JP7467116B2 - Skin preparation containing extract of rose of the bank - Google Patents

Description

The present invention relates to a composition for topical application to the skin that has an elastase activity inhibitory effect.

Wrinkles and sagging skin, which are signs of skin aging, are known to occur due to a decrease or cross-linking of the extracellular matrix (collagen (collagen fibers), elastin (elastic fibers), etc.) caused by UV exposure, dryness, or aging. Elastin in particular contributes to tissue elasticity by forming cross-links with other molecules, but it is known to denature and degrade due to UV exposure or aging as a result of overexpression of elastase, an elastin-degrading enzyme. In fact, there have been reported cases in which wrinkles have been improved by the application of elastase inhibitors (Patent Documents 1 and 2). From the above, in order to prevent wrinkles and sagging skin caused by aging, it is important to inhibit elastase activity and prevent the breakdown of elastin.

Natural ingredients are preferred on the market for topical skin preparations that are applied directly to the skin, so naturally derived ingredients are desirable. One example of such naturally derived elastase inhibitors is the hybrid tea rose. However, hybrid tea roses are susceptible to disease and are difficult to cultivate, so there are still issues with their industrial use (Patent Document 3).

On the other hand, the species of rose known as Rosa japonica is an original species of rose native to China, has no thorns on its branches, is robust and easy to grow, and although small, produces very good flowers, making it suitable for industrial use. The effects of the species known to be antibacterial and anti-glycation effects, but its elastase inhibitory activity was not known (Patent Documents 4 to 7).

JP 11-335235 JP2006-008562A Patent Publication 2011-236147 JP 9-255518 A JP 9-255517 A Patent Publication 2015-160842 JP2004-189663

The present invention aims to provide an elastase activity inhibitor that is naturally derived and has excellent effects. It also aims to provide an agent for preventing and improving wrinkles and sagging skin with the above-mentioned effects.

The present inventors conducted extensive research to solve the above problems. As a result, they discovered that an extract of Rosa platyphylla (Rosa platyphylla) of the family Rosaceae has an excellent effect of inhibiting elastase activity, exerts an anti-aging effect, and makes it possible to provide a naturally derived topical skin composition.

The present invention provides a skin topical composition containing an extract of Rosa sieboldii (Rosa sieboldii) of the Rosaceae family as an active ingredient, which has a significantly superior effect of preventing and improving aging phenomena (wrinkles, sagging, etc.) due to the elastase activity inhibitory effect of the extract.

4 shows the elastase inhibitory activity of extracts of yellow rose flower, ladylac flower, and Oklahoma flower.

Preferred embodiments of the present invention will now be described in detail.
The Banksia species used in the present invention is of the Rosa genus of the Rosaceae family, and is also known as bank's rose. As the Banksia species, for example, yellow Banksia, white Banksia, or their variants and hybrids can be used. The parts of the plant used are not particularly limited. The whole plant, leaves, stems, flowers, etc. can be used, and multiple parts such as leaves and flowers can be used, but it is preferable to use the flowers. The harvesting time is not particularly limited, and any harvesting time can be used.

The method for preparing the extract is not particularly limited, but for example, any part (e.g., flowers, whole plant, etc.) of the species Rosa spp. of the Rosaceae family, Rosa genus, can be washed with water if necessary to remove foreign matter, and then either as is or dried, shredded or crushed as necessary, and then contacted with an extraction solvent to perform extraction. Extraction can be performed by contacting with an extraction solvent according to a conventional method such as the immersion method, but supercritical extraction or steam distillation can also be used. However, it is not necessary to prepare the extract in advance, and the active ingredient can be dissolved in the skin topical preparation by directly adding, for example, a dried part of the species of Rosa spp.

The extraction solvent is not particularly limited, but examples include water; lower alcohols such as methanol, ethanol, and propanol; and polyhydric alcohols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, and glycerin, which may be used alone or in combination of two or more.

Among these extraction solvents, hydrophilic solvents such as water, lower alcohols, or polyhydric alcohols are preferred in the present invention from the standpoint of the effectiveness of the resulting extract, as well as skin irritation, and because they can be widely applied to topical skin preparations. Preferred examples of hydrophilic solvents include the use of mixed solvents with water, lower alcohols (especially ethanol), or polyhydric alcohols (especially 1,3-butylene glycol and glycerin).

The extraction method for the extract that can be used in the present invention is not particularly limited, but for example, the mass ratio of the dried part of a plant of the genus Rosa of the family Rosaceae to the extraction solvent is 1 to 1000 times, and particularly 10 to 100 times, of the solvent, and in the case of extraction at room temperature, it is preferable to carry out the extraction at 0°C or higher, particularly 20°C to 40°C, for 1 hour or more, and particularly 3 to 7 days. It is also possible to carry out heating extraction at 60 to 100°C for 1 hour.

The extract obtained under the above conditions may be used as is, or, if necessary, may be further processed by filtration or the like, concentrated, or powdered, and used accordingly.

The amount of the extract used in the present invention is not particularly limited, but is preferably 0.01 to 20.0% by mass, calculated as the evaporated dry matter, and is most preferably in the range of 0.1 to 10.0% by mass.

The form of the Rose of Banks extract used in the present invention may be any of liquid, solid, powder, paste, gel, etc., and the most suitable form for constructing the final product can be selected at will.

In the present invention, in addition to the essential components of the present application, for example, fats and oils, waxes, hydrocarbon oils, ester oils, water-soluble polymers, thickeners, powders, skin protective agents, whitening agents, wrinkle improving agents other than Rose of Banks and/or extracts of Rose of Banks, anti-aging agents, plant extracts, preservatives, anti-inflammatory agents, pH adjusters, sequestering agents, antioxidants, stabilizers, fragrances, colorings, pigments, etc. can be mixed and appropriately blended as necessary within the scope that does not impair the effects of the present invention, to form the topical composition into a lotion, emulsion, cream, pack, powder, spray, ointment, dispersion, cleanser, and various dosage forms such as liquid, paste, capsule, powder, tablet, etc.

The present invention will be explained in more detail below with reference to examples, but the present invention is not limited to these examples.

(Example 1) Preparation of extract Yellow Banksweet flowers (dried material), Lady Luck flowers (dried material), a type of hybrid tea rose known to have elastase inhibitory activity, and Oklahoma flowers (dried material) were extracted with a 10-fold amount of 50% (v/v) aqueous ethanol solution for three days, and the dried products of the obtained extract components were used as samples.

<Elastase inhibition test>
Elastase activity was measured as follows. 0.1 M HEPES and 0.5 M NaCl (pH 7.4) were used as the reaction buffer. Methoxy-succinyl-alanyl-alanyl-prolyl-valine-p-nitroanilide was dissolved in DMSO as the elastase substrate to 80 mM, and diluted with the reaction buffer to 8 mM before use. Human leukocyte-derived elastase (SIGMA) was used as the elastase, and dissolved in the reaction buffer to 0.25 Unit/mL. The sample was prepared with a 50% (v/v) ethanol aqueous solution to a solid content of 250 to 1000 ppm. 25 μL of 8 mM elastase substrate was dispensed into a 96-well plate, and 50 μL of the sample was added. Next, 25 μL of 0.25 Unit/mL elastase was added and incubated at 37° C. for 20 minutes. Then, absorbance was measured at 415 nm. The inhibition rate was calculated according to the following function:

The results are shown in Figure 1. As a comparative example, Figure 1 also shows the results of extracts from Oklahoma and Lady Lack, which are types of hybrid tea roses already known to have elastase inhibitory activity. At solids concentrations of 250 to 1000 ppm, Banksea rose had a higher elastase inhibitory effect than Lady Lack and Oklahoma. This makes it clear that Banksea rose exhibits a more effective elastase activity inhibitory effect than hybrid tea rose.

Next, a skin topical preparation according to the present invention was prepared. The blending ratios are in mass %. For the rose of Banksea, 2g of dried yellow Banksea flowers were extracted with 10 times the amount of 50% ethanol, 2g of dried white Banksea leaves were extracted with 10 times the amount of water, and 2g of dried yellow Banksea stems were extracted with 10 times the amount of 100% ethanol, and the resulting aqueous solutions containing 1% of the dried extract components were used to prepare the respective extracts.

Formulation Example 1 is shown in Table 1. The ingredients shown in Table 1 were added to purified water and mixed uniformly to prepare the formulation.

Formulation Example 2 is shown in Table 2. The ingredients for the aqueous phase are mixed, heated and kept at 70°C to form the aqueous phase. Meanwhile, the ingredients for the oil phase are mixed, heated and dissolved at 70°C to form the oil phase. This oil phase is added to the aqueous phase described above and pre-emulsified, homogenized with a homomixer, and cooled to 30°C to obtain a cosmetic cream.

Formulation Example 3 is shown in Table 3. The ingredients for the aqueous phase were mixed and heated to 70°C to form the aqueous phase. Meanwhile, the ingredients for the oil phase were mixed and heated to dissolve at 70°C to form the oil phase. This oil phase was added to the aqueous phase and emulsified, and then cooled to 30°C to obtain a cosmetic emulsion.

As a representative example, Formulation Example 1, which contains yellow Rosa candida (flower) extract, was used in a one-month usage test by five panelists skilled in sensory evaluation. Formulation Example 1, which contains yellow Rosa candida (flower) extract, or a control, Formulation Example 1 without yellow Rosa candida (flower) extract, was applied to half of each face. After one month of use, an evaluation was conducted on the effect of improving wrinkles and sagging. The results regarding the effect of improving wrinkles are shown in Table 4, and the results regarding the effect of improving sagging are shown in Table 5.

From the above, it has been confirmed that the use of extract from Banksea laurel has the effect of improving wrinkles and sagging skin.

According to the present invention, an elastase activity inhibitor containing an extract of Rosa batatas (Rosa canadensis) of the Rosaceae family as an active ingredient can be provided, and due to the elastase activity inhibitory effect of the substance, it is possible to provide an external skin composition which has superior effects in preventing and improving aging phenomena (wrinkles, sagging, etc.) compared to conventional compositions.

Claims (3)

An elastase activity inhibitor (excluding wound treatment applications) containing as an active ingredient at least one of a mixed solvent extract of Rosa banksiae flowers with water and ethanol (excluding cell cultures) or a mixed solvent extract of water and 1,3-butylene glycol ( excluding cell cultures) . The present invention provides an agent for preventing and improving wrinkles and sagging, which contains as an active ingredient at least one of a mixed solvent extract of the flower of Rosa japonica of water and ethanol (excluding cell cultures) or a mixed solvent extract of water and 1,3-butylene glycol ( excluding cell cultures) . A cosmetic skin preparation for external application containing at least one of an extract of a flower of Rosa montana with a mixed solvent of water and ethanol (excluding cell cultures) or an extract of a flower of Rosa montana with a mixed solvent of water and 1,3-butylene glycol (excluding cell cultures) as an active ingredient .