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α-Glucosidase inhibition: (a) inhibition performed by extracts obtained from pulp (n = 6); (b) inhibition performed by extracts obtained from peel (n = 6); (c) inhibition performed by sample 5 for DEPe and DEPu, sample 6 for LEPe and LEPu, and acarbose in a concentration dependent manner (n = 3). One-way analysis of variance (ANOVA) followed by Dunnet's test for multiple comparisons: * p < 0.05; ** p < 0.01; *** p < 0.001 against acarbose. DEPe: dried peel methanolic extract; LEPe: lyophilized peel methanolic extract; DEPu: dried pulp methanolic extract; LEPu: lyophilized pulp methanolic extract.

α-Glucosidase inhibition: (a) inhibition performed by extracts obtained from pulp (n = 6); (b) inhibition performed by extracts obtained from peel (n = 6); (c) inhibition performed by sample 5 for DEPe and DEPu, sample 6 for LEPe and LEPu, and acarbose in a concentration dependent manner (n = 3). One-way analysis of variance (ANOVA) followed by Dunnet's test for multiple comparisons: * p < 0.05; ** p < 0.01; *** p < 0.001 against acarbose. DEPe: dried peel methanolic extract; LEPe: lyophilized peel methanolic extract; DEPu: dried pulp methanolic extract; LEPu: lyophilized pulp methanolic extract.

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The phytochemical profile of the methanolic extracts (pulp and peel) obtained from two dehydration methods (drying and freeze-lyophilization) of the traditional Italian apple Mela Rosa dei Monti Sibillini, as well as their inhibitory properties against some biological enzymes (α-glucosidase, lipase, monoamine oxidase A, tyrosinase and acetylcholine...

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... the results, both DEPu and LEPu at concentrations of 1 mg/mL inhibited the enzyme at a percentage less than 50% (Figure 1a). Similarly, almost all LEPe (exception with sample 5) and samples 1, 2, 3 and 4 of DEPe have shown an inhibitory effect less than 50%. ...
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... almost all LEPe (exception with sample 5) and samples 1, 2, 3 and 4 of DEPe have shown an inhibitory effect less than 50%. While at the same concentration (1 mg/mL), DEPe from samples 5 and 6 inhibited α-GLU with a percentage higher than that of acarbose (90% and 80%, respectively) ( Figure 1b). DEPe and LEPe inhibited α-GLU in a concentration dependent manner ( Figure 1c). ...
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... at the same concentration (1 mg/mL), DEPe from samples 5 and 6 inhibited α-GLU with a percentage higher than that of acarbose (90% and 80%, respectively) ( Figure 1b). DEPe and LEPe inhibited α-GLU in a concentration dependent manner ( Figure 1c). IC 50 values calculated by nonlinear regression are reported in Table 3. ...
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... the results, both DEPu and LEPu at concentrations of 1 mg/mL inhibited the enzyme at a percentage less than 50% (Figure 1a). Similarly, almost all LEPe (exception with sample 5) and samples 1, 2, 3 and 4 of DEPe have shown an inhibitory effect less than 50%. ...
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... almost all LEPe (exception with sample 5) and samples 1, 2, 3 and 4 of DEPe have shown an inhibitory effect less than 50%. While at the same concentration (1 mg/mL), DEPe from samples 5 and 6 inhibited α-GLU with a percentage higher than that of acarbose (90% and 80%, respectively) (Figure 1b). DEPe and LEPe inhibited α-GLU in a concentration dependent manner (Figure 1c). ...
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... at the same concentration (1 mg/mL), DEPe from samples 5 and 6 inhibited α-GLU with a percentage higher than that of acarbose (90% and 80%, respectively) (Figure 1b). DEPe and LEPe inhibited α-GLU in a concentration dependent manner (Figure 1c). IC50 values calculated by nonlinear regression are reported in Table 3. ...
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... dried peel methanolic extract; LEPe: lyophilized peel methanolic extract; DEPu: dried pulp methanolic extract; LEPu: lyophilized pulp methanolic extract. Figure 1. α-Glucosidase inhibition: (a) inhibition performed by extracts obtained from pulp (n = 6); (b) inhibition performed by extracts obtained from peel (n = 6); (c) inhibition performed by sample 5 for DEPe and DEPu, sample 6 for LEPe and LEPu, and acarbose in a concentration dependent manner (n = 3). ...

Citations

... For example, non-commercial varieties present higher polyphenol content or less allergenic genotypes than fruits developed after the green revolution, when genetic improvement of vegetables was focused on [19,20]. Some varieties have been demonstrated in vitro inhibitory effects against the enzymes α-glucosidase, lipase, monoamine oxidase A, tyrosinase and acetylcholinesterase [21]. Those biochemical traits, as well as other agronomical characteristics, could also be interesting for a better understanding of apple genomes, particularly to elucidate causal genes associated with human wellness [22]. ...
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Apples (Malus domestica Borkh.) have a great agricultural and economic impact worldwide; they also present an interesting nutritional value, and their consumption has been associated with beneficial health effects. In this study, 15 apple varieties (three commercial, 12 autochthonous genotypes) were collected from mountainous areas in Spain and were evaluated for their phenolic content, antioxidant, anti-obesity and antidiabetic activities. Quercetin was tested as the reference substance in bioassays due to its role as one of the most common flavonoids in apples and other vegetables. Total Phenolic Content (TPC) of apple pulp extracts was quantified using the Folin-Ciocalteu method. The antioxidant activity was determined by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging and xanthine/xanthine oxidase (X/XO) scavenging assays. Antidiabetic and anti-obesity potential were evaluated by inhibition of alpha-glucosidase (α-GLU), advance glycation end products (AGEs) formation and pancreatic lipase. The results showed in general higher phenol content in autochthonous varieties than in commercial apple pulp extracts. Phenolic-rich extracts showed better antioxidant profiles and significantly inhibited AGEs production and the α-glucosidase enzyme in a dose-dependent manner. None of them showed pancreatic lipase inhibitory effects but in general, the genotype known as “Amarilla de Octubre” was the best in terms of TPC and bioactive properties.
... These endeavors have guided researchers towards natural alternatives and the renewed interest in natural inhibitors from herb-based molecules to modulate biochemical effects of enzymes related to several pathologies such as Alzheimer's, diabetes, blood pressure, and obesity. Pharmacologically active compounds from medicinal plants have led to the phytochemical screening of various plants [37][38][39][40] . Although various researchers have been conducted on Seseli species for their biological effect, the extract of S. resinosum has not been evaluated for its potential to inhibit different enzymes and its phenolic compound content. ...
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Seseli taxa are widely known as a traditional medicinal herb, and S. resinosum collected from stony and rocky areas is endemic to the flora of Turkey. In this study, to reveal the plant's pharmacological importance, its ability to inhibit some medicinal enzymes was examined, assisted by molecular docking studies and phytochemical component analysis. The IC50 values for studied enzymes were calculated between 0.434 - 92.81 μg/mL, and the extract has lower inhibitory concentrations against α-glucosidase, α-amylase, and HMG_CoA reductase involved in carbohydrate and cholesterol metabolism. In addition, reverse-phase HPLC analysis was performed to correlate the enzyme inhibition ability with phenolic compositions. Benzoic acid and methyl chavicol were detected as the most abundant ingredients with the amount of 204.50±2.23 and 93.18±1.01 μg gˉˡ, respectively. TPC and TFC of the extract were founded at 31.23 ± 0.56 GAE/g and 5.54 ± 0.11 QE/g, respectively. The extract showed inhibitory and lethal effects, especially against all tested gram-negative strains at 7.5 and 15 mg mLˉˡ, respectively. In conclusion, the present study demonstrated that S. resinosum extract harbors bioactive compounds with inhibitory properties such as benzoic acid and catechin. It is expected that these primary data on the S. resinosum may contribute to building new experimental studies to open new avenues for research to support the pharmacological effects.
... The MS/MS spectra of the 3 most intense ions exceeding 1 × 10 4 counts of the full MS scan were acquired by the linear ion trap (LTQ) by using a normalized collision energy (CID) of 40 eV. A database containing the known components of apples and derivatives was built for the targeted data analysis [28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44]: the putative identification was obtained by comparing the accurate Antioxidants 2022, 11, 1577 4 of 27 mass (5 ppm mass tolerance), the isotopic pattern and the fragmentation pattern with the compounds in the database. The identity of some molecules was confirmed by means of pure standards available in our laboratory. ...
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The qualitative profile of thinned apple polyphenols (TAP) fraction (≈24% of polyphenols) obtained by purification through absorbent resin was fully investigated by LC-HRMS in positive and negative ion mode and using ESI source. A total of 68 polyphenols were identified belonging to six different classes: flavanols, flavonols, dihydrochalchones, flavanones, flavones and organic and phenolic acids. The antioxidant and anti-inflammatory activities were then investigated in cell models with gene reporter for NRF2 and NF-κB and by quantitative proteomic (label-free and SILAC) approaches. TAP dose-dependently activated NRF2 and in the same concentration range (10–250 µg/mL) inhibited NF-κB nuclear translocation induced by TNF-α and IL-1α as pro-inflammatory promoters. Proteomic studies elucidated the molecular pathways evoked by TAP treatment: activation of the NRF2 signaling pathway, which in turn up-regulates protective oxidoreductases and their nucleophilic substrates such as GSH and NADPH, the latter resulting from the up-regulation of the pentose phosphate pathway. The increase in the enzymatic antioxidant cellular activity together with the up-regulation of the heme-oxygenase would explain the anti-inflammatory effect of TAP. The results suggest that thinned apples can be considered as a valuable source of apple polyphenols to be used in health care products to prevent/treat oxidative and inflammatory chronic conditions.
... In vitro antityrosinase assay was a spectrophotometric analysis based on the methods previously described [33][34][35]. L-DOPA (3,4-dihydroxyphenylalanine) and L-tyrosine were using as the substrate, respectively. ...
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The melanogenesis inhibition effect in zebrafish (Danio rerio) and antityrosinase activity of the ethanolic extract and its phytochemicals from Ceylon olive (Elaeocarpus serratus Linn.) leaves were investigated in this study. Among the leaf extract and four soluble fractions, the ethyl acetate soluble fraction exhibits the best antityrosinase and antimelanogenesis activities. One phenolic acid, gallic acid, and two flavonoids, myricetin and mearnsetin, are isolated from the active subfractions through the bioassay-guided isolation; their structures are elucidated based on the 1D and 2D NMR, FTIR, UV, and MS spectroscopic analyses. These compounds have significant antityrosinase activity whether using l-tyrosine or l-DOPA as the substrate; mearnsetin shows the optimal activity. In the enzyme kinetic investigation, both gallic acid and mearnsetin are the competitive-type inhibitors against mushroom tyrosinase, and myricetin acts as a mixed-type tyrosinase inhibitor. Leaf extract and an ethyl acetate soluble fraction show effective performance in the inhibition of melanin formation in zebrafish embryos. Mearnsetin also possesses a promising antimelanogenesis effect, which is superior to the positive control, arbutin. Results reveal that the Ceylon olive leaf extract and its phytochemicals, especially mearnsetin, have the potential to be used as antimelanogenesis and skin-whitening ingredients.
... properties of the MRM pulp (López et al., 2020;Nkuimi Wandjou et al., 2019;Yousefi-Manesh et al., 2019, very little is available regarding the secondary metabolites produced by apple pulp callus culture (Baldelli et al., 2019) as well their biological effect. ...
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The biological effects of the ethanolic extract from Mela Rosa Marchigiana pulp callus were investigated. In terms of the antioxidant activity, the extract exhibited free radical scavenging activity of 67% and 39% using the DPPH assay and ABTS assay respectively. Furthermore, it reduced the ROS production in the keratinocyte cell model of H2O2 induced oxidative stress. The genoprotective effect was evaluated using the DNA nicking assay, which revealed significant protection up to 70%. The anti-inflammatory response was detected at 0.5 mg/ml through the release of nitric oxide using bacterial LPS and RAW 264.7 cells. Finally, preliminary studies on keratinocytes suggested a possible positive effect of the extract on mitochondrial biogenesis and wound healing. The obtained results encourage further studies to deep the biological effects of this callus with the future objective to propose a product for nutraceutical, cosmetic and food-tech industries, as well as an alternative to normal ways of chemical synthesis.
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