JP2010241779A - Skin care preparation for external use for ameliorating rough skin - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a skin care preparation for external use having the effect of ameliorating rough skin, and capable of preventing inflammations stemming from sensitive skin, skin dryness and dry skin. <P>SOLUTION: The skin care preparation for external use is characterized in including, as active ingredient(s), one or more of the powder, extract, extracted fraction and/or saponin fraction of Aralia elata and its analogous plant(s). This skin care preparation for external use having the effect of ameliorating rough skin can inhibit apoptosis in keratinized cells and ameliorate sensitive skin, skin dryness and dry skin each accompanied by inflammation reactions. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention relates to an external preparation for skin which prevents and / or improves rough skin, inflammation, sensitive skin and eczema caused by increased apoptosis of cells constituting the skin.

  Apoptosis, also called programmed cell death, is an originally morphologically defined concept, a mode of cell death in contrast to cell necrosis (necrosis). As the induction mechanism of apoptosis, various mechanisms such as a pathway through binding of Fas molecule and Fas ligand (FasL) by cytotoxic T cells or NK cells, a pathway through paforin and granzyme are becoming clear. [Nagata S. , Cell, 88, 355-365 (1997); Ashkenazi A .; and Dixit V. M.M. , Science, 281, 1305-1308 (1998); , Annu. Rev. Genetics, 33, 29-55 (1999); Pinkoski M. et al. J. et al. and Green D. R. Curr. Opin. Hematol. 9, 43-49 (2002)].

  Apoptotic cells shrink and the nuclei aggregate and fragment. Fragmented nuclei form apoptotic bodies encased in cell membranes, which are processed by phagocytic cells. This process is controlled by a series of genes and is actively performed by consuming energy. Unlike necrosis, it has been considered to be an important mechanism for maintaining homeostasis of the cellular environment in vivo due to the fact that it does not cause inflammation in principle. Recently, however, it has been shown that a part of caspases responsible for apoptosis is involved in the onset and development of lesions including inflammation [Daemen M. et al. A. et al. , Clin. Invest. Miwa K., 104, 541-549 (1999); et al. , At. Mod. , 4, 1287, 761-767 (1998)].

  Therefore, an improvement effect is expected for certain inflammatory reactions by suppressing apoptosis. In fact, it has been reported that FasL neutralizing antibody has an excellent therapeutic effect on experimental inflammatory pulmonary fibrosis and inflammatory bowel disease model animals [Via C. et al. S. et al. , J .; Immunol. 157, 5387-5393 (1996); et al. , Int. Immunol. , 11, 925-931 (1999); Kuwano K. et al. et al. , J .; Clin. Invest. , 104, 13-19 (1999)], apoptosis inhibitors are expected to have excellent effects in the prevention or treatment of symptoms, pathological conditions, and tissue disorders in various inflammatory diseases.

  In skin, the expression of Fas molecules on keratinocytes is markedly induced by the action of IFN-γ produced by lymphocytes infiltrating the skin during acute and chronic inflammation, and apoptosis is caused by reaction with FasL expressed by lymphocytes. [Trautmann A. et al. et al. , J .; Clin. Invest. 106, 25-35 (2000); Takahashi H. et al. et al. , J .; Invest. Dermatol. , 105, 810-815 (1995); et al. , Int. J. et al. Cancer, 80, 564-572 (1999)]. In addition, keratinocytes are strongly bound to each other by a binding device called desmosome, causing the formation of sponge-like blisters due to apoptosis of keratinocytes, resulting in characteristic pathological changes called spongiosis and exhibiting eczema symptoms [Trautmann A. et al. , J .; Allergy Clin. Immunol. , 108, 839-846 (2001)].

  It is thought that such barrier injury of the epidermis due to apoptosis facilitates the entry of various stimulating substances from the outside into the living body, causes further inflammatory reactions, and causes symptom deterioration. In addition, damage to the epidermis promotes the turnover of keratinocytes, but in a chronic inflammatory state, the regularity of the turnover is lost, and an undifferentiated stratum corneum tends to be formed. On such undifferentiated keratinocytes, the production of water-soluble amino acids that are moisturizing is reduced and the skin's moisturizing ability is easily lost. [Fragrance Journal, vol. 10 (2002); Hachiro Tagami, Skin Medicine, Chuko Shinsho (1999)].

  Therefore, the suppression of Fas-mediated apoptosis of skin keratinocytes normalizes the turnover of keratinocytes, and prevents or improves skin abnormalities with various symptoms such as dry skin and sensitive skin as well as suppression of inflammatory symptoms. It seems to be connected. Examples of anti-apoptotic substances include substrate analogs such as Z-VAD-FMK that inhibits the caspase system in addition to FasL neutralizing antibodies, and various synthetic peptides are commercially available as research reagents. Since these are proteins or peptides, there are problems from the viewpoint of safety, that is, action and side effects, and the present situation is that they do not exhibit a safe action when administered to the human body.

  The object of the present invention is to normalize the metabolism of cells constituting the skin, that is, to normalize the balance between apoptosis and cell neoplasia, and to prevent or improve skin diseases, symptoms, pathological conditions and tissue disorders caused by increased apoptosis of cells constituting the skin It is to provide an external preparation for skin.

  In this invention, the said subject was solved by making the skin external preparation base contain 1 or more types selected from the powder or extract, etc. and / or the saponin fraction of a cypress and its related plants. The present invention will be described in detail below.

  The skin roughening external preparation for skin roughness according to the present invention is configured to contain one or more selected from powders or extracts or extract components and / or saponin fractions of cypress and related plants as described above.

  It is preferable that the saponin fraction used in the present invention is extracted from a crabs. What was concentrated and refine | purified from the extract can also be used.

    The herbal medicine can be pulverized or extracted by a conventional method. Extraction can be performed, for example, by drying and chopping the herbal medicine or by adding an extraction solvent in the form of a powder, followed by cooling or heating. As an extraction solvent, 1 type, or 2 or more types of mixed solvents, such as water, ethanol, 1, 3- butanediol, and isopropanol, can be used.

  The extract in the present invention means any of an extract, a diluted or concentrated solution of the extract, a dried product obtained by drying the extract, or an extract. Rough purification and purification of the saponin fraction from the above extract may be carried out by conventional methods (Nobutori Natori, Nobuo Ikekawa, Nobuaki Suzuki, Natural Organic Compound Experimental Method-Extraction and Separation of Bioactive Substances, 1977, Kodansha ), For example, a solid-phase extraction method using a synthetic resin carrier such as porous beads such as DIAION HP-20, or adsorption with an adsorbent such as Sephadex LH-20 (Sephadex LH-20), silica gel, alumina, etc. In addition, elution chromatography and other various chromatographies can be combined appropriately.

  As described above, the powder of the crabs, the extract, the crudely purified product, the purified product, and the components of the extract obtained as described above have an effect of improving the rough skin. It can be used as an active ingredient. The skin roughening external preparation of the present invention is considered to be highly safe because it does not show cytotoxicity in the anti-apoptotic effect test, and no skin irritation which is a problem in the use test of Examples is observed.

  The skin roughening external preparation for skin roughness of the present invention can be provided as a quasi-drug or a cosmetic without any problem. The blending amount is suitably about 10% by weight or less in consideration of the effective concentration in the external preparation and the stability of the external preparation. The form of the external preparation can take various forms such as lotion, emulsion, cream, ointment and the like. It can also be provided as a rough skin-improving skin cosmetic such as lotion, cosmetic liquid, or milky lotion.

  EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples. However, the scope of the present invention is not limited to these examples. “%” Means wt% unless otherwise specified.

Evaluation of anti-apoptotic activity of cypress extract or saponin fraction and chicksetsusaponin V against apoptosis of Jurkat cells induced via Fas / FasL pathway

Jurkat cells (derived from human leukemia T lymphoma) prepared to 4 × 10 ⁵ cells / mL were dispensed into a 96-well plate, and the cypress extract or saponin fraction or chixetsu saponin V (final) prepared by a conventional method was used. (Concentration: 12.5-50 μg / mL) was added and cultured for 1 hour, and then stimulated with 5 ng / mL FasL and further cultured for 24 hours. As controls, caspase family inhibitors [Z-VAD-FMK, Caspase Family Inhibitor (Fluoromethyl ketone), Medical & Biological Laboratories Co. Ltd .. ] Was added to 2 μM. Cell viability was determined by the Alamar Blue method [Page, B. et al. et al. , Int. J. et al. Oncol. 3, 473-476 (1993)], and the inhibition rate of apoptosis [[viability of cells to which extract or product and FasL were added) − (viability of cells to which FasL was added) / (untreated) Cell viability) − (viability of cells added with FasL)] × 100 was calculated and evaluated for anti-apoptotic activity. The results are shown in Table 1.

  Table 1 shows the anti-apoptotic activity of Tranoki extract or saponin fraction, Chiksetsu saponin V against Jurkat cell apoptosis induced through Fas / FasL pathway. Z-VAD-FMK in the table is a known peptide having an anti-apoptotic effect and was used as a positive control. From this study, it was clarified that the arabian extract or saponin fraction and chixetsu saponin V remarkably suppresses Fas molecule-mediated apoptosis of Jurkat cells. It was also revealed that saponins other than chixetsu saponin V are also active. In addition, no significant cytotoxicity was observed at each concentration of the extracted fraction.

Table 2 shows the prescription for skin roughening skin lotion.

  (5) and (6) are added to (9) in the table to swell, respectively, (1), (2), (4) and (7) are mixed and dissolved by heating to 80 ° C. After dissolution, Cool to 40 ° C., add (3), (8) and mix. In the table (8), a crab extract fraction was prepared by extracting 500 g of crabs with 5 L of 50% ethanol for 1 week at room temperature. Moreover, what mixed 50% ethanol instead of (8) in the table | surface was made into the comparative example.

  Subsequently, usage tests were conducted on the examples and comparative examples of the present invention. Since it is presumed that rough skin is improved when apoptosis is suppressed, the following test was performed. Panelists who feel rough skin are grouped into 25 groups, and each group is allowed to use the examples and comparative examples blindly on their faces. About rough skin, “Improved”, “No change”, “Slightly worse”, “ The four stages of “deterioration” and the amount of water were evaluated in four stages of “increased”, “no change”, “slightly reduced”, and “decreased”, and the number of panelists obtained for each evaluation is shown in Table 3 below.

  As shown above, compared to the comparative example with ethanol, the use of the examples of the present invention containing the extract of the arabay extract improves the rough skin in most panelists, and the water content increases remarkably in 16 cases. It was recognized that

The invention's effect

  As described above in detail, the skin roughness improving external preparation for skin roughness according to the present invention can suppress the induction of apoptosis due to inflammation in the skin, and can exert an effect on prevention of sensitive skin and skin roughness. In addition, the anti-apoptosis test does not show cytotoxicity, and the skin irritation that causes problems in the use test of the examples is not observed. It is an excellent external preparation for skin.

Claims (5)

Araliaceae (Araliaceae) Aralia elata, characterized in that it contains a powder or extract or extracted ingredient (Aralia elata), rough skin improving skin external agent. Araliaceae (Araliaceae) Aralia elata (Aralia elata) and analogs plant [luchuensis Aralia elata (Aralia ryukyuensis), Miyamaudo (Aralia glabra), Mallotus Aralia elata (Aralia bipinnata), Fuku phosphorus Aralia elata (Aralia elata f.variegata), Medara (Aralia elata f.subinermis), Kimontaranoki (Aralia elata f.aureovariegata), Oobaudo (Aralia cordata f.biternata), Karafutoudo (Aralia cordata var.sachalinensis), cytidine tow Aralia elata (Aralia ryukyuensis var.ine characterized in that it contains a powder or extracts or extracted components of mis)], rough skin recovering skin external agent. Araliaceae (Araliaceae) Aralia elata rough improving skin external agent comprising as an active ingredient powder or consisting of saponin fraction prepared from the extract composition (Aralia elata). Araliaceae (Araliaceae) Aralia elata (Aralia elata) or claim 2 roughening improving skin external preparation comprising as an active ingredient of the related plant powder or consisting of saponin fraction prepared from the extract composition.   Roughness improvement characterized by containing one or more kinds of powder, extract or extract fraction of taranoki, powder, extract or extract fraction of related plant according to claim 2 and saponin fraction Topical agent.