Lipids containing omega-3 and omega-6 fatty acids

Abstract

A lipid preparation including a glycerophospholipid or salt, conjugate and derivatives thereof, particularly phosphatidylserine (PS), phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidyl-inositol (PI), phosphatidylglycerol (PG) and phosphatidic acid (PA), and poly-unsaturated fatty acid (PUFA) acyl groups, particularly long-chain poly-unsaturated fatty acid (LC-PUFA) acyl groups such as omega-3 and/or omega-6 acyl groups, wherein said PUFA is covalently bound to said glycerophospholipid. The preparation possesses an improved bioactivity, and is useful in the treatment of various cognitive and mental conditions and disorders and for maintenance of normal functions of brain-related systems and processes.

1 . A lipid preparation, wherein said lipid is selected from the group consisting of a glycerophospholid and salts, conjugates and derivatives and thereof and any mixture thereof, and poly-unsaturated fatty acid (PUFA) acyl groups, particularly long-chain poly-unsaturated fatty acid (LC-PUFA) acyl groups, preferably omega-3 and/or omega-6 acyl groups, at a concentration of least 5% (w/w) of total fatty acids content of said preparation, preferably more than 10% (w/w), more preferably 20-50% (w/w), wherein said PUFA is covalently bonded to said lipid.  
     
     
         2 . A lipid preparation of  claim 1  wherein said lipid is a naturally occurring lipid, or a synthetic lipid.  
     
     
         3 . A lipid preparation of  claim 2 , wherein said lipid is a glycerophospholipid in which at least some of the sn-1 or sn-2 groups of the glycerol backbone are substituted with said poly-unsaturated fatty acid (PUFA) acyl groups.  
     
     
         4 . A lipid preparation of  claim 1 , wherein said lipid is a glycerophosphlipid of formula I:  
       
         
           
           
               
               
           
         
       
       wherein R″ represents a moiety selected from serine (PS), choline (PC), ethanolamine (PE), inositol (PI), glycerol (PG) and hydrogen (phosphatidic acid—PA), and R and R′, which may be identical or different, independently represent hydrogen or an acyl group, wherein said acyl group is selected from saturated, mono-unsaturated or poly-unsaturated acyl groups (PUFA), particularly long-chain poly-unsaturated fatty acids (LC-PUFA), more preferably omega-3 and/or omega-6 acyl groups, and salts thereof, with the proviso that R and R′ cannot simultaneously represent hydrogen, and wherein said polyunsaturated acyl groups comprise at least 5% (w/w) of total lipid fatty acids, preferably more than 10% (w/w), and particularly 20-50% (w/w).  
     
     
         5 . A preparation of  claim 4 , wherein R represents hydrogen and R′ represents an acyl group.  
     
     
         6 . A preparation of  claim 4 , wherein R′ represents hydrogen and R represents an acyl group.  
     
     
         7 . A preparation of  claim 4 , wherein said acyl group is an omega-3 acyl group, preferably an eicosapentaenoyl (EPA), a docosahexaenoyl (DHA) group, or linolenic omega-3 group.  
     
     
         8 . A preparation of  claim 4 , wherein said acyl group is an omega-6 acyl group, preferably an arachidonoyl (ARA) group, or a linoleic omega-6 group.  
     
     
         9 . A preparation of  claim 4 , wherein said acyl group is a linolenoyl (18:3) group.  
     
     
         10 . A preparation of  claim 4 , wherein R″ represents serine, choline, ethanolamine, inositol, glycerol, and H.  
     
     
         11 . A preparation according to  claim 4 , wherein the identity and content of R and R′ are predetermined.  
     
     
         12 . A preparation of  claim 10 , wherein R″ is serine, characterized in that it mimics the composition of human brain PS.  
     
     
         13 . A preparation of  claim 10 , wherein R″ is serine, characterized in that it is different from human brain PS and has improved bioactivity compared to soybean-PS.  
     
     
         14 . A PS preparation, wherein said PS is derived from any one of plant, animal or microorganism source, said preparation being enriched with PS of formula I, wherein R″ represents a serine moiety.  
     
     
         15 . A preparation of  claim 12 , characterized in that it is effective at a lower dosage compared to soybean-PS, while having similar and/or improved bioactivity compared to soybean-PS.  
     
     
         16 . A preparation of  claim 1 , wherein said omega-3 or omega-6 is more stable than a omega-3 or omega-6 in the free fatty acid form, bonded to a triglyceride or as an ethyl ester.  
     
     
         17 . A preparation of  claim 1 , characterized in having a reduced or absent of fish-related organoleptic effects.  
     
     
         18 . A preparation of  claim 1 , said preparation being enriched with PS of formula I, characterized in having a reduced or absent of fish-related organoleptic effects.  
     
     
         19 . A preparation of  claim 1 , for use in the reduction and/or prevention of serum oxidative stress leading to atherosclerosis, cardiovascular disorders and/or coronary heart disease.  
     
     
         20 . A preparation of  claim 1 , for use in the improvement and treatment of cognitive and mental conditions and disorders as well as the maintenance of normal functions of brain-related systems and processes, preferably ADHD, aging, Alzheimer's disease, Parkinson's disease, multiple sclerosis (MS), dyslexia, depression, learning capabilities, intensity of brain waves, stress, anxiety, mental and psychiatric disorders, concentration and attention, mood, brain glucose utilization, general cognitive and mental well being, neurological disorders and hormonal disorders.  
     
     
         21 . A preparation of  claim 1 , said preparation being enriched with PS of formula I, for use in any one of the improvement and treatment of ADHD, and reducing ADHD symptoms in children.  
     
     
         22 . A preparation of  claim 1 , for enhancing the bioavailability of polyunsaturated fatty acids, particularly omega-3 and/or omega-6 fatty acids.  
     
     
         23 . A preparation of  claim 1 , for use in combined improvement of cognitive and mental functions together with improvement of additional health disorders or conditions.  
     
     
         24 . The preparation of  claim 23 , wherein said additional health disorders or conditions are at least one of high blood cholesterol levels, high triglycerides levels, high blood fibrinogen levels, HDL/LDL ratio, diabetes, metabolic syndrome, menopausal or post-menopausal conditions, hormone related disorders, vision disorders, inflammatory disorders, immune disorders, liver diseases, chronic hepatitis, steatosis, phospholipid deficiency, lipid peroxidation, dysrhythmia of cell regeneration, destabilization of cell membranes, coronary artery disease, high blood pressure, cancer, hypertension, aging, kidney disease, skin diseases, edema, gastrointestinal diseases, peripheral vascular system diseases, allergies, neurodegenerative and psychiatric diseases.  
     
     
         25 . A nutraceutical composition comprising a phospholipid preparation as claimed in  claim 1 .  
     
     
         26 . A nutraceutical composition of  claim 25 , in the form of softgel capsules, tablets, syrups, or any other common dietary supplement delivery system.  
     
     
         27 . A functional food article comprising the phospholipid preparation of  claim 1 .  
     
     
         28 . The functional food article of  claim 27 , selected from dairy products, ice-creams, biscuits, soy products, bakery, pastry and bread, sauces, soups, prepared foods, frozen foods, condiments, confectionary, oils and fats, margarines, spreads, fillings, cereals, instant products, drinks and shakes, infant formulas, infant foods (biscuits, mashed vegetables and fruits, cereals), bars, snacks, candies and chocolate products.  
     
     
         29 . A pharmaceutical composition comprising the phospholipids preparation of  claim 1 , and optionally at least one pharmaceutically acceptable additive, diluent or excipient.  
     
     
         30 . A pharmaceutical composition of  claim 29 , further optionally comprising at least one pharmaceutically active agent.  
     
     
         31 . The preparation of  claim 1 , wherein said PUFA has increased bioavailability to the organism when comparing to a composition comprising PUFA alone.