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Melanotan-2: Scientific Tanning and Skin Protection

network_duotone By Cocer Peptides     network_duotone 1 month ago 


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Overview of Melanotan-2


Melanotan-2 (MT-2) is a synthetic cyclic heptapeptide and an analog of α-melanocyte-stimulating hormone (α-MSH). It plays a crucial role in regulating melanocyte-stimulating hormone receptors. MT-2 primarily exerts its effects by interacting with the melanocortin 1 receptor (MC1R). MC1R is widely expressed on the surface of melanocytes. Upon binding to this receptor, MT-2 initiates a series of intracellular signaling pathways, ultimately promoting melanin synthesis and distribution, thereby causing changes in skin color.


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Figure 1 The structure of melanotan II.




Applications of Melanotan-2 in Scientific Tanning


(1) Tanning Mechanism

Promotion of melanin synthesis: After MT-2 binds to MC1R, it activates adenylate cyclase, promoting the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP) within the cell. cAMP acts as a second messenger to activate protein kinase A (PKA), which in turn phosphorylates the small eye-related transcription factor (MITF). MITF is a key regulatory factor in melanin synthesis, upregulating the expression of melanin synthesis enzymes such as tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2), thereby accelerating melanin synthesis.


Distribution and transport of pigment granules: In addition to promoting melanin synthesis, MT-2 also influences the distribution and transport of pigment granules within melanocytes. Studies have shown that MT-2 can regulate the activity of cytoskeletal-related proteins, promoting the movement of melanosomes (organelles containing melanin) from the central region of melanocytes to the peripheral areas of the cell, ultimately transferring melanin to keratinocytes, thereby darkening the overall skin color.


(2) Comparison with traditional tanning methods

Limitations of traditional tanning methods: Traditional tanning methods primarily include sun exposure and the use of tanning beds. However, prolonged exposure to ultraviolet (UV) radiation—whether from natural sunlight or UV emitted by tanning beds—carries significant risks. UV radiation can cause sunburn and redness, and long-term exposure increases the risk of skin cancer while accelerating skin aging, leading to wrinkles and sagging.


Advantages of Melanotan-2 Tanning: In contrast, the tanning process induced by MT-2 does not rely on UV exposure, theoretically reducing the risk of UV-related skin damage. Additionally, MT-2 can cause noticeable changes in skin color in a relatively short time, and this tanning effect is relatively uniform, avoiding the uneven skin tone issues caused by improper sun exposure or tanning bed use.


(3) Application Examples of MT-2 Tanning

Fitness and Bodybuilding: MT-2 is widely used among fitness and bodybuilding enthusiasts. These individuals often seek tanning to highlight muscle definition, making their physique more striking on stage or during training demonstrations. MT-2 enables them to achieve the desired bronze skin tone quickly without relying on prolonged sun exposure or frequent tanning bed use, thereby enhancing their overall appearance.


Everyday Tanning Enthusiasts: Some individuals seeking a fashionable tanned complexion also express interest in MT-2. For those who desire healthy, bronze-toned skin but are concerned about the potential skin damage from traditional tanning methods, MT-2 offers an alternative option. They can perform the tanning process at home using appropriate application methods, which is relatively convenient.




The Role of Melanotan-2 in Skin Protection


(1) Photoprotective Mechanism

Melanin's photoprotective effect: The melanin synthesized by MT-2 absorbs ultraviolet (UV) energy, converting it into harmless thermal energy and dissipating it, thereby reducing direct damage to skin cell DNA caused by UV radiation. Melanin acts as a natural protective umbrella for the skin, effectively absorbing and scattering UV radiation before it reaches deep skin cells, thereby lowering the risk of UV-induced gene mutations and cellular damage.


Enhanced antioxidant activity: MT-2 not only promotes melanin synthesis but also upregulates the activity of antioxidant enzymes within skin cells, such as superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). These antioxidant enzymes can eliminate reactive oxygen species (ROS) generated by UV irradiation, such as superoxide anions and hydroxyl radicals, preventing ROS from causing oxidative damage to lipids, proteins, and DNA in skin cells, thereby maintaining normal cellular physiological functions.


(2) Skin Protection

In some animal experiments, experimental animals were treated with MT-2 before being exposed to UV radiation. The results showed that the degree of sunburn in the MT-2-treated group was significantly reduced, with decreased areas of erythema and inflammatory cell infiltration. Additionally, levels of DNA damage markers such as 8-hydroxy-2'-deoxyguanosine (8-OHdG) in skin cells were reduced, indicating that MT-2 has a certain protective effect against UV-induced DNA damage.


In vitro cell experiments also confirmed the skin protective efficacy of MT-2. Cultured melanocytes or keratinocytes were pretreated with MT-2 and then exposed to a UV environment. This study found that cell survival rates increased, apoptosis rates decreased, and antioxidant enzyme activity within cells enhanced, with improvements in oxidative stress-related indicators. This indicates that MT-2 can enhance the skin's resistance to UV damage at the cellular level.


(3) Application Scenarios  

For individuals frequently engaged in outdoor activities, such as athletes and outdoor workers, prolonged sun exposure exposes them to a higher risk of UV damage. The potential skin protective effects of MT-2 can provide them with an additional protective measure. By appropriately using MT-2 in combination with traditional sun protection measures such as applying sunscreen and wearing a sun hat, skin protection against UV radiation can be further enhanced, reducing the risk of sunburn, tanning, and skin diseases associated with long-term UV exposure. Certain populations, due to genetic factors, a history of prolonged UV exposure, or specific skin conditions, are at higher risk for skin cancer. The photoprotective and antioxidant effects of MT-2 may help reduce their risk of developing skin cancer.




Current Research Status


Currently, there is a relatively thorough understanding of the mechanism of action of MT-2, including its binding pattern with the MC1R receptor, activation of intracellular signaling pathways, and regulation of melanin synthesis and distribution. However, some details remain to be further explored, such as the long-term effects of MT-2 on melanocyte metabolism and its differential mechanisms of action in individuals with different skin types.




Conclusion


Melanotan-2 plays a significant role in scientific tanning and skin protection. From a cosmetic perspective, it offers individuals seeking a healthy skin tone a scientific tanning method that does not rely on UV exposure, thereby avoiding the sunburn and skin aging associated with traditional sunbathing and tanning beds, and meeting the dual demands for safety and efficiency in tanning. In terms of skin protection, MT-2 builds a defense against UV rays by promoting melanin synthesis and enhancing antioxidant capacity, offering new options for those engaged in outdoor activities.




Sources


[1] McKenzie N, Gonzalez N, Huang C, et al. Poster presentationsPS09 User experiences of Melanotan II injection for tanning[J]. British Journal of Dermatology, 2024,191(Supplement_1):i179-i180.DOI:10.1093/bjd/ljae090.380.


[2] Wekwejt P, Wojda U, Kiryk A. Melanotan-II reverses memory impairment induced by a short-term HF diet[J]. Biomedicine & Pharmacotherapy, 2023,165:115129.DOI:10.1016/j.biopha.2023.115129.


[3] Gilhooley E, Daly S, McKenna D. Melanotan II User Experience: A Qualitative Study of Online Discussion Forums[J]. Dermatology, 2021,237(6):995-999.DOI:10.1159/000514492.


[4] Gao L, Yu Z, Meng D, et al. Analogue of Melanotan II (MTII): A Novel Melanotropin with Superpotent Action on  Frog Skin[J]. Protein and Peptide Letters, 2015,22(8):762-766.DOI:10.2174/0929866522666150622101944.


[5] Ryakhovsky V V, Khachiyan G A, Kosovova N F, et al. The first preparative solution phase synthesis of melanotan II[J]. Beilstein Journal of Organic Chemistry, 2008,4:39.DOI:10.3762/bjoc.4.39.


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