Comparative study on melanin production and collagen expression profile of polyphenols and their glycosides

A total of twenty different polyphenol aglycones and their biochemically synthesized glycoside derivatives were accessed for cell toxicity, collagen synthesis and melanin content inhibition assays to illustrate the double-edged sword role of glycobiology, in particular, modification of hydroxyl group in polyphenol structure without glycone moiety over anti-aging and defense to oxidative stress in skin dermatology. All molecules at (0.1-200) µM concentration inhibited cell growth in a dose dependent manner on human dermal fibroblast (HDF) and melanoma skin cancer (B16F10) cells. At lower concentrations of (0.1-10) µM, most of the molecules were nontoxic to HDF cells, while the same molecules were toxic to B16F10 cells except astilbin (6), baicalein (13), baicalein 7-O-β-D-glucoside (14) and mangostin (18). Results showed that two molecules, quercetin (1) and diosmin (17), inhibited melanogenesis in α-melanocyte stimulating hormone (α-MSH)-stimulated melanoma skin cancer cells (B16F10) in comparison to the control at 0.1 µM concentration, indicating the possible use of these molecules in skin-whitening products. Similarly, the maintenance of collagen in HDF cells was found to be highly activated by the compound, kaempferol (11), at 1.0 µM concentration, at which the cell viability was above 95%. Compound 1, apigenin 7-O-β-D-glucoside (10) andbaicalein (13) exhibited comparable collagen biosynthesis activity to control with significantly low cell toxicity