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Methods for Treating Skin Pigmentation

Inactive Publication Date: 2008-10-09
SHAPIRO STANLEY S +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0098]Compound I, a trypsin and thrombin inhibitor, for example, inhibits melanosome transfer to keratinocytes. STI works by the same mechanism, The accumulation of undelivered melanosomes in the melanocytes could induce a negative feed back mechanism, that slows new melanosome formation. The production of TRP-1, the major glycoprotein in melanocytes, is down-regulated, which leads to destabilization of tyrosinase. This results in reduced melanin formation, and in a color switch to a lighter brown, as the ratio of TRP-1:TRP-2 is reduced. The melanosomes accumulation in the melanocyte after Compound I treatment, or after STI treatment, therefore, have reduced and altered melanin content, which adds to the whitening effect of compound I or STI.

Problems solved by technology

Many of these previous solutions have not been found acceptable.
Many of these compounds have been found to be quite irritating to the skin and therefore undesirable for use.
While the function of the TR is well documented, the biology of the PAR-2 has not yet been fully identified.

Method used

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  • Methods for Treating Skin Pigmentation
  • Methods for Treating Skin Pigmentation
  • Methods for Treating Skin Pigmentation

Examples

Experimental program
Comparison scheme
Effect test

example 1

Protease Inhibitors Affect Pigmentation

[0049]In order to study the possible roles of the PAR-2 pathway in pigmentation, an in vitro epidermal equivalent system was used. The epidermal equivalent system used contained melanocytes. One epidermal equivalent system which is useful in performing this study is the MelanoDerm system, available commercially from MatTek Co. This system contains human normal melanocytes, together with normal, human-derived epidermal keratinocytes, which have been cultured to form a multi layered, highly differentiated model of the human epidermis. In the following examples, equivalents were treated with test compounds for three days and samples were harvested on the fourth day after beginning of treatment. The harvested equivalents were stained with DOPA (a substrate for tyrosinase) and H&E (a standard histological stain) or with Fontana-Mason (F&M) staining, another stain known to those of skill in the art. F&M staining is a silver staining technique that cl...

example 2

A Protease-Activated Receptor is Involved in Pigmentation

[0055]Example 1 demonstrates that STI reduces pigmentation. STI inhibits trypsin. Because trypsin is known to activate TR and PAR-2, we tested the possible involvement of TR and PAR-2 in pigmentation. MelanoDerm human epidermal equivalents were treated with the TR and PAR-2 agonists and antagonists set forth in Table B below daily for three days. On the fourth day, the samples were harvested, fixed, and DOPA, H&E or F&M staining was performed. Histological and whole-equivalent examination revealed changes in pigmentation following the treatments. FIG. 2 depicts the results of this example. As shown therein, the PAR-2 peptide agonist SLIGRL induced pigmentation in individual melanocytes. Treatment with Compound I, an inhibitor of thrombin and trypsin, resulted in decreased pigmentation.

[0056]FIG. 3 shows the results of the studies set forth in this example, representing the level of pigmentation in MelanoDerm equivalents treate...

example 3

A Dose-Response Relation Between Protease-Activated Receptors Signaling and Melanogenesis

[0057]MelanoDerm equivalents were treated with increasing concentrations of SLIGRL, the PAR-2 peptide agonist, at 0, 10 and 50 μM in the same manner as set forth in Example 2. F&M staining was performed in the fourth day. As shown in FIG. 4A, increasing concentrations of SLIGRL, the PAR-2 activator, result in increased pigmentation. Trypsin, a PAR-2 activator, has the same effect. Treatment with increasing concentrations of Compound I, the thrombin and trypsin inhibitor, from 0.1 pM to 1 μM resulted in decreasing pigmentation (see FIG. 4A). Pretreatment of the equivalents with UVB irradiation increased melanogenesis, relative to untreated controls. Compound I was able to reduce this UVE-induced pigmentation as well (FIG. 4B). This example demonstrates a dose-response relation for increasing and decreasing pigmentation with the modulation of PAR-2 signaling. This example also demonstrates that Co...

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Abstract

This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway.

Description

1. FIELD OF THE INVENTION[0001]This invention is related to methods and compositions for bringing about skin pigmentation and / or for causing skin depigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin.2. BACKGROUND OF THE INVENTION[0002]Skin coloring has been of concern to human beings for many years. In particular, the ability to remove hyperpigmentation, such as found in age spots, freckles or aging skin generally, is of interest to individuals desiring a uniform complexion. In certain areas of the world, general body whitening is desirable. There are also hypopigmentation and hyperpigmentation disorders that are desirable to treat. Likewise, the ability to generate a tanned appearance without incurring photodamage due to solar radiation is important to many individuals. There have been many methods proposed to accomplish depigmentation, as well as to accomplish darken...

Claims

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Application Information

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IPC IPC(8): A61K38/06A61K8/00A61K8/14A61K8/37A61K8/39A61K8/41A61K8/42A61K8/44A61K8/46A61K8/49A61K8/64A61K8/67A61K8/96A61K8/97A61K36/48A61K36/81A61K36/899A61K38/46A61K45/00A61P17/16A61P43/00A61Q17/04A61Q19/00A61Q19/02A61Q19/04
CPCA61K8/14A61K8/41A61K8/42A61K8/44A61K8/46A61K8/4926A61K8/64A61K8/676A61K8/678A61K8/97A61Q19/02A61Q19/04A61K8/9789A61K8/9794A61P17/00A61P17/16A61P43/00A61K8/40A61K8/33
Inventor SHAPIRO, STANLEY S.SEIBERG, MIRINIEMIEC, SUSANKUNG, JOHN
Owner SHAPIRO STANLEY S
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