Moringa sp. whole seed extract and using it in cosmetic and/or dermatologic compositions

FIELD: medicine.

SUBSTANCE: group of inventions refers to an anti-ageing product. Moringa sp. whole seed extract for an anti-ageing effect containing oil and polyphenols representing an extract prepared of a moderately polar solvent. Using Moringa sp. whole seed extract as an active anti-ageing ingredient. Using Moringa sp. whole seed extract for enhancing and recovering a skin barrier function. A cosmetic and/or dermatologic anti-ageing composition. A cosmetic method for the anti-ageing effect in the individuals with mature skin, involving using topical or oral administration of Moringa sp. whole seed extract. A method for preparing Moringa sp. whole seed extract.

EFFECT: extract is effective for the anti-ageing effect.

12 cl, 1 tbl, 5 ex, 1 dwg

 

The present invention relates to the extract of whole seeds ofMoringasp., containing oil (including triglycerides, fatty acids and polar lipids) and polyphenols, and the use of this extract in cosmetic and/or dermatological compositions.

Moringa is a small tree native to India, but is cultivated around the world and which caught on and became popular in various climatic conditions. There are 13 species of Moringa, belonging to the familyMoringaceaewhile the most well-knownM. oleifera(synonym:Moringa pterygosperma).

Moringa oleiferais a small tree, 4 to 8 metres tall with an open crown, spreading like an umbrella. The leaves of this plant are deciduous, 30 to 70 cm long, the flowers are white and very fragrant, the fruit is an elongated, oblong leathery hanging box triangular shape, which reaches 30 to 40 cm in length. The seeds are rounded triangles with a length of 1.2 cm and a width of 1 cm, with three membranous lateral lobes extending from seeds and having a length of 2 cm.

Wild or cultivated in tropical, humid or very dry climates this tree can survive in extreme conditions and grow very quickly. Very deep root system Moringa lets her Dodge�Sya without water for several months.

Moringa has many local names, including the tree Ben, Winged Ben, neverdié, yamamba, horseradish tree, wood "drum sticks" (Drumstick tree), and "the tree that never dies" or "the miracle tree". Indeed, Moringa is known in Ayurvedic medicine as a cure 300 diseases and, in addition, as a plant with a very high nutritional value. Its fruits are eaten cooked, the leaves are consumed as a vegetable and have a nutritional value that in some countries allow to solve the problem of malnutrition.

Edible oil, rich in oleic acid, is extracted from the seeds, which are also used as flocculants for water disinfection. The oil is obtained by pressing or by extraction with hexane from the seeds, the shell has been removed. For use flocculation properties after extraction extracted pomace oil seeds.

The seeds can be eaten as beans while they are still green. Mature seeds contain approximately 40% oil. The oil fromMoringasp. is a culinary good quality oil (like olive oil) and is also used in perfumery to produce soap or light oil (it is very resistant to oxidation).

In traditional medicine this oil is used for pain relief in �burden of gout or rheumatism (The Indian Materia Medica, pp. 811-816). Seeds is taken orally as an antipyretic agent (Hukkeri et al., Indian J. Pharm. Sci. (2006) 68, pp. 124-126).

Seed oil is obtained by pressing or extraction with the use of highly non-polar solvent (in particular, hexane), widely used in cosmetics due to its nutritional properties, due to the triglycerides contained in the oil.

Describe the use of aqueous seed extract in cosmetics: it contains peptides and proteins are active against wrinkles and cleansing properties; seeds are first peeled and degreased (U.S. patents 6500470 and USA 2006/0275247). Water and low fat protein fractions extracted from whole or peeled skin seedsMoringasp., have on the skin moisturizing, regenerating and protivooterne impact (patent EP 1064008). Specified the protein fraction of the seeds can be described as “very divided”.

According to the literature, the seeds consist of sterols (campestrini, stigmasterol, β-sitosterol, Δ5-auenstein, larosterna...), fatty acids (C18:1-oleic - from 68 to 76%, C16:0 - from 6 to 7.8%, C18:0 - from 4 to 7.6%, C20:0 - from 2.8 to 4%, and C22:0 - from 5 to 6.7%), proteins (from 26% to 32%), fibers, tocopherol (α, γ, δ: accordingly, 134, 93 and 48 mg/kg of oil).

The seeds also contain glucosinolates, including 4-(α-L-rhamnopyranoside)benzylglycine. It was also describing�about, the leaves and seeds ofMoringasp.contain some cytokinins, such as zeatin, dihydrotheelin and isopentenyladenine (U.S. patent 2006/0222682).

The applicant has demonstrated the use of a specific extract of whole seeds ofMoringasp., containing oil (including triglycerides, fatty acids and polar lipids) and polyphenols, as an active ingredient in cosmetic and/or dermatological compositions.

Thus, an object of the present invention is the extract of whole seeds ofMoringasp., containing oil (including triglycerides, fatty acids and polar lipids) and polyphenols. In the context of the present invention under “whole seeds” seeds should be understood, the shell of which has not been removed.

The extract of whole seeds ofMoringasp. characterized by (% by weight relative to the dry weight of the extract):

- an oil content of from 5% to 50%, including (i) from 2% to 10% of triglycerides and fatty acids and (ii) from 5% to 15% polar lipids;

- all content of polyphenols from 0.01% to 5% (expressed in g of pyrogallol per 100 g of dry extract).

According to the characteristic of the present invention, the oil content in the specified extract is from 25% to 40% (% by weight relative to the dry weight of the extract).

According to another feature of the present invention,Moringapreferably presents with�battle Moringa oleiferaorMoringa drouhardii.

The specified extract ofMoringasp. according to the present invention, the cosmetic and dermatological value of which was demonstrated, produced from whole seeds ofMoringasp., mostly dried, milled and then subjected to at least one extraction with the use of a moderately polar solvent.

In the context of the present invention, the term "moderately polar solvent" means the solvent is selected from the group consisting of C1-C4alcohol, acetone, a mixture of water/alcohol mixture and water/acetone, applied individually or in combination.

The solvent preferably is a mixture of ethanol/water. Mostly, when such a mixture ethanol/water is characterized by varying ratios of ethanol/water in the range of from 9/1 to 7/3 (about./vol.).

More preferably, the moderately polar solvent is a mixture of ethanol/water in a ratio of 9/1 or 3/1 (vol./vol.).

The extraction was carried out with stirring or static conditions, when heated with a reverse refrigerator or at ambient temperature, when the ratio plant/volume of solvent, which can vary from 1/5 to 1/20 for 30 minutes to 48 hours. Extraction can be repeated 2 or 3 times.

Then the pomace is separated from the ex�rakta by centrifugation or filtration, and the solution can more or less concentrate to obtain a dry extract with a yield of from 5% to 10%. Since the extract is not vysokopatogennym, during the drying phase, you can add the carrier in a weight ratio relative extractable dry matter, which can vary from 1% to 75%. The media can be a maltodextrin, lactose, silicon dioxide, or any other kosmetologicheskii acceptable carrier, solubilizers extract, such as, for example, propylene glycol/ethoxylated oleic alcohol in different ratios.

The obtained extract ofMoringasp. characterized by a content of oil (including triglycerides, fatty acids and polar lipids) and polyphenols.

Another object of the present invention is related to the specified extract ofMoringasp. for use as an active ingredient against aging.

Preferably, the specified extract standardised to fight against all signs of skin aging in people with Mature skin. In the context of the present invention, the term “Mature skin” means skin in people over the age usually over 55 years old, and preferably older than 60 years.

The signs of skin aging are characterized, in particular, loss of density and/or elasticity and/or tone and/or skin elasticity � the appearance of wrinkles and fine wrinkles.

Thus, the present invention is to obtain a new active ingredient, is able to simultaneously provide protection, hydration and nourishment of the epidermis/Mature skin and therefore provide a smoothing effect on the skin, restoring its structure and reducing sagging.

With the help of various types of tests, the Applicant has estimated the total effect of the extracts ofMoringa sp.according to the present invention against aging.

It has been shown that this new extract at the same time causes various required actions, namely:

- antioxidant, protivopedikuleznoe action to limit oxidative process associated with internal and external aging;

- the effect on the recovery of the barrier function of the skin (protein and lipid structure of the epidermis), changing with age: the use of this extract allows you to limit dehydration of the skin and thus protect the skin;

- action on the extracellular matrix to enhance the mechanical properties of Mature skin (density, elasticity, tone).

The extract according to the present invention promotes moisturizing, smoothing, preventing sagging and restoring skin structure. Thus, the extract according to the present invention allows to improve the appearance and to align the color�I.

Another object of the present invention relates to the use of the extract as defined above to enhance and restore the barrier function of the skin.

In the context of the invention, the term “strengthen the barrier function of the skin” means to improve the barrier function of the skin.

One of the fundamental functions of the skin is to provide a barrier between the body and the external environment, opposing, in one direction, the penetration through the epidermis fungi, bacteria and allergens from the environment (outside-in) and, in the other direction, the water loss (inside-out).

The epidermis is a multilayered epithelium of ectodermal origin, which is constantly updated. We can distinguish several layers of different morphological nature and cellular composition, listing from the inside out: the basal layer, the layer of cells, the keratinocytes which have a very high proliferation capacity, which leads to healing of the epidermis, adbaseline layers (granular, spinous layers), and finally the Horny layer of the epidermis (Stratum Corneum, SC). These levels correspond to increasingly higher levels of differentiation of keratinocytes. The basal layer keratinocytes lose their ability to proliferate once they start the process of moving towards the surface of the epidermis, while �otorogu keratinocytes following a program of differentiation, leading to keratinization, a process of programmed cell death. Skin barrier function first performs the Horny layer of the epidermis, firm and compacted composite structure consisting of two components:

- micropositioner cement rich in lipids: lipids arranged in a plate and covalently associated with the cell, limiting the penetration of molecules through the stratum corneum of the epidermis;

- layers of keratinized, dead cells deprived of organico (corneocytes) that corresponds to the final stage of differentiation of keratinocytes.

The integrity of the extracellular lipid cement, as well as all cellular elements of the Horny layer of the epidermis and the balance between proliferation and differentiation of keratinocytes play a key role in maintaining a functional barrier function of the epidermis.

Breach the barrier function, chronic or acute, makes the body sensitive to external influences and dehydration.

In particular, improved barrier function is crucial when the skin's barrier function has changed and needs to be restored. This occurs under certain physiological conditions, under the influence of time (aging skin) or due to hormonal disturbance or stress. The speed of such recovery, allowing the return to homeostasis, slow. In addition, barriers / crowd�RNA function of the skin is changed when the majority of the most common pathologies of the skin in the population, often accompanied by inflammation (dry skin...).

Improving the barrier function may also be useful in case you need to enhance the original function of the skin, in particular, to ensure the best resistance to external influence, which it may be subjected, in particular environmental influences (UV rays, humidity, ambient temperature, pollution, burns). Barrier function of the skin include all of the natural defense mechanisms against the stress inflicted on the skin. The most important element that performs this function is located in the most superficial part of the epidermis, in the area of the stratum corneum of the epidermis, calledstratum corneum.

Through various tests it was demonstrated that an extract as defined above, mainly affects the recovery of the lipid structure and protein structure of the epidermis.

The use of the extract according to the present invention is particularly effective to enhance and restore the barrier function of the skin.

Another object of the present invention relates to cosmetic and/or dermatological composition containing as an active beginning of the extract of whole seeds ofMoringasp. according to the invention and at least one kosmetologicheskii and/or dermatologically acceptable �excipient.

Specified cosmetic and/or dermatological composition according to the present invention contains a dry extract of whole seeds ofMoringasp., constituting from 0.1 g to 5 g per 100 g of the specified composition.

Preferably, the specified amount of the extract ofMoringasp. ranges from 0.25 g to 1 g per 100 g of the cosmetic and/or dermatological composition.

In particular, the invention relates to a cosmetic composition for anti-aging. Specified cosmetic composition is preferably adapted to fight against all signs of skin aging in people with Mature skin.

Cosmetic anti-aging composition according to the present invention may also contain one or more active ingredients such as active ingredients, tailored to protect from the sun and/or active ingredients, tailored for depigmentation of the skin.

Active ingredients adapted to protect from the sun, optionally selected from molecules obtained by chemical synthesis, known for its effect against ultraviolet rays And, by action against the ultraviolet rays of the spectrum, such as octocrylene and/or deactivatedelegation and/or bis-.

In addition, the active ingredients adapted for depigmentation of the skin, lightening and aligned�experiences of colour, may represent Niacinamide, vitamin C and its derivatives.

Kosmetologicheskii acceptable excipient considering obtaining cosmetic anti-aging composition selected so as to allow topical or oral administration.

Preferably, the form for topical application selected from the group consisting of milk, cream, balm, oil, lotion, gel, foaming gel, ointment, spray, etc.

Preferably, the oral form selected from the group consisting of tablets, capsules, lozenges, powders, granules, solutions or suspensions to be taken orally.

In particular, the invention also relates to cosmetic and/or dermatological composition adapted to enhance and restore the barrier function of the skin.

Kosmetologicheskii and/or dermatologically acceptable excipient providing cosmetic and/or dermatological composition, enhancing and restoring skin barrier function, selected so as to allow topical application.

Preferably, a form for topical application selected from the group consisting of milk, cream, balm, oil, lotion, gel, foaming gel, ointment, spray, etc.

Another object of the present invention relates to a cosmetic method to fight in�Yomi signs of skin aging in people with Mature skin, characterized by the fact that it involves the application, with local or oral administration, the extract of whole seeds ofMoringasp. according to the invention.

Further as non-limiting examples of methods of obtaining and compositions proposed in the invention.

EXAMPLES of preparation of PLANT EXTRACT

Example 1

2.5 kg of whole seedMoringa oleiferadried and ground, was extracted with 17.5 km 90 liters of ethanol (ratio of ethanol/water = 9/1) using two countercurrent extraction at 80°C. After cooling to 50°C extracted solution was removed by separating the solids from the liquid. The sample is dried, which allowed us to obtain 243 g of the extract. This extract was characterized by 36% oil content, including (i) 10% of the triglycerides and fatty acids and (ii) 10% of the polar lipids, and the total content of all polyphenols equal to 0.02% (expressed in g of pyrogallol per 100 g of dry extract).

Example 2

20 g of whole seeds ofMoringa oleiferadried and milled, extracted by heating to reflux in 100 ml of a mixture ethanol/water 75:25 V for 1 hour. Extracted solution was removed by separating the solids from the liquid and dried by using rotary evaporator at 50°C. Thus was obtained 1.66 g of the extract in the form of a brown paste, titrated at 5% oil and 068% polyphenols, expressed as pyrogallol.

Example 3

20 g of whole seeds ofMoringa drouhardiidried and milled, extracted by heating to reflux in 200 ml of a mixture ethanol/water 90:10 V for 1 hour. Extracted solution was removed by separating the solids from the liquid and dried by using rotary evaporator at 50°C. Thus was obtained 1.29 g of the extract in the form of a yellow-brown paste, titrated at 35% oil (triglycerides, fatty acids and polar lipids) and 1.3% of polyphenols, expressed as pyrogallol.

EXAMPLES of COSMETIC COMPOSITIONS

Example 4: to care for the eye area

CompositionNumber
Dry extract of the seed ofMoringasp.0.5 g
Tocopheryl acetate (alpha)0.5 g
Dextran sulfate0.3 g
Deactivatedelegation1-10 g
Octocrylene1-10 g
Bis-ethylhexyloxyphenol methoxyphenyl triturate1-10 g
Wax glycoside 2021-5 g
Stearate GLY./PEG-100 stearate1-5 g
C12-C15benzoate5 g
Pentanoate(neo)Isodecyl1-8 g
Siloxane(cyclopenta)decamethyl1-8 g
Glycerin 99,5%1-5 g
A copolymer of hydroxyethylacrylate and
acryloyldimethyltaurate sodium
1 g
Gum xanthan TF0.3 g
Capriglioneqs
Potassium sorbateqs
Purified waterqs 100 g

Example 5: anti-aging cream that improves skin color

CompositionNumber
Dry extract of the seed ofMoringasp.0.5 g
Tocopheryl acetate (alpha)
Niacinamide2 g
Methoxycinnamate(p)ethylhexyl1-10 g
Octocrylene1-10 g
Bis-ethylhexyloxyphenol methoxyphenyl triturate1-10 g
Beginin(three)/PEG-201-8 g
Cetyl alcohol >95%1 g
Political2 g
Siloxane(cyclopenta)decamethyl1-5 g
Matichon(di)200FL1-5 g
Capric Caprylic/triglyceride levels.30 701-5 g
Matichon(cyclo) Mel.90401-5 g
Gum xanthan TF0.3 g
A copolymer of hydroxyethylacrylate and
acryloyldimethyltaurate sodium
0.7 g
Glycerin 99,5%1-5 g
Capriglione qs
Sorbic acidqs
Stabilizer0.01 g
Titanium oxide/AI/sericite Mel.1-5 g
Sodium hydroxideqs
Purified waterqs 100 g

EVALUATION of ANTIOXIDANT ACTIVITY

Test applying DHPG

Antioxidant activity of seed extract ofMoringa oleiferaaccording to the present invention was evaluated using a test application DPPG. This test is based on measuring the ability of antioxidants to catch using the stable radical 2,2-diphenyl-1-picrylhydrazyl (DPPH). This stable radical, characterized by the absorption at 517 nm, is reduced to the corresponding hydrazine when chemical interaction with the donor of hydrogen.

Results:

The results are expressed in IC50, the concentration causing 50% reduction in the absorption of methanolic solution of DPPH at 0.06 mm.

Test productIC50(ág/ml)
Napoleon�th extract (hexane) of whole seeds >1000 (inactive)
Seed extract, deprived of their shell,
with 90% EtOH
1000 (inactive)
Extract according to Example 1280
Extract membrane in 90% EtOH30
Vitamin E (reference)6-10

The extract according to the invention has antioxidant activity, provided mainly by molecules present in the shell.

Chemiluminescence

Chemiluminescence is the method that ensures the formation of free radicals (superoxide radical O2°-under the action of photochemical signal. The intensity of oxidation at 1000 times greater than the intensity obtained under normal conditions. Detection is performed using chemiluminescence allows us to evaluate the antioxidant activity of lipo - or girorastvorimie extracts or molecules. The results are expressed, respectively, in an equivalent amount of vitamin C or trolox (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid). The sensitivity is of the order of nanomolar. Scheme is shown in Figure 1.

Results:

Need 65 ug ek�tract according to Example 1 to obtain equivalent activity relative to activity, found 1 µg of trolox: equivalent activity of lycopene, molecules, known due to its antioxidant activity.

This test also confirmed that the observed antioxidant activity determined mainly by molecules contained in the shell: only 4.7 mcg 90% EtOH extract of the shell is necessary for 1 µg of trolox (equivalent to activity in respect of genistein). This confirms the importance of the application according to the invention the whole seedsMoringasp.

Free radicals, production of which increases under conditions of external stress (cold, pollution, tobacco, UV), responsible for changing the DNA of skin cells and cell membranes and mitochondria. Antiradical activity of the extract obtained according to Example 1, allows you to fight against the internal and external skin aging.

ASSESSMENT ACTIVITY IN RELATION TO the RESTORATION of BARRIER FUNCTION

The epidermis plays a major role in protecting the skin, providing a chemical and mechanical barrier body. It guarantees the preservation of isolation, mainly the barrier function of the skin. Corneocytes, keratinocytes of the stratum corneum of the epidermis associated with the lipid matrix, provide a huge part of this function. However, regulation contribute to deeper layers, and not the executors of the said function. Regulated�e provides the ability of the keratinocytes of the epidermis to differentiation, not a barrier in the form of functional selective permeability (Elias PM.J Invest Dermatol125 183-200 (2005)).

From the point of view of proteins of the epidermal differentiation mainly focused on the development of structural proteins, which are keratins and which contribute to the integrity of the structure of the epidermis. Their expression varies as a function of the degree of maturation of keratinocytes. Basically keratin 1 and acidic keratin 10 are early markers of differentiation of keratinocytes present in the basal layer of the epidermis. You can trace the expression of other markers of this biological process, a later marker, e.g., expression of proteins of the cornea, such as involucrin, as well as some of the key enzymes in the initial phase the crosslinking of structural proteins with each other and with the lipids in keratinocytes, transglutaminase, such as transglutaminase 1 (TG1) (Houben E, et al.Skin Pharmacol Physiol.; 20(3):122-32 (2007)).

At the same time, the synthesis and transport of lipids in keratinocytes at the initial stage of education megameeting lipid cement required skin barrier, the formation of which constitutes the last phase of the final epidermal differentiation. This extracellular lipid matrix provides the main barrier to percutaneous move water and electrolyte� (Mizutani Y., et al.FEBS Lett.563: 93 (2004)). Accordingly, a number of enzymes and transporters of lipids show the expression of the relevant keratinocytes supplemented with differentiation. In particular, a major role during regulation play, some members of the family of ABC transporters (cassette Transporter, binding the adenosine triphosphate), and not the lipid barrier. So, are sensitive markers ABC G1, which, in particular, transports glycerol, and ABC A12 required for the migration of the precursors of lipids in lamellar bodies. Epidermal ceramides play a major specific role and represent a critical marker of the level of functionality of the skin barrier. Thus, enzymes that promote the synthesis of ceramides in the skin, show its expression and its activity, which increase especially during the destruction of the epidermal barrier function and depending on the level of epidermal differentiation. The above is, in particular, in the case of sphingolipid C4-hydroxylase/Delta-4 desaturase or hDES2, dihydroergotoxine activity which contributes to the synthesis phytoceramides in human skin (Feingold, K. R. J Lipid Res 48: 2531-2546 (2007)).

First of all, the effect of the extracts according to the invention was first studied on the model of differentiated normal human ke�of atenolol (NHK).

Then this action was studied on the model of aging keratinocytes.

The model of differentiation of normal human keratinocytes

It was analyzed the effect of extracts ofMoringasp. on gene expression of various proteins involved in the synthesis or transport of epidermal lipids, ABC G1 and hDES2.

Results:

Results are expressed as percent stimulation of gene expression (mRNA) of various markers of epidermal differentiation, expressed with the help of NHK (relative to untreated cells). Significant positive effect of stimulation was considered 100%. The results are presented in the table below.

Table 1
The action of vitamin D3, rosiglitazone and extract according to the invention in a model of differentiated normal human keratinocytes (NHK)
Methods of treatment of cellsABC G1hDES2
Vit D3 5 µm170%780%
Rosiglitazone 10 µm330%190%
Extract according to Example 1 (20 mg/ml)150% 100%

The extract obtained according to Example 1, at 20 µg/ml caused the expression of genes hDES2 G1 and ABC. Instead of the hydrophobic barrier of the extract obtained according to Example 1, allowed for the recovery of epidermal differentiation of lipids at the initial stage of regulation, which allowed to limit dehydration of the skin, particularly occurring in the case of Mature skin.

The model of aging keratinocytes

To study the ability of the skin barrier to regeneration, which is reduced in Mature subjects (Tagami, Arch. Derm. Res. 2007), used a model that simulates the aging process of the keratinocytes with the use of lines of differentiation of human HaCaT keratinocytes treated with H2O2. Analyzed the effect of extracts ofMoringasp. to restore the gene expression (mRNA) of protein markers of differentiation whose expression was inhibited in aging cells, such as K1 and involucrin.

Results:

Extract according to Example 1, with 1 and 10 μg/ml resulted in the restoration of the expression of K1 (11 and 35%, respectively) and involucrin (15% for 10 μg/ml).

Conclusion

The results obtained using the two models show good complementarity of the action (both in regard to the restoration of the lipid structure and protein structure of the epidermis) extract, proposed in the present invention.

ESTIMATED�KA ACTIVITY of EXTRACELLULAR MATRIX

Extracellular matrix (ECM) is a dynamic structure that plays a structural and regulatory role in the tissues, so the skin has the property of swelling and mechanical properties: density, elasticity and tone. In the area of the epidermis matrix fills the intercellular space and plays a role in maintaining epidermal structure. It also provides exchanges between the epidermal cells and involved in cellular activity. ECM epidermis consists, in particular, of collagen (a fibrous protein) type IV. When a cell gets old, ECM components primarily destroyed under the action of the enzyme type zinc-dependent endopeptidases called matrix metalloproteinases or MMP. The latter are actively involved in the process of scarring, but they also contribute to sagging skin and wrinkles, which are the first signs of skin aging. Among them, MMP-9 is gelatinase that exhibits activity against molecules denatured collagen (gelatin), but can also break down the natural molecules of collagen type IV, V and VII.

The effect of extracts ofMoringasp. the mRNA expression of MMP-9 were analyzed for the differentiation of human HaCaT keratinocytes treated with the use of H2O2, mimicking the aging process of cells.

Results:

Extra�t, obtained according to Example 1, significantly suppresses the gene expression of MMP-9 at three concentrations of 1, 10 and 30 μg/ml.

The extract obtained according to Example 1, allows you to restore the mechanical properties of the ECM density, elasticity and tone of the ECM of the skin and also allows you to restore the protein structure of the epidermis.

1. The extract of whole seeds of Moringa sp. to fight against all signs of skin aging, containing, in % by weight relative to the dry weight of the extract:
- from 5% to 50% oil, including (i) from 2% to 10% of triglycerides and fatty acids and (ii) from 5% to 15% polar lipids;
- from 0.01% to 5% total polyphenols, expressed as g of pyrogallol per 100 g of dry extract,
representing the extract derived from moderately polar solvent.

2. The extract of whole seeds of Moringa sp. according to claim 1, characterized in that the extract is, in particular, an extract of Moringa oleifera or Moringa drouhardii.

3. The use of the extract of whole seeds of Moringa sp. according to any one of claims.1 and 2 as an active ingredient against skin aging.

4. The use according to claim 3, characterized in that the active component adapted to fight against all signs of skin aging in people with Mature skin.

5. The use of the extract of whole seeds of Moringa sp. according to any one of claims.1 and 2 to enhance and restore the barrier function of the skin.

6. Cosmetic and/and�and dermatological composition for the fight against all signs of skin aging, containing the active beginning of the extract of whole seeds of Moringa sp. according to any one of claims.1 and 2, and at least one kosmetologicheskii and/or dermatologically acceptable excipient.

7. The composition of claim 6 containing dry extract of whole seeds of Moringa sp. at a level of from 0.1 g to 5 g per 100 g of the specified composition.

8. A composition according to claim 6, further comprising one or more active components adapted to protect from the sun and/or depigmentation of the skin.

9. Cosmetic way to combat all signs of skin aging in people with Mature skin, characterized in that it comprises applying, by topical or oral administration, the extract of whole seeds of Moringa sp. according to any one of claims. 1 and 2.

10. Method for producing extract of whole seeds of Moringa sp. according to any one of claims.1 and 2, wherein the following stages:
- grinding the whole seeds;
- at least one extraction with the use of a moderately polar solvent;
- centrifugation or filtration;
- and drying.

11. A method according to claim 10, wherein the moderately polar solvent is selected from the group consisting of C1-C4alcohol, acetone, a mixture of water/alcohol mixture and water/acetone, used individually or in combination.

12. A method according to claim 10 or 11, wherein the moderately polar solvent is a with�ect ethanol/water, preferably with a ratio of ethanol/water from 9/1 to 7/3 (about./vol.).



 

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9 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetic industry and represents a cosmetic product which has the following composition in each specific case calculated using the total composition: at least 0.1 wt % of at least one hydrophilic softening product, 2 to 40 wt % of at least one surfactant specified in a group of fatty alcohol ethoxylates, fatty alcohol ether sulphates and salts of sulphated and/or sulphonated fatty acids, 30 to 90 wt % of water, 1 to 30 wt % of one or more abrasives with the total ingredients making 10%; the product contains at least 0.1 wt % of at least one hydrophilic softening product with a hydrophilic-lipophilic balance ≥8 and flour thermally treated by saturated vapour; the flour is natural flour of shell or kernels characterized by a light absorption at wave length 660 nm of less than 1 prepared by reacting the flour 1 g with a solution prepared of water 10 ml and 0.1% aqueous methylene blue 1 ml.

EFFECT: invention provides the lower effect on viscosity, possesses the high cleaning action and high tolerability.

16 cl, 5 ex, 3 tbl

Foaming detergent // 2543713

FIELD: chemistry.

SUBSTANCE: invention relates to aqueous foaming composition for hands, containing castor oil maleate in amount from 0.1 to 1% of composition weight, PEG-7 glyceryl cocoate in amount from 0.05 to 0.3% of composition weight, glycerol in amount from 0.5 to 6% of composition weight, PEG-6 of glycerides of caprylic/capric acid in amount from 0.05 to 1% of composition weight and SAS. Glycerol is present in amount greater than amount of castor oil maleate or glyceryl cocoate PEG-7, and said composition has viscosity from 1 to 100 mPa·s (sP).

EFFECT: obtaining aqueous foaming composition for hands, which is capable of providing foam stability, has lower tendency for flowing and soiling when applied and creates more pleasant sensations for skin.

7 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to oral care compositions containing a basic amino acid or its salt. The presented oral care composition promoting the dentine defect closure in the oral cavity contains arginine in the free form or in the form of a salt, and an abrasive substance representing synthetic amorphous silica and containing small particle fractures making at least approximately 5% of total weight of the composition, wherein the particles of the small particle fracture having d50 from 3 to 4 mcm. What is also presented is a method of treating sensitive teeth in the oral cavity involving using the oral treatment with this composition, as well as using arginine as a part of the oral care composition and for producing a therapeutic agent, wherein the above composition and agent contain the above abrasive material containing the small particle fracture.

EFFECT: group of inventions provide the effective dentin defect closure in the patient's oral cavity.

8 cl, 1 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: rejuvenating effect is ensured by exposing high-molecular hyaluronic acid to gamma-radiation to preparing a stable low-molecular hyaluronic acid, which is used as a prescribed ingredient alongside with synthesised matrix peptide of specific amino acid sequence.

EFFECT: prescribed combination of low-molecular hyaluronic acid and matrix peptides of the developed cosmetic product enables achieving the pronounced aesthetic effect by a physiological mechanism of stimulation of developing proper hyaluronic acid in the skin.

2 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents an oral care composition, which contains 5 - 95 wt % of an orally acceptable carrier; and a film, wherein the above film contains 10 - 60 wt % of the film of an odour control active ingredient (a zinc-containing compound), 2 - 5 wt % of the film of a mucoadhesive polymer (polyacrylic acid or polyacrylate, polyalkylacrylate, polyvinylpyrrolidone, poly(acrylate)/polyvinylpyrrolidone copolymer, chitosan, 20 - 30 wt % of the film of one or more release controlling polymers (polyvinyl acetate or hydroxyethyl cellulose), 25 - 50 wt % of the film of a polymeric base (hydroxypropyl methyl cellulose, methyl cellulose, hydroxypropyl cellulose and a copolymer thereof) and a flavouring agent, wherein the above film is integrated into the above orally acceptable carrier and makes 0.1 - 5 wt % of the orally acceptable carrier.

EFFECT: invention provides creating the agent able to keep the breath fresh for a long period of time.

5 cl, 5 ex, 7 tbl, 6 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a foaming personal care composition containing: - a carrier; - an oil phase containing at least one terpene alcohol, which has a cyclic structure; - at least partially fluorinated compound; and - a stabilising agent, wherein the mass ratio of at least partially fluorinated compound and terpene alcohol makes from 2:1 to 4:1.

EFFECT: composition possesses higher stability and provides initial foaming and a longer positive skin effects, including cleansing and moistening.

16 cl, 12 tbl, 14 ex

FIELD: food industry.

SUBSTANCE: method for production of Siberian cedar seeds liqueur (with hepatoprotective, antioxidant, antihypoxic, hypolipidemic effect) by way of maceration with ethyl alcohol usage; whole Siberian cedar seeds are loaded into the reactor, poured with 70% ethyl alcohol water solution; extraction is performed under preset conditions. The medicinal preparation with hepatoprotective, antioxidant, antihypoxic, hypolipidemic effect contains Siberian cedar seeds liqueur. Usage of the medicinal preparation as a hepatoprotective remedy.

EFFECT: liqueur has pronounced hepatoprotective, antioxidant, antihypoxic and hypolipidemic effect.

6 cl, 3 dwg, 8 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and dermatology and represents a skin care composition applicable for local skin application, wherein the above composition contains salicylic acid or its salt in a combination with glycyrrhizic acid, or its salt or its derivative, cetylhydroxyproline palmitamide, lactic acid or its salt, bisabolol and niacinamide.

EFFECT: invention provides extending the range of effective skin care agents.

41 cl, 11 ex, 11 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions concerns oral care compositions effective for treating dental hypersensitivity, and a method of treating using them. The composition contains a compound of formula I: M1-A-M2-B-M1; wherein M1 and M3 represent potassium (K); M2 represents Ti or titanium (Ti) oxide; A and B independently represent C2-C6 dibasic acid; and at least one orally acceptable solvent. The oral care composition has pH falling within the range of 2.0 to 7.0. There are also presented a version of the composition, which contains at least one additional desensitising agent, and a method of treating sensitive teeth with the use of this composition.

EFFECT: using the group of inventions provides the effective dental desensitisation by creating a protective barrier on the tooth surface and/or sealing the effective dental tubules effectively.

11 cl, 8 tbl, 12 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to novel pyridine derivatives of the general formula

and to their pharmaceutically acceptable salts, where R1 stands for (C1-6) alkyloxy, CN or halogen, R2 stands for a hydrogen atom, R3 stands for a hydrogen atom or (C1-6) alkyl, R4, R5, R6, R7 are similar or different and stand for a hydrogen atom or halogen. The invention also relates to the cosmetic application of the formula (I) compound.

EFFECT: novel pyridine derivatives, useful in the treatment of diseases associated with a receptor of androgens, are obtained.

9 cl, 1 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to health-promoting compositions and methods for preparing them. A method for preparing the composition of non-living lactic acid bacilli, possessing an ability of specific binding to Streptococcus mutans, involves the following stages: heating a cell suspension of lactic acid bacillus or a mixture of lactic acid bacilli possessing an ability of specific binding to Streptococcus mutans from an initial temperature of less than 40°C to a pasteurisation temperature of 75 to 85°C with a temperature variation within the range of 0.5 to 2°C/min, keeping the heated suspension at a pasteurisation temperature of 20 to 40 minutes and cooling the suspension to a final temperature of less than 40°C within the range of 0.5 to 2°C/min. The specific binding the cell suspension of the lactic acid bacillus or the mixture of lactic acid bacilli to Streptococcus mutans is stable to heat treatment and/or resistant to proteases and/or calcium-dependent and/or is observed within the range of pH values falling within the range of 4.5 and 8.5, and/or in the saliva environment.

EFFECT: invention enables producing the agent preventing or delaying the caries lesion formation.

9 cl, 4 ex

FIELD: medicine.

SUBSTANCE: 0.5% dihydroquercetin is instilled into the rectum of a patient with temporary colostomy until he/she starts feeling intestinal inflation. The procedure is performed twice a day, daily up until the restorative surgery.

EFFECT: method reduces a rate and a degree of colitis manifestations by the local antioxidant, anti-inflammatory effect, unfolding the excluded colon.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetic industry and represents a cosmetic product which has the following composition in each specific case calculated using the total composition: at least 0.1 wt % of at least one hydrophilic softening product, 2 to 40 wt % of at least one surfactant specified in a group of fatty alcohol ethoxylates, fatty alcohol ether sulphates and salts of sulphated and/or sulphonated fatty acids, 30 to 90 wt % of water, 1 to 30 wt % of one or more abrasives with the total ingredients making 10%; the product contains at least 0.1 wt % of at least one hydrophilic softening product with a hydrophilic-lipophilic balance ≥8 and flour thermally treated by saturated vapour; the flour is natural flour of shell or kernels characterized by a light absorption at wave length 660 nm of less than 1 prepared by reacting the flour 1 g with a solution prepared of water 10 ml and 0.1% aqueous methylene blue 1 ml.

EFFECT: invention provides the lower effect on viscosity, possesses the high cleaning action and high tolerability.

16 cl, 5 ex, 3 tbl

Foaming detergent // 2543713

FIELD: chemistry.

SUBSTANCE: invention relates to aqueous foaming composition for hands, containing castor oil maleate in amount from 0.1 to 1% of composition weight, PEG-7 glyceryl cocoate in amount from 0.05 to 0.3% of composition weight, glycerol in amount from 0.5 to 6% of composition weight, PEG-6 of glycerides of caprylic/capric acid in amount from 0.05 to 1% of composition weight and SAS. Glycerol is present in amount greater than amount of castor oil maleate or glyceryl cocoate PEG-7, and said composition has viscosity from 1 to 100 mPa·s (sP).

EFFECT: obtaining aqueous foaming composition for hands, which is capable of providing foam stability, has lower tendency for flowing and soiling when applied and creates more pleasant sensations for skin.

7 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to oral care compositions containing a basic amino acid or its salt. The presented oral care composition promoting the dentine defect closure in the oral cavity contains arginine in the free form or in the form of a salt, and an abrasive substance representing synthetic amorphous silica and containing small particle fractures making at least approximately 5% of total weight of the composition, wherein the particles of the small particle fracture having d50 from 3 to 4 mcm. What is also presented is a method of treating sensitive teeth in the oral cavity involving using the oral treatment with this composition, as well as using arginine as a part of the oral care composition and for producing a therapeutic agent, wherein the above composition and agent contain the above abrasive material containing the small particle fracture.

EFFECT: group of inventions provide the effective dentin defect closure in the patient's oral cavity.

8 cl, 1 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing technetium-99m labelled nanocolloid for radionuclide diagnosis. The disclosed method includes preparing a starting suspension of a nanocolloid in 0.1% sodium dodecylbenzene sulphate and passing said suspension through a filter with pore diameter of 100 nm, adding a technetium-99m eluate, then adding 0.20-0.25 mg ascorbic acid, 2.5-4.0 mg gelatine and 0.02-0.03 mg tin (II) chloride dihydrate per 1 ml of the mixture. The obtained mixture is heated in a water bath at 70-80°C for 30 minutes, cooled to room temperature in an ultrasonic bath and then subjected to sterilisation filtration. The nanocolloid used is iron-carbon particles whose surface is chemically modified with arenediazonium tosylate.

EFFECT: invention enables to obtain technetium-99m labelled nanocolloid, for which not less than 80% of particles have a size in the range of 20-100 nm, relative content of particles with a size smaller than 20 nm is not more than 6% and radiochemical purity is higher than 90% and is maintained for not less than 4 hours.

1 dwg, 4 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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