KR20130130421A - Compositions containing a trans-communic acid for anti-aging - Google Patents

Abstract

The present invention relates to a composition for anti-aging containing trans-communic acid as an effective component which has an excellent skin cell and collagen biosynthesis promotion effect without causing side effects on the skin, and is capable of being applied to a skin external application for anti-aging and wrinkle prevention. The composition for anti-aging contains 0.001-10 wt% of trans-communic acid.

Description

Anti-aging composition containing transcumnic acid as an active ingredient {COMPOSITIONS CONTAINING A TRANS-COMMUNIC ACID FOR ANTI-AGING}

The present invention relates to an anti-aging composition containing a transcumnic acid as an active ingredient.

Skin is the body's primary protective film that protects organs in the body from changes in temperature and humidity, irritation from the external environment such as UV and pollutants, and plays an important role in maintaining homeostasis such as body temperature control. However, excessive physical and chemical stimuli, stress, and malnutrition from the outside will degrade the normal function of the skin and promote skin aging such as loss of elasticity, keratinization, and wrinkle formation. In order to maintain the skin, there have been efforts to effectively suppress skin aging by maintaining skin's intrinsic function and activating skin cells by using cosmetics which have been strengthened with conventional bioactive substances obtained from various plants and microorganisms. However, existing cosmetic raw materials have various problems such as insufficient efficacy or skin side effects.

It is an object of the present invention to provide a composition for preventing skin aging, which is excellent in promoting skin cell and collagen production without causing skin side effects by containing a transcumnic acid as an active ingredient.

One embodiment of the present invention to solve the above object provides an anti-aging composition containing a transcumnic acid represented by the following formula (1), an isomer thereof, a precursor thereof, a salt thereof, a hydrate thereof or a solvate thereof as an active ingredient. do.

Said "isomers" include in particular optical isomers, form isomers, positional isomers (particularly tautomers) or geometric isomers.

The "precursor" means a chemical change of a compound to control physical and chemical properties, and itself does not exhibit physiological activity, but after administration, the compound is changed to the original compound by the action of a chemical or an enzyme to exert its effect. Can be.

The term " pharmaceutically acceptable "as used herein refers to salts which are generally safe, non-toxic, and which are useful for preparing biologically or otherwise preferred pharmaceutical compositions, But also for pharmacological use in humans.

The term "pharmaceutically acceptable salts" refers to salts that are pharmaceutically acceptable and have the desired pharmacological activity as defined above. Such salts include (1) inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like, or organic acids such as acetic acid, propionic acid, hexanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, stone Sinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3- (4-hydroxybenzoyl) benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, 4-methylbicyclo [2.2.2] -oct-2- Formed by en-1-carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, tertiary butylacetic acid, lauryl sulfuric acid, gluconic acid, glutamic acid, hydroxynaphric acid, salicylic acid, stearic acid, muconic acid and the like Acid addition salts; Or (2) salts formed when the acidic protons present in the parent compound are replaced.

The term “hydrate” means “pharmaceutically acceptable hydrate”. The "hydrate" is present when the compound of the present invention contains water. Hydrates may contain one or more water molecules per molecule of the compounds of the invention. Exemplary non-limiting examples include monohydrates, dihydrates, trihydrates, and tetrahydrates. Hydrates may contain one or more compound molecules of the invention per one water molecule. Exemplary non-limiting examples include semihydrates. In one embodiment, water may be retained in the crystal in a variety of ways such that water molecules may occupy lattice positions within the crystal, or may form bonds with salts of the compounds described above. A luggage must be "acceptable" in the sense that it is not harmful to its reception.

The term "solvate" means "pharmaceutically acceptable solvate," and "solvate" means that the compound of the present invention contains one or more pharmaceutically acceptable solvents. It may contain one or more solvent molecules per molecule of the compound of the invention, or may contain one molecule of compound of the invention per molecule of solvent. Can be retained within the crystals, thus water molecules can occupy lattice positions in the crystals or form bonds with salts of the compounds described above.

The transcumnic acid may be represented by the following [Formula 1].

In one embodiment of the present invention, the content of transcumnic acid may be 0.0001 to 10% by weight based on the total weight of the composition.

In one embodiment of the present invention, the anti-aging composition may have a use of skin wrinkle improvement.

In one embodiment of the present invention, the anti-aging composition may have a use of skin elasticity promotion.

In one embodiment of the present invention, the anti-aging composition may be to prevent aging through the proliferation of skin cells or fibroblasts.

In one embodiment of the present invention, the anti-aging composition may be to prevent aging through promoting collagen biosynthesis.

The anti-aging composition containing the transcumnic acid of the present invention as an active ingredient is excellent in promoting skin cell and collagen biosynthesis without causing skin side effects. Due to this effect, it can be usefully applied to external skin preparations for the purpose of anti-aging and wrinkle improvement.

Hereinafter, preferred embodiments of the present invention will be described in detail in order to facilitate the present invention by those skilled in the art.

The present invention provides an anti-aging composition containing a transcumnic acid as an active ingredient.

The transcumnic acid content may be 0.0001 to 10% by weight based on the total weight of the composition. When the content is less than 0.0001% by weight, the efficacy is weak, and when it exceeds 10% by weight, there is no apparent increase in efficacy due to the increase in content, which is not economical.

The anti-aging composition containing a transcumnic acid according to the present invention as an active ingredient may be, for example, a pharmaceutical composition or a cosmetic composition.

The anti-aging pharmaceutical composition may further contain pharmaceutical supplements such as preservatives, stabilizers, hydrating or emulsifiers, salts and / or buffers for the control of osmotic pressure and other therapeutically useful substances, according to conventional methods. It can be formulated in a variety of parenteral dosage forms. Parenteral dosage forms, and may be, for example, but not limited to lotions, ointments, gels, creams, patches or spray formulations.

Determination of the dosage of the active ingredient is within the level of those skilled in the art, and the daily dosage of the drug depends on various factors such as less progression, onset, age, health condition, complications, etc. of the subject to be administered. Generally, the composition may be administered by dividing 1 μg / kg to 200 mg / kg, preferably 50 μg / kg to 50 mg / kg, once or three times a day, and the dosage may be determined by any method. Nor does it limit the scope of the invention.

The anti-aging cosmetic composition is not particularly limited in formulation, and may be appropriately selected as desired. For example, skin lotion, skin softener, skin toner, astringent, lotion, milky lotion, moisturizing lotion, nutrition lotion, massage cream, nutritional cream, moisturizing cream, hand cream, foundation, essence, nutrition essence, pack, soap, cleansing But the present invention is not limited thereto, and may be manufactured by any one or more formulations selected from the group consisting of a foam, a cleansing lotion, a cleansing cream, a body lotion and a body cleanser.

When the formulation of the present invention is a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, and especially in the case of spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

In the case of the solution or emulsion of the present invention, a solvent, a solvent or an emulsifier is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

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 suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.

When the formulation of the present invention is an interfacial active agent-containing cleansing, the carrier component may include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolenic derivatives or ethoxylated glycerol fatty acid esters.

The cosmetic composition may further include a functional additive and components included in a general cosmetic composition, in addition to the added transcumnic acid. The functional additives may include water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymeric polysaccharides, sphingolipids and seaweed extracts.

In addition to the said functional additive, you may mix | blend the component contained in a general cosmetic composition with the cosmetic composition of this invention as needed. In addition to the other components included, oils and fats, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, blood circulation And accelerators, cooling agents, limiting agents, purified water, and the like.

Furthermore, the present invention relates to an external preparation for skin comprising the anti-aging composition, and the external preparation for skin is a generic term that can include anything applied outside of the skin, and cosmetics and medicines of various formulations can be included therein. The external preparation for the skin is also not particularly limited, but may be, for example, an external preparation for preventing skin aging or improving skin wrinkles.

The present invention has found excellent skin anti-aging effects using compositions containing transcumnic acid. The anti-aging composition according to the present invention can improve skin wrinkles by having a function of promoting skin cell and collagen biosynthesis, as can be seen in the test examples described later.

The present invention is described in more detail through the following implementation. However, the examples are provided to illustrate the present invention, and the scope of the present invention is not limited only to these examples.

Test Example 1 Cell Proliferation Effect

Wrinkle improvement effect measurement test of the transcumnic acid of Chemical Formula 1 purchased from Nanjing Elegant Nutraceuticals. In order to see skin cell proliferation effect as wrinkle improvement effect, human normal fibroblasts were inoculated to be 1 × 10 ⁴ cells in each well of a 96-well microplate. Incubated for 24 hours in DMEM (Dulbecco's Modified Eagle's Medium) medium. After incubation, transcumnic acid was adjusted to a final concentration of 10 μM and replaced with DM medium without serum, followed by further incubation for 24 hours. 3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium (MTT: (3- (4,5-dimdimeth-thiazol-2-yl) 2,5-diphenyl tetrazolium: 5 mg / ml) was added 10 µl and left for 4 hours, after which the media portion was discarded, and 100 µl of dimethyl sulfoxide solution was added to each well, and the absorbance was measured at 570 nm using a microplate reader.

By performing the test of the above procedure to obtain the cell proliferation effect from the following equation 1 shown in Table 1 below.

Wrinkle improvement effect Transcumnic acid concentration (μM) Absorbance (570nm) Cell proliferation effect (%) 0 (control group) 0.300 - 10 0.530 76.6

As shown in Table 1, the transcumnic acid was found to exhibit the cell proliferation effect of normal fibroblasts.

Test Example 2 Collagen Biosynthesis Promoting Effect

The collagen biosynthesis promoting effect measurement test of the transcumnic acid of Chemical Formula 1 purchased from Nanjing Elegant Nutraceuticals was conducted. In order to investigate the effect of promoting collagen biosynthesis as a wrinkle improving effect, human normal fibroblasts were inoculated to be 1 × 10 ⁴ cells in each well of a 96-well microplate. Incubate for 24 hours in DMEM: Dulbecco's Modified Eagle's Medium. After incubation, transcumnic acid is replaced with DM medium without serum adjusted to a final concentration of 10 μM, followed by further incubation for 48 hours. 50 μg / ml of ascorbic acid is added to promote collagen synthesis 24 hours before the last 24 hours of culture. After incubation, each well is washed, replaced with DM medium without serum, and incubated for another 24 hours. After incubation, the supernatant of each well was collected, and the amount of newly synthesized collagen was measured by PICP amount using a kit (Kit, Takara, Kyoto, Japan). The PICP amount is shown in Table 2 below to express collagen in terms of ng / 2 × 10 ⁴ cells.

Collagen biosynthesis promoting effect Transcumnic acid concentration (μM) Collagen Synthesis Amount (ng / 2 × 10 ⁴ ) 0 (control group) 130 10 240

As shown in Table 2, the amount of collagen synthesis was increased by transcumnic acid compared to the control group, and thus, transcumonic acid was found to have an effect of promoting collagen biosynthesis.

Although the formulation example of the composition containing the transcumnic acid of this invention as an active ingredient is demonstrated below, the composition of this invention is not limited only to this example.

Formulation Example 1 Lotion Formulation

ingredient Content (% by weight) Transcumnic acid 3.00 L-ascorbic acid-2-phosphate magnesium salt 1.00 Water soluble collagen (1% aqueous solution) 1.00 Sodium citrate 0.10 Citric acid 0.05 Licorice Extract 0.20 1,3-butylene glycol 3.00 Purified water Balance system 100

Formulation Example 2 Cream-Type Formulation

ingredient Content (% by weight) Transcumnic acid 1.00 Polyethylene Glycol Monostearate 2.00 Self emulsifying monostearic acid glycerin 5.00 Cetyl alcohol 4.00 Squalene 6.00 Tri-2-ethylhexane glyceryl 6.00 Sphingolipid 1.00 1,3-butylene glycol 7.00 Purified water Balance system 100

[Formulation Example 3] Packed preparation

ingredient Content (% by weight) Transcumnic acid 5.00 Polyvinyl alcohol 13.00 L-ascorbic acid-2-phosphate magnesium salt 1.00 Lauroylhydroxyproline 1.00 Water soluble collagen (1% aqueous solution) 2.00 1,3-butylene glycol 3.00 ethanol 5.00 Purified water Balance system 100

Formulation Example 4 Cosmetic Liquid Formulation

ingredient Content (% by weight) Transcumnic acid 2.00 Hydroxyethylene Cellulose (2% aqueous solution) 12.00 Xanthan gum (2% aqueous solution) 2.00 1,3-butylene glycol 6.00 Concentrated glycerin 4.00 Sodium hyaluronate (1% aqueous solution) 5.00 Purified water Balance system 100

Claims (6)

An anti-aging composition containing a transcumnic acid as an active ingredient. The method of claim 1,
The transcumnic acid content is 0.0001 to 10% by weight based on the total weight of the composition. The method of claim 1,
The anti-aging composition is an anti-aging composition, characterized in that it has the use of skin wrinkle improvement. The method of claim 1,
The anti-aging composition is an anti-aging composition, characterized in that it has a use of skin elasticity enhancement. The method of claim 1,
The anti-aging composition is an anti-aging composition, characterized in that to prevent aging through the proliferation of skin cells or fibroblasts. The method of claim 1,
The anti-aging composition is an anti-aging composition, characterized in that to prevent aging through promoting collagen biosynthesis.