DE102011109522A1 - Extracts of Tradescantia virginiana - Google Patents

Abstract

The present invention relates to an extract of plant parts of Tradescantia virginiana, a process for its preparation, and its use in cosmetic and dermatological preparations. The invention further relates to preparations containing an extract of plant parts of Tradescantia virginiana, and to a process for their preparation.

Description

The present invention relates to an extract of plant parts of Tradescantia virginiana, a process for its preparation, and its use in cosmetic and dermatological preparations. The invention further relates to preparations containing an extract of plant parts of Tradescantia virginiana, and to a process for their preparation.

Skin and hair color are dependent on the content, size, distribution and type of the nitrogen-containing, dark dye melanin, which is produced in the melanocyte-capable cells (melanocytes). Starting from tyrosine and using various melanocyte-specific enzymes, such as. As tyrosinase or tyrosinase-related proteins, melanin is synthesized within the melanocytes. Subsequently, the melanin is transferred to the keratinocytes in the form of so-called melanosomes.

Although the melanin in the skin is a suitable protection against UV radiation, darker or over-pigmented skin can affect the beauty and lead to serious aesthetic problems. Hyperpigmented areas of the skin or lesions contain melasma (also called chloasma), d. H. irregularly shaped yellowish-brown spots.

In general, a distinction is made in pigment spots between freckles (ephelides), age spots (lentigines), so-called age warts (verrucae seborrhoicea) and hyperpigmentation (eg, chloasma or melasma). Freckles in particular are prone to skin type I, d. H. with very light skin and reddish hair. Hyperpigmentation (chloasma), on the other hand, is common in those women who routinely deliver estrogen to their bodies. Very often the sun plays an important role. You can prevent it especially by regular sunscreen with a high SPF. In order to remove unsightly pigment spots, various options are available, such as laser, dermabrasion or other electrosurgical methods, as well as so-called bleaching creams. The latter alternative has the advantage that it is much cheaper for the patient than the electrosurgical procedures. In addition, the application is easier and more enjoyable.

A large number of skin-whitening compounds for the treatment of pigmentation marks are available on the market. Among others, these are compounds such. As hydroquinone (1,4-dihydroxybenzene), kojic acid, arbutin, aloesin, niacinamide, vitamin C or rucinol, which prevent the production of melanin in the skin. Also plant extracts such. B. from Morus alba or Phyllanthus emblica, especially in the Southeast Asian region, application to brighten the Hautteint.

This can be done using different mechanisms. However, most of the skin lightening agents delay the conversion of tyrosine into melanin by blocking the enzyme tyrosinase. However, these known compounds have a number of disadvantages, such. B. low depigmentation efficiency, side effects such as skin irritation or skin exfoliation (skin peeling), cell damage, low skin penetration or low durability or stability of the formulations. Therefore, there is a need for new safeners with higher efficiency and good formulation properties.

In addition, the trend away from the noble paleness towards "healthy, sporty tanned skin" has been unbroken for years. To achieve a tanned complexion, people expose their skin to solar radiation because it causes pigmentation through melanin formation. However, the UV radiation of sunlight also has a damaging effect on the skin. In addition to the acute injury (sunburn), long-term damage from excessive exposure to light from the UVB range (wavelength 280-320 nm), such as an increased risk of developing skin cancer. Excessive exposure to UVB and UVA radiation (wavelength: 320-400 nm) produces highly reactive radical species that continue to multiply upon completion of irradiation, resulting in wrinkling and skin aging.

Natural protection against the negative effects of solar radiation is provided by the tanning (pigmentation) of the skin. The epidermis contains in its lowest layer, the basal layer, in addition to the basal cells, individual pigment-forming cells, the melanocytes. UV light in these cells stimulates the production of melanin, which is transported to the keratinocytes (horny cells) where it becomes visible as a brown skin color. Melanin protects the cell nuclei from further irradiation and the resulting negative effects on the cell DNA.

Depending on the chemical composition of the biochemically formed pigments, a distinction is made between the brownish-black eumelanin and the reddish-yellow pheomelanin. The observed skin tone is determined by the ratio of these two types of melanin. This pigment formation originating from the amino acid tyrosine is predominantly initiated by UVB radiation and referred to as "indirect pigmentation". Their development runs over several days; the sun tan will last for several weeks. In the case of "direct pigmentation", which starts with sunlight, predominantly colorless melanin precursors are oxidized by UVA radiation to dark-colored melanin. Since this oxidation is reversible, it leads to a short-lasting tanning of the skin.

An artificial tanning of the skin can be produced externally with the help of make-up and orally by taking carotenoids.

Far more popular, however, is the artificial tanning of the skin, which can be achieved by applying so-called self-tanner. Many of these compounds have as a chemical structural feature keto or aldehyde groups in the vicinity of alcohol functions and belong predominantly to the substance class of sugars. Particularly frequently used self-tanning substances are 1,3-dihydroxyacetone (DHA), used in an amount of 700 t / a, and erythrulose.

Classic self-tanning agents can be reacted with the proteins and amino acids of the horny layer of the skin in the sense of a Maillard reaction or via a Michael addition, whereby polymers which give the skin a brownish hue emerge via a not yet fully elucidated reaction pathway. This reaction is completed in about 4 to 6 hours. The tan thus obtained is not washable and is removed only with the normal Hautabschuppung.

However, these color products themselves have no UV-absorbing properties, so that in sun exposure, an additional sunscreen (clothing, hat, UV filter) is required. In contrast to "tanned" skin, the tanned skin is not protected against sunburn.

There is therefore a need for dermatologically acceptable skin-dyeing substances which are suitable for use in cosmetic and / or dermatological preparations or medical products and which enhance the natural tanning of the skin by increasing melanin synthesis and at the same time improve skin protection or sun protection, in particular against UVB. Radiation, enable.

It is an object of the present invention to provide novel agents that affect the appearance and hue of the skin by acting as a self-tanning or skin whitening agent.

Surprisingly, it has now been found that extracts of plant parts of Tradescantia virginiana, depending on the selected extraction conditions, both have a high skin lightening effect and can act as a self-tanning agent.

For the purposes of the invention, the term self-tanning active is used synonymously with self-tanning substance, self-tanner or self-tanning substance.

Tradescantia virginiana is a herbaceous plant that is planted in gardens for ornamental purposes. It is also used in bioassays to test the presence of ionizing radiation, which causes its stamens to turn red.

For the purposes of the present invention, plant hybrids of Tradescantia virginiana are also included, i. H. Plants derived from a cross of Tradescantia virginiana with another species or subspecies of the genus Tradescantia.

The use of extracts of Tradescantia virginiana in cosmetic or dermatological preparations is not known in the prior art; for topical applications, only the use of the species Tradescantia spathacea is described:
JP 2009040753 describes skin repair compositions containing plant extracts of Tradescantia spathacea.

In EP 1009378 discloses the use of plant extracts of Rhoeo discolor (= Tradescantia spathacea) in cosmetic and pharmaceutical preparations.

DE 10 2007 042 009 A1 describes pharmaceutical formulations which can, inter alia, also be used for the treatment of skin diseases and contain an extract of Tradescantia spathacea.

A first subject of the present invention is therefore an extract of plant parts of Tradescantia virginiana.

In principle, all above-ground parts of the plant can be used for the extract. Plant parts preferably used for extraction are the leaves or flowers or mixtures thereof, more preferably the leaves are used.

The plant extract of Tradescantia virginiana can be prepared by methods known to those skilled in the art. A plant extract which is particularly suitable for the use according to the invention is obtainable by a) extraction of the plant parts of Tradescantia virginiana with the aid of a solvent and, optionally, b) removal of the solvent.

Accordingly, a process for producing an extract from plant parts of Tradescantia virginiana is also the subject of the invention, comprising the steps of a) extraction of the plant parts of Tradescantia virginiana with the aid of a solvent and, optionally, b) removal of the solvent.

The plant parts can be used directly for the extraction according to step a). Typically, however, the plant parts are first dried and crushed.

The drying can be carried out, for example, in air or preferably in a drying oven at elevated temperature, preferably between 30 and 50 ° C., more preferably at about 40 ° C. In addition, the drying can also be carried out under reduced pressure.

The crushing can be done by a common method, for example by using cutting tools such as knives or scissors, or by using a blender. For larger quantities, mills such. B. hammer mills are used.

Subsequently, the plant parts are extracted. The extraction is carried out by methods known to those skilled in the art. For this, the plant parts are mixed with a solvent.

Preference is given to using a solvent selected from water, organic solvents or mixtures thereof. Examples of organic solvents are methanol, ethanol, 1-propanol, 2-propanol, acetonitrile, acetone or ethyl acetate.

Solvent mixtures of water and organic solvents preferably contain 10-90% by volume of water, more preferably 30-70% by volume of water.

In a preferred embodiment of the present invention, the solvent is selected from water or alcohol. In a particularly preferred embodiment, an alcohol, in particular ethanol, is used as solvent. In a further preferred embodiment, water is used as the solvent.

The extraction is typically carried out at temperatures between 20 and 90 ° C, preferably between 50 and 90 ° C, more preferably at the boiling point of the solvent or solvent mixture. This means that when using water as the solvent, the extraction is particularly preferably carried out at about 100 ° C, while the extraction is particularly preferably carried out at about 78 ° C when using ethanol as a solvent.

In optional step b), the solvent is removed. This is typically done by filtration.

The method preferably comprises step b).

The resulting extract may optionally be further purified. Conventional methods can be used for this purpose, for example chromatographic methods such as solid phase adsorption with subsequent stepwise desorption by means of suitable solvents. The chromatography can also be carried out in countercurrent. Concentration and enrichment can also be achieved by means of supercritical gases or ionic liquids. It is also possible to achieve a depletion of unwanted constituents by liquid / liquid extraction. For this purpose, the dry extract obtained is usually taken up in a little water and extracted with a further solvent, such as heptane. If it is a water extract, it can also be purified directly as a concentrated crude extract (without further addition of water) with another solvent in a liquid / liquid extraction. Even by changing the solvent with subsequent filtration unwanted components can be removed.

Optionally, the extract obtained can then be concentrated and / or dried in a step c).

This can be done using methods common to the person skilled in the art. The concentration is carried out using, for example, a rotary evaporator or a falling film evaporator, and may also be carried out under reduced pressure. The extract can be dried, for example, by means of spray drying or freeze drying. The extract is preferably dried completely to constant weight.

Another object of the present invention is the use of an extract from plant parts of Tradescantia virginiana, as described above, in cosmetic or dermatological preparations.

In a preferred embodiment, the use is for lightening the skin.

According to the invention, the extracts of parts of Tradescantia virginiana with good compatibility at the same time valuable cosmetic and / or pharmacological properties by the lightening of the skin associated with a relative melanin content of less than 90%, preferably less than 80%, more preferably less than 70%.

A particularly preferred embodiment of the present invention is the use of an extract from plant parts of Tradescantia virginiana for the inhibition of melanin synthesis, for the prophylaxis, treatment and / or follow-up of pigmentary disorders of the skin.

Inhibition of melanin synthesis can be achieved, for example, by regulation of the transcription or activity of tyrosinase (e.g., inhibition or degradation of tyrosinase), TRP-1 (tyrosinase related protein-1), TRP-2 (tyrosinase related protein-2) and / or Peroxidase take place. This is also possible in vitro. The term "inhibition" refers to any reduction in activity that is based on the action of the specific extract of the invention and is made possible by recognition, binding and blocking of the target molecules.

The aforementioned use of the extract can be done in in vitro or in vivo models. The susceptibility of a particular cell to treatment with the extract can be determined by testing in vitro. Typically, a culture of the cell is incubated with the extract of the invention at various concentrations for a time sufficient to allow the active agents to inhibit the synthesis of melanin, usually between about one hour and one week. Cultured cells from a biopsy sample can be used for testing in vitro. The amount of post-treatment melanin in the cells is then determined. The use in vitro is particularly on samples of singer species that suffer from pigmentation of the skin. The host or patient may be of any mammalian species, e.g. As a primate species, especially humans, but also rodents (including mice, rats and hamsters), rabbits, horses, cattle, dogs, cats, etc.

The in vivo dose of the extract is advantageously matched to the susceptibility of the tyrosinase and / or severity of the patient's pigmentation disorder with respect to the in vitro data, thereby significantly increasing efficacy. Typically, a cosmetic dose will be sufficient to significantly reduce the undesirable amount of melanin in the target tissue while maintaining and ultimately improving the patient's quality of life.

Use will generally continue until there is a significant reduction in tyrosinase activity and / or melanin production, e.g. B. at least about 10% reduction in melanin content and can be continued until essentially no unwanted overproduction of melanin is detected. It is understood that a skin lightening is a repeated or ongoing treatment, since after discontinuation of the preparations, the normal melanin synthesis rate is resumed.

In accordance with the invention, extracts of plant parts of Tradescantia virginiana are also suitable for use in the prophylaxis, treatment and / or follow-up of pigment disorders selected, for example, from the group of hyperpigmentation, freckles, age spots and sunspots.

It is believed that the high skin lightening activity of the extracts of the present invention, without being bound by theory, is due to a combination of various active components in the extracts. In addition to the abovementioned possibilities for inhibiting melanin synthesis (for example by regulating the transcription or activity of tyrosinase, TRP-1, TRP-2 and / or peroxidase), skin whitening can generally also be regulated by regulating the uptake and distribution of Melanosomes in the recipient keratinocytes, the breakdown of melanin or melanosomes or the detachment of pigmented keratinocytes happen.

The skin-lightening effect of the extract is particularly good when it is prepared by the method described above and in particular according to its preferred embodiments.

Water skin extracts from plant parts of Tradescantia virginiana are particularly suitable for skin lightening, ie extracts in the preparation of which in step a) of the process according to the invention, as described above, water is used as solvent.

In a further preferred embodiment, the use of the extract according to the invention takes place as a self-tanning agent.

Extracts from plant parts of Tradescantia virginiana can therefore also have very good browning properties.

According to the invention, these are preferably used for increasing melanin synthesis, improving melanin transport and / or improving the distribution of melanin in suprabasal layers.

The extracts of the invention increase melanin synthesis and improve melanin transport from the melanocytes to the keratinocytes. This affects the color of the skin and causes a tanning effect.

Again, it is believed that the high tanning activity of the extracts of the invention, without being bound by theory, is due to a combination of different active components in the extracts.

The tanning effect of the extract is particularly good when it is prepared by the method described above and in particular according to its preferred embodiments.

Alcoholic extracts from plant parts of Tradescantia virginiana are particularly suitable as self-tanning agents, ie extracts in the preparation of which in step a) of the process according to the invention, as described above, an alcohol is used as solvent.

This is particularly preferably ethanol.

The use of extracts of plant parts of Tradescantia virginiana for skin lightening, as well as for self-tanning has the advantage that even at very low concentration, a strong effect can be achieved. They advantageously show a high and long-lasting activity with regard to their action as skin-whitening or skin-tanning active ingredients.

In addition, the extracts are also characterized by high application safety and good formulatability. So they are easy to incorporate into preparations and have increased stability in the preparations. The preparation of the extracts is very environmentally friendly, since only small amounts of solvent must be used and no other chemicals are necessary.

The use of the extracts from plant parts of Tradescantia virginiana can therefore be cosmetic or pharmaceutical, in particular dermatological, nature. It is preferably a cosmetic use, more preferably a non-therapeutic cosmetic use.

Another object of the present invention is a preparation containing an extract of plant parts of Tradescantia virginiana as described above.

The preparations are usually topically applicable preparations, for example cosmetic or pharmaceutical (dermatological) formulations or medical products. The preparations in this case contain a cosmetically or dermatologically suitable carrier and, depending on the desired property profile, optionally further suitable ingredients. In the case of pharmaceutical preparations, the preparations in this case contain a pharmaceutically acceptable carrier and optionally further pharmaceutical active ingredients.

It is preferably a cosmetic or pharmaceutical preparation; most preferably it is a cosmetic preparation.

For the purposes of the present invention, the term "preparation" is synonymous with the term "agent", "composition" or "formulation" used.

Topically applicable means according to the invention that the preparation is applied externally and locally, d. H. that the preparation must be suitable, for example, to be applied to the skin can.

The preparations may comprise or contain, consist essentially of or consist of said necessary or optional ingredients. Any compounds or components which may be used in the compositions are either known and commercially available or may be synthesized by known methods.

The preparations according to the invention preferably contain from 0.01 to 99% by weight of the extract of plant parts of Tradescantia virginiana, based on the total weight of the preparation. Preferably, an amount of 0.05 to 30 wt .-% is used, more preferably from 0.1 to 10 wt .-%. The expert does not have any difficulties in selecting the quantities according to the intended effect of the preparation.

The preparations according to the invention may contain further ingredients.

Preferred preparations according to the invention may contain at least one self-tanning substance as further ingredient. This can be either a self-tanner, which reacts with the amino acids of the skin in the sense of a Maillard reaction or via a Michael addition, as well as a so-called melanogenesis promoter or propigmentation, which calls for the natural tanning of the skin. Advantageous self-tanning substances which can be used include: 1,3-dihydroxyacetone, glycerolaldehyde, hydroxymethylglyoxal, γ-dialdehyde, erythrulose, 6-aldo-D-fructose, ninhydrin, 5-hydroxy-1,4-naphthoquinone (juglone) or Hydraxy-1,4-naphthoquinone (Lawson). Very particular preference is given to 1,3-dihydroxyacetone, erythrulose or their combination. In principle, propigmentation substances can be all active ingredients known to the person skilled in the art. Examples of these are glycyrrhetinic acid, melanocyte stimulating hormone (alpha-MSH), peptide analogs, thymidine dinucleotides, L-tyrosine and its esters or bicyclic monoterprenediols (described in US Pat Brown et al., Photochemistry and Photobiology B: Biology 63 (2001) 148-161 ).

Preferably, the at least one self-tanning substance in the preparation in an amount of 0.01 to 20 wt .-%, particularly preferably in an amount of 0.5 to 15 wt .-% and most preferably in an amount of 1 to 8 wt .-%, based on the total amount of the preparation.

Preparations with self-tanning properties, especially those containing dihydroxyacetone, when used on the human skin, tend to produce off-odors presumably caused by degradation products of the dihydroxyacetone itself or by products of side reactions which are sometimes found to be unpleasant to users. It has been found that these off-odors are avoided when using formaldehyde scavengers and / or flavonoids. Therefore, the preparation according to the invention may also contain formaldehyde scavengers and optionally flavonoids for improving the odor.

• – Verlängerung der Bräunungs-Reaktion aufgrund der indirekten Bräunungs-Reaktion (UV-freie Bräunungsverlängerung),
• – Verstärkung der Bräunungs-Reaktion,
• – Vermeidung von ungleichmäßiger Bräunung durch ungeschicktes Auftragen,
• – die erzielte Bräunung kommt der natürlichen Bräunung nahe,
• – Verbesserung des Schutzes vor UV-Strahlung.

If the extract according to the invention already has a skin-tanning effect on its own (for example, if it is an alcoholic extract), the preparation according to the invention which has a skin tanning effect Self-tanning substance and the extract of plant parts of Tradescantia virginiana combined, compared to a self-tanning product without the addition of the extract according to the invention the following advantages:

• - Extension of the tanning reaction due to the indirect tanning reaction (UV-free tanning extension),
• - strengthening of the tanning reaction,
• - avoidance of uneven browning due to clumsy application,
• - the tanning achieved is close to the natural tanning,
• - Improved protection against UV radiation.

If the extract according to the invention itself has a skin-lightening effect (for example a water extract), a corresponding preparation which combines the extract and a self-tanning substance generally has a contrast-reducing effect and makes it possible to achieve an even skin tone. Accordingly, the extracts of plant parts of Tradescantia virginiana can also be used according to the invention in combination with self-tanning substances for the purpose of reducing the contrast and achieving an even skin tone. A contrast reducing agent is a substance that reduces uneven skin coloration by reducing the contrast between stronger and less-colored areas of the skin. In this case, such an uneven skin coloration can be caused by an uneven pigmentation and / or a different distribution of the cornea. Uneven pigmentation is by no means uncommon in the population and is due to a different degree of melanin production of the melanocytes or an irregular distribution of the melanocytes in the skin. The combination of tanning mixtures based on the Maillard reaction or Michael addition with melanogenesis inhibiting substances causes already hyperpigmented areas of skin to lose their high melanin concentrations and the hue produced by the coloring agent on the skin surface to spread over a large area.

A contrast reduction can be achieved in particular by preparations in which an extract of parts of Tradescantia virginiana with a self-tanning substance, preferably containing dihydroxyacetone (DHA) and derivatives derived therefrom, DHA rapid, DHA plus or erythrulose, or a mixture of self-tanning substances, preferably DHA, DHA rapid, containing DHA plus and / or erythrulose is combined. Advantageous self-tanning agents in a mixture or preparation containing dihydroxyacetone may be, inter alia, glycerolaldehyde, hydroxymethylglyoxal, γ-dialdehyde, 6-aldo-D-fructose, ninhydrin, 5-hydroxy-1,4-naphthoquinone (juglone) or 2-hydroxy -1,4-naphthoquinone (Lawson) or a mixture of said compounds. Erythrulose is particularly preferably used in the mixture containing dihydroxyacetone. Very particular preference is given to using dihydroxyacetone or a derivative derived therefrom without further self-tanning substances.

In addition to the extract of Tradescantia virginiana, the preparations according to the invention may also contain at least one active substance or extract with a skin-lightening activity. If the extract according to the invention itself has a skin-lightening effect, the addition of a further skin-lightening active substance can enhance the skin-lightening effect.

Skin-lightening active ingredients (or synonymously depigmenting agents) which can be used in the preparations according to the invention can, in principle, be all active ingredients known to the person skilled in the art. For combination are commercially available melanogenesis inhibitors such. As ascorbic acid and its derivatives, aloesin, niacinamide, emblica, elagic acid, licorice extract, mulberry extract, kojic acid, licorice root extract, rucinol, hydroquinone and its derivatives, azelaic acid, arbutin, magnesium ascorbyl phosphate, pantothenic acid and its derivatives or salts, glucosamine and its Derivatives, mercaptoamines, hinokitol, tocopherols, ubiquinones, glabridin, 4-hydroxyanisole, 4-tert-butylphenol, resveratrol, 4-S-cystaminylphenol, glutathione, lactic acid or the like. Preferred examples of compounds having skin-lightening activity are hydroquinone, niacinamide, ascorbic acid and physiologically acceptable salts thereof, kojic acid, arbutin, aloesin, azelaic acid, elagic acid or rucinol. Preferred examples of extracts with skin-lightening activity are licorice extract, mulberry extract or emblica.

The preparations according to the invention may also contain at least one UV filter in addition to the extracts according to the invention.

Organic UV filters, so-called hydrophilic or lipophilic sunscreen filters, are effective in the UVA range and / or UVB range and / or IR and / or VIS range (absorber). These substances can be found in particular among cinnamic acid derivatives, salicylic acid derivatives, camphor derivatives, triazine derivatives, β, β-diphenylacrylate derivatives, p-aminobenzoic acid derivatives and polymeric filters and silicone filters which are described in US Pat registration WO-93/04665 be selected. Further examples of organic filters are in the patent application EP-A 0 487 404 specified. In the following, the named UV filters are usually named according to the INCI nomenclature.

In particular suitable for a combination are:

para-aminobenzoic acid and its derivatives: PABA, ethyl PABA, ethyl dihydroxypropyl PABA, ethylhexyl dimethyl PABA, e.g. B. sold under the name "Escalol 507" from the company. ISP, glyceryl PABA, PEG-25 PABA, z. B. sold under the name "Uvinul P25" from the company. BASF.

Salicylates: Homosalates are sold under the name "Eusolex HMS" by Merck; Ethyl hexyl salicylates, e.g. B. sold under the name "Neo Heliopan OS" from the Fa. Symrise, Dipropylene glycol salicylate, z. B. sold under the name "Dipsal" from the company. Scher, TEA salicylates, z. B. marketed under the name "Neo Heliopan TS" of the Fa. Symrise.

β, β-diphenylacrylate derivatives: octocrylenes, e.g. Sold under the name "Eusolex ^® OCR" from Merck "," Uvinul N539 "from BASF, Etocrylene, z. B. sold under the name "Uvinul N35" from BASF.

Benzophenone Derivatives: Benzophenone-1, e.g. Sold under the name "Uvinul 400"; Benzophenone-2, e.g. Sold under the name "Uvinul D50"; Benzophenone-3 or oxybenzone, e.g. Sold under the name "Uvinul M40"; Benzophenone-4, e.g. Sold under the name "Uvinul MS40"; Benzophenone-9, e.g. B. marketed under the name "Uvinul DS-49" from the company. BASF, Benzophenone-5, Benzophenone-6, z. B. marketed under the name "Helisorb 11" by the company Norquay, Benzophenone-8, z. Sold under the name "Spectra-Sorb UV-24" by American Cyanamid, Benzophenone-12 n-hexyl 2- (4-diethylamino-2-hydroxybenzoyl) benzoate or 2-hydroxy-4-methoxybenzophenone, marketed by Fa. Merck, Darmstadt under the name Eusolex ^® 4360th

Benzylidene camphor derivatives: 3-benzylidenecamphor, e.g. Sold under the name "Mexoryl SD" from the company. Chimex, 4-Methylbenzylidenecamphor, z. B. sold under the name "Eusolex 6300" from the company Merck, Benzylidenecamphorsulfonsäure, z. B. sold under the name "Mexoryl SL" from the company. Chimex, Camphor benzalkonium methosulfate, z. Sold under the name "Mexoryl SO" from the company. Chimex, Terephthalylidenedicamphorsulfonsäure, z. Sold under the name "Mexoryl SX" from the company Chimex, Polyacrylamidomethylbenzylidenecamphor sold under the name "Mexoryl SW" from the company Chimex.

Phenylbenzimidazole derivatives: phenylbenzimidazolesulfonic acid, e.g. B. sold under the name "Eusolex 232" from the company. Merck, disodium phenyl dibenzimidazole tetrasulfonate, z. B. marketed under the name "Neo Heliopan AP" by Fa. Symrise.

Phenylbenzotriazole derivatives: Drometrizole trisiloxanes, e.g. B. marketed under the name "Silatrizole" by the company. Rhodia Chimie, Methylenebis (benzotriazolyl) tetramethylbutylphenol in solid form, for. B. marketed under the name "MIXXIM BB / 100" from the company. Fairmount Chemical, or in micronized form as an aqueous dispersion, eg. B. marketed under the name "Tinosorb M" from BASF.

Triazine derivatives: ethylhexyltriazone, e.g. B. sold under the name "Uvinul T150" from the company. BASF, Diethylhexylbutamidotriazone, z. Sold under the name "Uvasorb HEB" from the company Sigma 3V, 2,4,6-tris (diisobutyl 4'-aminobenzalmalonate) -s-triazines or 2,4,6-tris (biphenyl) -1, 3,5-triazines sold as Tinosorb A2B by BASF, 2,2 '- [6- (4-methoxyphenyl) -1,3,5-triazine-2,4-diyl] bis [5- (2-ethylhexyl) oxy ] -phenol, sold as Tinosorb S by BASF, N2, N4-bis [4- [5- (1,1-dimethylpropyl) -2-benzoxazolyl] phenyl] -N6- (2-ethylhexyl) -1,3,5 -triazine-2,4,6-triamine sold as Uvasorb K 2A from Sigma 3V.

Anthraniline derivatives: menthyl anthranilate, e.g. B. marketed under the name "Neo Heliopan MA" by Fa. Symrise.

Imidazole derivatives: Ethylhexyldimethoxybenzylidenedioxoimidazoline propionate.

Benzalmalonate derivatives: Polyorganosiloxanes containing functional benzalmalonate groups, such as. B. polysilicone-15, z. Sold under the name "Parsol SLX" by Hoffmann LaRoche.

4,4-Diarylbutadiene derivatives: 1,1-dicarboxy (2,2'-dimethylpropyl) -4,4-diphenylbutadiene.

Benzoxazole Derivatives: 2,4-bis [5- (1-dimethylpropyl) benzoxazol-2-yl (4-phenyl) imino] -6- (2-ethylhexyl) imino-1,3,5-triazines, e.g. B. sold under the name Uvasorb K2A from the company. Sigma 3V and mixtures containing this.

oder die UV-Filter der folgenden Strukturen

oder

Piperazine derivatives such as the compound

or the UV filters of the following structures

or

It is also possible to use UV filters based on polysiloxane copolymers with a random distribution in accordance with the following formula, where z. B. a = 1, 2; b = 58 and c = 2.8 are:

The compounds listed in the list are examples only. Of course, other UV filters can be used.

Suitable organic UV-protective substances are preferably selected from the following list: ethylhexyl salicylate, phenylbenzimidazolesulfonic acid, benzophenone-3, benzophenone-4, benzophenone-5, n-hexyl 2- (4-diethylamino-2-hydroxybenzoyl) benzoate, 4- Methylbenzylidenecamphor, terephthalylidenedicamphorsulfonic acid, disodium phenyldibenzimidazoletetrasulfonate, methylenebis (benzotriazolyl) tetramethylbutylphenol, ethylhexyl triazone, diethylhexyl butamido triazone, drometrizole trisiloxane, polysilicone-15, 1,1-dicarboxy (2,2'-dimethylpropyl) -4,4-diphenylbutadiene, 2,4- Bis [5-1 (dimethylpropyl) benzoxazol-2-yl (4-phenyl) imino] -6- (2-ethylhexyl) imino-1,3,5-triazines and mixtures thereof.

These organic UV filters are usually incorporated in formulations in an amount of from 0.01% to 20% by weight, preferably from 1% to 10% by weight.

The preparations may contain, in addition to the extracts according to the invention and the optionally organic UV filters, as described above, further inorganic UV filters, so-called particulate UV filters.

These combinations with particulate UV filters are possible both as a powder and as a dispersion or paste of the following types.

In this case, both those from the group of titanium dioxides such. For example, coated titanium dioxide (for. Example Eusolex ^® T-2000, Eusolex ^® T-AQUA, Eusolex ^® T-AVO, Eusolex ^® T-OLEO), zinc oxides (eg. As Sachtotec® ^®), iron oxides and also cerium and / or zirconium oxides are preferred.

Furthermore, combinations with pigmentary titanium dioxide or zinc oxide are possible, wherein the particle size of these pigments is greater than or equal to 200 nm, for example ^® Hombitan FG or Hombitan ^® FF-Pharma.

Furthermore, it may be preferred if the preparations contain inorganic UV filters which are prepared by conventional methods, as for example in Cosmetics & Toiletries, February 1990, Vol. 105, pp. 53 64 described, were treated. Here, one or more of the following aftertreatment components may be selected: amino acids, beeswax, fatty acids, fatty acid alcohols, anionic surfactants, lecithin, phospholipids, sodium, potassium, zinc, iron or aluminum salts of fatty acids, polyethylenes, silicones, proteins (especially Collagen or elastin), alkanolamines, silica, alumina, other metal oxides, phosphates, such as sodium hexametaphosphate or glycerol.

• – unbehandelte Titandioxide wie z. B. die Produkte Microtitanium Dioxide MT 500 B der Fa. Tayca; Titandioxd P25 der Fa. Degussa,
• – Nachbehandelte mikronisierte Titandioxide mit Aluminiumoxid und Siliciumdioxid Nachbahandlung wie z. B. das Produkt „Microtitanium Dioxide MT 100 SA der Tayca; oder das Produkt „Tioveil Fin” der Fe. Uniqema,
• – Nachbehandelte mikronisierte Titandioxide mit Aluminiumoxid und/oder Aluminiumstearate/laurate Nachbehandlung wie z. B. Microtitanium Dioxide MT 100 T der Fa. Tayca, Eusolex T-2000 der Firma Merck,
• – Nachbehandelte mikronisierte Titandioxide mit Eisenoxid und/oder Eisenstearate Nachbehandlung wie z. B. des Produkt „Microtitanium Dioxide MT 100 F” der Fa. Tayca,
• – Nachbehandelte mikronisierte Titandioxide mit Siliciumdioxide, Aluminiumoxid und Silicon Nachbehandlung wie z. B. das Produkt ”Microtitanium Dioxide MT 100 SAS”, der Fa. Tayca,
• – Nachbehandelte mikronisierte Titandioxide mit Natrumhexameta-phosphate, wie z. B. das Produkt ”Microtitanium Dioxide MT 150 W” der Fa. Tayca.

Preferably used particulate UV filters are:

• - untreated titanium dioxides such. The products Microtitanium Dioxide MT 500 B from Tayca; Titanium Dioxide P25 from Degussa,
• - Aftertreated micronized titanium dioxides with alumina and silica Nachbahandlung such. For example, the product "Microtitanium Dioxide MT 100 SA from Tayca; or the product "Tioveil Fin" of Fe. Uniqema,
• - Aftertreated micronized titanium dioxides with alumina and / or aluminum stearates / laurate aftertreatment such. B. Microtitanium Dioxide MT 100 T from. Tayca, Eusolex T-2000 from Merck,
• - Aftertreated micronized titanium dioxides with iron oxide and / or iron stearates aftertreatment such. B. the product "Microtitanium Dioxide MT 100 F" Fa. Tayca,
• - Aftertreated micronized titanium dioxides with silicas, alumina and silicon aftertreatment such. B. the product "Microtitanium Dioxide MT 100 SAS", the company Tayca,
• - Aftertreated micronized titanium dioxides with Natrumhexameta-phosphate, such as. As the product "Microtitanium Dioxide MT 150 W" Fa. Tayca.

• – Octyltrimethoxysilane; wie z. B. das Produkt Tego Sun T 805 der Fe. Degussa,
• – Siliciumdioxid; wie z. B. das Produkt Parsol T-X der Fa. DSM,
• – Aluminiumoxid und Stearinsäure; wie z. B. das Produkt UV-Titan M160 der Fa. Sachtleben,
• – Aluminium und Glycerin; wie z. B. das Produkt UV-Titan der Fa. Sachtleben
• – Aluminium und Silikonölen, wie z. B. das Produkt UV-Titan M262 der Fa. Sachtleben,
• – Natriumhexamethaphosphat und Polyvinylpyrrolidon,
• – Polydimethylsiloxane, wie z. B. das Produkt 70250 Cardre UF TiO2Sl3” der Fa. Cardre,
• – Polydimethylhydrogensiloxane, wie z. B. das Produkt Microtitanium Dioxide USP Grade Hydrophobic” der Fa. Color Techniques.

The treated micronized titanium dioxides used for combination may also be post-treated with:

• - octyltrimethoxysilanes; such as B. the product Tego Sun T 805 of Fe. Degussa,
• - silica; such as B. the product Parsol TX from DSM,
• Alumina and stearic acid; such as B. the product UV titanium M160 Fa. Sachtleben,
• - aluminum and glycerin; such as B. the product UV titanium from Fa. Sachtleben
• - Aluminum and silicone oils, such as. B. the product UV titanium M262 Fa. Sachtleben,
• Sodium hexamethaphosphate and polyvinylpyrrolidone,
• - Polydimethylsiloxane, such as. Example, the product 70250 Cardre UF TiO2Sl3 "the Fa. Cardre,
• - Polydimethylhydrogensiloxane, such as. Example, the product Microtitanium Dioxide USP Grade Hydrophobic "from the company Color Techniques.

• – Unbehandelte Zinkoxide wie z. B. das Produkt Z-Cote der Fa. BASF (Sunsmart), Nanox der Fa. Elementis
• – Nachbehandelte Zinkoxide wie z. B die folgenden Produkte: • ”Zinc Oxide CS-5” der Fa. Toshibi (ZnO nachbehandelt mit polymethylhydrogenosiloxane) • Nanogard Zinc Oxide FN der Fa. Nanophase Technologies • ”SPD-Z1” der Fa Shin-Etsu (ZnO nachbehandelt mit einem Silikongepfropften Acrylpolymer, dispergiert in Cyclodimethylsiloxane • ”Escalol Z100” der Fa ISP (Aluminiumoxid nachbehandeltes ZnO dispergiert in einer ethylhexyl methoxycinnamate/PVP-hexadecene/methicone copolymer Mischung) • ”Fuji ZNO-SMS-10” der Fa. Fuji Pigment (ZnO nachbehandelt mit Siliciumdioxid und Polymethylsilesquioxan); • Unbehandeltes Ceroxide Mikropigment z. B. mit der Bezeichnung ”Colloidal Cerium Oxide” der Fa Rhone Poulenc • Unbehandelte und/oder nachbehandelte Eisenoxide mit der Bezeichnung Nanogar der Fa. Arnaud.

Furthermore, the combination with the following products may also be advantageous:

• - Untreated zinc oxides such. For example, the product Z-Cote from BASF (Sunsmart), Nanox from the company Elementis
• - After-treated zinc oxides such. B the following products: • "Zinc Oxide CS-5" from Toshibi (ZnO aftertreated with polymethylhydrogenosiloxanes) Nanogard Zinc Oxide FN from Nanophase Technologies "" SPD-Z1 "from Shin-Etsu (ZnO aftertreated with a silicone grafted Acrylic polymer dispersed in cyclodimethylsiloxanes • "Escalol Z100" from ISP (alumina aftertreated ZnO dispersed in an ethylhexyl methoxycinnamate / PVP-hexadecenes / methicone copolymer blend) "Fuji ZNO-SMS-10" from Fuji Pigment (ZnO aftertreated with silica and polymethylsilsquioxane); untreated ceroxide micropigment, for example with the name "Colloidal Cerium Oxide" from Rhone Poulenc • Untreated and / or post-treated iron oxides with the name Nanogar from Arnaud.

By way of example, mixtures of various metal oxides, such as. As titanium dioxide and cerium oxide are used with and without Nachbenhandlung, such. As the product Sunveil A Fa. Ikeda. In addition, mixtures of alumina, silica and silicon post-treated titanium dioxide, zinc oxide mixtures such. B. the product UV titanium M261 Fa. Sachtleben be used.

These inorganic UV filters are usually incorporated in the formulations in an amount of from 0.1% to 25% by weight, preferably from 2% to 10% by weight.

By combining one or more of said compounds with UV filter action, the protective effect against harmful effects of UV radiation can be optimized.

All mentioned UV filters can also be used in encapsulated form. In particular, it is advantageous to use organic UV filters in encapsulated form.

In this case, the capsules in preparations to be used according to the invention are preferably present in amounts which ensure that the encapsulated UV filters are present in the preparation in the above-indicated weight percentages.

In the described preparations containing the extract according to the invention, color pigments may furthermore furthermore be present, the layer structure of the pigments not being limited.

Preferably, the color pigment when used from 0.5 to 5 wt .-% should be skin-colored or brownish. The selection of a corresponding pigment is familiar to the person skilled in the art.

Furthermore, at least one further active ingredient can be present in the preparations according to the invention. The further active ingredient is preferably selected from the group of antioxidants, vitamins, anti- Aging active ingredients, anti-inflammatory agents, antimicrobial agents, active ingredients to improve the moisture content of the skin (skin moisturizing regulators), anti-cellulite agents, anti-wrinkle agents, anti-dandruff agents, anti-acne agents, deodorants and pigments , more preferably from the group of antioxidants, vitamins, anti-aging agents and anti-cellulite agents, most preferably from the group of antioxidants and vitamins.

Substances which serve to maintain and / or to improve the moisture content of the skin may, without being construed as limiting, also be, among others, substances which belong to the so-called natural moisturizing factors, such as natural moisturizing factors. B. 2-oxopyrrolidines 5-carboxylic acid.

The protective effect of preparations against oxidative stress or against the action of radicals can be improved if the preparations contain one or more antioxidants, wherein the skilled person has no difficulty in selecting suitable fast or delayed-acting antioxidants.

There are many known and proven substances in the literature that can be used as antioxidants, e.g. For example, amino acids (eg, glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles, (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L-carnosine and their Derivatives (eg anserine), carotenoids, carotenes (eg α-carotene, β-carotene, lycopene) and derivatives thereof, chlorogenic acid and its derivatives, lipoic acid and derivatives thereof (eg dihydrolipoic acid), aurothioglucose, Propylthiouracil and other thiols (e.g., thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl , γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and derivatives thereof (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) and sulfoximine compounds (eg buthionine sulfoximines, homocysteinsulfoximine, buthionine sulfones , Penta-, hexa-, heptathionine sulfoximine) in very poor compatibility doses (eg. Pmol to μmol / kg), further (metal) chelators (eg, α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (e.g., citric acid, lactic acid, malic acid), humic acid, bile acids , Bile extracts, bilirubin, biliverdin, EDTA, EGTA, pentasodium ethylenediaminetetramethylene phosphonate and their derivatives, unsaturated fatty acids and their derivatives, vitamin C and derivatives (eg ascorbyl palmitate, magnesium ascorbyl phosphate, ascorbyl acetate), tocopherols and derivatives (e.g. Vitamin E acetate), vitamin A and derivatives (eg, vitamin A palmitate), benzoic acid coniferyl benzoate, rutinic acid and derivatives thereof, α-glycosylrutin, ferulic acid, furfurylidene glucitol, carnosine, butylhydroxytoluene, butylhydroxyanisole, nordohydroguajaretic acid, trihydroxybutyrophenone , Quercitin, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (eg ZnO, ZnSO ₄ ), selenium and its derivatives (eg selenium methionine), stilbenes and their de derivatives (eg stilbene oxide, trans-stilbene oxide).

worin
R¹ aus der Gruppe -C(O)CH₃, -CO₂R³, -C(O)NH₂ und -C(O)N(R⁴)₂ ausgewählt werden kann,
X O oder NH,
R² lineares oder verzweigtes Alkyl mit 1 bis 30 C-Atomen,
R³ lineares oder verzweigtes Alkyl mit 1 bis 20 C-Atomen,
R⁴ jeweils unabhängig voneinander H oder lineares oder verzweigtes Alkyl mit 1 bis 8 C-Atomen,
R⁵ H, lineares oder verzweigtes Alkyl mit 1 bis 8 C-Atomen oder lineares oder verzweigtes Alkoxy mit 1 bis 8 C-Atomen und
R⁶ lineares oder verzweigtes Alkyl mit 1 bis 8 C-Atomen bedeutet, vorzugsweise Derivate der 2-(4-Hydroxy-3,5-dimethoxybenzyliden)-malonsäure und/oder 2-(4-Hydroxy-3,5-dimethoxybenzyl)-malonsäure, besonders bevorzugt 2-(4-Hydroxy-3,5-dimethoxybenzyliden)-malonsäure-bis-(2-ethylhexyl)ester (z. B. Oxynex^® ST Liquid) und/oder 2-(4-Hydroxy-3,5-dimethoxybenzyl)-malonsäure-bis-(2-ethylhexyl)ester (z. B. RonaCare^® AP).Suitable antioxidants are also compounds of the formulas A or B.

wherein
R ^{1 can be selected} from the group -C (O) CH ₃ , -CO ₂ R ³ , -C (O) NH ₂ and -C (O) N (R ⁴ ) ₂ ,
XO or NH,
R ^{2 is} linear or branched alkyl having 1 to 30 C atoms,
R ^{3 is} linear or branched alkyl having 1 to 20 C atoms,
R ⁴ each independently of one another are H or linear or branched alkyl having 1 to 8 C atoms,
R ^{5 is} H, linear or branched alkyl having 1 to 8 C atoms or linear or branched alkoxy having 1 to 8 C atoms and
R ⁶ denotes linear or branched alkyl having 1 to 8 C atoms, preferably derivatives of 2- (4-hydroxy-3,5-dimethoxybenzylidene) malonic acid and / or 2- (4-hydroxy-3,5-dimethoxybenzyl) - malonic acid, particularly preferably 2- (4-hydroxy-3,5-dimethoxybenzylidene) malonic acid-bis (2-ethylhexyl) ester (z. B. Oxynex ^® ST Liquid) and / or 2- (4-hydroxy-3, 5-dimethoxybenzyl) -malonic acid-bis- (2-ethylhexyl) ester (z. B. RonaCare ^® AP).

Mixtures of antioxidants are also suitable for use in the formulations of the invention. Known and commercial mixtures mixtures are, for example comprising, as active ingredients, lecithin, L - (+) - ascorbyl palmitate and citric acid, natural tocopherols, L - (+) - ascorbyl palmitate, L - (+) -. Ascorbic acid and citric acid (for example Oxynex ^® K LIQUID), tocopherol extracts from natural sources, L - (+) - ascorbyl palmitate, L - (+) - ascorbic acid and citric acid (for example Oxynex ^® L LIQUID), DL-α-tocopherol, L (+) -. ascorbyl palmitate, citric acid and lecithin (. eg Oxynex ^® LM) or butylhydroxytoluene (BHT), L - (+) - ascorbyl palmitate and citric acid (eg Oxynex ^® 2004th). Such antioxidants are usually employed in the compositions according to the invention in amounts of from 0.1 to 20% by weight, preferably in amounts of from 0.1 to 10% by weight.

Among the phenols which can be used according to the invention, the polyphenols, which occur in part as natural substances, are of particular interest for applications in the pharmaceutical, cosmetic or nutritional field. For example, the flavonoids or bioflavonoids, which are mainly known as plant dyes, frequently have an antioxidant potential. With effects of the substitution pattern of mono- and dihydroxyflavons deal K. Lemanska, H. Szymusiak, B. Tyrakowska, R. Zielinski, IMCM Rietjens; Current Topics in Biophysics 2000, 24 (2), 101-108 , It is observed there that dihydroxyflavones having an OH group adjacent to the keto function or OH groups in the 3'4 'or 6,7 or 7,8 position have antioxidant properties, while other mono- and dihydroxyflavones sometimes have no antioxidant properties ,

Quercetin (cyanidanol, cyanidolone 1522, meletin, sophoretine, ericin, 3,3 ', 4', 5,7-pentahydroxyflavone) is frequently cited as a particularly effective antioxidant (eg. CA Rice-Evans, NJ Miller, G. Paganga, Trends in Plant Science 1997, 2 (4), 152-159 ). K. Lemanska, H. Szymusiak, B. Tyrakowska, R. Zielinski, AEMF Soffers and IMCM Rietjens (Free Radical Biology & Medicine 2001, 31 (7), 869-881 investigate the pH dependence of the antioxidant activity of hydroxyflavones. Quercetin shows the highest activity of the investigated structures over the entire pH range.

Suitable anti-aging active substances, in particular for skin-care preparations, are preferably so-called compatible solutes. These are substances that are involved in the osmoregulation of plants or microorganisms and can be isolated from these organisms. Under the generic term compatible solutes are also in the German patent application DE-A-10133202 described osmolytes. Suitable osmolytes are, for example, the polyols, methylamine compounds and amino acids and in each case their precursors. As osmolytes in the sense of the German patent application DE-A-10133202 especially substances from the group of polyols, such as myo-inositol, mannitol or sorbitol and / or one or more of the following osmolytically active substances understood: taurine, choline, betaine, phosphorylcholine, Glycerophosphorylcholine, glutamine, glycine, α-alanine, glutamate , Aspartate, proline, and taurine. Precursors of these substances are, for example, glucose, glucose polymers, phosphatidylcholine, phosphatidylinositol, inorganic phosphates, proteins, peptides and polyamic acids. Precursors are z. B. Compounds that are converted to osmolytes by metabolic steps.

Preferably according to the invention as compatible solute substances selected from the group consisting of pyrimidinecarboxylic acids (such as ectoine and hydroxyectoine), proline, betaine, glutamine, cyclic diphosphoglycerate, N. acetylornithine, trimethylamine-N-oxide di-myoinositol-phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-diglycerol phosphate (DGP), β-mannosylglycerate (Firoin), β-mannosylglyceramide (Firoin-A) or / and di-mannosyl-di-inositol phosphate (DMIP) or optical isomer, derivative, e.g. As an acid, a salt or ester of these compounds or combinations thereof.

In particular, ectoine ((S) -1,4,5,6-tetrahydra-2-methyl-4-pyrimidinecarboxylic acid) and hydroxyectoine ((S, S) -1,4,5,6-tetrahydro-5 are among the pyrimidinecarboxylic acids hydroxy-2-methyl-4-pyrimidinecarboxylic acid) and their derivatives.

Additional can be used as anti-aging active ingredients Merck products such. B. 5,7-dihydroxy-2-methylchromone, marketed under the trade name used 5 RonaCare Luremine ^{®, ®} Ronacare isoquercetin, Ronacare ^® tiliroside or Ronacare ^® cyclopeptides.

The preparations to be used may contain vitamins as further ingredients. Preference is given to vitamins and vitamin derivatives selected from vitamin A, vitamin A propionate, vitamin A palmitate, vitamin A acetate, retinol, vitamin B, thiamin chloride hydrochloride (vitamin B ₁ ), riboflavin (vitamin B ₂ ), nicotinamide , Vitamin C (ascorbic acid), Vitamin D, Ergocalciferol (Vitamin D ₂ ), Vitamin E, DL-α-Tocopherol, Tocopherol E-acetate, Tocopherol hydrogen succinate, Vitamin K ₁ , Esculin (Vitamin P active ingredient), Thiamine (Vitamin B ₁ ), Nicotinic acid (niacin), pyridoxine, pyridoxal, pyridoxamine, (vitamin B ₆ ), pantothenic acid, biotin, folic acid and cobalamin (vitamin B ₁₂ ), particularly preferably vitamin A palmitate, vitamin C and its derivatives, DL-α-tocopherol, Tocopherol E acetate, nicotinic acid, pantothenic acid and biotin. Vitamins are usually added to the flavonoid-containing premixes or preparations when applied cosmetically in the range of 0.01% to 5.0% by weight, based on the total weight. Nutritional physiology applications are based on the recommended vitamin requirement.

The described retinoids are also effective anti-cellulite agents. Another well-known anti-cellulite drug is caffeine.

Another embodiment of the present invention relates to a pharmaceutical composition containing an extract of plant parts of Tradescantia virginiana.

A "medicament", "medicament" as well as a "pharmaceutical composition", "pharmaceutical formulation" or "pharmaceutical preparation" is any agent that can be used in the prophylaxis, therapy, follow-up or treatment of patients who are at least temporarily pathogenic Show modification of the overall state or condition of individual parts of the patient organism, preferably as a result of pigmentary disorders of the skin.

To increase the protective or therapeutic effect of the compounds of the invention, pharmaceutically acceptable adjuvants may be added. For the purposes of the invention, any substance that enables, amplifies or modifies the extracts according to the invention is an "adjuvant". Known adjuvants are z. B. aluminum compounds, such as. As aluminum hydroxide or aluminum phosphate, saponins, such as. As QS 21, muramyl dipeptide or muramyl tripeptide, proteins such. Gamma interferon or TNF, MF 59, phosphatidylcholine, squalene or polyols. Furthermore, DNA encoding a protein with adjuvant effect can be administered in parallel or in a construct.

The introduction of the pharmaceutical agent into a cell or an organism can be done according to the invention in any way. The pharmaceutical agent of the present invention may be administered orally, topically, transdermally, transmucosally, transurethally, vaginally, rectally, pulmonarily, enterally and / or parenterally, preferably topically or transdermally. The chosen mode of administration will depend on the indication, dose to be administered, individual specific parameters, etc. In particular, the different modes of administration will allow for site specific therapy that minimizes side effects and reduces the drug dose.

The dosage forms of the pharmaceutical agent are prepared with the usual solid or liquid carriers and / or diluents and the commonly used excipients according to the desired mode of administration in a suitable dosage and in a conventional manner. In principle, therefore, pharmaceutically acceptable excipients known to those skilled in the art may form part of the pharmaceutical composition of the invention, the amount of excipient material combined with the active ingredient to produce a single dosage varying with the individual to be treated and the mode of administration. These pharmaceutically acceptable additives include salts, buffers, fillers, stabilizers, chelants, antioxidants, solvents, binders, lubricants, tablet coatings, flavors, colors, preservatives, sizing agents, and the like. Examples of such excipients are water, vegetable oils, benzyl alcohols, alkylene glycol, polyethylene glycol, glycerol triacetate, gelatin, carbohydrates, such as. As lactose or starch, magnesium stearate, talc and Vaseline.

The pharmaceutical formulation may be in the form of tablet, film-coated tablet, dragee, lozenge, capsule, pill, powder, granule, syrup, juice, drops, solution, dispersion, suspension, suppository, emulsion, implant, cream, gel, ointment, paste, lotion, serum , Oil, spray, aerosol, glue, plaster or dressing. As an oral dosage form preferably tablets, coated tablets, dragees, lozenges, capsules, pills, powders, granules, syrups, juices, drops, solutions, dispersions or suspensions - also prepared as a depot form - Furthermore, parenteral dosage forms such. As suppositories, suspensions, emulsions, implants or solutions to be considered, preferably oily or aqueous solutions. For topical application of the drug with at least one pharmaceutically acceptable excipient, such as. As microcrystalline cellulose, and optionally other excipients, such as. As moisturizers, applied to the skin solid formulations such. As creams, gels, ointments, pastes, powders or emulsions or to be applied to the skin liquid formulations such. As solutions, suspensions, lotions, serums, oils, sprays or aerosols formulated in a conventional manner. Preferably, the pharmaceutical agent is for topical application. The pharmaceutical agent may also be used as a solid composition, for example in the lyophilized state, and then by addition of a resolving agent, such as. B. distilled water, prior to use. The basics of the preparation of lyophilizates are familiar to those skilled in the art.

The concentration of the extract in the formulation may be from 0.01 to 99% by weight. It is crucial that the pharmaceutical composition comprises as active ingredient an effective amount of the extract together with the pharmaceutically acceptable excipients. The terms "effective amount" or "effective dose" are used interchangeably herein to denote an amount of the pharmaceutical agent that has a prophylactically or therapeutically relevant effect on a disease or pathological change in the cell, tissue, organ or mammal. A "prophylactic effect" prevents the onset of disease and also includes the increase in normal physiological function. Prophylaxis is particularly advisable if an individual has predispositions for the outbreak of the aforementioned diseases, such as. As a family history, a genetic defect or a recent disease. A "therapeutically relevant effect" partially or wholly relieves one, several or all disease symptoms or results in the partial or complete return of one or more or all of the physiological or biochemical parameters associated with or causative of the disease or pathological change the normal state. Also, follow-up is understood as a mode of therapeutic treatment when the extract is administered at specific intervals, e.g. B. to completely eliminate the symptoms of a disease. The particular dose or range of administration for the dose is large enough to achieve the desired prophylactic or therapeutic effect of inducing a biological or medical response. In general, the dose will vary with the age, constitution and gender of the patient, as well as the severity of the disease. It should also be understood that the specific dose, frequency and duration of administration will depend on a variety of factors, such as: The targeting and binding ability of the compounds, dietary habits of the individual to be treated, route of administration, excretion rate and combination with other drugs. The individual dose can be adjusted both in relation to the primary illness and in relation to the occurrence of possible complications. The exact dose can be determined by a person skilled in the art by known means and methods.

In one embodiment of the invention, in order to promote the medicinal effect, the pharmaceutical composition may also comprise one or more further active ingredients, simultaneous or sequential administration being conceivable. The therapeutic effect of the pharmaceutical composition according to the invention may consist, for example, in the fact that inhibiting the tyrosinase as a desired side effect causes certain skin brighteners to work better or reducing the number of side effects of these medications by reducing the dose.

The present invention also provides a process for the preparation of a preparation as described above, characterized in that the extract of plant parts of Tradescantia virginiana is mixed with a carrier suitable for topical applications. Optionally, the mixing can also be carried out with other auxiliaries and / or fillers. Suitable excipients and auxiliaries or fillers are described in detail in the following part.

The said constituents of the preparation can be incorporated in the usual way, by means of techniques which are well known to the person skilled in the art. The mixing may result in dissolution, emulsification or dispersion of the extract as described above in the carrier.

The cosmetic and dermatological preparations can be in various forms. So they can z. For example, a solution, an anhydrous preparation, an emulsion or microemulsion of the water-in-oil (W / O) type or of the oil-in-water (O / W) type, a multiple emulsion, for example of the Waser-in type. Oil-in-water (W / O / W) or O / W / O, a gel, a solid stick, an ointment or even an aerosol. Preference is given to emulsions. O / W emulsions are particularly preferred. Emulsions, W / O emulsions and O / W emulsions are available in the usual way.

For use, the cosmetic and dermatological preparations according to the invention are applied to the skin in a sufficient amount in the manner customary for cosmetics.

As an application form of the preparations to be used z. As: solutions, suspensions, emulsions, PIT emulsions, pastes, ointments, gels, creams, lotions, powders, soaps, surfactant-containing cleaning preparations, oils, aerosols, patches, envelopes, dressings and sprays, especially for external use. Other applications are z. As sticks, shampoos and shower rooms. Further, typical cosmetic applications are also lipsticks, lip balms, powder, emulsion and wax make-up and sunscreen, pre-Sun and after-sun preparations.

Preferred excipients come from the group of preservatives, stabilizers, solubilizers, colorants, d. H. Pigments / dyes, emulsifiers or odor improvers.

Ointments, pastes, creams and gels may contain the usual excipients suitable for topical administration, e.g. As animal and vegetable fats, waxes, paraffins, starch, tragacanth, cellulose derivatives, polyethylene glycols, silicones, bentonites, silica, talc and zinc oxide or mixtures of these substances.

Powders and sprays may contain the usual excipients, for. As lactose, talc, silica, aluminum hydroxide, calcium silicate and polyamide powder or mixtures of these substances. Sprays can additionally the usual volatile, liquefied propellant, z. For example, chlorofluorocarbons, propane / butane or dimethyl ether. Also, compressed air is advantageous to use.

Solutions and emulsions may contain the usual carriers such as solvents, solubilizers and emulsifiers, eg. As water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3 butylglycol, oils, especially cottonseed oil, peanut oil, corn oil, olive oil, castor oil and sesame oil, XTend 226 (L'Oréal), glycerin fatty acid esters, polyethylene glycols and Fatty acid esters of sorbitan or mixtures of these substances.

A preferred solubilizer in general is 2-isopropyl-5-methylcyclohexanecarbonyl-D-alanine methyl ester.

Suspensions may be the usual carriers such as liquid diluents, for. For example, water, ethanol or propylene glycol, suspending, z. For example, ethoxylated isostearyl, Polyoxyethylensorbitester and Polyoxyethylensorbitanester, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar and tragacanth or mixtures of these substances.

Soaps may contain the usual excipients such as alkali metal salts of fatty acids, salts of fatty acid monoesters, fatty acid protein hydrolysates, isothionates, lanolin, fatty alcohol, vegetable oils, plant extracts, glycerol, sugars or mixtures of these substances.

Surfactant-containing cleaning products may contain the usual excipients such as salts of fatty alcohol sulfates, fatty alcohol ether sulfates, sulfosuccinic monoesters, fatty acid protein hydrolysates, isothionates, imidazolinium derivatives, methyl taurates, sarcosinates, fatty acid amide ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable and synthetic oils, lanolin derivatives, ethoxylated glycerol fatty acid esters or mixtures of these substances.

Facial and body oils may contain the usual excipients such as synthetic oils such as fatty acid esters, fatty alcohols, silicone oils, natural oils such as vegetable oils and oily vegetable extracts, paraffin oils, lanolin oils or mixtures of these substances.

In particular, the preferred forms of preparation include emulsions which are present as cream or milk and contain, for. As mentioned fats, oils, waxes and other fatty substances, and water and an emulsifier, as it is commonly used for such a type of preparation.

Further preferred embodiments are oily lotions based on natural or synthetic oils and waxes, lanolin, fatty acid esters, in particular triglycerides of fatty acids, or oily alcoholic lotions based on a lower alcohol such as ethanol or a glycerol such as propylene glycol and / or a polyol such as Glycerol, and oils, waxes and fatty acid esters, such as triglycerides of fatty acids.

The preparation may also be in the form of an alcoholic gel comprising one or more lower alcohols or polyols, such as ethanol, propylene glycol or glycerin, and a thickener, such as silica. The oily alcoholic gels also contain natural or synthetic oil or wax.

The solid sticks consist of natural or synthetic waxes and oils, fatty alcohols, fatty acids, fatty acid esters, lanolin and other fatty substances.

If a preparation is formulated as an aerosol, the usual blowing agents are generally used, such as alkanes, air, nitrogen, dinitrogen monoxide, preferably alkanes or air.

• – Mineralöle, Mineralwachse
• – Öle, wie Triglyceride der Caprin oder der Caprylsäure, ferner natürliche Öle wie z. B. Rizinusöl;
• – Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C Zahl, z. B. mit Isopropanol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C Zahl oder mit Fettsäuren;
• – Silikonöle wie Dimethylpolysiloxane, Diethylpolysiloxane, Diphenylpolysiloxane sowie Mischformen daraus.

The lipid phase can advantageously be selected from the following substance group:

• - mineral oils, mineral waxes
• - Oils such as triglycerides of capric or caprylic acid, also natural oils such. Castor oil;
• - Fats, waxes and other natural and synthetic fats, preferably esters of fatty acids with alcohols of low C number, z. With isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids;
• - Silicone oils such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiloxanes and mixed forms thereof.

The oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the context of the present invention is advantageously selected from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 3 to 30 C atoms and saturated and / or unsaturated, branched and / or unbranched alcohols of a chain length of 3 to 30 C atoms, from the group of esters of aromatic carboxylic acid and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 C atoms. Such ester oils can then advantageously be selected from the group isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexadecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, oleyl erucate, Erucyl oleate, erucyl erucate and synthetic, semi-synthetic and natural mixtures of such esters, eg. B. Jojoba oil.

Furthermore, the oil phase can advantageously be selected from the group of branched and unbranched hydrocarbons and waxes, silicone oils, dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and fatty acid triglycerides, in particular the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a chain length of 8 to 24, in particular 12-18 C atoms. The fatty acid triglycerides can be selected, for example, advantageously from the group of synthetic, semi-synthetic and natural oils, for. For example, olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like.

Any mixtures of such oil and wax components are also advantageous to use in the context of the present invention. It may also be advantageous, if appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.

If appropriate, the aqueous phase of the preparations to be used advantageously contains alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products, furthermore lower C number alcohols, e.g. For example, ethanol, isopropanol, 1,2-propanediol, glycerol and in particular one or more thickeners, which or which can be advantageously selected from the group of silica, aluminum silicates, polysaccharides and their derivatives, for. As hyaluronic acid, xanthan gum, hydroxypropylmethylcellulose, particularly advantageous from the group of polyacrylates, preferably a polyacrylate from the group of so-called carbopols, for example Carbopols types 980, 981, 1382, 2984, 5984, each individually or in combination.

In particular, mixtures of the abovementioned solvents are used. For alcoholic solvents, water can be another ingredient.

In a preferred embodiment, the preparations to be used contain hydrophilic surfactants. The hydrophilic surfactants are preferably selected from the group of alkylglucosides, acyl lactylates, betaines and cocoamphoacetates.

As emulsifiers, for example, the known W / O and O / W emulsifiers can be used. It is advantageous to use other conventional co-emulsifiers in the preferred O / W emulsions.

For example, O / W emulsifiers are selected as co-emulsifiers, principally from the group of substances with HLB values of 11-16, very particularly advantageously with HLB values of 14.5-15.5, provided that the O / W Emulsifiers have saturated radicals R and R '. Assign the O / W Emulsifiers unsaturated radicals R and / or R ', or are Isoalkylderivate, the preferred HLB value of such emulsifiers may also be lower or higher.

It is advantageous to choose the fatty alcohol ethoxylates from the group of ethoxylated stearyl alcohols, cetyl alcohols, cetylstearyl alcohols (cetearyl alcohols).

It is also advantageous to choose the fatty acid ethoxylates from the following group:
Polyethylene glycol (20) stearate, polyethylene glycol (21) stearate,
Polyethylene glycol (22) stearate, polyethylene glycol (23) stearate,
Polyethylene glycol (24) stearate, polyethylene glycol (25) stearate,
Polyethylene glycol (12) isostearate, polyethylene glycol (13) isostearate,
Polyethylene glycol (14) isostearate, polyethylene glycol (15) isostearate,
Polyethylene glycol (16) isostearate, polyethylene glycol (17) isostearate,
Polyethylene glycol (18) isostearate, polyethylene glycol (19) isostearate,
Polyethylene glycol (20) isostearate, polyethylene glycol (21) isostearate,
Polyethylene glycol (22) isostearate, polyethylene glycol (23) isostearate,
Polyethylene glycol (24) isostearate, polyethylene glycol (25) isostearate,
Polyethylene glycol (12) oleate, polyethylene glycol (13) oleate,
Polyethylene glycol (14) oleate, polyethylene glycol (15) oleate,
Polyethylene glycol (16) oleate, polyethylene glycol (17) oleate,
Polyethylene glycol (18) oleate, polyethylene glycol (19) oleate,
Polyethylene glycol (20) oleate.

As the ethoxylated alkyl ether carboxylic acid or its salt, the sodium laureth-11-carboxylate can be advantageously used. As the alkyl ether sulfate, sodium laureth-4 sulfate can be advantageously used. As the ethoxylated cholesterol derivative, polyethylene glycol (30) cholesteryl ether can be advantageously used. Also polyethylene glycol (25) soybean oil has been proven. As ethoxylated triglycerides, the polyethylene glycol (60) Evening Primrose Glycerides can advantageously be used (Evening Primrose = evening primrose).

It is furthermore advantageous to use the polyethylene glycol glycerol fatty acid esters from the group consisting of polyethylene glycol (20) glyceryl laurate, polyethylene glycol (21) glyceryl laurate, polyethylene glycol (22) glyceryl laurate, polyethylene glycol (23) glyceryl laurate, polyethylene glycol (6) glyceryl caprate / cprinate, polyethylene glycol (20) glyceryl oleate, polyethyleriglycol ( 20) glyceryl isostearate, polyethylene glycol (18) glyceryl oleate (cocoate).

It is also convenient to select the sorbitan esters from the group of polyethylene glycol (20) sorbitan monolaurate, polyethylene glycol (20) sorbitan monostearate, polyethylene glycol (20) sorbitan monaisostearate, polyethylene glycol (20) sorbitan monopalmitate, polyethylene glycol (20) sorbitan monooleate.

As optional, but according to the invention optionally advantageous W / O emulsifiers can be used:
Fatty alcohols having 8 to 30 carbon atoms, monoglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 8 to 24, in particular 12-18 C atoms, diglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 8 to 24, in particular 12-18 C-atoms, monoglycerol ethers of saturated and / or unsaturated, branched and / or unbranched alcohols of a chain length of 8 to 24, in particular 12-18 C-atoms, diglycerol ethers of saturated and / or unsaturated, branched and / or or unbranched alcohols having a chain length of 8 to 24, in particular 12-18 C atoms, propylene glycol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 8 to 24, in particular 12-18 C atoms and sorbitan esters saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a Chain length of 8 to 24, in particular 12-18 C atoms.

Particularly advantageous W / O emulsifiers are glyceryl monostearate, glyceryl, glyceryl monomyristate, glyceryl, diglyceryl monostearate, Diglycerylmonoisostearat, propylene glycol, propylene glycol monoisostearate, propylene glycol monocaprylate, propylene glycol, sorbitan, sorbitan, sorbitan, Sorbitanmonoisooleat, sucrose, cetyl alcohol, stearyl, arachidyl, behenyl, Isobehenylalkohol, selachyl, Chimyl alcohol, polyethylene glycol (2) stearyl ether (steareth-2), glyceryl monolaurate, glyceryl monocaprinate, glyceryl monocaprylate or PEG-30 dipolyhydroxystearate.

The preparation may contain cosmetic adjuvants, which are commonly used in this type of preparations, such as. Thickening agents, emollients, humectants, surfactants, emulsifiers, preservatives, antifoaming agents, perfumes, waxes, lanolin, propellants, dyes and / or pigments, and other ingredients commonly used in cosmetics.

It is possible to use as dispersion or solubilizing agent an oil, wax or other fatty substance, a low monoalcohol or a low polyol or mixtures thereof. Particularly preferred monoalcohols or polyols include ethanol, i-propanol, propylene glycol, glycerine and sorbitol.

Even without further statements, it is assumed that a person skilled in the art can make the most of the above description. The preferred embodiments and examples are therefore to be considered as merely illustrative, in no way limiting, disclosure. The complete disclosure of all applications and publications cited above and below are incorporated by reference into this application.

Examples:

Example 1: Ethanol extract from Tradescantia virginiana

35.3 g of fresh Tradescantia virginiana leaves (plant commercially available) are extracted at 78 ° C with 250 ml of ethanol for 60 min under reflux. After removal of the solvent in a rotary evaporator, the extract obtained is taken up in 100 ml of water and shaken out for further purification of lipophilic substances and chlorophyll against heptane. After discarding the heptane phase, the water residue is evaporated. This gives 730 mg of substance.

Example 2: Water extract from Tradescantia virginiana

43.6 g fresh Tradescantia virginiana leaves are extracted at 100 ° C with 250 ml of water for 60 min. After removal of the solvent on a rotary evaporator, 490 mg of the extract are obtained.

Example 3 Stimulation of Melanin Synthesis with Ethanol Extracts from Example 1

Performing the B16V Mouse Melanoma Cell Assay:
B16V mouse melanoma cells (manufacturer: DSMZ; article number: ACC370) are translated into RPMI medium (Invitrogen, item no: 31870), which additionally contains 10% FBS (fetal bovine serum; Invitrogen, item no: 10499044 ), 2mM L-glutamine (Invitrogen, Item No: 25030) and 1mM sodium pyruvate (Invitrogen, Item No: 11360) are added, and incubated for 72 hours at 37 ° C and 5% CO ₂ . The medium is separated and the cells are washed once with 10 ml of DPBS (Dulbecco's Phosphate-Buffered Salines, Invitrogen, Item No. 14190) and the medium is then aspirated off. Add 1 mL of HyQtase-Cell Detachment Solution (Hyclone, Item No. SV30030.01) to the cells. The bottle is swiveled several times and the HyQtase-Cell Detachment Solution is then removed by suction. Then the cells are incubated for 5 min in the incubator at 37 ° C and 5% CO ₂ . The cells are taken up in the modified RPMI medium (see above) and the number of cells determined. For this, the cells are stained with trypan blue and counted in a Neubauer counting chamber. Subsequently, the cells are seeded again in the modified RPMI medium (see above) in a defined cell number of 80,000 cells per well (6-well Clear Plate, TCT, PS (Nunc)).

The cells are incubated for 24 h at 37 ° C and 5% CO2, then the medium removed. Subsequently, 1980 μL of the substance dilution are added. For this dilution of the substance, the ethanol extract from Example 1 is dissolved in DMSO and then filtered through a sterile filter (0.2 μm, Millipore, Article No. SLLG013SL). The solution is then diluted with the modified RPMI medium (see above, but in this case the FBS content is only 5%) such that the final concentration of the extract is 0.1 mg / ml, 0.05 mg / ml and 0, respectively , 01 mg / ml.

Then, 20 μL of an alpha-MSH solution (alpha-melanocyte stimulating hormone, DMSO, Sigma, item No .: D2650) is added so that the alpha-MSH concentration in the well is 10 ^-8 M. The mixture is then incubated again for 24 h at 37 ° C and 5% CO ₂ . The process described in this section is repeated twice more.

After the last incubation period, the medium is aspirated and the cells are washed with 1000 μL DPBS (Invitrogen, Item No. 14190). The medium is sucked off again. 250 μL HyQtase-Cell Detachment Solution (Hyclone, Item No. SV30030.01) is added to the cells. The 6-well plate is pivoted several times and the HyQtase-Cell Detachment Solution is then removed by suction. Then the cells are incubated for 5 min in the incubator at 37 ° C and 5% CO ₂ . The cells are taken up in 1.5 mL DPBS (Invitrogen, Item No. 14190) and transferred to a cup (SARSTEDT, Ref. 72.692.005). Subsequently, the cell number is determined. For this, the cells are stained with trypan blue and counted in a Neubauer counting chamber. Centrifuge the cells at 3500 g for 1 min. The resulting pellets are photographed and then the supernatant is suctioned off. The pellets are dissolved in 1 mL of 1N NaOH for 1 h at 80 ° C and then cooled to RT. Then 200 μL (as a quadruple determination) are pipetted four times per cup into a 96-well plate (VWR, article no. 4100636981) and the absorption at 405 nm wavelength determined (Safire, Tecan). By means of a calibration line, the content of melanin can be determined

As a comparison, a sample without extract but with 0.1% DMSO or with 0.1% DMSO and alpha-MSH (concentration in the well at 10 ^-8 M) is used in parallel. The positive control used is IBMX (3-isobutyl-1-methylxantine (Calbiochem, No. 410957).

Results (Table 1):

The extract of Tradescantia virginiana from Example 1 causes an increase in the melanin content in both the non-stimulated and in the α-MSH for tanning stimulated melanocytes. This means that the extracts according to the invention can even stimulate cells which have already been stimulated by α-MSH, in addition to further synthesizing melanin.

The extract also has an inverse concentration dependence with respect to its skin tanning action. He is already effective in very low concentrations. Table 1: Content of melanin per cell: Melanin content [pg / cell] standard deviation IBMX (200 μM) 36.39 4.48 DMSO (0.1%) 13.21 0.61 DMSO (0.1%) + α-MSH 29.52 3.37 Extract of Example 1 (100 μg / ml) + α-MSH 35.48 1.35 Extract of Example 1 (100 μg / ml) 14.05 1.65 Extract of Example 1 (50 μg / ml) + α-MSH 37.82 1.01 Extract of Example 1 (50 μg / ml) 16.35 1.06 Extract of Example 1 (10 μg / ml) + α-MSH 49.17 7.26 Extract of Example 1 (10 μg / ml) 17.58 1.00

Example 4: Skin lightening effect of water extracts from Tradescantia virginiana:

B16V mouse melanoma cells (manufacturer: DSMZ; article number: ACC370) are translated into RPMI medium (Invitrogen, item no: 31870), which additionally contains 10% FBS (fetal bovine serum; Invitrogen, item no: 10499044 ), 2mM L-glutamine (Invitrogen, Item No: 25030) and 1mM sodium pyruvate (Invitrogen, Item No: 11360) are added, and incubated for 72 hours at 37 ° C and 5% CO ₂ . The medium is separated and the cells are washed once with 10 ml of DPBS (Dulbecco's Phosphate-Buffered Salines, Invitrogen, Item No. 14190) and the medium is then aspirated off. Add 1 mL of HyQtase-Cell Detachment Solution (Hyclone, Item No. SV30030.01) to the cells. The bottle is swiveled several times and the HyQtase-Cell Detachment Solution is then removed by suction. Then the cells are incubated for 5 min in the incubator at 37 ° C and 5% CO ₂ . The cells are taken up in the modified RPMI medium (see above) and the number of cells determined. For this, the cells are stained with trypan blue and counted in a Neubauer counting chamber. Subsequently, the rows are again sown in the modified RPMI medium (see above) in a defined number of cells of 80,000 lines per well (6-well Clear Plate, TCT, PS (Nunc)).

The cells are incubated for 24 h at 37 ° C and 5% CO2, then the medium removed. Subsequently, 1980 μL of the substance dilution are added. For this dilution of the substance, the water extract from Example 2 is dissolved in water and then filtered through a sterile filter (0.2 μm, Millipore, Article No. SLLG013SL). The solution is then diluted with the modified RPMI medium (see above, but in this case the FBS content is only 5%) such that the final concentration of the extract is 0.1 mg / ml, 0.05 mg / ml and 0, respectively , 01 mg / ml.

Then, 20 μL of an alpha-MSH solution (alpha-melanocyte stimulating hormone, DMSO, Sigma, item No .: D2650) is added so that the alpha-MSH concentration in the well is 10 ^-8 M. The mixture is then incubated again for 24 h at 37 ° C and 5% CO ₂ . The process described in this section is repeated twice more.

After the last incubation period, the medium is aspirated and the cells are washed with 1000 μL DPBS (Invitrogen, Item No. 14190). The medium is sucked off again. 250 μL HyQtase-Cell Detachment Solution (Hyclone, Item No. SV30030.01) is added to the cells. The 6-well plate is pivoted several times and the HyQtase-Cell Detachment Solution is then removed by suction. Then the cells are incubated for 5 min in the incubator at 37 ° C and 5% CO ₂ . The cells are taken up in 1.5 mL DPBS (Invitrogen, Item No. 14190) and transferred to a cup (SARSTEDT, Ref. 72.692.005). Subsequently, the cell number is determined. For this, the cells are stained with trypan blue and counted in a Neubauer counting chamber. Centrifuge the cells at 3500 g for 1 min. The resulting pellets are photographed and then the supernatant is suctioned off. The pellets are dissolved in 1 mL of 1N NaOH for 1 h at 80 ° C and then cooled to RT. Then 200 μL (as a quadruple determination) are pipetted four times per cup into a 96-well plate (VWR, article no. 4100636981) and the absorption at 405 nm wavelength determined (Safire, Tecan). By means of a calibration line, the content of melanin can be determined

For comparison, a sample without extract but with 0.1% water or with 0.1% water and alpha-MSH (concentration in the well at 10 ^-8 M) is used in parallel. The positive control is hydroquinone (5 μM).

Results:

The water extract from Tradescantia virginiana from example 2 causes a reduction of the melanin content in the melanocytes stimulated by browning by α-MSH. Table 2: Melanin content per cell: Melanin content [pg / cell] standard deviation Hydroquinone (5 μM) + alpha-MSH 12.37 2.95 Water (0.1%) 17.52 3.49 Water (0.1%) + α-MSH 41.02 3.64 Extract of Example 2 (100 μg / ml) + α-MSH 29,50 2.61 Extract from Example 2 (100 μg / ml) 11.44 1.31 Extract of Example 2 (50 μg / ml) + α-MSH 24.07 4.76 Extract from Example 2 (50 μg / ml) 10.21 1.61 Extract of Example 2 (10 μg / ml) + α-MSH 35.57 3.90 Extract from Example 2 (10 μg / ml) 10.88 1.74 Example 5: O / W emulsions for skin lightening or tanning enhancement, data in% by weight ingredients 1-1 1-2 1-3 1-4 1-5 Titanium dioxide 2 5 Methylene bis-benztriazolyltetramethylbutylphenol Tradesantia virginiana extract from Example 1 or 2 0.5 0.25 0.1 0.25 0.1 4-methylbenzylidenecamphor 2 3 4 BMDBM 1 3 3 3 Stearyl alcohol (and) steareth-7 (and) steareth-10 3 3 3 3 3 Glyceryl stearate (and) ceteth-20 3 3 3 3 3 glyceryl stearate 3 3 3 3 3 Microwax 1 1 1 1 1 cetearyl 11.5 11.5 11.5 11.5 11.5 Caprylic / Capric triglycerides 6 6 6 6 6 oleate 6 6 6 6 6 propylene glycol 4 4 4 4 4 Propylparaben 0.05 0.05 0.05 0.05 0.05 methylparaben 0.15 0.15 0.15 0.15 0.15 tromethamine 1.8 water Ad 100 Ad 100 Ad 100 Ad 100 Ad 100 Example 6: O / W formulation Components / Handeisname source INCI [Wt .-%] A Marlipal 1618/11 (1) CETEARETH-11 3 Lanette O (2) CETEARYLALCOHOL 7 Luvitol EHO (3) CETEARYLOCTANOATE 5 Tegosoft TN (4) C12-15 ALKYL BENZOATE 2.5 Miglyol 812 N (1) CAPRYLIC / CAPRIC TRIGLYCERIDE 2.5 Propyl-4-hydroxybenzoate (5) PROPYLPARABEN 12:05 Tradescantia virginiana extract from Example 1 or 2 B 0.5 1,2-Prapandiol (5) PROPYLENE GLYCOL 4 Methyl 4-hydroxybenzoate (5) METHYLPARABEN 12:15 Water, demineralized AQUA (WATER) ad 100 total 100.00

Production method:

First, phase A is heated to 75 ° C and phase B to 80 ° C. Thereafter, phase B is slowly added with stirring to phase A and stirred until a homogeneous mixture is formed.

Sources:

• (1) Sasol Germany GmbH
• (2) Cognis GmbH
• (3) BASF AG
• (4) Degussa Goldschmidt AG
• (5) Merck KGaA / ^Rona®

Example 7: O / W formulation Ingredients / Trade Name source INCI [Wt .-%] A Marlipal 1618/11 (1) CETEARETH-11 3 Lanette O (2) CETEARYLALCOHOL 7 Luvitol EHO (3) CETEARYLOCTANOATE 5 Tegosoft TN (4) C12-15 ALKYL BENZOATE 2.5 Miglyol 812 N (1) CAPRYLIC / CAPRIC TRIGLYCERIDE 2.5 Propyl-4-hydroxybenzoate (5) PROPYLPARABEN 12:05 B 1,2-propanediol (5) PROPYLENE GLYCOL 4 Methyl 4-hydroxybenzoate (5) METHYLPARABEN 12:15 Tradescantia virginiana extract from Example 1 or 2 1.0 Water, demineralized AQUA (WATER) ad 100 total 100.00

Production method:

First, phase A is heated to 75 ° C and phase B to 80 ° C. Thereafter, phase B is slowly added with stirring to phase A and stirred until a homogeneous mixture is formed.

Sources:

• (1) Sasol Germany GmbH
• (2) Cognis GmbH
• (3) BASF AG
• (4) Degussa Goldschmidt AG
• (5) Merck KGaA / ^Rona®

Example 8: O / W formulation Ingredients / Trade Name source INCI [Wt .-%] A Tego Care 150 (1) GLYCERYL STEARATE, STEARETH-25, CETETH-20, STEARYL ALCOHOL 8th Lanette O (2) CETEARYL ALCOHOL 1.5 Luvitol EHO (3) CETEARYL OCTANOATE 5 Miglyol 812 N (4) CAPRYLIC / CAPRIC TRIGLYCERIDE 5 Paraffin liquid (5) PARAFFINUM LIQUIDUM (MINERAL OIL) 3 AbilWax 2434 (1) STEAROXY DIMETHICONE 1.6 Dow Corning 200 Fluid (350 cs) (6) DIMETHICONE 0.5 Propyl-4-hydroxybenzoate (5) PROPYLLPARABEN 12:05 B 1,2-propanediol (5) PROPYLENE GLYCOL 3 Methyl 4-hydroxybenzoate (5) METHYLPARABEN 12:15 Water, demineralized AQUA (WATER) ad 100 C Probiol L 05018 (Empty liposomes) (7) AQUA, ALCOHOL DENATE, LECITHIN, GLYCERINE, DISODIUM PHOSPHATE 5 Water, demineralized AQUA (WATER) 10:00 Tradescantia virginiana extract from Example 1 or 2 1.0 total 100.00

Production method:

First, phases A and B are heated to 80 ° C. Thereafter, phase B is slowly added with stirring to phase A and homogenized.

It is then cooled and the phase C at 40 ° C was added.

Sources:

• (1) Degussa-Goldschmidt AG,
• (2) Cognis GmbH,
• (3) BASF AG,
• (4) Sasol Germany GmbH,
• (5) Merck KGaA / ^Rona® ,
• (6) Dow Corning,
• (7) Kuhs GmbH & Co. KG

Example 9: W / O formulation Ingredients / Trade Name source INCI [Wt .-%] A Dow Corning 3225 C (1) CYCLOMETHICONE, DIMETHICONE COPOLYOL 23.6 Propyl-4-hydroxybenzoate (2) PROPYLPARABEN 12:05 B Tradescantia virginiana extract from Example 1 or 2 2.0 Methyl 4-hydroxybenzoate (2) METHYLPARABEN 12:15 1,2-propanediol (2) PROPYLENE GLYCOL 35.9 Water, demineralized AQUA (WATER) ad 100 total 100.00

Production method:

First, phase B is dissolved and then it is given to phase A. The pH is adjusted to pH = 6.0 with sodium hydroxide solution or citric acid.

Sources:

• (1) Dow Corning
• (2) Merck KGaA / ^Rona®

Example 10: O / W Anti-aging Cream with UV A / B protection Ingredients / Trade Name source INCI [Wt .-%] A Eusolex ^® 2292 (1) ETHYLHEXYL METHOXYCINNAMATE, BHT 3 Eusolex ^® 4360 (1) BENZOPHENONE-3 0.5 Tego Care 150 (2) GLYCERYL STEARATE, STEARETH-25, CETETH-20, STEARYL ALCOHOL 8th Lanette O (3) CETEARYL ALCOHOL 1.5 Luvitol EHO (4) CETEARYL OCTANOATE 5 Miglyol 812 N (5) CAPRYLIC / CAPRIC TRIGLYCERIDE 5 Paraffin liquid (1) PARAFFINUM LIQUIDUM (MINERAL OIL) 3 Abil wax 2434 (2) STEAROXY DIMETHICONE 1.6 Dow Corning 200 Fluid (350 cs) (6) DIMETHICONE 0.5 Propyl-4-hydroxybenzoate (1) PROPYLPARABEN 12:05 B 1,2-propanediol (1) PROPYLENE GLYCOL 3 Methyl 4-hydroxybenzoate sodium salt (1) SODIUM METHYLPARABEN 12:17 Tradescantia virginiana extract from Example 1 or 2 0.5 Water, demineralized AQUA (WATER) ad 100 total 100.00

Production method:

First, phases A and B are mixed separately and heated to 80 ° C. Thereafter, phase B is slowly added with stirring to phase A. It is homogenized cooled to room temperature.

Sources:

• (1) Merck KGaA / ^Rona® ,
• (2) Degussa-Goldschmidt AG,
• (3) Cognis GmbH,
• (4) BASF AG,
• (5) Sasol Germany GmbH, (6)

QUOTES INCLUDE IN THE DESCRIPTION

This list of the documents listed by the applicant has been generated automatically and is included solely for the better information of the reader. The list is not part of the German patent or utility model application. The DPMA assumes no liability for any errors or omissions.

Cited patent literature

• JP 2009040753 [0020]
• EP 1009378 [0021]
• DE 102007042009 A1 [0022]
• WO 93/04665 [0080]
• EP 0 487 404 A [0080]
• DE 10133202 A [0110, 0110]

Cited non-patent literature

• Brown et al., Photochemistry and Photobiology B: Biology 63 (2001) 148-161 [0071]
• K. Lemanska, H. Szymusiak, B. Tyrakowska, R. Zielinski, IMCM Rietjens; Current Topics in Biophysics 2000, 24 (2), 101-108 [0108]
• CA Rice-Evans, NJ Miller, G. Paganga, Trends in Plant Science 1997, 2 (4), 152-159 [0109]
• K. Lemanska, H. Szymusiak, B. Tyrakowska, R. Zielinski, AEMF Soffers and IMCM Rietjens (Free Radical Biology & Medicine 2001, 31 (7), 869-881 [0109]

Claims (15)

Extract of plant parts of Tradescantia virginiana. A process for producing an extract according to claim 1, comprising the steps of a) extracting the plant parts of Tradescantia virginiana using a solvent and optionally b) removing the solvent. A method according to claim 2, characterized in that the solvent is selected from water, organic solvents or mixtures thereof. A method according to claim 2 or 3, characterized in that in a step c) the extract obtained is concentrated and / or dried. Use of an extract from plant parts of Tradescantia virginiana according to claim 1 in cosmetic or dermatological preparations. Use according to claim 5 for lightening the skin. Use according to claim 6 for the inhibition of melanin synthesis, for the prophylaxis, treatment and / or follow-up of pigmentary disorders of the skin. Use according to one or more of claims 5 to 7, characterized in that it is a water extract. Use according to claim 5 as self-tanning agent. Use according to claim 9 for increasing melanin synthesis, improving melanin transport and / or improving the distribution of melanin in suprabasal layers. Use according to one or more of claims 5, 9 and 10, characterized in that it is an ethanol extract A preparation containing an extract of plant parts of Tradescantia virginiana according to claim 1. Preparation according to claim 12, characterized in that it is a cosmetic or dermatological preparation. A preparation according to claim 12 or 13, characterized in that the preparation contains 0.01 to 99 wt .-% of the extract from plant parts of Tradescantia virginiana, based on the total weight of the preparation. Process for the preparation of a preparation according to one or more of Claims 12 to 14, characterized in that the extract of plant parts of Tradescantia virginiana is mixed with a carrier suitable for topical applications.