JPH0418026A - Testosterone 5 alpha-reductase inhibitor - Google Patents
Testosterone 5 alpha-reductase inhibitorInfo
- Publication number
- JPH0418026A JPH0418026A JP2119057A JP11905790A JPH0418026A JP H0418026 A JPH0418026 A JP H0418026A JP 2119057 A JP2119057 A JP 2119057A JP 11905790 A JP11905790 A JP 11905790A JP H0418026 A JPH0418026 A JP H0418026A
- Authority
- JP
- Japan
- Prior art keywords
- testosterone
- hair
- alpha
- cosmetic
- extracted solutions
- 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.)
- Granted
Links
- 108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 title claims abstract description 18
- 102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 title claims abstract description 18
- 229940113178 5 Alpha reductase inhibitor Drugs 0.000 title claims abstract 3
- 239000002677 5-alpha reductase inhibitor Substances 0.000 title claims abstract 3
- 244000025221 Humulus lupulus Species 0.000 claims abstract description 5
- 241000086254 Arnica montana Species 0.000 claims abstract 2
- 235000008694 Humulus lupulus Nutrition 0.000 claims abstract 2
- 235000004357 Mentha x piperita Nutrition 0.000 claims abstract 2
- 241001479543 Mentha x piperita Species 0.000 claims abstract 2
- 239000001771 mentha piperita Substances 0.000 claims abstract 2
- 241001529742 Rosmarinus Species 0.000 claims description 9
- 239000000469 ethanolic extract Substances 0.000 claims description 6
- 235000017309 Hypericum perforatum Nutrition 0.000 claims description 4
- 244000141009 Hypericum perforatum Species 0.000 claims description 4
- 244000042664 Matricaria chamomilla Species 0.000 claims description 4
- 235000007232 Matricaria chamomilla Nutrition 0.000 claims description 4
- 235000007866 Chamaemelum nobile Nutrition 0.000 claims description 3
- 235000017276 Salvia Nutrition 0.000 claims description 2
- 235000002020 sage Nutrition 0.000 claims description 2
- 241000218228 Humulus Species 0.000 claims 1
- 235000017945 Matricaria Nutrition 0.000 claims 1
- 241000275031 Nica Species 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 23
- 230000015572 biosynthetic process Effects 0.000 abstract description 8
- 239000002537 cosmetic Substances 0.000 abstract description 8
- 206010000496 acne Diseases 0.000 abstract description 7
- 230000002401 inhibitory effect Effects 0.000 abstract description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 6
- 239000000284 extract Substances 0.000 abstract description 5
- 239000003795 chemical substances by application Substances 0.000 abstract description 2
- 239000003814 drug Substances 0.000 abstract description 2
- 239000000843 powder Substances 0.000 abstract description 2
- 238000002360 preparation method Methods 0.000 abstract description 2
- 210000002374 sebum Anatomy 0.000 abstract description 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 241000782597 Hypericum erectum Species 0.000 abstract 1
- 240000007164 Salvia officinalis Species 0.000 abstract 1
- 235000002912 Salvia officinalis Nutrition 0.000 abstract 1
- 241001530490 Salvia rosmarinus Species 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 235000008216 herbs Nutrition 0.000 abstract 1
- 235000015639 rosmarinus officinalis Nutrition 0.000 abstract 1
- 239000001296 salvia officinalis l. Substances 0.000 abstract 1
- 230000001256 tonic effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 description 13
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 10
- 239000012676 herbal extract Substances 0.000 description 9
- 230000036425 denaturation Effects 0.000 description 7
- 238000004925 denaturation Methods 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- 210000003491 skin Anatomy 0.000 description 6
- 208000002874 Acne Vulgaris Diseases 0.000 description 5
- 102000004169 proteins and genes Human genes 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- 229960003604 testosterone Drugs 0.000 description 5
- 201000004384 Alopecia Diseases 0.000 description 4
- 230000003054 hormonal effect Effects 0.000 description 4
- 150000002632 lipids Chemical class 0.000 description 4
- 210000000056 organ Anatomy 0.000 description 4
- 210000001732 sebaceous gland Anatomy 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000007795 chemical reaction product Substances 0.000 description 3
- 238000004817 gas chromatography Methods 0.000 description 3
- 229940088597 hormone Drugs 0.000 description 3
- 239000005556 hormone Substances 0.000 description 3
- 239000001632 sodium acetate Substances 0.000 description 3
- 241000208983 Arnica Species 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 240000002657 Thymus vulgaris Species 0.000 description 2
- 235000007303 Thymus vulgaris Nutrition 0.000 description 2
- 231100000360 alopecia Toxicity 0.000 description 2
- 206010068168 androgenetic alopecia Diseases 0.000 description 2
- 210000004207 dermis Anatomy 0.000 description 2
- 210000002615 epidermis Anatomy 0.000 description 2
- 230000003779 hair growth Effects 0.000 description 2
- 231100000508 hormonal effect Toxicity 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 231100000957 no side effect Toxicity 0.000 description 2
- 239000012488 sample solution Substances 0.000 description 2
- JHJLBTNAGRQEKS-UHFFFAOYSA-M sodium bromide Chemical compound [Na+].[Br-] JHJLBTNAGRQEKS-UHFFFAOYSA-M 0.000 description 2
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 2
- 239000001585 thymus vulgaris Substances 0.000 description 2
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 1
- 229930182816 L-glutamine Natural products 0.000 description 1
- 108010058846 Ovalbumin Proteins 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
- 108090000854 Oxidoreductases Proteins 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 244000178231 Rosmarinus officinalis Species 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- APKFDSVGJQXUKY-INPOYWNPSA-N amphotericin B Chemical compound O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 APKFDSVGJQXUKY-INPOYWNPSA-N 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 230000002280 anti-androgenic effect Effects 0.000 description 1
- 239000000051 antiandrogen Substances 0.000 description 1
- 230000008687 biosynthesis inhibition Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000012159 carrier gas Substances 0.000 description 1
- 210000000845 cartilage Anatomy 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- OSVXSBDYLRYLIG-UHFFFAOYSA-N chlorine dioxide Inorganic materials O=Cl=O OSVXSBDYLRYLIG-UHFFFAOYSA-N 0.000 description 1
- 235000019398 chlorine dioxide Nutrition 0.000 description 1
- QBWCMBCROVPCKQ-UHFFFAOYSA-N chlorous acid Chemical compound OCl=O QBWCMBCROVPCKQ-UHFFFAOYSA-N 0.000 description 1
- 238000012258 culturing Methods 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 239000003676 hair preparation Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 102000027411 intracellular receptors Human genes 0.000 description 1
- 108091008582 intracellular receptors Proteins 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229940092253 ovalbumin Drugs 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 230000002250 progressing effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 1
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 1
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000001430 tilia cordata extract Substances 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Landscapes
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
【発明の詳細な説明】
〈産業上の利用分野〉
本発明は、育毛・養毛、ニキビ用の化粧料や医薬品等に
応用可能で、かつ副作用のない、テストステロン 5α
−リダクターゼ阻害剤に関する。[Detailed Description of the Invention] <Industrial Application Field> The present invention provides testosterone 5α, which can be applied to cosmetics and pharmaceuticals for hair growth/nourishment and acne, and has no side effects.
-Relating to reductase inhibitors.
〈従来の技術〉
男性型禿頭や脱毛症、あるいはO漏、ニキビ(尋常性ざ
f)等は、男性ホルモンの過剰によるといわれている。<Prior Art> Male pattern baldness, alopecia, O leakage, acne (acne vulgaris), etc. are said to be caused by an excess of male hormones.
特に、毛根、皮脂腺等の器官におけるこの男性ホルモン
活性の本体は、これら標的器官においてテストステロン
がテストステロン5α−リダクターゼ(TSR)によっ
て還元されて生νVする、5α−ジヒドロテストステロ
ンCD HT )であることが知られている。すなわち
、精巣や副腎で生合成され分泌されたテストステロン(
男性ホルモン)は、血流によって皮脂腺に到達し、皮I
l¥1腺細胞中のTSRによってDHTに変換される。In particular, it is known that the main body of this androgen activity in organs such as hair roots and sebaceous glands is 5α-dihydrotestosterone (CDHT), which is produced by reducing testosterone to νV by testosterone 5α-reductase (TSR) in these target organs. It is being In other words, testosterone (
Male hormones) reach the sebaceous glands through the bloodstream and
Converted to DHT by TSR in l\1 gland cells.
このD HTは細胞内の受容体と結合し、核に作用して
皮脂腺細胞の増殖を促す一方1毛母細胞にも作用してそ
の細胞分裂を抑制し、毛の成長を妨げるものとされてい
る。This DHT binds to intracellular receptors and acts on the nucleus to promote the proliferation of sebaceous gland cells, while also acting on hair matrix cells to suppress their cell division and impede hair growth. There is.
従来、男性型禿頭や脱毛症またはニキビ等の治療には、
エストラジオール等の女性ホルモン作用を有する物質や
、酢酸シブロチロン等の抗男性ホルモン作用を有する物
質5強い酸化力を有する物質(ClO2等)が用いられ
ていた。また、上記のテストステロンの作用機序に着目
し、TSR活性を阻害する物質の研究も進められている
。Traditionally, treatments for male pattern baldness, alopecia, acne, etc.
Substances with female hormone effects, such as estradiol, and substances with anti-androgen effects, such as cybrothyrone acetate5, have been used.5 Substances with strong oxidizing power (such as ClO2) have been used. Furthermore, focusing on the above-mentioned mechanism of action of testosterone, research on substances that inhibit TSR activity is also progressing.
〈発明が解決しようとする11g>
しかし、ホルモン剤や酸化剤は副作用や安全性の面で問
題があり、化粧料への配合が不可能なものや、医師の管
理下でのみ使用が可能なものばかりであった、
また、TSR活性を阻害する物質として報告されている
ものも、その作用・効果が不十分であったり、安全性が
十分でなかったり、あるいはコスト的に高価であったり
と、種々の問題が存在するわく課題を解決するための手
段〉
我々は長年にわたり、副作用や安全性の面で問題がなく
、化粧料等に配合の可能な薬草抽出物のスクリーニング
を行ってきた。そして上記の課題についても、特定の薬
草抽出物の応用が有効であることを見い出した。<11g that the invention seeks to solve> However, hormones and oxidizing agents have problems in terms of side effects and safety, and they cannot be incorporated into cosmetics or can only be used under the supervision of a doctor. In addition, the substances that have been reported to inhibit TSR activity may not have sufficient action or efficacy, may not be safe enough, or may be expensive. For many years, we have been screening medicinal herbal extracts that have no side effects or safety issues and can be incorporated into cosmetics. We have also found that the application of specific medicinal herbal extracts is effective in solving the above problems.
すなわち、薬草のri燥粉末を99,5%または50″
Lエタノールに1g八へmlの割合で各々浸漬し、1週
間静置した後ろ過し、ろ液を分離してTSR活性を訓べ
た、その結果、セージ(Salvia officin
alisL、)、ホップ (Hu tIlu 1 u
s 4 L 、 )、ローズマリー(Rosmarin
us officinalis し、)、オトギリソウ
(ijz: erectum Thunj、)、ノ\ツ
カ(10−tha 紅■旦9L、) 、 カミツレ(
Matricariachど蛋用り、)、アルニカ(^
−…μ卯nta。! L、) 。i.e. 99,5% or 50″ of medicinal herbal ri powder
They were immersed in L ethanol at a ratio of 1 g to 8 ml, allowed to stand for one week, filtered, and the filtrate was separated to study TSR activity. As a result, sage (Salvia officin)
alisL, ), hop (Hu tIlu 1 u
s 4 L, ), Rosemary (Rosmarin)
us officinalis (), Hypericum perforatum (ijz: erectum Thunj,), Not\Tsuka (10-tha), Chamomile (
Matricariach for dogs,), Arnica (^
-...μu nta. ! L.).
タイム(辻■胚腹1■nL、)の各エタノール抽出物が
有効であることを見い出した。It was found that ethanol extracts of thyme (Tsuji 1 nL) were effective.
〈作用〉
表1に上記薬草抽出物のTSR活性活性阻害薬びタンパ
ク変性率を示す。<Effect> Table 1 shows the TSR activity inhibition and protein denaturation rates of the above medicinal herb extracts.
TSR液として、ラット肝臓のホモジネートの9 、0
00x g上清(S−9)を用いた。まず、テストステ
ロン 3μmをプロピレングリコール10滴に溶解し、
Tris−HC1緩衝液(pH7,2) 5 ml
を加える。これに、〜ADP)l 5mg、 S −
91ml、 Mび薬草抽出物0.5r+1を加え、37
℃で30分間インキュベートした後、ジクロロメタン5
0m1を加えて反応を停止させ、ジクロロメタン層を分
取し減圧乾燥した後、ガスクロマトグラフィー(GC)
にて反応生成物であるDHT、アントロスタンジオール
等を検出定量した(GC条件:カラム; ULBON
HR−1,キャリアーガス; He 20m1/l1l
in、カラム温度;200℃)、、TSR活性活性阻害
薬草抽出物無添加時(コントロール)の反応生成物量と
、薬草抽出物添加時の反応生成物量の比較により求めた
。9,0 of rat liver homogenate as TSR solution.
00xg supernatant (S-9) was used. First, dissolve 3 μm of testosterone in 10 drops of propylene glycol.
Tris-HC1 buffer (pH 7,2) 5 ml
Add. To this, ~ADP)l 5mg, S-
91ml, add 0.5r+1 of Mibi herbal extract, 37ml
After incubation for 30 min at °C, dichloromethane 5
0ml was added to stop the reaction, the dichloromethane layer was separated and dried under reduced pressure, and then subjected to gas chromatography (GC).
The reaction products DHT, anthrostanediol, etc. were detected and quantified (GC conditions: column; ULBON
HR-1, carrier gas; He 20ml/l1l
in, column temperature: 200°C), by comparing the amount of the reaction product when the TSR activity-inhibiting herbal extract was not added (control) and the amount of the reaction product when the herbal extract was added.
一方、タンパク変性率は、0.02%卵白アルブミンを
含む0.15M硫酸ナトリウム/ 0.05Mリン酸緩
衝液(pH7,0) 9 mlに薬草抽出物1mlを加
え、5分間攪拌した後、メンブランフィルタ−でろ過し
、高速液体クロマトグラフィー(カラム: TSK−g
el G−30005W)でアルブミンを定量して求め
た。On the other hand, the protein denaturation rate was determined by adding 1 ml of medicinal herbal extract to 9 ml of 0.15 M sodium sulfate/0.05 M phosphate buffer (pH 7.0) containing 0.02% ovalbumin, stirring for 5 minutes, and then removing the membrane. Filter with a filter and perform high performance liquid chromatography (column: TSK-g
el G-30005W).
No、1〜8の各薬草抽出物については、99.5%あ
るいは50χエタノールのいずれの抽出物も高いTSR
S性活性阻害率した。これらのタンパク変性率は、ロー
ズマリー(No、3)の99.5%エタノール抽出物及
びオトギリソウ(No、4)の50%エタノール抽出物
において若干高い値を示したものの、概ね低い値であっ
た。従って、これら薬草抽出物は高いTSR活性阻害作
用を示し、かつこの作用は酵素タンパク質の変性による
ものではなかった。For each herbal extract No. 1 to 8, either the 99.5% or 50χ ethanol extract has a high TSR.
S activity inhibition rate was calculated. Although these protein denaturation rates were slightly higher in the 99.5% ethanol extract of rosemary (No. 3) and the 50% ethanol extract of Hypericum perforatum (No. 4), they were generally low values. . Therefore, these medicinal herb extracts exhibited a high TSR activity inhibiting effect, and this effect was not due to denaturation of the enzyme protein.
No、9のリンデン抽出物はTSRS性活性阻害率いも
のの、タンパク変性率も92.21%と大きく、酵素タ
ンパク質の変性による阻害作用を有すると思われ、我々
の目的には好ましくない。Although linden extract No. 9 has a high inhibition rate of TSRS activity, the protein denaturation rate is as high as 92.21%, and it seems to have an inhibitory effect due to denaturation of enzyme protein, which is not preferable for our purposes.
No、 1(1−15の各薬草抽出物については、有
意なTSR活性阻害作用は認められなかった。No significant TSR activity inhibition effect was observed for each herbal extract No. 1 (1-15).
なお、この測定系においてエタノールの影響は認められ
なかった。Note that no influence of ethanol was observed in this measurement system.
さらに、上記8種の薬草抽出物中には、皮脂腺の+Il
I質生合成を抑制する作用を示すものが存在する。すな
わち、10週令のゴールデンノ1ムスターの耳介皮膚の
器官培養において、FiI質生合成の阻害がHめられた
。器官培養はハム入ター耳介皮膚片(6mmφ)より内
側皮膚を剥離して軟骨を除去した後、 [!4C]−酢
酸ナトリウム4.4μCiと試料液20μ】を添加した
培養液(10%FMS含有Eagle MEM培地にペ
ニシリン、ストレプトマイシン、ファンギゾン、L−グ
ルタミンを添加したもの)2mlに表皮側が上になるよ
うに浮かせて、37℃で6時間行った。対照としてもう
一方の耳介皮膚を、試料液の代わりに溶媒のみを添加し
た培養液で培養した。Furthermore, the above eight medicinal herbal extracts contain +Il of sebaceous glands.
There are some substances that exhibit the effect of suppressing I biosynthesis. That is, in organ culture of the auricular skin of 10-week-old golden gnomes, inhibition of FiI biosynthesis was observed. For organ culture, after exfoliating the inner skin and removing the cartilage from a piece of Ham's ear skin (6 mm diameter), [! 4C] - 4.4 μCi of sodium acetate and 20 μC of sample solution] were added to 2 ml of culture solution (Eagle MEM medium containing 10% FMS with penicillin, streptomycin, fungizone, and L-glutamine added) so that the epidermis side was facing up. It was floated at 37°C for 6 hours. As a control, the other auricular skin was cultured in a culture solution to which only a solvent was added instead of the sample solution.
培養後、生理食塩水で洗浄し、2NNaBr液に入れて
37℃で1時間静置した後、真皮と表皮を分離し、得ら
れた真皮シートをクロロホルム:メタノール(2:l)
2mlに入れ、 12時間0質の抽出を行った、脂質
生合成の阻害率は、 [!4C]−酢酸ナトIJウムの
取り込み阻害率として求め、結果を第1図に示した。After culturing, the dermis was washed with physiological saline, placed in 2N NaBr solution, and allowed to stand at 37°C for 1 hour. The dermis and epidermis were separated, and the resulting dermal sheet was placed in chloroform:methanol (2:l)
The inhibition rate of lipid biosynthesis was extracted in 2 ml for 12 hours. The inhibition rate of uptake of 4C]-sodium acetate was determined and the results are shown in FIG.
ホップ(Hul!1ulus 7 L、)抽出液及びロ
ーズマリー(Rosmarinus officina
lis L、)抽出液においで顕著な取り込み抑制が認
められた。これらの抑制率は各々46.21%及び19
.89%であり、一般に脂質生合成を抑制するといわれ
るビタミンである塩酸ピリドキシンよりも高い抑制率を
示した。Hop (Hul!1ulus 7 L) extract and rosemary (Rosmarinus officina)
lis L.), remarkable inhibition of uptake was observed in the extract. These inhibition rates were 46.21% and 19%, respectively.
.. The inhibition rate was 89%, which was higher than that of pyridoxine hydrochloride, a vitamin that is generally said to inhibit lipid biosynthesis.
この脂質生合成抑制作用は、TSR活性阻害を介する可
能性が高い。This inhibitory effect on lipid biosynthesis is likely to be mediated by inhibition of TSR activity.
また、一般に、培養系における[“4Clラベル物質取
り込みによる生合成実験では、ホルモン作用による生合
成の促進、抑制は培養後12時間以上経過しないと出現
しないことが知られている(v。In addition, it is generally known that in biosynthesis experiments using 4Cl-labeled substance incorporation in culture systems, the promotion or inhibition of biosynthesis due to hormonal action does not appear until 12 hours or more have passed after culture (v.
Wheatly and J、 Br1nd
; J、 Invest、 Der+natol
。Wheatly and J, Br1nd
; J, Invest, Der+natol
.
76293−296.1981)。従って、上記の作用
はホルモン作用を介するものではなく1重篤な副作用の
生ずる心配がない、
く効果〉
以上のように、セージ(Salvia officin
alisL、3 、 ホップ (f(umulus
□ L、) 、 ローズマリー(Rosmarinu
s officinalis L、)、 オトギリソ
ウ(L田七」erectu+n Thunb、)、ハツ
カ(Ros−tha pj2erjja L、)、カミ
ツレ(F+atricaria値ζF−9吋11旦り、
)、アルニカ(^unjcaユ律ユL、)、タイム(■
□hx=u≦7 L 、 )のエタノール抽出物は、T
SR阻害作用及び皮脂生成抑制作用を示す5 従って、
これらより1種または2種以上を選択してTSR阻害剤
として、養毛・育毛剤あるいは毛髪用化粧料、またはニ
キビ治療用皮膚外用剤や皮膚化粧料に配合することがで
きる。その際、上記作用がタンパク変性作用やホルモン
作用によるものではないので、皮膚に対するll’1l
ltや副作用のない安全な化粧料等を提供することがで
きる。76293-296.1981). Therefore, the above-mentioned effects are not mediated by hormonal effects, and there is no need to worry about serious side effects.
alisL, 3, hop (f(umulus
□ L, ), Rosemary (Rosmarinu)
s officinalis L,), Hypericum perforatum (Ltanachi"erectu+n Thunb,), Ros-tha pj2erjja L,), Chamomile (F+atricaria value ζF-9 x 11 d),
), arnica (^unjca yuritsuyu L,), thyme (■
The ethanol extract of □hx=u≦7L, ) is T
5 showing SR inhibiting effect and sebum production suppressing effect, therefore,
One or more of these can be selected as a TSR inhibitor and incorporated into hair nourishing/growth agents or hair cosmetics, or external skin preparations for treating acne or skin cosmetics. At that time, since the above effects are not due to protein denaturation or hormonal effects,
It is possible to provide safe cosmetics and the like that are free from LT and side effects.
I!1図は脂質生合成の阻害率を表すj!4C]−酢酸
ナトリウムの取り込み阻害を示す図である。
特許出願人 株式会社 ノエビアI! Figure 1 shows the inhibition rate of lipid biosynthesis. 4C]-sodium acetate uptake inhibition. Patent applicant Noevir Co., Ltd.
Claims (1)
L.)、ホップ(¥Humulus¥¥lupulus
¥L.)、ローズマリー(¥Ros¥−¥marinu
s¥¥officinalis¥L.)、オトギリソウ
(¥Hy¥−¥pericum¥¥erectum¥¥
Thunb¥.)、ハッカ(¥Menthapiper
ita¥L.)、カミツレ(¥Matricaria¥
¥chamomi−lla¥L.)、アルニカ(¥Ar
nica¥¥montana¥L.)、タイム(¥Th
ymus¥¥vulgaris¥L.)のエタノール抽
出物より選択した、1種または2種以上よりなるテスト
ステロン5α−リダクターゼ阻害剤。Sage (¥Salvia¥¥officinalis¥
L. ), hops (¥Humulus¥¥lupulus
¥L. ), rosemary (¥Ros¥-¥marinu
s¥¥officinalis¥L. ), Hypericum perforatum (\Hy\-\pericum\\erectum\\
Thunb¥. ), Menthapiper
ita¥L. ), chamomile (¥Matricaria¥
¥chamomi-lla¥L. ), arnica (¥Ar
nica¥¥montana¥L. ), Time (\Th
ymus¥¥vulgaris¥L. ) A testosterone 5α-reductase inhibitor consisting of one or more kinds selected from the ethanol extracts of.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2119057A JPH0647554B2 (en) | 1990-05-09 | 1990-05-09 | Testosterone 5α-reductase inhibitor |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2119057A JPH0647554B2 (en) | 1990-05-09 | 1990-05-09 | Testosterone 5α-reductase inhibitor |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH0418026A true JPH0418026A (en) | 1992-01-22 |
JPH0647554B2 JPH0647554B2 (en) | 1994-06-22 |
Family
ID=14751840
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2119057A Expired - Fee Related JPH0647554B2 (en) | 1990-05-09 | 1990-05-09 | Testosterone 5α-reductase inhibitor |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPH0647554B2 (en) |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0873324A (en) * | 1994-09-06 | 1996-03-19 | Kao Corp | Hair-tonic and hair-growing agent |
WO1996039157A1 (en) * | 1994-11-08 | 1996-12-12 | Taisho Pharmaceutical Co., Ltd. | TESTOSTERONE 5α-REDUCTASE INHIBITOR |
EP1023889A1 (en) * | 1999-01-29 | 2000-08-02 | Revlon Consumer Products Corporation | A hair lotion for preventing hair loss comprising extracts of hop, rosemary and Swertia, further containing silanodiol salicylate |
ES2157850A1 (en) * | 1999-12-28 | 2001-08-16 | Perdigon Jose Diaz | Natural capillary hair growth stimulator consists of e.g. arnica, white nettle and juniper extracts with incorporated alcohol and water |
CN1076380C (en) * | 1995-01-13 | 2001-12-19 | 金坚敏 | Efficient natural antioxidants and their preparation |
WO2002076410A3 (en) * | 2001-03-23 | 2003-09-25 | Beiersdorf Ag | Cosmetic and dermatological preparations comprising a content of a hop extract or hop-malt extract |
US6638523B1 (en) | 1999-10-27 | 2003-10-28 | Nagase & Company, Ltd. | Method of treating ulcers |
JP2006219407A (en) * | 2005-02-09 | 2006-08-24 | Maruzen Pharmaceut Co Ltd | Hair papilla cell proliferation promoter and hair tonic |
JP2015020949A (en) * | 2013-07-16 | 2015-02-02 | 日華化学株式会社 | HAIR COSMETIC AND SKIN COSMETIC CONTAINING PGD2 PRODUCTION INHIBITOR AND 5α-REDUCTASE ACTIVITY INHIBITOR |
JP2016006021A (en) * | 2014-06-20 | 2016-01-14 | 株式会社ノエビア | Thioredoxin-related factor expression promoter |
CN118557489A (en) * | 2024-07-31 | 2024-08-30 | 霸王(广州)有限公司 | Antibacterial oil control composition and preparation method and application thereof |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS4858114A (en) * | 1971-11-25 | 1973-08-15 | ||
JPS60146829A (en) * | 1984-01-05 | 1985-08-02 | Rooto Seiyaku Kk | Testosterone 5alpha-reductase inhibitor |
JPH0248516A (en) * | 1988-08-11 | 1990-02-19 | Shiseido Co Ltd | Hair tonic |
JPH03188013A (en) * | 1989-12-15 | 1991-08-16 | Shiseido Co Ltd | Testosterone-5alpha-reductase inhibitor |
-
1990
- 1990-05-09 JP JP2119057A patent/JPH0647554B2/en not_active Expired - Fee Related
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS4858114A (en) * | 1971-11-25 | 1973-08-15 | ||
JPS60146829A (en) * | 1984-01-05 | 1985-08-02 | Rooto Seiyaku Kk | Testosterone 5alpha-reductase inhibitor |
JPH0248516A (en) * | 1988-08-11 | 1990-02-19 | Shiseido Co Ltd | Hair tonic |
JPH03188013A (en) * | 1989-12-15 | 1991-08-16 | Shiseido Co Ltd | Testosterone-5alpha-reductase inhibitor |
Cited By (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0873324A (en) * | 1994-09-06 | 1996-03-19 | Kao Corp | Hair-tonic and hair-growing agent |
WO1996039157A1 (en) * | 1994-11-08 | 1996-12-12 | Taisho Pharmaceutical Co., Ltd. | TESTOSTERONE 5α-REDUCTASE INHIBITOR |
CN1076380C (en) * | 1995-01-13 | 2001-12-19 | 金坚敏 | Efficient natural antioxidants and their preparation |
EP1023889A1 (en) * | 1999-01-29 | 2000-08-02 | Revlon Consumer Products Corporation | A hair lotion for preventing hair loss comprising extracts of hop, rosemary and Swertia, further containing silanodiol salicylate |
ES2147538A1 (en) * | 1999-01-29 | 2000-09-01 | Revlon Consumer Prod Corp | A hair lotion for preventing hair loss comprising extracts of hop, rosemary and Swertia, further containing silanodiol salicylate |
US6638523B1 (en) | 1999-10-27 | 2003-10-28 | Nagase & Company, Ltd. | Method of treating ulcers |
ES2157850A1 (en) * | 1999-12-28 | 2001-08-16 | Perdigon Jose Diaz | Natural capillary hair growth stimulator consists of e.g. arnica, white nettle and juniper extracts with incorporated alcohol and water |
WO2002076410A3 (en) * | 2001-03-23 | 2003-09-25 | Beiersdorf Ag | Cosmetic and dermatological preparations comprising a content of a hop extract or hop-malt extract |
JP2006219407A (en) * | 2005-02-09 | 2006-08-24 | Maruzen Pharmaceut Co Ltd | Hair papilla cell proliferation promoter and hair tonic |
JP2015020949A (en) * | 2013-07-16 | 2015-02-02 | 日華化学株式会社 | HAIR COSMETIC AND SKIN COSMETIC CONTAINING PGD2 PRODUCTION INHIBITOR AND 5α-REDUCTASE ACTIVITY INHIBITOR |
JP2016006021A (en) * | 2014-06-20 | 2016-01-14 | 株式会社ノエビア | Thioredoxin-related factor expression promoter |
CN118557489A (en) * | 2024-07-31 | 2024-08-30 | 霸王(广州)有限公司 | Antibacterial oil control composition and preparation method and application thereof |
Also Published As
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---|---|
JPH0647554B2 (en) | 1994-06-22 |
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