Objective(s): Growing evidence supports that isothiocyanates exert a wide range of bioactivities amongst of which is their capacity to interact with the epigenetic machinery in various cancers including melanoma. Our aim was to characterise the effect of sulforaphane and iberin on histone acetylation and methylation as a potential anti-melanoma strategy.
Methods: We have utilised an in vitro model of malignant melanoma [consisting of human (A375, Hs294T, VMM1) and murine (B16F-10) melanoma cell lines as well as a non-melanoma (A431) and a non-tumorigenic immortalised keratinocyte (HaCaT) cell line] exposed to sulforaphane or iberin. Cell viability was evaluated by the Alamar blue assay whilst total histone deacetylases and acetyltransferases activities were determined by the Epigenase HDAC Activity/Inhibition and EpiQuik HAT Activity/Inhibition assay kits, respectively. The expression levels of specific histone deacetylases and acetyltransferases together with those of lysine acetylation and methylation marks were obtained by western immunoblotting.
Results: Overall, both sulforaphane and iberin were able to (1) reduce cell viability, (2) decrease total histone deacetylase activity and (3) modulate the expression levels of various histone deacetylases as well as acetyl and methyl transferases thus modulating the acetylation and methylation status of specific lysine residues on histones 3 and 4 in malignant melanoma cells.
Conclusions: Our findings highlight novel insights as to how sulforaphane and iberin differentially regulate the epigenetic response in ways compatible with their anticancer action in malignant melanoma.
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http://dx.doi.org/10.1007/s00394-020-02227-y | DOI Listing |
Molecules
June 2024
National Centre for the Control and Evaluation of Medicines, Chemical Medicines Unit, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.
Sulforaphane is a chiral phytochemical with chemopreventive properties. The presence of a stereogenic sulfur atom is responsible for the chirality of the natural isothiocyanate. The key role of sulfur chirality in biological activity is underscored by studies of the efficacy of individual enantiomers as chemoprotective agents.
View Article and Find Full Text PDFBiochem Biophys Res Commun
September 2024
School of Pharmacy, Pacific University, 222 SE 8th Ave, Ste. 451, Hillsboro, OR, 97123, USA.
Goal: The long-term goal of our research is to develop safe and effective soluble epoxide hydrolase (sEH) inhibitors. The objective of this study is to evaluate the potency and selectivity of six natural isothiocyanates (ITCs) as sEH inhibitors.
Methods: Molecular docking was used to model likely interactions between the ligands and receptors.
Curr Res Food Sci
March 2023
Food Science Institute, Zhejiang Academy of Agricultural Sciences, Hangzhou, 310021, China.
Vegetables from the species are excellent sources of glucosinolates (GLSs), the precursors of health-promoting isothiocyanates (ITCs). Fermentation enhances the biotransformation of GLSs into potential bioactive ITCs. To explore the biotransformation of GLSs during fermentation, the changes in GLSs during the fermentation of two species (i.
View Article and Find Full Text PDFBiomed Pharmacother
June 2023
Posgrado en Botánica, Colegio de Postgraduados Campus Montecillo, Carretera México-Texcoco Km. 36.5, Montecillo, Texcoco 56230, Estado de México, Mexico. Electronic address:
Raphanus sativus L. (Brassicaceae), commonly known as radish, is consumed worldwide as a vegetable. However, its benefits on mental health are unknown.
View Article and Find Full Text PDFNutrients
August 2021
School of Biological and Population Health Sciences, Nutrition Program, Oregon State University, 101 Milam Hall, Corvallis, OR 97331, USA.
Isothiocyanates, such as sulforaphane and iberin, derived from glucosinolates (GLS) in cruciferous vegetables, are known to prevent and suppress cancer development. GLS can also be converted by bacteria to biologically inert nitriles, such as sulforaphane-nitrile (SFN-NIT) and iberin-nitrile (IBN-NIT), but the role of the gut microbiome in this process is relatively undescribed and SFN-NIT excretion in humans is unknown. An ex vivo fecal incubation model with in vitro digested broccoli sprouts and 16S sequencing was utilized to explore the role of the gut microbiome in SFN- and IBN-NIT production.
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