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
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
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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