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Lignin nanoparticles (LNP), extracted from spent materials of Dashamoola Arishta (Ayurvedic formulation), shared a molecular weight of 14.42 kDa with commercial lignin. Processed into LNPs (496.43 ± 0.54 nm) via planetary ball milling, they demonstrated stability at pH 8.0 with a zeta potential of -32 ± 0.27 mV. Operating as Pickering particles, LNP encapsulated curcumin and vitamin D3 in sunflower oil, forming LnE + Cu + vD3 nanoemulsions (particle size: 347.40 ± 0.71 nm, zeta potential: -42.27 ± 0.72 mV) with high encapsulation efficiencies (curcumin: 87.95 ± 0.21%, vitamin D3: 72.66 ± 0.11%). The LnE + Cu + vD3 emulsion exhibited stability without phase separation over 90 days at room (27 ± 2 °C) and refrigeration (4 ± 1 °C) temperatures. Remarkably, LnE + Cu + vD3 exhibited reduced toxicity, causing 29.32% and 34.99% cell death in L6 and RAW264.7 cells respectively, at the highest concentration (50 µg/mL). This underscores the potential valorization of Ayurvedic industry spent materials for diverse industrial applications.
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Porous starch (PS), a modified form of starch with unique properties, is attracting substantial attention for its diverse advantages and applications. Its intricate porous structure, crystalline and amorphous characteristics, and hydrophilic-hydrophobic properties stem from pore formation via physical, chemical, enzymatic, and combined synergistic methods. Porous starch offers benefits like improved gelatinization temperature, water absorption, increased surface area, tunable crystallinity, and enhanced functional properties, making it appealing for diverse food industry applications. To optimize its properties, determining the parameters governing porous structure formation is crucial. Factors such as processing conditions, starch source, and modification methods substantially impact porosity and the overall characteristics of the material. Understanding and controlling these parameters allows customization for specific applications, from pharmaceutical drug delivery systems to enhancing texture and moisture retention in food products. To date, studies shedding light on how porosity formation can be fine-tuned for specific applications are fewer. This review critically assesses the existing reports on porous starch, focusing on how preparation methods affect porosity formation, thereby influencing the product's crystallinity/hydrophilic-hydrophobic nature and overall applicability.
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Cornea-related injuries are the most common cause of blindness worldwide. Transplantation remains the primary approach for addressing corneal blindness, though the demand for donor corneas outmatches the supply by millions. Tissue adhesives employed to seal corneal wounds have shown inefficient healing and incomplete vision restoration. We have developed a biodegradable hydrogel - Kuragel, with the ability to promote corneal regeneration. Functionalized gelatin and hyaluronic acid form photo-crosslinkable hydrogel with transparency and compressive modulus similar to healthy human cornea. Kuragel composition was tuned to achieve sufficient adhesive strength for sutureless integration to host tissue, with minimal swelling post-administration. Studies in the New Zealand rabbit mechanical injury model affecting corneal epithelium and stroma demonstrate that Kuragel efficiently promotes re-epithelialization within 1 month of administration, while stroma and sub-basal nerve plexus regenerate within 3 months. We propose Kuragel as a regenerative treatment for patients suffering from corneal defects including thinning, by restoration of transparency and thickness.
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Small particles of size ranging from 1 to 100 nm are referred to as nanoparticles. Nanoparticles have tremendous applications in various sectors, including the areas of food and pharmaceutics. They are being prepared from multiple natural sources widely. Lignin is one such source that deserves special mention due to its ecological compatibility, accessibility, abundance, and low cost. This amorphous heterogeneous phenolic polymer is the second most abundant molecule in nature after cellulose. Apart from being used as a biofuel source, lignin is less explored for its potential at a nano-level. In plants, lignin exhibits cross-linking structures with cellulose and hemicellulose. Numerous advancements have taken place in synthesizing nanolignins for manufacturing lignin-based materials to benefit from the untapped potential of lignin in high-value-added applications. Lignin and lignin-based nanoparticles have numerous applications, but in this review, we are mainly focusing on the applications in the food and pharmaceutical sectors. The exercise we undertake has great relevance as it helps scientists and industries gain valuable insights into lignin's capabilities and exploit its physical and chemical properties to facilitate the development of future lignin-based materials. We have summarized the available lignin resources and their potential in the food and pharmaceutical industries at various levels. This review attempts to understand various methods adopted for the preparation of nanolignin. Furthermore, the unique properties of nano-lignin-based materials and their applications in fields including the packaging industry, emulsions, nutrient delivery, drug delivery hydrogels, tissue engineering, and biomedical applications were well-discussed.
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Nanopartículas , Nanoestructuras , Lignina/química , Celulosa , Nanopartículas/química , Hidrogeles/químicaRESUMEN
BACKGROUND: Rheumatoid arthritis (RA) is a chronic inflammatory disorder causing cartilage and joint degeneration. In spite of the availability of several robust drugs like biologics, most of the patients are unresponsive, and reports of severe adverse effects following long-term use are also there. Subsequently the use of natural plant-based products in RA therapy is broadening over the years. Tinospora cordifolia is a widely used medicinal plant in Ayurveda against various inflammatory disorders including RA. However, there is very limited knowledge regarding the actual molecular events responsible for its therapeutic effect, and this has limited its acceptance among the professionals. PURPOSE: To explore the anti-inflammatory and anti-arthritic effect of hydro-alcoholic extract from Tinospora cordifolia. METHODS: The rich polyphenol nature of the extract was elucidated using HPLC. LPS-stimulated murine macrophage cell line RAW 264.7 was used for in vitro studies, and collagen-induced arthritis (CIA) model was used for in vivo studies. RESULTS: The polyphenols in TCE were identified using HPLC. TCE effectively downregulated the level of pro-inflammatory mediators (IL-6, TNF-α, PGE2, and NO) in LPS-stimulated RAW 264.7 cells. Subsequently the upregulated expression of COX-2 and iNOS following LPS stimulation were also downregulated by TCE. Furthermore, TCE targeted the upstream kinases of the JAK/STAT pathway, a crucial inflammatory pathway. The expression of VEGF, a key angiogenic factor as well as an inflammatory mediator was also decreased following pre-treatment with TCE. The anti-arthritic effect of TCE (150 mg/kg) was evaluated in the CIA model as well. From the results of histopathology, oral administration of TCE was found to be effective in reducing the clinical symptoms of arthritis including paw edema, erythema, and hyperplasia. In vivo results validated the in vitro results and there was a significant reduction in serum level of pro-inflammatory cytokines and mediators (IL-6, TNF-α, IL-17, NO, and PGE2). The phosphorylation of STAT3 and the expression of VEGF were also downregulated following TCE treatment. CONCLUSION: Our study provided a detailed insight into the molecular events associated with anti-inflammatory and anti-arthritic effect of Tinospora cordifolia.
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Artritis Experimental , Artritis Reumatoide , Tinospora , Humanos , Ratones , Animales , Quinasas Janus/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Lipopolisacáridos/farmacología , Interleucina-6/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Factores de Transcripción STAT/metabolismo , Transducción de Señal , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Citocinas/metabolismo , Artritis Reumatoide/tratamiento farmacológico , Artritis Experimental/metabolismo , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
BACKGROUND: The physicochemical and functional properties of pectin (JFP) extracted from edible portions (including pericarp and seed) of raw jackfruit (an underutilized tropical fruit) at four different maturity stages (referred to as stages I, II, III, and IV) were characterized in terms of extraction yields, chemical composition, molecular weight, and antioxidant properties to evaluate its potential use in foods. RESULT: The JFP yield increased from 9.7% to 21.5% with fruit maturity, accompanied by an increase in the galacturonic acid content (50.1%, 57.1%, 63.6%, and 65.2%) for stages I-IV respectively. The molecular weight increased from 147 kDa in stage I to 169 kDa in stage III, but decreased to 114 kDa in stage IV, probably due to cell-wall degradation during maturation. The JFP was of the high methoxyl type and the degree of esterification increased from 65% to 87% with fruit maturity. The functional properties of JFP were similar to or better than those reported for commercial apple pectin, thus highlighting its potential as a food additive. Although the phenolics and flavonoids content of JFP decreased with fruit maturity, their antioxidant capacity increased, which may be correlated with the increased content of galacturonic acid upon fruit development. Gels prepared from JFP showed viscoelastic behavior. Depending on the maturity stage in which they were obtained, different gelation behavior was seen. CONCLUSION: The study confirmed the potential of pectin extracted from edible parts of jackfruit as a promising source of high-quality gelling pectin with antioxidant properties, for food applications. © 2022 Society of Chemical Industry.
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Artocarpus , Pectinas , Pectinas/química , Artocarpus/química , Antioxidantes/análisis , Frutas/químicaRESUMEN
Food industry is actively looking for alternative ingredients to replace saturated and trans fats in foods while preserving their original organoleptic attributes to ensure consumers' acceptance. A plausible approach is the replacement of solid fats with oleogels. Oleogels can be engineered to mimic properties that are commonly played by regular solid fats but using hydrophobic liquid vegetable oil with an optimum fatty acid profile and, they can also act as carriers for lipophilic bioactive substance. Low molecular weight oleogelators (LMOGs) are well studied and reviewed. In contrast, high molecular weight oleogelators (HMOGs) e.g., polysaccharides and proteins, are not fully researched yet. This review focusses on development of HMOG oleogels produced by means of emulsion templated, direct dispersion, foam templated and solvent exchange methods that can influence the stability, physicochemical properties and their potential application in food industry. Multi-component oleogels can solve the inefficiencies in a single component oleogel and, thus, combinations of HMOGs and HMOGs & LMOGs can produce oleogels with desired properties. These new oleogels can find application as fat substitutes in food products, providing better nutritional and sensory acceptance. A comprehensive overview of recent developments in the field of HMOG and multicomponent oleogels with HMOG is deeply reviewed.
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Lactoferrin (Lf) is a natural iron-binding globular glycoprotein, present mainly in milk. It maintains human health through its multifunctional activities, including immunomodulation, iron metabolism, and antioxidant and prebiotic efficacy. It also shows anti-microbial, anti-fungal, and anti-viral activities against a broad spectrum of viruses, including SARS-CoV-2 that causes COVID-19. In addition, several investigations established that Lf is involved in bone metabolism, neural development, and metabolic disorders. In this review, we summarize the in vitro and in vivo studies on the health benefits of Lf and its bioavailability. Furthermore, we briefly describe the production, industrial applications and future prospects of Lf.
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COVID-19 , Lactoferrina , Humanos , Animales , Lactoferrina/metabolismo , SARS-CoV-2 , Leche/metabolismo , Hierro/metabolismoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Dillenia indica L. is an edible plant from the Dilleniaceae family present in the forest of India and other Asian countries. Different parts of this plant are being used in the traditional system of medicines for various diseases like diabetes, indigestion, asthma, jaundice, and rheumatic pain by various rural communities. This plant is very common among Khamptis traditional healers, the rural community of the Dhemaji district of Assam, ethnic communities of Dibru-Saikhowa Biosphere Reserve of Northeast, India for various medicinal uses. It is observed as a 'vat' suppressant and 'pitta' boosting medicine in Ayurveda. AIM OF THE STUDY: The aim of this research was to evaluate the effect of hydroethanolic extract of Dillenia indica leaf (DI-HET) against non-alcoholic fatty liver disease (NAFLD) as it is reported effective against jaundice in traditional medicine. We are also planning to see the various molecular mechanisms responsible for its effect if it is efficacious. STUDY DESIGN/METHOD: An in vitro model for NAFLD was employed in this study. For this HepG2 cells were incubated with 100 µM of oleic acid (OA) for 24 h. For evaluation of the effect of DI-HET, the extracts (5 or 10 µg/mL) were pretreated to the OA group. Fenofibrate was the positive control. Various parameters relevant to lipogenesis and ß-oxidation of fatty acids like intracellular lipid accumulation, reactive oxygen species (ROS), mitochondrial stress, and key proteins were studied. RESULTS: DI-HET significantly reduced the intracellular lipid accumulation in OA treated cells. And also substantially decreased the expression of lipogenic proteins and increased ß-oxidation in the OA group. OA induced ROS generation was found to reduce with DI-HET treatment. Western blot analysis showed that the expression of LXR-α, SREBP-1C, SREBP-2, HMGCR, FAS, CD-36, and ACOX-1 were downregulated while that of SIRT-1, p-LKB-, p-AMPK, p-ACC, CPT-1, and PPAR-α upregulated in DI-HET treatment. LCMS/MS analysis showed the presence of polyphenols like naringenin, catechin, epicatechin, shikimic acid, syringic acid, vanillic acid, and kaempferol. CONCLUSION: These results suggest that DI-HET is effective against NAFLD by activation of the SIRT-1/p-LKB-1/AMPK signaling pathway via polyphenols present in the extract.
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Dilleniaceae , Enfermedad del Hígado Graso no Alcohólico , Sirtuinas , Proteínas Quinasas Activadas por AMP/metabolismo , Dilleniaceae/metabolismo , Células Hep G2 , Humanos , Hidroximetilglutaril-CoA Reductasas/metabolismo , Hidroximetilglutaril-CoA Reductasas/farmacología , Hidroximetilglutaril-CoA Reductasas/uso terapéutico , Metabolismo de los Lípidos , Enfermedad del Hígado Graso no Alcohólico/tratamiento farmacológico , Enfermedad del Hígado Graso no Alcohólico/metabolismo , Ácido Oléico/farmacología , PPAR alfa/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Polifenoles/farmacología , Especies Reactivas de Oxígeno , Transducción de Señal , Sirtuinas/metabolismoRESUMEN
Pectin hydrogel is a soft hydrocolloid with multifaceted utilities in the food sector. Substantial knowledge acquired on the gelation mechanisms and structure-function relationship of pectin has led to interesting functions of pectin hydrogel. Food applications of pectin hydrogels can be categorized under four headings: food ingredients/additives, food packaging, bioactive delivery and health management. The cross-linked and tangly three-dimensional structure of pectin gel renders it an ideal choice of wall material for the encapsulation of biomolecules and living cells; as a fat replacer and texturizer. Likewise, pectin hydrogel is an effective satiety inducer due to its ability to swell under the simulated gastric and intestinal conditions without losing its gel structure. Coating or composites of pectin hydrogel with proteins and other polysaccharides augment its functionality as an encapsulant, satiety-inducer and food packaging material. Low-methoxyl pectin gel is an appropriate food ink for 3D printing applications due to its viscoelastic properties, adaptable microstructure and texture properties. This review aims at explaining all the applications of pectin hydrogels, as mentioned above. A comprehensive discussion is presented on the approaches by which pectin hydrogel can be transformed as a resourceful material by controlling its dimensions, state, and rheology. The final sections of this article emphasize the recent research trends in this discipline, such as the development of smart hydrogels, injectable gels, aerogels, xerogels and oleogels from pectin.
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Hidrogeles , Pectinas , Hidrogeles/química , Pectinas/química , Polisacáridos , Impresión Tridimensional , ReologíaRESUMEN
BACKGROUND: Tidal expiratory flow limitation (EFLT) is common among COPD patients. Whether EFLT changes during sleep and can be abolished during home ventilation is not known. METHODS: COPD patients considered for noninvasive ventilation used a ventilator which measured within-breath reactance change at 5 Hz (∆Xrs) and adjusted EPAP settings to abolish EFLT. Participants flow limited (∆Xrs > 2.8) when supine underwent polysomnography (PSG) and were offered home ventilation for 2 weeks. The EPAP pressure that abolished EFLT was measured and compared to that during supine wakefulness. Ventilator adherence and subjective patient perceptions were obtained after home use. RESULTS: Of 26 patients with supine EFLT, 15 completed overnight PSG and 10 the home study. In single night and 2-week home studies, EFLT within and between participants was highly variable. This was unrelated to sleep stage or body position with only 14.6% of sleep time spent within 1 cmH2O of the awake screening pressure. Over 2 weeks, mean EPAP was almost half the mean maximum EPAP (11.7 vs 6.4 cmH2O respectively). Group mean ∆Xrs was ≤ 2.8 for 77.3% of their home use with a mean time to abolish new EFLT of 5.91 min. Adherence to the ventilator varied between 71 and 100% in prior NIV users and 36-100% for naïve users with most users rating therapy as comfortable. CONCLUSIONS: Tidal expiratory flow limitation varies significant during sleep in COPD patients. This can be controlled by auto-titrating the amount of EPAP delivered. This approach appears to be practical and well tolerated by patients. TRIAL REGISTRATION: The trial was retrospectively registered at CT.gov NCT04725500.
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Espiración/fisiología , Ventilación no Invasiva/métodos , Polisomnografía/métodos , Enfermedad Pulmonar Obstructiva Crónica/fisiopatología , Enfermedad Pulmonar Obstructiva Crónica/terapia , Volumen de Ventilación Pulmonar/fisiología , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Enfermedad Pulmonar Obstructiva Crónica/diagnóstico , Estudios RetrospectivosRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Alpinia galanga, commonly known as greater galangal or raasna, is widely used in Ayurveda against various inflammatory disorders. It is also known as Kulinjan, Aratha, Rasna or Sugandhamula. Some of the Ayurvedic preparations using the rhizome of Alpinia galanga are Rasnadi kashayam, Rasna panchakam, Rasnapthakam, and Rasnarendadi. The aromatic rhizome is the source of the drug greater galangal and it is also used as a spice in South and South East Asia. However, the molecular mechanism of action of A galanga against inflammation remains poorly understood. AIM OF THE STUDY: To elucidate the anti-inflammatory effect of hydroalcoholic extract of Alpinia galanga rhizome. STUDY DESIGN/METHOD: The mechanism of the anti-inflammatory effect of hydroalcoholic extract of Alpinia galanga (AGE) was investigated by enzyme-linked immunosorbent assay (ELISA), Western blot, and immunofluorescence in LPS stimulated murine macrophage cell line (RAW 264.7). HPLC analysis was done to elucidate the rich polyphenolic nature of AGE. RESULTS: The study showed that pre-treatment with AGE downregulated the release of pro-inflammatory mediators (IL-6, TNF-α, NO, and ROS) and stimulated the release of anti-inflammatory mediator IL-10 in LPS stimulated RAW 264.7 cells. The vital enzymes of inflammation (iNOS, COX-2, and MMP-9) were also downregulated by pre-treatment with AGE. AGE targeted the upstream elements of the inflammatory cascade by blocking LPS induced activation of TLR4 and JAK/STAT pathway. The phosphorylation of downstream kinases was significantly affected. The inhibition of nuclear translocation of NFκB further confirmed the specific inhibition of the TLR4 pathway. Particularly AGE inhibited the phosphorylation of JNK, p38, IκBα, and STAT. HPLC analysis of the AGE showed the polyphenol-rich nature of the extract. CONCLUSIONS: The results from this study provide firm evidence that AGE exerts its anti-inflammatory effect via modulation of TLR4 and JAK/STAT pathway.
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Alpinia/química , Quinasas Janus/genética , Factor 88 de Diferenciación Mieloide/genética , Extractos Vegetales/farmacología , Factores de Transcripción STAT/genética , Receptor Toll-Like 4/genética , Proteínas Quinasas p38 Activadas por Mitógenos/genética , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Supervivencia Celular/efectos de los fármacos , Ciclooxigenasa 2/metabolismo , Citocinas/metabolismo , Regulación hacia Abajo/efectos de los fármacos , Gelatinasas/metabolismo , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Quinasas Janus/metabolismo , Lipopolisacáridos/toxicidad , Metaloproteinasa 9 de la Matriz/metabolismo , Ratones , Factor 88 de Diferenciación Mieloide/metabolismo , FN-kappa B/antagonistas & inhibidores , FN-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Extractos Vegetales/química , Células RAW 264.7 , Especies Reactivas de Oxígeno/metabolismo , Rizoma/química , Factores de Transcripción STAT/metabolismo , Transducción de Señal/efectos de los fármacos , Receptor Toll-Like 4/metabolismo , Proteínas Quinasas p38 Activadas por Mitógenos/metabolismoRESUMEN
A new, dynamic diastereomeric crystallization method has been developed, in which the mother liquors are continuously separated, racemized over a fixed-bed catalyst, and recirculated to the crystallizer in a resolution-racemization-recycle (R3) process. Separating the racemization from crystallization overcomes problems of using catalysts in situ, that suffer conflicting sets of conditions, inhibition, and separation. Continuous racemization has been achieved through the covalent attachment of [IrCp*I2]2 SCRAM catalyst to Wang resin solid support to give a fixed-bed catalyst. One tertiary and a variety of secondary optically enriched amines have been racemized efficiently, with residence times compatible with the crystallization (2.25-30 min). The catalyst demonstrates lower turnover (TOF) than the homogeneous analogue but with reuse shows a long lifetime (e.g., 40 recycles, 190 h) giving acceptable turnover number (TON) (up to 4907). The slow release of methylamine during racemization of N-methyl amines was found to inactivate the catalyst, which could be partially reactivated using hydroiodic acid. Dynamic crystallization is achieved in the R3 process through the continual removal of the more soluble diastereomer and supply of the less soluble one. The solubility of the diastereomers was determined, and the difference correlates to the rate of resolution but is also affected by the rates of racemization, crystal growth, and dissolution. A variety of cyclic and acyclic amine salts were resolved using mandelic acid (MA) and ditoluoyl tartaric acid (DTTA) with higher resolvability (S = yield × d.e.) than the simple diastereomeric crystallization alone. Comparing resolvabilities, resolutions were 1.6-44 times more effective with the R3 process than batch, though one case was worse. Further investigation of this revealed an unusual thermodynamic switching behavior: rac-N-methylphenethylamine was initially resolved as an (S,S)-bis-alkylammonium tartrate crystal but over time became the equivalent (R,S) salt. Thermal, mixing, concentration, stoichiometry, and seeding conditions were all found to affect the onset of the switching behavior which is only associated with difunctional resolving reagents.
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Coffee foam is the frothy layer that forms above the liquid phase of espresso and instant coffee beverages. While the carbon dioxide formed during roasting is responsible for crema formation in espresso, gasification is the established foaming approach in instant coffee. The protein-like fractions and polysaccharides extracted from roasted coffee promote foamability and foam stability, respectively. Crema of consolidated texture retains the volatile aromatic substances and prevents the espresso from cooling too rapidly. Further, an inverse relationship has been observed between foam persistence and volatility of aroma molecules above the cup. Gasified spray-dried instant coffee exhibited an accelerated delivery rate of hydrophobic aroma compounds. Thus, foam is the signature of a high-quality cup of coffee. Despite its various functionalities, coffee foam is scarcely investigated owing to its metastable nature. Only recently, the chemical, structural, and interfacial rheology properties of the coffee foam have been looked at. The current study intends to review the scientific knowledge acquired on coffee foam, thus far. The initial sections describe the general attributes and functions of espresso and instant coffee foam. Further, the mechanisms of formation and stabilization of coffee foam are detailed, followed by the factors influencing the same. The following discussions focus on the role of coffee foam in determining the sensory and aroma release characteristics of the beverages. The scope for future research in this field of study is highlighted in the concluding section.
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Café , Odorantes , Bebidas , Dióxido de Carbono , Odorantes/análisis , VolatilizaciónRESUMEN
Advanced glycation end products (AGEs) are implicated to be the key players in most of the diabetic complications. The AGE's interfere with the proteins heterogeneously, thereby rendering denaturation and the consequent loss of function and accumulation. Thus, a novel natural product inspired indeno[2,1-c]pyridinone (4a-4ad) molecular templates with AGE's trapping potential was designed through scaffold hopping approach and synthesized via facile two-step synthetic route. Amongst the tested indeno[2,1-c]pyridinone hybrids, 4i, 4x and 4aa exhibited excellent efficiency in trapping the AGE's. The percentage of antiglycation is measured by the analytical model system, i.e. via MG trapping capacity; here the compounds 4i, 4x and 4aa with 50.03%, 69.58%, and 93.37% respectively has displayed promising efficiency. In particular, 4aa demonstrated better activity than the positive control aminoguanidine (79.82%). The in-vitro toxicity of compounds was tested on L6 rat skeletal muscle cell lines revealed that none of the compounds showed any significant toxicity at concentrations up to 1000 µM.
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Productos Biológicos/farmacología , Diseño de Fármacos , Productos Finales de Glicación Avanzada/antagonistas & inhibidores , Piridonas/farmacología , Productos Biológicos/síntesis química , Productos Biológicos/química , Línea Celular , Relación Dosis-Respuesta a Droga , Productos Finales de Glicación Avanzada/análisis , Humanos , Estructura Molecular , Piridonas/síntesis química , Piridonas/química , Relación Estructura-Actividad CuantitativaRESUMEN
Isoniazid (INH), one of the first-line drugs used for the treatment of tuberculosis, is a prodrug which is activated by the intracellular KatG enzyme of Mycobacterium tuberculosis The activated drug hinders cell wall biosynthesis by inhibiting the InhA protein. INH-resistant strains of M. tuberculosis usually have mutations in katG, inhA, ahpC, kasA, and ndh genes. However, INH-resistant strains which do not have mutations in any of these genes are reported, suggesting that these strains may adopt some other mechanism to become resistant to INH. In the present study, we characterized Rv2170, a putative acetyltransferase in M. tuberculosis, to elucidate its role in inactivating isoniazid. The purified recombinant protein was able to catalyze the transfer of the acetyl group to INH from acetyl coenzyme A (acetyl-CoA). High-performance liquid chromatography (HPLC) and liquid chromatography-mass spectrometry (LC-MS) analyses showed that following acetylation by Rv2170, INH is broken down into isonicotinic acid and acetylhydrazine. A drug susceptibility assay and confocal analysis showed that Mycobacterium smegmatis, which is susceptible to INH, is not inhibited by INH acetylated with Rv2170. Mutant proteins of Rv2170 failed to acetylate INH. Recombinant M. smegmatis and M. tuberculosis H37Ra overexpressing Rv2170 were found to be resistant to INH at MICs that inhibited wild-type strains. Besides, intracellular M. tuberculosis H37Ra overexpressing Rv2170 survived better in macrophages when treated with INH. Our results strongly indicate that Rv2170 acetylates INH, and this could be one of the strategies adopted by at least some M. tuberculosis strains to overcome INH toxicity, although this needs to be tested in INH-resistant clinical strains.
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Isoniazida , Mycobacterium tuberculosis , Acetilación , Antituberculosos/farmacología , Proteínas Bacterianas/genética , Catalasa/genética , Farmacorresistencia Bacteriana/genética , Isoniazida/farmacología , Pruebas de Sensibilidad Microbiana , Mutación , Mycobacterium tuberculosis/genéticaRESUMEN
The present study investigated the nutritional composition of bran from rice (RB) and wheat (WB) and compared the natural virtues of crude extracts based on phenolic composition, antidiabetic and anticancer activities. The profiling of phenolic-rich ethyl acetate extracts (RBE and WBE) confirms that RBE is rich in catechol (0.122 mg/g dw), p-coumaric acid (0.159 mg/g dw), kaempferol (0.374 mg/g dw) and apigenin (0.399 mg/g dw); and WBE is affluent with catechol (0.144 mg/g dw), ferulic acid (0.160 mg/g dw), caffeic acid (0.083 mg/g dw) and ellagic acid (0.074 mg/g dw). RBE exhibited better antioxidant activity, inhibited the activity of α-amylase (IC50-353.41 µg/mL) and α-glucosidase (IC50-314.22 µg/mL), hindered glycation process (IC50-451.11 µg/mL), and enhanced glucose uptake in L6 muscle cells (20.4%) indicating its potential in diabetic management. RBE was toxic to HT29 colon cancer cells and decreased cell membrane integrity. RBE and WBE arrested cell-cycle transition in HT29 cells from G0 to G1 and G2 to M phase respectively and induced apoptosis (27.15% and 5.9%, respectively for RBE and WBE) suggesting anticancer activities of the extract. The study indicates that bran from rice and wheat are a potential source of dietary fibre and phytochemicals with antidiabetic and anticancer properties for developing value-added products with nutraceutical benefits.
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BACKGROUND: Soursop (Annona muricata L.) is an underutilized tropical and subtropical fruit with high nutritional and therapeutic benefits. This fruit is faced with enormous post-harvest losses due to its high perishability. This work was aimed to optimize the pectinase-assisted extraction conditions of soursop juice using Doehlert design and to study the effect of pectinase on its pectin structure. RESULTS: The predicted models were validated for all the responses studied and the regression coefficients ranged from 0.905 to 0.987 (P ≤ 0.05). An incubation time of 172 min, enzyme concentration of 0.04% (w/w) and incubation temperature at 42.9 °C were found to be the optimal conditions for soursop juice extraction, which resulted in 75.20%, 3.74, 7.35 °Brix, 87.06%T, and 0.44% MAE for soursop juice yield (%), pH, total soluble solids (TSS) (°Brix), clarity (%T) and titratable acidity (% malic acid equivalent, MAE), respectively. Morphologically, untreated soursop pulp presented a non-uniform spherical surface; enzyme hydrolyzed soursop exhibited ruptured and wrinkled surface; meanwhile for the different pectin obtained, untreated soursop pectin depicted porous surface and enzyme hydrolyzed soursop pectin showed whirling rough surface. Fourier-transform infrared (FTIR) confirmed the presence of similar chemical group stretching and vibrations in commercial pectin and soursop pectin. CONCLUSION: Under the optimum conditions, the numerical predictions were similar to the experimental data obtained, thus confirming the validity of the models. Application of enzyme treatment caused the breakdown of pectin structure as illustrated by scanning electron microscopy (SEM) and FTIR analyses.
Asunto(s)
Annona/química , Manipulación de Alimentos/métodos , Jugos de Frutas y Vegetales/análisis , Pectinas/química , Preparaciones de Plantas/aislamiento & purificación , Poligalacturonasa/química , Frutas/química , Preparaciones de Plantas/análisisRESUMEN
In this study, the prebiotic potential of soluble dietary fibre extracted from plantain inflorescence (PIF) was investigated. PIF demonstrated prebiotic potential by enhancing the growth of the probiotics under study and thereby hindered colon cancer development. The soluble dietary fibre from Musa paradisiaca inflorescence (PIF) was fermented using Lactobacillus casei and Bifidobacterium bifidum. The fermentation supernatants (LS and BS) were enriched with short chain fatty acids (SCFA) and were able to initiate apoptotic signalling in HT29 colon cancer cells leading to cell death. Both BS and LS exhibited cytotoxic effect; induced DNA damage and enhanced generation of reactive oxygen species in HT29 cells leading to apoptosis. The induction of apoptosis was facilitated by the reduction of membrane potential of mitochondria and ATP synthesis; enhanced delivery of cytochrome c and interference with the expression of pro/antiapoptotic proteins. BS, which exhibited better activity, was further analysed for the identification of differentially regulated proteins by performing two dimensional electrophoresis and MALDI-TOF mass spectrometry. Results emphasized on the fact that, the exposure to BSalteredthe HT29 proteins expression, particularly the upregulation of apoptosis- inducing factor-AIFM1 leading to apoptosis of HT29 cells.