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Title:  Method for preventing or treating elevated blood lipid level-related diseases by administering rutin and quercetin

United States Patent:  6,509,372

Issued:  January 21, 2003

Inventors:  Bok; Song-Hae (Daejeon, KR); Jeong; Tae-Sook (Daejeon, KR); Bae; Ki-Hwan (Daejeon, KR); Park; Yong-Bok (Daegu, KR); Choi; Myung-Sook (Daegu, KR); Moon; Surk-Sik (Gongju, KR); Kwon; Yong-Kook (Daejeon, KR); Lee; Eun-Sook (Daejeon, KR); Hyun; Byung-Hwa (Daejeon, KR); Choi; Yang-Kyu (Daejeon, KR); Lee; Chul-Ho (Daejeon, KR); Lee; Sae-Bom (Daejeon, KR); Park; Young-Bae (Seoul, KR); Kim; Hyo-Soo (Seoul, KR)

Assignee:  Korea Research Institute of Bioscience and Biotechnology (Daejon, KR)

Appl. No.:  804956

Filed:  March 13, 2001

Abstract

A method for treating or preventing an elevated blood lipid level-related disease in a mammal, which comprises administering thereto an effective amount of rutin, quercetin or a mixture thereof.

DETAILED DESCRIPTION OF THE INVENTION

Throughout the specification, the term "blood lipid" designates a lipid present in blood. The blood lipid is represented by cholesterol and triglycerides carried in the blood.

The term "high or elevated level" of a blood lipid means a higher than normal level, the normal level varying with specific conditions of a patient, such as age, gender and body weight. A high level of blood lipid or glucose in ordinarily considered to be harmful to health.

The term "elevated blood lipid level-related disease" means a disease which is caused by a high or elevated level of blood lipid, and/or a disease whose symptoms include a high or elevated level of blood lipid. Examples of such a disease include hyperlipidemia, arteriosclerosis, angina pectoris, stroke, hepatic diseases such as fatty liver and the like.

Rutin(C27 H30 O16, M. W. 610.51, glycosylated quercetin, see Merck Index 11th ed. (1989)) and quercetin(C15 H10 O7, M. W. 302.23) may be extracted from various plants including vegetables such as lettuce and onion, fruits such as citrus, and grains such as buckwheat, or synthesized in accordance with the conventional process described by Zemplen, Bognar in Ber., 1043 (1943) and Seka, Prosche, Monatsh., 69, 284(1936).

For example, rutin exist in buckwheat seeds, leaves, stems, flowers and sprouts in an amount ranging from 0.1 to 10 wt %. Thus, rutin and quercetin may be extracted from buckwheat by using a suitable solvent such as water or aqueous alcohol under a high temperature and pressure. Alternatively, buckwheat seeds, leaves, stems, flowers and/or sprouts may be allowed to stand overnight in an aqueous solution of Ca(OH)2 or NaOH, and then crude rutin precipitates may be collected after neutralization. Further, dry powders of buckwheat seeds, leaves, stems and flowers may also be used. Generally, the content of rutin in leaves and stems of buckwheat is about 0.6% and that in buckwheat flower is about 3%.

Rutin and quercetin exert an inhibitory effect on elevated blood lipid level-related diseases such as hyperlipidemia, arteriosclerosis, angina pectoris, stroke and hepatic diseases as well as therapeutic effect. Further, in spite of their potent efficacies, quercetin or rutin exhibits no toxicity when it is orally administered to a mouse at a dose of 1,000 mg/kg and 160 mg/kg, respectively. Moreover, they exert no adverse effects on the liver function.

A pharmaceutical formulation may be prepared in accordance with any of the conventional procedures. In preparing the formulation, the active ingredient is preferably admixed or diluted with a carrier, or enclosed within a carrier which may be in the form of a capsule, sachet or other container. When the carrier serves as a diluent, it may be a solid, semi-solid or liquid material acting as a vehicle, excipient or medium for the active ingredient. Thus, the formulations may be in the form of a tablet, pill, powder, sachet, elixir, suspension, emulsion, solution, syrup, aerosol, soft and hard gelatin capsule, sterile injectable solution, sterile packaged powder and the like.

Examples of suitable carriers, excipients, and diluents are lactose, dextrose, sucrose, sorbitol, mannitol, starches, gum acacia, alginates, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxy-benzoates, propylhydroxybenzoates, talc, magnesium stearate and mineral oil. The formulations may additionally include fillers, anti-agglutinating agents, lubricating agents, wetting agents, flavoring agents, emulsifiers, preservatives and the like. The compositions of the invention may be formulated so as to provide quick, sustained or delayed release of the active ingredient after their administration to a mammal by employing any of the procedures well known in the art.

The pharmaceutical composition of the present invention contains the active ingredient in an amount ranging from 0.01 to 100 wt %, preferably, from 0.1 to 70 wt %. Further, the pharmaceutical composition of the present invention can be administered via various routes including oral, transdermal, subcutaneous, intravenous and intramuscular introduction. In case of human, a typical daily dose of the bioflavonoid may range from about 0.1 to 500 mg/kg body weight, preferably 0.5 to 100 mg/kg body weight, and can be administered in a single dose or in divided doses.

However, it should be understood that the amount of the active ingredient actually administered ought to be determined in light of various relevant factors including the condition to be treated, the chosen route of administration, the age, sex and body weight of the individual patient, and the severity of the patient's symptom; and, therefore, the above dose should not be intended to limit the scope of the invention in any way.

Moreover, rutin and quercetin can be advantageously incorporated in foods or beverages for the purpose of treating or preventing hyperlipidemia, arteriosclerosis, angina pectoris, stoke and hepatic diseases. The foods or beverages may include meats; juices such as a vegetable juice(e.g., carrot juice and tomato juice) and a fruit juice(e.g., orange juice, grape juice, pineapple juice, apple juice and banana juice); chocolates; snacks; confectionery; pizza; food products made from cereal flour such as breads, cakes, crackers, cookies, biscuits, noodles and the likes; gums; dairy products such as milk, cheese, yogurt and ice creams; soups; broths; pastes, ketchups and sauces; teas; alcoholic beverages; carbonated beverages; vitamin complexes; and various health foods.

The content of the rutin and quercetin in a food or beverage may range from 0.01 to 10 wt %. In particular, the beverage according to the present invention may comprise 10 to 100 g of rutin, quercetin or a mixture thereof per 1000 ml of the beverage.

As described above, rutin or quercetin can be used as an effective, non-toxic pharmaceutical agent for treating or preventing elevated blood lipid level-related diseases such as hyperlipidemia, arteriosclerosis, angina pectoris, stroke and hepatic diseases.

Claim 1 of 11 Claims

What is claimed is:

1. A method for inhibiting the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase in a mammal, which comprises administering thereto rutin, quercetin or a mixture thereof in an amount effective to inhibit the activity of HMG-CoA reductase.

 


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