Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1989-12-11
1992-11-17
Rollins, John W.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
424450, 514 78, 514844, A61K 3578, A61K 7222, A61K 31685
Patent
active
051641828
DESCRIPTION:
BRIEF SUMMARY
The present invention relates essentially to a composition based on hydrated lipidic lamellar phases or on liposomes containing an extract of mulberry, preferably Morus Alba, and to a pharmaceutical composition, especially a dermatological composition, with skin-lightening or antiinflammatory activity, or a cosmetic composition in which it is incorporated. The extract preferred according to the invention is obtained from the aerial or underground parts of the mulberry, preferably Morus Alba L. or Morus Rubra, especially the leaves, the ends of the stems and the bark of the shoots or roots.
It is known that the mulberry grows naturally everywhere in the mountains and fields. It is a plant which has long been cultivated for sericulture. Parts of the mulberry, in particular the bark of its roots or shoots, or extracts of this bark, also called "sohakuhi", have already been in use for a very long time, especially in Chinese medicine.
Therapeutic virtues, especially antiphlogistic, diuretic and febrifugal properties, are attributed to the dried bark of mulberry shoots or roots, or to extracts thereof, as a remedy for pain, in the treatment of bronchitis, asthma etc.
The presence of bleaching compounds has relatively recently been discovered in the extract of the bark of mulberry shoots or roots, or sohakuhi, these compounds having been incorporated into cosmetic compositions in order to inhibit the activity of tyrosinase--which is an enzyme responsible for the coloration of the skin--thereby producing a skin-lightening effect (see C.A. Essential Oils, Cosmetics, volume 88, 1978, page 227, abstract 88:65874z, or Japanese patent document A-50-135-236).
For pharmacological studies, see the document Japan Journal of Pharmacology, 1976, 26 (4), 461-9, or C.A., volume 85, 1976, page 48, abstract 85:137465e. An application of mulberry extract as an antidiabetic is described in French patent document A-2 336 941.
Furthermore, numerous substances have already been isolated from the extract of the bark of mulberry shoots or roots, the vast majority of which are active principles. They are generally flavones, flavone derivatives and, in particular, kuwanones.
The first document relates to the isolation of a white crystalline powder (C.A , 45 (1951), abstract 9513g).
The isolation of a yellowish white powder is described in C.A., 57 (1962), abstract 3970g.
The isolation of 4 flavones was first described in Tetrahedron Letters no. 14, pages 1715-1719, 1968, with a corresponding abstract in Chemical Abstracts, volume 69, 1968, page 3340, abstract 35869s. Other flavones, such as rubraflavone A, B, C or D, are described in Indian Journal of Chemistry, volume 12, May 2, 1974, pages 431-436, with an abstract in C.A., volume 82, 1975, page 557, abstract 57520s. -Tocopherol has also been isolated from the bark of mulberry roots (C.A., volume 82, 1975, page 213, abstract 70272a). Other flavones, such as mulberranol, and a phenol, such as alboctalol, have also been isolated (C.A., 86 (1977), page 551, abstract 86:139896r). Subsequently, other flavones, such as morusine and cyclomorusine, have been isolated and described in C.A., volume 87, 1977, page 566, abstract 87:167917n.
The isolation of kuwanone E is also described in C.A , volume 89, 1978. abstract 89:211925f.
The isolation of kuwanone A, B and C and oxydihydromorusine is also described in C.A., volume 89, 1978, page 429, abstract 89:103271c.
The synthesis of tetrahydrokuwanone C tetramethyl ether has also been described in Heterocycles, volume 9, no. 10, 1978, pages 1355-1366.
A more detailed description of the isolation of kuwanone E is also described in Heterocycles, volume 9, no. 9, 1978.
The isolation of phenolic constituents is described in C.A., volume 90, 1979, abstract 90:83661y. The structure of moracenine D, constituting a particular flavone, is described as having a hypotensive activity in Heterocycles, volume 16, no. 6, 1981, and also in C.A., volume 94, 1981, abstract 94:117759m, where its extraction process is also described.
The isolation of mulberrofuran B is
REFERENCES:
patent: 3856934 (1974-12-01), Kligman
Dumas Marc
Meybeck Alain
Cave Bryan
LVMH Recherche
Rollins John W.
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