JPH0867615A - Cosmetic - Google Patents

Abstract

PURPOSE: To obtain a cosmetic high in whitening activity, capable of inhibiting the activity of hyaluronidase, and effective for preventing skin chapping, containing, as active ingredient, a solvent extract from Rumex cyprius used as a crude drug in Egypt. CONSTITUTION: This cosmetic contains, as active ingredient, an extract derived from Rumex cyprius, a kind of plant belonging to Polygonaceae and used as a crude drug in Egypt by subjecting the plant to extraction with water or a hydrophilic organic solvent such as ethanol, methanol or acetone. This extract presents skin whitening activity, hyaluronidase activity-inhibitory effect, active oxygen-inhibitory activity, antioxidative effect, antiplasminic activity, and collagenase activity-inhibitory effect. Formulation of this extract in a cosmetic results in excellent skin whitening effect and preventing skin chapping, and has significant effect of retaining skin luster and firmness.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a cosmetic which has a strong whitening effect, inhibits the activity of hyaluronidase and is effective in preventing rough skin.

[0002]

[Prior Art] Rumex cyprius
us) is a plant of the Polygonaceae genus, which is used as a crude drug in Egypt.

Various substances are known as substances having a whitening effect that can be used as a raw material for cosmetics, but synthetic products are not guaranteed to be safe when applied to human skin for a long period of time and cannot be used. Being limited. On the other hand, many natural products have a weak whitening effect. However, from the viewpoint of safety for human skin, it is a natural product that is guaranteed for safety by being eaten by many people for many years, has a strong whitening effect, and also has other effects on the skin. Was desired.

[0004]

The object of the present invention is to provide a cosmetic composition which is safe when applied to the skin, has a large whitening effect, inhibits the activity of hyaluronidase, and further contains an ingredient effective for rough skin and the like. Is to provide.

[0005]

[Means for Solving the Problems] In order to solve the above problems, the present inventors screened and investigated plants that have been used for food for many years and confirmed to be safe for the human body, and used as cosmetics. Considered something of value. As a result, they have found that Rumex cyprius is effective as a raw material for cosmetics or as a quasi drug. As the confirmed effects, whitening action, hyaluronidase activity inhibitory action, active oxygen suppressing action, antioxidant property, antiplasmin action, and collagenase activity inhibiting action were confirmed.

That is, the present invention is a cosmetic containing a solvent extract of Rumex cyprius.

As a method of utilizing Rumex cyprius, extraction is carried out with water or a hydrophilic organic solvent such as ethanol, methanol or acetone. However, it is natural that extraction with water, ethanol, or a mixed solvent thereof is preferable since it is extraction of cosmetic raw materials. In some cases, a polyhydric alcohol such as glycerin, 1,3 butylene glycol, propylene glycol or the like or a mixed liquid of polyhydric alcohol and water can be used for extraction. Further, freeze-drying and using it as powder is also effective depending on the method of use.

This substance can be used as other cosmetic raw materials such as liquid oils such as squalane and jojoba oil, solid oils such as beeswax and cetyl alcohol, various activators, moisturizers such as glycerin and 1,3 butylene glycol, and various drugs. It can be added to prepare cosmetics in various dosage forms. For example, a lotion, a cream, a milky lotion, a pack, or the like may be used depending on the purpose.

As described above, the effect of the extract of the present invention is, firstly, the whitening effect on the skin. Secondly, it has an activity of suppressing hyaluronidase activity. Hyaluronidase is an enzyme that is widely distributed in the living body and is also present in the skin. As its name implies, it decomposes hyaluronic acid. Hyaluronic acid is β-DN
-Acetylglucosamine and β-D-glucuronic acid are alternately bonded to each other to form a linear polymer polysaccharide, which is a kind of glycosaminoglucan widely existing in connective tissues of mammals along with chondroitin sulfate and the like. As a function of hyaluronic acid in connective tissue, it retains water in the intercellular spaces, forms a jelly-like matrix in the tissue to retain cells, maintains skin lubricity and flexibility, and exerts external force (mechanical force). Disability)
And is believed to prevent bacterial infections. It is said that hyaluronic acid in the skin decreases with age, resulting in aging such as wrinkles and roughness.
Therefore, suppressing the activity of hyaluronidase, which decomposes this, stabilizes the stability of hyaluronic acid used in the formulation and the stability of hyaluronic acid in the formulation after application to the skin and hyaluronic acid present in the skin. It is thought to contribute.

Thirdly, it has an effect of suppressing active oxygen. There is oxygen in the air, and without it, living things (except anaerobic ones) cannot exist. However, oxygen becomes active oxygen under the influence of ultraviolet rays and enzymes. Active oxygen oxidizes fatty acids and produces peroxides. It also oxidizes and damages the phospholipids of biological membranes in the body. Furthermore, it is said that the generated peroxide and active oxygen damage DNA and accelerate aging. This active oxygen also influences the mechanism of making melanin from tyrosine and is also involved in the blackening of the skin. Suppressing this active oxygen is an important factor for the skin, in other words, an important factor required for cosmetics. The Rumex cyprius of the present invention also has this active oxygen suppressing action, fourthly antioxidative action, fifthly antiplasmin action and sixthly
It also has an inhibitory effect on collagenase activity.

Fifth, Rumex cyprius acts as a plasmin inhibitor. Plasmin is one of the proteolytic enzymes present in blood, and the precursor plasminogen in blood is cleaved by an enzyme called plasminogen activator to become plasmin. An important physiological effect of plasmin is thrombolysis. Plasminogen activator in blood has an affinity for fibrin, which is a component of thrombus, and acts on plasminogen in the fibrin clot (thrombus) to be activated to plasmin.

As a result, plasmin formed in the fibrin clot dissolves the thrombus from the inside of the clot. There are several kinds of substances that inhibit the activity of plasmin in blood, and plasmin released in the blood is rapidly inactivated, and nonspecific proteolysis other than fibrin is suppressed. One of the proteases, plasmin, has a function of dissolving fibrin (fibrin) formed in the blood coagulation process. Factors that antagonize this effect of plasmin are plasmin inhibitors. It is already known as a plasmin inhibitor in which tranexamic acid and ε-aminocaproic acid have been chemically synthesized, and they are mixed in toothpaste etc. with the expectation of a bleeding prevention effect.

There is a natural plasmin inhibitor called α ₂ plasmin inhibitor in human blood, which acts on generated plasmin to rapidly deactivate it and suppress its action. Plasmin inhibitors are said to have potential applications in cancer metastasis prevention.

Sixth, Rumex cyprius also acts as a collagenase activity inhibitor. Collagen is also called collagen. A protein that forms the connective tissue of animal cells and is widely distributed in the body. It is believed to exist in multicellular animals. To date, at least 11 types of molecules have been discovered, and these differ in genes.

Collagen is the main component of the skeletal structure,
It has a platelet aggregation action and is also involved in thrombus formation. It has also been suggested that collagen is involved in cirrhosis and arteriosclerosis. Collagenase refers to an enzyme produced by animal tissue cells, inflammatory cells, tumor cells, etc., which decomposes type I, type II, and type III collagen.

The collagenase activity inhibitor means a protein which inhibits the activity of collagenase as described above. Abnormality of collagenase activity is observed in the tissue destruction and repair processes during pathological conditions. These pathologies include rheumatoid arthritis, periodontitis, corneal ulcers, and congenital epidermolysis bullosa. Collagenase inhibitors are thought to prevent or cure the deterioration of these pathological conditions by inhibiting the collagenase activity.

[0017]

EXAMPLE An example of an actual usage will be described below, but the present invention is not limited to this example. An example of producing the extract of Rumex cyprius used in the present invention is shown below.

(Production Example 1) To 10 g of Ruumex Cyprius leaf (dry product) was added 300 ml of ethanol, and the mixture was left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried.

(Production Example 2) Ruumex Cyprius leaf (dried product) was added to 10 g of 50% ethanol aqueous solution 300.
ml was added and left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried.

(Production Example 3) 10 g of Rumex cyprius leaf (dry product) was added with 300 ml of purified water and heated for 3 hours. This was allowed to cool, then filtered and freeze-dried.

(Example 1) Lotion Olive oil 0.5 Ethanol extract of Rumex cyprius of Production Example 1 0.5 Polyoxyethylene (20.EO) sorbitan monostearate 2.0 Polyoxyethylene (60.EO) Hardening Castor oil 2.0 Ethanol 10.0 1.0% sodium hyaluronate aqueous solution 5.0 Purified water 80.0

Example 2 Cream A Squalane 20.0 Olive Oil 2.0 Mink Oil 1.0 Jojoba Oil 5.0 Beeswax 5.0 Cetostearyl Alcohol 2.0 Glycerin Monostearate 1.0 Sorbitan Monostearate 2 0.0 Rumex Cyprius 50% ethanol extract of Production Example 1.0 1.0 B Purified water 47.9 Polyoxyethylene (20.EO) sorbitan monostearate 2.0 Polyoxyethylene (60.EO) hydrogenated castor oil 1. 0 Glycerin 5.0 1.0% sodium hyaluronate aqueous solution 5.0 Methyl paraoxybenzoate 0.1 A and B were weighed and heated to 70 ° C., and A was gradually added to B while stirring. , Stirring slowly, 30
Cooled to ° C.

Example 3 is a cream prepared by replacing the extract of Production Example 2 of Example 2 with the extract of Production Example 3.

(Tyrosinase activity inhibition test) (Test method) Mcllvaln buffer solution 0.9
ml, 1.66 mM Tyrosine solution 1.0 ml, 0.1 wt / v% aqueous solution of the above-mentioned production example (freeze-dried product) After removing the ethanol,
1.0 ml (prepared to 0.1 wt / v%) was placed in a screw vial and heated in a 37 ° C. constant temperature water bath for 5 minutes or more. Add 0.1 ml of tyrosinase solution (Sigma, mushroom-derived, 914 units / ml) to 37 ° C.
The temperature was kept in a constant temperature water bath, and after 10 minutes, the absorbance was measured at 475 nm. As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner. The final concentration of the sample in this test is 0.03
It becomes 3%. (Calculation formula) Tyrosinase activity inhibition rate (%) = {B- (A-
P)} / B × 100 However, A: Absorbance of sample specimen B: Absorbance of control P: Absorbance due to coloring of sample specimen (3-fold dilution) The results are shown in Table 1.

[0025]

[Table 1]

(Hyaluronidase activity inhibition test) (Test method) 0.4% sodium hyaluronate 0.1M
(PH 6.0) Weigh 6 g of phosphate buffer solution, and
After standing in a constant temperature water bath at ℃ for 5 minutes, 0.1 wt / v% aqueous solution of the above production example (freeze-dried product) (if it is difficult to dissolve, add ethanol and dissolve, then add purified water and evaporate 0.1wt / v% after removing
1.0 ml of a sample solution prepared so that the mixture becomes agitated and stirred, and 1 ml of 0.01% hyaluronidase (manufactured by Sigma, beef testicles, type I-S) 0.1 M (pH 6.0) phosphate buffer solution was added. Immediately after stirring, 6 ml was placed in an Ostwald viscometer in a constant temperature water bath at 37 ° C. The viscosity was measured after 1 minute, 5 minutes, 10 minutes, 20 minutes, and 40 minutes.
As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner. In this test, the final concentration of the sample is 0.0125%. The results are shown in Tables 2 and 3 as indexes with the viscosity after 1 minute being 100.

[0027]

[Table 2]

[0028]

[Table 3]

(Active oxygen suppression test) There are various methods for measuring the effect of suppressing active oxygen, but the following method was used this time. pH 7.8, 50 mM potassium phosphate buffer (containing 1.3 mM DETAPAC) 133 ml 40 unit / ml Catalase above potassium phosphate buffer 5 ml 2 mM Nitroblue tetrazolium above potassium phosphate buffer 5 ml 1.8 ml Xanthine above Potassium phosphate buffer 17 ml 160 ml Xanthine oxynase by adding 2.4 ml of the mixture of the above reagents and 0.3 ml of the sample (when the sample is water beforehand, the absorbance increases about 0.02 per minute when performing the experiment. (Prepared with the above-mentioned potassium phosphate buffer solution).
Immediately after adding 1 ml, the absorbance (560 nm) is measured. (Measurement is performed in two quantiles to confirm linearity) Calculation formula Inhibition rate = ((AB) / A) × 100 A: Change in absorbance per minute when the sample is water B: Sample Change in Absorbance Per Minute Several concentration steps were performed to search for a 50% active oxygen production inhibitory concentration. The preparation method of the sample is that the above production example (freeze-dried product) is dissolved in an aqueous solution (if it is difficult to dissolve, ethanol is added and then purified water is added, and then evaporated.
After removing ethanol, the concentration was adjusted to an appropriate concentration). The results are shown in Table 4.

[0030]

[Table 4]

(Antioxidant test) The following test solutions were prepared in 50 ml test tubes with a screw cap. Specimen 5 mg 2% ethanolic linoleic acid solution 10 ml 0.1 M, pH 7.0 phosphate buffer 10 ml purified water 5 ml This is left in a thermostat bath at 50 ° C while being shielded from light. The following measurements were performed before putting this in a constant temperature bath and at intervals of several days. Test solution 0.125 ml, 75% ethanol 12.125 ml, 30
% 0.13 ml of ammonium thiocyanate was added, stirred and left for 3 minutes, then 0.02N ferrous chloride 3.5% HCl
Add 0.125 ml of aqueous solution, stir, and leave it for 3 minutes. Wavelength 5
Absorbance was measured at 00 nm. The cell length is 10 mm, and the control cell has the test solution replaced with water. The results are shown in Tables 5 and 6.

[0032]

[Table 5]

[0033]

[Table 6]

(Antiplasmin test) (Test method) Plaminogen-removing fibrinogen type 2-0.6% aqueous solution 4 ml was put in a 9 cm Petri dish, and the pH was adjusted.
7.4 ml of 0.1 M phosphate buffer of 7.4 was added and stirred, 0.1 ml of thrombin (10 units / ml) was added dropwise, and the mixture was gently mixed and left for 30 minutes. The addition of thrombin changes the fibrinogen type to fibrin, forming a gel. 30 μl of a solution prepared by mixing 0.1 ml of the sample with 0.1 ml of the plasmin solution (10 units / ml) was placed on the gel of a Petri dish and left at 37 ° C. for 2 hours. Sample is 5mM3
A 3% dimethylsulfoxide solution was used. Then, the dissolved area of the fibrin gel was measured. 3 instead of specimen
The same experiment was carried out using a 3% dimethylsulfoxide aqueous solution, and the inhibition rate of plasmin activity was calculated by the following formula. The results are shown in Table 7.

[0035]

[Equation 1]

[Table 7]

When tranexamic acid and ε-aminocaproic acid were tested as controls, the 50% inhibitory concentrations were 30 mg / ml of tranexamic acid and 40 mg / ml of ε-aminocaproic acid.

(Collagenase Inhibition Test) (Test Method) Type I Collagenase Activity Measurement Kid YU-
16001 Experiments were performed using Cosmo Bio. That is, fluorescence labeled type I collagen (50
μg / 50 μl / tube), and reagents and samples were added as shown in Table 8 below. The neutralization solution is 0.1M tris (hydroxymethyl) aminomethane pH buffer solution with 0.1M Tris-HCl, pH 7.5 (0.4M NaCl, 0.0
1 M CaCl ₂ and NaN ₃ are included) and the enzyme reaction terminator is an O-phenanthrone (containing ethanol) solution.
Collagenase solution means collagenase (Amano 1
000 unit / mg) of 1 unit / mg of 2-fold diluted neutralizing solution.

[0038]

[Table 8]

The collagenase activity inhibition rate was calculated by the following formula.

[Equation 2]

Table 9 shows the measurement results of the collagenase activity inhibition rate.

[Table 9]

(Usage test) The faces of 6 females were divided into left and right sides, one as an example and the other as a comparative example every day.
I had them use it more than once, and after 3 months I conducted a questionnaire.
In Comparative Examples, various Rumex cyprius extracts produced in Production Examples were replaced with water. (Comparative Examples 1 and 2) Twelve people were divided into two groups, and experiments were conducted using the samples shown in Table 10 below.

[0042]

[Table 10]

The judgment criteria are as follows, and the total value of these scores is shown in Table 11 below. Example is much better 3 Example is much better 2 Example is slightly better 1 No difference 0 Comparative example is slightly better -1 Comparative example is much better -2 Comparative example Is much better -3

[0044]

[Table 11]

[0045]

EFFECTS OF THE INVENTION The solvent extract of Rumex cyprius of the present invention has a skin whitening effect, a hyaluronidase activity suppressing effect, an active oxygen suppressing effect, an antioxidant effect, an antiplasmin effect and a collagenase activity inhibiting effect, and is incorporated into cosmetics. It has an excellent whitening effect on the skin, prevents rough skin, and has a great effect on keeping the skin gloss and elasticity.

Continuation of the front page (51) Int.Cl. ⁶ Identification number Reference number within the agency FI technical display location // C12N 9/99 (72) Inventor Kenji Shimomura 3-16-32 Funae, Ise City, Mie Prefecture (72) Inventor Koichi Iida 56-1 Kurose-cho, Ise-shi, Mie (72) Inventor Yukihisa Yamabe 3-1-6 Kawasaki, Ise-shi, Mie

Claims (1)

[Claims] 1. A cosmetic comprising a solvent extract of Rumex cyprius.