JPS638335A - External preparation suppressing melanin formation - Google Patents
External preparation suppressing melanin formationInfo
- Publication number
- JPS638335A JPS638335A JP15201986A JP15201986A JPS638335A JP S638335 A JPS638335 A JP S638335A JP 15201986 A JP15201986 A JP 15201986A JP 15201986 A JP15201986 A JP 15201986A JP S638335 A JPS638335 A JP S638335A
- Authority
- JP
- Japan
- Prior art keywords
- ergothioneine
- placenta
- extracted solution
- external preparation
- active ingredients
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 title abstract description 10
- 238000002360 preparation method Methods 0.000 title abstract description 8
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 210000002826 placenta Anatomy 0.000 claims abstract description 24
- SSISHJJTAXXQAX-ZETCQYMHSA-N L-ergothioneine Chemical compound C[N+](C)(C)[C@H](C([O-])=O)CC1=CNC(=S)N1 SSISHJJTAXXQAX-ZETCQYMHSA-N 0.000 claims abstract description 23
- 229940093497 ergothioneine Drugs 0.000 claims abstract description 22
- 229940079593 drug Drugs 0.000 claims abstract description 13
- 239000003814 drug Substances 0.000 claims abstract description 13
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 8
- 239000000284 extract Substances 0.000 claims description 21
- 230000008099 melanin synthesis Effects 0.000 claims description 16
- 230000000699 topical effect Effects 0.000 claims description 11
- 230000000694 effects Effects 0.000 abstract description 12
- 239000004480 active ingredient Substances 0.000 abstract description 7
- 206010008570 Chloasma Diseases 0.000 abstract description 5
- 208000003351 Melanosis Diseases 0.000 abstract description 5
- 239000000126 substance Substances 0.000 abstract description 5
- 238000002560 therapeutic procedure Methods 0.000 abstract description 5
- 239000002674 ointment Substances 0.000 abstract description 4
- 230000007246 mechanism Effects 0.000 abstract description 3
- 230000002195 synergetic effect Effects 0.000 abstract description 3
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 229940124543 ultraviolet light absorber Drugs 0.000 abstract 1
- 239000006097 ultraviolet radiation absorber Substances 0.000 abstract 1
- 239000011782 vitamin Substances 0.000 abstract 1
- 229940088594 vitamin Drugs 0.000 abstract 1
- 229930003231 vitamin Natural products 0.000 abstract 1
- 235000013343 vitamin Nutrition 0.000 abstract 1
- 150000003722 vitamin derivatives Chemical class 0.000 abstract 1
- 208000012641 Pigmentation disease Diseases 0.000 description 9
- 238000012360 testing method Methods 0.000 description 6
- 238000011282 treatment Methods 0.000 description 6
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 5
- 230000005764 inhibitory process Effects 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 4
- 102000003425 Tyrosinase Human genes 0.000 description 4
- 108060008724 Tyrosinase Proteins 0.000 description 4
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- 239000000839 emulsion Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 210000002752 melanocyte Anatomy 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 230000002087 whitening effect Effects 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 150000005208 1,4-dihydroxybenzenes Chemical class 0.000 description 2
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 2
- JPVYNHNXODAKFH-UHFFFAOYSA-N Cu2+ Chemical compound [Cu+2] JPVYNHNXODAKFH-UHFFFAOYSA-N 0.000 description 2
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 2
- 229930003268 Vitamin C Natural products 0.000 description 2
- 229910001431 copper ion Inorganic materials 0.000 description 2
- 239000002537 cosmetic Substances 0.000 description 2
- 239000007854 depigmenting agent Substances 0.000 description 2
- 229960000735 docosanol Drugs 0.000 description 2
- VJNCICVKUHKIIV-UHFFFAOYSA-N dopachrome Chemical compound O=C1C(=O)C=C2NC(C(=O)O)CC2=C1 VJNCICVKUHKIIV-UHFFFAOYSA-N 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 229940075507 glyceryl monostearate Drugs 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 208000000069 hyperpigmentation Diseases 0.000 description 2
- 230000003810 hyperpigmentation Effects 0.000 description 2
- 238000007689 inspection Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000006210 lotion Substances 0.000 description 2
- QPJVMBTYPHYUOC-UHFFFAOYSA-N methyl benzoate Chemical compound COC(=O)C1=CC=CC=C1 QPJVMBTYPHYUOC-UHFFFAOYSA-N 0.000 description 2
- 150000004702 methyl esters Chemical class 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 2
- 230000019612 pigmentation Effects 0.000 description 2
- 230000003169 placental effect Effects 0.000 description 2
- 210000003491 skin Anatomy 0.000 description 2
- 238000010998 test method Methods 0.000 description 2
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 2
- 235000019154 vitamin C Nutrition 0.000 description 2
- 239000011718 vitamin C Substances 0.000 description 2
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 1
- 229940058015 1,3-butylene glycol Drugs 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- DCXXMTOCNZCJGO-UHFFFAOYSA-N Glycerol trioctadecanoate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 206010042496 Sunburn Diseases 0.000 description 1
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 206010047642 Vitiligo Diseases 0.000 description 1
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 239000006096 absorbing agent Substances 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000012752 auxiliary agent Substances 0.000 description 1
- 235000021302 avocado oil Nutrition 0.000 description 1
- 239000008163 avocado oil Substances 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 235000019437 butane-1,3-diol Nutrition 0.000 description 1
- 230000009920 chelation Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000001339 epidermal cell Anatomy 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 208000021760 high fever Diseases 0.000 description 1
- 229920002674 hyaluronan Polymers 0.000 description 1
- 229960003160 hyaluronic acid Drugs 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- VYQNWZOUAUKGHI-UHFFFAOYSA-N monobenzone Chemical compound C1=CC(O)=CC=C1OCC1=CC=CC=C1 VYQNWZOUAUKGHI-UHFFFAOYSA-N 0.000 description 1
- 229960000990 monobenzone Drugs 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- -1 polyoxyethylene Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000012264 purified product Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 238000002798 spectrophotometry method Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000001308 synthesis method Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明は肝斑などの色素沈着症に対する外用療法に用い
られるメラニン生成抑制外用薬剤に関するものである。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a melanin production inhibiting topical drug used for topical treatment of pigmentation disorders such as melasma.
(従来の技術〕
肝斑をはじめとする色素沈着症に対する治療法としては
、ビタミンCの連続内服などによる方法が行われている
が、色素沈着の程度が冑度になるとビタミンCの連続内
服では改善されない場合が多い。また外用療法として色
素沈着症がメラノサイトの機能昂進によりひきおこされ
た表皮細胞のメラノサイトの量の増大と考えられ、この
メラニンの過剰生成を抑制させる方法としてメラノサイ
ト機能を昂進させる紫外線の影響を防止する方法として
、タルク、亜鉛華、酸化チタン等の粉末などの光線を散
乱させる物質、又は紫外線吸収剤例えばパラアミノ安息
香酸などを含む軟膏などを用いる方法が行われていた。(Conventional technology) Continuous oral administration of vitamin C has been used as a treatment for pigmentation disorders such as melasma, but once the degree of pigmentation has reached a certain level, continuous oral administration of vitamin C is insufficient. In many cases, it does not improve.Additionally, as a topical therapy, hyperpigmentation is thought to be caused by an increase in the amount of melanocytes in the epidermal cells caused by the enhancement of melanocyte function, and as a way to suppress this excessive production of melanin, it is recommended to enhance melanocyte function. As a method of preventing the effects of ultraviolet rays, methods have been used to use substances that scatter light rays, such as powders such as talc, zinc white, and titanium oxide, or ointments containing ultraviolet absorbers, such as para-aminobenzoic acid.
また、表皮におけるメラニン生成の抑制作用を持つ物質
、ハイドロキノン、ハイドロキノン誘導体などの脱色剤
を含有した外用剤を用いることも知られている。It is also known to use an external preparation containing a depigmenting agent such as a substance that suppresses melanin production in the epidermis, hydroquinone, or a hydroquinone derivative.
更に、エルゴチオネインを含有した色白化粧料は特公昭
55−27883号公報に開示されている。Furthermore, a fair skin cosmetic containing ergothioneine is disclosed in Japanese Patent Publication No. 55-27883.
また、胎盤抽出液を化粧料に配合した、化粧料も開示さ
れている(特公昭35−15399号公報)。Furthermore, cosmetics containing placenta extracts have also been disclosed (Japanese Patent Publication No. 15399/1983).
従来技術において、色素沈着症の外用療法における外用
薬剤に用いられる光線遮断剤は色素沈着が日光光線によ
り増大するのを防止するために用いるものであるから、
他の療法と共に使用するものであり、この薬剤の単独使
用によっては色素沈着症の外用薬剤としての効果は期待
できない。In the prior art, light blocking agents used in external drugs for topical treatment of pigmentation disorders are used to prevent pigmentation from increasing due to sunlight;
It is used in conjunction with other therapies, and if used alone, it cannot be expected to be effective as a topical drug for pigmentation disorders.
脱色剤として用いられるハイドロキノン、ハイドロキノ
ン誘導体(ハイドロキノンモノベンジルエーテル等)の
外用剤は斑状ないし網状の白斑を副作用として生ずるお
それがあり、色素沈着症などの外用治療剤としては好ま
しくない。External preparations of hydroquinone and hydroquinone derivatives (hydroquinone monobenzyl ether, etc.) used as depigmenting agents may cause patchy or reticular vitiligo as a side effect, and are not preferred as external treatments for pigmentation disorders and the like.
本発明は色素沈着症などの外用療法に用いる外用薬剤に
おいてメラニン生成を充分に抑制する薬剤を提供するこ
とを目的とするものである。An object of the present invention is to provide an external drug that sufficiently suppresses melanin production for use in external treatment of pigmentation disorders and the like.
本発明は胎盤抽出液とエルゴチオネインを含有すること
によって、色素沈着症等の皮膚疾患に対し顕著な効果を
奏するメラニン生成抑制外用薬剤fである。The present invention is a melanin production suppressing topical drug f that contains placenta extract and ergothioneine and has a remarkable effect on skin diseases such as hyperpigmentation.
本発明に用いるエルゴチオネインは下記構造式を有する
既知化合物である。Ergothioneine used in the present invention is a known compound having the following structural formula.
C0〇−
この物質は人体の血液や肝臓などの臓器中に含まれてい
ることが知られており、〔ジャーナル・オブ・バイオロ
ジカル・ケミストリー206巻、221頁、1954年
(ディ・ビイ・メイビル、ダブリユウ・エイチ・ホーナ
ー、アール・レブシェツ)〕(D、 8.Melv i
le、 W、 H,Horner、 R,Lubsch
ez ;J、 Biol 、 Chem。C0〇- This substance is known to be contained in the human body's blood and organs such as the liver. , D. H. Horner, Earl Levshec)] (D, 8. Melvi
le, W, H, Horner, R, Lubsch.
ez ; J, Biol, Chem.
206221P 1954)、またその合成法も報告さ
れている、〔ジャーナル・オブ・ケミカル・ソサエティ
2215M 1951年(エイチ、ヘース、エイ・ロア
ンソン、シイ・リミングトン)) (H,Heath、
A、Lawason。206221P 1954), and its synthesis method has also been reported [Journal of Chemical Society 2215M 1951 (H, Heath, A. Roanson, C. Rimington)] (H, Heath,
A. Lawson.
C,Rimington;J、Chem、 Soc、2
215P、 1951)。C, Rimington; J, Chem, Soc, 2
215P, 1951).
本発明には上記の生物体より抽出精製物、合成物何れで
も使用することができる。In the present invention, both extracted and purified products and synthetic products from the above-mentioned organisms can be used.
上述の胎盤抽出液とエルゴチオ茅インを配合する割合は
胎盤抽出液10(重量)に対し、エルゴチオネイン5〜
0.01 (重量)が好適である。The ratio of the above placenta extract and ergothioneine is 10 parts (by weight) of placenta extract to 5 to 5 parts ergothioneine.
0.01 (weight) is suitable.
そして、これらのを効成分の外用薬剤に含有させる割合
は胎盤抽出液は全薬剤の0.1〜lO%(重量)、エル
ゴチオネインは0.01〜5%(重量)程度で充分その
効果を奏することができる。The proportion of these active ingredients in topical drugs is approximately 0.1 to 10% (by weight) for placenta extract and 0.01 to 5% (by weight) for ergothioneine, which is sufficient to achieve its effect. be able to.
本発明の外用薬剤は主として乳剤、ローション剤、軟頁
などの外用薬剤である。これらの各製剤は上記存効成分
を各製剤に通常使用される基剤。The external medicines of the present invention are mainly emulsions, lotions, soft pages, and the like. Each of these preparations contains the above-mentioned active ingredients as a base commonly used in each preparation.
助剤などと通常用いられる方法により製剤化する。It is formulated using auxiliary agents and other commonly used methods.
次に本発明のメラニン生成抑制外用薬剤のメラニン生成
抑制を示す試験例を挙げる。Next, a test example showing the inhibition of melanin production by the melanin production-inhibiting topical drug of the present invention will be given.
(1) チロシナーゼ抑制試験
(試験方法)
試験管にL−ドーパ溶液(lomM) I m/、マ
フクルへイン緩衝液(pH6,!3) 0.9 m!及
び試料1dを入れ、37°Cの恒温水槽で10分間イン
キュベートし、後チロシナーゼ活性1(B16マウスメ
ラノーマの11.0OOG上li”?)0.1−を入れ
、よく撹拌した後、直ちに分光光度計にセットし、47
5 nmにおける吸光度を経時的に測定した。(1) Tyrosinase inhibition test (test method) In a test tube, add L-dopa solution (lomM) I m/Mafkulhein buffer (pH 6, !3) 0.9 m! Add sample 1d and incubate for 10 minutes in a thermostatic water bath at 37°C. Then add tyrosinase activity 1 (11.0OOG above li" of B16 mouse melanoma) 0.1-, stir well, and immediately check spectrophotometry. Set it on the meter, 47
Absorbance at 5 nm was measured over time.
試料は、胎盤抽出液、0.1%エルゴチオネイン、胎盤
抽出液に0.1%エルゴチオネインを含有する液、及び
対照として水である。なお阻止率は対照を100とした
場合、8分後のドーパクロム生成阻害の割合である。The samples are placenta extract, 0.1% ergothioneine, placenta extract containing 0.1% ergothioneine, and water as a control. Note that the inhibition rate is the percentage of inhibition of dopachrome production after 8 minutes when the control is set as 100.
以上の測定結果を添付図面で示す。図面より明らかな如
く、エルゴチオネインと胎盤抽出液の併用は、各単独の
ものより相果的にチロシナーゼ活性を阻害することがわ
かる。The above measurement results are shown in the attached drawings. As is clear from the figures, the combination of ergothioneine and placenta extract inhibits tyrosinase activity more effectively than either alone.
なお、本発明の有効成分であるエルゴチオネイン、胎盤
抽出液はそれぞれ単独でもメラニン生成阻止作用を存す
ることは知られているが、本発明者の研究によって、本
実験に使用したB16細胞の細胞系でのメラニン生成阻
止の機序を解析した結果、エルゴチオネインはメラニン
生成の初期段階に関与するチロシナーゼの活性に及ぼす
銅イオンとキレ−ジョンしてチロシナーゼ活性を抑制し
、メラニンの生成を阻害するのに対し、胎盤抽出液は銅
イオンのキレ−ジョンを示さず、胎盤抽出液のメラニン
生成抑制の機序はエルゴチオネインのそれと作用が異な
ることが実証された。この結果エルゴチオネインと胎盤
抽出液の相異なるメラニン生成阻害作用により両者の相
乗効果が得られるものと考えられる。Although it is known that ergothioneine and placenta extract, which are the active ingredients of the present invention, have the effect of inhibiting melanin production even when used alone, the inventor's research has shown that ergothioneine and placenta extract have the effect of inhibiting melanin production. As a result of analyzing the mechanism of inhibition of melanin production, it was found that ergothioneine inhibits melanin production by chelating with copper ions and suppressing tyrosinase activity, which is involved in the initial stage of melanin production. It was demonstrated that the placental extract did not show copper ion chelation, and that the mechanism of melanin production suppression in the placental extract was different from that of ergothioneine. As a result, it is thought that the synergistic effect of ergothioneine and placenta extract is obtained due to their different melanin production inhibiting effects.
(2) ヒトの皮FJ塗布試験
(試験方法)
A、B、Cの3個所の病院において、シミ、日焼けの患
者60人を対象に本発明の軟膏の雪布試験を行った。(2) Human skin FJ application test (test method) A snow cloth test of the ointment of the present invention was conducted on 60 patients with age spots and sunburn at three hospitals, A, B, and C.
最終判定は塗布開始より、3箇月後に肉眼で観察して、 無効:白色化が認められないもの。The final judgment was made by visual observation 3 months after the start of application. Invalid: Whitening is not observed.
やや有効:僅かに白色化が認められるもの。Slightly effective: Slight whitening is observed.
有効:明らかに白色化が認められるもの。Effective: Those with obvious whitening.
著効:完治又はそれに近いもの。Effective results: Complete recovery or something close to it.
として判定した。It was judged as.
以上の結果から3個所の病院で合計60名中熱効4名、
やや有効11名、有効33名、著効12名であった。や
や有効から著効までを合計すると56名で有効率93.
33%であった。Based on the above results, a total of 60 patients at three hospitals, 4 with high fever,
The results were moderately effective in 11 patients, effective in 33 patients, and excellent in 12 patients. The total efficacy rate was 93.5 for 56 patients, ranging from moderately effective to excellent efficacy.
It was 33%.
次に本発明の実施例を挙げる。 Next, examples of the present invention will be described.
例1
(軟膏剤)
モノステアリン酸ポリエチレングリコール(40E、o
、)2.OOg、自己乳化型モノステアリン酸グリセリ
ン5.00 g 、ステアリンMS−00g、ベヘニル
アルコール1.OOg、流動パラフィン10.00 g
、トリオクタン酸グリセリル10.00 g、パラオキ
ン安息香酸メチルエステル0.20gを加温溶解する。Example 1 (Ointment) Polyethylene glycol monostearate (40E, o
,)2. OOg, self-emulsifying glyceryl monostearate 5.00 g, stearin MS-00g, behenyl alcohol 1. OOg, liquid paraffin 10.00 g
, 10.00 g of glyceryl trioctanoate, and 0.20 g of paraoquine benzoic acid methyl ester were dissolved by heating.
これに1.3−ブチレンゲリコール5.00g及び精製
水51.8 gを加温した溶液に加え乳化攪拌し、冷却
する。かくして得られた乳化液にエルゴチオネイン2.
0g、人胎盤抽出液8.0gを加え、混合攪拌し、冷却
後容器に充填し、検査後製品とする。A heated solution of 5.00 g of 1.3-butylene gellicol and 51.8 g of purified water was added to this, emulsified, stirred, and cooled. 2. Ergothioneine was added to the emulsion thus obtained.
Add 0g of human placenta extract and 8.0g of human placenta extract, mix and stir, cool, and then fill in a container to obtain a product after testing.
例2
(乳剤)
モノステアリン酸ポリオキンエチレンソルビタン(20
E、O,)1.00 g、テトラオレイン酸ポリオキシ
エチレンソルビノト(60E、O,)0.50 g 、
親油型モノステアリン酸グリセリン1.OOg、ステア
リン酸0.50g、ベヘニルアルコール0.50 g、
アボガド油4.0Og、トリオクタン酸グリセリル4.
OOg、パラオキシ安に、香酸メチルエステル0.20
gを加温溶解する。それに1.3−ブチレングリコール
5.00g1キサンタンガム0.14g、エルゴチオネ
イン1.0g、大胎盤抽出液5.0g及び精製水77.
16 gに加温した溶液を加え乳化攪拌し、冷却する。Example 2 (Emulsion) Polyoquine ethylene sorbitan monostearate (20
E, O,) 1.00 g, polyoxyethylene sorbinotetraoleate (60E, O,) 0.50 g,
Lipophilic glyceryl monostearate 1. OOg, stearic acid 0.50g, behenyl alcohol 0.50g,
Avocado oil 4.0Og, glyceryl trioctanoate 4.
OOg, paraoxyammonium, fragrant methyl ester 0.20
Dissolve g by heating. In addition, 5.00 g of 1,3-butylene glycol, 0.14 g of xanthan gum, 1.0 g of ergothioneine, 5.0 g of placenta extract, and 77 g of purified water.
Add 16 g of the heated solution, stir to emulsify, and cool.
この液に香料を微量加え撹拌、混合する。かくして得ら
れた液を冷却後、容器に充填し、検査後製品とする。Add a small amount of fragrance to this liquid and stir to mix. After cooling the liquid obtained in this way, it is filled into a container and used as a product after inspection.
例3
(ローション剤)
エルゴチオネイン0.5gと人胎盤抽出W3.0gトハ
ラオキシ安息香酸メチルエステル0.10g、ヒアルロ
ン酸0.01 g、香料微量と精製水を加え全量を10
0gとし撹拌、混合し、容器に充填し、検査後製品とす
る。Example 3 (Lotion) Add 0.5 g of ergothioneine, 3.0 g of human placenta extract W, 0.10 g of tohaloxybenzoic acid methyl ester, 0.01 g of hyaluronic acid, a trace amount of fragrance, and purified water, and bring the total amount to 10 g.
0g, stir and mix, fill in a container, and use as a product after inspection.
本発明のメラニン生成抑制外用薬剤は、その症状により
適宜使用されるが、一般に1日3回洗顔後、患部に塗布
することより充分その効果が奏せられる。The melanin production inhibiting topical drug of the present invention is used as appropriate depending on the symptoms, but it is generally effective by applying it to the affected area three times a day after washing the face.
本発明の外用薬剤は、これを患部に塗布することにより
、エルゴチオネインと胎盤抽出液との相乗作用により、
肝斑などによる色素沈着症の予防、治療に掻めて有効な
ものである。By applying the topical drug of the present invention to the affected area, the synergistic action of ergothioneine and placenta extract can cause
It is extremely effective in the prevention and treatment of pigmentation disorders caused by melasma and the like.
図面は本発明の有効成分のドーパクロム生成を示す。 The figure shows the dopachrome production of the active ingredient of the invention.
Claims (1)
徴とするメラニン生成抑制外用薬剤。 2、胎盤抽出液が人胎盤抽出液である特許請求の範囲第
1項記載のメラニン生成抑制外用薬剤。[Scope of Claims] 1. An external drug for suppressing melanin production, characterized by containing placenta extract and ergothioneine. 2. The melanin production inhibiting topical drug according to claim 1, wherein the placenta extract is a human placenta extract.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15201986A JPS638335A (en) | 1986-06-27 | 1986-06-27 | External preparation suppressing melanin formation |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15201986A JPS638335A (en) | 1986-06-27 | 1986-06-27 | External preparation suppressing melanin formation |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS638335A true JPS638335A (en) | 1988-01-14 |
Family
ID=15531280
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP15201986A Pending JPS638335A (en) | 1986-06-27 | 1986-06-27 | External preparation suppressing melanin formation |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS638335A (en) |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1991015204A2 (en) * | 1990-04-09 | 1991-10-17 | The Rockefeller University | METHOD AND AGENTS FOR THE SELECTIVE REDUCTION OF Lp(a) |
US6103746A (en) * | 1997-02-20 | 2000-08-15 | Oxis International, Inc. | Methods and compositions for the protection of mitochondria |
WO2001087260A1 (en) * | 2000-05-18 | 2001-11-22 | L'oreal | Use of ergothioneine and/or its derivatives as anti-pollution agent |
FR2810548A1 (en) * | 2000-06-26 | 2001-12-28 | Oreal | USE OF ERGOTHIONEIN AND / OR ITS DERIVATIVES AS AN ANTI-GLYCATION AGENT |
US6479533B1 (en) | 1997-02-20 | 2002-11-12 | Applied Genetics Incorporated Dermatics | Methods and compositions for the protection of mitochondria |
WO2006124992A1 (en) * | 2005-05-17 | 2006-11-23 | The Procter & Gamble Company | Regulation of mammalian keratinous tissue using personal care compositions comprising ergothioneine |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6324967A (en) * | 1986-07-18 | 1988-02-02 | 株式会社 シエル石油大阪発売所 | Indoor tennis court and its apparatus |
-
1986
- 1986-06-27 JP JP15201986A patent/JPS638335A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6324967A (en) * | 1986-07-18 | 1988-02-02 | 株式会社 シエル石油大阪発売所 | Indoor tennis court and its apparatus |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1991015204A2 (en) * | 1990-04-09 | 1991-10-17 | The Rockefeller University | METHOD AND AGENTS FOR THE SELECTIVE REDUCTION OF Lp(a) |
WO1991015204A3 (en) * | 1990-04-09 | 1991-11-28 | Univ Rockefeller | Method and agents for the selective reduction of lp(a) |
US6103746A (en) * | 1997-02-20 | 2000-08-15 | Oxis International, Inc. | Methods and compositions for the protection of mitochondria |
US6479533B1 (en) | 1997-02-20 | 2002-11-12 | Applied Genetics Incorporated Dermatics | Methods and compositions for the protection of mitochondria |
WO2001087260A1 (en) * | 2000-05-18 | 2001-11-22 | L'oreal | Use of ergothioneine and/or its derivatives as anti-pollution agent |
FR2809000A1 (en) * | 2000-05-18 | 2001-11-23 | Oreal | The use of ergothionine and its derivatives in cosmetic compositions to protect against pollution, especially toxic gases and ozone |
FR2810548A1 (en) * | 2000-06-26 | 2001-12-28 | Oreal | USE OF ERGOTHIONEIN AND / OR ITS DERIVATIVES AS AN ANTI-GLYCATION AGENT |
EP1166768A1 (en) * | 2000-06-26 | 2002-01-02 | L'oreal | Use of ergothioneine and its derivatives as a glycation inhibitor |
WO2006124992A1 (en) * | 2005-05-17 | 2006-11-23 | The Procter & Gamble Company | Regulation of mammalian keratinous tissue using personal care compositions comprising ergothioneine |
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