FR2903309A1 - Compositions for combating hair loss comprise N-acetyl cysteine, cysteine, methionine, S-adenosyl methionine or N-acetyl methionylarginine ether ester, resveratrol, viniferin or grapevine extract, and arginine or lysine, - Google Patents
Compositions for combating hair loss comprise N-acetyl cysteine, cysteine, methionine, S-adenosyl methionine or N-acetyl methionylarginine ether ester, resveratrol, viniferin or grapevine extract, and arginine or lysine, Download PDFInfo
- Publication number
- FR2903309A1 FR2903309A1 FR0606207A FR0606207A FR2903309A1 FR 2903309 A1 FR2903309 A1 FR 2903309A1 FR 0606207 A FR0606207 A FR 0606207A FR 0606207 A FR0606207 A FR 0606207A FR 2903309 A1 FR2903309 A1 FR 2903309A1
- Authority
- FR
- France
- Prior art keywords
- cysteine
- methionine
- acetyl
- cosmetic
- lysine
- 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
- 239000000203 mixture Substances 0.000 title claims abstract description 29
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 title claims abstract description 24
- 229960004308 acetylcysteine Drugs 0.000 title claims abstract description 23
- QNVSXXGDAPORNA-UHFFFAOYSA-N Resveratrol Natural products OC1=CC=CC(C=CC=2C=C(O)C(O)=CC=2)=C1 QNVSXXGDAPORNA-UHFFFAOYSA-N 0.000 title claims abstract description 21
- 201000004384 Alopecia Diseases 0.000 title claims abstract description 20
- LUKBXSAWLPMMSZ-OWOJBTEDSA-N Trans-resveratrol Chemical compound C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC(O)=C1 LUKBXSAWLPMMSZ-OWOJBTEDSA-N 0.000 title claims abstract description 20
- 235000018417 cysteine Nutrition 0.000 title claims abstract description 20
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 title claims abstract description 20
- 235000021283 resveratrol Nutrition 0.000 title claims abstract description 20
- 229940016667 resveratrol Drugs 0.000 title claims abstract description 20
- -1 N-acetyl methionylarginine ether ester Chemical class 0.000 title claims abstract description 13
- 230000003676 hair loss Effects 0.000 title claims abstract description 13
- 229930182817 methionine Natural products 0.000 title claims abstract description 13
- 239000004475 Arginine Substances 0.000 title claims abstract description 12
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 title claims abstract description 12
- 239000004472 Lysine Substances 0.000 title claims abstract description 12
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 title claims abstract description 12
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 title claims abstract description 12
- FQWLMRXWKZGLFI-DAFODLJHSA-N 5-[6-hydroxy-2-(4-hydroxyphenyl)-4-[(e)-2-(4-hydroxyphenyl)ethenyl]-2,3-dihydro-1-benzofuran-3-yl]benzene-1,3-diol Chemical compound C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC2=C1C(C=1C=C(O)C=C(O)C=1)C(C=1C=CC(O)=CC=1)O2 FQWLMRXWKZGLFI-DAFODLJHSA-N 0.000 title claims abstract description 11
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- MEFKEPWMEQBLKI-AIRLBKTGSA-N S-adenosyl-L-methioninate Chemical compound O[C@@H]1[C@H](O)[C@@H](C[S+](CC[C@H](N)C([O-])=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 MEFKEPWMEQBLKI-AIRLBKTGSA-N 0.000 title claims abstract description 9
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- ZJBHFQKJEBGFNL-UHFFFAOYSA-N methylsilanetriol Chemical group C[Si](O)(O)O ZJBHFQKJEBGFNL-UHFFFAOYSA-N 0.000 claims description 9
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- OSCJHTSDLYVCQC-UHFFFAOYSA-N 2-ethylhexyl 4-[[4-[4-(tert-butylcarbamoyl)anilino]-6-[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)NC(C)(C)C)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 OSCJHTSDLYVCQC-UHFFFAOYSA-N 0.000 claims description 5
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- UYZLQWUFBLEIAJ-UHFFFAOYSA-N [hydroxy(dimethyl)silyl] 2-hydroxybenzoate Chemical compound C[Si](C)(O)OC(=O)C1=CC=CC=C1O UYZLQWUFBLEIAJ-UHFFFAOYSA-N 0.000 claims description 2
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Classifications
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
- A61K8/447—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof containing sulfur
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
- A61K8/585—Organosilicon compounds
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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]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Botany (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Compositions cosmétiques et dermatologiques destinées à lutter contre laCosmetic and dermatological compositions for combating
chute des cheveux La présente invention se rapporte au domaine des nécessités de la vie, et plus particulièrement 5 aux domaines de la dermatologie et de la cosmétologie. La présente invention concerne en particulier une nouvelle association de principes actifs destinée à être incorporée dans des produits pour lutter contre la chute des cheveux chez l'homme et chez la femme. La perte de cheveux considérée comme normale est de l'ordre de 100 par jours. Une perte de cheveux excessive et non compensée par une repousse conduit à la calvitie, gênante sur le plan esthétique et pouvant avoir des conséquences psychologiques non négligeables, notamment chez les sujets jeunes. Les causes de la chute des cheveux (ou alopécie) sont nombreuses ; elles peuvent être d'origine externe, comme un environnement pollué ou l'utilisation de produits cosmétiques présentant une certaine toxicité, comme les colorations ou d'autres produits capillaires. 20 L'alopécie peut également être la conséquence d'une perturbation du fonctionnement de l'organisme, affectant les mécanismes régulant la croissance du cheveu. Parmi ces perturbations, on peut recenser les troubles hormonaux, le dérèglement sébacé, l'amplification des 5a-réductases, l'inflammation, les modifications structurales du collagène, le facteur génétique, ainsi que le facteur psychique (stress, anxiété), qui a une influence très importante 25 sur l'alopécie. Le follicule pileux est composé de différentes entités telles que la papille dermique, la glande sébacée et les gaines épithéliales. La papille dermique constitue le tissu nourricier du bulbe pileux, leur lien est donc déterminant dans la croissance du cheveu. Le cycle pilaire est divisé en trois phases : La phase anagène, ou phase de croissance du cheveu, au cours de laquelle le bulbe pileux s'enfonce dans les tissus dermiques et connaît une phase intense de division cellulaire. Cette phase constitue l'étape la plus importante de la croissance du cheveu. 10 15 30 2903309 2 La phase catagène, durant laquelle le bulbe pileux se dissocie progressivement de la papille dermique. La papille dermique étant le tissu nourricier du bulbe, les divisions cellulaires régressent puis s'arrêtent. La phase télogène, durant laquelle le bulbe remonte à la surface de l'épiderme et finit 5 par tomber. De nombreux produits ont été proposés pour lutter contre l'alopécie. Pour la plupart, ils sont basés sur une association de principes actifs destinés à influencer favorablement les mécanismes de régulation de la croissance capillaire. Parmi les produits les plus fréquemment utilisés, on pourra citer des vitamines (A, E, B5, B6, C, H, PP...), des oligoéléments (Zn, Cu, Mg...), des acides aminés soufrés (méthionine, cystine, cystéine...), des agents antifongiques (piroctone olamine, cyclopiroxolamine...), ainsi que des extraits végétaux. La présente invention concerne des compositions cosmétiques et dermatologiques destinées à lutter contre la chute des cheveux, basée sur une association des principes actifs suivants : - N-acétylcystéine (NAC) et/ou cystéine et/ou méthionine et/ou S-adénosyl - méthionine et/ou N-acétyl méthionylarginyl éthylester et/ou leurs dérivés, - Resvératrol et/ou Viniférine et/ou leurs dérivés, - Arginine et/ou lysine et/ou leurs dérivés ; en association ou en mélange avec un ou plusieurs excipients ou véhicules inertes, non toxiques, dermatologiquement acceptables. 25 Ces différents composés sont décrits comme ayant les effets suivants : NAC, cystéine, méthionine : réduction de la dégénérescence cellulaire : * par protection contre le stress oxydatif , qui induit une inflammation au niveau du bulbe capillaire * par limitation en amont de facteurs de l'apoptose (mort cellulaire) 30 Resvératrol, Viniférine : prolongement de la durée de vie des cellules du bulbe capillaire : * par limitation des effets délétères des androgènes (testostérone, A4-androstènedione) * par activation des Sirtuines, notamment SIRT-1 Arginine, Lysine : retardement de la rigidification des fibres autour du bulbe capillaire : * par réduction du processus de glycation et de glycoxydation des fibres de collagène 10 15 20 2903309 3 Parmi les dérivés de la N-acétylcystéine, de la cystéine, de la méthionine et de la S-adénosylméthionine, on pourra citer leurs sels et leurs esters, notamment les esters lipophiles (ester de propyle, butyle, cyclohexyle...), ainsi que leurs amides lipophiles. Parmi les dérivés du Resvératrol, on citera notamment les oligomères du Resvératrol autres que la Viniférine, éventuellement sous forme d'extrait de sarments de vigne Vitis vinifera. Parmi les dérivés de l'Arginine et de la Lysine, on citera particulièrement ceux de la L-10 Arginine et de la L-Lysine, comme leurs esters ou leurs sels, notamment le chlorhydrate, le sulfate ou le pidolate. Selon une forme préférentielle de l'invention, on utilise en tant que dérivé de la lysine le Silanetriol Lysinate (dénomination INCI), un produit de couplage entre la lysine et le 15 méthylsilanetriol. Ce composé est notamment commercialisé sous la marque SILYSIN C" (EXSYMOL). Selon une forme préférentielle de l'invention, les compositions contiennent également un ou des silanols, comme le Silanediol salicylate ou le Silanetriol salicylate (dénomination INCI), 20 qui présentent des propriétés antioxydantes et anti-inflammatoires. Selon une forme préférentielle de l'invention, les compositions contiennent également du cyclopirox et/ou de la ciclopiroxolamine et/ou de la piroctone olamine et/ou un autre agent antibactérien et/ou antifongique, de manière à réduire l'inflammation du cuir chevelu induite 25 par les microorganismes, notamment les espèces de Malassezia, comme M.globosa, M.furfur, M. sympodialis et M restricta. Mécanisme d'action des différents actifs : 30 - La N-acétylcystéine (NAC) et la cystéine HSNHAc HSH2 COOH COOH N-acétylcystéine Cystéine 2903309 4 - Propriétés anti-oxydantes L'un des facteurs de l'alopécie est la réaction inflammatoire provoquée par la présence d'oxydants et de radicaux libres (stress oxydatif). 5 La NAC et la cystéine possèdent un groupe sulfhydryle libre (-SH). Ce goupe sulfhydryle a le pouvoir d'interagir directement avec des radicaux libres tels que le peroxyde d'hydrogène (H202) pour former de l'eau (H20) et de l'oxygène (02). 2(RûSH)+H202 RûSûSûR+2H20 Dans cette réaction, deux molécules soufrées sont oxydées, formant ainsi un pont disulfure (R = résidu). La NAC et la cystéine éliminent aussi le radical hydroxyle (OH.). En plus de sa fonction anti-radicalaire directe, il a été démontré que NAC et la cystéine 15 stimulent la production de glutathion. Le glutathion est un agent antioxydant intracellulaire essentiel dont le rôle est de piéger et de décomposer les peroxydes lipidiques et le peroxyde d'hydrogène. La NAC et la cystéine peuvent donc fournir deux types de protection contre les lésions inflammatoires causées par le stress oxydatif : une protection directe et une protection indirecte, par le biais du glutathion. 20 -Limitation en amont de facteurs de l'apoptose La N-acétylcystéine et la cystéine inhibent l'action du facteur de transcription nucléaire : Facteur-kB, probablement en vertu de leur aptitude à maintenir le potentiel Redox à l'intérieur de la cellule (Senaldi et. al., Protective effect of N-acetylcystein in hapten-induced 25 irritant and contact hypersensitivity reactions, 1994, The Society for Investigative Dermatologie, Inc.). Le facteur de transcription nucléaire est connu pour provoquer la transcription de plusieurs gènes, parmi lesquels se trouvent les gènes codant pour les cytokines pro-inflammatoires : TNF-a et IL-1-a. De plus, on a montré que la NAC antagonise le développement de l'inflammation et des réactions d'hypersensibilité retardées, 30 et que son action inclue une réduction du taux d'ARNm codant pour le TNF-a (op. cit.). Comme, les lésions inflammatoires causées par le TNF-a sont partiellement provoquées par des intermédiaires oxydatifs réactifs , dont la production est stimulée par le TNF-a, la 2903309 5 NAC et la cystéine pourraient inhiber le développement des réactions inflammatoires TNF-a/dépendantes, en bloquant à la fois le stress oxydatif (radicaux libres) et en empêchant la synthèse de TNF-a par inhibition du facteur de transcription nucléaire (NF-kB). 5 Le processus apoptotique d'une cellule est décrit ci-dessous : Destruction Au cours de la phase de signalisation, la cellule reçoit un ensemble de signaux qui peut générer différentes réponses. Ces taux sont alors intégrés par la cellule qui va répondre en fonction de son contexte génétique, de son état et de son environnement. Le processus 10 décisionnel est influencé par une série de médiateurs intracellulaires. La phase de dégradation aboutit aux manifestations visibles de l'apoptose, dont la condensation et la dégradation de la chromatine. Par leur inhibition de mécanismes de dégradation en amont du processus, la NAC et la 15 cystéine présentent donc un effet anti-apoptotique indirect. - La Méthionine et la S-adénosylméthionine L'intérêt de ces composés est de générer in situ de la cystéine, par le processus catabolique suivant : • dommages cellulaires (agents cytotoxiques, hypoxie. dateur, perte de l'adhésion .) • récepteurs (Fas1TNF-,,. glucocwticoïdes._ 1 • carence en facteurs de croissance (NGF. IL-2.. Signalisation 1 ( Régulation • p53 • BcI2/Ced-9 ? ^ Kinases • phosphatases • FADD!T S.4F;'tV ORTi TRADD/R I P)FLI C. E-MACH • cytochrome C. dATP • oncogènes tc-myc....( • protéines régulant te cylce cellulaire • Facteurs de transcriptions • proteii à Cvste_=te tcaspasesr • ntuclèases • AIF (apoptosis inducinQ factor) proteolyse dégradation de l'ADN 1 2903309 6 NH2 + moi\ COOH Ade OH J-adéUVsyhttélltivuilIL HO Méthionine SNH2 adénosyltransférase COOH ATP Pi + PPi Méthionine OH HO OH NH2 HS Adénosylhomocystéinase Ade COOH COOH OH2 HO OH S-adénosyl homocystéi ne Cystathionyl 13-synthase Adénosine Hornocystéine Sérine H2O NH2 HOOCSCOOH NH2 Cystathionine NH2 H000H + a-Cétobutyrate Cysté i ne Les compositions contenant de la méthionine ou de l'adénosylméthionine pourront donc présenter les effets décrits pour la cystéine. 5 - Le N-acétyl méthionylarginyl éthylester SMe O O OEt NH O NH2 Acétyl méthionylarginyl éthylester - Propriétés anti-oxydantes Les propriétés antioxydantes de l'acétyl méthionylarginyl éthylester (MR-LIP) ont été 10 déterminées selon 2 modèles expérimentaux : H H 2903309 7 • L'activité de désactivation des radicaux hydroxyle (OH.) a été déterminée selon la procédure décrite par Rehman et. al. (British J. ofPharmacol. 1997, 122, 1702-1706). Le MR-LIP et les produits issus de sa bioconversion enzymatique sont des désactiveurs efficaces de OH*. L'activité du MR-LIP est comparable à celle de l'acide 5 ascorbique. • L'activité de désactivation de l'anion superoxyde (02"•) a été déterminée selon la procédure décrite par Bagchi et. al. (General Pharmacol. 1997, 28, 85-91). L'activité du MR-LIP est comparable à celle de l'acétylméthionine. 10 -Propriétés anti-inflammatoires L'activité anti-inflammatoire de l'acétyl méthionylarginyl éthylester a été déterminée en étudiant la libération de cytokines pro-inflammatoires (IL-la, TNF-a, IL-8) après irradiation aux UVB d'un épiderme humain reconstitué (Exemple 1). The present invention relates to the field of the necessities of life, and more particularly to the fields of dermatology and cosmetology. The present invention relates in particular to a novel combination of active principles for incorporation into products for combating hair loss in men and women. Hair loss considered normal is of the order of 100 per day. An excessive loss of hair and not compensated by a regrowth leads to baldness, inconvenient aesthetically and can have significant psychological consequences, especially in young people. The causes of hair loss (or alopecia) are numerous; they may be of external origin, such as a polluted environment or the use of cosmetic products having a certain toxicity, such as colorings or other hair products. Alopecia can also be the consequence of a disruption of the functioning of the body, affecting the mechanisms regulating the growth of the hair. Among these disturbances, we can identify hormonal disorders, sebum disorders, amplification of 5a-reductases, inflammation, structural changes in collagen, the genetic factor, as well as the psychic factor (stress, anxiety), which has a very important influence on alopecia. The hair follicle is composed of different entities such as the dermal papilla, the sebaceous gland and the epithelial sheaths. The dermal papilla is the nourishing tissue of the hair bulb, so their link is crucial in the growth of the hair. The hair cycle is divided into three phases: The anagen phase, or hair growth phase, during which the hair bulb sinks into the dermal tissues and undergoes an intense phase of cell division. This phase is the most important stage of hair growth. The catagen phase, during which the hair bulb gradually dissociates from the dermal papilla. The dermal papilla being the nourishing tissue of the bulb, the cellular divisions regress and then stop. The telogen phase, during which the bulb rises to the surface of the epidermis and eventually falls. Many products have been proposed to fight against alopecia. For the most part, they are based on an association of active principles intended to favorably influence the mechanisms for regulating capillary growth. Among the most frequently used products, mention may be made of vitamins (A, E, B5, B6, C, H, PP, etc.), trace elements (Zn, Cu, Mg, etc.) and sulfur amino acids ( methionine, cystine, cysteine ...), antifungal agents (piroctone olamine, cyclopiroxolamine ...), as well as plant extracts. The present invention relates to cosmetic and dermatological compositions for combating hair loss, based on a combination of the following active ingredients: N-acetylcysteine (NAC) and / or cysteine and / or methionine and / or S-adenosyl-methionine and / or N-acetyl methionylarginyl ethyl ester and / or their derivatives, - Resveratrol and / or Viniferin and / or their derivatives, - Arginine and / or lysine and / or their derivatives; in combination or in admixture with one or more inert, non-toxic, dermatologically acceptable excipients or carriers. These various compounds are described as having the following effects: NAC, cysteine, methionine: reduction of cell degeneration: * by protection against oxidative stress, which induces inflammation in the capillary bulb * by limitation upstream of factors of the apoptosis (cell death) Resveratrol, Viniferin: prolongation of the lifespan of capillary bulb cells: * by limiting the deleterious effects of androgens (testosterone, A4-androstenedione) * by activating Sirtuins, in particular SIRT-1 Arginine, Lysine: retardation of the stiffening of the fibers around the capillary bulb: by reduction of the glycation and glycoxidation process of the collagen fibers Among the derivatives of N-acetylcysteine, cysteine, methionine and S-adenosylmethionine, may be mentioned their salts and their esters, especially lipophilic esters (propyl ester, butyl, cyclohexyl ... ), as well as their lipophilic amides. Among the derivatives of Resveratrol, mention may be made of the oligomers of Resveratrol other than Viniferin, optionally in the form of vine shoot extract Vitis vinifera. Among the Arginine and Lysine derivatives, mention will be made especially of those of L-10 Arginine and L-Lysine, such as their esters or their salts, in particular the hydrochloride, the sulphate or the pidolate. According to one preferred form of the invention, Silanetriol Lysinate (INCI name), a coupling product between lysine and methylsilanetriol, is used as a derivative of lysine. This compound is especially marketed under the trade name SILYSIN C. (EXSYMOL) According to one preferred form of the invention, the compositions also contain one or more silanols, such as silanediol salicylate or silanetriol salicylate (INCI name), which have According to one preferred form of the invention, the compositions also contain cyclopirox and / or ciclopiroxolamine and / or piroctone olamine and / or another antibacterial and / or antifungal agent, so as to reduce the anti-inflammatory and anti-inflammatory properties. reduce microorganism-induced scalp inflammation, especially Malassezia species, such as M.globosa, M.furfur, M. sympodialis and M restricta Mechanism of action of the various active ingredients: N-acetylcysteine ( NAC) and cysteine HSNHAc HSH2 COOH COOH N-Acetylcysteine Cysteine 2903309 4 - Antioxidant Properties One of the factors of alopecia is the inflammatory reaction pr ovoed by the presence of oxidants and free radicals (oxidative stress). NAC and cysteine have a free sulfhydryl group (-SH). This sulfhydryl group has the ability to interact directly with free radicals such as hydrogen peroxide (H2O2) to form water (H2O) and oxygen (O2). In this reaction, two sulfur molecules are oxidized, thus forming a disulfide bridge (R = residue). NAC and cysteine also remove the hydroxyl radical (OH). In addition to its direct anti-radical function, NAC and cysteine 15 have been shown to stimulate glutathione production. Glutathione is an essential intracellular antioxidant whose role is to trap and break down lipid peroxides and hydrogen peroxide. NAC and cysteine can therefore provide two types of protection against inflammatory lesions caused by oxidative stress: direct protection and indirect protection through glutathione. Upstream Limitation of Apoptosis Factors N-acetylcysteine and cysteine inhibit the action of the nuclear transcription factor: kB-Factor, probably by virtue of their ability to maintain redox potential within the cell (Senaldi et al., Protective effect of N-acetylcystein in hapten-induced irritant and contact hypersensitivity reactions, 1994, The Society for Investigative Dermatology, Inc.). The nuclear transcription factor is known to cause the transcription of several genes, among which are the genes encoding pro-inflammatory cytokines: TNF-a and IL-1-a. In addition, NAC has been shown to antagonize the development of delayed inflammation and hypersensitivity reactions, and its action includes a reduction in the level of mRNA encoding TNF-α (op cit). Since inflammatory lesions caused by TNF-α are partially elicited by reactive oxidative intermediates, the production of which is stimulated by TNF-α, NAC and cysteine could inhibit the development of TNF-α / dependent inflammatory reactions. by blocking both oxidative stress (free radicals) and preventing the synthesis of TNF-α by inhibition of the nuclear transcription factor (NF-κB). The apoptotic process of a cell is described below: Destruction During the signaling phase, the cell receives a set of signals that can generate different responses. These rates are then integrated by the cell that will respond according to its genetic context, its state and its environment. The decision process is influenced by a series of intracellular mediators. The degradation phase results in visible manifestations of apoptosis, including condensation and chromatin degradation. By their inhibition of degradation mechanisms upstream of the process, NAC and cysteine therefore exhibit an indirect anti-apoptotic effect. - Methionine and S-adenosylmethionine The interest of these compounds is to generate in situ cysteine, by the following catabolic process: • cell damage (cytotoxic agents, hypoxia, date, loss of adhesion.) • receptors ( Fas1TNF - ,,. Glucoctticoids._ 1 • deficiency in growth factors (NGF, IL-2 .. Signaling 1 (Regulation • p53 • BcI2 / Ced-9 ™) Kinases • phosphatases • FADD! T S.4F; 'tV ORTi TRADD / RIP) FLI C. E-MACH • cytochrome C. dATP • oncogene tc-myc .... (• proteins regulating the cell cycle • Transcription factors • Tc-proteinase = tcaspasesr • ntuclèases • AIF (apoptosis inducinQ factor) proteolysis degradation of DNA ## STR4 ## HO 2 Methionine SNH2 Adenosyltransferase COOH ATP Pi + PPi Methionine OH HO OH NH2 HS Adenosylhomocysteinase Ade COOH COOH OH2 HO OH S-adenosyl homocysteine Cystathionyl 13 -synthase Adenosine Hornocysteine The compositions containing methionine or adenosylmethionine may thus have the effects described for cysteine. 5 - N-acetyl methionylarginyl ethyl ester SMe OO EtO NH O NH2 Acetyl methionylarginyl ethyl ester - Antioxidant properties The antioxidant properties of acetyl methionylarginyl ethyl ester (MR-LIP) were determined according to 2 experimental models: HH 2903309 7 • L The hydroxyl radical deactivation activity (OH) was determined according to the procedure described by Rehman et al. al. (British J. of Pharmacol 1997, 122, 1702-1706). MR-LIP and products derived from its enzymatic bioconversion are effective deactivators of OH *. The activity of MR-LIP is comparable to that of ascorbic acid. • Superoxide anion (02 "•) deactivation activity was determined according to the procedure described by Bagchi et al., (General Pharmacol 1997, 28, 85-91) The activity of MR-LIP is comparable to that of acetylmethionine Anti-inflammatory properties The anti-inflammatory activity of acetyl methionylarginyl ethyl ester was determined by studying the release of pro-inflammatory cytokines (IL-1α, TNF-α, IL-8). ) after UVB irradiation of a reconstituted human epidermis (Example 1).
Des quantités millimolaires de MR-LIP réduisent fortement la libération des cytokines pro-inflammatoires IL-la, TNF-a et IL-8. En conséquence, de même que la NAC, l'acétyl méthionylarginyl éthylester présente une activité anti-apoptotique indirecte par inhibition en amont de certains mécanismes de 20 l'apoptose. - Le Resvératrol et la Viniférine OH Resvératrol - Limitation des effets délétères des androgènes 25 L'alopécie androgéno-génétique touche des hommes dont les cheveux ont une sensibilité héréditaire au effets des androgènes (Hamilton. JB., 1951, 1971). Cette alopécie androgéno- OH HO 2903309 8 génétique se caractérise par une perte visible des cheveux sur certaines zones du cuir chevelu, consécutive à une miniaturisation progressive des follicules pileux. Elle ne s'observe pas chez les hommes porteurs d'un déficit génétique en 5a-réductase (5a-R) de type II : "pseudo-hermaphrodisme", enzyme assurant la réduction de la testostérone en 5 dihydrotestostérone (DHT), suggérant ainsi le rôle de la de la DHT dans la pathogenèse de cette condition (Imperato-McGinley J., Science 1974). Le Resvératrol ou 3,4,5'-trihydroxystilbène, se trouve à l'état naturel dans différentes classes de végétaux et particulièrement dans la vigne Vitis vinifera ou les extraits de sarments de 10 vigne. La Viniférine est un dimère du Resvératrol. Le Resvératrol et la Viniférine présentent la particularité d'inhiber l'activité de l'enzyme 5a-réductase (Exemple 2), limitant par conséquent les effets des androgènes sur les follicules pileux. - Activation des Sirtuines 15 Les Sirtuines sont une famille de déacétylases NAD(+)-dépendantes. (NAD = nicotinamide dinucléotide). Les Sirtuines sont connues pour améliorer la stabilité de l'ADN : elles interviennent dans des mécanismes dépendants de la protéine p53 (Luo et. al., Cell 2001, 107, 137-148), cette protéine étant fortement impliquée dans la réparation de l'ADN, notamment après agression UV. Les Sirtuines sont également des médiateurs de la régulation de la transcription (Motta et. al., Cell 2004, 116, 551-563) et de l'allongement de la durée de vie des cellules (Howitz et. al., Nature 2003, 425, 191-196 ; Wood et. al., Nature 2004, 430, 686-689). Les Sirtuines sont par conséquent susceptibles de prolonger la durée de vie des cellules du 25 bulbe capillaire, donc de lutter contre la chute des cheveux. Le Resvératrol et ses dérivés sont des activateurs de Sirtuines humaines, notamment de SIRT-1 (Borra et. al., J. Biol. Chem. 2005, 280, 17187-17195). Cette propriété du Resvératrol a conduit à son utilisation dans des préparations antivieillissement (voir par exemple 30 FR2867977) et justifie également son incorporation dans une composition anti-chute de cheveux. 9 2903309 - L'Arginine et la Lysine NH O O H2NN NH2 Arginine Lysine OH - Inhibition du processus de glycation du collagène Le processus de glycation englobe l'ensemble des réaction non enzymatiques intervenant 5 entre un sucre réducteur (glucose, fructose, ribose...) et un acide aminé ou la chaîne latérale d'un acide aminé appartenant à une protéine. Il peut dans certains cas, s'il est irréversible, contribuer à la détérioration des fonction cellulaires et tissulaires vitales de l'organisme. Ainsi, lorsqu'une protéine de demi-vie longue, comme le collagène, se lie à un sucre 10 réducteur, il s'ensuit de profondes modifications structurales qui aboutissent à la formation de liaisons chimiques croisées stables, ou "cross-linking" intra- ou intermoléculaires. Cette réticulation anarchique du réseau de fibres collagéniques augmente avec l'âge ; il peut conduire à une rigidification des fibres par accumulation de collagène réticulé, engendrant 15 une diminution de la souplesse et de la tonicité de ces mêmes fibres. Ce phénomène est favorisé entre autres par le stress oxydatif, d'où la notion de glycoxydation . 20 Lors du processus de glycation, le groupement aldéhyde d'un sucre réducteur se lie à la fonction amine d'un reste lysyle ou d'un reste arginyle porté par le collagène. Etant porteuses de fonctions identiques, la lysine et l'arginine entrent en compétition avec les groupements lysyle et arginyle du collagène, bloquant ainsi les sucres réducteurs en réagissant avec leur fonction aldéhyde. Elles inhibent ainsi le processus de glycation et/ou de glycoxydation, et la rigidification des fibres du collagène. Or, le collagène est un élément important de la lame basale, mince lacis de composants (collagène de type IV, lamiline, protéoglycanes, intégrines) qui permet de maintenir la 2903309 lo jonction entre la papille dermique et le pôle basal des cellules germinatives du bulbe pileux. L'arginine et la lysine, inhibant la dégradation de la lame basale, sont donc des facteurs de préservation des cellules capillaires. 5 Le Silanetriol Lysinate présente également des propriétés antiglycation, comparables voire supérieures à celles de la lysine. Selon une forme préférentielle de l'invention, la teneur des compositions en N-acétylcystéine (NAC) et/ou cystéine et/ou méthionine et/ou S-adénosyl méthionine et/ou N-acétyl 10 méthionylarginyl éthylester et/ou leurs dérivés est de 0,001 à 10% par rapport au poids total de la composition. Selon une forme préférentielle de l'invention, la teneur des compositions en Resvératrol et/ou Viniférine et/ou leurs dérivés est de 0,001 à 10% par rapport au poids total de la composition. Selon une forme préférentielle de l'invention, la teneur des compositions en arginine et/ou lysine et/ou Silanetriol Lysinate et/ou leurs dérivés est de 0,01 à 20% par rapport au poids total de la composition. 20 Les compositions selon l'invention comprennent un support inerte, non toxique, cosmétiquement ou dermatologiquement acceptable, en association ou en mélange avec le principe actif. Elles peuvent renfermer les adjuvants couramment utilisés dans les domaines cosmétiques et dermatologiques, comme par exemple des agents adoucissants, des gélifiants, des antioxydants, des solvants, des filtres, des conservateurs, des pigments ou des parfums. 25 Elles peuvent comporter un véhicule approprié destiné à une forme compatible avec l'application topique, comme une solution aqueuse, hydroalcoolique, hydroglycolique ou huileuse, une dispersion, une suspension, une émulsion huile dans eau ou eau dans huile, un gel aqueux ou huileux, une crème, un lait, une pommade, une lotion, une pâte, une mousse ou un aérosol. Millimolar amounts of MR-LIP strongly reduce the release of pro-inflammatory cytokines IL-1α, TNF-α, and IL-8. Accordingly, like NAC, acetyl methionylarginyl ethyl ester exhibits indirect anti-apoptotic activity by upstream inhibition of certain mechanisms of apoptosis. Resveratrol and Viniferine OH Resveratrol - Limitation of the deleterious effects of androgens Androgenetic alopecia affects men whose hair has a hereditary sensitivity to the effects of androgens (Hamilton, J.B., 1951, 1971). This genetic androgenic alopecia is characterized by a visible loss of hair on certain areas of the scalp, following a progressive miniaturization of the hair follicles. It is not observed in men with a genetic deficiency of type II 5a-reductase (5a-R): "pseudo-hermaphroditism", an enzyme that reduces testosterone to dihydrotestosterone (DHT), thus suggesting the role of DHT in the pathogenesis of this condition (Imperato-McGinley J., Science 1974). Resveratrol or 3,4,5'-trihydroxystilbene is found naturally in different classes of plants and particularly in Vitis vinifera vines or vine shoot extracts. Viniferine is a dimer of Resveratrol. Resveratrol and Viniferin have the particularity of inhibiting the activity of the enzyme 5α-reductase (Example 2), thereby limiting the effects of androgens on hair follicles. Sirtuins Activation Sirtuins are a family of NAD (+) - dependent deacetylases. (NAD = nicotinamide dinucleotide). Sirtuins are known to improve the stability of DNA: they intervene in mechanisms dependent on the p53 protein (Luo et al., Cell 2001, 107, 137-148), this protein being strongly involved in the repair of DNA, especially after UV aggression. Sirtuins are also mediators of transcriptional regulation (Motta et al., Cell 2004, 116, 551-563) and of longer cell life (Howitz et al., Nature 2003, 425, 191-196, Wood et al., Nature 2004, 430, 686-689). Sirtuines are therefore likely to prolong the life of the cells of the hair bulb, so to fight against hair loss. Resveratrol and its derivatives are activators of human Sirtuins, especially SIRT-1 (Borra et al., J. Biol Chem 2005, 280, 17187-17195). This property of Resveratrol has led to its use in anti-aging preparations (see for example FR2867977) and also justifies its incorporation into an anti-hair loss composition. Arginine and Lysine NH OO H2NN NH2 Arginine Lysine OH Inhibition of the Collagen Glycation Process The glycation process encompasses all non-enzymatic reactions occurring between a reducing sugar (glucose, fructose, ribose, etc.). .) and an amino acid or side chain of an amino acid belonging to a protein. It can in some cases, if irreversible, contribute to the deterioration of vital cellular and tissue functions of the body. Thus, when a long half-life protein, such as collagen, binds to a reducing sugar, it results in profound structural changes which result in the formation of stable cross-linking or cross-linking. - or intermolecular. This anarchic crosslinking of the collagen fiber network increases with age; it can lead to a stiffening of the fibers by accumulation of cross-linked collagen, causing a decrease in the suppleness and the tonicity of these same fibers. This phenomenon is favored among other things by oxidative stress, hence the notion of glycoxidation. In the glycation process, the aldehyde moiety of a reducing sugar binds to the amine function of a lysyl residue or an arginyl residue carried by the collagen. Since they carry identical functions, lysine and arginine compete with the lysyl and arginyl groups of collagen, thus blocking reducing sugars by reacting with their aldehyde function. They thus inhibit the glycation and / or glycoxidation process and the stiffening of the collagen fibers. However, collagen is an important element of the basal lamina, thin lacis of components (type IV collagen, lamilin, proteoglycans, integrins) which makes it possible to maintain the junction between the dermal papilla and the basal pole of the germinal cells of the bulb. hair. Arginine and lysine, which inhibit the degradation of the basal lamina, are therefore factors for the preservation of capillary cells. Silanetriol Lysinate also has anti-glycation properties, comparable to or even greater than those of lysine. According to a preferred form of the invention, the content of the compositions of N-acetylcysteine (NAC) and / or cysteine and / or methionine and / or S-adenosyl methionine and / or N-acetyl 10 methionylarginyl ethyl ester and / or their derivatives is from 0.001 to 10% relative to the total weight of the composition. According to a preferred form of the invention, the content of Resveratrol and / or Viniferin compositions and / or their derivatives is from 0.001 to 10% relative to the total weight of the composition. According to a preferred form of the invention, the content of arginine and / or lysine and / or Silanetriol Lysinate compositions and / or their derivatives is from 0.01% to 20% relative to the total weight of the composition. The compositions according to the invention comprise an inert, non-toxic, cosmetically or dermatologically acceptable carrier, in combination or in admixture with the active ingredient. They may contain adjuvants commonly used in the cosmetic and dermatological fields, such as, for example, softening agents, gelling agents, antioxidants, solvents, filters, preservatives, pigments or perfumes. They may comprise a suitable vehicle intended for a form compatible with topical application, such as an aqueous, hydroalcoholic, hydroglycolic or oily solution, a dispersion, a suspension, an oil-in-water or water-in-oil emulsion or an aqueous or oily gel. , a cream, a milk, an ointment, a lotion, a paste, a mousse or an aerosol.
L'invention a également pour objet l'utilisation à des fins cosmétiques des compositions selon l'invention, pour lutter contre la chute des cheveux. A cette fin, les compositions selon l'invention seront appliquées sur le cuir chevelu en quantité efficace, de préférence à raison de 1 à 3 applications par jour. The subject of the invention is also the use for cosmetic purposes of the compositions according to the invention for combating hair loss. For this purpose, the compositions according to the invention will be applied to the scalp in an effective amount, preferably at a rate of 1 to 3 applications per day.
15 11 2903309 Les exemples suivants illustrent l'invention sans toutefois la limiter. Exemple 1 : Activité anti-inflammatoire de l'acétyl méthionylarginyl éthylester (MRLIP) 5 L'activité anti-inflammatoire de l'acétyl méthionylarginyl élliylesler a clé déteiuuuuéc ~rr utilisant de l'épiderme humain reconstitué (EHR), un modèle de culture cellulaire tridimensionnel ayant une forte homologie histo-morphologique et biochimique avec l'épiderme humain normal (Rosdy et. al., J. of Investigative Dermatology 1990, 65, 409-414).The following examples illustrate the invention without, however, limiting it. Example 1: Anti-Inflammatory Activity of Acetyl Methionyl Arginyl Ethyl Ester (MRLIP) The anti-inflammatory activity of acetyl methionyl arginyl elylylester was determined using reconstituted human epidermis (EHR), a cell culture model three-dimensional with strong histo-morphological and biochemical homology with normal human epidermis (Rosdy et al., J. of Investigative Dermatology 1990, 65, 409-414).
10 L'EHR a été irradié aux UVB (300 mJ.cm"2) et la libération de cytokines pro-inflammatoires (IL-la, TNF-a, IL-8) a été contrôlée durant 24 heures post-irradiation. L'activité du MR-LIP est comparée à celle de l'hydrocortisone (HC). Les résultats sont rassemblés ci-dessous : Contrôle UVB UVB UVB UVB (pas d'irradiation) HC 0,1% MR-LIP 1mM MR-LIP 5mM IL-la (pg/ml) 0 150 59 90 63 TNF-a (pg/ml) 0 121 5 25 13 IL-8 (pg/ml) 0 620 130 104 231 Tableau 1 Des quantités millimolaires de MR-LIP réduisent fortement la libération des cytokines pro-15 inflammatoires IL-la, TNF-a et IL-8. Le MR-LIP a une activité comparable à l'hydrocortisone. Exemple 2 : Quantification de l'activité inhibitrice du Resvératrol et de la Viniférine sur la 5a-R (in vitro) 20 Les essais in vitro ont été réalisés sur des fibroblastes isolés de derme humain. Les cellules sont d'abord mises en culture, puis pré-incubées pendant 2 heures dans des milieux de culture contenant du Resvératrol, de la Viniférine et de l'extrait de sarment de vigne (Resvératrox ), aux concentrations de 1, 10 et 50 g/mL. Les fibroblastes sont ensuite 25 incubés pendant 22 heures à 37 C dans une atmosphère à 5% de CO2, en présence du produit testé (Resvératrol, Viniférine ou extrait de sarment de vigne) et du milieu de culture additionné de testostérone tritiée (4 .tM). Des cultures témoins sont menées en parallèle en milieu de culture additionné de testostérone. Les résultats du test sont détaillés dans le Tableau 2 : 30 2903309 12 Inhibition de l'activité 5-a-réductasique (résultats exprimés en pourcentage d'inhibition) Concentration Resvératrol Viniférine Extrait de sarments de vigne 1 g/mL 9% 15% 10% 10 g/mL 20% 32% 25% 50 p.g/mL 60% 72% 66% Tableau 2 Le test a été validé par comparaison avec l'activité du Finastéride, inhibiteur de référence de la 5-a-réductase. Le résultat est présenté sur le Graphique 1 : "inh trition/5a-R 5ù40 ù 3o ù 20 ù 1' ê 0 Finastéride Resvèratrte Extrait de sarments 2.S nig rn' 1 g/m1 de vigne 2;5 ngtrr t 1 G Ngirr 1 pcc]rn 50 pend pg.trr 50i .r 'rra 5 Graphique 1 Les résultats représentés ci-dessus montrent que le Resvératrol et les dérivés du Resvératrol inhibent de façon significative l'activité de l'enzyme 5-a-réductase. L'inhibition de l'activité 5-a-réductase est dose-dépendante. 60 ù 60 - 10 2903309 Exemple 3 : Lotion anti-chute des cheveux Constituants Nomenclature INCI Qté (% massique) Pyridoxine chlorhydrate Vit. B6 Pyridoxine hydrochloride 0,1 Butylène glycol û 1,3 Butylene glycol 2,0 Dow CorningV 193 Dimeticone copolyol 1,0 Silysin C" Silanetriol lysinate 5,0 Ethylargininoate Ethylargininoate 1,0 acétamidométhionamide acétamidométhionamide Alcool hydrochloride 25,0 Alcohol Piroctone olamine Piroctone olamine 0,2 Resvératrox" Vitis vinifera vine extract 0,2 Eau purifiée Aqua Qsp 100 13The EHR was irradiated with UVB (300 mJ.cm -2) and the release of pro-inflammatory cytokines (IL-1α, TNF-α, IL-8) was monitored for 24 hours post-irradiation. MR-LIP activity is compared with that of hydrocortisone (HC) The results are summarized below: UVB UVB UVB UVB (no irradiation) HC 0.1% MR-LIP 1mM MR-LIP 5mM IL (1 μg / ml) TNF-α (μg / ml) IL-8 (μg / ml) Table 1 Millimolar quantities of MR-LIP strongly reduce the release of the pro-inflammatory cytokines IL-1α, TNF-α and IL-8 MR-LIP has an activity comparable to hydrocortisone Example 2: Quantification of the inhibitory activity of Resveratrol and Viniferin on the 5α R (in vitro) The in vitro tests were carried out on fibroblasts isolated from human dermis The cells are first cultured and then preincubated for 2 hours in culture media containing Resveratrol, Viniferin and vine shoot extract (Resveratrox), at concentrations of 1, 10 and 50 g / mL. The fibroblasts are then incubated for 22 hours at 37 ° C. in a 5% CO 2 atmosphere, in the presence of the tested product (Resveratrol, Viniferine or vine shoot extract) and the culture medium supplemented with tritiated testosterone (4 μM). ). Control cultures are run in parallel in culture medium supplemented with testosterone. The results of the test are detailed in Table 2: Inhibition of 5-α-reductase activity (results expressed as percent inhibition) Concentration Resveratrol Viniferin Vine shoot extract 1 g / ml 9% 15% % 10 g / mL 20% 32% 25% 50 μg / mL 60% 72% 66% Table 2 The test was validated by comparison with the activity of Finasteride, a reference inhibitor of 5-α-reductase. The result is shown in Fig. 1: "Inhibition / 5a-R 5u40 to 3o to 20 ° to 0 ° Finasteride Resvertree Extract from vine shoots 2. Seed 1 g / m2 vine 2; 5 ngtrr t 1 G The results shown above show that Resveratrol and Resveratrol derivatives significantly inhibit the activity of the enzyme 5-alpha-reductase. Inhibition of 5-a-reductase activity is dose-dependent 60 - 60 - 2903309 Example 3: Anti-Hair Loss Lotion Constituents INCI Nomenclature Qty (% by weight) Pyridoxine hydrochloride Vit B6 Pyridoxine hydrochloride 0.1 1,3-Butylene glycol Butylene glycol 2.0 Dow CorningV 193 Dimeticone copolyol 1.0 Silysin C Silanetriol lysinate 5.0 Ethylargininoate Ethylargininoate 1.0 acetamidomethionamide acetamidomethionamide Alcohol hydrochloride 25.0 Alcohol Piroctone olamine Piroctone olamine 0.2 Resveratrox "Vitis vinifera vine extract 0.2 Aqua purified water Qs 100 13
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2354103A1 (en) * | 2010-12-27 | 2011-03-10 | Cosmetica Cosbar S.L. | Capillary composition activator of the sirtuinas and use of the sirtuinas. (Machine-translation by Google Translate, not legally binding) |
| GB2481712A (en) * | 2010-06-30 | 2012-01-04 | Pangaea Lab Ltd | Composition including ciclopirox olamine and VEGF for treating hair loss |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1103738A (en) * | 1964-08-18 | 1968-02-21 | Oreal | Composition for treating the scalp |
| FR2152935A1 (en) * | 1971-09-13 | 1973-04-27 | Treuhandvereinigung Ag | |
| EP0335554A2 (en) * | 1988-03-23 | 1989-10-04 | Unilever Plc | Cosmetic composition |
| JP2001072552A (en) * | 1999-09-07 | 2001-03-21 | Sunstar Inc | Hair growth composition |
| US6207713B1 (en) * | 1997-09-17 | 2001-03-27 | Eric T. Fossel | Topical and oral delivery of arginine to cause beneficial effects |
| US6294520B1 (en) * | 1989-03-27 | 2001-09-25 | Albert T. Naito | Material for passage through the blood-brain barrier |
| FR2816843A1 (en) * | 2000-11-23 | 2002-05-24 | Actichem | 5-Alpha reductase inhibitor used for treating disorders due to excess dihydrotestosterone e.g. acne and alopecia comprise cis or trans resveratrol and its derivatives |
| WO2004034820A2 (en) * | 2002-10-16 | 2004-04-29 | L'oreal | Cosmetic composition for preventing and/or correcting the functional disorders of the pilo-sebaceous unit of mammals |
-
2006
- 2006-07-07 FR FR0606207A patent/FR2903309B1/en not_active Expired - Fee Related
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1103738A (en) * | 1964-08-18 | 1968-02-21 | Oreal | Composition for treating the scalp |
| FR2152935A1 (en) * | 1971-09-13 | 1973-04-27 | Treuhandvereinigung Ag | |
| EP0335554A2 (en) * | 1988-03-23 | 1989-10-04 | Unilever Plc | Cosmetic composition |
| US6294520B1 (en) * | 1989-03-27 | 2001-09-25 | Albert T. Naito | Material for passage through the blood-brain barrier |
| US6207713B1 (en) * | 1997-09-17 | 2001-03-27 | Eric T. Fossel | Topical and oral delivery of arginine to cause beneficial effects |
| JP2001072552A (en) * | 1999-09-07 | 2001-03-21 | Sunstar Inc | Hair growth composition |
| FR2816843A1 (en) * | 2000-11-23 | 2002-05-24 | Actichem | 5-Alpha reductase inhibitor used for treating disorders due to excess dihydrotestosterone e.g. acne and alopecia comprise cis or trans resveratrol and its derivatives |
| WO2004034820A2 (en) * | 2002-10-16 | 2004-04-29 | L'oreal | Cosmetic composition for preventing and/or correcting the functional disorders of the pilo-sebaceous unit of mammals |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2481712A (en) * | 2010-06-30 | 2012-01-04 | Pangaea Lab Ltd | Composition including ciclopirox olamine and VEGF for treating hair loss |
| GB2481712B (en) * | 2010-06-30 | 2013-01-30 | Pangaea Lab Ltd | Composition comprising vascular endothelial growth factor (VEGF) for the treatment of hair loss |
| ES2354103A1 (en) * | 2010-12-27 | 2011-03-10 | Cosmetica Cosbar S.L. | Capillary composition activator of the sirtuinas and use of the sirtuinas. (Machine-translation by Google Translate, not legally binding) |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2903309B1 (en) | 2008-10-10 |
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| CD | Change of name or company name |
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