WO2015078396A1 - 一种5α-还原酶抑制剂及其用途 - Google Patents

一种5α-还原酶抑制剂及其用途 Download PDF

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WO2015078396A1
WO2015078396A1 PCT/CN2014/092431 CN2014092431W WO2015078396A1 WO 2015078396 A1 WO2015078396 A1 WO 2015078396A1 CN 2014092431 W CN2014092431 W CN 2014092431W WO 2015078396 A1 WO2015078396 A1 WO 2015078396A1
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litchi
shell extract
weight
personal care
litchi shell
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PCT/CN2014/092431
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English (en)
French (fr)
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卢玲巧
祝乐
赵亚
向胜习
吕洛
戴竟
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上海家化联合股份有限公司
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Publication of WO2015078396A1 publication Critical patent/WO2015078396A1/zh

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

Definitions

  • the present invention relates to a traditional Chinese medicine having 5 ⁇ -reductase inhibitory action and its use in personal care products, in particular to litchi shell extract and its use in personal care products.
  • T Testosterone
  • DHT dihydrotestosterone
  • testosterone can be converted to dihydrotestosterone by 5 ⁇ -reductase, while dihydrotestosterone has an affinity of more than 5 times that of testosterone. Therefore, the increase or increase in the activity of 5 ⁇ -reductase may lead to the occurrence and deterioration of acne and hair loss.
  • Type I 5 ⁇ -reductase mainly exists in non-genital skin, hair follicle (hair bulb, fiber, lateral epithelial root sheath), sebaceous gland, liver, brain, mainly related to hirsutism, acne, male hair loss; type II 5 ⁇ -reductase mainly Expressed in the prostate, in the seminal vesicle, genital skin, hair follicle inner epithelial root sheath also existed, mainly related to some diseases caused by androgen disorders such as benign prostatic hyperplasia, polycystic ovary syndrome; type III 5 ⁇ -reductase expressed in the liver, The prostate, kidney, and skin are associated with N-linked nascent protein glycosylation.
  • type 1 5 ⁇ -reductase can be used as a molecular target for screening oil secretion, anti-acne and anti-hair loss effects.
  • Litchi shell the outer peel of Litchi Chinensis Sonn.
  • the lychee shell tastes bitter, cold, and enters the heart.
  • Chinese medicine believes that litchi shell has qi, analgesic, Shengjin, benefiting blood, treating polydipsia, collecting phlegm, attending dysentery, blood stasis, eczema; stomach pain, toothache, traumatic bleeding; stomach cramps, hernia, and women's blood stab.
  • litchi shell contains flavonoids, phenolic acids, polysaccharides and other ingredients, which have antioxidant, regulate lipid metabolism, anti-cancer, immune regulation, whitening and other functions in the body; in the existing patents related to litchi shell, reported Methods for obtaining certain components in litchi shells, such as a process for extracting root bark from litchi skin (CN201110219029.5), a method for extracting litchi polyphenols from litchi (CN200510093663.3), and phloretin powder Purification method (CN201010172018.1), a process for extracting proanthocyanidins (CN102898411A), a method for extracting and purifying phlorizin from litchi peel (CN102086220A), and the like.
  • a process for extracting root bark from litchi skin CN201110219029.5
  • a method for extracting litchi polyphenols from litchi CN200510093663.3
  • phloretin powder Purification method CN201010172018.
  • litchi pulp is a common food.
  • the litchi core is a traditional Chinese medicine that relies on qi and pain.
  • the utilization of litchi shell is still insufficient.
  • Litchi shells are usually cleaned directly as waste during litchi processing and consumption.
  • the inventors unexpectedly found that litchi shell has a good 5 ⁇ -reductase inhibitory effect, and can be developed into a cosmetic product for controlling oil, acne, and hair loss. Because of its low cost, wide source and good application prospects, it can also improve the current situation of waste of litchi shell resources. There is no report on the inhibitory effect of litchi shell on 5 ⁇ -reductase.
  • the present invention has found for the first time that litchi shell extract can be used as a nutraceutical for inhibiting oil secretion, anti-acne or anti-hair loss, and added to personal care products.
  • the object of the present invention is to provide a Chinese medicine extract having a 5 ⁇ -reductase inhibitory action, which can be added as an additive to a personal care product having the functions of inhibiting oil secretion, anti-acne or anti-hair loss. in.
  • Lychee shell extract can be extracted by:
  • Pure Chinese herbal medicines are thoroughly mixed with a certain amount of solvent, placed in an extractor, and extracted by the corresponding extraction method. After the end of the extraction, the solvent is recovered to obtain the extract powder, which is directly applied to the personal care product; the extract may be reconstituted with water or a solvent which can be added in the formulation of the personal care product such as glycerin or butylene glycol or propylene glycol or fat to a certain amount.
  • the concentration can also be added to the personal care product by adding an appropriate amount of preservative as needed.
  • the preparation of the litchi shell extract can also be carried out by supercritical extraction, subcritical extraction, and organic solvent extraction.
  • the solvent for organic solvent extraction includes medium and low polarity solvents such as n-hexane, ethyl acetate, diethyl ether, petroleum ether, acetone, and the like, and different concentrations of ethanol, methanol, and polyol.
  • the extraction method may be a method such as reflux extraction, impregnation, or osmosis.
  • ultrasonic or microwave methods can also be used for assisting during the extraction process.
  • the invention relates to the use of a litchi shell extract for the inhibition of 5 ⁇ -reductase.
  • the present invention relates to the use of a litchi shell extract as an additive having 5 ⁇ -reductase inhibitory action in the preparation of a personal care product having oil control anti-acne efficacy.
  • the present invention relates to the use of a litchi shell extract as an additive having 5 ⁇ -reductase inhibitory action in the preparation of a personal care product having anti-hair loss efficacy.
  • the litchi shell extract is used in an amount of from 0.0001% to 100%, preferably from 0.01% to 50%, more preferably from 0.1% to 10% by weight.
  • the personal care product of the present invention may be any dosage form acceptable to the skin or hair, including: facial cleansers, lotions, lotions, creams, gels, masks, shampoos, conditioners, hair care essences, soaps, but not limited to this.
  • the personal care product of the present invention comprises a litchi shell extract and an acceptable adjuvant.
  • the personal care product comprises from 0.0001 to 100% by weight of litchi shell extract. In another embodiment, the personal care product comprises from 0.01% to 50% by weight of litchi shell extract. In another embodiment, the personal care product comprises from 0.1% to 10% by weight of litchi shell extract.
  • Figure 1 shows the 5 ⁇ -reductive enzymatic reaction rates of normal, control, and different concentrations of litchi shell extract.
  • Figure 2 shows the inhibition rate of the 5 ⁇ -reductive enzymatic reaction of the positive control and the different concentrations of litchi shell extract.
  • litchi shell The inhibitory effect of litchi shell on 5 ⁇ -reductase has not been reported, and it is the first discovery. Moreover, the inventors unexpectedly found through experiments that the inhibition of 5 ⁇ -reductase by the litchi shell was remarkable. Litchi shells are widely available, safe and non-toxic, so consider an additive that can be used as an ideal personal care product. In addition, since the inventors unexpectedly discovered the inhibitory effect of the litchi shell extract on 5 ⁇ -reductase, the litchi shell extract can be used as an additive for preparing various personal care products having functions of inhibiting oil secretion, anti-acne, and hair loss prevention.
  • the inventors of the present invention have found after extensive and intensive research that the litchi shell extract has a 5 ⁇ -reductase inhibitory action.
  • litchi shell extract can be added to personal care products as an efficacy additive.
  • the present invention firstly proposes that the litchi shell extract has a 5 ⁇ -reductase inhibitory action and can be added as a functional additive to a personal care product, and as a personal care product additive added to a personal care product, it can function as an oil control or anti-decubitus, or It can prevent hair loss when added to hair care products.
  • litchi shell extract can be applied to human skin or facial cleanser, lotion, lotion, cream, gel, mask, shampoo, conditioner, hair care essence, soap, etc.
  • the dosage form of the hair can be applied to human skin or facial cleanser, lotion, lotion, cream, gel, mask, shampoo, conditioner, hair care essence, soap, etc.
  • the ingredients other than the litchi shell extract may be any ingredients required for the formulation of the personal care product, such as: water, ethanol, butylene glycol, propylene glycol, oils, emulsifiers, thickeners, preservatives, etc.; other functional ingredients may also be added Reaching complex functions, such as: adding moisturizing ingredients to become oil-control moisturizing personal care products, adding whitening ingredients to become acne whitening personal care products, adding anti-aging ingredients to become oil control anti-aging personal care products, adding scalp nourishing ingredients to nourish anti-off shampoo / Conditioner / hair care essence, add anti-dandruff agent to become oil control anti-dandruff shampoo / conditioner / hair care essence and so on.
  • other functional ingredients may also be added Reaching complex functions, such as: adding moisturizing ingredients to become oil-control moisturizing personal care products, adding whitening ingredients to become acne whitening personal care products, adding anti-aging ingredients to become oil control anti-aging personal care products, adding scalp nourishing ingredients to nourish anti-off shampoo / Conditioner
  • the litchi shell extract may be used in a concentration ranging from 0.0001% to 100% by weight.
  • the litchi shell extract is used in a concentration ranging from 0.01 to 50%. More preferably, the litchi shell extract may be used in a concentration ranging from 0.1% to 10%.
  • the litchi shell extract is used at a concentration of from 0.001% to 10% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.001% to 5% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.001% to 1% by weight. In one embodiment, the litchi shell extract is used at a concentration of from 0.01 to 10% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.01 to 5% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.01 to 1% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.1 to 10% by weight.
  • the litchi shell extract is used at a concentration of from 0.1 to 5% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.1 to 1% by weight. In another embodiment, the litchi shell extract is used at a concentration of from 0.1 to 0.5% by weight.
  • the litchi shell extract can be added to various personal care products in a ratio of 0.01-50% by weight.
  • the litchi shell extract may be used in an amount of 0.01 to 20% by weight, such as 0.01 to 10% by weight, for example 0.01 to 5% by weight.
  • the litchi shell extract can be added to various personal care products in a ratio of from 0.1 to 10% by weight.
  • the litchi shell extract is used in the personal care product in an amount of from 0.1 to 2% by weight.
  • the litchi shell extract is used in the personal care product in an amount of from 0.5 to 2% by weight.
  • the litchi shell extract prepared in Example 1 was dissolved and diluted to 5 concentration gradients with 45% (v/v) DMSO (Tris buffer 55%): 3.4% by weight, 1.7% by weight, 0.85% by weight, 0.43 % by weight, 0.21% by weight.
  • the 5 ⁇ -reductase inhibition experiment was carried out as follows.
  • the reaction system of the experimental platform was 1 ml, and the sample additive amount was 0.1 ml. Therefore, the initial concentration was 0.34% by weight of the crude drug, and the system concentrations were: 0.34% by weight, 0.17% by weight, 0.085% by weight, 0.043% by weight, and 0.021% by weight, respectively. Because the system contained 4.5% (v/v) DMSO, a 4.5% (v/v) DMSO solvent control was set at the same time, and 1 mg/L of dutasteride was used as a positive control.
  • the enzyme was extracted from the liver of SD rats and stored frozen for storage.
  • the enzyme reaction system contained the substrate testosterone (T), coenzyme NADPH, enzyme, enzyme reaction temperature of 37 ° C, pH of 7.
  • the reaction that does not involve any sample intervention is a normal enzymatic reaction, and the resulting reaction rate is the normal reaction rate.
  • the reaction rate after the addition of the sample was lowered as compared with the normal reaction rate, and the sample was considered to have an inhibitory effect.
  • reaction rate of the normal 5 ⁇ -reductive reaction The reaction rate of the normal 5 ⁇ -reductive reaction, the reaction rate after adding 1 mg/L of dutasteride as a positive control, the reaction rate after adding 4.5% (v/v) DMSO, and the enzyme after adding different concentrations of the sample
  • the reaction rate for promoting the reaction is shown below.
  • Extract additives to the product formula can play the role of oil control, acne or anti-hair loss.
  • Oil-control skin care water containing the litchi shell extract of the present invention was prepared according to the ingredients and amounts of Table 1.
  • Phase A water 95.58 glycerin 1.0 Lychee shell extract 0.8 EDTA-2Na 0.02 Phase B
  • Preparation method Weigh the three phases of A, B and C according to the above ratios, stir them separately, slowly add phase B to phase A while stirring, add phase C after stirring, stir and dissolve evenly to obtain oil-control skin care products.
  • An oil control acne cream comprising the litchi shell extract of the present invention was prepared according to the ingredients and amounts of Table 2.
  • Preparation method Hansheng gum was dispersed in water for 15 minutes, all ingredients in phase A were added and heated to 70-75 °C. Also weigh all the ingredients in phase B and heat to 75-80 °C. Add phase B to phase A, homogenize for 5 minutes, cool to 45 ° C, add phase C, stir well to obtain oil control acne cream.
  • An acne gel comprising the litchi shell extract of the present invention was prepared according to the ingredients and amounts of Table 3.
  • Preparation method Weigh A, B, C three phases according to the proportion, heat phase A to 70-75 ° C, stir and dissolve evenly, add phase B, stir evenly, cool to 30-35 ° C, add phase C, mix That is to get acne gel.
  • An oil control shampoo comprising the litchi shell extract of the present invention was prepared according to the ingredients and amounts of Table 4.
  • Preparation method the water is heated to 70-75 ° C, the components are added separately according to the proportion, stirred and dissolved uniformly, cooled to 30-35 ° C, added to the litchi shell extract, mixed to obtain oil control shampoo.

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Abstract

荔枝壳提取物作为5α-还原酶抑制剂的用途。荔枝壳提取物作为5α-还原酶抑制剂在制备具有控油和抗痤疮功效的个人护理产品中的用途。荔枝壳提取物作为具有5α-还原酶抑制剂在制备具有防脱发功效的个人护理产品中的用途。

Description

一种5α-还原酶抑制剂及其用途 技术领域
本发明涉及一种具有5α-还原酶抑制作用的中药及其在个人护理产品中的应用，具体涉及荔枝壳提取物及其在个人护理产品中的应用。
背景技术
痤疮、脱发都是临床常见的顽症，发生人群广泛，尽管痤疮、脱发疾病并不会危急生命，但常常给患者造成严重的精神负担。随着当今社会竞争日趋激烈，居住环境恶化，近年来痤疮、脱发发生率有上升的趋势，但目前用于痤疮、脱发的有效产品仍较匮乏。
导致痤疮、脱发的因素很多，但是现代医学认为局部雄激素代谢异常可能是最主要的病因。因为，雄激素过多可导致皮脂腺体积增大和皮脂分泌增多，毛囊皮脂腺导管角化异常，致皮脂排泄不畅，形成脂栓，引发痤疮；在头发方面，雄激素过度能促使头发毛囊萎缩，缩短头发的生长周期，导致头发细软、稀疏、脱落。睾酮(T)、二氢睾酮(DHT)是两种重要的内源性雄激素，都能与雄激素受体结合产生相应的生理作用。值得注意的是，睾酮可通过5α-还原酶转化成二氢睾酮，而二氢睾酮的亲和力是睾酮的5倍以上。所以，5α-还原酶活性增强或数量增多都可能导致痤疮、脱发的发生和恶化。
在人体内，已发现5α-还原酶3个亚型，研究较多的是1型和2型。Ⅰ型5α-还原酶主要存在于非生殖器皮肤、毛囊(毛球、纤维、外侧上皮根鞘)、皮脂腺、肝脏、大脑，主要与多毛症、痤疮、男性脱发相关；Ⅱ型5α-还原酶主要表达于前列腺，在精囊、生殖器皮肤、毛囊内侧上皮根鞘也有一定存在，主要与一些雄激素紊乱所致疾病如良性前列腺增生、多囊卵巢综合症有关；Ⅲ型5α-还原酶表达于肝脏、前列腺、肾脏、皮肤，与N-连接的初生蛋白糖基化有关。目前研究认为，痤疮、脱发与1型5α-还原酶最为相关，所以1型5α-还原酶可以作为控制油脂分泌、抗痤疮、防脱发功效成分筛选时的分子靶。
随着天然、安全与环保要求的提出，绿色个人护理产品越来越为人们所青睐。中药资源丰富，具有几千年的应用历史，具有天然安全的特点，所以开发中药来源的有效个人护理产品的添加剂，将得到消费者的欢迎。
荔枝壳，无患子科荔枝属植物荔枝(Litchi Chinensis Sonn.)的外果皮，是荔枝的副产物之一，容易获取、产量大，开发应用价值高。荔枝壳性味苦、寒，入心经。中医认为荔枝壳具有理气、止痛、生津、益血、治烦渴、收涩作用，主治痢疾，血崩，湿疹；胃痛、牙痛、外伤出血；胃脘痛、疝气痛、妇女血气刺痛等。根据文献报道，荔枝壳含有黄酮类、酚酸、多糖类等成分，具有抗氧化、调节体内脂质代谢、抗癌、免疫调节、美白等功能；在荔枝壳相关的现有专利中，报道了荔枝壳中某些成分的获取方法，如从荔枝皮中提取根皮甙的工艺(CN201110219029.5)、一种从荔枝中提取荔枝多酚的方法(CN200510093663.3)、根皮素粉剂的提纯方法(CN201010172018.1)、一种原花青素的提取工艺(CN102898411A)、一种荔枝果皮中根皮苷的提取和纯化方法(CN102086220A)等。也有学者对植物荔枝的另一药用部位做过一些研究，即荔枝的干燥成熟种子荔枝核，认为它具有降糖、降血脂、抗肿瘤、抗菌抗病毒等作用，在皮肤方面有抗氧化、抗衰老、抗糖化等功效公开，如专利3-脱氧葡糖醛酮的天然产物抑制剂(CN200980121805.2)，专利抗糖化剂(CN201010546567.0)。
荔枝果肉是常见食品，荔枝果核是一味理气止痛的中药材，目前对荔枝壳的利用还很不充分。在荔枝加工和消费过程中,荔枝壳通常作为废弃物直接清理掉。发明人在研究过程中，意外发现荔枝壳具有很好的5α-还原酶抑制作用，可以开发成作为控油、祛痘、防脱发的中草药添加剂应用于化妆品中。因为成本低廉，来源广泛，具有很好的应用前景，也可以改善荔枝壳资源浪费的现状。荔枝壳对5α-还原酶抑制作用尚无任何报道。本发明首次发现荔枝壳提取物可以作为抑制油脂分泌、抗痤疮或防脱发活性成分加入个人护理产品中使用。
发明内容
本发明目的在于提供一种具有5α-还原酶抑制作用的中药提取物，其可作为添加剂加入具有抑制油脂分泌、抗痤疮或防脱发功能的个人护理产品 中。
荔枝壳提取物可以通过以下方式提取：
纯正中药材，与一定配比用量的溶剂充分混合，放置于提取器中，用相应的提取方法进行提取。待提取结束后，回收溶剂得到提取物粉末，直接应用于个人护理产品；也可将提取物用水或甘油或丁二醇或丙二醇或油脂等个人护理产品配方中可添加的溶剂进行复溶至一定浓度，也可根据需要添加适量防腐剂，应用于个人护理产品。
荔枝壳提取物的制取也可采取超临界萃取、亚临界萃取、有机溶剂提取法。有机溶剂提取的溶剂包括正己烷、乙酸乙酯、乙醚、石油醚、丙酮等中低极性溶剂以及不同浓度的乙醇、甲醇以及多元醇等。提取方法可以是回流提取、浸渍、渗漉等方法。而且，提取过程中还可以使用超声或微波的方法进行辅助。
第一方面，本发明涉及荔枝壳提取物在5α-还原酶抑制中的用途。
第二方面，本发明涉及荔枝壳提取物作为具有5α-还原酶抑制作用的添加剂在制备具有控油抗痤疮功效的个人护理产品中的用途。
第三方面，本发明涉及荔枝壳提取物作为具有5α-还原酶抑制作用的添加剂在制备具有防脱发功效的个人护理产品中的用途。
根据本发明的一个优选的实施方式，以重量百分比计，荔枝壳提取物的用量为0.0001％-100％，优选0.01％-50％，更优选0.1％-10％。
本发明的个人护理产品可以是皮肤或头发可接受的任意剂型，包括：洁面乳、化妆水、乳液、膏霜、啫喱、面膜、洗发水、护发素、护发精华、香皂，但不限于此。在一个实施方式中，本发明的个人护理产品包含荔枝壳提取物以及可接受的辅料。
在一个实施方式中，个人护理产品包含0.0001-100重量％的荔枝壳提取物。在另一个实施方式中，个人护理产品包含0.01％-50重量％的荔枝壳提取物。在另一个实施方式中，个人护理产品包含0.1％-10重量％的荔枝壳提取物。
附图说明
图1显示了正常组、对照组以及不同浓度的荔枝壳提取物的5α-还原酶促反应速率。
图2显示了阳性对照以及不同浓度的荔枝壳提取物对5α-还原酶促反应的抑制率。
具体实施方式
荔枝壳对5α-还原酶的抑制作用未见任何报道，属于首次发现。而且，发明人通过实验意外发现，荔枝壳对5α-还原酶的抑制作用显著。荔枝壳来源广泛，安全无毒，因此考虑可以作为理想的个人护理产品的功效添加剂。此外，由于发明人意外发现了荔枝壳提取物对5α-还原酶的抑制作用，荔枝壳提取物可以作为添加剂用于制备具有抑制油脂分泌、抗痤疮、防脱发功能的各种个人护理产品。
本发明的发明人在经过了广泛而深入的研究之后发现：荔枝壳提取物具有5α-还原酶抑制作用。
因此，荔枝壳提取物可作为功效添加剂加入到个人护理产品中。
文献中均未涉及荔枝壳提取物具有5α-还原酶抑制作用，也未提及将其作为功能添加剂加入个人护理产品中。因此，本发明首次提出荔枝壳提取物具有5α-还原酶抑制作用，可以作为功能添加剂加入个人护理产品中，作为个人护理产品添加剂添加到个人护理产品中能起到控油、抗痤疮的作用，或者添加到护发产品中时能起到防脱发作用。
在个人护理产品应用中，荔枝壳提取物应用形式可以是洁面乳、化妆水、乳液、膏霜、啫喱、面膜、洗发水、护发素、护发精华、香皂等任何可以应用于人体皮肤或头发的剂型。
荔枝壳提取物以外的其他成分可以是个人护理产品配方需要的任何成分，如：水、乙醇、丁二醇、丙二醇、油脂、乳化剂、增稠剂、防腐剂等；也可以添加其他功效成分达到复合功能，如：添加保湿成分成为控油保湿个人护理产品，添加美白成分使成为祛痘美白个人护理产品，添加抗衰老成分成为控油抗衰老个人护理产品，添加头皮滋养成分成为滋养防脱洗发水/护发素/护发精华，添加去屑剂成为控油去屑洗发水/护发素/护发精华等等。
一般而言，以重量百分比计，荔枝壳提取物的使用浓度可以在0.0001％-100％范围。优选地，荔枝壳提取物的使用浓度可以在0.01-50％范围。 更优选地，荔枝壳提取物的使用浓度可在0.1％-10％范围。
在一个实施方式中，荔枝壳提取物的使用浓度为0.001-10重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.001-5重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.001-1重量％。在一个实施方式中，荔枝壳提取物的使用浓度为0.01-10重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.01-5重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.01-1重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.1-10重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.1-5重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.1-1重量％。在另一个实施方式中，荔枝壳提取物的使用浓度为0.1-0.5重量％。
可以将荔枝壳提取物按照0.01-50重量％的比例加到各种个人护理产品中。例如，荔枝壳提取物的用量可以是0.01-20重量％，例如0.01-10重量％，例如0.01-5重量％。在另一个实施方式中，可以将荔枝壳提取物按照0.1-10重量％的比例加到各种个人护理产品中。在一个优选的实施方式中，个人护理产品中荔枝壳提取物的用量为0.1-2重量％。在另一个优选的实施方式中，个人护理产品中荔枝壳提取物的用量为0.5-2重量％。
下面结合具体的实施例进一步阐述本发明。但是，应该明白，这些实施例仅用于说明本发明而不构成对本发明范围的限制。下列实施例中未注明具体条件的试验方法，通常按照常规条件，或按照制造厂商所建议的条件。除非另有说明，所有的百分比和份数按重量计。
实施例1：荔枝壳的提取
荔枝壳50g，加入8倍量的30％乙醇，加热回流提取1h，过滤。取滤液，减压回收乙醇并干燥得荔枝壳提取物。
实施例2：荔枝壳提取物对5α-还原酶的抑制作用
用45％(v/v)DMSO(Tris缓冲液55％)将实施例1制备的荔枝壳提取物溶解稀释成5个浓度梯度：3.4重量％，1.7重量％，0.85重量％，0.43重 量％，0.21重量％。如下所述进行5α-还原酶抑制实验。实验平台的反应体系为1ml，样品添加剂量为0.1ml，所以起始浓度从生药0.34重量％开始，体系浓度分别是：0.34重量％，0.17重量％，0.085重量％，0.043重量％，0.021重量％；因为体系中含有4.5％(v/v)的DMSO，所以同时设置4.5％(v/v)DMSO溶剂对照，1mg/L的度他雄胺为阳性对照。
5α-还原酶实验平台
从SD大鼠肝脏提取酶，冷冻保存备用；酶反应体系中含有底物睾酮(T)，辅酶NADPH，酶，酶反应温度37℃，pH为7。不加任何样品进行干预的反应为正常酶促反应，得到的反应速率为正常反应速率。加入样品以后的反应速率与正常反应速率相比，有所降低，认为样品具有抑制作用。
5α-还原酶实验结果
正常5α-还原酶促反应的反应速率、加入1mg/L的度他雄胺为阳性对照后的反应速率、加入4.5％(v/v)DMSO后的反应速率、以及加入不同浓度样品后的酶促反应的反应速率如下图。
从图1-2可知，浓度为0.021重量％-0.34重量％的荔枝壳提取物均具有抑制5α-还原酶活性的作用，浓度在0.17重量％及其以上的效果尤为显著，可以说明将荔枝壳提取物添加剂到产品配方中能起到相应的控油、祛痘或防脱发的作用。
实施例3：含荔枝壳提取物的控油护肤水的制备
按照表1的成分和用量制备包含本发明所述荔枝壳提取物的控油护肤水。
表1
成分 ％浓度(重量)
A相  
水 95.58
甘油 1.0
荔枝壳提取物 0.8
EDTA-2Na 0.02
B相  
香精 0.02
1,3-丁二醇 2.0
HPS 0.08
C相  
防腐剂 0.5
制备方法：按以上比例分别称取A、B、C三相，各自搅匀，边搅拌边将B相缓慢加入至A相，搅匀后加入C相，搅拌溶解均匀即得控油护肤水成品。
实施例4：控油祛痘面霜的制备
按照表2的成分和用量制备包含本发明所述荔枝壳提取物的控油祛痘面霜。
表2
成分 ％浓度(重量)
A相  
水 76.63
汉生胶 0.1
甘油 5.0
尼泊金甲酯 0.15
尼泊金丙酯 0.1
EDTA-2Na 0.02
B相  
十六十八醇 4.0
辛酸/葵酸甘油三酯 3.0
甘油硬脂酸+ 1.0
PEG100 3.0
二甲聚硅氧烷 1.0
C相  
荔枝壳提取物 1.0
水 5.0
制备方法：将汉生胶分散于水中15分钟，加入A相中的所有成分并加热至70-75℃。另称取B相内的所有成分，加热至75-80℃。将B相加入到A相中，均质5分钟，冷却至45℃，加入C相，搅匀即得控油祛痘面霜。
实施例5：祛痘凝胶
按照表3的成分和用量制备包含本发明所述荔枝壳提取物的祛痘凝胶。
表:3
成分 ％浓度(重量)
A相  
水 80.48
甘油 2.0
汉生胶 0.2
尼泊金甲酯 0.2
尼泊金丙酯 0.1
EDTA-2Na 0.02
霍霍巴油 3.0
B相  
Sepigel305 2.0
C相  
荔枝壳提取物 2
水 10.0
制备方法：按比例分别称取A、B、C三相，将A相加热至70-75℃，搅拌溶解均匀，加入B相，搅拌均匀，冷却至30-35℃，加入C相，混匀即得祛痘凝胶。
实施例6：控油洗发水
按照表4的成分和用量制备包含本发明所述荔枝壳提取物的控油洗发水。
表:4
Figure PCTCN2014092431-appb-000001
Figure PCTCN2014092431-appb-000002
制备方法：将水加热至70-75℃，按比例分别加入各个成分，搅拌溶解均匀，冷却至30-35℃，加入荔枝壳提取物，混匀即得控油洗发水。

Claims (10)

  1. 荔枝壳提取物作为5α-还原酶抑制剂的用途。
  2. 荔枝壳提取物作为具有5α-还原酶抑制作用的添加剂在制备具有控油抗痤疮功效的个人护理产品中的用途。
  3. 荔枝壳提取物作为具有5α-还原酶抑制作用的添加剂在制备具有防脱发功效的个人护理产品中的用途。
  4. 如权利要求1，2或3所述的用途，其特征在于，以重量百分比计，所述荔枝壳提取物的用量为0.0001-100％。
  5. 如权利要求4所述的用途，其特征在于，以重量百分比计，所述荔枝壳提取物的用量为0.01％-50％。
  6. 如权利要求5所述的用途，其特征在于，以重量百分比计，所述荔枝壳提取物的用量为0.1％-10％。
  7. 如权利要求2或3所述的用途，其特征在于，所述个人护理产品选自：洁面乳、化妆水、乳液、膏霜、啫喱、面膜、洗发水、护发素、护发精华、香皂。
  8. 如权利要求7所述的用途，其特征在于，所述个人护理产品包含荔枝壳提取物以及可接受的辅料。
  9. 如权利要求7所述的用途，其特征在于，所述个人护理产品包含0.01-50重量％的荔枝壳提取物。
  10. 如权利要求7所述的用途，其特征在于，所述个人护理产品包含0.1-10重量％的荔枝壳提取物。
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