Melanin inhibition

Since the melanin formation assay was run against a cell viability assay, the activity peak maximum at fraction Dll was most likely due to cytotoxicity. The dereplication of another active peak located from fractions D7 to D2 is illustrated in Figure 9. Every active fraction was analyzed by HPLC/PDA/MS. There was a peak located at Rt=16.33 min in the LC/MS total ion chromatogram of active fractions. This peak showed the same pattern of increasing to decreasing intensity as the trend exhibited by the melanin inhibition activities of those fractions. 

Macro affinity, 160 Magnus, Rudolph, 34 Materia Medica, 147 Mathematical models, 42-43 Maximal fractional inhibition, 65 Maximal response of agonists, 85, 98 Medicinal chemistry, 1-2 Melanin, 50 Melanophores... 

N-ras, H-ras, K-ras Signal transduction pathway Inhibition of cell proliferation and colony formation change in morphology, enhanced melanin synthesis decrease of in vivo tumorigenicity... 

MDR-ABC Transporters Mechanism-based Inhibition Meglitinide-related Compounds Melanin-concentrating Hormone Melanocortins... 

Hydroquinone inhibits melanin production when applied to the skin. The effect is reversible by exposure to ultraviolet light. 

Skin lighteners, freckle and age spot removers, and other remedies for hyperpigmentation are not actually bleaches like the products listed so far. The active ingredient is hydroquinone, which inhibits melanin formation when applied to the skin. Since the effect is easily reversed by exposure to sunlight or ultraviolet light, a sunscreen is usually included in the formula. 

Khan MTH (2007) Recent Advances on the Sugar-Derived Heterocycles and Their Precursors as Inhibitors Against Glycogen Phosphorylases (GP). 9 33-52 Khan MTH (2007) Heterocyclic Compounds Against the Enzyme Tyrosinase Essential for Melanin Production Biochemical Features of Inhibition. 9 119-138 Khan MTH (2007) Molecular Modeling of the Biologically Active Alkaloids. 10 75-98 Khan MTH, Ather A (2007) Microbial Transformation of Nitrogenous Compoimds. 10 99-122... 

Heterocyclic Compounds against the Enzyme Tyrosinase Essential for Melanin Production Biochemical Features of Inhibition... 

Seiji, M.T., Yoshida, T., Itakura, H. and Irimajiri, T. (1969). Inhibition of melanin formation by sulfhydryl compounds. J. Invest. Dermatol. 52, 280-286. 

Hydroquinone interferes with the production of the pigment melanin by epidermal melanocytes through at least two mechanisms it competitively inhibits tyrosinase, one of the principal enzymes responsible for converting tyrosine to melanin, and it selectively damages melanocytes and melanosomes (the organelles within which melanin is stored). 

C. Hydroquinone inhibits the enzyme tyrosine kinase, which converts tyrosine to melanin. It also damages melanocytes. Becaplermin (A) is a recombinant human platelet-derived growth factor that is useful in enhancing wound healing. Etanercept (B) is a recombinant fusion protein approved for treatment of psoriatic arthritis and rheumatoid arthritis. Botulinum toxin (D) is a purified form of bofu-linum foxin fype A approved for fherapy of blepharospasm and sfrabismus. 

The mechanism of action of these compounds appears to involve inhibition of the enzyme tyrosinase, thus interfering with the biosynthesis of melanin. In addition, monobenzone may be toxic to melanocytes, resulting in permanent loss of these cells. Some percutaneous absorption of these compounds takes place, because monobenzone may cause hypopigmentation at sites distant from the area of application. Both hydroquinone and monobenzone may cause local irritation. Allergic sensitization to these compounds can occur. Prescription combinations of hydroquinone, fluocinolone... 

Three compounds have been developed that utilise the inhibition of melanin biosynthesis as the basis of disease control (Figure 4.18). The first and most valuable of these is tricyclazole. Tricyclazole is readily absorbed by the foliage and roots of rice plants and redistributed acropetally. On treated plants, conidial germination of P. oryzae and... 

Tricyclazole is reported to inhibit the melanin biosynthesis pathway between 1,3,8 trihydoxynaphthalene and vermelone whereas chromatographic analysis of P. oryzae culture media indicates that KTU 3616 treatment stimulates the accumulation of the intermediate, scytalone. 

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