Optimization and application of a fluorimetric assay for the identification of histone deacetylase inhibitors from plant origin

Krasteva, Stanimira; Heiss, Elke H.; Krenn, Liselotte

doi:10.3109/13880209.2010.536556

Cited by 7 publications

(5 citation statements)

References 26 publications

(36 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…HDAC5 (Histone Deacetylase 5, FC = 1.550; q = 0.099) can influence the critical role of histones in transcriptional regulation, cell cycle progression and developmental events. The upregulation of HDAC5 in the control group is in agreement with the reported inhibitory role of tannic acid on HDACs [82]. These findings may be related to previously reported anti-proliferative and pro-apoptotic effects of hydrolysable tannins [83].…”

Section: Tannin Effect On Transcriptomesupporting

confidence: 91%

Muscle Transcriptome Analysis Reveals Molecular Pathways Related to Oxidative Phosphorylation, Antioxidant Defense, Fatness and Growth in Mangalitsa and Moravka Pigs

Núñez

Radović

Savić

et al. 2021

Animals

View full text Add to dashboard Cite

This work was aimed at evaluating loin transcriptome and metabolic pathway differences between the two main Serbian local pig breeds with divergent characteristics regarding muscle growth and fatness, as well as exploring nutrigenomic effects of tannin supplementation in Mangalitsa (MA) pigs. The study comprised 24 Mangalitsa and 10 Moravka (MO) males, which were kept under identical management conditions. Mangalitsa animals were divided in two nutritional groups (n = 12) receiving a standard (control) or tannin–supplemented diet (1.5%; MAT). Moravka pigs were fed the standard mixture. All animals were slaughtered at a similar age; 120 kg of average live weight (LW) and loin tissue was used for RNA-seq analysis. Results showed 306 differentially expressed genes (DEGs) according to breed, enriched in genes involved in growth, lipid metabolism, protein metabolism and muscle development, such as PDK4, FABP4, MYOD1 and STAT3, as well as a relevant number of genes involved in mitochondrial respiratory activity (MT-NDs, NDUFAs among others). Oxidative phosphorylation was the most significantly affected pathway, activated in Mangalitsa muscle, revealing the basis of a different muscle metabolism. Also, many other relevant pathways were affected by breed and involved in oxidative stress response, fat accumulation and development of skeletal muscle. Results also allowed the identification of potential regulators and causal networks such as those controlled by FLCN, PPARGC1A or PRKAB1 with relevant regulatory roles on DEGs involved in mitochondrial and lipid metabolism, or IL3 and TRAF2 potentially controlling DEGs involved in muscle development. The Tannin effect on transcriptome was small, with only 23 DEGs, but included interesting ones involved in lipid deposition such as PPARGC1B. The results indicate a significant effect of the breed on muscle tissue gene expression, affecting relevant biological pathways and allowing the identification of strong regulatory candidate genes to underlie the gene expression and phenotypic differences between the compared groups.

show abstract

Section: Tannin Effect On Transcriptomesupporting

confidence: 91%

Muscle Transcriptome Analysis Reveals Molecular Pathways Related to Oxidative Phosphorylation, Antioxidant Defense, Fatness and Growth in Mangalitsa and Moravka Pigs

Núñez

Radović

Savić

et al. 2021

Animals

View full text Add to dashboard Cite

show abstract

“…Other naturally occurring HDACi have been isolated from fungi (e.g., depudecin and trapoxin A and B) and marine life (e.g., largazole and azumamides). The HDAC activity of these novel marine natural products can occur at nanomolar concentrations [ 49 , 115 , 116 ]. Given their rich source of biologically active compounds, extensive efforts have also been undertaken to identify novel plant-derived HDACi.…”

Section: Hdac Inhibitorsmentioning

confidence: 99%

“…[ 136 ] demonstrated that green tea polyphenols, of which the major constituent is epigallocatechin-3-gallate, can inhibit class I HDACs to induce cell cycle arrest and apoptosis. The continued development of high throughput HDACi assays will help to identify novel plant polyphenols which have HDACi activity and further elucidate the particular HDACs they restrict [ 115 ].…”

Section: Dietary Hdac Inhibitors As Therapeuticsmentioning

confidence: 99%

The Role of Dietary Histone Deacetylases (HDACs) Inhibitors in Health and Disease

2014

View full text Add to dashboard Cite

Modification of the histone proteins associated with DNA is an important process in the epigenetic regulation of DNA structure and function. There are several known modifications to histones, including methylation, acetylation, and phosphorylation, and a range of factors influence each of these. Histone deacetylases (HDACs) remove the acetyl group from lysine residues within a range of proteins, including transcription factors and histones. Whilst this means that their influence on cellular processes is more complex and far-reaching than histone modifications alone, their predominant function appears to relate to histones; through deacetylation of lysine residues they can influence expression of genes encoded by DNA linked to the histone molecule. HDAC inhibitors in turn regulate the activity of HDACs, and have been widely used as therapeutics in psychiatry and neurology, in which a number of adverse outcomes are associated with aberrant HDAC function. More recently, dietary HDAC inhibitors have been shown to have a regulatory effect similar to that of pharmacological HDAC inhibitors without the possible side-effects. Here, we discuss a number of dietary HDAC inhibitors, and how they may have therapeutic potential in the context of a whole food.

show abstract

“…For this reason, tannins are reported to interfere with enzyme-based assays (Wall et al 1996) and in the purification process. Thus, the detannification of tannin-rich extracts is essential before performing assays in order to avoid false-positive results (Krasteva et al 2011) and to facilitate purification. The modified detannification process of the crude extract yielded the dichloromethane extract (CtE 1, 81% inhibition at 75 µg/mL), which -from the dose-response curve obtained at different dilutions of the extract -gave the IC 50 value of 40.16 ug/mL.…”

Section: Resultsmentioning

confidence: 99%

α-Glucosidase Inhibitors from the Bark Extract of Ethno-Antidiabetic Ceriops tagal (Perr.) C.B. Rob

Canusa

Lawag²,

Villaflores

et al. 2021

Philipp J Sci

View full text Add to dashboard Cite

The bark of Ceriops tagal has been used in the Philippines for folk treatment of diabetes mellitus (DM). Through an α-glucosidase inhibition assay guided isolation, constituents from the detannified methanolic bark extract were isolated and identified to be methyl 2,4-dihydroxy-3,6- dimethyl benzoate (1), isopimar-7-ene-15S,16-diol (2), betulinic acid (3), lupeol (4), and methyl 2,4-dihydroxy-6-methyl benzoate (5). Compounds 3 (IC50 = 5.31 μM) and 4 (IC50 = 55.84 μM) showed a more potent activity against α-glucosidase than the positive control, 1-deoxynojirimycin(IC50 = 79.16 μM). This is the first report on the presence of the weakly active compounds (1,2, and 5) (IC50 > 75 μM) in the genus Ceriops and the first report on the biological activity ofCompound 2. Enzyme kinetic studies suggested that betulinic acid is an uncompetitive type ofinhibitor, with lupeol as a non-competitive type. This study provides evidence on the possiblemechanism of the antidiabetic property of C. tagal associated with its traditional use. It supportsthe possible utilization of the bark for development to prevent or treat diabetes.

show abstract

Optimization and application of a fluorimetric assay for the identification of histone deacetylase inhibitors from plant origin

Cited by 7 publications

References 26 publications

Muscle Transcriptome Analysis Reveals Molecular Pathways Related to Oxidative Phosphorylation, Antioxidant Defense, Fatness and Growth in Mangalitsa and Moravka Pigs

Muscle Transcriptome Analysis Reveals Molecular Pathways Related to Oxidative Phosphorylation, Antioxidant Defense, Fatness and Growth in Mangalitsa and Moravka Pigs

The Role of Dietary Histone Deacetylases (HDACs) Inhibitors in Health and Disease

α-Glucosidase Inhibitors from the Bark Extract of Ethno-Antidiabetic Ceriops tagal (Perr.) C.B. Rob

Contact Info

Product

Resources

About