WO2011009757A2 - Utilisation de bêta-défensine humaine pour influencer le processus de pigmentation naturel - Google Patents

Utilisation de bêta-défensine humaine pour influencer le processus de pigmentation naturel Download PDF

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Publication number
WO2011009757A2
WO2011009757A2 PCT/EP2010/060026 EP2010060026W WO2011009757A2 WO 2011009757 A2 WO2011009757 A2 WO 2011009757A2 EP 2010060026 W EP2010060026 W EP 2010060026W WO 2011009757 A2 WO2011009757 A2 WO 2011009757A2
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Prior art keywords
hair
human beta
defensin
use according
seq
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German (de)
English (en)
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WO2011009757A3 (fr
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Melanie Giesen
Sabine GRÜDL
Guido Fuhrmann
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Henkel AG and Co KGaA
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Henkel AG and Co KGaA
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • 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

Definitions

  • the invention relates to the use of at least one human beta-defensin, its analogues or agents which can stimulate expression of human beta-defensins, to influence the natural pigmentation process of skin and / or skin appendages.
  • hair has a psychosocial function that should not be underestimated.
  • they serve as a means of interpersonal communication and are a sign of their own individuality. Changes, such as the graying, can lead to a massive impairment of the self-confidence of the person concerned.
  • Pigmentation in the hair follicle is controlled by a defined complex set of molecular signals. Since melanogenesis in gray follicles is obviously influenced, it can be assumed that parts of this network are modified in the gray follicle. A sequelae is the reduction of melanin synthesis, which leads to the graying of the follicle.
  • the complex set of molecular signals affecting melanogenesis includes, among others, the expression of MCR1 (melanocortin receptor 1), gp100 and ckit. MCR1 and ckit are receptors that relay key melanogenesis signals through the binding of their ligands alpha-melanocyte stimulating hormone and stem cell factor to the cell interior.
  • GpIOO is a protein of the melanosome membrane and also regulates other melanogno-relevant proteins. Since these parameters are of essential importance in hair follicle pigmentation, it is advantageous to influence these parameters if the application of a test formulation is intended to maintain or reactivate melanin synthesis in the hair follicle cells. Maintaining the pigmentation and thus the youthfulness of the hair through suitable formulations of active ingredients is a challenge for cosmetic research.
  • Beta defensins are small, often about 30-50 amino acids long, peptides that have three intramolecular disulfide bridges. They are found in all animal organisms and higher plants and serve to repel microbial pathogens, especially bacteria, but also fungi and toxins.
  • US 20040091493 describes a screening method for the discovery of drugs that stimulate hBD-2 or hBD-3 expression without simultaneously stimulating at least one proinflammatory molecule or inflammatory mediator. It describes the usefulness of the drugs mentioned therein for the treatment of dandruff or acne. Prevention of hair graying in humans by the use of human beta-defensins is neither described nor suggested.
  • the object of the present invention is therefore to provide active ingredients which are suitable for influencing the natural pigmentation process, in particular in the hair or hair follicle, without the described disadvantages of the methods known in the prior art for influencing hair color or hair graying degree and youthfulness Appearance of the hair.
  • the object is achieved by the use of at least one human beta-defensin, its analogues or agents that can stimulate expression of human beta-defensins, to influence the natural pigmentation process of the skin and / or skin appendages.
  • the ß-defensins occur in humans, especially in the mucous membranes and the epithelial cells, especially in or on the skin on.
  • Human ⁇ -defensin 1 (hBD1) is found predominantly in the kidneys, saliva, lungs and skin, while human ⁇ -defensin 2 (hBD2) is mainly expressed in the skin, trachea and lungs when bacterial Stimulus is present.
  • Defensive skin cells, beta-defensin 2 are highly effective against bacteria such as Escherichia coli and Pseudomonas aeruginosa and the fungus Candida albicans.
  • Beta-defensin 3 has a broad spectrum of antimicrobial activity and is produced by keratinocytes in particular.
  • defensins form a large proportion of the proteins (about 30%) in the granules of neutrophilic granulocytes.
  • the mechanism of action of defensins has not yet been fully elucidated. It is known that defensins carry many cationic and hydrophobic amino acid residues. So they are amphipathic peptides. These positive charges interact with the negative ones Charges of the pathogen membranes.
  • the preference of the defensins are membranes which are characterized by a low proportion of cholesterol and thus differ from those of the eukaryotic organisms.
  • the use of at least one human beta-defensin, its analogues or agents capable of stimulating expression of human beta-defensins is able to synergize the natural pigmentation process, especially in the hair or hair follicle To positively influence and, in particular, stimulate a positive way.
  • the combination according to the invention induced both gene expression of MCR-1 and that of ckit and gp100 in a synergistic manner. In addition, a synergistic increase in melanin synthesis was observed.
  • the natural pigmentation process can thus be influenced, in particular stimulated, by the skin and / or skin appendages.
  • this can be used to influence, in particular stimulate, the natural pigmentation process of the hair, the hair follicle or in the hair follicle.
  • the compositions used in the invention are suitable for stimulating and / or improving the pigmentation of the hair, stimulating melanogenesis, in particular in the hair follicle, preventing and / or reducing hair graying, and repigmenting grayed hair.
  • the term "influencing the natural pigmentation process” means the positive or negative influence on the natural coloration / coloring and / or pigmentation of the skin and / or skin appendages, in particular the stimulation or the partial or complete inhibition of the natural, i. understood biological pigmentation process in skin and / or skin appendages, in particular hair or hair follicles.
  • the skin, the mucosa, the hair and its hair follicles, glands and nails especially skin, mucous membranes, hair and hair follicles to understand.
  • the term skin is particularly preferably to be understood as meaning the skin without mucous membrane.
  • Hair and hair follicles, preferably body hair, beard hair and head hair, very particularly preferably beard hair and head hair, very particularly preferably hair on the head or the corresponding hair follicles are to be understood by the term skin appendages.
  • the influencing of the natural pigmentation process means the positive or negative influencing at least one partial step of the natural pigmentation process.
  • This influence relates in particular to the regulation of such molecular signals that influence the biological or natural pigmentation process.
  • the regulation of the biological or natural pigmentation process by gene regulation, ie the regulation at the expression level, and / or enzyme regulation, ie the regulation at the activity level, and / or the regulation at the hormone level.
  • melanogenesis including the regulation of gene expression of MCR1 (melanocortin receptor 1), gp100 and ckit. Furthermore, the regulation of tyrosinase, both the gene expression of tyrosinase and the regulation at the enzyme level includes.
  • the natural pigmentation process of the hair is influenced, in particular stimulated or stimulated.
  • the positive influence preferably the positive regulation (upregulation or activation or excitation or increase) is understood as influencing, which leads to a stimulation of the natural, biological pigmentation process.
  • the pigmentation process in particular the melanogenesis, the skin and the skin appendages, preferably the hair or the hair follicle
  • the natural pigmentation process in particular melanogenesis
  • the pigmentation process, preferably the melanogenesis, of the human hair or of the human hair follicle is influenced.
  • the stimulation, enhancement, stimulation or improvement of the melanin synthesis in the melanocytes is particularly preferred according to the invention.
  • This is achieved, for example, by increasing the gene expression of signal molecules such as MCR1 (melanocortin receptor 1), gp100 and ckit.
  • the influence, preferably stimulation, of the melanogenesis is achieved by the use according to the invention.
  • melanogenesis is stimulated in the hair or hair follicles of the hairy scalp and / or the beard, in particular in humans.
  • the stimulation of the pigmentation means in particular, the improvement, enhancement and / or stimulation of the transport of the melanosomes into the keratinocytes surrounding the hair follicle, and furthermore the pigmentation of the individual hair perceptible with the eye or correspondingly suitable measuring methods, a selection of hairs , in particular an area of hairy skin, in particular the scalp, or of the entire head and / or whisker.
  • the use according to the invention of at least one human beta-defensin, its analogues or active substances which can stimulate expression of human beta-defensins is suitable for stimulating or improving the pigmentation of the hair.
  • the use according to the invention prevents, preferably substantially prevents, and / or reduces hair graying, in particular of human hair.
  • hair graying is understood as meaning both the hair graying which is visually discernible by the mixture of white and pigmented hair and the pigment dilution in a single hair, that is to say the graying of a single hair.
  • a prevention of hair graying takes place especially in hair not grayed, a reduction in hair graying can take place both in already grayed as well as hair not yet graying.
  • hair follicles in which the melanogenesis is not, no longer or not completely or disturbed or reduced again stimulated / stimulated to melanogenesis, while in non-grayed hair / hair follicles a disorder, reduction or down-regulation of melanogenesis not first or only to a lesser extent.
  • hair that has already become gray is repigmented by the use according to the invention of at least one human beta-defensin, its analogues or active substances which can stimulate expression of human beta-defensins.
  • the use according to the invention is a cosmetic use which is non-therapeutic.
  • the use according to the invention which aims at the hair growth caused by the natural aging process, in particular non-diseased hair graying, is a purely cosmetic use which does not represent a treatment and / or prophylaxis of a disease and is therefore non-therapeutic.
  • the use according to the invention is topical, i. by applying to the skin and / or skin appendages, in particular the face and / or scalp, in particular the scalp.
  • the use concentration of the human beta-defensins or their analogs is 0.0001-100 ⁇ g / ml, preferably 0.01-10 ⁇ g / ml, in particular 0.05-5 ⁇ g / ml, very particularly preferably 0.1 to 2 ⁇ g / ml.
  • At least one of the human beta-defensins 1 to 6 or 8 or their analogues is used.
  • the analogs of the human beta-defensins are selected from proteins which have at least one 80% identity, preferably at least one 90% identity, in particular at least 95% identity with the respective human beta-defensins.
  • the at least one human beta-defensin is selected from hbd1, hbd2 and / or hbd3 or their analogs.
  • Human beta-defensins and / or beta-defensin analogs, also called defensin derivatives, are peptides which according to the invention preferably have a structure or a structural motif according to Seq. ID. 1 have.
  • the structural motifs mentioned may occur one or more times. Furthermore, one or more other essential or nonessential amino acids may be attached at both ends. A maximum of 15, preferably a maximum of 10, in particular 5, very particularly preferably one to three essential or non-essential amino acids are preferably added at one end or at both ends of the structural motif.
  • the human beta-defensin according to the invention is hbd2 or an analogue thereof.
  • ⁇ -defensins 2 or their analogs or ⁇ -defensin-2 derivatives are to be understood, preferably those peptides which have a structure or a structural motif according to Seq. ID no.
  • X is selected from C, G, T, K. More preferably, X at position 29 of the indicated sequence is selected from T (Thr) and G (Gly). Most preferably, X is independently selected at positions 8, 15, 20, 30, 37 and 38 of the indicated sequence selected from C (Cys). Most preferably, X is independently selected at positions 39 and 40 of the indicated sequence selected from K (Lys).
  • X is at position 39 and 40 of the indicated sequence selected from K.
  • peptides which, as structure or structural motif, the derivative of the human ⁇ -defensin 2 according to Seq. -No. 4 included:
  • GIGDPVTCLKSGAICHPVFCPRRYKQIGGCGLPGTKCCKKP SEQ ID NO: 4
  • the peptides may be present as monomers, but also to homo or hetero dimers or
  • the human beta-defensin is hbd3 or an analog thereof.
  • the analog of human beta is
  • Defensin hbd3 selected from a peptide having a structure or a structural motif of the ⁇ -
  • Human ⁇ -defensin 3 is an antimicrobial peptide having the following amino acid sequence (SEQ ID NO: 6):
  • the active agents capable of stimulating expression of human beta-defensins are selected from vermouth root, Canadian horseweed, elderberry bark, redcurrant, pineapple juice, peppermint, betel nut, quinoa, arnica, broom shrub, sarsaparilla, walnut leaf, hibiscus flower , pumpkin, sunflower, peony, St. John's Wort or any of its extracts, jasmonic acid or vitamin A, derivatives and precursors thereof, isoleucine esters, calcium salts, in particular organic or mineral calcium salts.
  • the active substances can be used individually or in combination with one or more of the other active substances mentioned. It may be advantageous if the effective human beta-defensin is not applied directly, but is stimulated in situ by the body through the corresponding active ingredient, in order to develop its activity there. Therefore, in agents used in the invention, the above-mentioned agents are used to induce human beta-defensins on the skin or the face and / or scalp.
  • beta-defensin-inducing or expressing human beta-defensin-stimulating active ingredients together with one or more of the beta-defensins to be used according to the invention, preferably hbd2, hbd3 or their analogues, preferably hbd2 or hbd3.
  • the agent to be used according to the invention a direct and, additionally, a time-delayed effect can be produced which further enhances the effect stimulating the natural pigmentation process.
  • the cosmetic compositions to be used according to the invention show improved care effects on skin and hair. Especially on keratinic fibers, the positive effects are clearly pronounced, so that preferred cosmetic agents to be used according to the invention are hair treatment agents.
  • Hair treatment compositions for the purposes of the present invention are, for example, hair dyes, bleaching agents, hair shampoos, hair conditioners, conditioning shampoos, hair sprays, hair rinses, hair treatments, hair wraps, hair tonics, perming solutions, hair dye shampoos, hair dyes, hair fixatives, hair dressings, hair styling preparations, hair lotions , Mousse, hair gels, hair waxes or combinations thereof.
  • Particularly preferred hair treatment agents are characterized in that they are used as a shampoo, Hair Tonics, hair conditioner, hair conditioner, hair foam, hair fixative, hair spray, hair gel and / or Haarfärbemitte are made up.
  • the use of these means is particularly advantageous.
  • At least one hair conditioning agent selected from cationic polymers, cationic surfactants, silicones and / or vegetable oils is contained.
  • the agents used in the invention may contain other active ingredients and adjuvants. These are described below.
  • compositions to be used according to the invention may contain surfactants, in particular cationic surfactants.
  • surfactants for surfactant-containing agents to be used according to the invention, protection is desired or protection may be desired;
  • Surfactants, in particular cationic surfactants contribute to the technical aim of the invention and thus to the solution of the technical problem underlying the application according to the invention.
  • compositions according to the invention are disclosed in priority document DE 102009044970 on pages 10 to 20, the features mentioned there belong clearly implicitly to the description of the invention contained in the filed application and thus to the disclosure content of this application .
  • Particularly preferred hair treatment compositions according to the invention are characterized in that they contain as cationic care substance - based on their weight - 0.05 to 7.5 wt .-%, preferably 0.1 to 5 wt .-%, particularly preferably 0.2 to 3, 5 wt .-% and in particular 0.25 to 2.5 wt .-% cationic (s) surfactant (s) from the group of quaternary ammonium compounds and / or the esterquats and / or the amidoamines containing preferred cationic (s)
  • Surfactant (s) is / are selected from alkyltrimethylammonium chlorides having preferably 10 to 18 carbon atoms in the alkyl radical and / or dialkyldi
  • the agents used according to the invention may contain from 0.01 to 10% by weight of at least one polymer from the group of cationic and / or amphoteric polymers.
  • polymers for polymer-containing agents to be used according to the invention protection is desired or protection can be desired;
  • Polymers in particular cationic polymers, contribute to the technical aim of the invention and thus to the solution of the according to the application Invention underlying technical task.
  • Preferred polymers, the amounts in which they are contained in compositions to be used according to the invention, are disclosed in the priority document DE 102009044970 on pages 20 to 29, the features mentioned therein clearly belong implicitly to the description of the invention contained in the filed application and thus to the disclosure content this application.
  • vitamins, provitamins or vitamin precursors are vitamins, provitamins or vitamin precursors. These are described below:
  • vitamin A includes retinol (vitamin A 1 ) and 3,4-didehydroretinol (vitamin A 2 ).
  • the ß-carotene is the provitamin of retinol.
  • vitamin A component according to the invention for example, vitamin A acid and its esters, vitamin A aldehyde and vitamin A alcohol and its esters such as the palmitate and the acetate into consideration.
  • the agents used according to the invention preferably contain the vitamin A component in quantities of 0.05-1% by weight, based on the total preparation.
  • the vitamin B group or the vitamin B complex include, among others, vitamin B 1 (thiamine), vitamin B 2 (riboflavin), vitamin B 3 .
  • the compounds nicotinic acid and nicotinamide (niacinamide) are often performed.
  • Preferred according to the invention is the nicotinic acid amide which is contained in the agents used according to the invention preferably in amounts of from 0.05 to 1% by weight, based on the total agent.
  • vitamin B 5 pantothenic acid, panthenol and pantolactone. Panthenol and / or pantolactone are preferably used in the context of this group.
  • panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and also cationically derivatized panthenols.
  • Individual representatives are, for example, the panthenol triacetate, the panthenol monoethyl ether and its monoacetate and also the cationic panthenol derivatives disclosed in WO 92/13829.
  • the said compounds of the vitamin B 5 type are preferably contained in the agents used according to the invention in amounts of 0.05-10% by weight, based on the total agent. Amounts of 0.1-5 wt .-% are particularly preferred.
  • vitamin B 6 pyridoxine and pyridoxamine and pyridoxal
  • Vitamin C ascorbic acid
  • Vitamin C is used in the compositions according to the invention preferably in amounts of 0.1 to 3 wt .-%, based on the total agent.
  • Use in the form of palmitic acid ester, glucosides or phosphates may be preferred.
  • the use in combination with tocopherols may also be preferred.
  • Vitamin E tocopherols, especially ⁇ -tocopherol).
  • Vitamin F is usually understood as meaning essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid.
  • Vitamin H is the compound (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-c /] imidazole-4-valeric acid, for which, however, the trivial name biotin enforced. Biotin is contained in the agents used according to the invention preferably in amounts of 0.0001 to 1, 0 wt .-%, in particular in amounts of 0.001 to 0.01 wt .-%.
  • Particularly preferred hair treatment agents used according to the invention are characterized in that they contain as care substance - based on their weight - 0.0001 to 1 wt .-%, preferably 0.001 to 0.5 wt .-% and particularly preferably 0.005 to 0.1 wt. % of at least one ubiquinone and / or at least one ubiquinol and / or at least one derivative of these substances, with agents to be used particularly preferably containing coenzyme Q 10, preferably from 0.005 to 0.1% by weight.
  • the agents used according to the invention may also contain plastoquinones (polyprenylated 2,3-dimethylbenzoquinone derivatives).
  • preferred agents used in the invention are characterized by being 0.0002 to 4% by weight, preferably 0.0005 to 3% by weight, more preferably 0.001 to 2% by weight, more preferably 0.0015 to 1 and In particular, 0.002 to 0.5 wt .-% of at least one plastoquinone.
  • the agents used according to the invention may with particular preference contain one or more amino acids.
  • Amino acids which can be used particularly preferably according to the invention are selected from the group consisting of glycine, alanine, VaNn, leucine, isoleucine, phenylalanine, tyrosine, tryptophan, proline, aspartic acid, glutamic acid, asparagine, glutamine, serine, threonine, cysteine, methionine, lysine, arginine, histidine, ⁇ Alanine, 4-aminobutyric acid (GABA), betaine, L-cystine (L-Cyss), L-citrulline, L-theanine, 3 ', 4'-dihydroxy-L-phenylalanine (L-dopa), 5'-hydroxy -L-tryptophan, L-homocysteine, S-methyl-L-methionine, S-allyl-L-L-
  • Preferred agents used according to the invention comprise one or more amino acids in narrower quantitative ranges.
  • preferred hair treatment compositions are characterized in that they as care substance - based on their weight - 0.01 to 5 wt .-%, preferably 0.02 to 2.5 wt .-%, particularly preferably 0.05 to 1, 5 % By weight, more preferably 0.075 to 1 wt .-% and in particular 0.1 to 0.25 wt .-% amino acid (s), preferably from the group of glycine and / or alanine and / or valine and / or lysine and / or leucine and / or threonine.
  • compositions preferably to be used according to the invention contain as care substance - based on their weight - 0.01 to 15 wt .-%, preferably 0.025 to 12.5 wt .-%, particularly preferably 0.05 to 10 wt .-%, more preferably 0 , 1 to 7.5% by weight and in particular 0.5 to 5% by weight of at least one 2-furanone derivative of the formula (Fur I) and / or of the formula (Fur-II)
  • preferred hair-treatment compositions contain as care substance - based on their weight - 0.01 to 15 wt .-%, preferably 0.025 to 12.5 wt .-%, particularly preferably 0.05 to 10 wt .-%, more preferably 0.1 to 7.5% by weight and in particular 0.5 to 5% by weight of taurine (2-aminoethanesulfonic acid).
  • compositions used according to the invention may contain, in addition to optional further ingredients, other substances which prevent, alleviate or heal hair loss.
  • a content of hair root stabilizing agents is advantageous.
  • Propecia (finasteride) is currently the only preparation that is approved worldwide and has been proven in many studies to be effective and tolerable. Propecia causes less DHT to form from testosterone.
  • Minoxidil is probably the oldest proven hair restorer with or without supplemental additives. For the treatment of hair loss, it may only be used for external application.
  • hair tonic with up to 2% minoxidil content is available without prescription.
  • Spironolactone be applied in the form of hair tonic and in combination with Minoxidil.
  • Spironolactone acts as an androgen receptor blocker, ie. the binding of DHT to the hair follicles is prevented.
  • cosmetic agents to be used according to the invention which additionally contain, based on their weight, from 0.001 to 5% by weight of hair root stabilizing substances, in particular minoxidil and / or finasteride and / or ketoconazole.
  • a preferred form of preparation of the hair treatment agent according to the invention takes place in the form of hair tonics or hair lotions.
  • These preferably contain at least one monohydric alcohol, optionally a gelling agent and at least one human beta-defensin, its analogues or agents capable of stimulating expression of human beta-defensins, and optionally at least one particular conditioning enhancer.
  • the present invention is in a further embodiment, a hair treatment agent containing
  • Particularly preferred is a hair treatment agent with
  • compositions used according to the invention contain from 0.1 to 90% by weight of at least one monohydric alcohol from the group of ethanol, n-propanol, isoporopanol, n-butanol. Among these, ethanol and / or isopropanol are particularly preferred.
  • Particularly preferred hair treatment compositions according to the invention are characterized in that they contain, based on their weight, from 0.5 to 85% by weight, preferably from 1 to 80% by weight, more preferably from 5 to 75% by weight, more preferably from 10 to 70 Wt .-% and in particular 25 to 60 wt .-% ethanol and / or isopropanol.
  • hair treatment agents contain only ethanol.
  • hair treatment compositions according to the invention which - based on their weight - 5 to 80 wt .-%, preferably 7.5 to 70 wt .-%, particularly preferably 10 to 60 wt .-%, more preferably 20 to 55 wt .-% and in particular 25 to 50 wt .-% ethanol, more preferably.
  • the agents used according to the invention may additionally contain a gelling agent.
  • a gelling agent By using these gelling agents, the adhesion of the agents to the hair can be improved and the application can be made more pleasant.
  • Hair-treatment compositions according to the invention are preferred here which, based on their weight, contain 0.15 to 9% by weight, preferably 0.2 to 8% by weight, more preferably 0.25 to 7% by weight, more preferably 0, From 3 to 6% by weight and in particular from 0.4 to 5% by weight of at least one gelling agent from the groups of silicic acids and / or layered silicates and / or organophosphorus silicates and / or metal soaps and / or hardened castor oil and / or modified fatty derivatives and / or polyamides and / or hydroxyethylcellulose (HEC) and / or carboxymethylcellulose (CMC) and / or hydroxypropylmethylcellulose (HPMC) and / or hydroxypropylcellulose (HPC) and / or
  • the agents used according to the invention may contain emulsifiers (F). Protection is sought or protection can be sought for emulsifier-containing agents to be used in the present invention; Emulsifiers contribute to the technical aim of the invention and thus to the solution of the technical problem underlying the application according to the invention.
  • emulsifiers the amounts in which they are contained in compositions according to the invention are disclosed in the priority document DE 102009044970 on pages 44 to 45, the features mentioned there belong clearly implicitly to the description of in the filed application contained invention and thus to the disclosure of this application.
  • an agent according to the invention may also contain UV filters (I).
  • the UV filters to be used according to the invention are not subject to any general restrictions with regard to their structure and their physical properties. On the contrary, all UV filters which can be used in the cosmetics sector and whose absorption maximum lies in the UVA (315-400 nm), in the UVB (280-315 nm) or in the UVC ( ⁇ 280 nm) range are suitable. UV filters with an absorption maximum in the UVB range, in particular in the range from about 280 to about 300 nm, are particularly preferred.
  • the UV filters used according to the invention can be selected, for example, from substituted benzophenones, p-aminobenzoic acid esters, diphenylacrylic acid esters, cinnamic acid esters, salicylic acid esters, benzimidazoles and o-aminobenzoic acid esters.
  • Examples of UV filters which can be used according to the invention are 4-aminobenzoic acid, N, N, N-trimethyl-4- (2-oxoborn-3-ylidenemethyl) aniline methylsulfate, 3,3,5-trimethylcyclohexyl salicylate (homosalates), 2-hydroxy-4-methoxy-benzophenone
  • water-insoluble UV filters are those which dissolve in water at not more than 1% by weight, in particular not more than 0.1% by weight, at 20 ° C. Furthermore, these compounds should be soluble in the usual cosmetic oil components at room temperature to at least 0.1, in particular at least 1 wt .-%).
  • the use of water-insoluble UV filters may therefore be preferred according to the invention.
  • These UV filters have the general structure U - Q.
  • the structural part U stands for a UV-absorbing group.
  • This group can in principle be derived from the known UV filters which can be used in the cosmetics sector, in which a group, generally a hydrogen atom, of the UV filter is replaced by a cationic group Q, in particular having a quaternary amino function ,
  • Compounds from which the structural part U can be derived are, for example, substituted benzophenones, p-aminobenzoic acid esters, diphenylacrylic acid esters, cinnamic acid esters, salicylic acid esters, benzimidazoles and o-aminobenzoic acid esters.
  • Structural parts U which are derived from cinnamic acid amide or from N, N-dimethylaminobenzoic acid amide are preferred according to the invention.
  • the structural parts U can in principle be chosen such that the absorption maximum of the UV filters can be in both the UVA (315-400 nm) and in the UVB (280-315 nm) or in the UVC ( ⁇ 280 nm) range.
  • UV filters with an absorption maximum in the UVB range are particularly preferred.
  • the structural part U also as a function of structural part Q, is preferably selected so that the molar extinction coefficient of the UV filter at the absorption maximum is above 15,000, in particular above 20,000.
  • the structural part Q preferably contains, as a cationic group, a quaternary ammonium group.
  • This quaternary ammonium group can in principle be connected directly to the structural part U, so that the structural part U represents one of the four substituents of the positively charged nitrogen atom.
  • one of the four substituents on the positively charged nitrogen atom is a group, especially an alkylene group of 2 to 6 carbon atoms, which functions as a compound between the structural portion U and the positively charged nitrogen atom.
  • the group Q has the general structure - (CH 2 ) X -N + R 1 R 2 R 3 X ' , where x is an integer from 1 to 4, R 1 and R 2 independently of one another are Ci_ 4 Alkyl groups, R 3 is a Ci_ 22 alkyl group or a benzyl group and X 'is a physiologically acceptable anion.
  • x preferably represents the number 3
  • R 1 and R 2 each represent a methyl group and R 3 represents either a methyl group or a saturated or unsaturated, linear or branched hydrocarbon chain with 8 to 22, in particular 10 to 18 , Carbon atoms.
  • Physiologically acceptable anions are, for example, inorganic anions such as halides, in particular chloride, bromide and fluoride, sulfate ions and phosphate ions and organic anions such as lactate, citrate, acetate, tartrate, methosulfate and tosylate.
  • inorganic anions such as halides, in particular chloride, bromide and fluoride, sulfate ions and phosphate ions and organic anions such as lactate, citrate, acetate, tartrate, methosulfate and tosylate.
  • UV filters with cationic groups are the commercially available compounds cinnamic acid-trimethylammonium chloride (lncroquat ® UV-283) and dodecyl tosylate (Escalol ® HP 610).
  • the teaching of the invention also includes the use of a combination of several UV filters.
  • the combination of at least one water-insoluble UV filter with at least one UV filter with a cationic group is preferred.
  • the UV filters (I) are contained in the compositions according to the invention usually in amounts of 0.1-5 wt .-%, based on the total agent. Levels of 0.4-2.5 wt .-% are preferred.
  • the UV filters in the compositions used according to the invention improve the results of the repigmentation process, especially in the long term, and are therefore particularly suitable.
  • the aforementioned UV filters are combined with human beta-defensin 2 or human beta-defensin 3.
  • the agents used in the invention may further contain a 2-pyrrolidinone-5-carboxylic acid and its derivatives (J).
  • a 2-pyrrolidinone-5-carboxylic acid and its derivatives Preference is given to the sodium, potassium, calcium, magnesium or ammonium salts in which the ammonium ion carries, in addition to hydrogen, one to three C 1 - to C 4 -alkyl groups.
  • the sodium salt is most preferred.
  • the amounts used in the compositions according to the invention are preferably from 0.05 to 10% by weight, based on the total composition, particularly preferably from 0.1 to 5, and in particular from 0.1 to 3,% by weight.
  • compositions used according to the invention may also contain plant extracts (L).
  • plant extracts usually these extracts are produced by extraction of the whole plant. However, in individual cases it may also be preferred to prepare the extracts exclusively from flowers and / or leaves of the plant.
  • extracts of green tea, almond, aloe vera, coconut, mango, apricot, lime, wheat, kiwi and melon are especially suitable for the use according to the invention.
  • alcohols and mixtures thereof can be used as extraction agent for the preparation of said plant extracts water.
  • the alcohols are lower alcohols such as ethanol and isopropanol, but especially polyhydric alcohols such as ethylene glycol and propylene glycol, both as sole extractant and in admixture with water, are preferred.
  • Plant extracts based on water / propylene glycol in a ratio of 1:10 to 10: 1 have proven to be particularly suitable.
  • the plant extracts can be used according to the invention both in pure and in diluted form. If used in diluted form, they usually contain about 2 to 80% by weight of active substance and, as solvent, the extractant or extractant mixture used in its production.
  • mixtures of several, in particular two, different plant extracts may be preferable to use mixtures of several, in particular two, different plant extracts in the compositions used according to the invention.
  • the agents used according to the invention contain penetration aids and / or swelling agents (M).
  • M penetration aids and / or swelling agents
  • M include, for example, urea and urea derivatives, guanidine and its derivatives, arginine and its derivatives, water glass, imidazole and its derivatives, histidine and its derivatives, benzyl alcohol, glycerol, glycol and glycol ethers, propylene glycol and propylene glycol ethers, for example propylene glycol monoethyl ether, carbonates, bicarbonates, Diols and triols, and in particular 1, 2-diols and 1, 3-diols such as 1, 2-propanediol, 1, 2-pentanediol, 1, 2-hexanediol, 1, 2-dodecanediol, 1, 3-propanediol, 1 , 6-hexanediol, 1, 5-pentanediol, 1,
  • Another object of the present invention is a method for influencing the natural pigmentation process of the skin and / or skin appendages, in particular stimulation of the natural pigmentation process, in particular the melanogenesis and / or pigmentation of the hair, to prevent and / or reduce the Haarergrauung and / or for the repigmentation of gray hair, characterized in that at least one human beta-defensin, its analogues or agents that can stimulate expression of human beta-defensins, topically contacts hair and / or skin.
  • the statements made on the uses according to the invention apply.
  • the ligands involved in melanogenesis such as SCF or alpha-MSH (melanocyte stimulating hormone alpha) bind to various receptors, by which the corresponding signal is transmitted to the cell interior.
  • the receptor for SCF is ckit
  • the receptor for alpha-MSH is MCR-1 (melanocortin receptor 1).
  • MCR-1 melanocortin receptor 1
  • GpIOO is a protein that occurs in the membrane of melanosomes and stabilizes them. Since melanin is increasingly produced in the cells after the application of substances that have a positive influence on melanogenesis, there is an increase in the number of melanosomes required for transport. A substance that induces gene expression of gp100 is therefore a pigment stimulating agent.
  • Particularly preferred substances which stimulate the natural pigmentation process of skin and / or skin appendages, in particular hair or hair follicles, are those which which induce both gene expression of MCR-1 and / or ckit and induce gene expression of gp100.
  • the determination of the extent of the change in gene expression after administration of such substances to suitable cells / cell systems / tissue cultures can provide information about the effectiveness of the active ingredient.
  • RNA from the organotypic cell cultures is first isolated with the aid of the RNeasy Mini Kit from Qiagen and transcribed into cDNA by means of reverse transcription.
  • the formation of the PCR products is detected online via a fluorescence signal.
  • the fluorescence signal is proportional to the amount of the PCR product formed. The stronger the expression of a particular gene, the greater the amount of PCR product produced and the higher the fluorescence signal.
  • the untreated control is set equal to 1 and the expression of the genes to be determined referred to (x-fold expression).
  • values greater than or equal to 1.8 times the expression or less than or equal to 0.5 times the expression of the untreated control are classified as significantly differentially expressed.
  • Values greater than or equal to 1.5-fold expression or less than or equal to 0.7-fold expression of the untreated control are considered to tend to be differentially expressed.
  • gp100 In addition to the induction of gene expression, translation into the corresponding proteins is also important for influencing cellular mechanisms.
  • the expression of gp100 was therefore additionally detected at the protein level by Western Blot technique. These were made from three-dimensional organotypic hair follicle cell cultures from dermal
  • Melanin is a dye that is produced and stored in the melanosomes of melanocytes. Melanin gives the hair its actual color, whereby the
  • Coloring is caused by a mixture of two types of melanin, eu- and pheomelanin.
  • Tyrosine by the enzyme tyrosinase in L-dihydroxyphenylalanine (L-DOPA) and then implemented via several intermediate steps in the different melanin pigments.
  • L-DOPA L-dihydroxyphenylalanine
  • Melanogenesis positively influenced and increased melanin content in the Hair follicle melanocytes is particularly suitable to influence the natural pigmentation process of the skin and / or skin appendages, prevent hair graying and / or stimulate pigmentation.
  • hair follicle melanocytes and outer root sheath keratinocytes were treated with human beta-defensin 2 and human beta-defensin 3 (each 0.5 ⁇ g / ml and 1.0 ⁇ g / ml) for 7 days.
  • human beta-defensin 2 and human beta-defensin 3 each 0.5 ⁇ g / ml and 1.0 ⁇ g / ml

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Abstract

L'invention concerne l'utilisation d'au moins une bêta-défensine humaine, de ses analogues ou agents actifs pouvant stimuler une expression de la bêta-défensine humaine, pour influencer le processus de pigmentation naturel de la peau et/ou des phanères.
PCT/EP2010/060026 2009-07-23 2010-07-13 Utilisation de bêta-défensine humaine pour influencer le processus de pigmentation naturel Ceased WO2011009757A2 (fr)

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DE102009027953 2009-07-23
DE102009027953.9 2009-07-23
DE102009044970A DE102009044970A1 (de) 2009-07-23 2009-09-24 Verwendung von humanem beta-Defensin zur Beeinflussung des natürlichen Pigmentierungsprozesses
DE102009044970.1 2009-09-24

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Cited By (2)

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WO2017105413A1 (fr) * 2015-12-15 2017-06-22 Medicell Technologies, Llc Compositions de stimulation de cellules souches et procédés de traitement du mélasma
US20250000774A1 (en) * 2023-06-27 2025-01-02 Medicell Technologies Llc Stem cell stimulating compositions and methods

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Publication number Priority date Publication date Assignee Title
DE102009044970A1 (de) 2009-07-23 2011-01-27 Henkel Ag & Co. Kgaa Verwendung von humanem beta-Defensin zur Beeinflussung des natürlichen Pigmentierungsprozesses
ES2741656T3 (es) * 2012-12-14 2020-02-11 Unilever Nv Niacinamida para inducir la generación de péptidos antimicrobianos
PT3157504T (pt) * 2014-06-18 2019-11-11 Medicell Tech Llc Composições estimuladoras das células estaminais
DE102022109519A1 (de) 2022-04-20 2023-10-26 Güven Öztürk Haarpflegemittel auf Pflanzenbasis

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WO1992013829A1 (fr) 1991-02-06 1992-08-20 Smith Ronald J Composes quaternaires de panthenol et utilisation desdits composes
US20040091493A1 (en) 2002-08-02 2004-05-13 Coletica Active ingredients stimulating type 2 and/or type 3 human beta-defensins and cosmetic or pharmaceutical compositions containing such active ingredients
DE102005014687A1 (de) 2005-03-29 2006-10-12 Henkel Kgaa Zusammensetzung enthaltend ß-Defensin 2
DE102009044970A1 (de) 2009-07-23 2011-01-27 Henkel Ag & Co. Kgaa Verwendung von humanem beta-Defensin zur Beeinflussung des natürlichen Pigmentierungsprozesses

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DE3725030A1 (de) 1987-07-29 1989-02-09 Henkel Kgaa Oberflaechenaktive hydroxysulfonate
DE4413686C2 (de) 1994-04-20 1996-10-24 Henkel Kgaa Kationische Zuckertenside, Verfahren zu ihrer Herstellung und deren Verwendung
DE102006042244A1 (de) * 2006-09-06 2008-03-27 Henkel Kgaa Verfahren zur molekularen Charakterisierung von Altershaar

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WO1992013829A1 (fr) 1991-02-06 1992-08-20 Smith Ronald J Composes quaternaires de panthenol et utilisation desdits composes
US20040091493A1 (en) 2002-08-02 2004-05-13 Coletica Active ingredients stimulating type 2 and/or type 3 human beta-defensins and cosmetic or pharmaceutical compositions containing such active ingredients
DE102005014687A1 (de) 2005-03-29 2006-10-12 Henkel Kgaa Zusammensetzung enthaltend ß-Defensin 2
DE102009044970A1 (de) 2009-07-23 2011-01-27 Henkel Ag & Co. Kgaa Verwendung von humanem beta-Defensin zur Beeinflussung des natürlichen Pigmentierungsprozesses

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017105413A1 (fr) * 2015-12-15 2017-06-22 Medicell Technologies, Llc Compositions de stimulation de cellules souches et procédés de traitement du mélasma
US11020452B2 (en) 2015-12-15 2021-06-01 Medicell Technologies, Llc Stem cell stimulating compositions and methods of treating melasma
US20210244794A1 (en) * 2015-12-15 2021-08-12 Medicell Technologies, Llc Stem Cell Stimulating Compositions for Treatment of Melasma
US11806384B2 (en) 2015-12-15 2023-11-07 Medicell Technologies, Llc Stem cell stimulating compositions for treatment of melasma
US20250000774A1 (en) * 2023-06-27 2025-01-02 Medicell Technologies Llc Stem cell stimulating compositions and methods

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