Title:  Preventive, alleviative or remedy for hypertension

United States Patent:  6,458,392

Issued:  October 1, 2002

Inventors:  Okawa; Wataru (Tokyo, JP); Mitsui; Yuki (Tokyo, JP); Watanabe; Takuya (Tokyo, JP); Eguchi; Yasuteru (Tokyo, JP); Takahashi; Hirokazu (Tokyo, JP); Suzuki; Atsushi (Tochigi, JP)

Assignee:  Kao Corporation (Tokyo, JP)

Appl. No.:  901909

Filed:  July 11, 2001

Provided is a preventive, ameliorant or remedy for hypertension excellent in both blood pressure lowering action and blood pressure-rise suppressing action and having high safety. This preventive, ameliorant or remedy for hypertension comprises a coffee bean extract.

BEST MODE FOR CARRYING OUT THE INVENTION

The extract of coffee beans to be used in the present invention is an extract from coffee beans which are fruits of a coffee tree. As the coffee tree, any one of C. arabica, C. robusta, C. liberica and C. arabusta is usable.

As the coffee beans to be extracted in the present invention, either raw beans or decaffeine treated beans or roasted beans are usable, with raw beans being particularly preferred.

Examples of the method for extracting, from coffee beans, an ingredient effective for the prevention, amelioration or treatment of hypertension include solvent extraction and supercritical fluid extraction. The extract obtained from coffee beans may be purified or may be adjusted by treatment with an ion exchange resin or the like (for example, Japanese Patent Application Laid-Open (Kokai) No. Hei 4-145048, Japanese Patent Application Laid-Open (Kokai) No. Hei 4-145049, etc.).

Examples of the extracting solvent used for solvent extraction include water and hydrophilic organic solvents such as methanol, ethanol, 2-propanol, acetone and methyl ethyl ketone. As the extracting solvent, a water-containing hydrophilic organic solvent having a water content of 5 wt. % (which will hereinafter be called %, simply) or greater, particularly, hydrous ethanol.

The extract of coffee beans to be used in the present invention contains various substances such as known already for example polysaccharides, lipids, chlorogenic acids, proteins, caffeine, minerals and fatty acids etc. It preferably contains chlorogenic acids and caffeine at a weight ratio of 2 or greater, preferably 2 to 1000, more preferably 2.5 to 500, especially 2.5 to 100 from the viewpoints of effects for preventing, ameliorating or treating hypertension, and sour taste with astringency upon intake. Caffeine suppresses pungency and chlorogenic-acid-induced sourness, whereby such a taste is attained. The components of the coffee bean extract may be adjusted to fall within the above-described range by the addition of chlorogenic acid or caffeine.

Examples of the chlorogenic acid include those having caffeine acid ester-bonded to one or two hydroxy groups, at the 3-, 4- or 5-position of quinic acid. Specific examples include 3-caffeoylquinic acid (chlorogenic acid) having caffeine acid ester-bonded to the hydroxyl group at the 3-position of quinic acid; 5-caffeoylquinic acid having caffeine acid ester-bonded to the hydroxyl group at the 5-position of quinic acid; 4-caffeoylquinic acid (cryptochlorogenic acid) having caffeine acid ester-bonded to the hydroxyl group at the 4-position of quinic acid; and isochlorogenic acids having caffeine acid ester-bonded to two hydroxyl groups, among hydroxyl groups at the 3-, 4- and 5-positions of quinic acid (ex. 3,5-caffeoylquinic acid). Salts of them are also embraced in the term "chlorogenic acid" used herein.

No particular limitation is imposed on the salts of a chlorogenic acid insofar as they are pharmaceutically acceptable salts. Examples include salts of an alkali (alkaline earth) metal such as sodium, potassium, calcium and magnesium. The chlorogenic acid exists also as a salt in naturally-occurring substances.

The preventive, ameliorant or remedy for hypertension according to the present invention may further contain another antihypertensive (agents) materials (such as .alpha.-blocker, .beta.-blocker, .alpha..beta.-blocker, ACE inhibitor, angiotensin II receptor antagonist, Ca blocker, diuretic, or psychotropic agent); vitamin (such as Vitamin A, Vitamin B₁, B₂, B₆, B₁₂, Vitamin C, Vitamin D or Vitamin E); and another active ingredient having blood pressure lowering action [physiologically active substance (ex. high unsaturated fatty acids of .omega.-3 type such as .alpha.-linolenic acid, EPA or DHA, triglyceride and/or diglyceride having this fatty acid as a component fatty acid, catechin which is a tea polyphenol or polymer thereof, or rutin which is a buckwheat polyphenol), Litchi Chinensis Sonn., ginkgo tree, Zizyphi Fructus, Polygonati Rhizoma, Cassiae Semen, Cortinellus shiitake, Momovdicae grosvenori, flowers of Chrysanthemum morifolium, leaves of Samallanthus sonchifolius, mulberry leaves, leaves of Banaba (Lagestroemia speciosa), Senpo, Plantaginis semen, and these extract etc.]

When used as a medicament, the preventive, ameliorant or remedy for hypertension according to the present invention can be formed into an oral administrable composition by adding thereto a pharmaceutically acceptable carrier. Examples of the oral administrable composition include tablets, granules, fine subtilaes, pills, powders, capsules (hard capsules and soft capsules), troches, chewables and liquid preparations (medical drink).

The preventive, ameliorant or remedy for hypertension according to the present invention is available as a food by adding thereto another component. Examples include foods in a liquid, emulsion or paste form such as beverage, soy sauce, milk, yogurt and miso to which ordinarily employed food additives have been added; semi-solid foods such as jelly and gummy; solid foods such as gum, tofu and supplement; powdery foods. Although it is available in any form, beverages, particularly soft drinks, are preferred.

An effective administration amount of the coffee bean extract of the present invention is preferably 5 to 5000 mg, especially 10 to 500 mg, a day per adult (weight: 60 kg) in terms of a chlorogenic acid contained in a dry solid content of the coffee bean extract.

Claim 1 of 17 Claims

What is claimed is:

1. A soy sauce, comprising a raw coffee bean extract, said soy sauce comprising:

a) chlorogenic acid; and

b) caffeine;

wherein the chlorogenic acid and caffeine is contained in the raw coffee bean extract.
 

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