Abstract
Bioactivity-guided isolation of a crude extract from a culture broth of Bacillus sp. has led to the isolation of (-)-4-hydroxysattabacin (1). The inhibitory effect of (-)-4-hydroxysattabacin (1) was investigated on melanogenesis in the murine melanoma cell line, B16F10, and human melanoma cell line, MNT-1, as well as a pigmented 3D-human skin model. (-)-4-Hydroxysattabacin treatment decreased melanin contents in a dose-dependent manner in α-melanocyte stimulating hormone (α-MSH)-stimulated B16F10 cells. Quantitative real time PCR (qRT–PCR) demonstrated that treatment with (-)-4-hydroxysattabacin down-regulated several melanogenic genes, including tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2) while their enzymatic activities were unaffected. The anti-melanogenic effects of (-)-4-hydroxysattabacin were further demonstrated in a pigmented 3D human epidermal skin model, MelanodermTM, and manifested as whitening and regression of melanocyte activation in the tissue.
Highlights
The skin plays a vital role as a physiological barrier for the inner body against harmful factors.Keratinocytes and melanocytes constitute the epidermis, the outermost layer of the skin, wherein melanin, a key molecule for the defense against harmful UV irradiation and reactive oxygen species (ROS), is synthesized [1]
A number of compounds, such as hydroquinone, arbutin, and kojic acids have been employed as hypopigmenting agents but skin irritation, contact dermatitis, or ochronosis may occur following the chronic exposure to these compounds
Comparison of nuclear magnetic resonance (NMR) spectroscopic data of 2 to those of the reported one permitted that the planar structure of 2 was identified as sattabacin [16]
Summary
The skin plays a vital role as a physiological barrier for the inner body against harmful factors. Α-Melanocyte stimulating hormone (α-MSH), a potent stimulator of melanin formation in most cultured murine melanoma cell lines and some human melanoma lines, acts through the transcriptional regulation of these melanogenic enzymes as do other pro-melanogenic stimuli such as UV and adrenocorticotropin (ACTH) [11,12]. Regulation of these enzymes may be an important strategy for preventing cutaneous pigmentation [13,14,15]. The mechanism underlying the anti-melanogenic effects of (-)-4OH-ST (1) was elucidated along with confirmation of its activity in a 3D pigmented human epidermis model to propose it as a new natural hypopigmenting agent
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