at the cellular level (Lotan R., Lotan D. Cancer Res . 40: 3345-3350, 1980). To evaluate the toxicity of melanoma cells in rats before the experiment, whitening evaluation was performed by selecting a concentration that is not toxic.

The compound of the formula (1) was added to the culture medium to give final concentrations of 1 ppm and 10 ppm, and the control group, arbutin, was added to the medium so as to be treated with B-16 melanoma cells and cultured for 3 days.

Cells were then trypsinized, detached from the culture, centrifuged, and then melanin was extracted. The removed cells were incubated with 1 ml of sodium hydroxide solution (1N concentration), boiled for 10 minutes to dissolve melanin, and the absorbance was measured at 400 nm using a spectrophotometer to measure the amount of melanin produced.

The amount of melanin was measured by an absorbance of 1 × 10 ⁶ cells per unit cell, and the total amount of melanin relative to the control group was calculated as inhibition (%). The results are summarized in Table 1.

Reduction of total melanin levels at the cellular level by concentration

sample Melanin production
(abs) Inhibition rate (%) Control group (DMSO, 10 ppm) 0.33 - Positive control (arbutin, 100 ppm) 0.228 31.06 The compound of formula (1) (10 ppm) 0.213 35.35 The compound of formula (1) (1 ppm) 0.279 15.46

As can be seen from the results of the above Table 2, the compound of the formula (I) has a better inhibition of melanin formation even when a smaller concentration is applied to cultured rat melanoma cells as compared with arbutin known as a whitening substance , Indicating less total melanin content.

Therefore, it was found that the compound of formula (1) can be used for whitening purposes.

Claims (3)

A composition for skin whitening comprising a compound represented by the following formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient.
[Chemical Formula 1]

The composition according to claim 1, wherein the composition is used as a cosmetic composition, a pharmaceutical composition or a health food. The composition according to claim 1 or 2, wherein the compound represented by Formula 1 or a pharmaceutically acceptable salt thereof is contained in an amount of 0.00001 to 10% by weight based on the total weight of the composition.