# US 5,700,450 A · Methods for enhancing melanin synthesis in melanocytes using diacyglycerols and uses thereof

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- Number: US 5,700,450 A
- Document ID: US5700450A
- Status: Granted
- Kind: A
- Application number: 08/314,470
- Filed: 1994-09-28
- Granted: 1997-12-23
- Earliest claimed: 1988-03-30
- Assignees: Trustees of Boston University
- Inventors: Barbara A. Gilchrest; Philip R. Gordon
- Web page: https://patentgrep.com/patent/US5700450A

## CPC

- C12N 5/0626: {Melanocytes}
- A61K 8/375: {the alcohol moiety containing more than one hydroxy group}
- A61Q 5/10: Preparations for permanently dyeing the hair
- A61Q 19/04: for chemically tanning the skin (topical sun or radiation screening or tanning preparations A61Q17/04)
- C12N 2500/36: Lipids
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Methods for enhancing melanin synthesis in melanocytes, thereby increasing the melanin content of melanocytes with subsequent transfer of the melanic pigments to keratinocytes resulting in increased pigmentation of vertebrate skin and hair; melanocytes with increased melanin content produced by these methods; and uses thereof are disclosed.

## Claims

### Claim 1

A method of increasing pigmentation of vertebrate skin by increasing the melanin content of melanocytes present in vertebrate skin comprising topically applying to the skin of the vertebrate, or subcutaneously administering to the vertebrate, an effective amount of a diacylglycerol wherein the diacylglycerol comprises a hydroxyl in the three position and two carboxylic acid esters in the one and two positions, said carboxylic acid esters having from one to twenty four carbon atoms, and which enhances melanin synthesis in the melanocytes.

### Claim 2 (depends on 1)

The method of claim 1, wherein the diacylglycerol is 1-oleoyl-2-acetyl-glycerol.

### Claim 3 (depends on 1)

The method of claim 1, wherein the diacylglycerol is 1,2-dioctanoylglycerol.

### Claim 4 (depends on 1)

The method of claim 1, wherein the diacylglycerol is 1,2-didecanoylglycerol.

### Claim 5 (depends on 1)

The method of claim 1, wherein the vertebrate is a human being.

### Claim 6 (depends on 1)

The method of claim 1, wherein the pigmentation of skin occurs irrespective of exposure to an irradiation selected from the group consisting of ultraviolet irradiation and sunlight irradiation.

### Claim 7 (depends on 1)

The method of claim 1, wherein the effective amount of the diacylglycerol is present in a composition containing from 0.1 to 10% by weight of diacylglycerol with respect to the total weight of the composition.

### Claim 8 (depends on 7)

The method of claim 7 further comprising admixing the diacylglycerol with a topically acceptable carrier selected from the group consisting of water, glycerol, alcohol, propyleneglycol, a fatty alcohol, a triglyceride a fatty acid ester, a mineral oil, liquid petrolatum, isopropyl palmitate, polyethylene glycol, ethanol, polyoxyethylene monolaurate at 5% in water, sodium lauryl sulfate at 5% in water and mixtures thereof.

### Claim 9

A method of increasing pigmentation of acquired or congenital white patches of skin of a vertebrate comprising the implantation of skin grafts on the patches, the skin grafts comprising melanocytes activated by contact with an effective amount of a diacylglycerol which wherein the diacylglycerol comprises a hydroxyl in the three position and two carboxylic acid esters in the one and two positions, said carboxylic acid esters having from one to twenty-four carbon atoms, and enhances melanin synthesis in the melanocytes.

### Claim 10 (depends on 9)

The method of claim 9, wherein the patches of skin to be pigmented are vitiligo patches.

### Claim 11 (depends on 9)

The method of claim 9, wherein the diacylglycerol is 1-oleoyl-2-acetyl-glycerol.

### Claim 12 (depends on 9)

The method of claim 9, wherein the diacylglycerol is 1,2-dioctanoylglycerol.

### Claim 13 (depends on 9)

The method of claim 9, wherein the diacylglyercol is 1,2-didecanoylglycerol.

### Claim 14 (depends on 9)

The method of claim 9, wherein the vertebrate is a human being.

### Claim 15 (depends on 9)

The method of claim 9, wherein the pigmentation occurs irrespective of exposure to an irradiation selected from the group consisting of ultraviolet irradiation and sunlight irradiation.

### Claim 16 (depends on 9)

The method of claim 9, wherein the effective amount of the diacylglycerol ranges from 10 .mu.M to 1000 .mu.M.

### Claim 17 (depends on 16)

The method of claim 16 wherein the effective amount of the diacylglycerol ranges from 50 .mu.M to 300 .mu.M.