Method and compositions for lowering blood lipids

• US 5,665,359 A
• Filed: 04/29/1994
• Issued: 09/09/1997
• Est. Priority Date: 04/29/1994
• Status: Expired due to Term

• Current Assignee: Chi-Ming Lee, Hson-Mou Chang, Walter Kwok Keung Ho
• Original Assignee: Chi-Ming Lee, Hson-Mou Chang, Walter Kwok Keung Ho
• Inventors: Lee, Chi-Ming, Chang, Hson-Mou, Ho, Walter Kwok Keung
• Primary Examiner(s): Rollins, John W.
• Application Number:
  US08/235,550
• Time in Patent Office: 1,229 Days
• Field of Search: 424/195.1, 424/514
• US Class Current: 424/765
• CPC Class Codes: A61K 36/734 Crataegus (hawthorn)

Abstract

It has been discovered that the Chinese fruit known as shanzha, and extracts and purified component derived therefrom, can be administered orally to animals to reduce levels of cholesterol in the blood. The mechanism of action is believed to include the "up-regulation" of LDL receptors on cell surfaces and inhibition of transcription factors for sterol responsive genes. Examples demonstrate the isolation of active components and extracts, potential mechanisms of action in animals and cell culture, and conditions promoting retention of activity during storage.

Claims

1. A method of decreasing blood lipid levels comprising administering to a patient in need thereof an effective amount of shanzha to decrease the level of lipid in the blood.

2. The method of claim 1 wherein an isolated active component of the shanzha is administered to a patient.

3. The method of claim 1, wherein the active component is an extract of the shanzha fruit.

4. The method of claim 3, wherein the active component is extracted from the dried fruit with an alcohol/water mixture, the resulting water extract is extracted with a chloroform/water mixture, the resulting water extract is extracted with an ethylacetate/water mixture, and the resulting water extract contains the active shanzha extract.

5. The method of claim 4, wherein the active component is extracted from the dried fruit with an ethanol/water mixture, the resulting water mixture is extracted with a chloroform/water mixture, the resulting water extract is extracted with an ethylacetate/water mixture, and the resulting ethylacetate extract contains the active shanzha extract.

6. The method of claim 1 wherein the shanzha is whole fruit or fruit juice.

7. The method of claim 1, wherein the shanzha is administered orally.

8. The method of claim 1, wherein the shanzha is administered to a patient with atherosclerosis.

9. The method of claim 1, wherein the shanzha is administered to a patient with hypercholesterolemia.

10. The method of claim 1 comprising administering to the patient a HMG CoA reductase inhibitor.

11. A composition effective when administered to a patient to decrease blood lipids comprising a component present in an organic solvent/water extract of shanzha fruit which is active in hepatocyte cell culture to increase cellular uptake of lipids from the culture media.

12. The composition of claim 11, wherein the active component is extracted from dried shanzha fruit with an alcohol/water mixture, the resulting water extract is extracted with a chloroform/water mixture, the resulting water extract is extracted with an ethylacetate/water mixture, and the resulting water extract contains the active shanzha extract.

13. The composition of claim 11, wherein the active component is extracted from the dried fruit with an ethanol/water mixture, the resulting water mixture is extracted with a chloroform/water mixture, the resulting water extract is extracted with an ethylacetate/water mixture, and the resulting ethylacetate extract contains the active shanzha extract.

14. The composition of claim 13, wherein the active component is further purified from the other components of the ethyl acetate extract by chromatography.