IP Library › Granted Patent US 10,016,474
Granted Patent B2
US 10,016,474 · App. 14/621,359 · Granted Jul 10, 2018

Plant extract, compositions containing same, method of extraction and uses thereof

Inventors: Chen Xie (Beijing, CN); Yingshu Zou (Beijing, CN)
Assignee: Botanic Century Beijing Co. Ltd.
A61K36/605A23L33/105A61K8/97A61Q19/02A23V2002/00
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Quick Facts
Patent No.
US 10,016,474
App. No.
14/621,359
Granted
Jul 10, 2018
Kind
B2
Abstract

An extract from leaves of mulberry is disclosed. The extract has an IC 50 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 (33)

1. A plant extract obtained from Morus plant leaves which has an IC 50 value of less than 90 μg/ml with respect to inhibition of α-glucosidase I, comprising:

5-40% (w/w) total imino sugars, as measured by at least one of quantitative High Performance Liquid Chromatography (HPLC) and liquid chromatography/mass spectrometry (LC-MS), the imino sugars including at least one of 1-deoxynojirimycin (DNJ), fagomine and N-methyl-DNJ; and

20-70% (w/w) total amino acids, wherein the extract is at least one of a pale yellow and nearly white powder that is easily soluble in water.

2. The plant extract as claimed in claim 1 , wherein the IC 50 value is 5-40m/ml with respect to inhibition of α-glucosidase I.

3. The plant extract as claimed in claim 1 , wherein the total imino sugars is 8-30% (w/w).

4. The plant extract as claimed in claim 1 , wherein the total imino sugar is 15-20% (w/w).

5. The plant extract as claimed in claim 1 , wherein the imino sugars further include at least one of 1,4 dideoxy-1,4-imino-D-arabinitol (DAB), 2-O-α-D-galactopyranosyl-DNJ (GAL-DNJ) and calystegin B.

6. The plant extract as claimed in claim 1 , wherein the total amino acids range from 30-60% (w/w).

7. The plant extract as claimed in claim 6 , wherein the total amino acids is 40-50% (w/w).

8. The plant extract as claimed in claim 1 , wherein the Morus is selected from

a. Morus alba L.,

b. Morus alba var multicaulis L.,

c. Morus nigra , and

d. Morus australis Poir.

9. The plant extract as claimed in claim 1 , wherein said extract contains 1-20% (w/w) of calculated on the basis of the total weight of the extract.

10. The plant extract as claimed in claim 1 , wherein the DNJ is included at a concentration of 2-10% (w/w) calculated on the basis of the total weight of the extract.

11. The plant extract as claimed in claim 1 wherein the DNJ is included at a concentration of 4-6% (w/w) calculated on the basis of the total weight of the extract.

12. The plant extract as claimed in claim 1 , wherein the DNJ is included at a concentration of 1-3% (w/w) calculated on the basis of the total weight of the extract.

13. The plant extract as claimed in claim 1 , further comprising a pH value between 5.5-6.5 in a 1% water solution.

14. The plant extract as claimed in claim 1 , wherein a UV spectrum of the extract shows a maximum absorption at 218 nm and 263 nm.

15. A cosmetic or medicament comprising a therapeutically effective amount of the plant extract as claimed in claim 1 in combination with one or more skin lightening agents selected from the group consisting of: 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 ellagic acid.

16. The cosmetic or medicament as claimed in claim 15 , wherein said vitamin C derivative is magnesium L-ascorbyl-2-phosphate (VC-PMG).

17. The cosmetic or medicament as claimed in claim 15 , wherein a ratio of the extract and the one or more skin lightening agents is from 10:1 to 1:1.

18. A method for producing the extract as claimed in claim 1 , comprising the steps of:

a. conducting a water or alcoholic extraction step from leaf material the Morus plant leaves to obtain a liquid extract;

b. filtering the liquid extract to result in a solution;

c. conducting a column chromatography purification step on the solution using a strong acidic cation exchange resin, washing with water, and eluting with an ammonia solution collecting the eluent and removing the ammonia therefrom to result in a collected fluid; and

d. concentrating the collected fluid to result in a concentrate, and drying the concentrate.

19. The method as claimed in claim 18 , wherein:

a. prior to conducting the water or alcoholic extraction step, further comprising the step of drying the Morus plant leaves and making them into coarse powder, and wherein the extraction step is conducted with 5-18 folds of 0-40% of a low molecular weight alcohol per the quantity of the Moms plant leaves (w/w), and repeated up to 5 times,

b. the step of conducting the column chromatography purification step includes washing the column with 1-2 folds of water of the column volume and discarding the wash, eluting the column 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 collecting the eluent with a pH value of between 9.0 and 11.0, and

c. the step of concentrating and drying the extract includes pulverizing the dried extract to pass through a mesh sieve.

20. The method as claimed in claim 18 , wherein following the step of conducting the column chromatography purification step, further comprising the step of subjecting the eluent to column chromatography using a macroporous absorption resin and collecting the solution, wherein the column is eluted with a volume ratio between the solution and the column of between 20:1 to 5:1.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 1, 2015
From: XIE, CHEN; ZOU, YINGSHU
To: BOTANIC CENTURY BEIJING CO. LTD
Reel/Frame 035548/0552 →
Priority Claims (1)
CN 2009 1 0307065 · Sep 16, 2009 · national
Continuity (2)
Continuation 13496427
Related Publication 20150224160A1 · Aug 13, 2015
Cited By (1)
US 12,661,313