Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-11-18
2004-03-16
Owens, Amelia (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C549S399000
Reexamination Certificate
active
06706756
ABSTRACT:
FIELD OF INVENTION
This invention relates to compounds that demonstrate anti-oxidant and vascular properties, including vasodilation.
BACKGROUND OF THE INVENTION
The antioxidant properties of various plant favonoids, including procyanidins, are well known. Procyanidins possess endothelium-dependent relaxing (EDR) activity in blood vessels in vitro. The original finding that red wines, grape juice and other grape products exhibited EDR activity was companied by strong evidence that this activity was due to stimulation of nitric oxide (NO) production by the endothelial cells which form the lining of all blood vessels. Vasorelaxation induced by grape extracts, wines and the like was reversed by NO synthase inhibitors, and vasorelaxation could be restored by exposure of the vessel to L-arginine, the normal substrate for NO synthase. The importance of nitric oxide synthase system is underscored by the finding that a dysfunctional NO system can contribute to several diseases, including atherosclerosis. Therefore, consumption (and absorption) of NO-stimulating compounds in the diet, or in the form of dietary supplements, could contribute to prevention or halting the progress of atherosclerosis, other chronic age-related diseases, or conditions known to involve failure of the NO/NO synthase system, e.g., erectile dysfunction. Although procyanidin compounds, particularly those from grape seed extracts are known to exhibit EDR activity, current supplements administered to patients and consumers do not identify, nor isolate the active and most potent compounds to achieve the desired EDR.
SUMMARY OF INVENTION
The present invention is an isolated compound and method of inducing endothelium-dependent relaxation in blood vessels including the step of introducing isolated procyanidins having a preponderance of (−)-epicatechins to a patient wherein the procyanidins are preferably galloylated. To achieve both bioavailability and potency, it is also preferred that the number of epicatechins monomers forming each procyanidin is between two and five. More specifically, isolated epicatechin-(4-8)epicatechin-(4-8)-epicatechin-gallate (C1-gallate) is administered to the patient. To enhance endothelium-dependent relaxation, a concomitant administration of L-arginine may be performed.
REFERENCES:
patent: 4925871 (1990-05-01), Gabetta et al.
patent: 5594032 (1997-01-01), Gonzalez-Cadavid et al.
patent: 5773262 (1998-06-01), Ariga et al.
patent: 5891459 (1999-04-01), Cooke et al.
patent: 5904924 (1999-05-01), Garnor et al.
patent: 5912363 (1999-06-01), Nafisi-Movaghar et al.
patent: 5945452 (1999-08-01), Cooke et al.
patent: 5976568 (1999-11-01), Riley
patent: 6007824 (1999-12-01), Duckett et al.
patent: 6039950 (2000-03-01), Khwaja et al.
patent: 6054128 (2000-04-01), Wakat
patent: 6117911 (2000-09-01), Grainger et al.
patent: 6149939 (2000-11-01), Strumor et al.
patent: 6180663 (2001-01-01), Lang
patent: 6200558 (2001-03-01), Saavedra et al.
Fitzpatrick, DF et al, ‘Isolation and characterization of endothelium-dependent vasorelaxing compouds from grape seeds’ J. Agr. and Food Chem. (2000), 48(12), 6384-6390.*
The Dominion Medical Briefing, West 2002 pp. 1 and 2.
ND Kim et. al., Ginsenosides Evoke Endothelium-Dependent Vascular Relaxation in Rat Aorta, Gen Pharmacol (FLK), Oct. 1994; 25 (6): 1071-7.
Emile Andriambeloson et. al., Nitric Oxide Production and Endothelium-Dependent Vasorelaxation Induced by Wine Polyphenols in Rat Aorta, British Journal of Pharmacology 1997.
Dr. John Briffa, Secret Healing Power in Your Christmas Tree, 2000 Associated Newspaper Ltd. Daily Mail (London).
Dr. John D. Folts, Ph.D., Synergistic Effect of Grape Seed and Grape Skin Extracts Points Toward Effectiveness of Whole Juice, According to Researcher, Food Ingredients Online News.
David F. Fitzpatrick et al., Isolation and Characterization of Endothelium-Dependent Vasorelaxing Compounds from Grape Seeds, vol. 48, No. 12, pp. 6384-6390.
D.F. Fitzpatrick et al., Grape Seed Procyanidins: Isolation, Identification, and Endothelium-Dependent Vasorelaxing Activity, The Journal of Heart Disease, 1(1):79 (May 1999).
David F. Fitzpatrick et al., Isolation, Identification, and Characterization of Grape Procyanidins Responsible for Endothelium-Dependent Vasorelaxing, Sub. to Welch's Jan. 21, 1999.
David F. Fitzpatrick et al., Endothelium-Dependent Vascular Effects of Pycnogenol, Journal of Cardiovascular Pharmacology, 32:509-515.
David F. Fitzpatrick et al., Endothelium-Dependent Vasorelaxing Activity of Wine and Other Grape Products, The American Physiological Society, 0363-6135/1993.
David F. Fitzpatrick et al., Endothelium-Dependent Vasorelaxation Caused by Various Plant Extracts, Journal of Cardiovascular Pharmacology, 26:90-95.
David F. Fitzpatrick et al., Endothelium-Dependent Vasorelaxing Activity of Wine, Grapes, and Other Plant Products, 1997 American Chemical Society.
David F. Fitzpatrick et al., Vasorelaxation, Endothelium, and Wine, 0951-6433/97, 1997 IOS Press.
Kathy's Herb Shop, Virilogarl by Olympian Labs—90 Capsul, http://www.kathysherbshop.com/shop.product75.html.
Whole Health MD.com, Supplements Grape Seed Extract, http://www.wholehealthmd.com/refshelf/substances_view/0,1525,793,00.html.
Unicity Network.com, Cure It Through the Grapevine: The Amazing Antioxidant Power of Grape Seed Extract, http://www.unicitynetwork.com/ibo/hwnews/health_wealth_110701.html.
Hopen Anton J.
Owens Amelia
Smith & Hopen , P.A.
University of South Florida
LandOfFree
Vasodilating compound and method of use does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Vasodilating compound and method of use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Vasodilating compound and method of use will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3278739