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Mar Drugs ; 15(5)2017 May 13.
Artículo en Inglés | MEDLINE | ID: mdl-28505073

RESUMEN

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.


Asunto(s)
Organismos Acuáticos , Bacillus/metabolismo , Hexanonas/farmacología , Animales , Línea Celular Tumoral , Supervivencia Celular , Relación Dosis-Respuesta a Droga , Epidermis/efectos de los fármacos , Hexanonas/química , Hexanonas/metabolismo , Humanos , Levodopa/administración & dosificación , Levodopa/farmacología , Melaninas/metabolismo , Melanoma/metabolismo , Ratones , Estructura Molecular , Pigmentación/efectos de los fármacos
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