植物皮肤脱色剂的研究进展

植物皮肤脱色剂的研究进展ResearchAndDevelopmentOnPhyto-activesForSkinDepigmentation美与白

Beautyandwhitening肤色决定因素皮肤内色素Pigmentsinskin黑素Melanin类胡萝卜素Carotenoid血红蛋白比例Ratioofhemoglobin皮肤厚薄Thicknessofskin表皮Epidermis真皮DermisCriticalfactorsforskincolor

表皮黑素细胞的原子力显微镜观察Observationofepidermalmelanocytesunderatomforcemicroscope(AFM)矛盾Conflicts化学剂-----天然植物Chemicalreagents naturalplants汞剂

Mercurials氢醌

Hydroquinone糖皮质激素

Glucocorticoids效果好，安全性差

Goodinefficacy，butbadinsafety研究流程1.植物筛选Plantscreening

酪氨酸活性测定-蘑菇酪氨酸酶、人酪氨酸酶多巴色素自动氧化生成黑素测定

Tyrosinaseactivitymeasurement-mushroomtyrosinaseand humantyrosinase

Dopamelaninautooxidationandmelaninformationmeasurement2.有效性安全性验证Efficacyandsafetytests黑素瘤细胞培养Melanomacellculture人表皮黑素细胞培养Humanmelanocytesculture豚鼠皮肤试验Guineapigskintest人临床效果观察Humanclinicalstudyandobservation3.活性基团，开发新药ActivegroupsandnewdrugdevelopmentStudyscheme酪氨酸

多巴酪氨酸酶

多巴醌

谷胱甘肽or半胱氨酸

多巴色素半胱氨酰多巴

TRP-25，6-二羟吲哚5，6-二羟吲哚-2-羧酸

(DHI)(DHICA)

TRP-1

DHI多聚体DHICA多聚体优黑素褐黑素TRP-1（多巴色素互变异构酶）TRP-2（5，6-二羟吲哚-2-羟酸聚合酶）主要机制

Primarymechanisms直接或间接抑制酪氨酸酶 Directorindirectinhibitioneffectontyrosinase还原剂和活性氧族

Reducingreagentandreactiveoxygenspecies降解酪氨酸酶

Tyrosinasedegradation抑制黑素体转运

Inhibitionofmelanosometransportation抑制炎症引起的合成黑素反应

Inhibitionofinflammationinducedmelaninsynthesis加速表皮更新

Accelerateturnoverrateofepidermis直接或间接抑制酪氨酸酶

Directorindirectinhibitioneffectontyrosinase

熊果苷Arbutin

(熊果、沙梨树叶)(Arctostaphylosuva-ursiL. Spreng;P.pyrifolia(Burm.)Nakaitreeleaves)

芦荟苦素Aloesin

(芦荟,Aloe)

甲酯龙胆酸2,5-Methylhydroxybenzoicacid(Gentisic methyl)

(龙胆)(GentianascabraBge)

生物类黄酮Bioflavonoid

山奈酚（银杏）Kaempferol(Gingko) 芹菜素（芹菜）OleanolicAcid/Apigenin(Celery) 柚皮素（柚）Naringenin(CitrusgrandisL.Osbeck)

熊果苷(arbutin)抑制酪氨酸酶活性

Inhibitionoftyrosinaseactivity抑制TRP-2活性

InhibitiononTRP-2activity有效性Efficacy:

黑素瘤细胞Melanoma人黑素细胞Humanmelanocytes动物模型Animalmodels人体临床试验Humanclinicalstudy熊果Arctostaphylosuva-ursiL.Spreng熊果苷Arbutin熊果苷--------- (Arbutin)Alpha-熊果苷-------- (Alpha-arbutin)脱氧熊果苷----------- (Deoxyarbutin)芦荟苦素(aloesin)竞争性抑制多巴氧化

Competetivelyinhibitondopaoxidation非竞争性抑制酪氨酸酶羟化

Non-competetivelyinhibittyrosinasehydroxidation龙胆酯酸

2,5-MethylHydroxybenzoicacid(Gentisicmethyl)草原龙胆Eustomaressellianum2,5-Methylhydroxybenzoicacid(Gentisicmethyl)

有效---选择性抑制酪氨酸酶,可能和铜离子鳌合相关

Ineffect---Selectivelyinhibittyrosinaseand maychelatewithcopperions安全---减轻氢醌的细胞毒性对哺乳动物细胞无致畸性

Safe---Reducecytotoxicityby hydroquinoneandnoteratogenicity

on mammaliancells生物类黄酮(bioflavonoid)银杏Gingko(GinkgobilobaL.)金银花Honeysuckle(LonicerajaponicaThunb)

芸香科豆科伞形科银杏科菊科RutaceaeLeguminosaeUmbelliferaeGinkgoaceaeAsteraceae黄酮醇---螯合铜离子，竞争性抑制酪氨酸酶活性

Flavonol---Chelatecopperionsandcompetetivelyinhibittyrosinaseactivity黄酮---非竞争性抑制酪氨酸酶活性

Flavone---Non-competetivelyinhibittyrosinaseactivity异黄酮---效果差

Isoflavone---Donothavegoodeffect兼有清除自由基的酪氨酸酶抑制剂

Tyrosinaseinhibitorwithfreeradicalscavengerfunction

多酚类Polyphenols——

鞣花酸（石榴皮）Ellagicacid(megranateskin) 白藜芦醇（葡萄酒）Resveratrol

(Wine) 茶多酚（绿茶）Teapolyphenol(Greentea) 原花青素（葡萄籽）Procyanidins(Grapeseed)

桑辛素F（桑科）

MoracinF(Moraceae)鞣花酸(ellagicacid)非竞争性抑制酪氨酸酶

Non-competetivelyinhibittyrosinaseactivity清除氧自由基

Eliminateoxidativefreeradicals豚鼠试验

Guineapigstudy石榴Megranate白藜芦醇(Resveratrol)竞争性抑制

Competetiveinhibition桑树Mulberry---氧化白藜芦醇(oxyresveratrol)更强抑制DOPA氧化话性oxyresveratrolhavestrongerinhibitioneffectonDOPAoxidativeactivity虎杖PolygonumcuspidatumSieb茶多酚Teapolyphenol绿茶Greentea表没食子儿茶素没食子酸酯（EGCG) (-)-epigallocatechin-3-gallate(EGCG)绿茶Greentea其它多酚Otherpolyphenols原花青素

Procyanidins构树(papermulberry)

桑白桑科树根皮提纯-桑辛素F抑制酪氨酸酶

Moraceae

treerootsandskinextracts-MoracinF Inhibitionoftyrosinase

清除氧自由基

Eliminatefreeradicals构树PapermulberryBroussonetiapapyrifera(Linn.)Vent.还原剂和活性氧族

Reducingagentsandreactiveoxygenspeciesα－生育酚（植物油、坚果、日本山椒）

α-tocopherols(vegetableoils,nuts,ZanthoxylumJaponica)抑制黑素细胞膜脂质过氧化反应

Inhibitiononmelanocytelipidmembraneperoxidation

降解酪氨酸酶

Tyrosinasedegradation不饱和脂肪酸Unsaturatedfattyacids激活酪氨酸酶降解酶Activationondegradationenzymesoftyrosinase抑制黑素体转运

Inhoibitiononmelanosometransportation

大豆Soybean：

两种丝氨酸蛋白酶抑制剂 Twokindsofserineproteaseinhibitors

Bowman-Birk胰蛋白酶抑制剂(BBI)

Bowman-Birktrypsininhibitor(BBI)

大豆胰蛋白酶抑制剂(STI)

Soybeantrypsininhibitor(STI)干扰蛋白酶活化受体-2途径

Interferewithproteaseactivated receptor-2(PAR-2)pathway

烟酰胺(niacinamide)抑制黑素体转运

Inhibitiononmelanosometransportation抗糖基化

Anti-advancedglycation抑制炎症引起的合成黑素反应

Inhibitionofinflammationinducedmelaninsynthesis

药用蜀葵---影响内皮素ET-1 Alcearosea---affect endothelin-1(ET-1)

独行菜(Lepidiumapetalum)---通过IL-6下调MITF

Peppergrass(Lepidium apetalum)---downregulateMITFthroughIL-6

应用----预防紫外线引起炎症性色斑

Application----preventUV-inducedpostinflammatoryhyperpigmenation独行菜Peppergrass蜀葵Hollyhock(Alcearosea)甘草提取物(licoriceextract)甘草黄酮-抗炎

licoflavone-anti-inflamation甘草黄苷-表皮更新

epidermalturnover/renewal甘草Licorice加速表皮更新

Accelerateturnoverrate/renewalsofepidermis 果酸（乳酸、苹果酸） Fruitacids(lacticacid,malicacid) 甘草黄苷（甘草） 甘草黄苷(licorice) 亚油酸、亚麻酸 linoleicacid、LinolenicAcid

中药研究

TraditionalChinesemedicineresearches筛选:300种醇和水提取物

Screening:alcoholandwatersoluble