PLANT EXTRACT, COMPOSITIONS CONTAINING SAME, METHOD OF EXTRACTION AND USES THEREOF

• US 20120244096A1
• Filed: 09/16/2010
• Published: 09/27/2012
• Est. Priority Date: 09/16/2009
• Status: Active Grant

• Current Assignee: Botanic Century Beijing Co., Ltd.
• Original Assignee: Botanic Century Beijing Co., Ltd.
• Inventors: Xie, Chen, Zou, Yingshu
• Granted Patent: US 8,980,343 B2
• Time in Patent Office: Days
• US Class Current: 424/62
• 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 2200/318 having an effect on skin health and hair or coat
• CPC Class Codes: A23V 2200/328 having effect on glycaemic control and diabetes
• CPC Class Codes: A23V 2250/21 Plant extracts
• CPC Class Codes: A61K 36/605 Morus (mulberry)
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61K 8/9794 Liliopsida [monocotyledons]
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/08 for glucose homeostasis pancreatic hormones A61P5/48
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61Q 19/02 for chemically bleaching or whitening the skin

Abstract

An extract from leaves of mulberry is disclosed. The extract has an IC₅₀ value sufficient to inhibit α-glucosidase I. The extract may comprise 5-40% (w/w) total imino sugars and 20-70% (w/w) total amino acids. The extract may reduce the production of melanin for the treatment of such ailments or diseases caused by pigmentation as freckle, chloasma, striae gravidarum, sensile plaque and melanoma. The extract may also control blood glucose level.

Claims

1. A plant extract, obtained from Morus plant leaves, which has an IC₅₀ value, to inhibit α

-glucosidase I, at a concentration of less than 90 μ

g/ml.

2. A plant extract as claimed in claim 1 which has an IC₅₀ value, to inhibit α

-glucosidase I, at a concentration of from 5-40 μ

g/ml.

3. A plant extract as claimed in any of the preceding claims which comprises 5-40% (w/w) total imino sugars as measured by quantitative HPLC and/or LC-MS (liquid chromatography/mass spectrometry).

4. A plant extract as claimed in any of the preceding claims which comprises 8-30% (w/w) total imino sugars.

5. A plant extract as claimed in any of the preceding claims which comprises 15-20% (w/w) total imino sugars.

6. A plant extract as claimed in any of the preceding claims wherein the imino sugars further include DNJ, fagomine, N-methyl-DNJ, 1,4 dideoxy-1,4-imino-D-arabinitol (DAB), 2-O-α

-D-galactopyranosyl-DNJ (GAL-DNJ) and calystegin B.

7. A plant extract as claimed in any of the preceding claims which further comprises 20-70% (w/w) total amino acids.

8. A plant extract as claimed in claim 7 comprising 30-60% (w/w) total amino acids.

9. A plant extract as claimed in claim 8 comprising 40-50% (w/w) total amino acids.

10. A plant extract as claimed in any of the preceding claims wherein the Morus is selected from:

a. Morus alba L.

b. Morus alba var. multicaulis L.

c. Morus nigra and

d. Morus australis Poir.

11. A plant extract as claimed in claim 3 wherein said extract contains 1-20% (w/w) of (DNJ) calculated on the basis of the total weight of the extract.

12. A plant extract as claimed in claim 3 wherein said extract contains 2-10% (w/w) of (DNJ) calculated on the basis of the total weight of the extract.

13. A plant extract as claimed in claim 3 wherein said extract contains 4-6% (w/w) of (DNJ) calculated on the basis of the total weight of the extract.

14. A plant extract as claimed in claim 3 wherein said extract contains 1-3% (w/w) of (DNJ) calculated on the basis of the total weight of the extract.

15. A plant extract as claimed in any of the preceding claims characterised in that it is pale yellow or nearly white.

16. A plant extract as claimed in any of the preceding claims characterised in that it is easily soluble in water.

17. A plant extract as claimed in any of the preceding claims characterised in that it has a pH value of between 5.5-6.5 in a 1% water solution.

18. A plant extract as claimed in any of the preceding claims characterised in that a UV spectrum of the extract shows a maximum absorption at 218 nm and 263 nm.

21. A plant extract as claimed in any of claims 1-18 or the product of the method as claimed in claim 19 or 20 for use as a cosmetic or medicament to treat conditions caused by pigmentation.

22. A plant extract as claimed in claim 21 which is for reducing the production of melanin.

23. A plant extract as claimed in claim 21 or 22 for the treatment of ailments or disease caused by hyperpigmentation including:

freckle, chloasma, striae of pregnancy, senile plaque and melanoma.

24. A plant extract as claimed in any of claims 1-18 or the product of the method as claimed in claim 19 or 20 for use in controlling blood glucose level or lowering the glycaemic index of a food or drink.

25. A cosmetic or medicament comprising a plant extract as claimed in any of claims 1-18 or the product of the method as claimed in claim 19 or 20 in combination with one or more skin lightening agents selected from:

vitamin C and its derivatives, kojic acid, arbutin, diacetylboldin, azelaic acid, octadecenedioic acid, undecylenoylphenylalanine, liquorice extract, aloe extract, watercress extract, ascophyllum extract, hops extract, glutathione, ecdysone and/or ellagic acid.

26. A cosmetic or medicament as claimed in claim 25 wherein said vitamin C derivative is magnesium L-ascorbyl-2-phosphate (VC-PMG).

27. A cosmetic or medicament as claimed in claim 25 or 26 wherein the ratio of the extract and the other skin lightening agents is from 10:

1 to 1;

1.

28. A pharmaceutical, nutraceutical or a food or drink additive or supplement comprising a plant extract as claimed in any of claims 1-18 or the product of the method as claimed in claim 19 or 20.

29. A food or drink comprising a plant extract as claimed in any of claims 1-18 or the product of the method as claimed in claim 19 or 20.

19. A method for producing an extract, from Morus plant leaves, which has an IC₅₀ value to inhibit α

-glucosidase I at a concentration of less than 90 μ

g/ml comprising the steps of;

a. Conducting a water or alcoholic extraction step from leaf material;

b. Conducting a column chromatography purification step using a strong acidic cation exchange resin, washing with water, and eluting with an ammonia solution collecting the eluent and removing the ammonia therefrom;

c. Subjecting the eluent to column chromatography using a macroporous absorption resin, collecting the solution; and

d. Concentrating and drying the extract.

20. A method as claimed in claim 19 in which

a. The plant leaves are dried and made into coarse powder, the extraction step is conducted with 5-18 folds of 0-40% of a low molecular weight alcohol per the quantity of the Morus plant leaves (w/w), and repeated up to 5 times,

b. the column is washed with 1-2 folds of water of the column volume and the wash discarded, the column is eluted with 2-8 folds of 0.2-1.0N ammonia water solution of the column volume, at an elution rate of 1-3 folds of the volume of the column per hour, and the eluent is collected with a pH value of between 9.0 and 11.0,

c. the column is eluted with a volume ratio between the solution and column of between 20:

1 to 5;

1, and

d. the dried extract is pulverized to pass through a mesh 80 sieve.