# US 2021/0330727 A1 · Plant extract obtained from morus plant leaves, compositions containing same, method of extraction and uses thereof

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- Number: US 2021/0330727 A1
- Document ID: US20210330727A1
- Status: Published application
- Kind: A1
- Application number: 17/367,308
- Filed: 2021-07-02
- Published: 2021-10-28
- Earliest claimed: 2009-09-16
- Assignees: Botanic Century (Beijing) Co. Ltd.
- Applicants: Botanic Century (Beijing) Co. Ltd.
- Inventors: Chen Xie; Yingshu Zou
- Web page: https://patentgrep.com/patent/US20210330727A1

## CPC

- A61K 36/605: Morus (mulberry)
- A23L 33/105: Plant extracts, their artificial duplicates or their derivatives
- A61K 8/9789: Magnoliopsida [dicotyledons]
- A61K 8/9794: Liliopsida [monocotyledons]
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 17/00: Drugs for dermatological disorders
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/02: for chemically bleaching or whitening the skin
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

An extract from leaves of mulberry is disclosed. The extract has an IC50 value sufficient to inhibit a-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

### Claim 1

A plant extract obtained from Morus plant leaves which has an IC50 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 031% fagomine and N-methyl-DNJ; and
20-70% (w/w) total amino acids, wherein the extract is at least one of pale yellow and nearly white and is easily soluble in water.

### Claim 2 (depends on 1)

The plant extract as claimed in claim 1, wherein the IC50 value is 5-40 μg/ml with respect to inhibition of α-glucosidase I.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

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.

### Claim 6 (depends on 1)

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

### Claim 7 (depends on 6)

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

### Claim 8 (depends on 1)

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.

### Claim 9 (depends on 1)

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.

### Claim 10 (depends on 1)

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.

### Claim 11 (depends on 1)

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.

### Claim 12 (depends on 1)

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

### Claim 13 (depends on 1)

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

### Claim 14 (depends on 1)

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

### Claim 15

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 μg/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; and
d. Concentrating and drying the extract.

### Claim 16 (depends on 15)

The method as claimed in claim 15, wherein:
a. prior to conducting the water or alcoholic extraction step, further comprising the step of drying the plant leaves 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 Morus 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
d. the step of concentrating and drying the extract includes pulverizing the dried extract to pass through a mesh sieve.

### Claim at position 17

17-19. (canceled)

### Claim 20 (depends on 15)

The method as claimed in claim 15, 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.

### Claim 21 (depends on 1)

A cosmetic or medicament comprising a 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.

### Claim 22 (depends on 21)

The cosmetic or medicament as claimed in claim 21, wherein said vitamin C derivative is magnesium L-ascorbyl-2-phosphate (VC-PMG).

### Claim 23 (depends on 21)

The cosmetic or medicament as claimed in claim 21, wherein a ratio of the extract and the one or more skin lightening agents is from 10:1 to 1:1.

### Claim at position 22

24-25. (canceled)