Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1997-04-22
2002-11-12
Nutter, Nathan M. (Department: 1711)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S456000, C549S354000, C549S355000
Reexamination Certificate
active
06479539
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to cocoa extracts such as polyphenols preferably polyphenols enriched with procyanidins. This invention also relates to methods for preparing such extracts, as well as to uses for them; for instance, as antineoplastic agents and antioxidants.
Documents are cited in this disclosure with a full citation for each appearing in a References section at the end of the specification, preceding the claims. These documents pertain to the field of this invention; and, each document cited herein is hereby incorporated herein by reference.
BACKGROUND OF THE INVENTION
Polyphenols are an incredibly diverse group of compounds (Ferreira et al., 1992) which widely occur in a variety of plants, some of which enter into the food chain. In some cases they represent an important class of compounds for the human diet. Although some of the polyphenols are considered to be nonnutrative, interest in these compounds has arisen because of their possible beneficial effects on health. For instance, quercitin (a flavonoid) has been shown to possess anticarcinogenic activity in experimental animal studies (Deshner et al., 1991 and Kato et al., 1983). (+)-Catechin and (−)-epicatechin (flavan-3-ols) have been shown to inhibit Leukemia virus reverse transcriptase activity (Chu et al., 1992). Nobotanin (an oligomeric hydrolyzable tannin) has also been shown to possess anti-tumor activity (Okuda et al., 1992). Statistical reports have also shown that stomach cancer mortality is significantly lower in the tea producing districts of Japan. Epigallocatechin gallate has been reported to be the pharmacologically active material in green tea that inhibits mouse skin tumors (Okuda et al., 1992). Ellagic acid has also been shown to possess anticarcinogen activity in various animal tumor models (Bukharta et al., 1992). Lastly, proanthocyanidin oligomers have been patented by the Kikkoman Corporation for use as antimutagens. Indeed, the area of phenolic compounds in foods and their modulation of tumor development in experimental animal models has been recently presented at the 202nd National Meeting of The American Chemical Society (Ho et al., 1992; Huang et al., 1992).
However, none of these reports teaches or suggests cocoa extracts, any methods for preparing such extracts, or, any uses as antineoplastic agents for cocoa extracts.
Since unfermented cocoa beans contain substantial levels of polyphenols, the present inventors considered it possible that similar activities of and uses for cocoa extracts, e.g., compounds within cocoa, could be revealed by extracting such compounds from cocoa and screening the extracts for activity. The National Cancer Institute has screened various Theobroma and Herrania species for anti-cancer activity as part of their massive natural product selection program. Low levels of activity were reported in some extracts of cocoa tissues, and the work was not pursued. Thus, in the antineoplastic or anti-cancer art, cocoa and its extracts were not deemed to be useful; i.e., the teachings in the antineoplastic or anti-cancer art lead the skilled artisan away from employing cocoa and its extracts as cancer therapy. Since a number of analytical procedures were developed to study the contributions of cocoa polyphenols to flavor development (Clapperton et al., 1992), the present inventors decided to apply analogous methods to prepare samples for anti-cancer screening, contrary to the knowledge in the antineoplastic or anti-cancer art. Surprisingly, and contrary to the knowledge in the art, e.g., the National Cancer Institute screening, the present inventors discovered that cocoa polyphenol extracts which contain procyanidins, have significant utility as anti-cancer or antineoplastic agents. Additionally, the inventors demonstrate that cocoa extracts containing procyanidins have utility as antioxidants.
OBJECTS AND SUMMARY OF THE INVENTION
It is an object of the present invention to provide a method for producing cocoa extract.
It is another object of the invention to provide a cocoa extract.
It is another object of the invention to provide an antioxidant composition.
It is another object of the invention to demonstrate inhibition of DNA topoisomerase II enzyme activity.
It is yet another object of the present invention to provide a method for treating tumors or cancer.
It is still another object of the invention to provide an anti-cancer, anti-tumor or antineoplastic composition.
It is a further object of the invention to provide a method for making an anti-cancer, anti-tumor or antineoplastic composition.
And, it is an object of the invention to provide a kit for use in treating tumors or cancer.
It has been surprisingly discovered that cocoa extract has anti-tumor, anti-cancer or antineoplastic activity; or, is an antioxidant composition or, inhibits DNA topoisomerase II enzyme activity. Accordingly, the present invention provides a substantially pure cocoa extract. The extract preferably comprises polyphenol(s) such as polyphenol(s) enriched with cocoa procyanidin(s), such as polyphenols of at least one cocoa procyanidin selected from (−) epicatechin, procyanidin B-2, procyanidin oligomers 2 through 12, preferably 2 through 5 or 4 through 12, procyanidin B-5, procyanidin A-2 and procyanidin C-1. The present invention also provides an anti-tumor, anti-cancer or antineoplastic or antioxidant or DNA topoisomerase II inhibitor composition comprising a substantially pure cocoa extract or synthetic cocoa polyphenol(s) such as polyphenol(s) enriched with procyanidin(s) and a suitable carrier. The extract preferably comprises cocoa procyanidin(s). The cocoa extract is preferably obtained by a process comprising reducing cocoa beans to powder, defatting the powder and, extracting active compound(s) from the powder.
The present invention further comprehends a method for treating a patient in need of treatment with an anti-tumor, anti-cancer, or antineoplastic agent or an antioxidant or a DNA topoisomerase II inhibitor comprising administering to the patient a composition comprising an effective quantity of a substantially pure cocoa extract or synthetic cocoa polyphenol(s) or procyanidin(s) and a carrier. The cocoa extract can be cocoa procyanidin(s); and, is preferably obtained by reducing cocoa beans to powder, defatting the powder and, extracting active compound(s) from the powder.
Additionally, the present invention provides a kit for treating a patient in need of treatment with an anti-tumor, anti-cancer, or antineoplastic agent or antioxidant or DNA topoisomerase II inhibitor comprising a substantially pure cocoa extract or synthetic cocoa polyphenol(s) or procyanidin(s) and a suitable carrier for admixture with the extract or synthetic polyphenol(s) or procyanidin(s).
These and other objects and embodiments are disclosed or will be obvious from the following Detailed Description.
REFERENCES:
patent: 4698360 (1987-10-01), Masquelier
patent: 4704292 (1987-11-01), Kattonberg
patent: 4797421 (1989-01-01), Ariga
patent: 5391568 (1995-02-01), Chung
patent: 5554645 (1996-09-01), Romanzcyk, Jr. et al.
patent: 6297273 (2001-10-01), Romanczyk, Jr. et al.
patent: 0 348 781 (1989-06-01), None
patent: 4-190774 (1990-11-01), None
patent: 4-190774 (1992-07-01), None
patent: 08205818 (1996-08-01), None
Toshiaki Ariga and Katsumi Yuasa, Antioxidative Properties of Oligomeric Proanthocyanidins and Their Applications, Fragrance Journal, 1994-7:52-56( Japanese version) and English version (pp. 1-11).
Wen-Chang Chang and Feng-Liu Hsu, Inhibition of Platelet Aggregation and Arachidonate Metabolism in Platelets by Procyanidins, Prostaglandins Leukotrienes and Essential Fatty Acids, 38:181-188, 1989.
V.J. Paolino and S. Kashket, Inhibition by Cocoa Extracts of Biosynthesis of Extracellular Polysaccharide by Human Oral Bacteria, Archs Oral. Biol., 30:359-363, 1985.
David F. Fitzpatrick, Steven L. Hirschfield, and Ronald G. Coffey, Endothelium-Dependent Vasorelaxing Activity of Wine and Other Grape Products, pp. H774-H778, American Physiological Society, 1993.
M.J
Buck Margaret M.
Hammerstone, Jr. John F.
Romanczyk Jr. Leo J.
Clifford Chance Rogers and Wells
Mars Incorporated
Nutter Nathan M.
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