Composition for skin external application containing gallocatechin gallate for moisturizing effect on the skin

The present invention relates to a composition for external skin application having a skin-moisturizing effect, which comprises gallocatechin gallate as an active ingredient. More particularly, the composition for external skin application according to the present invention comprises gallocatechin gallate as an active ingredient to activate peroxisome proliferator activated receptor isoform alpha (PPAR-α), to stimulate expression of filaggrin and involucrin that are skin-moisturizing factors, and thus to provide excellent anti-drying and skin-moisturizing effects. More particularly, the composition for external skin application according to the present invention may further comprise theobromine and quercetin in addition to gallocatechin gallate to maximize such effects.

In general, the skin is divided into the epidermis, the dermis and the subcutaneous tissue when viewed from the exterior, and functions to protect the whole organs in the body from variations in temperature and humidity, ultraviolet rays, and other external physical and chemical environmental irritations. Particularly, the epidermis has an important role in preventing evaporation of moisture in the human body.

The epidermis is divided into the stratum corneum, the stratum granulosum, the stratum spino and the stratum basale. Additionally, keratinocytes present in the stratum corneum serve as bricks and intercellular lipids present between keratinocytes serve as mortar, thereby forming skin barriers (J. Invest. Dermatol. 80 (Suppl.) 44-49, 1983). Further, a high concentration of natural moisturizing factors (NMF) is present in keratinocytes of healthy humans so that the skin retains moisture. For example, amino acids, which are water soluble materials, are effectively bound to moisture, thereby inhibiting moisture from drying on the skin (J. Invest. Dermatol., 54, 24-31, 1970).

However, skin drying and roughening phenomena, caused by a drop in moisture content of the stratum corneum and including loose, dry and inanimate skin conditions, occur due to various causes. Such causes include artificial temperature control for cooling/warming an indoor space depending on variations in the living environment and pattern, diverse stresses generated from social activities and skin stresses caused by environmental pollution, frequent face-washing depending on makeup habits, and natural skin aging. Therefore, there has been an increasing need for a skin moisturizing agent.

According to the prior art, a humectant capable of absorbing moisture or an occlusive moisturizer capable of preventing moisture evaporation have been used as moisturizing agents so as to increase moisture retainment in the stratum corneum. Such humectants include glycerin, propylene glycol, 1.3-butylene glycol, polyethylene glycol, sorbitol, sodium 2-pyrrolidone-5-carboxylate, or the like. However, such humectants have a disadvantage in that they have a highly sticky and dense feel when applied on the skin. Additionally, as the occlusive moisturizers, lipids such as ceramides or essential fatty acids and lipid complexes have been used (J. Invest. Dermatol. (5), 731-740, 1994). However, such occlusive moisturizers have difficulty in maintaining stability of an emulsified formulation and are not amenable to production of transparent gel-like cosmetic products.

Meanwhile, peroxisome proliferator activated receptors (PPAR) are known nuclear hormone receptors having the three isoforms of α, β/δ and γ distributed over various tissues. Peroxisome proliferator activated receptor isoform α (also referred to as ‘PPAR-α’) has been identified first based on the mechanism of controlling genes encoding fatty acid oxidase by the reaction with a peroxisome proliferator factor such as a fibric acid derivative (Issemann and Green, Nature, 1990, 347: 645-650). Additionally, it is disclosed that fatty acids play an important role in tissues expressed by PPAR-α (Leone et al., Proc. Natl. Acad. Sci. USA, 1999, 96: 7473-7478). Lipid activators of PPAR-α, such as linoleic acid, etc., are known to those skilled in the art. It is demonstrated that such activators enhance formation of an epithelial barrier in vitro (Hanley et. al., J. Clin. Inv., 1977, 100: 705-712). However, in the relevant art, there is no disclosure of a skin cosmetic agent utilizing a mechanism of controlling PPAR activities other than a cosmetic composition (WO01/008653) for preventing and treating skin aging.

Accordingly, the present invention has been made to solve the above-mentioned problems occurring in the prior art. The inventors of the present invention have many studies to search for the components that shows a skin-moisturizing effect by controlling activity of the peroxisome proliferator activated receptor isoform alpha (PPAR-α), among various factors affecting the skin in terms of skin moisturization and skin protection. Then, we have found that when a composition for external skin application comprises gallocatechin gallate contained in green tea leaves, it activates the peroxisome proliferator activated receptor isoform alpha (PPAR-α) and stimulates expression of skin moisturizing factors such as filaggrin and involucrin, and thus provides excellent skin moisturizing and anti-drying effects. Particularly, we have also found that when the composition further comprises theobromine and quercetin, besides gallocatechin galate, at an optimized ratio, the above effects can be maximized. The present invention is based on these findings.

Therefore, it is an object of the present invention to provide a composition for external skin application having a skin-moisturizing effect, which comprises gallocatechin gallate as an active ingredient.

It is another object of the present invention to provide a composition for external skin application having a skin-moisturizing effect, which further comprises theobromine and quercetin at an optimized ratio in addition to the above composition comprising gallocatechin gallate.

According to an aspect of the present invention, the composition for external skin application having a skin-moisturizing effect comprises gallocatechin gallate as an active ingredient. According to another aspect of the present invention, the composition further comprises theobromine and quercetin at an optimized ratio.

DESCRIPTION OF DRAWINGS

Further objects and advantages of the invention can be more fully understood from the following detailed description taken in conjunction with the accompanying drawings, in which:

FIG. 1 is a graph illustrating how to select an optimal concentration by a response optimizer;

FIG. 2 is a graph illustration how to select an optimal concentration by using an overlaid contour plot;

FIG. 3 is a view showing expression of filaggrin via RT-PCR analysis; and

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