Α-glucosidase Inhibitory Activity Research Articles

Agrocybe cylindracea Dietary Fiber Modification: Sodium Hydroxide Treatment Outperforms High-Temperature, Cellulase, and Lactobacillus Fermentation.

Agrocybe cylindracea dietary fiber (ADF) contains 95% water-insoluble dietary fiber, resulting in poor application performance. To address this issue, ADF was modified by four methods (cellulase, sodium hydroxide, high-temperature, and Lactobacillus fermentation) in this paper. By comparing the physicochemical properties, microstructures, monosaccharide compositions, and functional characteristics (antioxidant and α-glucosidase inhibitory activities in vitro) of all modified ADF samples, the optimal modification method was selected. Results showed that sodium hydroxide treatment was deemed the most effective modification method for ADF, as alkali-treated ADF (ADF-A) revealed a higher oil-holding capacity (2.02 g/g), swelling capacity (8.38 mL/g), cholesterol adsorption (6.79 mg/g), and α-glucosidase inhibitory activity (more than 70% at 0.4-0.6 mg/mL) than the other modified samples. The looser microstructure in ADF-A might be attributed to molecular rearrangement and spatial structure disruption, which resulted in smaller molecular sizes and decreased viscosity, hence improving ADF's physicochemical and functional qualities. All these findings indicate the greater application potential of modified ADF products in food and weight-loss industries, providing a comprehensive reference for the industrial application of ADF.

Investigation of the chemical composition, antioxidant, and enzyme inhibitory activities of Ononis natrix subsp. natrix, performance of in silico analyses of its major compounds

In this study, phytochemical composition, antioxidant, anti-Alzheimer, anti-diabetic, tyrosinase activities and in silico analyses of methanol, ethyl acetate and water extracts obtained from the aerial parts of Ononis natrix subsp. natrix, which is naturally distributed in the flora of Mediterranean area, were performed. The extracts were first analyzed for their phytochemical composition using quantitative chromatographic techniques. As a result of spectrophotometric analyses (Agilent Technologies 1260 Infinity liquid chromatography system with 6420 Triple Quad mass spectrometer), it was determined that the methanol extract was the richest in terms of total phenolics (74.60 mg GAEs/g dry weight), while the water extract was found to be richest in terms of total flavonoids (27.88 mg REs/g dry weight). As a result of quantitative phytochemical analyses, taxifolin, hyperoside, eriodictiol and quercetin were found to be present in high concentrations. As a result of quantitative phytochemical analyses, taxifolin, hyperoside, eriodictyol, and quercetin were found to be present in high concentrations. The methanol extract displayed higher activity in all test systems except for DPPH radical scavenging activity. The results from the phosphomolybdenum, ABTS radical scavenging, CUPRAC, FRAP, and metal chelating tests for the methanol extract were: 1.71, 1.07, 1.02 mg, 0.91, and 1.47 mg /ml, respectively. When the AChE, BChE and α-glucosidase inhibitory activity tests were evaluated in terms of IC50, the methanol extract showed higher activity with IC50 values of 1.02, 1.70 and 1.02 mg/ml, respectively. In contrast, the ethyl acetate extract showed higher activity in the tyrosinase and α-amylase tests, with IC50 values of 1.42 and 1.78 mg/ml, respectively. It was found that there was a strong correlation between the total phenolic and flavonoid contents of the extracts and their antioxidant and enzyme inhibitor activities. The study also conducted in silico molecular docking, MM/GBSA, drug-likeness, and ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) analyses to describe the pharmacokinetic and pharmacodynamic properties of bioactive compounds with potential pharmacological action present in O. natrix subsp. natrix extracts. The compounds studied were eriodictyol, hyperoside, quercetin, and taxifolin. Researchers have found that, based on molecular docking, MM/GBSA, and key interactions within the enzyme active sites, hyperoside may inhibit α-amylase and BChE, eriodictyol may inhibit α-glucosidase and AChE, and both hyperoside and eriodictyol may inhibit tyrosinase. The presented data on antioxidant and enzyme inhibitory activity, along with in silico studies, represent the first recorded findings in the literature.

Research Progresses of Plant Polysaccharides with α-Glucosidase Inhibition activities

Research Progresses of Plant Polysaccharides with α-Glucosidase Inhibition activities

Whole genome sequence analysis and in vitro probiotic characteristics of Lactococcus lactis ZFM559

Lactococcus lactis, a candidate probiotic, is extensively applied in the fermentation of the food industry and is recognized for its potential to enhance human health. In this study, L. lactis ZFM559, which exhibits probiotic properties, was isolated from fresh milk. In vitro assays have demonstrated it has the ability to inhibit and co-aggregate with multiple pathogenic strains, as well as good tolerance to high osmotic pressure (10% NaCl), low pH (3.0), and simulated gastrointestinal conditions. Moreover, L. lactis ZFM559 is capable of producing folate and inhibiting α-glucosidase activity. Whole-genome sequencing has revealed the components of its genome, which include one circular chromosome and three linear plasmids. Functional annotation of the genome has identified the pathway for γ-aminobutyric acid synthesis, genes and enzymes associated with flavor production and lactose decomposition, and proteins related to environmental stress tolerance. Additionally, a complete gene cluster (including LanT, HlyD, LcnB, and GlyS) for the synthesis of bacteriocins was identified. In summary, L. lactis ZFM559 can be considered a probiotic with significant potential for applications in the food industry and human health.

Bioactive Naphthoquinone and Phenazine Analogs from the Endophytic Streptomyces sp. PH9030 as α-Glucosidase Inhibitors.

A talented endophytic Streptomyces sp. PH9030 is derived from the medicinal plant Kadsura coccinea (Lem.) A.C. Smith. The undescribed naphthoquinone naphthgeranine G (5) and seven previously identified compounds, 6-12, were obtained from Streptomyces sp. PH9030. The structure of 5 was identified by comprehensive examination of its HRESIMS, 1D NMR, 2D NMR and ECD data. The inhibitory activities of all the compounds toward α-glucosidase and their antibacterial properties were investigated. The α-glucosidase inhibitory activities of 5, 6, 7 and 9 were reported for the first time, with IC50 values ranging from 66.4 ± 6.7 to 185.9 ± 0.2 μM, as compared with acarbose (IC50 = 671.5 ± 0.2 μM). The molecular docking and molecular dynamics analysis of 5 with α-glucosidase further indicated that it may have a good binding ability with α-glucosidase. Both 9 and 12 exhibited moderate antibacterial activity against methicillin-resistant Staphylococcus aureus, with minimum inhibitory concentration (MIC) values of 16 μg/mL. These results indicate that 5, together with the naphthoquinone scaffold, has the potential to be further developed as a possible inhibitor of α-glucosidase.

Parkia javanica Edible Pods Reveal Potential as an Anti-Diabetic Agent: UHPLC-QTOF-MS/MS-Based Chemical Profiling, In Silico, In Vitro, In Vivo, and Oxidative Stress Studies.

According to the World Health Organization, over 422 million people worldwide have diabetes, with the majority residing in low- and middle-income countries. Diabetes causes 1.5 million fatalities a year. The number of diabetes cases and its prevalence have progressively increased over the last few decades. This study aims to determine the phytochemicals in the edible part of Perkia javanica, predict their α-glucosidase inhibitory potential, one of the promising targets for diabetes, and then carry out in vitro and in vivo studies. The phytochemicals present in the n-butanol fraction of the methanol extract of P. javanica pods were analyzed using UHPLC-QTOF-MS/MS (Ultra-High-Performance Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry). The UHPLC-QTOF analysis revealed the presence of 79 different compounds in the n-butanol fraction. Among these, six compounds demonstrated excellent binding affinities with α-glucosidase, surpassing the performance of two standard inhibitors, Miglitol and Voglibose. In vitro α-glucosidase inhibitory activities were assessed by the n-butanol fraction, followed by in vivo studies. According to the in vitro study, the inhibitory efficiency against α-glucosidase was determined to have an IC50 value of 261.9 µg/mL. The in vivo findings revealed a significant reduction in blood glucose levels in Swiss albino mice treated with the same extract, decreasing from 462.66 mg/dL to 228.66 mg/dL. Additionally, the extract significantly increased the activity of the enzymes catalase and superoxide dismutase (SOD) and decreased the amount of malondialdehyde (MDA) in the liver and kidney tissue. The predicted physicochemical parameters indicated that most of the compounds would be excreted from the body after inhibition in the small intestine without being absorbed. Considering the low cost and wide availability of raw materials, P. javanica pods can serve as a good food supplement that may help prevent type 2 diabetes management.

Isolation of New Secondary Metabolites from Kedrostis gijef and Evaluation of Their α-Glucosidase Inhibitory Activity

Isolation of New Secondary Metabolites from Kedrostis gijef and Evaluation of Their α-Glucosidase Inhibitory Activity

Integrative metabolomics and chemometrics depict the metabolic alterations of differently processed red kidney beans (Phaseolus vulgaris L.) and in relation to in-vitro anti-diabetic efficacy

Red kidney beans (RKB) serve as a powerhouse packed with a plethora of largely unexplored extraordinary chemical entities with potential significance. However, their nutraceutical applications as a functional hypoglycemic food still lag behind and warrant further investigation. With a scope to optimize chemical and biological traits of RKB, green modification approaches (processing methods) seem inevitable. Accordingly, the current study offered the first integrative workflow to scrutinize dynamic changes in chemical profiles of differently processed RKB and their potential entanglements on diabetes mitigation using Ultra Performance Liquid Chromatography-mass spectrometry (UPLC-MS/MS) coupled with chemometrics. Different physical and biological processing treatments namely germination, fermentation, cooking and dehulling were preliminarily implemented on RKB. Complementarily, the concomitant metabolite alterations among differently processed RKB were monitored and interpreted. Next, an in-vitro α-amylase and α-glycosidase inhibitory testing of the differently processed samples was conducted and integrated with orthogonal projection to latent structures (OPLS) analysis to pinpoint the possible efficacy compounds. A total of 72 compounds spanning fatty acids and their glycerides, flavonoids, phenolic acids, amino acids, dipeptides, phytosterols and betaxanthins were profiled. Given this analysis and compared with raw unprocessed samples, it was found that flavonoids experienced notable accumulation during germination while both fermentation and dehulling approaches sharply intensified the content of amino acids and dipeptides. Comparably, Fatty acids, phytosterols and betaxanthins were unevenly distributed among the comparable samples. Admittedly, OPLS-DA revealed an evident discrimination among the processed samples assuring their quite compositional discrepancies. In a more targeted approach, kaempferol-O-sophoroside, quercetin, carlinoside and betavulgarin emerged as focal discriminators of sprouted samples while citrulline, linoleic acid, linolenoyl-glycerol and stigmasterol were the determining metabolites in cooked samples. Our efficacy experimental findings emphasized that the different RKB samples exerted profound inhibitory actions against both α-amylase and α-glycosidase enzymes with the most promising observations in the case of sprouted and cooked samples. Coincidently, OPLS analysis revealed selective enhancement of possible efficacy constituents primarily citrulline, formononetin, gamabufotalin, kaempferol-O-sophoroside, carlinoside, oleic acid and ergosterol in sprouted and cooked samples rationalizing their noteworthy α-amylase and α-glucosidase inhibitory activities. Taken together, this integrated work provides insightful perspectives beyond the positive impact of different processing protocols on bioactives accumulation and pharmacological traits of RKB expanding their utilization as functional hypoglycemic food to rectify diabetes.

Study on ferritin glycation with dextran: Physicochemical characterization and its application in the delivery of resveratrol

Ferritin exhibits promising prospects for nanoencapsulation applications, however, its susceptibility to environmental factors as a standalone carrier necessitates further consideration. In this study, the recombinant human H-chain ferritin (rHuHF) was modified with dextran (Dex) to enhance its physicochemical and functional properties. Moreover, the glycated rHuHF cavity was utilized for the encapsulation of resveratrol (Res). The results demonstrated that the glycoconjugates (Dex–rHuHF) achieved the highest grafting degree of 34.71% under the following conditions: Dex molecular weight of 40 kDa, mass ratio of rHuHF to Dex at 1:2, pH value of 7.8, relative saturation humidity of 79%, reaction temperature at 50 °C, and reaction time of 30 h. Dex interacted with rHuHF and exhibited protective effects on rHuHF under extremely acidic conditions. Each Dex–rHuHF cavity encapsulated approximately 22 Res molecules with an encapsulation rate of 10.84%. The Dex–rHuHF–Res nanoparticles displayed excellent photothermal stability and sustained release properties. Furthermore, the Dex–rHuHF–Res simulated digesta showed enhanced abilities in scavenging DPPH free radicals and inhibiting α-glucosidase activity. This work investigated the impact of Dex on the physicochemical properties of rHuHF and developed a novel approach by grafting Dex onto rHuHF for encapsulating hydrophobic substances like resveratrol, which holds potential applications in water-based food and nutraceutical formulations.

The Leaf Extract of Dysoxylum parasiticum (Osbeck) Kosterm. Contains Anti-oxidant and α-Glucosidase Inhibitor Activities

The medicinal plant Dysoxylum parasiticum (Osbeck) Kosterm. (Meliaceae) is native to Indonesia, but its bioactive potential has been little explored. This study de- termined the phenolic content, antioxidant, and antidiabetic activities of D. parasitic- cum leaf extracts. Dried, powdered leaves were sequentially extracted with hexane, ethyl acetate, and methanol. Total phenolic and flavonoid contents were quantified by colorimetric assays. The ethyl acetate extract had the highest phenolic content at 21.54 mg gallic acid equivalents/g dry weight. Antioxidant capacity was evaluated by DPPH radical scavenging assay, while antidiabetic activity was assessed as inhibition of α-glucosidase enzyme. The ethyl acetate extract showed potent antioxidant (IC50 30.72 μg/mL) and α-glucosidase inhibitory (IC50 16.32 μg/mL) activities compared to standard controls. Putative bioactive components were identified by LC-MS/MS, including stylosin, capillartemisin A, 19β-glucosyl-14-deoxy-11,12- didehydroandrographoside, daturametelin H, stigmas-3,6-dione, 2α,3β,4α-trihy- droxy nortropane and arnebinone. The traditional use of D. parasiticum is validated by its antioxidant and anti-diabetic potential, which is associated with its phenolic content.

Isoxerophilusins A and B, Two Novel Polycyclic Asymmetric Diterpene Dimers from Isodon xerophilus: Structural Elucidation, Modification, and Inhibitory Activities against α-Glucosidase.

Isoxerophilusins A (1) and B (2), two unprecedented diterpene heterodimers biogenetically from ent-atisanes and abietanes, were isolated from the rhizomes of Isodon xerophilus. Their structures were determined by extensive spectroscopic analysis and single-crystal X-ray diffraction. Selective esterification of 1 generated 11 new derivatives. All derivatives showed excellent α-glucosidase inhibitory activity in comparison to acarbose. Compounds 12 and 13 demonstrated significant inhibition against α-glucosidase with IC50 values of 4.92 and 3.83 μM, respectively.

Synthesis of modified Schiff base appended 1,2,4-triazole hybrids scaffolds: elucidating the invitro and in silico α-amylase and α-glucosidase inhibitors potential.

The current study involves the synthesis of Schiff bases based on 1,2,4-triazoles skeleton and assessing their α-amylase and α-glucosidase profile. Furthermore, the precise structures of the synthesized derivatives were elucidated using various spectroscopic methods such as 1H-NMR, 13C-NMR and HREI-MS. Using glimepiride as the reference standard, the invitro α-glucosidase and α-amylase inhibitory activities of the synthesized compounds were evaluated in order to determine their potential anti-diabetic properties. All analogues showed varied range of inhibitory activity having IC50 values ranging from 17.09±0.72 to 45.34±0.03 μM (α-amylase) and 16.35±0.42 to 42.31±0.09 μM (α-glucosidase), respectively. Specifically, the compounds 1, 7 and 8 were found to be significantly active with IC50 values of 17.09±0.72, 19.73±0.42, and 23.01±0.04 μM (against α-amylase) and 16.35±0.42, 18.55±0.26, and 20.07±0.02 μM (against α-glucosidase) respectively. The obtained results were compared with the Glimepiride reference drug having IC50values of 13.02±0.11 μM (for α-glucosidase) and 15.04±0.02 μM (for α-amylase), respectively. The structure-activity relationship (SAR) studies were conducted based on differences in substituent patterns at varying position of aryl rings A and B may cause to alter the inhibitory activities of both α-amylase and α-glucosidase enzymes. Additionally, the molecular docking study was carried out to explore the binding interactions possessed by most active analogues with the active sites of targeted α-amylase and α-glucosidase enzymes.

Magnetic ligand fishing protocol combined with HPLC-FT-ICR-MS for screening potential α-Glucosidase inhibitors from UCG and in silico analysis

Uremic Clearance Granule (UCG) is a traditional Chinese medicines (TCMs) that has been recognized as potentially effective treatment for diabetic nephropathy (DN). However, the chemical composition and the hypoglycemic ingredients of UCG remain unclear. In this experiment, a magnetic ligand fishing protocol combined with HPLC coupled Fourier transform ion cyclotron resonance mass spectrometry (HPLC-FT-ICR-MS) technology was developed to screen and identify α-Glucosidase inhibitors from UCG. First, constituents of UCG was identified by HPLC-FT-ICR-MS. Next, α-Glucosidase coated Fe3O4@SiO2@NH2 (Fe3O4@SiO2@NH2@α-Glucosidase) nano composites was synthesized. The essential parameters (concentration of Glutaraldehyde (GA), ratio of Fe3O4@SiO2@NH2 to enzyme, crosslinking time and immobilization time) were optimized to obtain maximum enzyme activity and the performance of immobilized enzyme was compared with that of free enzyme. The α-Glucosidase inhibitory activities were then evaluated using autodock and the 4-Nitrophenyl-α-D-glucopyranoside (pNPG) method. As a result, 142 compounds were identified were identified by comparing the retention time, molecular ions and fragmentation behaviors with the reference compounds or the in-house database. 20 possible α-Glucosidase activity inhibitory components were identified using HPLC-FT-ICR-MS. Molecular docking and inhibition studies showed that 4 compuunds including Limonexic acid, Sanggenol A, Glabrone, Matrine were more likely to stronger α-Glucosidase inhibitory activities than acarbose. In conclusion, the proposed approach, which combined highly specific screening with HPLC-FT-ICR-MS, provided a powerful platform for discovering bioactive components from multi-component and multi-target traditional Chinese medicines (TCMs).

Design, synthesis and biological Evaluation of novel chromones having 3,4-dihydropyrimidin-2(1H)-one core at C-8 in combination with triazoles: New α-glucosidase inhibitors and anti-bacterial agents

The Biginelli reaction synthesizes dihydropyrimidones through a multi-component reaction. A β-ketoester, aldehyde, and urea or thiourea react in the presence of an acid catalyst to form these dihydropyrimidones. 3,4-Dihydropyrimidin-2(1H)-One/Chromone/Triazole hybrids (9a-9l) were synthesized by multiple steps including one pot Biginelli multicomponent reaction depicted in the scheme. An efficient method for the Biginelli reaction of Chromone aldehyde, acetoacetate esters, and urea employed in the presence of ferric chloride is described. In the end, we have successfully synthesized twelve derivatives of 3,4-Dihydropyrimidin-2(1H)-One/Chromone/Triazole hybrids and subjected them to testing for Antibacterial activity and α-glucosidase inhibition activity. Among these derivatives, compound 9g (IC50 = 142.92 nmol) and 9e (144.49 nmol) exhibited significant inhibitory activity in comparison to the positive control acarbose (IC50 = 350.91 nmol). Compound 9g demonstrated the most significant suppression against Escherichia coli and Bacillus cereus, with zone diameters of 8.8 ± 1.35 mm and 9.1 ± 0.23 mm, respectively. Compound 9b displayed a clear area where bacterial growth was inhibited, measuring 7.5 ± 1.25 mm against Klebsiella pneumonia. Compound 9k exhibited a zone of inhibition measuring 8 ± 1.2 mm in radius against Staphylococcus epidermidis. The docking results for the synthesized compounds indicate that compound 9b exhibited the most favorable docking score of −10 kcal/mol, whereas compound 9a had the second-best docking score of −8.7 kcal/mol. Molecular docking was utilized to examine the interactions between the title compounds and α-glucosidase, in order to provide valuable insights. The data obtained revealed significant interactions that contribute to the inhibitory effects of the drugs against α-glucosidase. These compounds exhibit significant potential as attractive initial candidates for the development of new α-glucosidase inhibitors.

Optimization of subcritical water extraction, UPLC–triple–TOF–MS/MS analysis, antioxidant and α-glucosidase inhibitory activities of anthocyanins from Nitraria sibirica Pall. fruits

This study aimed to optimize subcritical water extraction process, characterize chemical composition and investigate the biological activities of Nitraria sibirica Pall. (NSP) anthocyanin. Overall, the optimization was achieved under following conditions: extraction temperature 140 °C, extraction time 45 min and flow rate 7 mL/min with the extraction yield of 1.075 mg/g. 3 cyanidin, 3 petunidin, 1 delphinidin and 1 pelargonidin compounds were identified in the anthocyanic extract from NSP via UPLC–Triple–TOF–MS/MS. NSP anthocyanin exhibited better DPPH free-radical scavenging activity than ascorbic acid. It displayed superior α-glucosidase inhibition activity, which was ∼14 times higher than that of acarbose. Moreover, enzyme kinetics results indicated that NSP anthocyanin behaved as a reversible, mixed-type inhibitor. Molecular docking and molecular dynamics simulation results revealed that NSP anthocyanin interacted with α-glucosidase mainly via van der Waals forces, hydrogen bond and possessed fairly stable configuration. Therefore, NSP anthocyanin is a promising α-glucosidase inhibitor for diabetes mellitus.

Interaction between orange juice and < 1 kDa leaf peptides: effect on the antioxidant and antidiabetic related enzyme inhibitory activities

Designing a good vehicle for functional ingredients is the major focus of this study. Small molecular weight peptides (< 1 kDa) extracted from amaranth leaf protein (ALP), eggplant leaf protein (ELP) and fluted pumpkin leaf protein (FLP) were incorporated into freshly prepared orange juice at an effective and inhibitory concentrations of the peptides. The rate of degradation of ascorbic acid was more in the control juice (140.06 to 18.43 mg/mL) when compared with juice containing peptides at both storage conditions (140.08 to 32.32 mg/mL). However, the rate of ascorbic acid reduction during storage (refrigerated and ambient) was least in the juice containing peptide, isolated from ELP when compared with the juice samples that contained peptides isolated from ALP and FLP. After the eighth week of storage, juice that contained FLP peptide had greater amounts of residual total phenolic content (370.53 & 432.33 µg GAE/100 mL), juice that contained ALP peptide retained better ability to scavenge DPPH radicals (52.32 & 66.84%) while juice sample that contained ELP retained more metal chelating activities (44.82 and 51.03%). The results of antidiabetic property showed that juice containing peptide isolated from ALP contained greater amounts of α-amylase inhibitory activity (41.50 and 46.89%) while greater amounts of α-glucosidase inhibitory activities were retained in juice that contained peptide isolated from FLP. The results concluded that orange juice may be considered a veritable vehicle for functional ingredients for improved health.Graphical

Comprehending the inhibition mechanism of indole-based bis-acylhydrazone compounds on α-glucosidase: Spectral and theoretical approaches

Indole-based bis-acylhydrazone compounds can inhibit the activity of α-glucosidase and control the concentration of blood glucose. In this paper, the characteristics of three indole-based bis-acylhydrazone compounds with different inhibitory activities of α-glucosidase as well as the interaction with α-glucosidase were studied by experiments and computational simulation techniques. Enzyme kinetic and spectral experiments showed that the indole-based bis-acylhydrazone compounds were able to inhibit enzyme activity through mixed inhibition dominated by competitive inhibition, and during the binding reaction, indole-based bis-acylhydrazone compounds can quench the intrinsic fluorescence of α-glucosidase through static quenching and an aggregation of the indole-based bis-acylhydrazone with α-glucosidase produces a stable complex with a molar ratio of 1:1, and the combination of indole-based bis-acylhydrazone compounds could lead to slight change in the conformation of α-glucosidase. The theoretical simulation demonstrated that the stability of the complex systems was positively correlated with the inhibitory activity of indole-based bis-acylhydrazone compounds, and the indole-based bis-acylhydrazone compounds occupied the active site in the multi-ligand system, resulting in a significant decrease in the binding ability of starch to active amino acids. These results suggested that indole-based bis-acylhydrazone compound was expected to be a new type of α-glucosidase inhibitor.

Bioactive Phenylpropanoid Glycosides, Dimers, and Heterodimers from the Bark of Cinnamomum cassia (L.) J.Presl.

Six new phenylpropanoid glycosides (1-6), two new phenylethanol glycosides (7 and 8), one new phenylmethanol glycoside (9), three new phenylpropanoid dimers (10-12), two new phenylpropanoid-flavan-3-ol heterodimers (13 and 14), and six known relevant compounds (15-20) were isolated and identified from the well-liked edible and medicinal substance (the bark of Cinnamomum cassia (L.) J.Presl). The structures of these isolates were determined by using spectroscopic analyses, chemical methods, and quantum chemical calculations. Notably, compounds 4-9 were rare apiuronyl-containing glycosides, and compounds 13 and 14 were heterodimers of phenylpropanoids and flavan-3-ols linked through C-9″-C-8 bonds. The antioxidant and α-glucosidase inhibitory activities of all isolates were evaluated. Compounds 10 and 12 exhibited DPPH radical scavenging capacities with IC50 values of 20.1 and 13.0 μM, respectively (vitamin C IC50 value of 14.3 μM). In the ORAC experiment, all these compounds exhibited different levels of capacity for scavenging free radicals, and compound 10 displayed extraordinary free radical scavenging capacity with the ORAC value of 6.42 ± 0.01 μM TE/μM (EGCG ORAC value of 1.54 ± 0.02 μM TE/μM). Compound 12 also showed significant α-glucosidase inhibitory activity with an IC50 of 56.3 μM (acarbose IC50 of 519.4 μM).

Design of Scaffolds Based on Zinc-Modified Marine Collagen and Bilberry Leaves Extract-Loaded Silica Nanoparticles as Wound Dressings.

In this study, wound dressings were designed using zinc-modified marine collagen porous scaffold as host for wild bilberry (WB) leaves extract immobilized in functionalized mesoporous silica nanoparticles (MSN). These new composites were developed as an alternative to conventional wound dressings. In addition to the antibacterial activity of classic antibiotics, a polyphenolic extract could act as an antioxidant and/or an anti-inflammatory agent as well. Wild bilberry leaves extract was prepared by ultrasound-assisted extraction in ethanol and its properties were evaluated by UV-Vis spectroscopy (radical scavenging activity, total amount of polyphenols, flavonoids, anthocyanins, and condensed tannins). The extract components were identified by HPLC, and the antidiabetic properties of the extract were evaluated via α-glucosidase inhibitory activity. Spherical MSN were modified with propionic acid or proline moieties by post-synthesis method and used as carriers for the WB leaves extract. The textural and structural features of functionalized MSN were assessed by nitrogen adsorption/desorption isotherms, small-angle XRD, SEM, TEM, and FTIR spectroscopy. The composite porous scaffolds were prepared by freeze drying of the zinc-modified collagen suspension containing WB extract loaded silica nanoparticles. The properties of the new composites demonstrated enhanced properties in terms of thermal stability of the zinc-collagen scaffold, without altering the protein conformation, and stimulation of NCTC fibroblasts mobility. The results of the scratch assay showed contributions of both zinc ions from collagen and the polyphenolic extract incorporated in functionalized silica in the wound healing process. The extract encapsulated in functionalized MSN proved enhanced biological activities compared to the extract alone: better inhibition of P. aeruginosa and S. aureus strains, higher biocompatibility on HaCaT keratinocytes, and anti-inflammatory potential demonstrated by reduced IL-1β and TNF-α levels. The experimental data shows that the novel composites can be used for the development of effective wound dressings.

Augmentation of α-amylase and α-glucosidase inhibitory properties of Callerya speciosa root extracts: An exploration through simulated human gastrointestinal digestion

The present work represents the first effort to evaluate the effect of an in vitro simulated human digestion model on the α-amylase and α-glucosidase inhibitory activities of Callerya speciosa root extracts. Through bioguided fractionation, a series of fractions were obtained from hexane (CSH) and ethyl acetate (CSE) extracts. Initial screening identified active fractions (CSH2, CSH3, CSE2, CSE3, and CSE4) for further in vitro digestion evaluation. The results showed a decrease in antioxidant activity across all samples after digestion, while a simultaneous increase in α-amylase and α-glucosidase inhibitory activities was observed during the small intestinal phase. Notably, compared with the undigested fraction, CSE3 demonstrated a 1.7-fold increase in α-amylase inhibition (IC50 = 0.86 mg/mL). Moreover, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were significantly greater after digestion, with IC50 values of 0.18, 0.05, and 0.02 mg/mL, respectively. Impressively, during the small intestinal phase, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were substantially greater than those of acarbose by 13.2-, 47.6-, and 119.0-fold, respectively, and greater than those of palmitic acid by 1.7-, 6.0-, and 15.0-fold, respectively. GC-MS and LC-ESI-MS/MS analyses identified isoflavonoids, fatty acids, and triterpenoids as key bioactive compounds in these fractions. The present work provided foundational insights for the future exploration of C. speciosa root extracts for diabetes management.