Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1996-09-18
1998-05-05
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
424 7803, 424 7806, 424 401, 514828, 514887, 536 41, A61K 748
Patent
active
057475385
DESCRIPTION:
BRIEF SUMMARY
This application is a 37T of PCT/FR95/00326 published Mar. 17, 1995.
The invention relates to the use of ginsenoside R.sub.0 and plant extracts in which it is present for the preparation of cosmetic or pharmaceutical compositions, especially dermatological compositions, for stimulating the synthesis of collagen, particularly collagen I and collagen III. It further relates to fibroblast culture media containing ginsenoside R.sub.0 or plant extracts in which it is present.
The Panax family is known by its numerous varieties, the best known of which are as follows: attributes,
Panax ginseng seems to be among the most saponin-rich and the most effective.
Panax originate essentially from three countries:
The varieties cultivated in these different zones can be slightly different and are exposed to different geoclimatic conditions.
Nevertheless, it is found for example that the best quality of ginseng comes from China and then from Japan.
A ginseng tuber reaches maturity in 4 to 6 years. The optimal quality is obtained with 6-year-old tubers.
Very different saponin contents are found in the different parts of the plant. The root part is the most frequently used and generally the most active.
The highest saponin content is observed in the end of the root (ninjin in Japanese) and in the hairy roots (keninjin in Japanese).
The saponins most frequently encountered in the plants of the Panax family are of the damaran type. However, among the Panax saponins, there is one particular saponin, ginsenoside R.sub.0 or Chikusetsusaponin V, which has an oleanan structure of the following formula: ##STR1## in which: the substituent R.sup.1 in the 3-position consists of two sugars linked together, namely a beta-D-glucuronopyranoside and a beta-D-glucopyranosyl, represented symbolically by GIcA.sup.2 Glc, and the substituent R.sup.2 in the 28-position is a beta-D-glucopyranosyl, represented symbolically by Glc.
There is a high proportion of this ginsenoside in Panax japonicus (Japanese) and Chinese P. japonicus, P. japonicus var. mayor and P. japonicus var. angustifolius, as is apparent from the following literature reference:
In Japan, P. japonicus is also known under the name Chikusetsu Ninjin. The structure of Chikusetsusaponin V was described in 1971 by:
KONDO N., MARUMOTO Y., SHOJI J., Studies on the constituents of Panacis Japonici Rhizoma. IV The structure of chikusetsusaponin V. Chem. Pharm. Bull. (1971) 19 (6), 1103-1107.
This natural molecule can be extracted in particular by the process described by J. SHOJI in Advances in Chinese Medicinal Material Research 1985, p. 455 et seq.
Different uses, in particular in the medical field, of ginsenosides and particularly ginsenoside R.sub.0 have been described in the literature; thus: R.sub.0, is described by Li, Jingbo et al. in Baiqiien Yike Daxue Xuebao 1992, 18(1), 24-26, ginsenoside Rb on the aortic endothelium is described by Liao, Duanfang et al. in Hunan Yike Daxue Huebao 1992, 17(1), 13-15, treatment of hepatitis, an antidiabetic, as a platelet aggregation inhibitor,
Different documents also describe the use of Panax japonicus extracts in the cosmetic field. The following may be cited in this connection: promoting hair growth, extract as a hair tonic, containing an extract of Panax japonicus roots in combination with mucopolysaccharides.
It has now been discovered that ginsenoside R.sub.0 and plant extracts in which it is present have a surprising stimulating activity on the synthesis of collagen, particularly collagens of types I and III, hereafter abbreviated respectively to "collagen I" and "collagen III", which makes them particularly useful for combating the effects of skin ageing and for firming the skin or improving healing.
Changes in the appearance and especially the mechanical properties of the skin are in fact essentially due to changes in the components of the dermis.
Now, type I collagen represents 80 to 90% of the total skin collagen, the remainder, i.e. about 10 to 15% of the total skin collagen, consisting mainly of type III collagen. Type I and type
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patent: 5401502 (1995-03-01), Wunderlich
patent: 5564207 (1996-10-01), Kashibuchi
"Recent Advances in Ginseng Research in China", Liu Cx et al., Feb. 1992, vol. 36, No. 1, J. Ethnopharmacol, pp. 27-38.
"Dermocosmetic Activity of Ginsenosides. Note II: Instrumental Evaluation of Cutaneous Hydration and Elasticity", A. Gezzi et al., 1986, vol. 57, Fitoterapia, pp. 15-28.
"Dermocosmetic Activity of Ginsenosides. Note III: Long-Term Evaluation of the Moisturizing and Tonifying Effect on the Face Skin", S.B. Curri et al., 1986, vol. 57, Fitoterapia, pp. 217-222.
"Effect of Panax Ginseng on the Production o fGlycosaminoglycans in Cultured Human Skin Fibroblast", H. Tanaka et al., 1991, vol. 115, No. 22, Chemical Abstracts, p. 464, col. 2.
Bonte Frederic
Chaudagne Catherine
Dumas Marc
Meybeck Alain
Faulkner D.
L.V.M.H. Recherche
Page Thurman K.
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