skin pigmentation

Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), demonstrating EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) across species such as human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is applied in the study of skin pigmentation.

γ-Oryzanol (Gamma-Oryzanol) is a natural nutrient extract isolated from rice bran oil that contains a mixture of sterols and ferulic acids, which may aid in the destruction of free radicals in the skin. It has recently been researched for its ability to slow the progress of melanin pigmentation by intercepting the ultraviolet rays at the skin's surface and hindering their transmission.

Azelaic acid (Anchoic acid) is a component of hair and skin conditioners and is produced by the ozonolysis of oleic acid. Azelaic acid has bacteriostatic activity against Propionibacterium acnes and Staphylococcus epidermidis by inhibiting protoprotein synthesis in microbial cells. Azelaic acid also has the ability to inhibit pigmentation due to its free radical scavenging action.

Nonapeptide-1 (Melanostatine™ 5) can inhibit the synthesis of melanin, which makes it of interest for treating certain skin conditions.

Vinaginsenoside R4 was isolated from the leaves of hydroponically grown ginseng. It inhibits melanin biosynthesis and enhances pigmentation in zebrafish without any cytotoxic effects on melan-a cells. It may have potential as a new skin whitening compound.

(R)-(+)-Deoxyarbutin, an isomer of deoxyarbutin, acts as a tyrosinase inhibitor. Effective at a concentration of 21 µM, it diminishes tyrosinase activity and has been demonstrated to lighten the skin in hairless guinea pigs with dark, medium, and light pigmentation when applied at a 1% concentration.

Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, functions as a selective and competitive antagonist of the melanocortin 1 receptor (MC1R) with a binding affinity (K i) of 40 nM. It effectively inhibits α-MSH-induced increases in intracellular cyclic AMP (cAMP) and melanosome dispersion in melanocytes, showcasing inhibitory concentrations (IC 50) of 2.5 nM and 11 nM, respectively. By inhibiting melanin synthesis, Nonapeptide-1 acetate salt finds application in research related to skin pigmentation, adrenal gland steroid production regulation, and skin cancer [1] [2] [3].