Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1997-12-09
1999-02-02
Henley, III, Raymond J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514561, A61K 3800, A61K 31195
Patent
active
058665374
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This application is a 371 of PCT/EP96/02079 filed May 15, 1996.
The present invention relates to pharmaceutical and/or dietetic compositions with antioxidant activity, consisting of and/or
BACKGROUND OF THE PRIOR ART
Free radicals and the peroxidative processes caused by them have been known for a long time to be one of the causes of the structural and functional degradations of human tissues during aging and of a number of pathologies related to them: tumours; diabetes; hypertension; muscular excessive strain; radiation and sunburn damages; intoxications; ischemia; atherosclerosis; hyperthermia; cerebral traumas; inflammations; cataract; multiple sclerosis; Down syndrome, Parkinson's disease, Alzheimer's disease; dermatitis; muscular dystrophy; obesity; hyperlipidemia; hypercholesterolemia; tabagism; alcoholism, etc. (B. Cestaro, (1994), in "Per una vita inossidabile", ETASLIBRI--RCS Medicine, pp. 7-59; G. D. Bompiani, A. Galluzzo, (1990), in "Radicali Liberi in Fisiologia and Minerva Medica", pp. 3-280; Supplement to "The American Journal of Clinical Nutrition" vol. 53 (n. 1), 1991. pp. 1895-391S; "Radicali Liberi in Medicina", Periodici UTET Scientifici n. 1. dicembre 1993. pp. 1-57; "Lipid Peroxidation: part II Pathological Implications", (1987), Chem and Physics of Lipids, vol. 45 (n. 2-4), pp. 103-353).
Therefore it is important, in order to prevent the aging processes and related pathologies, to keep the concentration of the natural antioxidant molecules, ("free radical scavengers") which are the physiological defenses against free radicals, high both in the different tissues of the organism and in the blood stream, with which a continuous functional interchange occurs; in other words, blood (and the erythrocytes contained therein) can act as a carrier: 1) to provide the necessary antioxydants (both exogenous and deriving from, for example, the oral administration, and taken from endogenous deposits) to a certain tissue (which is at that time subjected to a specific pathological stress condition); 2) to drain the products from the peroxidative processes accumulated in a specific district of the organism.
It is therefore evident that an appropriate chemical-clinical evaluation of the sensitivity of plasma and/or of the erythrocytes (i.e. of the different tissues of the organism) to peroxidation can be an effective prognostic means to evaluate the efficiency of human antioxidant defenses and the capability of the body of defending against the damage induced by said dysmetabolic processes, typical of aging and of the above cited pathologies.
Carnosine (.beta.-alanyl-L-histidine) and some derivatives thereof (homocarnosine, acetylcarnosine, acetylhomocarnosine, etc.) have been known for some time to be among the most important natural antioxidant agents (Boldyrev A., Severin S., (1990), Adv. Enz. Reg., 30. 175-194; Kohen R. et al., (1988), Proc. Natl. Acad. Sci. USA, 85. 3175-79; Yoshikawa T. et al., (1991), Biochim. Biophys. Acta, 1115. 15-22) and the administration of these compounds would allow to cause an effective therapeutical activity in a number of the above mentioned pathologies (Davey C. L., (1960), Arch. Biochem. Biophys., 89. 303-308; Severin S., (1964); Proc. 6th Intern. Biochem. Congress, 45-61; Nagai K. and Suda T., (1988), Meth. Find. Exp. Clin. Pharmacol., 10. 497-507; Boldyrev A., (1990), Int. J. Biochem., 22. 129-132; Kurelle E. et al., (1991), Byul. Exp. Biol. Med., 112. 52-53; Boldyrev A. et al.; (1993), Int. J. Biochem., 25 1101-1107; Boldyrev A. et al., (1993), Mol. Chem. Neuropathol., 19. 185-192), particularly where the peroxidative damage induced by free radicals is one of the main causes in inducing and/or worsening the pathology. The antiradicalic activity of exogenous carnosine (or of the homologues thereof) is however restricted by the instability shown by said peptide towards the enzyme carnosinase, which is capable of hydrolyzing it into aminoacids components. The carnosinase is present both in the bloodstream and in the various tissue districts
Farmila-Farmaceutici Milano S.R.L.
Henley III Raymond J.
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