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BACKGROUND: Previous research has supported the presence of an association between high glycated hemoglobin (HbA1c) levels and cardiovascular disease (CVD). The objective of the present study was to determine whether increased HbA1c levels are associated with high CVD prevalence among nondiabetics. Furthermore, we aimed to explore the possible interaction of HbA1c levels and age in regard to CVD. METHODS: This cross-sectional study analyzed data of 28,534 adult participants in the National Health and Nutrition Examination Survey 2005-2018. The association between HbA1c and CVD was assessed using univariate and multivariate logistic regression models. Propensity score matching was used to reduce selection bias. Subgroup analysis and restricted cubic spline (RCS) were used to further characterize the association between HbA1c levels and CVD. We modeled additive interactions to further assess the relationship between HbA1c levels and age. RESULTS: In the multivariate logistic regression model, a positive association was found between CVD and increased HbA1c levels (highest quartile [Q4] vs. lowest quartile [Q1]: odds ratio [OR] = 1.277, 95% confidence interval [CI] = 1.111-1.469, P = 0.001). In the stratified analyses, the adjusted association between HbA1c and CVD was significant for those younger than 55 years (Q4 vs. Q1: OR = 1.437, 95% CI = 1.099-1.880, P = 0.008). RCS did not reveal a nonlinear relationship between HbA1c levels and CVD among nondiabetics (P for nonlinearity = 0.609). Additionally, a high HbA1c level was favorably connected with old age on CVD, with a synergistic impact. CONCLUSIONS: Increased HbA1c levels were associated with high CVD prevalence among nondiabetics. However, we still need to carefully explain the effect of age on the relationship between HbA1c and CVD in nondiabetic population. Given the correlations of HbA1c with CVDs and CV events, HbA1c might be a useful indicator for predicting CVDs and CV events in the nondiabetic population.
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Biomarcadores , Enfermedades Cardiovasculares , Hemoglobina Glucada , Encuestas Nutricionales , Humanos , Hemoglobina Glucada/metabolismo , Hemoglobina Glucada/análisis , Enfermedades Cardiovasculares/epidemiología , Enfermedades Cardiovasculares/sangre , Enfermedades Cardiovasculares/diagnóstico , Estudios Transversales , Masculino , Persona de Mediana Edad , Femenino , Prevalencia , Estados Unidos/epidemiología , Adulto , Factores de Edad , Medición de Riesgo , Anciano , Biomarcadores/sangre , Regulación hacia Arriba , Factores de Riesgo , Factores de Tiempo , Adulto JovenRESUMEN
Methicillin-resistant Staphylococcus aureus (MRSA) is a widespread pathogen causing clinical infections and is multi-resistant to many antibiotics, making it urgent need to develop novel antibacterials to combat MRSA. Herein, we designed and prepared a series of novel osthole amphiphiles 6a-6ad by mimicking the structures and function of antimicrobial peptides (AMPs). Antibacterial assays showed that osthole amphiphile 6aa strongly inhibited S. aureus and 10 clinical MRSA isolates with MIC values of 1-2 µg/mL, comparable to that of the commercial antibiotic vancomycin. Additionally, 6aa had the advantages of rapid bacteria killing without readily developing drug resistance, low toxicity, good membrane selectivity, and good plasma stability. Mechanistic studies indicated that 6aa possesses good membrane-targeting ability to bind to phosphatidylglycerol (PG) on the bacterial cell membranes, thereby disrupting the cell membranes and causing an increase in intracellular ROS as well as leakage of proteins and DNA, and accelerating bacterial death. Notably, in vivo activity results revealed that 6aa exhibits strong anti-MRSA efficacy than vancomycin as well as a substantial reduction in MRSA-induced proinflammatory cytokines, including TNF-α and IL-6. Given the impressive in vitro and in vivo anti-MRSA efficacy of 6aa, which makes it a potential candidate against MRSA infections.
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Antibacterianos , Cumarinas , Staphylococcus aureus Resistente a Meticilina , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Cumarinas/química , Cumarinas/farmacología , Cumarinas/síntesis química , Animales , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Estructura Molecular , Relación Estructura-Actividad , Humanos , Relación Dosis-Respuesta a Droga , Ratones , Tensoactivos/farmacología , Tensoactivos/química , Tensoactivos/síntesis químicaRESUMEN
Polyethylene (PE) is a common component of microplastic pollution, and cadmium (Cd) is a prevalent pollutant in contaminated freshwater bodies in China. Among cyanobacteria, Microcystis aeruginosa (M. aeruginosa) plays a crucial role in the formation of algal blooms in these water systems. However, there has been limited research on how microplastics and heavy metals affect cyanobacteria ecologically. This study aimed to evaluate the physiological effects of individual and combined exposure to Cd pollutants and microplastics on M. aeruginosa. The solutions containing 13 µm and 6.5 µm PE particles (100 mg/L) with Cd were used in the research. The results indicated that the combined treatment led to a significant inhibition of chlorophyll a content, dropping to zero by day 5. The treated groups exhibited higher microcystins (MCs) content compared to the control group, suggesting increased MCs release due to pollutant exposure. Interestingly, the adsorption of heavy metals by microplastics partially alleviated the toxicity of heavy metals on algal cells. Moreover, the combined treatment significantly suppressed catalase (CAT) activity compared to Cd treatment, indicating a synergistic effect that led to greater oxidative stress. Overall, this study provides valuable insights into the impact of PE and Cd pollution on freshwater ecosystems, elucidates the physiological responses of cyanobacteria to these pollutants, and establishes a theoretical groundwork for addressing complex water pollution using cyanobacteria-based strategies.
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BACKGROUND: Obesity is a crucial risk factor for asthma. Observational studies have examined the association between abdominal obesity and asthma symptoms. This study aimed to investigate the causal relationship between visceral adipose tissue (VAT) and asthma and its potential as an independent indicator. METHODS: This study utilized data from the National Health and Nutrition Examination Survey spanning 2011-8. Multivariable logistic regression and stratified variable selection were employed to identify associations between asthma and VAT. Moreover, a two-sample Mendelian randomization analysis, using 221 genetic variants as instrumental variables, was conducted to assess this relationship further. RESULTS: Our findings indicated that individuals with higher VAT levels were more likely to develop asthma. Visceral obesity remained a significant risk factor for asthma after adjusting for demographic characteristics. Genetic predictions suggest a positive association between VAT and an elevated risk of asthma (odds ratio [OR] = 1.393, 95% confidence interval [CI]: 1.266-1.534, and P = 1.43E-11). No significant polymorphisms were detected using the Mendelian randomization-Egger intercept test. CONCLUSIONS: This study presents potential evidence supporting the causal role of VAT in asthma development. Furthermore, the findings from the Mendelian randomization analysis further reinforce the relationship between VAT and asthma risk.
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Asma , Grasa Intraabdominal , Análisis de la Aleatorización Mendeliana , Encuestas Nutricionales , Humanos , Asma/genética , Asma/epidemiología , Masculino , Femenino , Factores de Riesgo , Adulto , Persona de Mediana Edad , Obesidad Abdominal/genética , Obesidad Abdominal/complicaciones , Estados Unidos/epidemiologíaRESUMEN
Protocadherin 8 (PCDH8), a calcium-dependent transmembrane protein in the protocadherin family, regulates cell adhesion and signal transduction. While some studies have provided indirect evidence that PCDH8 has cancer-promoting properties, this association is controversial. In particular, its involvement in thyroid cancer (THCA) remains unclear. We aimed to elucidate the role of PCDH8 in THCA using bioinformatic analysis. Subsequently, the results were experimentally validated. The analysis conducted using the R programming language and online web tools explored PCDH8 expression levels, prognostic, and clinical implications, and its relationship with the tumor immune microenvironment in THCA. Furthermore, we examined the association between PCDH8 and co-expressed genes, highlighting their involvement in several biological processes relevant to THCA. The potential of PCDH8 as a therapeutic target for this pathology was also explored. Immunohistochemical (IHC) staining was performed on samples from 98 patients with THCA, and experimental validation was carried out. PCDH8 was significantly elevated in cancer tissues and associated with poor prognosis, several clinical factors, and immune cell and checkpoint abundance. Cox regression and survival analyses, together with Receiver Operating Curves (ROC) indicated that PCDH8 was an independent prognostic factor for THCA. Furthermore, PCDH8 impacts cell viability and proliferation, promoting tumorigenesis. Also, it influences tumor cell sensitivity to various drugs. Thus, PCDH8 might be a potential therapeutic target for THCA. IHC, cell culture, MTT, and colony formation experiments further confirmed our findings. This analysis provided insights into the potential carcinogenic role of PCDH8 in THCA, as it impacts cell viability and proliferation. Thus, PCDH8 might play an important role in its prognosis, immune infiltration, and diagnosis.
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Protocadherinas , Neoplasias de la Tiroides , Humanos , Pronóstico , Neoplasias de la Tiroides/genética , Proliferación Celular , Carcinogénesis , Biomarcadores , Microambiente TumoralRESUMEN
BACKGROUND: Kidney stones and thyroid disease are two common diseases in the general population, with multiple common risk factors. The associations between kidney stones and thyroid disease are unclear. AIM: This study aims to assess the association between 'once had a thyroid disease' and the odds of kidney stones. METHODS: Adult participants from the National Health and Nutrition Examination Survey (NHANES) 2007-2018 with reliable kidney stone and thyroid disease data were included. Adjusting for age, gender, race, education level, and marital status, diabetes, hypertension, gout, angina pectoris, stroke, and asthma, logistic regression was used to examine the relationship between kidney stones and thyroid illness. RESULTS: Using stratified analysis, the association between thyroid illness and kidney stones was investigated further. Among the participants, 4.9% had kidney stones, and 10.1% had thyroid disease. Kidney stone was associated with thyroid disease (OR=1.441, (95% CI:1.294-1.604), p <0.01), which remained significant (OR=1.166, (95% CI:1.041-1.305), p <0.01) after adjustments with age, gender, race, education level and marital status, diabetes, hypertension, gout, angina pectoris, stroke, and asthma. Stratified by blood lead, blood cadmium, and blood urea nitrogen levels in the human body, the odds of kidney stones still increased with once having a previous thyroid disease. CONCLUSIONS: In this large nationally representative survey over 10 years, kidney stone was strongly associated with thyroid disease. In this cross-sectional study, we explored the association between thyroid disease and kidney stones, which may help clinicians intervene in them early.
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Cálculos Renales , Encuestas Nutricionales , Enfermedades de la Tiroides , Humanos , Masculino , Femenino , Adulto , Persona de Mediana Edad , Estados Unidos/epidemiología , Cálculos Renales/epidemiología , Cálculos Renales/sangre , Cálculos Renales/diagnóstico , Cálculos Renales/etiología , Enfermedades de la Tiroides/epidemiología , Enfermedades de la Tiroides/diagnóstico , Factores de Riesgo , Estudios Transversales , Anciano , Adulto JovenRESUMEN
The emergence of multi-drug-resistant bacteria is threatening to human health and life around the world. In particular, methicillin-resistant Staphylococcus aureus (MRSA) causes fatal injuries to human beings and serious economic losses to animal husbandry due to its easy transmission and difficult treatment. Currently, the development of novel, highly effective, and low-toxicity antimicrobials is important to combat MRSA infections. Thiazole-containing compounds with good biological activity are widely used in clinical practice, and appropriate structural modifications make it possible to develop new antimicrobials. Here, we review thiazole-containing compounds and their antibacterial effects against MRSA reported in the past two decades and discuss their structure-activity relationships as well as the corresponding antimicrobial mechanisms. Some thiazole-containing compounds exhibit potent antibacterial efficacy in vitro and in vivo after appropriate structural modifications and could be used as antibacterial candidates. This Review provides insights into the development of thiazole-containing compounds as antimicrobials to combat MRSA infections.
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Antiinfecciosos , Staphylococcus aureus Resistente a Meticilina , Animales , Humanos , Tiazoles/farmacología , Tiazoles/química , Pruebas de Sensibilidad Microbiana , Antibacterianos/farmacología , Antibacterianos/química , Antiinfecciosos/farmacologíaRESUMEN
Infections caused by multidrug-resistant (MDR) bacteria are increasing worldwide, and with limited clinically available antibiotics, it is urgent to develop new antimicrobials to combat these MDR bacteria. Here, a class of novel amphiphilic xanthohumol derivatives were prepared using a building-block approach. Bioactivity assays showed that the molecule IV15 not only exhibited a remarkable antibacterial effect against clinical methicillin-resistant Staphylococcus aureus (MRSA) isolates (MICs: 1-2 µg/mL) but also had the advantages of rapid bactericidal properties, low toxicity, good plasma stability, and not readily inducing bacterial resistance. Mechanistic studies indicated that IV15 has good membrane-targeting ability and can bind to phosphatidylglycerol and cardiolipin in bacterial membranes, thus disrupting the bacterial cell membranes and causing increased intracellular reactive oxygen species and leakage of proteins and DNA, eventually resulting in bacterial death. Notably, IV15 exhibited remarkable in vivo anti-MRSA efficacy, superior to vancomycin, making it a potential candidate to combat MRSA infections.
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Staphylococcus aureus Resistente a Meticilina , Antibacterianos/farmacología , Vancomicina/farmacología , Flavonoides/farmacología , Pruebas de Sensibilidad MicrobianaRESUMEN
BACKGROUND: Soluble dietary fiber (SDF) obtained from Lentinula edodes byproducts has beneficial effects on human intestinal health. This study aimed to examine the combined preventive and ameliorative effects of a kind of synbiotic (SDF with a molecular weight of 1.58 × 102 kDa and Lactobacillus plantarum LP90 (LP) at 1 × 109 CFU kg-1 ) on dextran sulfate sodium-induced colitis mice. RESULTS: The results demonstrated that synbiotic treatment could alleviate weight loss, decrease the disease activity index level and cause histological amelioration. Synbiotic treatment also promoted the production of goblet cells, increased the expression of tight junction proteins, and adjusted the production of myeloperoxidase, malondialdehyde and superoxide dismutase to repair intestinal epithelial injury. Clinical symptoms were alleviated by maintaining Th17/Treg balance, increasing interleukin 10 and immunoglobulin A levels, reducing interleukin 17a and tumor necrosis factor α production, and promoting mRNA to highly express of Foxp3 and vitamin D receptors. Moreover, synbiotic treatment could upregulate butyric acid production (4.71 ± 0.46 mol g-1 feces, P < 0.05) and diversity of intestinal microbial to maintain intestinal homeostasis. CONCLUSION: This study suggested that the combination of LP and SDF as a synbiotic has the potential for use as a nutritional supplement to alleviate colitis. © 2022 Society of Chemical Industry.
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Colitis , Lactobacillus plantarum , Hongos Shiitake , Simbióticos , Humanos , Ratones , Animales , Sulfato de Dextran/efectos adversos , Modelos Animales de Enfermedad , Colitis/inducido químicamente , Colitis/prevención & control , Colitis/tratamiento farmacológico , Fibras de la Dieta/metabolismo , Colon/metabolismo , Ratones Endogámicos C57BL , Mucosa IntestinalRESUMEN
Improving energy homeostasis and the gut microbiota is a promising strategy to improve obesity and related metabolic disorders. Mulberry leaf is one of the traditional Chinese medicines and functional diets. In this work, a mouse model induced by high-fat diet (HFD) was used to reveal the role of mulberry leaf polysaccharides (MLP). It was found that MLP had a significant effect in limiting body weight gain (reduced by 19.95%, 35.47% and 52.46%, respectively), ameliorating hepatic steatosis and regulating lipid metabolism in HFD induced obese mice (P < 0.05). RT-PCR and western blot analysis suggested that these metabolic improvements were mediated by inducing the development of brown-like adipocytes in inguinal white adipose tissue and enhancing brown adipose tissue activity. Besides, 16S rRNA sequencing results led to the inference that MLP could mitigate the composition and function of the gut microbiota. Together, these findings indicated that MLP possess great potential as a diet supplement or medication for obesity.
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Tejido Adiposo Pardo/efectos de los fármacos , Microbioma Gastrointestinal/efectos de los fármacos , Morus/química , Hojas de la Planta/química , Polisacáridos , Animales , Dieta Alta en Grasa/efectos adversos , Masculino , Ratones , Ratones Endogámicos C57BL , Polisacáridos/análisis , Polisacáridos/química , Polisacáridos/farmacologíaRESUMEN
Pancreatic lipase (PL) is a key enzyme related to the prevention and treatment of obesity. The aim of the study was to evaluate the inhibitory effects of mulberry leaf polysaccharides (MLP) on PL and possible interaction mechanism, inhibition on lipid accumulation in vitro and in vivo. The results revealed that MLP had obvious inhibitory effects on PL (P < 0.05). The interaction of MLP-PL complexes was in a spontaneous way driven by enthalpy, and hydrogen bonds were the main factors in the binding. MLP could significantly inhibit the development of lipid accumulation in HepG2 cells (P < 0.05). Furthermore, consumption of high-fat diet containing MLP showed protective effects on liver and adipose tissue damages in mice, and inhibited the lipid absorption in digestive tract. MLP also significantly reduced the increased expression level of pancreatic digestive enzymes (P < 0.05). The study indicated that the anti-obesity effect of MLP might be caused by inhibition of lipid absorption via reducing PL activity.
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Inhibidores Enzimáticos/farmacología , Morus/química , Pancrelipasa/antagonistas & inhibidores , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Tejido Adiposo , Animales , Dieta Alta en Grasa , Activación Enzimática/efectos de los fármacos , Inhibidores Enzimáticos/química , Humanos , Metabolismo de los Lípidos , Hígado/efectos de los fármacos , Hígado/metabolismo , Ratones , Peso Molecular , Obesidad , Pancrelipasa/química , Extractos Vegetales/química , Hojas de la Planta/química , Polisacáridos/química , Análisis EspectralRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Chrysophyllum cainito L. (C. cainito) is a traditional folk medicine in tropical area which can be an alternative agent for diabetes mellitus. Although the antioxidant and antidiabetic activity of the extracts are reported, little is known on the antiglycation activity and effects on diabetic complications. AIM OF THE STUDY: This work was aimed to investigate the chemical profile, antidiabetic, antioxidant activities of C. cainito. Especially, the antiglycation potential as well as the relationships between components and activities were evaluated. MATERIALS AND METHODS: The content of the primary components (polyphenols, flavonoids, steroids, and triterpenes), antioxidant, and hypoglycemic effects of ethanolic extracts from C. cainito leaves (CCE-1, 2, 3, 4) and stems (CSE-1, 2, 3, 4) were analyzed and detected. The chemical profiles of CCE-2 were characterized by HPLC-Q-TOF-MS/MS. The antiglycation and protection against oxidative stress effects were determined by in vitro assays. Relationship between bioactivities and components was analyzed by principal component analysis (PCA), heatmap analysis, and Pearson correlation analysis. RESULTS: The composition was diverse between leaves and stem extracts with different activities. CCE-2 possessed the highest DPPH scavenging activity. CSE-2 displayed the highest ABTS scavenging activity and ferric reducing power. While CCE-3 showed the most effective inhibition on α-amylase and α-glucosidase activity (IC50 4.103 ± 0.332 µg/mL and 0.180 ± 0.006 mg/mL, respectively). PCA analysis showed that the most important variables in PC1 (60.7%) were total polyphenol and antioxidant activities. The hypoglycemic activity and contents of steroids showed important correlation. Advanced glycation end products formation was effectively inhibited by CCE-2 with myricetin 3-O-rhamnoside as the main constituent. CCE-3 displayed the highest protection effect against L02 cell line oxidation damage. CONCLUSIONS: C. cainito leaves might be a promising candidate for antioxidant, hypoglycemic and antiglycation dietary supplement or potential agent against diabetes associated chronic diseases.
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Antioxidantes/farmacología , Hipoglucemiantes/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Sapotaceae/química , Antioxidantes/química , Benzotiazoles , Compuestos de Bifenilo , Línea Celular , Glucosa/metabolismo , Humanos , Hipoglucemiantes/química , Estrés Oxidativo , Fitoquímicos , Fitoterapia , Picratos , Componentes Aéreos de las Plantas/química , Ácidos SulfónicosRESUMEN
Inonotus obliquus (Chaga mushroom) is a kind of medicine and health food widely used by folk in China, Russia, Korea, and some occidental countries. Among the extracts from Inonotus obliquus, Inonotus obliquus polysaccharide (IOPS) is supposed to be one of the major bioactive components in Inonotus obliquus, which possesses antitumor, antioxidant, anti-virus, hypoglycemic, and hypolipidemic activities. In this review, the current advancements on extraction, purification, structural characteristics, and biological activities of IOPS were summarized. This review can provide significant insight into the IOPS bioactivities as their in vitro and in vivo data were summarized, and some possible mechanisms were listed. Furthermore, applications of IOPS were reviewed and discussed; IOPS might be a potential candidate for the treatment of cancers and type 2 diabetes. Besides, new perspectives for the future work of IOPS were also proposed.
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Hydrodynamic drag not only results in high-energy consumption for water vehicles but also impedes the increase of vehicle speed. The introduction of a low-viscosity gas lubricating film is assumed to be an effective and promising method to reduce hydrodynamic drag. However, the poor stability of the gas film and massive extra energy consumption restricts the practical application of the gas lubricating method. Herein, inspired by the microhairs with low surface energy wax covering the abdomen of water spiders, superhydrophobic sphere surfaces were designed. Attributed to numerous neighboring nanoneedle branches with low surface energy chemicals, an air-entrained cavity with a large surface area was captured and stabilized by the superhydrophobic sphere, changing its shape from a sphere to a streamlined body. The cavity continued attaching to the superhydrophobic sphere without bursting at a depth of 70.0-90.0 cm underwater and reduced the hydrodynamic drag by more than 90%. This work provides a simple, cost-effective, and energy-efficient way to stabilize the underwater gas-liquid interface to achieve a reduction in the hydrodynamic drag.
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Aimed to explore different corn silk polysaccharide (CSP) fractions derived by ethanol precipitation on the physicochemical properties and biological activities, four fractions (CSP20, CSP40, CSP60, and CSP80) were obtained. CSPs consisted of mannose, galactose, arabinose, rhamnose, xylose, and glucose with different ratios, and exhibited different total sugar content, uronic acid content, protein content, and total phenols content. All fractions also showed different physical properties, such as molecular weight, intrinsic viscosity, particle size, and microstructure. Besides, CSP80 exhibited stronger antioxidant activity and α-glucosidase inhibitory activity than the other three fractions. Enzyme kinetic analysis suggested that CSP80 inhibited α-glucosidase by mixed type and reversible mechanisms, respectively. Fluorescence intensity measurements confirmed that the secondary structure of α-glucosidase was changed by the binding of CSP80. Isothermal titration calorimetry (ITC) results illustrated that the binding of CSP80 to α-glucosidase complex was spontaneous driven by enthalpy and hydrogen bonds played a major role in the binding.
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The polysaccharides (CSPw, CSPc, CSPa, and CSPu) were prepared by hot water extraction, acid-assisted extraction, alkaline-assisted extraction, and ultrasound-assisted extraction from corn silk, respectively. High performance gel permeation chromatography (HPGPC), fourier-transform infrared (FT-IR) spectroscopy, and scanning electron microscopy (SEM) results indicated that the extraction methods had an obvious impact on the molecular weight, structure, and morphology of the CSPs. Among the four polysaccharides, CSPu showed the highest inhibitory α-glucosidase activity, which might be related to its smaller molecular weight. Furthermore, kinetics analyses revealed that CSPu had significant inhibition of α-glucosidase in a non-reversible and competitive manner. Fluorescence quenching analysis illustrated that the interaction mechanism of CSPu and α-glucosidase was claimed as a static quenching mechanism. Isothermal titration calorimetry (ITC) analysis showed that the main driving forces for the interaction of CSPu with α-glucosidase was hydrogen bonding and the binding interactions of them occurred spontaneously.
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Antioxidantes/química , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Polisacáridos/química , Seda/química , Zea mays/química , alfa-Glucosidasas/metabolismo , Antioxidantes/farmacología , Enlace de Hidrógeno/efectos de los fármacos , Cinética , Peso Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Espectroscopía Infrarroja por Transformada de Fourier/métodosRESUMEN
Inonotus obliquus is a traditional mushroom well known for its therapeutic value. In this study, various solvent fractions of I. obliquus were preliminarily screened for their antioxidant, α-amylase and α-glucosidase inhibition properties. To improve the drug delivery, the active fraction (ethyl acetate fraction) of I. obliquus was synthesized into fungisome (ethyl acetate phophotidyl choline complex, EAPC) and its physical parameters were assessed using Fourier transform infrared spectroscopy (FTIR), High performance liquid chromatography (HPLC), Scanning electron microscope (SEM), and ς potential analysis. Then normal human hepatic L02 cells was used to evaluate the cytotoxicity of EAPC. The results showed that EA fraction possesses significant free radical scavenging, α-amylase and α-glucosidase inhibition properties. FTIR, SEM, and HPLC analysis confirmed the fungisome formation. The particle size of EAPC was 102.80 ± 0.42 nm and the ς potential was -54.30 ± 0.61 mV. The percentage of drug entrapment efficiency was 97.13% and the drug release rates of EAPC in simulated gastric fluid and simulated intestinal fluid were 75.04 ± 0.29% and 93.03 ± 0.36%, respectively. EAPC was nontoxic to L02 cells, however it could selectively fight against the H2 O2 induced oxidative damage in L02 cells. This is the first study to provide scientific information to utilize the active fraction of I. obliquus as fungisome. PRACTICAL APPLICATIONS: Inonotus obliquus (IO) is a traditional medicinal fungus. The extracts of IO have obvious antioxidant and hypoglycemic activities. Ethyl acetate (EA) fraction of IO was encapsulated in liposomes to form EAPC. EAPC has a sustained-release effect. It has nontoxic to L02 cells and could protect L02 cells from oxidative damage caused by hydrogen peroxide. This study could provide new ideas for the treatment of diabetes.
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Agaricales/química , Antioxidantes/farmacología , Basidiomycota/química , Inhibidores Enzimáticos/farmacología , Peróxido de Hidrógeno/toxicidad , Extractos Vegetales/farmacología , alfa-Amilasas/antagonistas & inhibidores , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Línea Celular , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Hepatocitos/efectos de los fármacos , Hepatocitos/metabolismo , Humanos , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , alfa-Amilasas/química , alfa-Glucosidasas/químicaRESUMEN
Aimed to evaluate the changes of three soluble dietary fibers from Lentinula edodes by-products (LESDF) with different molecular weights in the digestive system and their effects on large intestinal fermentation, fermentation products and the types of gut microbiota were determined. The 1D/2D NMR results showed that main form of glucose in LESDF-1 was methyl glycopyranosides and LESDF-3 had distinct branching structures in possible repetitive unit. LESDF-2 showed the beneficial fermentation performance with the slower changes of total carbohydrate consumption and highest production of propionic acid and butyric acid. Results suggested that branched chain structure could increase the consumption rate of LESDF, but not affect the concentration of total SCFAs produced. LESDF-3 was found to promote the production of Bacteroides, which indicated LESDF was one of the nutritional components with the influence on the composition and relative abundance of intestinal microbial community.
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Fibras de la Dieta/análisis , Microbioma Gastrointestinal/efectos de los fármacos , Hongos Shiitake/química , Reactores Biológicos , Conformación de Carbohidratos , Fermentación , HumanosRESUMEN
Soybean Bowman-Birk trypsin inhibitor (BBTI), an antinutritional factor of soy products, could strongly inhibit the protein digestion. The inactivation effect and mechanism of BBTI induced by tea polyphenols (TPs) and its major components (EGCG and EGC), were investigated in this study using fluorescence, FTIR, CD spectroscopy, isothermal titration calorimetry (ITC) and molecular docking. EGCG and EGC interacted with BBTI via static quenching process and hydrophobic interaction, with binding constant (Ka) of 2.19â¯×â¯103â¯M-1 and 0.25â¯×â¯103â¯M-1 at 298â¯K, respectively. TPs, EGCG and EGC induced a transition of BBTI conformation from disorder to order. ITC analysis and molecular docking revealed the interaction of EGCG-BBTI and EGC-BBTI were spontaneous, and hydrophobic interactions and hydrogen bonds were the predominant forces. Overall, this study clearly suggested that EGCG could be a promising inactivating agent for BBTI, which could also improve the safety and nutritional value of soy products.
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Catequina/análogos & derivados , Simulación del Acoplamiento Molecular , Inhibidor de la Tripsina de Soja de Bowman-Birk/química , Catequina/química , Catequina/farmacología , Fluorescencia , Enlace de Hidrógeno , Interacciones Hidrofóbicas e Hidrofílicas , Conformación Proteica , Termodinámica , Inhibidor de la Tripsina de Soja de Bowman-Birk/efectos de los fármacos , Inhibidor de la Tripsina de Soja de Bowman-Birk/metabolismoRESUMEN
Aimed to evaluate the hypolipidemic effects of high molecular weight soluble dietary fiber extracted from L. edodes (LEHSDF), this study investigated the structure and interaction mechanism of LEHSDF with pancreatic lipase (PL) and bile salts (BS) that were involved in lipid digestion. 1D/2D NMR spectra indicated that the main chain of LEHSDF consisted of (1 â 2,4)-linked ß-D-arabinopyranosyl, (1 â 3)-linked α-L-rhamnopyranosyl, (1 â 4)-linked ß-D-xylopyranosyl, (1 â 6)-linked and (1 â 4)-linked ß-D-glucopyranosyl, with ß-D-galactopyranosyl and α-D-mannopyranosyl as terminal unit. Oil red O staining results suggested that LEHSDF had an effective inhibitory effect on lipid accumulation in HepG2 cells. Isothermal titration calorimetry, fluorescence and circular dichroism spectra showed that BS did not specifically bind to LEHSDF, and the strong inhibitory effect of LEHSDF on lipase was dominated by hydrophobic forces, electrostatic forces, encapsulation and adsorption interactions. The results will be helpful for the design of food containing LEHSDF as a functional additive to control lipid digestion.