Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Reexamination Certificate
2000-09-29
2003-04-08
Seidel, Marianne C. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
C514S114000
Reexamination Certificate
active
06544966
ABSTRACT:
TECHNICAL FIELD
This invention relates to agents for promoting the production of laminin 5 in epidermic cells and skin potentiating compositions useful in the fields of cosmetics and dermatology. More particularly, this invention relates to the use of specific lysophospholipids and soybean-derived preparations for the purpose of potentiating skin functions through the medium of the promotion of laminin 5 production in epidermic cells.
BACKGROUND ART
In the fields of cosmetics and dermatology, a wide variety of means have been proposed and tried to mitigate or cure the damage of the skin due to the influence of an external environment (e.g., exposure to sunlight) and aging. For example, main skin changes caused by aging include wrinkle formation, hardening and reduced elasticity.
In connection with the causes of such changes, chief interest is directed not to the epidermis of the skin, but rather to the functions of collagen fibers and elastic fibers consisting of collagen and glycosaminoglycans and present in the dermis forming the substratum of the epidermis. As means for preventing or correcting such changes, the use of a hydroxycarboxylic acid (e.g., Japanese Patent No. 2,533,339) and the use of a lysophospholipid [Japanese Patent Laid-Open No. 67621/'96 or Journal of Japan Oil Chemists' Society, Vol. 46, No. 9 (1997), pp. 13-19] have been proposed. In the former patent, it is suggested that the stratum corneum and wrinkles can be exterminated by preventing a loss of collagen fibers. On the other hand, it is suggested in the latter patent that lysophospholipids enhance the ability of human fibroblasts to produce a glycosaminoglycan (specifically, hyaluronic acid) and hence exhibit a skin beautifying effect. It is also suggested that lysophospholipids exert little influence on the synthesis of collagenous protein in skin fibroblasts (see the aforementioned Journal of Japan Oil Chemists' Society).
In the year 1991, laminin 5 was discovered by Dr. Burgeson (Rousselle et al., J. Cell Biol., 114, 567, 1991). Subsequently, the presence of an autoimmune disease to laminin 5 (Fine et al., J. Am. Acad. Dermatol., 24, 119, 1991) and a serious disease caused by the genetic deficiency of laminin 5 (Aberdam et al., Nat. Genet., 6, 299, 1994) was discovered. In this disease, the formation of blisters was observed at the dermal-epidermal junction, revealing that laminin 5 is an indispensable component for the adhesion of them. It is known that compounds of the laminin family are synthesized in various types of cells. Among them, laminin 5 is a principal component of the structure (called the basement membrane) located at the dermal-epidermal junction, and composed of various glycoproteins and proteoglycans. Moreover, laminin 5 has an activity for promoting the adhesion of epidermic cells and thereby functions to bind epidermic cells directly to the basement membrane (Rousselle et al., J. Cell Biol., 114, 567, 1991). Furthermore, it is also known that the adhesion of epithelial cells to the basement membrane components is important in maintaining their cellular function (Schmidhauser et al., Proc. Natn. Acad. U.S.A., 87, 9, 118, 1990). Furthermore, in the skin of old persons, duplication of the basement membrane (Lavker et al., J. Invest. Dermatol., 73, 59, 1979) and a thickening of the basement membrane and a decrease of IV type collage constituting it (Vazquez, Maturitas, 25, 209, 1996) have been reported. Thus, there seems to be a possibility that structural changes of the basement membrane may be responsible for hypofunction of the skin in old persons.
As to Japanese Patent Laid-Open No. 67621/'96 and Journal of Japan Oil Chemists' Society, Vol. 46, No. 9 (1997), pp. 13-19, the latter more specifically explains the contents of the former with the aid of additional experimental data. According to the latter (i.e., the aforementioned Journal of Japan Oil Chemists' Society), it is suggested that, among the lysophospholipids represented by the formula
the compound in which R is a C
12
saturated fatty acid residue promotes the above-described production of hyaluronic acid, but the compounds in which R is a C
14
or higher saturated fatty acid residue inhibits its production strongly.
DISCLOSURE OF THE INVENTION
On the basis of the above-described findings, the present inventors have searched for substances capable of improving the function of the skin on the assumption that the firm binding of epidermic basal cells to the basement membrane is essential for the manifestation of normal skin functions and that it is more important to promote the production of laminin 5 in the corium and the like, rather than the production of collagen and hyaluronic acid.
As a result, the present inventors have now found that, in contrast to the aforementioned Journal of Japan Oil Chemists' Society suggesting that the compounds of the above formula in which R is a C
14
or higher saturated fatty acid residue strongly inhibits the production of hyaluronic acid in human skin fibroblasts, the compounds of the above formula in which R is a C
14-22
fatty acid residue optionally having up to six unsaturated double bonds, and soybean-derived preparations that are likely to contain such compounds or their precursors, are more effective in promoting the above-described production of laminin 5 and thereby potentiating the skin.
Accordingly, the present invention relates to a composition for promoting the production of laminin 5 in epidermic cells which contains a compound of the following formula (I) or a mixture of two or more such compounds, as an active ingredient.
wherein R is a C
14-22
fatty acid residue optionally having up to six unsaturated double bonds, A is a hydrogen atom or a —CH
2
CH
2
N
+
(CH
3
)
3
group, and M is a hydrogen atom or an alkali metal atom, but is a hydrogen atom when A is a —CH
2
CH
2
N
+
(CH
3
)
3
group.
In other embodiments, the present invention relates to a method for promoting the production of laminin 5 in epidermic cells by administering the composition to the skin of a mammal, and the use of a compound of the following formula (I) as an active ingredient of a composition for promoting the production of laminin 5.
In further embodiments, the present invention also relates to a composition for promoting the production of laminin 5 which contains a soybean-derived preparation that is likely to contain a compound of the above formula (I) or its precursor, as an active ingredient, a method for promoting the production of laminin 5 in epidermic cells by administering the composition to the skin of a mammal, and the use of the soybean-derived preparation as an active ingredient of a composition for promoting the production of laminin 5.
DETAILED DESCRIPTION OF THE INVENTION
According to the present invention, the compounds of the above formula (I) wherein R is a C
14-22
fatty acid residue, which may strongly inhibit the production of hyaluronic acid in human skin fibroblasts as suggested in the aforementioned Journal of Japan Oil Chemists' Society, and soybean-derived preparations that are likely to contain such compounds, can be effectively used especially for the purpose of promoting the production of laminin 5 and/or potentiating the skin through the medium of such action.
The mammals in which it is contemplated to promote the production of laminin 5 and/or potentiate the skin through the medium of such action according to the present invention include, but are not limited to, human beings, pet animals (e.g., dogs, cats, rats and guinea pigs) and domestic animals (e.g., cattle, pigs and sheep).
The compounds of the above formula (I), which are used in the present invention, are compounds known generically as lysophospholipids. These compounds may be directly or indirectly obtained from a wide variety of biological sources, but may also be chemically synthesized.
R in the above formula (I) is a radical selected from among C
14-22
fatty acid residues (acyl groups). Specifically, these acyl groups include residues derived
Amano Satoshi
Nishiyama Toshio
Kim Vickie
Seidel Marianne C.
Shiseido Company Ltd.
Wenderoth , Lind & Ponack, L.L.P.
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