What Is an Endothelin Receptor Antagonist?

Melanin is synthesized in melanocytes, it is easy to think: if there are no melanocytes, then there will be no problems, just like without a "factory", it is impossible to produce melanin, wouldn't it be wonderful? Therefore, in the development of the melanin metabolism mechanism, not everyone is locked in the tyrosine metabolism process, but another way.

Endothelin antagonist

Right!

Melanin is synthesized in melanocytes, it is easy to think: if there are no melanocytes, then there will be no problems, just like without a "factory", it is impossible to produce melanin, wouldn't it be wonderful? Therefore, in the development of the melanin metabolism mechanism, not everyone is locked in the tyrosine metabolism process, but another way.

Chinese name

Endothelin antagonist

Time

Mid 1990s

Features

Whitening

Category

Vasoactive peptide

In the mid-1990s, studies found that other cytokines did exist, which stimulated the division and proliferation of melanocytes, which opened a new page in the formulation of whitening and freckle products. Endothelin is one of them. The effect provided a new idea for the development of whitening and freckle products.

Endothelin (ET) is by far the most active and long-lasting active peptide that contracts blood vessels. There are three types of endothelin in humans, of which ET-1 is mainly expressed in endothelial cells and regulates local blood vessels by paracrine means. Tension. Although it has been known for a long time that endothelin has different effects on many cells, because the coronary arteries are very sensitive to endothelin, the research on endothelin is focused on the heart and blood vessels.

Studies have found that skin keratinocytes can also release endothelin, and the amount of endothelin released by keratinocytes after the skin is exposed to ultraviolet rays also increases. Then it was found that there are special receptors on melanocytes that can bind to endothelin. After being accepted by the receptors on the melanocyte membrane, endothelin stimulates the differentiation, proliferation and activation of tyrosinase activity of melanocytes, thereby making melanin sharp increase. The experiment also proved that endothelin can not only stimulate melanocytes to produce melanin, but also melanocyte dividing agent, and its cell signal transmission mechanism has begun to take shape.

If you add a substance that can fight the effects of endothelin, you can eliminate the negative effects of endothelin. This thing is called an endothelin antagonist.

The mechanism of action of endothelin antagonists is different from the inhibition of tyrosinase activity, and the whitening and freckle effect is achieved by inhibiting the regulation of endothelin on the proliferation of melanocytes.

Endothelin and the aforementioned tyrosinase, dopachrome isomerase, and DHICA oxidase are collectively referred to as " trienzyme one." The endothelin antagonist sounds wonderful, and formulators have the feeling of "a dark village and a bright village."

Endothelin antagonists are not new and have a long history in the application of hypertension and heart disease :) However, this type of antagonists with many cardiovascular applications are not all able to act on endothelins secreted by the skin and cannot be transplanted directly When it comes to cosmetics, this is really puzzling. So, the long journey to find endothelin antagonists for cosmetics began. It has now been reported that some useful endothelin antagonists have been discovered.

Because the endothelin antagonist is a relatively new raw material, there is very little related information, and the thunderstorm feels like a small raindrop. Although some manufacturers sell this type of additives, the technical materials are very confidential and secretive, which makes people feel a bit uneasy to use. There are also some products on the market that have been labeled with "endothelin antagonists". It is only known whether this is true.

Having said that, the mechanism by which endothelin regulates melanocyte proliferation is correct, and endothelin antagonists are still something to look forward to. It is believed that in the near future, more research results will be mature and applied to whitening and freckle cosmetics.

An endothelin antagonist whose active ingredient is a prostanoic acid derivative in which the alpha chain has 8 or more main chain carbon atoms.

An endothelin antagonist whose active ingredient is a prostanoic acid derivative in which the alpha chain has 8 or more main chain carbon atoms.

Endothelin antagonists are important skin lightening agents discovered in the 1990s. It can be extracted from the natural plant-chamomile, or it can be prepared by biological fermentation. Its whitening effect is through inhibiting endothelin to activate tyrosinase and inhibiting endothelin to promote melanocyte differentiation and reduce uneven pigment distribution. Its effect is 4 times that of general preparations, so it has received considerable attention.

In the early 1990s, Japan's Imokawa et al. Found that under ultraviolet radiation, keratinocytes release a cytokinin. When it is accepted by the melanocyte receptor, it stimulates melanocyte proliferation and stimulates tyrosinase activity. Thus increasing the amount of melanin synthesis. This cytokinin is endothelin.

Endothelin antagonist is a substance that fights endothelin and inhibits melanin production. Some people abroad have extracted endothelin antagonists from the European herb chamomile, and in vivo and in vitro experiments have shown the following three effects:

High efficiency: under the action of chamomile extract, an endothelin antagonist, endothelin can not be connected with the acceptor on melanin cells, so no additional melanin will be formed;

Rapid depigmentation: Because tyrosinase exists in the melanin of melanocytes, tyrosinase inhibitors must pass through the barrier of 4 layers (that is, the stratum corneum, deep epidermis, melanocyte membrane, and melanin membrane) to inhibit the effect Because the action point of the endothelin antagonist is outside the melanocyte membrane, it only needs to pass through two barriers to exert its effect. This is why for the elimination of pigmentation caused by ultraviolet rays, the use of endothelin is better than tyrosine. The reason that enzyme inhibitors are 4 times faster;

Uniform melanin distribution: Due to the formation of extracellular melanin caused by ultraviolet irradiation, skin pigmentation and uneven pigment distribution, and the situation will be fundamentally improved after using endothelin antagonists. However, some people think that the endothelin contained in placenta can be used to treat depigmented spots.