Drug – bio-affecting and body treating compositions – Extract – body fluid – or cellular material of undetermined... – Nervous system
Patent
1997-03-04
1998-06-02
Weber, Jon P.
Drug, bio-affecting and body treating compositions
Extract, body fluid, or cellular material of undetermined...
Nervous system
514143, 560205, A61K 3530, A01N 5710, C07C 6952
Patent
active
057595852
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION OF THE INVENTION
The present invention relates to the field of therapeutic chemistry and more particularly to the one of phosphoglycerids.
More precisely, it consists in pharmaceutical compositions notably intended for neurodegenerative diseases treatment, based on phosphoglyceroethers and phosphoglyceroesters.
STATE OF THE ART
Specifically, it consists in pharmaceutical compositions containing phosphoglyceroethers or plasmalogens, combined or not with phospholipids, admixed or diluted into inert, not toxic carriers, suitable for digestive or parenteral administration.
Phospholipids are defined as esters constituted of a glycerol molecule esterified in position 1 and 2 with saturated or unsaturated fatty acids chains, and, in position 3 with a phosphoric acid derivative. Most of natural phospholipids contains saturated fatty acids chains such as stearic acid or palmitic acid. Moreover, the phosphoric group is bound to an aminoalkyl chain to form the phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine and phosphatidylinositol. These compounds which form the lecithins class are principally of alimentary value.
The phospholipids, according to this invention, are characterized in that the glycerol moiety is esterified and/or etherified by non saturated fatty chains.
Previous tests have shown the relevance of phospholipids containing polyunsaturated fatty acids as an esterifying group.
Their function in nutrition and dietetic has already been the subject to several patent applications depending on whether they origin from cerebral tissues or whether they come from the yolk of hens egg extracts the food of which has been modified.
In fact, these phospholipids are carriers of fatty acids chains with a high number of carbons and they have a high unsaturation degree of the n-3 series, especially the acid in C.sub.22 :6.
The superiority in nutritional function of the cerebral phospholipids in comparison with other sources of n-3 fatty acids has been more particularly demonstrated (J. M. BOURRE J.Neur.Chem. 60 (1993) 2018-2028).
SUMMARY OF THE INVENTION
The present invention thus relates to pharmaceutical compositions in which the phosphoglycerids are, partially or predominantly, substituted by plasmalogens the formula of which is: ##STR1## wherein R is an alkyl radical and, preferably, an alkenyl radical having one or several double bonds up to 5 double bonds, and from 10 to 24 carbon atoms R' is a linear or branched, fatty, alkenyl of 10 to 24 carbon atoms and from 1 to 6 double bonds and the nitrogen atom is inserted into a secondary, tertiary or quaternary, linear or cyclic structure.
The Merck Index (1989) page 1194, defines plasmalogens as aldehydogenic lipids extracted from the animal kingdom and nothing is known about their therapeutic usefulness.
Their nomenclature is not already entirely determined and it is spoken as ethanolamine-phosphatidal or plasmalogen-ethanolamine, or plasmalogen-choline to define more precisely the nitrogenous structure carried by the phosphoric group.
Phosphoglycero-ethers of the invention seem to have a high affinity for polyunsaturated fatty acids with a long chain of the n-3 series and it can be deduced therefrom a great physiological significance for eicosanoids. In this case, one characteristic of plasmalogen is that it contains twice more from a polyunsaturated fatty acid (DHA i.e. C.sub.22 : 6 n-3) than other phospholipids.
Plasmalogens molecules are essentially present on the membrane and seem endowed with remarkable membrane exchange qualities. So, they would have a greatest metabolic activity at the level of the membrane reconstruction.
Moreover, it has been shown that cultured mutant cells which do not synthetize plasmalogen are very sensitive to agents generating free radicals (O. MORAND J.Biol.Chem. 263 (1988) 11.797). This leads to suppose a vitamin E-like protective effect of the plasmalogen with a role of anti-oxidizing in the oxidative stresses (B. ENGELMANN Biochem.Biophys.Res.Commun. 204 (1994) 1235).
The relevance of phosphoglyce
REFERENCES:
patent: 4613621 (1986-09-01), Horrmann
Martinez et al. "Lipids of the developing human retina: I. Total faty acids, plasmalogens and fatty acid composition of ethanolamine and choline phosphoglycerides", J. Neurosci. Res. (1988) 20: 484-490.
Markesbery et al. "Brain trace element concentrations in aging", Neurobiol. Aging (1984) 5: 19-28.
Gurr et al. Lipid Biochemistry: an Introduction, 3rd edition (1980) (Chapman and Hall: London), pp. 4, 5 and 25.
Mitani et al. "Aluminum deficiency in central nervous system (CNS) tissue with a mineral deficiency", Biomed. Res. Trace Elem. (1990) 1(2):149-50 (abstract only).
Hanley Susan
S.AR.L. Institut d'Hygiene et Dietetique
Weber Jon P.
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