Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-12-10
2004-06-08
Solola, Taofiq (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C549S399000, C549S406000
Reexamination Certificate
active
06747059
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to medical and nutritional uses of extracts and products containing cocoa polyphenols including cocoa procyanidins.
BACKGROUND OF THE INVENTION
Polyphenols are an incredibly diverse group of compounds (Ferriera et al., ‘Diversity of Structure and Function in Oligomeric Flavanoids, Tetrahedron, 48:10, 1743-1803, 1992). They 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 non-nutritive, interest in these compounds has arisen because of their possible beneficial effects on health.
For instance, quercetin (a flavonoid) has been shown to possess anticarcinogenic activity in experimental animal studies (Deshner et al., ‘Quercertin, and Rutin as Inhibitors of Azoxymethanol-induced Colonic Neoplasia’, Carcinogenesis, 7:1193-1196, 1991: and Kato et al., ‘Inhibition of 12-O-tetradecanoylphorbol-13-acetate Induced Tumor Promotion and Ornithine Decarboxylase Activity by Quercitin: Possible Involvement of lipoxygenase Inhibition’, Carcinogenesis, 4, 1301-1305 1983). (+)-catechin and (−)-epicatechin (flavan-3-ols) have been shown in inhibit Leukemia virus reverse transcriptase activity (Chu et al., Inhibitory Effects of Flavonoids on Maloney Murine Leukemia Virus Reverse Transcriptase Activity, J. of Natural Products, 55:2, 179-183, 1992). Nobotanin (an oligomeric hydrolyzable tannin) has also been shown to possess anti-tumor activity (Okuda et al., ‘Molecular Structures and Pharmacological Activities of Polyphenols—Oligomeric Hydrolyzable Tannins and Others’—Presented at the XVI
th
International Conference of the Groupe Polyphenols, Lisbon, Portugal, Jul. 13-16, 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, ‘Molecular Structures and Pharmacological Activities of Polyphenols—Oligomeric Hydrolyzable Tannins and Others. Presented at the XVIth International Conference of the Groupe polyphenols, Lisbon, Portugal, 1992). Osakabe et al. (JP 7274894 “Food and Drink For Preventing Gastric Ulcers—Contains Antioxidation Substance Extracted from Cacao Beans using Hot Water or Ethanol” October 1995; JP 7213251 “Method on Manufacturing an Antioxidation Substance and a Health Food or Drink Item Containing an Antioxidation Substance” August 1995) have reported that the antioxidant properties of cocoa bean extract, thought to contain epicatechin and analogous compounds, are responsible for inhibiting formation of gastric ulcers in rats. Ellagic acid has also been shown to possess anticarcinogen activity in various animal tumor models (Boukharta et al., Efficacy of Ellagitannins and Ellagic Acid as Cancer Chemopreventive Agents—Presented at the XVI
th
International Conference of the Groupe Polyphenols, Lisbon, Portugal, Jul. 13-16, 1992). Lastly, proanthocyanidin oligomers have been reported by the Kikkoman Corporation for use as antimutagens (‘Antimutagenic Agent Containing Proanthocyanidin Oligomer Preferably Having Flavan-3-ol-diol Structure’ JP 04190774A, Jul. 7, 1992). Indeed, the area of phenolic compounds in foods and their modulation of tumor development in experimental animal models has been recently presented to the 202
nd
National Meeting of The American Chemical Society (Phenolic Compounds in Foods and Their Effects on Health II. Antioxidants & Cancer Prevention, Huang, M.-T., Ho, C.-T., and Lee, C. Y. editors, ACS Symposium Series 507, American Chemical Society, Washington, D.C. 1992).
SUMMARY OF THE INVENTION
It has been surprisingly discovered that cocoa extract, and compounds therefrom, have anti-tumor, anti-cancer or antineoplastic activity or, is an antioxidant composition or, inhibits DNA topoisomerase II enzyme activity or, is an antimicrobial or, is a cyclo-oxygenase and/or lipoxygenase modulator or, is a NO or NO-synthase modulator or, is a blood or in vivo glucose modulator.
Accordingly, the present invention provides a substantially pure cocoa extract and compounds therefrom. The extract or compounds 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, (+) catechin, procyanidin B-2, procyanidin oligomers 2 through 12, preferably 2 through 4 or 4 through 12, more preferably 3 through 12, and most preferably 5 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, or antimicrobial, or cyclo-oxygenase and/or lipoxygenase modulator, or an NO or NO-synthase modulator, or blood or in vivo glucose modulator composition comprising a substantially pure cocoa extract or compound therefrom or synthetic cocoa polyphenol(s) such as polyphenol(s) enriched with procyanidin(s) and a suitable carrier, e.g., a pharmaceutically, veterinary or food science acceptable carrier. The extract or compound therefrom preferably comprises cocoa procyanidin(s). The cocoa extract or compounds therefrom is preferably obtained by a process comprising reducing cocoa beans to powder, defatting the powder and, extracting and purifying 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, or antimicrobial, or cyclo-oxygenase and/or lipoxygenase modulator, or an NO or NO-synthase modulator, or blood or in vivo glucose modulator comprising administering to the patient a composition comprising an effective quantity of a substantially pure cocoa extract or compound therefrom or synthetic cocoa polyphenol(s) or procyanidin(s) and a carrier, e.g., a pharmaceutically, veterinary or food science acceptable carrier. The cocoa extract or compound therefrom can be cocoa procyanidin(s); and, is preferably obtained by reducing cocoa beans to powder, defatting the powder and, extracting and purifying active compound(s) from the powder.
Anti-cancer, anti-tumor or antineoplastic or, antioxidant, DNA topoisomerase II enzyme inhibiting, antimicrobial, cyclo-oxygenase and/or lipoxygenase modulator NO- or NO-synthase and blood or in vivo glucose modulating activities, or compositions containing the inventive cocoa polyphenols or procyanidins can be prepared in accordance with standard techniques well known to those skilled in the pharmaceutical or food science or veterinary art(s).
Such compositions can be administered to a subject or patient in need of such administration in dosages and by techniques well known to those skilled in the medical, nutritional or veterinary arts taking into consideration such factors as the age, sex, weight, and condition of the particular subject or patient, and the route of administration. The compositions can be co-administered or sequentially administered with other antineoplastic, anti-tumor or anti-cancer agents, antioxidants, DNA topoisomerase II enzyme inhibiting agents, or cyclo-oxygenase and/or lipoxygenase, blood or in vivo glucose or NO or NO-synthase modulating agents and/or with agents which reduce or alleviate ill effects of antineoplastic, anti-tumor, anti-cancer agents, antioxidants, DNA topoisomerase II enzyme inhibiting agents, cyclo-oxygenase and/or lipoxygenase, blood or in vivo glucose or NO or NO-synthase modulating agents; again, taking into consideration such factors as the age, sex, weight, and condition of the particular subject or patient, and, the route of administration.
Further, the invention also comprehends a kit wherein the active cocoa extract is provided. The kit can include a separate container containing a suitable carrier, diluent or excipient. The kit can al
Romanczyk Jr. Leo J.
Schmitz Harold H.
Mars Incorporated
Nada Jain, P.C.
Solola Taofiq
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