Biologically active substances, their obtainment from human case

Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Reduced antigenicity – reduced ability to bind complement – or...

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260112R, 2601125R, 435 69, A61K 3700, C07G 700, C07C10352, C12P 2106

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active

044629907

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to biologically active substances obtained by fractionating enzymatic hydrolysates of the human casein and the compositions containing these substances.
The use of casein derivatives in biological compositions has already been proposed. In this respect, the following patents may be cited:
French Pat. No. 1,461,423 which relates to a biological composition for treating human skin; this composition comprises, either in the acid form or in the salt form, the chemical combination obtained by the association of the carbonyl group derived from the carboxyl group of palmitic acid with the aminated, imidazolic, phenolic and hydroxylated functions of the fractions of the chemically- or enzymatically-hydrolysed caseins.
French Pat. No. 1,466,141 which relates to biological substances for preparing detergent compositions for corporal use. These detergent compositions are characterized by the presence of acylated amino-acids or acylates peptides, or the mixture of both. Among the suitable acylated peptides are mentioned in particular caseinic acids substituted by a fatty acid residue.
U.S. Pat. No. 3,558,770 relating to wound treating compositions which contain a casein modified by the action of an enzyme.
French Pat. No. 1,411,478 which relates to a composition for protecting the skin against the aggressivity of solvents and various hydrophobic substances. This composition comprises a gelling substance of animal origin (for example casein) or of vegetable origin or of purely chemical origin, a partial or total hydrolysate of animal or vegetable proteins, a substance having a surface active character and a small amount of a chemical detergent.
There may also be mentioned as documents illustrating the state of the art, French Pat. Nos. 1,518,665 and 7,810,857.
It will be observed that all the compositions described in the aforementioned patents are essentially compositions for topical use, in particular for cosmetic purposes or for hygiene of the skin in which are present derivatives of casein obtained for example by enzymatic hydrolysis, said derivatives being coupled with lipidic fractions by chemical synthesis. This lipidic coupling imparts the desired topical activity to the casein derivatives. Nothing indicates that these derivatives come from human casein and that the fractionation of these derivatives, independently of any coupling with a lipidic fraction, would result in substances having an immunological activity, i.e. substances whose field of application and mode of administration are totally different from those described in the aforementioned prior art.
The presently claimed invention permits the obtainment, by the fractionation of human casein which has been subjected to the action of a proteolytic enzyme, of biologically active substances which are immunological agents stimulating in particular the formation of antibodies.
The human casein, which is a complex of proteins (.alpha..sub.5, .beta., .kappa., . . . ), is present essentially in maternal milk. Under the action of a proteolytic enzyme, the casein may produce after fractionation biologically active substances.
According to the present invention, the new substances are obtained by the treatment, with at least one proteolytic enzyme, of human casein which was delipidated and rendered soluble, followed by the fractionation of the hydrosoluble products, as a function of their mean molecular weight, by filtration on a suitable support.
The new substances according to the invention has a mean molecular weight of between 1000 and 5500. Of most particular interest are the substances according to the invention whose mean molecular weight is in the neighbourhood of 1200.+-.200; however, the substances whose mean molecular weight is in the neighbourhood of 2500 or 5500 also have interesting properties.
As a proteolytic enzyme there is advantageously employed in the process of the invention, trypsin, chymotrypsin, or some other analogous enzyme, or mixtures thereof, the trypsin being preferred.
As a suitable support, there may be

REFERENCES:
patent: 1631887 (1927-06-01), Posternak
patent: 1658289 (1928-02-01), Heidlberg
patent: 3186918 (1965-06-01), Salzberg et al.
patent: 3323929 (1967-06-01), Salzburg et al.
patent: 3558770 (1971-01-01), Gordon et al.
patent: 4358465 (1982-11-01), Brule et al.
patent: 4361587 (1982-11-01), Brule et al.
Biol. Abstr. 74, p. 64855.
Journal of Dairy Science, 54, No. 7, pp. 987-993, (1970).

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