Brassinin Abundant in Brassicaceae Suppresses Melanogenesis through Dual Mechanisms of Tyrosinase Inhibition

Abstract

Brassinin is a phytoalexin abundant in plants, especially in cabbage, and has been reported to act as an anti-cancer and anti-inflammatory agent. However, limited studies are available to elucidate the functionalities of brassinin. Here, we tested the effects of brassinin on melanogenesis using cell-free and cell-based biochemical analysis and docking simulation. Cell-free experiments exhibited that brassinin has antioxidant and anti-tyrosinase activities. When applied to B16F10 cells stimulated with a melanogenesis inducer α-MSH, brassinin pretreatment significantly reduced melanin accumulation and cellular tyrosinase activity. Docking simulation indicates that the docking score of brassinin to the binding pocket of tyrosinase is better than that of kojic acid or arbutin, anti-melanogenic positive controls, indicating that brassinin inhibits melanogenesis at least partially by binding to and inactivating tyrosinase. In addition, qPCR results showed that brassinin reduced tyrosinase mRNA levels. Together, these results suggest that brassinin exerts anti-melanogenesis effects by inhibiting both the activity and mRNA expression levels of tyrosinase. Therefore, our study showed that brassinin has the potential to be used in pharmaceutical or cosmetic products for depigmentation.