RESUMEN

BACKGROUND: Peganum harmala L. is used in traditional medicine to treat several health ailments. Hence, the present work aimed to investigate the DPPH free radical scavenging, α-amylase, cytotoxic, and antifibrotic effects of the hydrophilic extract and fixed oil obtained from P. harmala seeds. METHODS: The hydrophilic extract and fixed oil of P. harmala were assessed for their abilities to scavenge DPPH free radicals and inhibit α-amylase using reference bioassays. The cytotoxicity was assessed on several cancer and normal cell lines, including B16F1, Caco-2, COLO205, HeLa, Hep 3B and Hep G2, MCF-7, and HEK-293 T cells. The MTS assay was used to evaluate the antifibrotic capabilities utilizing the human hepatic stellate (LX-2) cell line. RESULTS: P. harmala plant fixed oil has potent DPPH free radical scavenging activity with an IC50 dose of 79.43 ± 0.08 µg/ml. Besides, the hydrophilic extract has a poor anti-α-amylase effect compared with the antidiabetic drug Acarbose, with IC50 doses of 398 ± 0.59 and 25.11 ± 1.22 µg/ml, respectively. In addition, the growth of MCF-7, Hep3B, HepG2, HeLa, COLO205, CaCo2, B16F1, and HeK293t was inhibited by P. harmala hydrophilic extract with IC50 doses of 121.34 ± 1.71, 268.3 ± 0.75, 297.20 ± 1.00, 155.60 ± 1.14, 150.01 ± 0.51, 308.35 ± 0.53, 597.93 ± 1.36, and 5.38 ± 0.99 µg/ml, respectively. In addition, at 1000 µg/ml, 5-Fluorouracil reduced fibrosis cells by 0.089%, while the hydrophilic extract decreased the number of LX-2 cells by 5.81%. CONCLUSION: P. harmala plant-fixed oil exhibits potential antioxidant properties. While the hydrophilic extract showed limited effectiveness as an anti-α-amylase agent and demonstrated notable cytotoxic effects against various tested cancer cell lines. Furthermore, this extract significantly reduces the number of LX-2 fibrotic cells. These findings emphasize the therapeutic potential of these products in managing various health disorders and warrant further investigation into their mechanisms of action and clinical applications.

Asunto(s)

Depuradores de Radicales Libres , Peganum , Extractos Vegetales , alfa-Amilasas , Humanos , Peganum/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , alfa-Amilasas/antagonistas & inhibidores , Depuradores de Radicales Libres/farmacología , Línea Celular Tumoral , Semillas/química

RESUMEN

Exopolysaccharides produced by lactic acid bacteria have gained attention for their potential health benefits and applications in functional foods. This study explores the isolation and characterization of a novel exopolysaccharide-producing strain from dairy products. The aim was to evaluate its probiotic potential and investigate the properties of the produced exopolysaccharide. A strain identified as Enterococcus faecium PCH.25, isolated from cow butter, demonstrated exopolysaccharide production. The study's novelty lies in the comprehensive characterization of this strain and its exopolysaccharide, revealing unique properties with potential applications in food, cosmetic, and pharmaceutical industries. The E. faecium PCH.25 strain exhibited strong acid tolerance, with a 92.24% viability rate at pH 2 after 2 h of incubation. It also demonstrated notable auto-aggregation (85.27% after 24 h) and co-aggregation abilities, antibiotic sensitivity, and absence of hemolytic activity, suggesting its probiotic potential. The exopolysaccharide produced by this strain showed bactericidal activity (MIC and MBC = 1.8 mg/ml) against Listeria monocytogenes and antioxidant properties (22.8%). Chemical analysis revealed a heteropolysaccharide composed of glucose and fructose monomers, with various functional groups contributing to its bioactivities. Physical characterization of the exopolysaccharide indicated thermal stability up to 270 °C, a negative zeta-potential (-27 mV), and an average particle size of 235 nm. Scanning electron microscopy and energy dispersive X-ray analysis revealed a smooth, nonporous structure primarily composed of carbon and oxygen, with an amorphous nature. These findings suggest that the exopolysaccharide from E. faecium PCH.25 has potential as a natural antibacterial and antioxidant polymer for use in functional foods, cosmetics, and pharmaceuticals.

Asunto(s)

Antibacterianos , Antioxidantes , Mantequilla , Enterococcus faecium , Listeria monocytogenes , Polisacáridos Bacterianos , Probióticos , Enterococcus faecium/metabolismo , Probióticos/aislamiento & purificación , Probióticos/farmacología , Antioxidantes/farmacología , Antioxidantes/metabolismo , Antioxidantes/química , Polisacáridos Bacterianos/metabolismo , Polisacáridos Bacterianos/química , Polisacáridos Bacterianos/aislamiento & purificación , Animales , Listeria monocytogenes/efectos de los fármacos , Mantequilla/microbiología , Bovinos , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana

RESUMEN

The health-promoting properties of black elderberry are related to its high content of polyphenols (natural antioxidants), which eliminate free radicals and prevent the formation of oxidative stress responsible for many diseases. The aim of this work was to determine, the anti-radical effect of Sambucus nigra infusions based on the reaction with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and galvinoxyl (Glv) radicals and to determine the function describing the disappearance curves of these radicals. The antioxidant properties of infusions obtained from the flowers and fruits of this plant were tested using the modified Brand-Williams method using DPPH and Glv radicals. Higher antioxidant activity towards both the DPPH and Glv radicals was found in flowers compared to fruits. In addition, it was found that the process of quenching radicals in the reaction with Sambucus nigra infusions proceeds in accordance with the assumptions of second-order reaction kinetics. The infusion obtained from flowers quenched radicals faster than fruit infusions. The applied second-order kinetics equation may enable estimation of antioxidants levels in natural sources of radicals.

RESUMEN

Recent evidence suggests that mulberry leaves have good antioxidant activity. However, what the antioxidant ingredient is and how the ingredient works are still not well understood. In this study, we enzymatically hydrolyze mulberry leaf proteins (MLPs) using neutral protease and find that the mulberry leaf protein hydrolysates (MLPHs) have stronger antioxidant activity compared to MLPs. We separate the core antioxidant components in MLPHs by ion-exchange columns and molecular sieves and identify 798 antioxidant peptides by LC-MS/MS. Through bioinformatics analysis and biochemical assays, we screen two previously unreported peptides, P6 and P7, with excellent antioxidant activities. P6 and P7 not only significantly reduce ROS in cells but also improve the activities of the antioxidant enzymes SOD and CAT. In addition, both peptides are found to exert protective effects against H2O2-induced chromatin damage and cell apoptosis. Collectively, these results provide support for the application of mulberry leaf peptides as antioxidants in the medical, food and livestock industries.

RESUMEN

Lipid metabolism dysregulation can lead to dyslipidemia and obesity, which are major causes of cardiovascular disease and associated mortality worldwide. The purpose of the study was to obtain and characterize six plant extracts (ACE-Allii cepae extractum; RSE-Rosmarini extractum; CHE-Cichorii extractum; CE-Cynarae extractum; AGE-Apii graveolentis extractum; CGE-Crataegi extractum) as promising adjuvant therapies for the prevention and treatment of dyslipidemia and its related metabolic diseases. Phytochemical screening revealed that RSE was the richest extract in total polyphenols (39.62 ± 13.16 g tannic acid/100 g dry extract) and phenolcarboxylic acids (22.05 ± 1.31 g chlorogenic acid/100 g dry extract). Moreover, the spectrophotometric chemical profile highlighted a significant concentration of flavones for CGE (5.32 ± 0.26 g rutoside/100 g dry extract), in contrast to the other extracts. UHPLC-MS quantification detected considerable amounts of phenolic constituents, especially chlorogenic acid in CGE (187.435 ± 1.96 mg/g extract) and rosmarinic acid in RSE (317.100 ± 2.70 mg/g extract). Rosemary and hawthorn extracts showed significantly stronger free radical scavenging activity compared to the other plant extracts (p < 0.05). Pearson correlation analysis and the heatmap correlation matrix indicated significant correlations between phytochemical contents and in vitro antioxidant activities. Computational studies were performed to investigate the potential anti-obesity mechanism of the studied extracts using target prediction, homology modeling, molecular docking, and molecular dynamics approaches. Our study revealed that rosmarinic acid (RA) and chlorogenic acid (CGA) can form stable complexes with the active site of carbonic anhydrase 5A by either interacting with the zinc-bound catalytic water molecule or by directly binding Zn2+. Further studies are warranted to experimentally validate the predicted CA5A inhibitory activities of RA and CGA and to investigate the hypolipidemic and antioxidant activities of the proposed plant extracts in animal models of dyslipidemia and obesity.

RESUMEN

Vacuum impregnation is a novel methodology for adding various substances to porous foods. This study aimed to develop a cost effective automate system for vacuum impregnation of food materials to enhance their nutritional, functional and sensory properties depending on the functionality of the impregnation solution. The developed vacuum impregnation system includes a vacuum chamber, vacuum pump and an automation setup for creating and maintaining vacuum conditions, feeding impregnated solutions to the samples and releasing vacuum. Fresh-cut spinach leaves were impregnated with ascorbic acid (AsA) and calcium chloride (Cacl2) (10% concentration) in the setup in order to test the effect of the process on some biochemical properties. Statistical analysis revealed significant effect of vacuum impregnation on the biochemical properties (total soluble solids, total phenolic content, flavonoid content and free radical scavenging activity) and color of spinach leaves during storage up to 4 days. Impregnation process showed significant increase in the total phenolic and flavonoid content of the spinach leaves. Increment up to 78% in antioxidant activity was seen for the uncoated impregnated leaves as compared to 59% activity in untreated samples. Thus, products with desired parameters can be produced with this process with minimal impact on their properties at a lower cost and in a shorter time period.

RESUMEN

In this investigation, three medicinal plant powders and a composite flour developed from them were analyzed. FESEM/EDS illustrated irregularly shaped particles in the plant powders except for Withania, which had round to oval shape particles. XRD analysis displayed a semi-crystalline nature of powders, except for Asparagus, which showed amorphous behavior. Both methanol and ethanol plant extracts exhibited significantly higher antioxidants, total phenols, and cell viability. Amongst, optimized composite flour (OCF) methanolic extract demonstrated the highest total phenolic content (69.2 ± 0.11 µg GAE/ml), potent cell viability against A549 cells (3.35 ± 0.15% at 50 µg/ml), and strong free-radical scavenging activity (48.89 ± 0.67 at 200 µg/ml). GCMS and FTIR analyses of the methanolic extracts demonstrated the presence of essential phytoconstituents and functional groups. In silico studies of the phytocomponents, ethyl isoallocholate, 3-Deoxy-d-mannoic lactone, and 4,5-Diamino-2-hydroxypyrimidine suggested good binding affinity against BAX, P53, and EGFR proteins with no toxicity and a good drug score.

Asunto(s)

Antioxidantes , Supervivencia Celular , Harina , Fitoquímicos , Extractos Vegetales , Plantas Medicinales , Humanos , Antioxidantes/química , Antioxidantes/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fitoquímicos/química , Fitoquímicos/farmacología , Plantas Medicinales/química , Harina/análisis , Supervivencia Celular/efectos de los fármacos , Células A549 , Fenoles/química

RESUMEN

A series of six unsymmetrical thiourea derivatives, namely 1-cyclohexyl-3-(pyridin-2-yl) thiourea (1), 1-cyclohexyl-3-(3-methylpyridin-2-yl)thiourea (2), 1-cyclohexyl-3-(2,4-dimethylphenyl) thiourea (3), 1-(4-chlorophenyl)-3-cyclohexylthiourea (4), 1-(3-methylpyridin-2-yl)-3-phenylthiourea (5), and 1-(3-chlorophenyl)-3-phenylthiourea (6), were successfully synthesized via reaction between different amines with isothiocyanates under a non-catalytic environment. Structural elucidation of compounds (1-6) was performed using FT-IR and NMR (1H and 13C) spectroscopy. The infrared spectra displayed characteristic stretching vibrations, while the 13C NMR chemical shifts of the thiourea moiety (C[bond, double bond]S) were observed in the range of 179.1-181.4 ppm. The antioxidative and antimicrobial properties of the compounds were assessed, as well as their inhibitory effects on acetylcholinesterase and butyrylcholinesterase were evaluated. In order to analyze the fluorescence characteristics of each compound (1-6), the excitation (λex) and emission (λem) wavelengths were scanned within the range of 250-750 nm, with the solvent blank serving as a standard. It was observed that when dissolved in acetone, toluene, tetrahydrofuran, and ethyl acetate, these compounds exhibited emission peaks ranging from 367 to 581 nm and absorption peaks ranging from 275 to 432 nm.

RESUMEN

Inflammation and the injuries produced by free radicals are interconnected and influence each other. The underlying mechanisms of inflammation are partially attributed to the release of free radicals by immune cells, prooxidants that can also cause protein alteration. This study was performed in order to assess the potential anti-inflammatory effect of two bee venom samples harvested from Apis mellifera. Free radical scavenging capacity was investigated using DPPH and ABTS.+ tests and protective effect on proteins through the inhibitory activity on thermal denaturation of albumin.

RESUMEN

Sophora exigua (SE) was sequentially extracted using hexane, ethyl acetate, and ethanol. The obtained extracts were tested for antioxidant activity. Among them, the fractionated ethyl acetate extract (SE-EA) showed the highest potential in free radical scavenging and ferric-reducing properties. The chemical analysis identified sophoraflavanone G as one of the active ingredients in SE-EA. According to SE-EA solubility, SE-EA liposomes were developed using a sonication-assisted thin film method. Cholesterol and phospholipids were used as the main compositions of the liposomes. The obtained liposomes were spherical with different nano-size ranges, size distribution, and zeta potential depending on SE-EA and total lipid concentrations. SE-EA liposomes were slightly bigger than their empty liposomes. All liposomes exhibited a phospholipid crystalline structure. Cholesterol and SE-EA existed in the liposomes as an amorphous state. SE-EA liposomes with high total lipid content exhibited high entrapment efficiency and sustained release behavior. Whereas liposomes with low total lipid content showed low entrapment efficiency and fast-release behavior. All SE-EA liposomes showed stronger antioxidant activity than the non-entrapped SE-EA. In conclusion, SE-EA is a natural source of potent antioxidants. The developed SE-EA liposomes are a promising pharmaceutical formulation to efficiently deliver the active ingredients of SE-EA and are suitable for further study in vivo.

Asunto(s)

Antioxidantes , Liposomas , Extractos Vegetales , Sophora , Sophora/química , Antioxidantes/farmacología , Antioxidantes/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Tamaño de la Partícula , Solubilidad , Colesterol/química

RESUMEN

Radiotherapy commonly causes damage to healthy tissues, particularly radiation-induced skin injury (RISI) that affects a significant majority of patients undergoing radiotherapy. Effective treatments for RISI are lacking. This study focuses on the pathogenesis of RISI, which primarily involves oxidative stress. Excessive reactive oxygen species (ROS) generation during radiation induces damage to biological macromolecules, triggering oxidative stress and inflammation. To address this, ergothioneine (EGT), a natural and biocompatibile thiol compound with excellent antioxidant activity, is explored as a potential radiation-protective agent. By utilizing its specific transport and absorption in the skin tissue, as well as its efficient and stable clearance of radiation-induced "ROS storm", EGT is combined with sodium hyaluronate (NaHA) to develop a novel radiation protective dressing suitable for the skin. This EGT-NaHA dressing demonstrates an effective ability to scavenge free radicals and reduce oxidative stress in vitro and in vivo, reducing cellular apoptosis and inflammation. These results demonstrate the protective properties of EGT against RISI, with far-reaching implications for research and development in the field of radioprotection.

Asunto(s)

Vendajes , Ergotioneína , Ácido Hialurónico , Estrés Oxidativo , Protectores contra Radiación , Piel , Ácido Hialurónico/química , Ácido Hialurónico/farmacología , Ergotioneína/farmacología , Ergotioneína/química , Animales , Estrés Oxidativo/efectos de los fármacos , Estrés Oxidativo/efectos de la radiación , Piel/efectos de los fármacos , Piel/efectos de la radiación , Piel/patología , Ratones , Humanos , Protectores contra Radiación/farmacología , Protectores contra Radiación/química , Protectores contra Radiación/uso terapéutico , Especies Reactivas de Oxígeno/metabolismo , Antioxidantes/farmacología , Antioxidantes/química , Apoptosis/efectos de los fármacos , Apoptosis/efectos de la radiación , Traumatismos por Radiación/tratamiento farmacológico , Traumatismos por Radiación/prevención & control

RESUMEN

Thrombotic diseases impose a significant global health burden, and conventional drug-based thrombolytic therapies are encumbered by the risk of bleeding complications. In this study, we introduce a novel drug-free nanomedicine founded on tea polyphenols nanoparticles (TPNs), which exhibits multifaceted capabilities for localized photothermal thrombolysis. TPNs were synthesized through a one-pot process under mild conditions, deriving from the monomeric epigallocatechin-3-gallate (EGCG). Within this process, indocyanine green (ICG) was effectively encapsulated, exploiting multiple intermolecular interactions between EGCG and ICG. While both TPNs and ICG inherently possessed photothermal potential, their synergy significantly enhanced photothermal conversion and stability. Furthermore, the nanomedicine was functionalized with cRGD for targeted delivery to activated platelets within thrombus sites, eliciting robust thrombolysis upon laser irradiation across diverse thrombus types. Importantly, the nanomedicine's potent free radical scavenging abilities concurrently mitigated vascular inflammation, thus diminishing the risk of disease recurrence. In summary, this highly biocompatible multifunctional nanomaterial holds promise as a comprehensive approach that combines thrombolysis with anti-inflammatory actions, offering precision in thrombosis treatment.

Asunto(s)

Nanomedicina , Trombosis , Humanos , Polifenoles/farmacología , Té , Terapia Trombolítica , Verde de Indocianina/farmacología , Verde de Indocianina/uso terapéutico , Inflamación/tratamiento farmacológico , Trombosis/tratamiento farmacológico

RESUMEN

Reactive oxygen species (ROS) are implicated in various pathological conditions due to their ability to induce oxidative damage to cellular components. In this study, we investigated the antioxidant properties of a peptide isolated from the hydrolysate of Manila clam (Ruditapes philippinarum) muscle. Purification steps yielded RPTE2-2-4, exhibiting potent scavenging activities against DPPH•, HO•, and O2•-, akin to Vitamin C. Structural analysis showed that the isolated peptide, LFKKNLLTL, exhibited characteristics associated with antioxidant activity, including a short peptide length and the presence of aromatic and hydrophobic amino acid residues. Moreover, our study demonstrated the cytoprotective effects of the peptide against H2O2-induced oxidative stress in HepG2 cells. Pretreatment with the peptide resulted in a dose-dependent reduction in intracellular ROS levels and elevation of glutathione (GSH) levels, indicating its ability to modulate cellular defense mechanisms against oxidative damage. Furthermore, the peptide stimulated the expression of the cytoprotective enzyme heme oxygenase-1 (HO-1), further reinforcing its antioxidant properties. Overall, our findings highlight the potential of the Manila clam-derived peptide as a natural antioxidant agent with therapeutic implications for oxidative stress-related diseases. Further investigation into its mechanisms of action and in vivo efficacy is warranted to validate its therapeutic potential.

RESUMEN

Microwave (MW) radiations are widely used in communications, radar and medical treatment and thus human exposure to MW radiations have increased tremendously, raising health concerns as MW has been implicated in induction of oxidative stress condition in our body. Few metallic nanoparticles (NPs) have been shown to mimic the activity of antioxidant enzymes and hence can be applied for the modulation of adverse effects caused by MW. Present study aimed to assess the biocompatibility of Bovine serum albumin (BSA) conjugated manganese dioxide nanoparticles (MNP*) and to counteract the impact of MW on the haematological system of male Wistar rats. Experiments were conducted in two sets. Set I involved biodistribution and antioxidant activity evaluation of MNP* at different doses. Results showed a dose-dependent increase in antioxidant potential and significant biodistribution in the liver, spleen, kidney, and testis, with no organ damage, indicating its biocompatibility. Experiment set II constituted the study of separate and combined effects of MW and MNP* on haematological parameters, oxidative status, and genotoxic study in the blood of rats. MW exposure significantly altered red blood cell count, hemoglobin, packed cell volume percentage, monocyte percentage, aspartate aminotransferase, Alanine aminotransferase and uric acid. MW also induced significant DNA damage in the blood. A significant increase in lipid peroxidation and a decrease in antioxidant enzyme superoxide dismutase was also observed in MW exposed group. However, these alterations were reduced significantly when MNP* was administered. Thus, MNP* showed biocompatibility and modulatory effects against MW-induced alterations in the haematological system of rats.

Asunto(s)

Compuestos de Manganeso , Microondas , Nanopartículas , Óxidos , Ratas Wistar , Albúmina Sérica Bovina , Animales , Masculino , Compuestos de Manganeso/química , Ratas , Albúmina Sérica Bovina/química , Óxidos/química , Nanopartículas/química , Estrés Oxidativo/efectos de los fármacos , Bovinos , Antioxidantes/farmacología , Nanopartículas del Metal/química

RESUMEN

In the last few decades, researchers have thoroughly studied the use of plants in Palestine, one of them is Cyclamen persicum Mill. (C. persicum). Cyclamen persicum has been historically cultivated since the 1700s due to its tuber. The tuber is known to stimulate the nasal receptors, thus triggering the sensory neurons. Cyclamen persicum has anti-inflammatory effects, reduces cholesterol levels, treats diabetes, and inhibits tumor growth. In this respect, in-vitro examination of antibacterial and anticancer activities and antioxidative potency of C. persicum ethanolic extract were evaluated. The antioxidative potency of the extracted plant material was determined spectrophotometrically using the DPPH free radical scavenging method and the HPLC-PDA method to evaluate its total phenolic content (TPC) and total flavonoid content (TFC). The experimental results revealed weak antibacterial activity of C. persicum extract against both gram negative (E. coli) and gram positive (Streptococcus aureus and S. aureus) bacterial strains, with the zones of inhibition found to be less than 8 mm. On the other hand, powerful activity against MCF7 breast cancer as well as HT29 colon cancer cell lines was obtained. The findings also revealed potent inhibition of free radicals and the presence of maximal levels of natural products such as phenolic compounds and flavonoids, which supportits biological activities and powerful ability to scavenge free radicals. HPLC results showed the presence of numerous flavonoid and phenolic compounds such as rutin, chlorogenic acid, kaempferol, trans-cinnamic acid, quercetin, sinapic acid, and p-coumaric acid.

Asunto(s)

Neoplasias de la Mama , Cyclamen , Humanos , Femenino , Antioxidantes/farmacología , Antioxidantes/química , Cyclamen/química , Staphylococcus aureus , Escherichia coli , Extractos Vegetales/farmacología , Extractos Vegetales/química , Flavonoides/farmacología , Fenoles/farmacología , Antibacterianos/farmacología , Radicales Libres

RESUMEN

This study focused on studying the bioaccesible phenolic compounds (PCs) from yellow pea flour (F) and protein isolate (I). Total phenolic contents (TPC), PCs composition and antioxidant activities were analysed in ethanol 60% extracts obtained by applying ultrasound assisted extraction (UAE, 15 min/40% amplitude). The preparation of I under alkaline conditions and the elimination of some soluble components at lower pH produced a change of PCs profile and antioxidant activity. After simulated gastrointestinal digestion (SGID) of both ingredients to obtain the digests FD and ID, notable changes in the PCs concentration and profiles could be demonstrated. FD presented a higher ORAC activity than ID (IC50 = 0.022 and 0.039 mg GAE/g dm, respectively), but lower ABTS•+ activity (IC50 = 0.8 and 0.3 mg GAE/g dm, respectively). After treatment with cholestyramine of extracts from FD and ID in order to eliminate bile salts and obtain the bioaccesible fractions FDb and IDb, ROS scavenging in H2O2-induced Caco2-TC7 cells was evaluated, registering a greater activity for ID respect to FD (IC50 = 0.042 and 0.017 mg GAE/mL, respectively). These activities could be attributed to the major bioaccesible PCs: OH-tyrosol, polydatin, trans-resveratrol, rutin, (-)-epicatechin and (-)-gallocatechin gallate for FD; syringic (the most concentrated) and ellagic acids, trans-resveratrol, and (-)-gallocatechin gallate for ID, but probably other compounds such as peptides or amino acids can also contribute.

Asunto(s)

Antioxidantes , Harina , Fenoles , Pisum sativum , Antioxidantes/farmacología , Antioxidantes/análisis , Pisum sativum/química , Fenoles/análisis , Fenoles/farmacología , Harina/análisis , Humanos , Células CACO-2 , Extractos Vegetales/farmacología , Extractos Vegetales/química , Proteínas de Plantas/aislamiento & purificación , Proteínas de Plantas/farmacología , Proteínas de Plantas/análisis , Proteínas de Guisantes/química , Digestión

RESUMEN

Discovered over a decade ago, sulfur quantum dots (SQDs) have rapidly emerged as a sustainable, safe, and inexpensive quantum material. Sustainably synthesizing SQDs using sublimed sulfur powders, typically produced as waste in industrial petrochemical refining processes, has attracted researchers to use these functional quantum materials in various research fields. SQDs quickly found applications in various research fields, such as electronics, environmental sensing, food packaging, and biomedical engineering. Although low production yields, time-consuming and energy-intensive synthetic methods, and low photoluminescence quantum yield (PLQY) have been some problems, researchers have found ways to improve synthetic methods, develop passivating agents, and systematically modify reaction schemes and energy sources to achieve large-scale synthesis of stable SQDs with high PLQY. Nonetheless, SQDs have succeeded tremendously in biomedical and related applications due to their low toxicity, antibacterial and antioxidant properties, biocompatibility, appropriate cellular uptake, and photoluminescent properties. Although the bioimaging applications of SQDs have been extensively studied, their other reported properties indicate their suitability for use as antimicrobial agents, free radical scavengers, and drug carriers in other biomedical applications, such as tissue regeneration, wound healing, and targeted drug delivery.

Asunto(s)

Puntos Cuánticos , Puntos Cuánticos/química , Sistemas de Liberación de Medicamentos/métodos , Portadores de Fármacos , Azufre

RESUMEN

Photothermal therapy (PTT) has gained widespread attention due to its significant advantages, such as noninvasiveness and ability to perform laser localization. However, PTT usually reaches temperatures exceeding 50 °C, which causes tumor coagulation necrosis and unfavorable inflammatory reactions, ultimately decreasing its efficacy. In this study, multifunctional two-dimensional Bi2Se3 nanodisks were synthesized as noninflammatory photothermal agents for glioma therapy. The Bi2Se3 nanodisks showed high photothermal stability and biocompatibility and no apparent toxicology. In addition, in vitro and in vivo studies revealed that the Bi2Se3 nanodisks effectively ablated gliomas at relatively low concentrations and inhibited tumor proliferation and migration. Moreover, the multienzymatic activity of the Bi2Se3 nanodisks inhibited the PTT-induced inflammatory response through their high ability to scavenge reactive oxygen species. Finally, the Bi2Se3 nanodisks demonstrated computed tomography capabilities for integrating diagnosis and treatment. These findings suggest that multifunctional Bi2Se3 nanodisk nanozymes can enable more effective cancer therapy and noninflammatory PTT.

Asunto(s)

Glioma , Hipertermia Inducida , Nanopartículas , Neoplasias , Fotoquimioterapia , Humanos , Fototerapia/métodos , Neoplasias/tratamiento farmacológico , Glioma/tratamiento farmacológico , Hipertermia Inducida/métodos , Línea Celular Tumoral

RESUMEN

Natural evolution has nurtured a series of active molecules that play vital roles in physiological systems, but their further applications have been severely limited by rapid deactivation, short cycle time, and potential toxicity after isolation. For instance, the instability of structures and properties has greatly descended when sanshool is derived from Zanthoxylum xanthoxylum. Herein, natural polyphenols are employed to boost the key properties of sanshool by fabricating a series of nanoparticles (NPs). The intracellular evaluation and in vivo animal model are conducted to demonstrate the decreased photodamage score and skin-fold thickness of prepared NPs, which can be attributed to the better biocompatibility, improved free radical scavenging, down-regulated apoptosis ratios, and reduced DNA double-strand breaks compared to naked sanshool. This work proposes a novel strategy to boost the key properties of naturally occurring active molecules with the assistance of natural polyphenol-based platforms.

Asunto(s)

Polifenoles , Piel , Polifenoles/farmacología , Animales , Ratones , Piel/efectos de los fármacos , Piel/metabolismo , Nanopartículas/química , Zanthoxylum/química , Apoptosis/efectos de los fármacos , Extractos Vegetales/farmacología , Modelos Animales de Enfermedad , Humanos

RESUMEN

Objective: To identify phytochemical constituents present in the extract of flowers of Xanthoceras sorbifolia and evaluate their anti-oxidant and anti-hyperglycemic capacities. Methods: The AlCl3 colorimetric method and Prussian Blue assay were used to determine the contents of total flavonoids and total phenolic acids in extraction layers, and the bioactive layers was screened through anti - oxidative activity in vitro. The Waters ACQUITY UPLC system and a Waters ACQUITY UPLC BEH C18 column (2.0 mm × 150 mm, 5 µm) were used to identify the ingredients. And anti-oxidative ingredients were screened by off-line UPLC-QTOF-MS/MS-free radical scavenging. The ameliorative role of it was further evaluated in a high-fat, streptozotocin-induced type 2 diabetic rat model and the study was carried out on NADPH oxidase (PDB ID: 2CDU) by molecular docking. Results: Combined with the results of activity screening in vitro, the anti - oxidative part was identified as the ethyl acetate layer. A total of 24 chemical constituents were identified by liquid chromatography-mass spectrometry in the ethyl acetate layer and 13 main anti-oxidative active constituents were preliminarily screened out through off-line UPLC-QTOF-MS/MS-free radical scavenging. In vivo experiments showed that flowers of X. sorbifolia could significantly reduce the blood glucose level of diabetic mice and alleviate liver cell damage. Based on the results of docking analysis related to the identified phytocompounds and oxidase which involved in type 2 diabetes, quercetin 3-O-rutinoside, kaempferol-3-O-rhamnoside, isorhamnetin-3-O-glucoside, and isoquercitrin showed a better inhibitory profile. Conclusion: The ethyl acetate layer was rich in flavonoids and phenolic acids and had significant anti-oxidant activity, which could prevent hyperglycemia. This observed activity profile suggested X. sorbifolia flowers as a promising new source of tea to develop alternative natural anti-diabetic products with a high safety margin.