JP2009242311A - Scf secretion inhibitor and skin care preparation for external use for making skin pore inconspicuous - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a novel agent for inhibiting secretion of a stem cell factor (SCF) from a fibroblast, and a skin care preparation for external use for making skin pores inconspicuous. <P>SOLUTION: The secretion inhibitor of the stem cell factor (SCF) from the fibroblast comprises as an effective ingredient an extract of a seed of Linum usitatissimum L. The skin care preparation for external use for making skin pores inconspicuous comprises as an effective ingredient an extract of a seed of Linum usitatissimum L. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to an agent for suppressing secretion of stem cell factor (SCF) from fibroblasts, and a skin external preparation for reducing the appearance of pores.

  The conspicuousness of pores is always listed as the top of women's skin problems. The structure of the conspicuous pores is that the pores (funnels) are not widened, but the periphery of the pores is depressed like a mortar, and that part is conspicuous as a shadow. One of the causes of such a pore structure is the keratinization of horny layer cells around the pores. In prominent pores, the amount of sebum secretion increases, and the unsaturated fatty acids in sebum, as well as the unsaturated fatty acids produced by the degradation of triacylglycerol and acylglycerol in sebum by lipase, cause inflammation, resulting in keratin. It is known to cause oxidization (Non-patent Document 1).

  On the other hand, it has been said that stress and pore conspicuity are related to each other. It is known that a neuropeptide called substance P (hereinafter abbreviated as SP) is released from nerve terminals due to stress, thereby increasing sebaceous glands and promoting sebum secretion (Non-patent Document 2). In addition, when this SP acts on dermal fibroblasts, the fibroblasts secrete SCF (stem cell factor) and activate mast cells, and then activate interleukin-6 (hereinafter referred to as activated mast cells). It is also revealed that IL-6 is abbreviated) and sebaceous glands are enlarged to promote sebum secretion (Non-patent Documents 3 and 4). Therefore, if SCF secretion can be suppressed in the presence of SP, enlargement of the sebaceous glands can be suppressed, and excessive sebum secretion can be suppressed, thereby reducing the conspicuous pores. Is done.

On the other hand, since an external preparation for skin is directly applied to the skin, high safety is required for a medicinal agent used as an active ingredient. Therefore, conventionally, the medicinal effects of various plant extracts have been studied. For example, it is known that an extract of flaxseed has a melanin production inhibitory effect (Patent Literature 1) and an extract of flax has an inhibitory effect on microbial lipase (Patent Literature 2). However, the secretory inhibitory action on SCF involved in the sebum secretion has not been known so far.
JP 2001-261570 A Japanese Patent No. 4404274 Fragrance Journal, March 2004, pages 41-47 Welfare Science Research Grant (Research Project on Sensory Organ Disorders, Immunity, Allergies, etc.) Report 218-220 Dermatology, 206 (1), 17-23 (2003) European Journal of Dermatology, 12 (5), 422-427 (2002)

An object of the present invention is to provide an agent for suppressing secretion of stem cell factor (SCF) from fibroblasts, which has good safety.
Moreover, this invention makes it a subject to provide the skin external preparation which reduces the conspicuousness of a pore by suppressing the secretion of excess sebum.

As a result of various studies to solve the above problems, the present inventor can suppress the secretion of SCF from fibroblasts promoted by the action of substance P (SP) by the presence of flaxseed extract. As a result, further studies were made based on this finding, and the present invention was completed.
That is, in order to solve the said subject, this invention provides the stem cell factor (SCF) secretion inhibitor from the fibroblast which uses the extract of the seed of a flax (Linum usitatissimum L.) as an active ingredient.
From another point of view, according to the present invention, there is provided a skin external preparation for reducing pore conspicuousness containing an extract of flax (Linum usitatissimum L.) seeds as an active ingredient.

ADVANTAGE OF THE INVENTION According to this invention, the stem cell factor (SCF) secretion inhibitor from a fibroblast which has favorable safety | security can be provided.
In addition, according to the present invention, it is possible to provide a novel external preparation for skin that suppresses the secretion of excessive sebum by suppressing the secretion of SCF from fibroblasts, thereby reducing the conspicuousness of pores. it can.

Hereinafter, the present invention will be described in detail. In the present specification, “to” means a range including numerical values before and after.
The present invention relates to an agent for inhibiting SCF secretion from fibroblasts, which contains an extract of flax (Linum usitatissimum L.) seeds as an active ingredient. Flax is a plant belonging to the genus flaxaceae and is native to Central Asia, but is an annual plant grown in Japan, China, the Korean Peninsula, the United States, Canada, Russia, Belgium, and other countries. Linseed oil obtained from seeds is a dry fatty oil and is used in industrial supplies such as oil paints and printing inks, as well as pharmaceutical supplies such as soaps and ointments.

  The flaxseed extract used in the present invention is preferably a water-soluble extract. Therefore, the flaxseed extract used in the present invention is preferably an extract extracted with an aqueous solvent. Examples of the aqueous solvent include water and a mixed solvent of water and a hydrophilic organic solvent. Examples of the hydrophilic solvent include, but are not limited to, lower monohydric alcohols such as methyl alcohol and ethyl alcohol; and liquid polyhydric alcohols such as glycerin, propylene glycol, and 1,3-butylene glycol. It is not something. Extraction can be performed by immersing flax seeds in a solvent for a predetermined time at room temperature or under heating. Moreover, pre-treatment such as drying, chopping, pressing or fermentation can be performed on the seed before extraction.

  The flaxseed extract can be used directly as the medicinal agent after preparation. Further, if desired, it can be left as it is for an appropriate period of time for aging and then used as the medicinal agent. If necessary, it can be used after being subjected to a purification treatment such as deodorization and decolorization by filtration or ion exchange resin within a range that does not affect the effect of the present invention. Further, a fraction having high activity can be taken out and used by using a separation means such as liquid chromatography.

  The flaxseed extract may be in any form such as liquid, paste or gel. The liquid extract containing the extraction solvent can also be used after it is solidified by drying under reduced pressure or freeze drying. It can also be dried by spray drying or the like and used as a powder.

  The extract of flaxseed has the effect of suppressing the secretion of stem cell factor (SCF) from dermal fibroblasts by the action of substance P (SP). SCF is known to activate mast cells, but activated mast cells secrete interleukin-6 (IL-6), which activates sebaceous glands to hypertrophy. Contributes to excessive sebum secretion. Since the extract of flax seed has the above-mentioned action, even if SP is secreted from nerve cells due to factors such as stress, the flax blast cells are applied by applying the flax seed extract to the skin and present it in the dermis. SCF can be suppressed from being secreted from the body. As a result, pore conspicuousness caused by excessive secretion of sebum can be reduced.

  The present invention also relates to a skin external preparation for reducing the appearance of pores, which contains an extract of flaxseed as an active ingredient. The content of the extract of flaxseed in the skin external preparation of the present invention is preferably 0.0001 to 20% by mass (hereinafter simply referred to as “%”) as a solid content, and more preferably 0.001 to 10%. If it exists in this range, the said extract can be mix | blended stably and the high reduction effect with respect to conspicuous pores can be exhibited.

  The external preparation for skin of the present invention can be prepared by blending the extract of flaxseed with various forms of bases according to a conventional method. Furthermore, by blending the extract in combination with one or more other medicinal agents, it is possible to prepare a topical skin preparation that further enhances the medicinal properties or exhibits other medicinal properties along with the medicinal properties. Examples of other medicinal agents include whitening agents, UV protection agents, antibacterial agents, bactericides, sebum secretion regulators, anti-inflammatory agents, cell activators, active oxygen scavengers, and moisturizers. It is not limited to.

  Examples of whitening agents include ascorbic acid or derivatives thereof, arbutin, ellagic acid, linoleic acid, vitamin E and derivatives thereof, glycyrrhizic acid and derivatives thereof, tranexamic acid, placenta extract, chamomile extract, seaweed extract, coconut extract , Gokahi extract, Rice bran extract, Wheat germ extract, Saisin extract, Hawthorn extract, Sunpens extract, Shirayuri extract, Peonies extract, Sempukuka extract, Soy extract, Tea extract, Molasses extract , Beechlen extract, grape extract, micaika extract, mokka extract, saxifrage extract and the like.

  Examples of the UV protection agent include paramethoxycinnamate-2-ethylhexyl, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxybenzophenone-5 sodium sulfate, 4-t-butyl-4′- Examples thereof include methoxydibenzoylmethane, 2-phenyl-benzimidazole-5-sulfuric acid, titanium oxide, and zinc oxide.

  Examples of the antibacterial agent include benzoic acid, sodium benzoate, paraoxybenzoic acid ester, phenoxyethanol, and the like.

  Examples of the disinfectant include salicylic acid, benzalkonium chloride, isopropylmethylphenol, hinokitiol, sulfur and derivatives thereof, eucalyptus extract, clove extract, and dokudami extract.

  Examples of the sebum secretion regulator include, for example, Citrus extract, Licorice extract, Age extract, Ogon extract, Oat extract, Kudin extract, Hops extract, Watercress extract, Pyridoxine and its derivatives, Auren extract, An example of the extract is an extract of pearl millet, mint extract, mugwort extract and the like.

  Anti-inflammatory agents include, for example, glycyrrhizic acid and its derivatives, glycyrrhetinic acid and its derivatives, artea extract, ashitaba extract, arnica extract, ginseng extract, nettle extract, buckwheat extract, hypericum extract, chamomile extract Products, goldfish extract, comfrey extract, salvia extract, sicon extract, perilla extract, birch extract, gentian extract and the like.

  Examples of cell activators include caffeine, chicken crown extract, shell extract, shell extract, royal jelly, silk protein and its degradation products or derivatives thereof, lactoferrin or degradation products thereof, chondroitin sulfate, hyaluronic acid, etc. Mucopolysaccharides or their salts, collagen, yeast extract, lactic acid bacteria extract, bifidobacteria extract, fermentation metabolic extract, ginkgo biloba extract, barley extract, assembly extract, peanut extract, carrot extract, rosemary Extracts, glycolic acid, citric acid, lactic acid, malic acid, tartaric acid, succinic acid and the like are included.

  The active oxygen scavenger has an action such as suppression of lipid peroxide production. For example, superoxide dismutase, mannitol, quercetin, catechin and derivatives thereof, rutin and derivatives thereof, button pi extract, yashajitsu extract, melissa extract , Rakan fruit extract, retinol and its derivatives, vitamin A such as carotenoid, thiamine and its derivative, riboflavin and its derivative, vitamin B such as nicotinic acid and its derivative, vitamin E such as tocopherol and its derivative, dibutyl Examples include hydroxytoluene and butylhydroxyanisole.

  Examples of the humectant include proteins such as elastin and keratin or derivatives thereof, hydrolysates and salts thereof, amino acids such as glycine, serine, aspartic acid, glutamic acid, arginine and theanine and derivatives thereof, sorbitol, erythritol, Trehalose, inositol, glucose, sucrose and derivatives thereof, dextrin and derivatives thereof, saccharides such as honey, D-panthenol and derivatives thereof, urea, phospholipid, ceramide, ginger extract, ginger extract, gypsum extract Products, dokudami extract, hamamelis extract, bodaige extract, maronier extract, quince extract and the like.

  Moreover, arbitrary ingredients other than the medicinal agent of this invention can be mix | blended with the skin external preparation of this invention. Examples of such components include, but are not limited to, physiologically active substances such as amino acids, lipids, sugars, hormones, enzymes, and nucleic acids. In addition, components that are usually used in the production of cosmetics, quasi-drugs, skin external preparations and the like, for example, water (purified water, hot spring water, deep water, etc.), oil agents, Surfactant, metal soap, gelling agent, powder, alcohol, water-soluble polymer, film-forming agent, resin, inclusion compound, fragrance, deodorant, salt, pH adjuster, refreshing agent, plant / animal -Extracts derived from microorganisms, blood circulation promoters, astringents, antiseborrheic agents, chelating agents, keratolytic agents, enzymes, hormones, other vitamins and the like can be used as necessary.

  The external preparation for skin of the present invention has various forms such as powders such as powder and powder foundation; solids such as soap and lipstick; emulsions such as cream, emulsion and cream foundation; It is preferable that it is a cosmetic composition. However, it is not limited to these.

  EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples. However, the scope of the present invention is not limited to the following examples.

[Example 1: Preparation of flaxseed extract]
After crushing 100 g of flax seed, 1.5 L of purified water was added and extraction was performed at room temperature for 7 days, followed by filtration to obtain 1 l of flax seed extract (dry solid content 5.9 in the extract). %).

[Example 2: SCF secretion inhibitory action test from fibroblasts]
Human-derived dermal fibroblasts were seeded in a 12-well plate at 70000 cells per well, and placed in a 5% CO ₂ incubator. One day later, the flaxseed extract prepared in Example 1 was added at a concentration of 1 (v / v)%, and substance P was added at a concentration of 10 ng / mL, and left again in the incubator. Two days later, the cells were collected to obtain a crude protein extract. Then, about this protein crude extract, SCF production amount was calculated | required by ELISA. In addition, the amount of SCF was determined in the same manner for a sample group to which only substance P was added at the same concentration as above and to which no flaxseed extract was added. The results are shown in the table below. In the following table, the amount of SCF produced in the sample group to which neither substance P nor flaxseed extract was added was defined as 100%, and the ratio relative thereto was shown.

  From the results shown in the above table, when only substance P is allowed to act on fibroblasts, the secretion of SCF is promoted and the amount of SCF production increases, but in the presence of substance P by adding flax seed extract. It can be understood that the secretion of SCF from the fibroblasts is suppressed and the amount of SCF production can be significantly reduced.

[Example 3: Evaluation of pore-reducing effect]
(Preparation of lotion)
A lotion having the following composition was prepared by the following method.
(Prescription) (%)
(1) Glycerin 5.0
(2) 1,3-butylene glycol 6.5
(3) Polyoxyethylene (20E.O.)
Sorbitan monolaurate ester 1.2
(4) Ethyl alcohol 8.0
(5) Flax seed extract * 1 4.0
(6) Preservative appropriate amount (7) Purified water remaining amount * 1 Prepared in Example 1 (Production method)
A. (3), (4) and (6) are mixed and dissolved.
B. (1), (2), (5) and (7) are mixed and dissolved.
C. A and B were mixed and uniformed to obtain a skin lotion.

  Further, a lotion for comparative example was prepared in the same manner except that the flaxseed extract was not mixed.

(Evaluation of lotion)
For 7 panelists who are concerned about the conspicuous pores, the makeup for the comparative example in which the above-prepared flax seed extract is blended on one of the left and right cheeks and the flax seed extract is not blended on the other Water was applied twice a day for 4 weeks. The degree of conspicuous pores in the left and right cheeks was determined by the following four-stage visual evaluation, and the average of all the panels was determined.
(Evaluation criteria)
1: Pore is not conspicuous 2: Pore is conspicuous 3: Pore is conspicuous 4: Pore is conspicuous

(Evaluation results)
The average value of the lotion of the Example which mix | blended the extract of flaxseed was 3.375 points before use, and was 2.625 points after use. On the other hand, the average value of the skin lotion of the comparative example was 3.375 points before use and 3.375 points after use. From this result, the extract of flaxseed does not lose its efficacy even if it is blended with a topical skin preparation such as lotion, and contributes to the suppression of sebum excess secretion by being applied to the skin. It can be understood that it has the effect of reducing the conspicuousness.

[Example 4: Latex]
(Prescription) (%)
(1) Polyoxyethylene (10E.O.) sorbitan monostearate 1.0
(2) Polyoxyethylene (60E.O.) sorbite tetraoleate 0.5
(3) Glyceryl monostearate 1.0
(4) Stearic acid 0.5
(5) Behenyl alcohol 0.5
(6) Squalane 5.0
(7) Preservative 0.1
(8) Carboxyvinyl polymer 0.1
(9) Sodium hydroxide 0.05
(10) Ethyl alcohol 5.0
(11) Purified water remaining amount (12) Flax seed extract * 1 1.0
(13) Stearyl glycyrrhetinate * 2 0.1
(14) Hop extract * 3 0.2
(15) Ages extract * 4 1.0
(16) Fragrance Appropriate amount * 1 Prepared in Example 1 * 2 Made by Maruzen Pharmaceutical * 3 Made by Maruzen Pharmaceutical * 4 Made by Maruzen Pharmaceutical

(Manufacturing method)
A. Ingredients (1) to (7) and (13) are heated and mixed and maintained at 70 ° C.
B. A part of components (9) and (11) are heated and mixed and kept at 70 ° C.
C. A is added to B, mixed and uniformly emulsified.
D. After cooling C, (12), (14), (15) and (8), (10), (16) dissolved in the remainder of (11) were added and mixed uniformly to obtain an emulsion.

[Example 5: Cream]
(Prescription) (%)
(1) Beeswaw 6.0
(2) Cetanol 5.0
(3) Reduced lanolin 5.0
(4) Squalane 30.0
(5) Lipophilic glyceryl monostearate 4.0
(6) Polyoxyethylene sorbitan monolaurate (20E.O) 2.0
(7) Flax seed extract * 1 0.5
(8) Artemisia extract * 2 0.5
(9) Daylily extract * 3 0.5
(10) mint extract * 4 0.5
(11) Preservative Appropriate amount (12) Fragrance Appropriate amount (13) Purified water Remaining amount * 1 Prepared in Reference Example 1 * 2 Made by Maruzen Pharmaceutical * 3 Made by Maruzen Pharmaceutical * 4 Made by SILAB (production method)
A. Ingredients (1)-(6) and (11) are mixed and heated to keep at 70 ° C.
B. A portion of component (13) is heated and maintained at 70 ° C.
C. B was added to A, (7) to (10) and (12) dissolved in the remainder of (13) were mixed, and then cooled to obtain a cream.

[Example 6: Gel ointment]
(Prescription) (%)
(1) Carboxyvinyl polymer 1.0
(2) Triethanolamine 1.0
(3) 1,3 butylene glycol 10.0
(4) Flax seed extract * 1 2.0
(5) Pyridoxine hydrochloride * 2 0.1
(6) Citrus extract * 3 0.3
(7) Tachi musk extract * 4 0.3
(8) Eucalyptus extract * 5 0.3
(9) Watercress extract * 6 0.3
(10) Purified water remaining * 1 Manufactured in Reference Example 1 * 2 Sigma * 3 SILAB * 4 Maruzen * 5 Maruzen * 6 Maruzen

(Manufacturing method)
A. Components (1) and (3) to (10) are mixed and dissolved.
B. Ingredient (2) was added to A and mixed to obtain a gel ointment.

  Examples 4 to 6 were external preparations for skin that alleviated the conspicuousness of pores by being continuously applied to the skin.

Claims (2)

An inhibitor of stem cell factor (SCF) secretion from fibroblasts, which contains an extract of flax (Linum usitatissimum L.) seeds as an active ingredient. Skin external preparation for reducing conspicuous pores, containing an extract of flax (Linum usitatissimum L.) seeds as an active ingredient.