Use of cysteine precursor compounds

Abstract

Use of a carboxymethylcysteine compound or a hair care composition comprising a carboxymethylcysteine compound for increasing melanin production and / or for increasing cellular metabolic activity of melanocytes.

Description

Technical Field

[0001] This invention relates to novel uses of carboxymethylcysteine ​​compounds or hair care compositions containing carboxymethylcysteine ​​compounds. Background Technology

[0002] As people age, the appearance of their hair may become less desirable. Graying and whitening of hair are common signs of aging. Hair also loses its elasticity, becoming thinner and more fragile. In addition, the diameter of hair follicles and the number of hairs can also decrease, resulting in a sparse appearance of the scalp.

[0003] For many consumers, maintaining hair color and good thickness, volume, and hair count is a way to mitigate signs of aging. Many people choose to dye their hair to mask age-related graying or whitening. However, hair dyeing does not help conceal other age-related changes in hair quality. On the contrary, chemical hair dyes are known to cause increased hair damage over time.

[0004] There remains a long-standing need to provide consumers with compositions that effectively reduce age-related functional changes in hair pigmentation. There is also a need for a composition that can reduce or prevent other harmful changes in age-related hair.

[0005] Surprisingly, carboxymethylcysteine ​​(CMC) precursor compounds have been found to be effective in reducing age-related functional changes in hair pigmentation, while also providing beneficial improvements in additional age-related hair characteristics. For example, CMC has surprisingly shown to enhance cellular metabolic activity and melanin production in melanocytes. Advantageously, CMC can increase melanin production in melanocytes above natural pigmentation levels. Summary of the Invention

[0006] In a first aspect, the present invention relates to the use of carboxymethylcysteine ​​compounds or hair care compositions containing carboxymethylcysteine ​​compounds for increasing melanin production in melanocytes, for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in hair (e.g., gray hair), for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, for reducing oxidative stress in the scalp and / or hair follicles, and for increasing cellular metabolic activity. Preferably, the present invention relates to carboxymethylcysteine ​​compounds or hair care compositions containing carboxymethylcysteine ​​compounds for increasing melanin production in hair follicles. Preferably, it is for increasing the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is for increasing the melanin production of melanocytes to a level exceeding the natural pigmentation level. Preferably, the present invention relates to a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound, which is used to enhance the cellular metabolic activity of melanocytes, preferably for enhancing the cellular metabolic activity of melanocytes in hair follicles. More preferably, it is used to increase the level of cellular metabolic activity of melanocytes to a level higher than that in unstressed melanocytes.

[0007] In a second aspect, the present invention relates to a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound for therapeutic purposes, which is used to increase melanin production in melanocytes, to reduce the appearance of gray or white hair in an individual, to reduce age-related functional changes in hair pigmentation, to increase melanin production in gray hair, to increase cell proliferation, to increase melanocyte proliferation, to increase melanosome transfer, to increase the level and / or activity of tyrosinase, to increase gene and / or protein expression in hair-related pigmentation pathways, to reduce oxidative stress in the scalp and / or hair follicles, and / or to improve cellular metabolic activity. Preferably, the present invention relates to a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound for therapeutic purposes, which is used to increase melanin production in melanocytes, preferably for increasing melanin production in hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase the melanin production level of melanocytes to a level exceeding the natural pigmentation level. Preferably, the present invention relates to a carboxymethylcysteine ​​compound for therapeutic use or a hair care composition containing a carboxymethylcysteine ​​compound, which is used to increase melanin production in melanocytes, preferably to increase melanin production in hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase the melanin production of melanocytes to a level exceeding natural pigmentation levels. Preferably, the present invention relates to a carboxymethylcysteine ​​compound for therapeutic use or a hair care composition containing a carboxymethylcysteine ​​compound, which is used to enhance the cellular metabolic activity of cells in hair follicles, preferably to enhance the cellular metabolic activity of melanocytes, preferably to enhance the cellular metabolic activity of melanocytes in hair follicles. Preferably, it is used to enhance the cellular metabolic activity level of melanocytes to a level higher than that in unstressed melanocytes.

[0008] In a third aspect, the present invention relates to the use of hair care compositions for increasing melanin production in melanocytes, for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, for reducing oxidative stress in the scalp and / or hair follicles, and / or for increasing cellular metabolic activity. Preferably, the present invention relates to the use of hair care compositions for increasing melanin production in melanocytes, more preferably for increasing melanin production in hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. More preferably, it is used to increase the melanin production of melanocytes to a level exceeding natural pigmentation levels. Preferably, the present invention relates to hair care compositions for therapeutic purposes that increase the cellular metabolic activity of melanocytes, more preferably for increasing the cellular metabolic activity of melanocytes in hair follicles. Preferably, it is used to increase the level of cellular metabolic activity in melanocytes to a level higher than that in unstressed melanocytes.

[0009] In a fourth aspect, the present invention relates to a method for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, and reducing oxidative stress in the scalp and / or hair follicles, the method comprising applying a hair care composition comprising a cysteine ​​precursor compound to hair or scalp. Preferably, the method is used to increase melanin production in melanocytes, more preferably to increase melanin production in hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase melanin production in melanocytes beyond the natural pigmentation level. Preferably, the method is used to increase the cellular metabolic activity of melanocytes, more preferably to increase the cellular metabolic activity of melanocytes in hair follicles. Preferably, the method is used to increase the level of cellular metabolic activity in melanocytes to a level higher than that in unstressed melanocytes. The method involves applying a cosmetic composition containing a carboxymethylcysteine ​​compound to hair or scalp.

[0010] In a fifth aspect, the present invention relates to the use of carboxymethylcysteine ​​compounds in methods for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, and reducing oxidative stress in the scalp and / or hair follicles, said methods comprising applying a cosmetic composition comprising a cysteine ​​precursor compound to hair or scalp. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in methods for increasing melanin production in melanocytes, more preferably for increasing melanin production in hair follicles. Preferably, it is used to increase the level of melanin production in melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase melanin production in melanocytes beyond the natural pigmentation level. Preferably, the method is used to enhance the cellular metabolic activity of melanocytes, and more preferably, to enhance the cellular metabolic activity of melanocytes in hair follicles. More preferably, it is used to increase the cellular metabolic activity level of melanocytes to a level higher than that of unstressed melanocytes.

[0011] In a sixth aspect, the present invention relates to the use of carboxymethylcysteine ​​compounds in the preparation of medicaments for increasing melanin production, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, reducing oxidative stress in the scalp and / or hair follicles, and / or increasing cellular metabolic activity. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in the preparation of medicaments for increasing melanin production in melanocytes, more preferably for increasing melanin production in hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase melanin production in melanocytes beyond the natural pigmentation level. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in the preparation of medicaments for increasing the cellular metabolic activity of melanocytes, more preferably for increasing the cellular metabolic activity of melanocytes in hair follicles. Preferably, it is used to increase the level of cellular metabolic activity in melanocytes to a level higher than that in unstressed melanocytes.

[0012] All other aspects of the invention will become more readily apparent upon consideration of the following detailed description and embodiments. Detailed Implementation

[0013] According to the present invention, a "cysteine ​​precursor compound" can be understood as a compound that increases the concentration of cysteine ​​in the body. For example, a cysteine ​​precursor can be a compound that increases the availability of cysteine ​​to cells, thereby providing delivery of cysteine ​​to cells to increase intracellular production of glutathione.

[0014] Surprisingly, it has been found that by including materials that can be converted into cysteine ​​in the body in hair care compositions, harmful changes in hair associated with aging can be reduced or prevented, as described above.

[0015] Not wanting to be bound by theory, it is believed that including materials that can be converted into cysteine ​​in the body in hair care compositions can increase the intracellular production of glutathione.

[0016] Glutathione (GSH) is a tripeptide composed of glutamic acid, cysteine, and glycine. It is present in all mammalian tissues. It is a major antioxidant in living organisms: it protects cells from oxidation by quenching reactive oxygen species. GSH and cysteine ​​are also involved in the melanin production pathway, which is responsible for the formation of colored hair, particularly blonde and / or red hair. GSH biosynthesis occurs in cells in a tightly regulated manner. The amount of glutathione in cells depends largely on the availability of cysteine. Therefore, agents that deliver cysteine-containing substances to cells are thought to increase intracellular glutathione production.

[0017] Cysteine ​​(a complex amino acid of GSH) can increase cellular GSH levels, but its exposed sulfhydryl groups make it unstable and reactive, and also cause a strong, unpleasant odor. Therefore, it is preferable to apply a carboxymethylcysteine ​​compound that can be safely administered and converted into cysteine ​​intracellularly, so that cysteine ​​can be used for intracellular GSH production.

[0018] In some embodiments, the carboxymethylcysteine ​​compound is present in an amount of 0.0001% to 5% of the total weight of the composition, more preferably at least 0.001%, even more preferably at least 0.01%, still even more preferably at least 0.1%, and most preferably at least 0.4% of the weight of the composition. Preferably, the carboxymethylcysteine ​​compound is present in an amount not exceeding 3% of the weight of the composition, even more preferably not exceeding 2%, even even more preferably not exceeding 1.5%, and most preferably not exceeding 1%.

[0019] A carboxymethylcysteine ​​compound refers to a compound selected from carboxymethylcysteine, a salt of carboxymethylcysteine, an ester of carboxymethylcysteine, an amide of carboxymethylcysteine, or a mixture thereof. Preferably, the carboxymethylcysteine ​​compound comprises carboxymethylcysteine, an ester of carboxymethylcysteine, and / or a salt of carboxymethylcysteine. More preferably, the carboxymethylcysteine ​​compound comprises carboxymethylcysteine ​​and / or a salt of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine ​​compound comprises a salt of carboxymethylcysteine. Still even more preferably, the carboxymethylcysteine ​​compound comprises a lysine carboxymethylcysteine ​​salt, and most preferably, the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt.

[0020] Preferably, the carboxymethylcysteine ​​compound is present in an amount of 0.0001% to 5% of the total weight of the composition, more preferably at least 0.001% of the weight of the composition, even more preferably at least 0.01%, even more preferably at least 0.1%, and most preferably at least 0.4%. Preferably, the carboxymethylcysteine ​​compound is present in an amount not exceeding 3% of the weight of the composition, even more preferably not exceeding 2%, even more preferably not exceeding 1.5%, and most preferably not exceeding 1%.

[0021] Preferably, lysine carboxymethylcysteine ​​is present in an amount of 0.0001% to 5% of the total weight of the composition, more preferably at least 0.001% of the weight of the composition, even more preferably at least 0.01%, even more preferably at least 0.1%, and most preferably at least 0.4%. Preferably, lysine carboxymethylcysteine ​​is present in an amount of no more than 3% of the weight of the composition, even more preferably no more than 2%, even more preferably no more than 1.5%, and most preferably no more than 1%.

[0022] Preferably, the use is non-therapeutic. Preferably, the method is non-therapeutic. The term non-therapeutic generally means used for cosmetic purposes rather than for curative or therapeutic purposes.

[0023] The hair care compositions of the present invention generally provide benefits for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, and for reducing oxidative stress in the scalp and / or hair follicles. Preferably, the benefits are selected from increasing melanin production and increasing cellular metabolic activity in melanocytes.

[0024] Preferably, the benefit is to increase melanin production in melanocytes within hair follicles. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that in unstressed melanocytes. Preferably, it is used to increase the melanin production of melanocytes to a level exceeding natural pigmentation levels. Preferably, the benefit is to enhance the metabolic activity of melanocytes within hair follicles. Preferably, it is used to enhance the cellular metabolic activity level of melanocytes to a level higher than that in unstressed melanocytes.

[0025] Preferably, the carboxymethylcysteine ​​compound is used as an agent to increase melanin production in melanocytes, such as increasing melanin production in melanocytes and / or enhancing cellular metabolic activity.

[0026] Preferably, the present invention provides the use of carboxymethylcysteine ​​compounds or hair care compositions containing carboxymethylcysteine ​​compounds for increasing melanin production in melanocytes, for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, for reducing oxidative stress in the scalp and / or hair follicles, and / or for increasing cellular metabolic activity.

[0027] Preferably, the present invention provides the use of a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound. Preferably, the present invention provides the use of a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound for increasing melanin production in melanocytes, more preferably for increasing melanin production in hair follicles. Preferably, the present invention provides the use of a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound for improving cellular metabolic activity in melanocytes, more preferably for improving cellular metabolic activity in melanocytes in hair follicles. Preferably, it is used to increase the level of cellular metabolic activity in melanocytes to a level higher than that in unstressed melanocytes. Most preferably, the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt.

[0028] More preferably, the present invention provides the use of lysine carboxymethyl cysteine ​​salt or hair care compositions containing lysine carboxymethyl cysteine ​​salt for increasing melanin production in melanocytes, preferably for increasing melanin production in hair follicles. More preferably, the present invention provides the use of lysine carboxymethyl cysteine ​​salt or hair care compositions for increasing melanin production in melanocytes, preferably for increasing melanin production in hair follicles, for increasing the melanin production level of melanocytes above the level of unstressed melanocytes, for increasing the melanin production of melanocytes above the natural pigmentation level, for improving the cellular metabolic activity of cells in hair follicles, preferably for improving the cellular metabolic activity of melanocytes in hair follicles.

[0029] Preferably, the present invention relates to the use of hair care compositions for increasing melanin production in melanocytes, for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, for reducing oxidative stress in the scalp and / or hair follicles, and / or for increasing cellular metabolic activity. Preferably, the present invention provides a hair care composition for increasing melanin production in melanocytes, preferably for increasing melanin production in hair follicles, preferably for increasing the melanin production level of melanocytes to a level higher than that in unstressed melanocytes, preferably for increasing the melanin production of melanocytes to a level exceeding natural pigmentation levels, preferably for increasing the cellular metabolic activity of cells in hair follicles, preferably for increasing the cellular metabolic activity of melanocytes in hair follicles, preferably for increasing the cellular metabolic activity level of melanocytes to a level higher than that in unstressed melanocytes, wherein the hair care composition comprises a carboxymethylcysteine ​​compound as an agent for increasing melanin production in melanocytes and / or for increasing the cellular metabolic activity of melanocytes.

[0030] Preferably, the present invention provides a hair care composition for increasing melanin production in melanocytes, more preferably for increasing melanin production in hair follicles, wherein the hair care composition comprises a carboxymethylcysteine ​​compound as an agent for increasing melanin production. Most preferably, the carboxymethylcysteine ​​compound is lysine carboxymethylcysteine ​​salt. Preferably, the present invention provides a hair care composition for improving the cellular metabolic activity of melanocytes, more preferably for improving the cellular metabolic activity of melanocytes in hair follicles, wherein the hair care composition comprises a carboxymethylcysteine ​​compound as an agent for improving the cellular metabolic activity of melanocytes. Most preferably, the carboxymethylcysteine ​​compound is lysine carboxymethylcysteine ​​salt.

[0031] Preferably, the present invention relates to a method for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, reducing oxidative stress in the scalp and / or hair follicles, and / or increasing cellular metabolic activity, the method comprising applying a hair care composition containing a carboxymethylcysteine ​​compound to hair or scalp. Most preferably, the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt. Preferably, the present invention relates to a method for increasing melanin production in melanocytes, preferably for increasing the melanin production level of melanocytes to a level higher than that in unstressed melanocytes, preferably for increasing the melanin production of melanocytes to exceed the natural pigmentation level, preferably for increasing cellular metabolic activity in cells or a combination thereof, and preferably for increasing the level of cellular metabolic activity of melanocytes to a level higher than that in unstressed melanocytes. Preferably, the present invention relates to a method for increasing melanin production in melanocytes, the method comprising applying a hair care composition containing a carboxymethylcysteine ​​compound.

[0032] Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in methods for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, reducing oxidative stress in the scalp and / or hair follicles, and / or increasing cellular metabolic activity, said methods comprising applying a cosmetic composition containing a carboxymethylcysteine ​​compound to hair or scalp. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in methods for increasing melanin production in melanocytes or increasing cellular metabolic activity in melanocytes, or combinations thereof. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds for increasing melanin production in melanocytes. Preferably, the compound is used to increase the melanin production level of melanocytes to a level higher than that of unstressed melanocytes, and more preferably, to increase melanin production in melanocytes to a level exceeding natural pigmentation. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds to increase cellular metabolic activity in melanocytes. Preferably, the compound is used to increase the cellular metabolic activity level of melanocytes to a level higher than that of unstressed melanocytes. Most preferably, the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt.

[0033] Preferably, the present invention provides the use of carboxymethylcysteine ​​compounds in the preparation of medicaments for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, reducing oxidative stress in the scalp and / or hair follicles, and / or increasing cellular metabolic activity. Preferably, the present invention relates to the use of carboxymethylcysteine ​​compounds in methods for increasing melanin production in melanocytes or increasing cellular metabolic activity in melanocytes, or combinations thereof. Preferably, the present invention provides the use of carboxymethylcysteine ​​compounds in the preparation of medicaments for increasing melanin production in hair follicles. Preferably, it is used to increase the level of melanin production in melanocytes to a level higher than that of unstressed melanocytes, and preferably to increase the level of melanin production in melanocytes to a level exceeding the natural pigmentation level. Preferably, the present invention provides the use of a carboxymethylcysteine ​​compound in the preparation of a medicament for enhancing cellular metabolic activity in hair follicles. Preferably, it is used to increase the cellular metabolic activity level of melanocytes to a level higher than that in unstressed melanocytes. Most preferably, the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt.

[0034] Preferably, lysine carboxymethylcysteine ​​salt is used as an agent for increasing melanin production in melanocytes, reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, increasing gene and / or protein expression in hair-related pigmentation pathways, reducing oxidative stress in the scalp and / or hair follicles, and / or increasing cellular metabolic activity. Preferably, it is used to increase the melanin production level of melanocytes to a level higher than that of unstressed melanocytes, and more preferably, to increase melanin production of melanocytes to a level exceeding natural pigmentation levels. Preferably, it is used to increase the cellular metabolic activity level of melanocytes to a level higher than that of unstressed melanocytes.

[0035] Hair care compositions containing lysine carboxymethylcysteine ​​generally provide more beneficial compounds that, compared to hair care compositions without lysine carboxymethylcysteine, increase melanin production in melanocytes, reduce the appearance of gray or white hair in an individual, reduce age-related functional changes in hair pigmentation, increase melanin production in gray hair, increase cell proliferation, increase melanocyte proliferation, increase melanosome transfer, increase tyrosinase levels and / or activity, increase gene and / or protein expression in hair-related pigmentation pathways, reduce oxidative stress in the scalp and / or hair follicles, and / or improve cellular metabolic activity.

[0036] Preferably, the carboxymethylcysteine ​​compounds and compositions of the present invention increase melanin production in melanocytes of the skin and / or hair. Preferably, the cysteine ​​precursor compounds and compositions of the present invention increase melanin production in hair follicles.

[0037] Preferably, the hair care composition according to the invention further comprises a glutamate source selected from glutamine, glutamine esters, glutamic acid, pyroglutamic acid, salts, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or salts of pyroglutamic acid. Even more preferably, the composition comprises a sodium salt of pyroglutamic acid. Preferably, the glutamate source is present in an amount of 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6%, and even more preferably 0.01 to 3% by weight of the composition.

[0038] Preferably, the composition comprises a polyol. The polyol may be selected from glycerol, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-butanediol, isopentyl glycol, ethoxylated glycerol, propoxylated glycerol, pentylene glycol, or mixtures thereof. The most preferred polyol is glycerol (also known as glycerol) or pentylene glycol. The amount of the polyol may be from 0.1% to 20% by weight of the composition, preferably from 0.5% to 15%, more preferably any range from 2% to 10%.

[0039] The compositions used in this invention (as described above) may contain additional active substances for improving the physical and / or aesthetic properties of the scalp and / or hair. Examples include amino acids, vitamins, minerals and / or antioxidants, emollients, moisturizers, sunscreens, anti-irritants, exfoliants, plant extracts (such as pomegranate, birch, green tea, chamomile and licorice extracts) and mixtures thereof, preservatives (such as sodium benzoate, potassium sorbate, phenoxyethanol, pentylene glycol and sodium metabisulfite), pH adjusters and fragrances (such as essential oils, flower oils, natural extracts from resins, gums, balms, legumes, mosses and other plants, as well as synthetic aromatic materials).

[0040] In some embodiments, the compositions of the present invention preferably further comprise a thickener. Suitable thickeners are selected from polyacrylic acid, crosslinked polymers of acrylic acid, copolymers of acrylic acid with hydrophobic monomers, copolymers of carboxylic acid-containing monomers with acrylates, crosslinked copolymers of acrylic acid with acrylates, heteropolysaccharide gums, and crystalline long-chain acrylic derivatives. Long-chain acrylic derivatives are ideally selected from ethylene glycol stearate, alkanolamides of fatty acids having 16 to 22 carbon atoms, and mixtures thereof. Ethylene glycol distearate and polyethylene glycol 3-distearate are preferred long-chain acrylic derivatives because they impart pearlescent properties to the composition. Polyacrylic acid is commercially available as Carbopol 420, Carbopol 488, or Carbopol 493. Polymers of acrylic acid crosslinked with multifunctional agents can also be used; these are commercially available as Carbopol 910, Carbopol 934, Carbopol 941, and Carbopol 980. An example of a suitable copolymer of carboxylic acid-containing monomers and acrylates is Carbopol 1342. All Carbopol (trademark) materials are available from Goodrich. Suitable crosspolymers of acrylic and acrylates are Pemulen TR1 or Pemulen TR2. Suitable heteropolysaccharide gum is xanthan gum, for example, available as Kelzan mu.

[0041] According to the present invention, a "penetration enhancer" can be understood as a compound that can penetrate hair follicles and / or scalp to reversibly reduce barrier resistance and increase the bioavailability of active substances to sites of action in hair follicles and / or scalp, such as compounds that increase the bioavailability of active substances to hair bulbs.

[0042] In some embodiments, the penetration enhancer is selected from glycols, such as polyethylene glycol; phospholipids, for example in the form of one or more liposomes; nonionic emulsifiers, such as polysorbate, lauryl ketone, isohexadecane, dodecane, DMSO, ethanol, decanol, isosorbide dimethyl ether and / or combinations thereof.

[0043] In some embodiments, the penetration enhancer is present in an amount of 0.01% to 20% of the total weight of the composition, more preferably at least 0.1% of the total weight of the composition, even more preferably at least 1%, even more preferably at least 2%, and most preferably at least 6%. Preferably, the penetration enhancer is present in an amount of no more than 15% of the total weight of the composition, even more preferably no more than 10%, even more preferably no more than 8%, and most preferably no more than 3%.

[0044] In some embodiments, the penetration enhancer is selected from ethanol, isosorbide dimethyl ether, or combinations thereof. Preferably, the penetration enhancer is a combination of isosorbide dimethyl ether and ethanol.

[0045] In some preferred embodiments, the penetration enhancer is isosorbide dimethyl ether.

[0046] In one embodiment, isosorbide dimethyl ether is present in an amount of 0.01 to 10% of the total weight of the composition, or in an alternative amount of 0.1 to 5% of the total weight of the composition, or 1 to 3% of the total weight of the composition, such as 2.5% of the total weight of the composition.

[0047] In some implementations, the penetration enhancer is ethanol.

[0048] Preferably, ethanol is present in an amount of 0.01% to 20% of the total weight of the composition, more preferably at least 0.1% of the weight of the composition, even more preferably at least 1%, even more preferably at least 2%, and most preferably at least 3%. Preferably, ethanol is present in an amount of no more than 15% of the weight of the composition, even more preferably no more than 10%, even more preferably no more than 8%, and most preferably no more than 7%.

[0049] The hair care compositions of the present invention are primarily intended for application to the hair and / or scalp of human subjects to improve hair properties.

[0050] Preferably, the hair care composition is selected from shampoo-free hair compositions, hair masks, leave-in hair care compositions, and pre-treatment hair care compositions, and most preferably from shampoo-free hair compositions, hair masks, and leave-in compositions. The pre-treatment composition is preferably a leave-in hair care composition. The hair care composition of the present invention can also be a "shampoo-free" composition applied to the hair and then partially rinsed off.

[0051] The wash-off compositions used in this invention are typically left on wet hair for 1 to 2 minutes before being washed off. Typically, about 1 g to about 50 g of the composition is applied to the hair or scalp.

[0052] The hair mask used in this invention is typically left on the hair for 3 to 10 minutes, preferably 3 to 5 minutes, more preferably 4 to 5 minutes, before rinsing it off.

[0053] The leave-in compositions used in this invention are typically applied to the hair and left on the hair for more than 10 minutes, and preferably applied to the hair after washing and not rinsed off until the next wash.

[0054] The hair care compositions of the present invention typically contain about 20% to about 95% by weight, preferably at least 30% by weight, more preferably at least 40% by weight, even more preferably at least 50% by weight, and even more preferably at least 60% by weight or even at least 70% by weight, but generally not exceeding 94% by weight, preferably not exceeding 93% by weight, more preferably not exceeding 92% by weight, even more preferably not exceeding 91% by weight, and even more preferably not exceeding 90% by weight or even not exceeding 80% by weight. Other organic solvents, such as lower alkyl alcohols and polyols, may also be present. Examples of lower alkyl alcohols include C1 to C6 monohydric alcohols, such as ethanol and isopropanol. Examples of polyols include propylene glycol, hexanediol, glycerol, and propanediol. Mixtures of any of the above-mentioned organic solvents may also be used.

[0055] The features disclosed in the foregoing specification or the appended claims may be used alone or in any combination of these features to implement the invention, when appropriate.

[0056] While the present invention has been described in conjunction with the foregoing exemplary embodiments, many equivalent modifications and variations will be apparent to those skilled in the art upon which this disclosure is given. Therefore, the exemplary embodiments of the invention set forth above are to be considered illustrative rather than restrictive. Various changes may be made to the described embodiments without departing from the spirit and scope of the invention.

[0057] To avoid any ambiguity, any theoretical explanations provided herein are for the purpose of enhancing the reader's understanding. The inventor does not wish to be bound by any of these theoretical explanations. Any section headings used herein are for organizational purposes only and should not be construed as limiting the subject matter described.

[0058] Throughout this specification, including the following claims, unless the context otherwise requires, the words “comprising” and “including”, as well as variations such as “containing,” “comprising,” and “including”, are to be understood as implying inclusion of the said integer or step or group of integers or steps, but not excluding any other integer or step or group of integers or steps.

[0059] It should be noted that, as used in the specification and appended claims, the singular forms “a,” “an,” and “the” include plural indicators unless the context clearly specifies otherwise. A range may be expressed herein as from “about” a particular value and / or to “about” another particular value. When expressing such a range, another embodiment includes from one particular value and / or to another particular value. Similarly, when a value is expressed as an approximation using the antecedent “about,” it should be understood that the particular value forms in another manner. The term “about” with respect to numerical values ​​is optional and means, for example, + / - 10%.

[0060] The invention will now be further described with reference to the following embodiments. Unless otherwise stated, all percentages are based on total weight by weight.

[0061] Example Example 1: Hair care shampoo Fill the container with deionized water. Separately disperse the carbomer and lysine carboxymethylcysteine ​​powders, then add them to the container, ensuring proper hydration. Heat the container to 60°C, then add the preservative, including pentylene glycol, until dissolved. Cool the container to room temperature. Once 35°C or lower is reached, add the remaining ingredients and mix. Then adjust the pH of the solution to 4.5–5.0 as needed using sodium hydroxide and / or citric acid solution.

[0062] Table 1

[0063] Example 2: Determination of melanin content Adult primary human epidermal melanocytes were cultured in melanocyte culture medium supplemented with melanocyte growth supplements and maintained at 37°C in a humid chamber with a 5% CO2 atmosphere. Cells were passaged in microtiter plates at a density of 35,000 cells / well. At 70% confluence (T0), cells were treated with various concentrations of lysine carboxymethyl cysteine ​​for 48 hours (T48). Untreated cells and cells treated with only 1 μM menadione were also cultured in parallel under the same conditions. Melanin content in the cell supernatant was measured at T48.

[0064] At T48, cell supernatant was collected and melanin content was determined. Melanin was assessed using a fluorescence-based melanin assay kit. This kit uses a substrate that produces a fluorescent product upon reaction with melanin. The fluorescence intensity is proportional to the amount of melanin in the sample.

[0065] Table 2

[0066] Example 3: Study on Cellular Metabolic Activity Adult primary human epidermal melanocytes were cultured in melanocyte culture medium supplemented with melanocyte growth supplements and maintained at 37°C in a humid chamber with a 5% CO2 atmosphere. Cells were passaged in microtiter plates at a density of 35,000 cells / well. After reaching 70% confluence (T0), cells were treated with various concentrations of lysine carboxymethyl cysteine ​​for 48 hours (T48). Untreated cells and cells treated with only 1 μM menadione were also cultured in parallel under the same conditions. Metabolic activity was measured at T0 and T48.

[0067] AlamarBlue™ Cell Viability Reagent is used to quantify cell viability, including cytotoxicity and cell proliferation. AlamarBlue™ dye is a redox indicator that produces colorimetric changes and fluorescent signals in response to metabolic activity, where damaged and / or non-viable cells have lower innate metabolic activity and produce a proportionally reduced signal. To quantify metabolic activity, 700 μL of culture medium + 10% alamarBlue reagent is added directly to the cells in each well and incubated at 37°C in a humidified chamber with a 5% CO2 atmosphere for 1 hour in the dark. Detection of the alamarBlue™ signal is performed using a TecanSpark® reader, with excitation at 544 nm and emission at 590 nm.

[0068] Table 3

[0069] Increased fluorescence indicates enhanced cellular metabolic activity.

[0070] The presented data show that the cysteine ​​precursor according to the present invention increases melanin production in cells and improves cellular metabolic activity. The results indicate that the compositions of the present invention containing the cysteine ​​precursor can increase melanin production in hair, thereby reducing age-related functional changes in hair pigmentation.

[0071] Example 4 - Determination of dichlorofluorescein diacetate (DCFDA) Adult primary human epidermal melanocytes were cultured in T75 flasks at 37°C in a humidified chamber with 5% CO2 in melanocyte culture medium supplemented with a mixture of melanocyte growth factors and antibiotics. Cells were then transferred in microtiter plates at approximately 5 × 10⁻⁶ cells / day. 4 Cells were further passaged at the desired density in a humidified chamber with 5% CO2 at 37°C for 24 hours. After 24 hours, cells were treated with the desired concentration of the test substance or a combination of test substances and 5 μM menadione, and further incubated for 6 hours as described above. Following incubation, ROS levels were assessed by incubating cells in DCFDA dye for 45 minutes. Cells were then washed, and fluorescence was measured at excitation 485 nm and emission 535 nm. Experiments were performed in duplicate (n=2) on three different donor cells (n=3). Data are expressed as % ROS levels compared to menadione.

[0072] Concentration of test substances in cell culture medium : Lysine carboxymethyl cysteine ​​(LCC) - 0.16% Statistical analysis For each test, the average of two replicates from three different experiments was used to show the percentage difference compared to the menadione-treated control. A t-test was used to assess statistical significance for comparisons between the menadione control and the corresponding treatment.

[0073] Table 4

[0074] Menadione induces oxidative stress in melanocytes by generating reactive oxygen species (ROS). The antioxidant effect of the test substance on melanocytes stressed with menadione was evaluated by comparing ROS levels in treated and untreated stressed cells. Compared to ROS levels in menadione-stressed cells, LCC was able to reduce ROS levels. This indicates that the inclusion of LCC in the formulation improves the antioxidant activity of melanocytes.

[0075] Example 5 - Catalase Activity Assay Adult primary human epidermal melanocytes were cultured in T75 flasks maintained at 37°C in a humidified chamber with 5% CO2 in melanocyte culture medium supplemented with a mixture of melanocyte growth factors and antibiotics. Cells were then transferred in microtiter plates at approximately 5 × 10⁻⁶ cells / mL. 4 Cells were further passaged at the desired density in a humidified chamber with 5% CO2 at 37°C for 24 hours. After 24 hours, cells were treated with the desired concentration of the test substance or a combination of test substances and 5 μM menadione, and further incubated for 6 hours as described above. Following incubation, catalase activity was assessed using a catalase colorimetric activity kit. Experiments were performed in duplicate (n=2) on three different donor cells (n=3). Data are expressed as % catalase activity compared to menadione.

[0076] Concentration of test substances in cell culture medium : Lysine carboxymethyl cysteine ​​(LCC) - 0.16% Statistical analysis For each test, the average of two replicates from three different experiments was used to show the percentage difference compared to the menadione-treated control. A t-test was used to assess statistical significance for comparisons between the menadione control and the corresponding treatment.

[0077] Table 5

[0078] Menadione induces oxidative stress in melanocytes by generating reactive oxygen species (ROS). The antioxidant effect of the test substance on melanocytes stressed with menadione was assessed by comparing catalase activity in treated and untreated stressed cells. Enhanced catalase activity indicates an increased ability of cells to reduce oxidative stress.

[0079] Compared with untreated stressed cells, cells treated with LCC showed a statistically significant increase in catalase activity.

Claims

1. Use of a carboxymethylcysteine ​​compound or a hair care composition containing a carboxymethylcysteine ​​compound for increasing melanin production in melanocytes and / or for enhancing cellular metabolic activity in melanocytes.

2. The use according to claim 1, wherein the use is for increasing melanin production.

3. The use according to claim 1, wherein the use is for improving cellular metabolic activity.

4. The use according to any of the preceding claims, wherein the carboxymethylcysteine ​​compound is selected from carboxymethylcysteine, salts of carboxymethylcysteine, esters of carboxymethylcysteine, amides of carboxymethylcysteine, or mixtures thereof, preferably the carboxymethylcysteine ​​compound comprises carboxymethylcysteine, esters of carboxymethylcysteine, and / or salts of carboxymethylcysteine, more preferably the carboxymethylcysteine ​​compound comprises carboxymethylcysteine ​​and / or salts of carboxymethylcysteine, even more preferably the carboxymethylcysteine ​​compound comprises salts of carboxymethylcysteine, even more preferably the carboxymethylcysteine ​​compound comprises lysine carboxymethylcysteine ​​salt, and most preferably the carboxymethylcysteine ​​compound is lysine carboxymethylcysteine ​​salt.

5. The use according to any of the preceding claims, wherein the carboxymethylcysteine ​​compound is a lysine carboxymethylcysteine ​​salt.

6. The use according to any of the preceding claims, wherein the carboxymethylcysteine ​​compound is present in an amount of 0.0001% to 5% of the total weight of the composition, more preferably at least 0.001% of the total weight of the composition, even more preferably at least 0.01% of the total weight of the composition, still even more preferably at least 0.1% of the total weight of the composition, and most preferably at least 0.2% of the total weight of the composition, preferably at no more than 3% of the total weight of the composition, even more preferably at no more than 2% of the total weight of the composition, still even more preferably at no more than 1.4% of the total weight of the composition, and most preferably at no more than 1% of the total weight of the composition.

7. The use according to any of the preceding claims is non-therapeutic.

8. A method for increasing melanin production in melanocytes and for enhancing cellular metabolic activity in melanocytes, the method comprising applying a hair care composition comprising a carboxymethylcysteine ​​compound to hair or scalp.

9. The method according to claim 8, wherein it is non-therapeutic.

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