Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from roseaceae
Reexamination Certificate
2001-05-04
2003-01-14
Tate, Christopher R. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from roseaceae
C424S777000
Reexamination Certificate
active
06506421
ABSTRACT:
The present invention relates to a process for the extraction of an active principle from teguments of apple and the active principle obtained. This active principle, in a suitable composition also claimed, particularly for cosmetological applications, permits counteracting the effects of oxidative stress of the skin, which is to say against cutaneous aging of the skin.
It is known that free radicals of oxygen give rise to pathologies, more particularly at the cutaneous level, still more particularly during aging. Such free radicals can arise from different endogenous actions (activation of the arachidonic acid metabolism, phagocytosic activation or accumulation of reduced metabolites), or exogenous (radiation, UV radiation, air pollution or certain smoke, particularly of cigarettes).
As a function of the magnitude of the oxidative stress, there can be a suitable defense by liberation of anti-oxidant enzymes in a quantity sufficient to compensate the actions of the generated free radicals.
These free radicals are neutralized in the cells thanks to chemical or enzymatic means, particularly anti-oxidant systems which permit them to protect themselves and to be regulated against harmful effects of these radicals.
Nevertheless, beyond a certain threshold, the anti-oxidant systems are no longer sufficient and are submerged by the radical flow leading to irreversible cellular damage. It is also known that age plays a large role and that the anti-oxidant systems are less and less effective to guard against free radicals produced in large quantity.
The damage to the cell occasioned by uncontrolled oxidative stress is essentially of three types:
1/ OXIDATION OF THE CELLULAR PROTEINS
This oxidation is associated with a parallel inactivation of the enzymatic system, leading to proteic fragmentation. The proteic modifications are generally initiated by OH radicals and the oxidation processes take place by intervention of the O
2
and O
2
−
radicals.
Such an oxidation takes place according to three mechanisms:
oxidation by the free radicals of the side chains of amino acids. More particularly the aromatic amino acids are oxidized into carbonyl derivatives. Furthermore, the reactions such as glycation or peroxidation take part in the oxidation of the proteins.
rupture of the peptide links which leads to fragmentation of the proteins and to the formation of inactive peptide segments.
formation of covalent cross bonds between proteins, under the influence of free OH radicals, promoted by disulfide or tyrosine bridges. These damaged proteins thus modified in their structure as in their function, are inactivated.
2/ DNA LESIONS OF THE CELL NUCLEI
Helical DNA chains are permanently endangered as to their integrity by endogenous free radicals, chemical agents, and different UV radiations.
Such lesions prevent the good functioning of the cells and can lead to genetic mutations.
There exists a system of repair of damaged DNA, particularly by excision, but the risks of genetic mutation remain if the lesion is not recognized or if its repair is not complete.
It is also necessary to protect the DNA molecules and to limit the UV induced mutations.
3/ MEMBRANE PEROXIDATION OF THE CELL
The membrane of the cell is less protected and remains the privileged target of free radicals, which lead to peroxidation of the polyunsaturated fatty acids of the phospholipidic membranes. There is thus the formation of cytotoxic peroxides which lead to membrane permeability and the death of the cell.
These three actions lead to major damages that are intense, targeted and above all irreversible.
Also, numerous natural or synthetic anti-oxidants are used to attempt to mitigate the actions of the free radicals.
On the other hand, these anti-oxidants each have one or more specific activities but against a well-defined group of free radicals or acting through targeted mechanisms on certain oxidated sequences such that it is difficult to act simultaneously on all of the effects of oxidative stress.
Thus, an anti-oxidant which inhibits lipidic peroxidation has no action on oxidation of the proteins or DNA lesions.
This is one of the principal interests of the active principle according to the present invention, which permits acting simultaneously against these three factors and hence permits acting against cutaneous aging.
The present invention covers a process for the extraction of this active principle.
To this end, the extraction process of an active principle according to the invention, for taking action against the consequences of oxidative stress permitting counteracting cutaneous aging, is characterized in that it comprises the following steps:
reduction to fine powder of dried apple tegument,
solubilization of this powder with a minimum of 8% volume of powder, in an aqueous solution,
conjoint enzymatic hydrolysis of the sugars and proteins,
heating, permitting total inactivation of the enzymes, and
sterilizing filtration to retain the microorganisms, yeasts, and molds as well as the total mesophilic flora.
The obtained solution can be concentrated lyophilized or atomized.
The invention also covers the active principle obtained by this process and at least one cosmetic composition to guard simultaneously against cellular protein oxidation, against mutations induced by UV radiation and against membrane peroxidation of the cells of the skin, this composition comprising this active principle associated in an suitable galenic form.
The invention also covers a process to combat cutaneous aging, which consists in applying preventatively to the skin such a cosmetic composition.
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Kootstra, A. Plant Molecular Biol. 1994. vol. 26, pp. 771-774.*
Database MEDLINE “en ligne” retrieved from STN database accession No. 97141165, XP002154645-Phytochem. vol. 43, No. 1, 1996-Abstract.
Societe Industrielle Limousine d'Application Biologique (Si
Tate Christopher R.
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