METHOD FOR PREPARING GYNOSTEMMA PENTAPHYLLUM EXTRACT WITH INCREASING DAMULIN A AND DAMULIN B CONTENTS, AND PHARMACEUTICAL COMPOSITIONS OF THE SAME FOR TREATING METABOLIC DISEASE

• US 20110015142A1
• Filed: 01/29/2010
• Published: 01/20/2011
• Est. Priority Date: 07/17/2009
• Status: Active Grant

• Current Assignee: TG Biotech Co., Ltd.
• Original Assignee: TG Biotech Co., Ltd.
• Inventors: Kim, Ji Eun, Oh, Won Keun, HUH, Tae Lin, JOON, So Young, SONG, He Bok
• Granted Patent: US 8,357,786 B2
• Time in Patent Office: Days
• US Class Current: 514/26
• CPC Class Codes: A23L 33/105 Plant extracts, their artificial duplicates or their derivatives
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2250/21 Plant extracts
• CPC Class Codes: A61K 36/424 Gynostemma
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Disclosed is an AMPK activating material used for improving and treating metabolic syndrome, in which AMPK (AMP-activated protein kinase) is a main enzyme for regulating an energy sensor and lipid/glucose metabolism in the body. The activation of AMPK inhibits the synthesis of fat and cholesterol, and accelerates the reduction of body fat and blood glucose, thereby improving obesity, diabetes, and hyperlipidaemia. The disclosed AMPK activating material contains, as active ingredients having an improving and treating effect on metabolic syndrome, including obesity, diabetes, and hyperlipidaemia, a novel compound 2α,3β,12β-trihydroxydammar-20(22)-E,24-diene-3-O-[β-D-glucopyranosyl-(1→)-β-D-glucopyranoside], named Damulin A, and a novel compound 2α,3β,12β-trihydroxydammara-20,24-diene-3-O-[β-D-glucopyranosyl-(1→)-β-D-glucopyranoside], named Damulin B. Herein, the contents of damulin A and damulin B (as active indicator ingredients for AMPK activation) can be increased by treating a Gynostemma pentaphyllum extract with high temperature/high pressure. Accordingly, the novel Gynostemma pentaphyllum extract with a significantly increased AMPK activating capability can be used for improving or treating metabolic syndrome, such as obesity, diabetes, and hyperlipidaemia.

Claims

1. A method for preparing a novel Gynostemma pentaphyllum extract having increased concentrations of damulin A and damulin B, comprising the step of:

treating a concentrate of an ethanol extract of Gynostemma pentaphyllum leaves with a high temperature and/or high pressure reaction for 0.1˜

24 hours, wherein the temperature is about 40-125°

C. and the pressure is about 1.2˜

1100 atmospheres and wherein the increased concentrations of damulin A and damulin B are 0.7-7% (w/w) and 0.5-6% (w/w), respectively, based on the total weight of a dry powder of the novel Gynostemma pentaphyllum extract.

2. The novel Gynostemma pentaphyllum extract for improving and treating a metabolic syndrome, which is prepared by the method of claim 1.

3. The novel Gynostemma pentaphyllum extract as claimed in claim 2, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

4. A functional food for improving a metabolic syndrome comprising the Gynostemma pentaphyllum extract as claimed in claim 2, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

5. The functional food as claimed in claim 4, which comprises a carrier of thermal waters, filtrated water, distilled water, aerated water, juice, yogurt, milk, or edible oil.

6. A pharmaceutical composition for improving and treating a metabolic syndrome comprising the Gynostemma pentaphyllum extract as claimed in claim 2, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

7. The pharmaceutical composition as claimed in claim 6, which increases enzyme activity of AMP-activated protein kinase (AMPK).

11. A method for improving or treating a metabolic syndrome comprising administering the novel Gynostemma pentaphyllum extract of claim 2 to a patient in need thereof in an effective amount for improving or treating the metabolic syndrome, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

8. A pharmaceutical composition for improving and treating a metabolic syndrome, comprising, as an active ingredient, at least one of damulin A and damulin B, represented by Formula 1:

9. The pharmaceutical composition as claimed in claim 8, which increases enzyme activity of AMP-activated protein kinase (AMPK).

12. A method for improving or treating a metabolic syndrome comprising administering the novel Gynostemma pentaphyllum extract of claim 8 to a patient in need thereof in an effective amount for improving or treating the metabolic syndrome, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

16. A pharmaceutical composition as claimed in claim 8, wherein Damulin A or Damulin B is included in an amount of 0.01-100% with respect to the total composition.

10. A novel Gynostemma pentaphyllum extract comprising 0.7-7% (w/w) of damulin A and 0.5-6% (w/w) of damulin B based on the total weight of a dry powder of the Gynostemma pentaphyllum extract.

13. A method for improving or treating a metabolic syndrome comprising administering the novel Gynostemma pentaphyllum extract of claim 10 to a patient in need thereof in an effective amount for improving or treating the metabolic syndrome, wherein the metabolic syndrome is obesity, diabetes or hyperlipidaemia.

14. Damulin A represented by the following formula:

15. Damulin B represented by the following formula: