Enzyme Inhibitory Activity Research Articles

Antibacterial activity of organic extracts from Solidago graminifolia leaves

Solidago graminifolia (syn. Euthamia graminifolia (L.) Nutt) is a native species plant from North America, with abundant flavonoids, diterpenes, and polyacetylenes metabolites that have shown cholinesterase enzyme inhibitory activity and antimicrobial activity. The aim of this study was to determine the antibacterial activity of Solidago graminifolia leaf extracts obtained with ethanol, dichloromethane, and hexane solvents. The S. graminifolia extracts were tested against Escherichia coli, Salmonella enterica, Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumoniae. The chemical composition of each extract was analyzed by UPLC-MS/MS. The yield extracts in ethanolic, dichloromethane and hexanoic solvents were 20.39 %, 18.34 %, and 5.3 %, respectively. The secondary metabolites identified were flavonoids, hyperoxide, quercetin, kaempferol, and some phenolic acids, such as chlorogenic acid and solidagoic acid derivatives. The ethanolic extract inhibited the five strains in all concentrations (15 mg/mL, 10 mg/mL, 5 mg/mL, and 2.5 mg/mL). The ethanol extract has a MIC of 2.0 mg/mL against S. aureus and 1.5 mg/mL for the Gram-negative bacteria E. coli, S. enterica, P. aeruginosa, and K. pneumoniae; the dichloromethane extract has MIC values of 2.5 mg/mL for Gram-negative strains and 2.0 mg/mL for S. aureus. This study showed that the ethanolic extract had the best antibacterial activity, and its biological activity can be attributed to its richness in polyphenolic compounds.

PHYTOCHEMICAL PROFILING BY LC-ESI-MS/MS AND DETERMINATION OF ANTIOXIDANT, ANTI-ALZHEIMER AND ANTITYROSINASE ACTIVITIES OF TWO ASPARAGACEAE SPECIES: Scilla hyacinthoides L. AND Scilla ingridiae SPETA

In this study, in vitro antioxidant, antialzheimer and antityrosinase activity, total phenolic and flavonoid components, chemical profiling, identified by LC-ESI-MS/MS analysis and also chemometric analysis, of two different parts of Scilla species (Scilla hyacinthoides L. and Scilla ingridiae Speta) were determined in detailed perspective. The highest contents of total phenolics and total flavonoids were determined in S1TU (S. hyacinthoides aerial parts) extract (11.72 µg GAE/mg) and S2TU (S. ingridiae aerial parts) extract (31.53 µg QE/mg). The highest ABTS and CUPRAC activities were found in S1TU and S2TU extracts. The inhibitory activities of the extracts on the enzyme acetylcholinesterase were investigated. S1TU and S2TU extracts again showed the highest activity. Although the antirosinase enzyme inhibitory activities of the extracts were generally similar and high, the S2TA extract (S.ingridiae corm parts) showed the highest activity. Liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS/MS) was used to determine the content of phenolic components of the extracts. Fourteen different bioactive components were determined in the analyzes and their amounts were measured. The data obtained were analyzed chemometrically such as pricipal component analysis (PCA),hierarchical comoponent analysis (HCA) and their relationships to each other were supported visually and numerically with Pearson correlation graphs, heat maps, etc. The research results have shown that the various components of the plant have a good effect on various biological activities, so that it can be used for various purposes in the future (especially with a good degree of antityrosinase activity), taking into account the results. The biological activities demonstrated here can rationalize the use of the plant in traditional medicine.

Harnessing Phytochemicals to Regulate Catalytic Residues of Alpha-Amylase and Alpha-Glucosidase in Type 2 Diabetes.

Type 2 diabetes (T2D), also known as non-insulin-dependent diabetes mellitus, represents the prevailing manifestation of diabetes, encompassing a substantial majority of cases, ~90-95%. Plant-derived antidiabetic leads are being intensively explored due to their safety and effectiveness. The main objective of the present study is to evaluate the anti-diabetic potential of the traditional formulation Karisalai Karpam through in-vitro and in-silico investigations. The in-vitro and in-silico investigation of traditional polyherbal preparation Karisalai Karpam (KK) chooranam were performed to ascertain its inhibitory potential against α-amylase and α-glucosidase enzymes along with antioxidant (DPPH and ABTS) and phytochemical analysis. The results of enzyme inhibitory activity of KK witnessed highest activity against α-glucosidase enzyme with a percentage inhibition of 84.66 ± 2.50% (IC50,187.9 ± 5.79 μg/ml) followed by moderate level of α-amylase inhibition exhibited with 72.94 ± 3.66% (IC50, 241.6 ± 9.76 μg/ml). Additionally, the strongest antioxidant activity was observed in quenching DPPH• (IC50,154.8 ± 14.53 μg/ml) and ABTS+• radicals (IC50,148.6 ± 29.74 μg/ml). The outcome of the molecular docking studies indicated that among the 17 compounds analysed, the lead such as acalyphin, apigenin, humulene, and indirubin exhibited a prominent binding affinity over the residual binding site of α-glucosidase. It's important to note that the catalytic site of the enzyme α-amylase is primarily occupied by amyrin, apigenin, arjunolic acid, β-sitosterol, geraniol, and tricetin. In conclusion, the formulation KK demonstrates robust alpha-glucosidase and alpha-amylase inhibitory activity. It's also worth noting that the formulation exhibits noteworthy antioxidant properties, which could provide additional health benefits. The binding mode and energies of the identified phytochemicals against the target enzymes further support the formulation's antidiabetic potential.

Algerian vine canes as a good source of phenolic compounds for several in vitro biological activities

<p>One of the most widely cultivated crops in the world is grapevine knowing that about 77.8 million tons of grapes are produced worldwide each year. Both of vine growing, pruning, and winemaking generate a vast quantity of wastes and byproducts such as skin, seed, and canes. Grape canes include a wide range of phenolic profiles which have several biological effects. In the present study four vine Algerian grape cane cultivars were selected for the evaluation of their phenolic contents and biological activities. The objective of this study was to evaluate the total phenolic and flavonoid contents, in vitro antioxidant activity (using DPPH, ABTS, and reducing power methods), enzyme inhibitory activity (towards alpha amylase, and urease) anti-inflammatory activity, and sun protection factor of each extract. All grape extracts were compared for their TPC and TFC values which ranged from 123 to 288 mg of Gallic acid equivalent (GAE)/g extract to 24.5 to 55.6 mg of quercetin equivalent (QCE)/g extract respectively. The highest TPC and TFC were found in the grape cultivar FR (288.8 mg GAE/g extract, 55,625 mg QCE/g extract respectively). The results revealed also that all extracts showed high antioxidant with the same trend of phenolic composition and significant enzymatic activity in all tests. Additionally, all extracts showed a moderate anti-inflammatory activity by inhibiting the denaturation of BSA, and given a high sun protection factor. These findings imply that grape canes which considered as undervalued parts have a significant potential to be used as a natural treatment for many physiological diseases and for the pharmaceutical and cosmetic sector and medical research.</p>

Simultaneous recycling of flavonone and polymethoxyflavonoids from Chenpi processing residue based on their complementary action on glycolipid lowering activity: Innovative combination use of yeast and aqueous two-phase system

This study aimed at recycling flavonoids with glycolipid lowering activity from Chenpi processing residue produced by essential oil extraction. The crude Chenpi flavonoids obtained by ethanol reflux mainly contained flavonone (hesperidin) and polymethoxyflavonoids (nobiletin, tangeretin, sinensetin, and isosinensetin), which complementally exerted strong glycolipid lowering activity as revealed by digestive enzyme inhibitory activity, molecular docking and network pharmacology. The reducing sugar and water-soluble impurities were efficiently removed by yeast fermentation and aqueous two-phase system (ATPS) extraction, respectively. The optimal combination use of yeast (2 % w/v, CN36) and ATPS formed by 22 % (w/w) (NH4)2SO4 and 25 % (w/w) ethanol improved flavonoid purity to 60.25 %, enriched flavonone and polymethoxyflavonoids by 6.69-fold, and enhanced digestive enzyme inhibitory activity, which was superior to the use of individual yeast or ATPS, unoptimized combination, macroporous resin (XAD-16), and ethyl acetate. This study was the first to develop a recyclable biophysical method for simultaneous enrichment of flavonone and polymethoxyflavonoids.

In vitro and in vivo activities of scutellarein, a novel polyphosphate kinase 1 inhibitor against Acinetobacter baumannii infection

BackgroundInorganic polyphosphate (polyP)-targeted polyphosphate kinase 1 (PPK1) has attracted much attention by virtue of its importance in bacterial pathogenicity and persistence, as well as its exclusive presence in microorganisms. However, only very few drugs have been found to be efficacious in inhibiting the Acinetobacter baumannii (A. baumannii) PPK1 protein.ResultsIn this study, we identified Scutellarein (Scu), a potent PPK1 inhibitor that could significantly influence PPK1-regulated motility, biofilm formation, and bacterial persistence, which was further validated by the results of transcriptome analysis. Mechanistic explorations revealed that Scu achieved its enzyme inhibitory activity predominantly through direct engagement with the active center of PPK1. Moreover, the survival rate of Galleria mellonella larvae was increased by about 35% with 20 mg/kg of Scu treatment. The remarkable therapeutic benefits of Scu were also observed in the mouse pneumonia model, shown mainly by reduced bacterial colonization, pathological lesions, and inflammatory factors.ConclusionOur results revealed that Scu could attenuate the pathogenicity and persistence of A. baumannii by interfering with its important kinase PPK1.

Phytochemical Profile and Antioxidant, Enzyme-Inhibitory, and Cytotoxic Potential of Endemic Cynoglottis chetikiana subsp. chetikiana

Background Cynoglottis chetikiana subsp. chetikiana, an endemic Boraginaceae plant growing in Turkey, has not been previously studied in terms of pharmacognosy. However, related species, such as Anchusa, Symphytum, and Rindera, have been known for their pharmacological effects attributed to compounds such as flavonoids, terpenoids, and other phenol derivatives. Purpose This study aimed to reveal the phytochemical composition and potential biological activity of C. chetikiana. Methods Phytochemical profiling analysis was performed by using the liquid chromatography–high-resolution mass spectrometry (LC–HRMS) system. The cytotoxic effects of the extracts were evaluated on the MCF-7 mammalian breast cancer cell line by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The in vitro α-glucosidase and tyrosinase enzyme inhibitory activities were assessed using literature methods. Additionally, antioxidant properties were investigated, leading to the bioactivity-guided isolation of the most active substance. Results LC–HRMS analysis revealed 27 major phenolic compounds and 2 pyrrolizidine alkaloids in C. chetikiana. Bioactivity-guided studies led to the isolation of a flavonoid, rutin. The n-butanol extract of the plant exhibited high antioxidant capacity and was rich in phenolic compounds. The methanol extract of C. chetikiana demonstrated low-moderate α-glucosidase inhibitory activity (IC50 = 608.62 ± 7.01 µg/mL). Moreover, the methanol extract showed significant anti-tyrosinase enzyme activity (195.84 ± 5.81 mg Kojic acid equivalent/g extract), and the petroleum ether extract displayed the highest cytotoxicity on MCF-7 cells (IC50 = 76.91 ± 3.12 µg/mL). Conclusion This is the first phytomedicinal study report for C. chetikiana, which gives promising insight for further pharmaceutical research.

Aktivitas Penghambatan Enzim α-Amilase Ekstrak Etanol dan Fraksi Buah Belimbing Wuluh (Averrhoa bilimbi L.)

The enzyme α-amylase is one of the enzymes that plays a role in the process of degrading starch into maltose and glucose. Organic compounds such as polyphenols and flavonoids are inhibitors of α-amylase. The star fruit plant (Averrhoa bilimbi L.) has α-amylase enzyme inhibition activity and has the potential to be used in the therapy of type 2 diabetes mellitus. This study aims to determine whether ethanol extract and the fraction of star fruit (Averrhoa bilimbi L.) have α-amylase enzyme inhibition activity, inhibition against α-amylase enzyme and better inhibition activity. The test of α-amylase enzyme inhibition activity was carried out using 3 test groups, namely negative control, positive control (acarbose) and samples (ethanol extract and star fruit fraction) with concentrations of 12.5 ppm, 25 ppm, 50 ppm, 100 ppm and 200 ppm. The results of testing the inhibitory activity of α-amylase enzyme of ethanol extract and the fraction of star fruit (Averrhoa bilimbi L.) obtained IC50 values of 5.581 μg/mL, 76.725 μg/mL, 43.152 μg/mL and 55.447 μg/mL, respectively. Based on these results, it can be concluded that the ethanol extract of star fruit (Averrhoa bilimbi L.) at a concentration of 200 ppm has a very strong activity in inhibiting the α-amylase enzyme with an inhibition percentage of 85.217% and an IC50 value of 5.581 μg/mL.

The Antioxidant Effects of Trypsin-Hydrolysate Derived from Abalone Viscera and Fishery By-Products, and the Angiotensin-I Converting Enzyme (ACE) Inhibitory Activity of Its Purified Bioactive Peptides.

Abalone is a rich source of nutrition, the viscera of which are discarded as by-product during processing. This study explored the biological activities of peptides derived from abalone viscera (AV). Trypsin-hydrolysate of AV (TAV) was purified into three fractions using a Sephadex G-10 column. Nine bioactive peptides (VAR, NYER, LGPY, VTPGLQY, QFPVGR, LGEW, QLQFPVGR, LDW, and NLGEW) derived from TAV-F2 were sequenced. LGPY, VTPGLQY, LGEW, LDW, and NLGEW exhibited antioxidant properties, with IC50 values of 0.213, 0.297, 0.289, 0.363, and 0.303 mg/mL, respectively. In vitro analysis determined that the peptides VAR, NYER, VTPGLQY, QFPVGR, LGEW, QLQFPVGR, and NLGEW inhibited ACE, with IC50 values of 0.104, 0.107, 0.023, 0.023, 0.165, 0.004, and 0.146 mg/mL, respectively. The binding interactions of ACE-bioactive peptide complexes were investigated using docking analysis with the ZDCOK server. VTPGLQT interacted with HIS513 and TYR523, and QLQFPVGR interacted with HIS353, ALA354, GLU384, HIS513, and TYR523, contributing to the inhibition of ACE activity. They also interacted with amino acids that contribute to stability by binding to zinc ions. QFPVGR may form complexes with ACE surface sites, suggesting indirect inhibition. These results indicate that AV is a potential source of bioactive peptides with dual antioxidant and anti-hypertensive dual effects.

Targeted and non-targeted metabolic characteristics of 6,7-dihydroxy-2,4- dimethoxyphenanthrene during simulated gastrointestinal digestion

6,7-dihydroxy-2,4-dimethoxyphenanthrene (PC4), isolated and identified from Chinese yam, was one of the important characteristic active ingredients. The present study established simulated gastrointestinal digestion and caco-2 intestinal epithelial models to investigate the digestive and metabolic characteristics of PC4. The results indicated that PC4 was mainly digested and metabolized in the intestine, with a digestion rate of 94 %, producing active characteristic metabolites including 2,6-dimethoxy-4-phenanthrenol (MC1) and 1-methoxyphenanthrene (MC2). Molecular docking indicated that the COX-2 enzyme inhibitory activity of MC1 might be superior to that of the prototype PC4. During 24 h co-incubation of PC4 with caco-2 monolayer epithelial, the signal pathway related to lipid decomposition was up-regulated within 0–12 h, while the diabetes complications AGE-RAGE was inhibited just in 0–6 h period significantly. The research database provided scientific basis for the digestion and metabolism of PC4, and laid theoretical foundation for the scientific development of Chinese yam functional foods.

Alkaloids from Stephania cephalantha and their enzyme inhibitory activities

A new protoberberine type alkaloid, 11-diethylaminomethyl corydalmine (1), and 27 known alkaloids (2-28) were isolated from the tuberous roots of Stephania cephalantha. Their structures were identified by spectral analysis. Enzyme inhibitory activities of the compounds on acetylcholinesterase (AChE), tyrosinase and α-glucosidase were evaluated. Compounds 13, 16 and 18 exhibited comparable AChE inhibitory activities to the positive control huperzine A, with the IC50 values of 0.046, 0.048, and 0.057 mg/mL, respectively.

Anti-hypertensive, anti-inflammatory, glycemic and satiety impact of cocoa flavoured soy-based powder drink mix enriched with bioactive hydrolysates from nests of Aerodramus fuciphagus

Abstract Objectives The edible bird’s nest hydrolysates (EBNH) are renowned for their health benefits. The study aimed to determine their contributory functional effect as an ingredient in the cocoa-flavoured soy-based powder drink mix (PDM). The product’s glycemic and satiety impact were also studied. Materials and Methods The product was enriched with a reasonably low amount of spray-dried EBNH. The product’s functional effect with respect to in vitro angiotensin converting enzyme (ACE) inhibitory activity and human red blood cells membrane stabilization (RBCMS) activity were evaluated, using its water extract (90 - 95 oC). The glycemic and satiety impact were evaluated using 12 and 30 subjects, respectively, who consumed 250 mL of the product, containing 25 g of available carbohydrates. Results The enriched PDM’s ACE inhibitory activity and RBCMS activity were significantly higher (p<0.05) than those that were devoid of EBNH. A 240 mL (12.5% w/v) of PDM (containing by weight 3.0% EBNH, 75.44% soybean powder, 20% cocoa powder, 0.5% xanthan gum, 1.0% silicon dioxide and 0.06% sucralose) provides about 3.7 kcal/g energy. Its 250 mL meal (consistency index of 14.17 Pa.sn) is high in protein and dietary fiber. The product’s glycemic index (GI) and glycemic load (GL) are low, 24 and 6.0, respectively, raising a normal level of 2 hours postprandial blood glucose (<6 mmol/L) and satisfies hunger for about 2.5 hours. Conclusion The EBNH, as an ingredient, enhances the PDM’s anti-hypertensive and anti-inflammatory properties. The overall findings suggest that the formulated PDM is a wellness food product capable of promoting good human health, including for dieters and individuals with diabetes.

Insights into nanoparticle toxicity against aquatic organisms using multivariate regression, read-across, and ML algorithms: Predictive models for Daphnia magna and Danio rerio

The production of nanoparticles (NPs) has recently become more prevalent owing to their numerous applications in the fast-growing nanotechnology industry. Although nanoparticles have growing applications, there is a significant concern over their environmental impact due to their inevitable release into the environment. With the increasing risk to aquatic organisms, D. magna and zebrafish (Danio rerio) have been preferred as important freshwater model organisms for risk assessment and ecotoxicological studies on metal oxide-based nanoparticles (MeOxNPs) in aquatic environments. It is unfeasible to assess the risks associated with every single NP through in vivo or in vitro experiments. As an alternative, in silico approaches are employed to evaluate the NP toxicity. To evaluate such performance, we have collected data from databases and literature reviews to develop models based on multivariate regression, read-across approach (RA), and machine learning (ML) algorithms following the principles of OECD (Organization for Economic Cooperation and Development) for QSAR modeling. This work has aimed to investigate which features are important drivers of nanotoxicity in D. magna and Danio rerio using simple periodic table-derived descriptors. Further, we have examined the effectiveness of read-across-derived similarity measures compared to traditional QSAR models. The results obtained from model 1 infers that nanoparticles' size, the number of metals, the core environment of the metal present in the metal oxide, and the oxidation number of the metal play a key role in the final expression of toxicity of nanoparticles to D. magna. On the other hand, the presence of higher molecular weight, the core of the metal, and the presence of oxygen influence the enzyme inhibition activity. The enzyme inhibition is correlated with the ability of zebrafish embryos to hatch, and therefore, the inhibition of ZHE1 seems to be the factor driving hatch delay. The study emphasized the importance of developing transferable, reproducible, and easily interpretable models for the early identification of nanoparticle features contributing to aquatic toxicity.

Exploring of Chemical Profile and Biological Activities of Three Ocimum Species From Comoros Islands: A Combination of In Vitro and In Silico Insights.

Ocimum species have a great interest in different traditional medicinal systems. This study examined the chemical composition, antioxidant properties, enzyme inhibitory effects, and antibacterial and antifungal activities of the aerial parts of Ocimum gratissimum, Ocimum americanum, and Ocimum basilicum from the Comoros Islands. The extracts were analyzed using high-performance liquid chromatography-mass spectrometry (HPLC-MS) to determine their chemical composition. Antioxidant activity was assessed using 2,2-Diphenyl-1-picrylhydrazyl (DPPH), 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing antioxidant power (FRAP), chelating ability, and phosphomolybdenum radical scavenging assays. Enzyme inhibitory activities against acetylcholinesterase (AChE), butrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase were evaluated using spectrophotometric methods. Antibacterial and antifungal activities were tested using the broth microdilution method against selected pathogenic microorganisms. The selected enzymes and proteins were evaluated using in silico methods with biomolecules from these plants. In addition, 111 different metabolites were identified in the tested extracts using advanced HPLC/MS techniques. The most significant number of detected compounds were derivatives of hydroxycinnamic acids, followed by flavonoid glycosides and aglycones and derivatives of hydroxybenzoic acids. All three Ocimum species exhibited significant antioxidant activities, O. gratissimum exhibited the best-reducing abilities in CUPRAC and FRAP assays. In addition, enzyme inhibitory assays revealed that O. americanum had the most potent inhibitory effect on tyrosinase (48.01 ± 3.89 mg kojic acid equivalent [KAE]/g), and amylase (1.08 ± 0.02 mmol acarbose equivalent [ACAE]/g). Antibacterial and antifungal tests demonstrated that the extracts possess broad-spectrum activity. Molecular docking results showed that compounds exhibited remarkable binding energies with target enzymes and proteins. The molecular dynamics simulations identified chicoric acid with MurE of Staphylococcus aureus complex as the most promising drug candidate. These findings support their traditional medical and nutraceutical uses and suggest possibilities for natural functional applications.

Structural Perspectives in the Development of Novel EGFR Inhibitors for the Treatment of NSCLC.

Non-small cell Lung cancer (NSCLC) is the most common type of lung cancer, which is caused by high consumption of tobacco and smoking. It is an epithelial lung cancer that affects about 2.2 million people across the globe, according to International Agency for Research on Cancer (IARC). Non-small cell lung cancer is a malignant tumor caused by EGFR mutation that occurs in the in-frame deletion of exon 19 and L858R point mutation in exon 21. Presently, clinically available inhibitors of EGFR (including erlotinib, lapatinib, gefitinib, selumetinib, etc.) are not specific and responsible for undesirable adverse effects. Moreover, to solve this problem search for newer EGFR inhibitors is the utmost need for the treatment and/or management of increasing lung cancer burden. The discovery of therapeutic agents that inhibit the specific target in tumorous cells, such as EGFR, is one of the successful strategies in treating many cancer therapies, including lung cancer. The exhaustive literature survey (2018-2023) has shown the importance of medicinally privileged pyrimidine derivatives together, fused and/or clubbed with other heterocyclic rings to design and develop novel EGFR inhibitors. Pyrimidine derivatives substituted with phenylamine, indole, pyrrole, piperazine, pyrazole, thiophene, pyridine and quinazoline derivatives substituted with phenylamine, pyrimidine, morpholine, pyrrole, dioxane, acrylamide, indole, pyridine, furan, pyrimidine, pyrazole etc. are privileged heterocyclic rings shown promising activity by inhibiting EGFR and TKIs. The present review summarizes the structure-activity relationship (SAR) and enzyme inhibitory activity, including IC50 values, percentage inhibition, and kinetic studies of potential compounds from various literature. The review also includes various aspects of molecular docking studies with compounds under clinical trials and patents filed on pyrimidine-based EGFR inhibitors in treating non-small cell lung cancer. The present review may benefit the medicinal chemist for developing novel compounds such as EGFR inhibitors.

Preparing Ganoderma lucidum slices by improved steam explosion enhances their apparent, functional and structural properties

Ganoderma lucidum slices exhibit antioxidant and enzyme inhibitory activity, enhancing vitality and longevity. However, untreated Ganoderma lucidum slices fail to meet specific physical and chemical requirements for consumption and processing because their bioactive compounds must be released before intake through effective pretreatment. We proposed developing a novel preparation method for Ganoderma lucidum slices through improved steam explosion (ISE). The effect of ISE (at 0.4–1.2 MPa for 5 min) on their chemical compounds, apparent properties, biological activity, sensory quality and structural characteristics was assessed. The results showed that ISE (0.8–1.2 MPa) increased the content of flavonoids (by 32.29 %–126.57 %), phenolics (by 31.79 %–96.28 %), triterpenes (by 1.74–5.24 times) and polysaccharides (by 6.27–18.03 times) in Ganoderma lucidum slices. Additionally, ISE improved the color saturation and hue of their infusions while reducing the color values of these slices. Under all conditions, ISE significantly increased the soluble solids content (by 1.31–11.44 times) and the inhibitory activity of tyrosinase and xanthine oxidase when compared to infusions of untreated slices. At 0.8–1.2 MPa, the radical scavenging activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) was also significantly higher in steam-exploded slices than in untreated slices. In the sensory evaluation, steam-exploded slices outperformed untreated slices in terms of color, taste, form attributes, and overall score. ISE disrupted the microstructure of Ganoderma lucidum slices, whose microscopic structure was broken into fragments, thereby promoting the dissolution of bioactive compounds and enhancing their biological functions, as shown in this study. Therefore, ISE improved the nutritional and medicinal effects of the fruiting body of Ganoderma lucidum by facilitating nutritional retention and resource utilization efficiency.

ACE inhibitory effect and saltiness-enhancing properties of chicken-derived umami peptides: Digestive stability, inhibition kinetics, multiple ligand docking and central composite design

Angiotensin-I-converting enzyme (ACE) inhibitory activity and saltiness-enhancing properties of chicken-derived umami peptides were investigated. DGGRYY and NEFGYSNR were screened and the IC50 values were 28.71 μM and 283.24 μM, indicating their potential as novel ACE inhibitors. DGGRYY and NEFGYSNR have good pH and thermal stability. After gastrointestinal digestion, the ACE-inhibitory activity of DGGRYY retained about 53 %, whereas NEFGYSNR retained about 57 %. The inhibition pattern of both peptides was determined to be uncompetitive, consisting with the result of multiple ligand docking that the binding sites were outside the ACE active pocket. Trp59, Tyr62, Asp121, Arg124, and Ser516 were the key binding sites that contributed to the total binding energy. In addition, saltiness and palatability models were established according to sensory analysis and central composite design. In 0.1 % ~ 0.3 % NaCl solutions, the addition of DGGRYY and NEFGYSNR could enhance the salty intensity and compensate for the palatability loss caused by salt reduction.

Optimization of ultrasound-assisted extraction method of Syzygium cumini leaves based on extraction yield, content of bioactive compound, and inhibition of dipeptidyl peptidase IV enzyme activity using response surface methodology

Syzygium cumini leaves show potential to be developed as herbal medicine products against diabetes mellitus due to their high polyphenol contents. S. cumini was optimized using response surface methodology and Box–Behnken design with solvent solid ratio, solvent concentration, time and temperature, extraction yield, total flavonoid content (TFC), total phenolic content (TPC), and dipeptidyl peptidase IV (DPP-IV) enzyme inhibitory activity to obtain an effective and optimal extraction method. The conditions were achieved using a 70% ethanol solvent for the extraction, with a solvent–solid ratio of 21 v/w and run at 20°C for 30 min. The results showed an extraction yield of 83.875%, with TFCs measuring at 3.068 mg QE/g, TPCs of 65.029 mg GAE/g, and DPP-IV enzyme inhibition activity of 66.079%. Further analysis of the phytochemical profile using untargeted liquid chromatography-high-resolution mass spectrometry showed the presence of amine, amide, and fatty acid derivatives as major constituents. In addition, major flavonoids observed were myricetin and myricitrin, accounting for 0.2%. Ursolic acid and 25-azacholesterol accounted for 1.03% of the phenolics detected.

Polyphenol compounds contributing to the improved bioactivities of fermented Rubus chingii Hu

This research aims to evaluate the phenolic composition, antioxidant and enzyme inhibition activities of fermented Rubus chingii Hu wine, and explore the correlation between them. TPC (Total Phenolic content) and TFC (Total Flavonoid content) increased rapidly from 0 h to 72 h, followed by a slight decrease in TPC and a significant decrease in TFC. Fermentation could significantly increase the antioxidant activity and α-amylase/α-glucosidase enzyme inhibitory activity of Rubus chingii Hu. A total of 39 polyphenols and organic acids in fermented Rubus chingii Hu were identified by UPLC-ESI-Q-TOF-MS/MS and 11 of them were quantitatively analyzed. After fermentation, the contents of all the detected polyphenol compounds, except for quercetin and ellagic acid, significantly increased (p < 0.05). Correlation analysis showed that protocatechuic acid and catechin played an important role in the antioxidant activity of fermented Rubus chingii Hu, while protocatechuic acid and hypericin played an important role in the α-amylase inhibition activity. This study indicated that Rubus chingii Hu could be applided as a potential meterial for the wine production, and has the potential to be a functional food for promoting health.

NMR Metabolite Profiling and Antioxidant Properties of Spartan, Jewels, Misty, and Camelia Blueberries.

The health-promoting properties of blueberries are widely recognized and are mainly attributed to anthocyanins. However, fruit's chemical composition includes also other components and strongly depends on varieties and climatic conditions. Here, 1H NMR metabolite profiling and biological activity of four blueberry cultivars (Spartan, Jewels, Misty, Camelia) grown in Central Italy over two years were reported. Untargeted and targeted NMR analyses allowed the quantification of sugars, organic acids, amino acids, anthocyanins, lipids, and other compounds. Spectrophotometric assays evaluated total phenolic and flavonoid content, antioxidant activity, and enzyme inhibitory activity toward cholinesterase, α-amylase, α-glucosidase, and tyrosinase. Statistical analysis showed a correlation between chemical composition and biological activity, revealing markers specific to blueberry cultivars (quinic acid, quercitrin, myo-inositol, myrtillin, and petunidin-3-O-glucoside). Almost all antioxidant assays were correlated with the chlorogenic acid levels. A strong effect of harvesting on chemical composition and biological activities was observed, with Misty cultivar having the highest antioxidant activity.