JP2006062990A - Restoration agent for ultraviolet damage to cell - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide new uses using extracts of a plant belonging to the Genus Ageratum, whose effect other than that on hair growth, or the like, is not found conventionally. <P>SOLUTION: The extracts of the plant belonging to the Genus Ageratum restore ultraviolet damage to epidermal keratinized cells. Several cutaneous aging symptoms such as wrinkles, skin roughening and skin somberness are found to be improved by compounding the extracts, with one or more of specific agents of humectants, cell activators, antiphlogistics, antioxidants, skin whitening agents, hyaluronidase inhibitors, antiplasmin agents, active oxygen-suppressing agents, collagenase activity inhibitors, antihistaminic agents and elastase activity inhibitors. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

In the present invention, an extract extracted from a plant of a specific genus significantly recovers UV damage of skin epidermal keratinocytes, and a moisturizer, cell activator, anti-inflammatory agent, antioxidant, whitening agent, Various skin aging symptoms such as rough skin, wrinkles, dull skin, etc. by combining and combining hyaluronidase inhibitors, antiplasmin agents, active oxygen inhibitors, collagenase activity inhibitors, antihistamines, elastase activity inhibitors The present invention relates to an external preparation for skin.

The genus Cuckoo thistle belongs to the family Asteraceae, and there are two types known in Japan: Ageratum conyzoides and Ageratum houstonianum. Cuckoo Thistle is often awarded for horticulture due to its distinctive flower form. Cuckoo thistle is a kind of herbal medicine used for antipyretic, sore throat, trauma, etc., and is a kind of plant used as a folk medicine in tropical Asia (Non-patent Document 1).

Utilization as a cosmetic raw material of the genus Cuckoo is only used as a hair growth agent and an inhibitor of tyrosinase activity in Patent Document 1 and Patent Document 2, and the field of use remains in a very limited range.

The composition of the skin is roughly classified into three, and is formed from the outer layer from the epidermis, dermis, and subcutaneous tissue, each of which plays various roles such as maintaining the body's homeostasis and protecting from the outside world. The epidermis is mainly protected from the entry of bacteria from the outside world and adverse environments (ultraviolet rays, drying, etc.).

Rough skin such as dryness and roughness of the skin is caused by damage to the epidermis. There are various causes of damage to the epidermis, one of which is various adverse effects caused by ultraviolet rays. Although the UV protection method in the epidermis is a method to prevent with a hat or clothes, it cannot be completely protected. Thus, some other method is needed to minimize the adverse effects of UV rays on the skin.
See page 55 of the World Useful Encyclopedia (Heibonsha) JP 09-295919 A Japanese Patent Laid-Open No. 10-265366

The object of the present invention has been variously studied in order to effectively utilize an extract of the genus Ageratum, which has been known to be effective only as a hair restorer or a whitening agent.

In order to achieve the above-mentioned object, the present inventors have conducted intensive studies, and as a result, specific agents (humectants, cell activators, anti-inflammatory agents, antioxidants, whitening agents, Hyaluronidase inhibitors, antiplasmin agents, active oxygen inhibitors, collagenase activity inhibitors, antihistamine agents, elastase activity inhibitors, etc.) improve various skin aging symptoms such as rough skin, wrinkles and dull skin I found out that

The form of the extract of the genus Ageratum is not limited in any way, but preferably, the whole plant is shade-dried, ground, and then extracted for 3 days with an extraction solvent (for example, alcohol such as ethanol, water or a mixture thereof). Use the filtered solution after immersion or heating at 100 degrees for 1 hour and cooling.

Test method for UV damage recovery ability Normal human epidermal keratinocytes are planted in a 35 mm dish and cultured until 50-60% confluent, then 0.5 ml of HEPES buffered salt solution is added, and UV is irradiated at 1.5 J / cm2. Thereafter, 0.5 ml of the test product solution prepared in the medium was added and cultured for 2 hours.
The culture solution was sampled, placed in a 1.5 ml tube and centrifuged, and lactate dehydrogenase activity was measured using the supernatant as damaged cells. After further washing the petri dish with HEPES buffered salt solution twice, add 1 ml of 0.1% polyoxyethylene sorbitan (20E.O.) monolaurate, peel off the remaining cells in the petri dish with a scraper, and add 1.5 ml tube. And centrifuged, and the supernatant was used as a living cell to measure lactate dehydrogenase activity.
Moreover, what performed the same operation omitting ultraviolet irradiation was made into the unirradiated group.
The ratio of the amount of lactate dehydrogenase activity of damaged cells in the total amount of lactate dehydrogenase activity in the petri dish was calculated as the damage rate, and the increase or decrease from the damage rate of the unirradiated group was defined as the ultraviolet ray damage rate.
The test products are shown below, and the test results are shown in Table 1.
Sample1: Hot water (200 mL) extract of dried cuckoo leaf leaves (10 g)
Sample 2: 50% ethanol-water (200 mL) extract of dried thistle leaves (10 g)
Sample 3: Ethanol (200 mL) extract of dried cassie leaf (10 g)
Sample 4: Ethanol (200 mL) extract of honey thistle leaf dry matter (10 g) (Note 1)
Sample 5: Ethanol (200 mL) extract (Note 2) of dried leaf leaf (10 g)
Sample 6: Dry extract (10 g) of ethanol flea leaves (200 mL) extract (Note 3)
(Note 1) Fox thistle is Asteraceae (Note 2) Asteroptera is Asteraceae (Note 3) Fujisami is Asteraceae

The extract of the genus Ageratum is preferably blended at 0.000001 to 20% by weight.
Furthermore, certain drugs (humectant, cell activator, anti-inflammatory agent, antioxidant, whitening agent, hyaluronidase inhibitor, antiplasmin agent, active oxygen inhibitor, collagenase activity inhibitor, antihistamine, It has been found that the incorporation of an elastase activity inhibitor and the like improves various skin aging symptoms such as rough skin, wrinkles and dull skin.
Listed particularly effective are the whole grass of morning glory, Asam wood, Adhatoda vasica wood, yellow ranch wood, Ixcate (Hippocratea celastroides) bark, Ibonashi shiraji branch, Indian salsa root, bark of neem, Woodfordia fruticosa flowers and leaves, lumberwood, lagerstroemia speciosa leaves, CASCA-DOCE (CASCA-DOCE) (scientific name Pradosia lactescens or Lucumaglyciphloea Or Chrysophyllum buranhem), wig material, Kapoor material, stalk and branch of swordfish, genus Kawaraketsume (Kemeko, Senna, Wangjiang South, Mountain pea, Nambansaikachi), whole plant of spinach, cinnamon flower, Cuachalalate (Cuachalalate) Juliania adstringens Schl) bark, guava leaf, Quercus pidankrate Quercus pedunculate fruit, cumin seeds, cubraco heartwood, coustigaya rhizome, costillas (Acalypha diversifolia Jacq.) Trunk and branch, bark of melanoleuca leucadendron, Gordolobo (Gnaphalium) sphacellatum), saffron pistil, Saraka indica bark, JEQUITIBA (Carinianabrasiliensis or Couratari legalis or Pyxidaria macrocarpa) bark, Shimoniro whole grass, Jatoba (Hymenaea couba) Bark of Eugenia jambolana, seeds of white dwarf morning glory, whole plant of Sphaeranthus indicus, bark of spruce, root of Smilax zeylanica, scepter wood, bark of barb tree, chaba Pepper root, Desmodium gangeticm Whole grass, Terminalia horrida fruit, Tragia involucrata whole grass, Nigella sativa seed, Scots grass whole plant, Hierba del sapo (Eryngium comosum) whole plant, Hijat root, Whole plant of Pirul (Schinus molle), whole plant of Phyllanthus nuriri, whole plant of Fusenkazura, PUCA (Cissus antiparaliticus), root of vetiver, Hedesalum austrobilis (Hedysarum) austrosibiricus root, Herpestris monnies whole grass, VERONICA (Veronica officinalis) bark, Borrelia hispida root and stem, Pongamia glabra root, Mizuki bark , Mimusops elengi whole plant, Murraya koenigii shoot, Munronia Whole plant of mira, wood of melapie, bark of magnoliaceae genus genus, mountain cherry, lumbo, rumex cyprius leaf, wattle bark, aitamago, one root, fateless, fossil grass , Shellfish mother, intruder, Iwabenkei root, Paeonia anomala root, chestnut, chestnut leaf, chicken blood wisteria, Saya, messenger, small gold cocoon, husk, spicy, Saiheyanagi, Ishirenko, stone potato bark , Stone persimmon skin, stone persimmon bark, sanctuary grass, pierced stone, persimmon, valley essence, Chinese white birch, iron wrapping, winter lion, persimmon leaves, Hishimi, Kashio grass, Ryo Wang, lotus leaf , Eggplant, cormorant sea, toothpick, coconut tree, samurai, sea urchin, seaweed of Ishigeaceae; pearl powder, conchiolin, conchyolin hydrolyzate, conchiolin hydrolyzate treated with succinic anhydride, shellfish Substances obtained by hydrolyzing mucus, sterols obtained from shellfish meat, acidic polysaccharides obtained from shellfish meat Collagen obtained from shellfish meat, glycogen obtained from shellfish meat, phospholipid obtained from shellfish meat, deoxyribonucleic acid obtained from shellfish meat, thiosalicylic acid and its salt, magnolol, honokiol, 1- (4 -Hydroxyphenthio) -2-propanol, 2- (4-hydroxyphenyl) -1,3-dithiane, 2- (4-acetoxyphenyl) -1,3-dithiane, 2,5-dihydroxybenzamide, 2,6 -Dihydroxybenzamide, 4-aminophenol, 4-hydroxythiophenol, 4-hydroxybenzamide, 5-hydroxyindole, 6-dihydroxy) -dihydrobenzofuran-3-yl- (3'4'-dihydroxy) -phenyl ketone, stilbengalo Ile glycoside, citracin C, ethylenediamine derivative, carahanaenone derivative, cashew nut shell oil, carda A peptide containing the sequence of nord, cardol, anacardic acid, sennoside, α-arbutin, Glu-Glu-Met-Gln-Arg-Arg, or the terminal of the carboxyl group of this peptide is converted to an amide or / and the amino group is acylated Peptides converted into isomers can be mentioned.
Examples of ethylenediamine derivatives include N-phenyl-N- (2,3,3 trimethyl-1-cyclopentene-1-ethyl) -N ′, N′-dimethylethanediamine, N-2-pyridyl-N- (3 , 7-Dimethyl-6-octen-1-yl) -N ', N'-dimethylethanediamine, N-2-pyridyl-N- (2-pinen-10-yl) -N', N'-dimethylethane Mention may be made of diamines, N-2-pyridyl-N- (1,8-p-menthadien-7-yl) -N ', N'-dimethylethanediamine.
For example, N-p-hydroxyphenyl-3,3,6-trimethyl-5-cycloheptan-2-one-1-carboxamide, 2-hydroxy-Np-hydroxyphenyl-3,3 , 6-trimethyl-5-cycloheptene-1-carboxamide. Examples of stilbene galloyl glycosides include 3,5,4'-trihydroxystilbene 4'-0-β-D- (6 "galloyl) glucopyranoside, 3,5,4'-trihydroxystilbene 4'- Mention may be made of 0-β-D- (2 ″ galloyl) glucopyranoside.

Furthermore, it has also been found that the effect can be further obtained by blending one or more of polyhydric alcohols containing two or more hydroxyl groups, lower alcohols, surfactants, and low molecular betaines.

The polyhydric alcohol that can be used is not particularly limited, and examples thereof include glycerin, 1,3 butylene glycol, propylene glycol, isoprene glycol, sorbitol, trehalose, maltose and the like. These are blended in an amount of 0.1 to 80% by weight, preferably 1 to 30% by weight. Needless to say, the blending amount varies depending on the type of polyhydric alcohol, and a plurality of polyhydric alcohols can be used.

Absorbability improves by mix | blending a lower alcohol. Although there are various kinds of lower alcohols, ethanol is usually used. The blending amount is not particularly limited but is preferably 2 to 70% by weight.
It is also effective to combine a surfactant with a polyhydric alcohol combination containing an extract of the genus Ageratum, and it is also effective to combine the lower alcohol.
There is no particular limitation on the surfactant, and the type and amount may be selected depending on the application and dosage form.
Surfactants are used for emulsification and solubilization of oils, etc., and are anionic (alkyl carboxylates, alkyl sulfonates, alkyl sulfate esters, alkyl phosphate esters), nonionic (ether type) Nonionic surfactant, ether ester type nonionic surfactant, ester type nonionic surfactant, block polymer type nonionic surfactant, nitrogen-containing type nonionic surfactant) and amphoteric (carboxylic acid type amphoteric surfactant) Agents (amino type, betaine type), sulfate ester type amphoteric surfactant, sulfonic acid type amphoteric surfactant, phosphate ester type amphoteric surfactant) and other surfactants (natural surfactants, protein hydrolysates) Derivatives, polymer surfactants, surfactants containing titanium and silicon, and fluorocarbon surfactants) can be used as appropriate.

Low molecular weight betaine is also one of the raw materials to be selected, and by blending this, the effect is further improved and the feeling of application is improved, and the effectiveness as an external preparation for skin is increased.
Low molecular weight betaines that can be utilized may include those that form zwitterions with internal salts such as quaternary ammonium bases, sulfonium bases, phosphonium bases and the like having a molecular weight of 200 or less. Examples include trimethylglycine, N, N, N-trimethylalanine, N, N, N-trimethylglutamic acid, triethylglycine, and the like, with trimethylglycine being preferred.
Those having a molecular weight of 200 or more have a surface-active ability, which is different from the effect of low molecular betaine. As described above, the use of a surfactant enhances the effect of the present invention, but the effect of low molecular betaine is Is different.

  The external preparation for skin of the present invention can be prepared by blending with various forms of base materials known as normal external preparations for skin according to conventional methods.

It does not specifically limit as a form of an external preparation, For example, arbitrary dosage forms, such as a milky lotion, cream, aqueous solution, a pack, can be selected.

In the external preparation for skin of the present invention, in addition to the above-mentioned essential components, components that are blended in normal external preparations, such as oils, powders, purified water, polymer compounds, gelling agents, UV absorbers, UV scattering Agents, antioxidants, pigments, preservatives, fragrances, and cosmetic ingredients can be appropriately selected and used within a range not impairing the effects of the present invention.

EXAMPLES Next, although an Example is given and this invention is demonstrated further in detail, this invention is not restrict | limited at all. Moreover, the extraction method about the extract of the used chemical | medical agent is not limited at all.
The formulations of the examples are shown in Tables 2 to 4. The preparation method was performed by a conventional method. Table 2 shows the lotion, Table 3 shows the serum, and Table 4 shows the cream. The amount is shown in parts by weight.

(Note 1) The extract of Cuckold Thistle 1 was obtained by adding 200 ml of purified water to 10 g of the dried product of Cuckoo Thistle and boiled for 1 hour, and then using the filtered extract.
(Note 2) For the Cuckoo Thistle Extract 2, the filtered extract was used after adding 100 ml of purified water and 100 ml of ethanol to 10 g of the dried product of Cuckoo Thistle and leaving it to stand for 10 days.
(Note 3) For the Cuckoo Thistle Extract 3 was used a filtered extract after adding 200 ml of ethanol to 10 g of dried dried Clover Thistle leaves for 10 days.
(Note 4) The hydrolyzed conchiolin solution used was a hydrolyzed conchyolin that had a molecular weight of 1000 or less.
(Note 5) For the saffron pistil extract, 300 ml of ethanol was added to 10 g of saffron pistil and allowed to stand for 5 days, and then the filtered extract was used.
(Note 6) Falco Rex Honoki E [Ichimaru Falcos Co., Ltd.] was used as the honoki extract.
(Note 7) As the guava extract, 300 ml of ethanol was added to 10 g of guava leaves and allowed to stand for 5 days, and then the filtered extract was used.
(Note 8) Nishi-Haruyanagi extract used Nishi-Haruyanagi extract [Nippon Seika Co., Ltd.].
(Note 9) Marine purge [manufactured by Ichimaru Falcos Co., Ltd.] was used as the seaweed extract.
(Note 10) As the acacia bark extract, 300 ml of ethanol was added to 10 g of bark and left for 5 days, and then the filtered extract was used.
(Note 11) Murayako Engii extract was used as an extract from Murayako Engui [Yamakawa Trading Co., Ltd.].
(Note 12) The giant crape myrtle extract used was the greater crested weevil extract [manufactured by Yamakawa Trading Co., Ltd.].

The skin beautification effect tests of Examples 1 to 12 and Comparative Examples 1 to 3 described in Tables 1 to 3 were performed. The test method consisted of 20 females aged 25 to 55 years old, and a suitable amount of a topical preparation was applied to the face after washing the face twice a day in the morning and night for 12 weeks. Table 5 shows the results of the skin beautifying effect by application.

  From the results in Table 5, an extract of Ageratum that has an effect of recovering UV damage from epidermal keratinocytes and specific drugs (humectants, cell activators, anti-inflammatory agents, antioxidants, whitening agents, hyaluronidase inhibition) 1 type or 2 or more types of agents, antiplasmin agents, active oxygen inhibitors, collagenase activity inhibitors, antihistamines, elastase activity inhibitors, etc., to prevent rough skin, spots, freckles, liver spots, wrinkles, Reduction and improvement effect became more effective. Furthermore, it turned out that the said effect increases synergistically.

Claims (4)

Cellular UV damage recovery agent comprising an extract of a plant belonging to the genus Ageratum Extracts and moisturizers of plants belonging to the genus Ageratum (Ageratum), cell activators, anti-inflammatory agents, antioxidants, whitening agents, hyaluronidase inhibitors, antiplasmin agents, active oxygen inhibitors, collagenase activity inhibitors, antihistamines The cell ultraviolet ray damage recovery agent according to claim 1, wherein any one or more of elastase activity inhibitors are added. Moisturizers, cell activators, anti-inflammatory agents, antioxidants, whitening agents, hyaluronidase inhibitors, antiplasmin agents, active oxygen inhibitors, collagenase activity inhibitors, antihistamines, elastase activity inhibitors Timber, Adhatoda vasica timber, yellow ranch timber bark, Ixcate (Hippocratea celastroides) bark, Ibana tsutsu rafu branch, Indian salsa root, neem bark, Woodfordia Fruticosa (Woodfordia) fruticosa) flowers and leaves, lumberjack, lagerstroemia speciosa leaves, CASCA-DOCE (scientific name Pradosia lactescens or Lucumaglyciphloea or Chrysophyllum buranhem), wigs, kapoor, stems , Branch, Kawaroketsumei (Kemeko, Senna, Minami Moe, Yamashirazu, Nanba Cypress, whole spinach, cinnamon blossom, Cuachalalate (Juliania adstringens Schl) bark, guava leaf, Quercus pedunculate fruit, cumin seeds, cubraco heartwood, cous iguaya rhizome, costilas (Costillas) (Acalypha diversifolia Jacq.) Trunks and branches, bark of Melaleuca leucadendron, whole grass of Gordolobo (Gnaphalium sphacellatum), bark of saffron, bark of Saraka indica, Bark of JEQUITIBA (Carinianabrasiliensis or Couratari legalis or Pyxidaria macrocarpa), whole plant of Simonilo, bark of Jatoba (Hymenaea coubaril), bark of Jugebora (Eugenia jambolana), seed of white moth (Sphaeranthus indicus) Bark, Smilax zeylanica (Smilax zeylanica) root, scepter wood, tablin bark, green pepper root, Desmodium gangeticm whole grass, Terminalia horrida fruit, Tragia involcata (rata) Whole plant, Nigella sativa seeds, alligator grass, Hierba del sapo (Eryngium comosum) whole plant, jade root, Pirul (Schinus molle) whole plant, Phyllanthus nuriri Whole plant, whole plant of Fusenkazura, PUCA (Cissus antiparaliticus), root of vetiver, root of Hedesalum austrosibiricus, whole plant of Herpestris monnies, Veronica ( VERONICA) (Veronica officinalis) bark, Borrelia hispida roots and stems, Pongamia gra Pongamia glabra root, Mizuki bark, Mizubark bark, Mimusops elengi whole plant, Murraya koenigii shoot, Munronia pumila whole plant, Melapi wood Bark of the genus, Yamazakura wood, Lambo wood, Rumex cyprius leaf, Watle bark, Ai Tamago, Ichione root, Wang immutable, Fossil grass, Shell mother, Intruder, Iwabenkei root, Paeonia anomala roots, chestnuts, chestnut leaves, chicken blood wisteria, Saya, ambassador, small gold cocoon, husk, spicy, Nishikawayanagi, Ishirenko, sarcophagus bark, sarcophagus bark, sarcophagus bark, sasakuru Fracture stones, cormorants, valley essences, Chinese white coral, iron wrapping, winter lions, cocoon leaves, Hishimi, Kashiwaso, Ryohao, lotus leaves, lions, 胖大海, 茘 枝, lions, Saito, 鵝 不 食草, Ishigeae seaweed, pearl powder, conchiolin, conchiolin water Decomposed product, substance obtained by treating hydrolyzate of conchiolin with succinic anhydride, substance obtained by hydrolyzing shellfish mucus, sterols obtained from shellfish meat, acidic polysaccharide obtained from shellfish meat, shellfish meat Collagen obtained, glycogen obtained from shellfish meat, phospholipid obtained from shellfish meat, deoxyribonucleic acid obtained from shellfish meat, thiosalicylic acid and its salt, magnolol, honokiol, 1- (4-hydroxypheny Thio) -2-propanol, 2- (4-hydroxyphenyl) -1,3-dithiane, 2- (4-acetoxyphenyl) -1,3-dithiane, 2,5-dihydroxybenzamide, 2,6-dihydroxybenzamide , 4-aminophenol, 4-hydroxythiophenol, 4-hydroxybenzamide, 5-hydroxyindo , 6-dihydroxy) -dihydrobenzofuran-3-yl- (3'4'-dihydroxy) -phenyl ketone, stilbengaloyl glycoside, citracin C, ethylenediamine derivative, caranahanaone derivative, cashew nut shell liquid, cardanol, cardol, anacard A peptide containing the sequence of acid, sennoside, α-arbutin, Glu-Glu-Met-Gln-Arg-Arg, or the carboxyl group terminal of this peptide was converted to an amide form, and / or the amino group terminal was converted to an acylated form The agent for recovering cellular UV damage according to claim 2, which is a peptide Furthermore, the cell ultraviolet ray damage recovery agent of Claim 1 thru | or 3 which contains any 1 type, or 2 or more types of the polyhydric alcohol containing two or more hydroxyl groups, a lower alcohol, surfactant, and low molecular betaine.