Ishophloroglucin A Isolated from Ishige okamurae Suppresses Melanogenesis Induced by α-MSH: In Vitro and In Vivo.

Xining Li,Bomi Ryu,Jae-Young Oh,Hye-Won Yang,You-Jin Jeon,Yunfei Jiang

doi:10.3390/md18090470

Abstract

Diphlorethohydroxycarmalol (DPHC) isolated from Ishige okamurae (IO) showed potential whitening effects against UV-B radiation. However, the components of IO as well as their molecular mechanism against α-melanocyte-stimulating hormone (α-MSH) have not yet been investigated. Thus, this study aimed to investigate the inhibitory effects of Ishophloroglucin A (IPA), a phlorotannin isolated from brown algae IO, and its crude extract (IOE), in melanogenesis in vivo in an α-MSH-induced zebrafish model and in B16F10 melanoma cells in vitro. Molecular docking studies of the phlorotannins were carried out to determine their inhibitory effects and to elucidate their mode of interaction with tyrosinase, a glycoprotein related to melanogenesis. In addition, morphological changes and melanin content decreased in the α-MSH-induced zebrafish model after IPA and IOE treatment. Furthermore, Western blotting results revealed that IPA upregulated the extracellular related protein expression in α-MSH-stimulated B16F10 cells. Hence, these results suggest that IPA isolated from IOE has a potential for use in the pharmaceutical and cosmetic industries.

Highlights

Marine algae have gained immense attention from the functional food, cosmetics, and pharmaceutical industries as they utilize various bioactive compounds such as phlorotannins, fucoidans, polysaccharides, and proteins [1,2,3,4,5,6,7]
We aimed to investigate the inhibitory effect of Ishophloroglucin A (IPA) and Ishige okamurae (IO) crude extract (IOE) in tyrosinase activity and melanogenesis on α-melanocyte-stimulating hormone (α-MSH)-induced zebrafish in vivo and B16F10 melanoma cells in vitro in order to evaluate their potential use in treating skin pigmentation and melanoma
30 μg/mL IOE inhibited pigmentation to a point that resembled the blank group (Figure 4D). These results suggest that IPA and IOE downregulated tyrosinase activity and that this inhibitory effect may lead to decreased cellular melanin synthesis in B16F10 cells

Summary

Introduction

Marine algae have gained immense attention from the functional food, cosmetics, and pharmaceutical industries as they utilize various bioactive compounds such as phlorotannins, fucoidans, polysaccharides, and proteins [1,2,3,4,5,6,7]. Diphlorethohydroxycarmalol (DPHC), was assessed for anti-melanogenesis activity induced by UV-B radiation in an in vitro model [8], no further studies were performed to explain the interaction between DPHC and melanogenesis-related proteins. A novel polyphenol compound, Ishophloroglucin A (IPA) [9], was evaluated for its interaction with tyrosinase in a molecular docking study, compared with that of DPHC. Molecular docking is an efficient computational method to predict the potential binding mode of small molecules or ligands within the active site of a protein or receptor of a known three-dimensional structure for studying their interaction patterns or for drug design [10,11,12]. Previous studies have reported the interaction site and energy value of tyrosinase enzyme as investigated by molecular docking studies [13,14].

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Conclusion