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1.
Pak J Pharm Sci ; 37(2(Special)): 451-458, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38822549

RESUMO

The research aimed to explore the antioxidant potential of extracts from different parts of Clinacanthus nutans growing in Vietnam, a member of the Acanthaceae family. The plant's roots, stem and leaves were extracted using 96% ethanol. The antioxidant actions of these extracts were evaluated by DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) assay on thin-layer plates and 96 well plates. The extract with the most potent activity was applied for distribution extraction with solvents with different polarities, including dichloromethane, ethyl acetate and water. Dry column vacuum chromatography was utilized to obtain the most antioxidant-potent extract fractions. The stem extract had the lowest IC50 value of 6.85µg/mL, showing the most potent antioxidant activity. The ethyl acetate fraction from the stem extract expressed the lowest IC50 value of 9.67µg/mL. Meanwhile, fraction 5, separated from the ethyl acetate fraction of the stem extract, had the lowest IC50 value of 9.89µg/mL. In conclusion, the extracts from different parts of Clinacanthus nutans all expressed antioxidant action at different levels, in which the stem extract, the ethyl acetate fraction and fraction 5 from the ethyl acetate fraction displayed the most effective actions. These findings highlight the promising potential of Clinacanthus nutans in treating oxidative stress-associated diseases, inspiring further research and exploration in this area.


Assuntos
Acanthaceae , Antioxidantes , Extratos Vegetais , Acanthaceae/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Folhas de Planta/química , Caules de Planta/química , Solventes/química , Compostos de Bifenilo/química , Raízes de Plantas/química , Picratos/química
2.
Sci Rep ; 14(1): 12825, 2024 06 04.
Artigo em Inglês | MEDLINE | ID: mdl-38834643

RESUMO

Cyclic tetrapeptides c(Pro-Phe-Pro-Phe) obtained by the mechanosynthetic method using a ball mill were isolated in a pure stereochemical form as a homochiral system (all L-amino acids, sample A) and as a heterochiral system with D configuration at one of the stereogenic centers of Phe (sample B). The structure and stereochemistry of both samples were determined by X-ray diffraction studies of single crystals. In DMSO and acetonitrile, sample A exists as an equimolar mixture of two conformers, while only one is monitored for sample B. The conformational space and energetic preferences for possible conformers were calculated using DFT methods. The distinctly different conformational flexibility of the two samples was experimentally proven by Variable Temperature (VT) and 2D EXSY NMR measurements. Both samples were docked to histone deacetylase HDAC8. Cytotoxic studies proved that none of the tested cyclic peptide is toxic.


Assuntos
Peptídeos Cíclicos , Peptídeos Cíclicos/química , Peptídeos Cíclicos/farmacologia , Humanos , Cristalografia por Raios X , Histona Desacetilases/metabolismo , Histona Desacetilases/química , Simulação de Acoplamento Molecular , Oligopeptídeos/química , Oligopeptídeos/farmacologia , Estereoisomerismo , Solventes/química
3.
BMC Biotechnol ; 24(1): 39, 2024 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-38849803

RESUMO

BACKGROUND: Melia azedarach is known as a medicinal plant that has wide biological activities such as analgesic, antibacterial, and antifungal effects and is used to treat a wide range of diseases such as diarrhea, malaria, and various skin diseases. However, optimizing the extraction of valuable secondary metabolites of M. azedarach using alternative extraction methods has not been investigated. This research aims to develop an effective, fast, and environmentally friendly extraction method using Ultrasound-assisted extraction, methanol and temperature to optimize the extraction of two secondary metabolites, lupeol and stigmasterol, from young roots of M. azedarach using the response surface methodology. METHODS: Box-behnken design was applied to optimize different factors (solvent, temperature, and ultrasonication time). The amounts of lupeol and stigmasterol in the root of M. azedarach were detected by the HPLC-DAD. The required time for the analysis of each sample by the HPLC-DAD system was considered to be 8 min. RESULTS: The results indicated that the highest amount of lupeol (7.82 mg/g DW) and stigmasterol (6.76 mg/g DW) was obtained using 50% methanol at 45 °C and ultrasonication for 30 min, and 50% methanol in 35 °C, and ultrasonication for 30 min, respectively. Using the response surface methodology, the predicted conditions for lupeol and stigmasterol from root of M. azedarach were as follows; lupeol: 100% methanol, temperature 45 °C and ultrasonication time 40 min (14.540 mg/g DW) and stigmasterol 43.75% methanol, temperature 34.4 °C and ultrasonication time 25.3 min (5.832 mg/g DW). CONCLUSIONS: The results showed that the amount of secondary metabolites lupeol and stigmasterol in the root of M. azedarach could be improved by optimizing the extraction process utilizing response surface methodology.


Assuntos
Melia azedarach , Triterpenos Pentacíclicos , Estigmasterol , Triterpenos Pentacíclicos/metabolismo , Estigmasterol/metabolismo , Estigmasterol/isolamento & purificação , Estigmasterol/química , Melia azedarach/química , Cromatografia Líquida de Alta Pressão , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Extratos Vegetais/química , Temperatura , Solventes/química , Lupanos
4.
Luminescence ; 39(6): e4801, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38855811

RESUMO

Atopic dermatitis (AD) is a persistent, inflammatory skin condition that impacts approximately 15 to 20% of children and 1 to 3% of adults globally. Common skin manifestations include papules, papulovesicular, and brown or red patches with swelling, crusting, and flaking. Therefore, the drug abrocitinib (ABR) was approved by the US FDA as an oral treatment for atopic dermatitis. The present study outlines the development of innovative, thermostable, and pH-stable organic solvent-free nitrogen-doped carbon dots (N@CQDs) synthesized through a one-step method for evaluating ABR with a notable quantum yield of 33.84% to minimize the use of organic solvents. Their cost-effectiveness, eco-friendly characteristics, and outstanding photocatalytic properties have established them as a promising alternative to conventional luminescent techniques like fluorescent dyes and luminous derivatization technique. The reaction of ABR with N@CQDs led to a significant decrease in the luminescent response of the produced green and stable carbon quantum dots at 513 nm. The detection range was determined to be 1.0-150.0 ng mL-1, with a lower limit of quantitation (LOQ) equal to 0.52 ng mL-1 based on the linear graph. The green method effectively used for analysis of ABR in pharmaceutical tablets and pharmacokinetic study with high sensitivity.


Assuntos
Carbono , Nitrogênio , Pontos Quânticos , Pontos Quânticos/química , Carbono/química , Nitrogênio/química , Humanos , Pirimidinas/química , Pirimidinas/sangue , Pirimidinas/síntese química , Fluorometria , Corantes Fluorescentes/química , Corantes Fluorescentes/síntese química , Solventes/química , Estrutura Molecular
5.
AAPS PharmSciTech ; 25(5): 132, 2024 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-38849590

RESUMO

Hydrogen sulfide (H2S) is a multifaceted gasotransmitter molecule which has potential applications in many pathological conditions including in lowering intraocular pressure and providing retinal neuroprotection. However, its unique physicochemical properties pose several challenges for developing its efficient and safe delivery method system. This study aims to overcome challenges related to H2S toxicity, gaseous nature, and narrow therapeutic concentrations range by developing polymeric microparticles to sustain the release of H2S for an extended period. Various formulation parameters and their interactions are quantitatively identified using Quality-by-Design (QbD) approach to optimize the microparticle-based H2S donor (HSD) delivery system. Microparticles were prepared using a solvent-evaporation coacervation process by using polycaprolactone (PCL), soy lecithin, dichloromethane, Na2S.9H2O, and silicone oil as polymer, surfactant, solvent, HSD, and dispersion medium, respectively. The microparticles were characterized for size, size distribution, entrapment efficiency, and H2S release profile. A Main Effects Screening (MES) and a Response Surface Design (RSD) model-based Box-Behnken Design (BBD) was developed to establish the relationship between critical process parameters (CPPs) and critical quality attributes (CQAs) qualitatively and quantitatively. The MES model identified polymer to drug ratio and dispersion medium quantity as significant CPPs among others, while the RSD model established their quantitative relationship. Finally, the target product performance was validated by comparing predicted and experimental outcomes. The QbD approach helped in achieving overall desired microparticle characteristics with fewer trials and provided a mathematical relationship between the CPPs and the CQAs useful for further manipulation and optimization of release profile up to at least 30 days.


Assuntos
Sulfeto de Hidrogênio , Tamanho da Partícula , Polímeros , Sulfeto de Hidrogênio/química , Polímeros/química , Química Farmacêutica/métodos , Solventes/química , Poliésteres/química , Microesferas , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Portadores de Fármacos/química , Tensoativos/química , Composição de Medicamentos/métodos
6.
Biophys Chem ; 311: 107272, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38824845

RESUMO

In the presented work, a study on the solubility and intermolecular interactions of l-serine and L-cysteine was carried out in binary mixtures of H2O + dimethylformamide (DMF), H2O + dimethylsulfoxide (DMSO), and H2O + acetonitrile (ACN) in the temperature range of T = 288.15 K to 308.15 K. l-serine exhibited the highest solubility in water, while L-cysteine was more soluble in water-DMF. The solvation process was assessed through standard Gibbs energy calculations, indicating the solvation stability order: water-ACN > water-DMSO > water-DMF for l-serine, and water-DMF > water-DMSO > water-ACN for L-cysteine. This study also explored the influence of these amino acids on solvent-solvent interactions, revealing changes in chemical entropies and self-association patterns within the binary solvent mixtures.


Assuntos
Acetonitrilas , Cisteína , Dimetil Sulfóxido , Dimetilformamida , Serina , Solubilidade , Temperatura , Água , Dimetil Sulfóxido/química , Serina/química , Acetonitrilas/química , Água/química , Cisteína/química , Dimetilformamida/química , Termodinâmica , Solventes/química
7.
Sci Data ; 11(1): 432, 2024 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-38693191

RESUMO

The genus Clostridium is a large and diverse group within the Bacillota (formerly Firmicutes), whose members can encode useful complex traits such as solvent production, gas-fermentation, and lignocellulose breakdown. We describe 270 genome sequences of solventogenic clostridia from a comprehensive industrial strain collection assembled by Professor David Jones that includes 194 C. beijerinckii, 57 C. saccharobutylicum, 4 C. saccharoperbutylacetonicum, 5 C. butyricum, 7 C. acetobutylicum, and 3 C. tetanomorphum genomes. We report methods, analyses and characterization for phylogeny, key attributes, core biosynthetic genes, secondary metabolites, plasmids, prophage/CRISPR diversity, cellulosomes and quorum sensing for the 6 species. The expanded genomic data described here will facilitate engineering of solvent-producing clostridia as well as non-model microorganisms with innately desirable traits. Sequences could be applied in conventional platform biocatalysts such as yeast or Escherichia coli for enhanced chemical production. Recently, gene sequences from this collection were used to engineer Clostridium autoethanogenum, a gas-fermenting autotrophic acetogen, for continuous acetone or isopropanol production, as well as butanol, butanoic acid, hexanol and hexanoic acid production.


Assuntos
Clostridium , Genoma Bacteriano , Filogenia , Clostridium/genética , Solventes , Fermentação
8.
Nat Commun ; 15(1): 3919, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38724503

RESUMO

Biological macromolecules can condense into liquid domains. In cells, these condensates form membraneless organelles that can organize chemical reactions. However, little is known about the physical consequences of chemical activity in and around condensates. Working with model bovine serum albumin (BSA) condensates, we show that droplets swim along chemical gradients. Active BSA droplets loaded with urease swim toward each other. Passive BSA droplets show diverse responses to externally applied gradients of the enzyme's substrate and products. In all these cases, droplets swim toward solvent conditions that favor their dissolution. We call this behavior "dialytaxis", and expect it to be generic, as conditions which favor dissolution typically reduce interfacial tension, whose gradients are well-known to drive droplet motion through the Marangoni effect. These results could potentially suggest alternative physical mechanisms for active transport in living cells, and may enable the design of fluid micro-robots.


Assuntos
Soroalbumina Bovina , Soroalbumina Bovina/química , Soroalbumina Bovina/metabolismo , Animais , Urease/metabolismo , Urease/química , Solubilidade , Bovinos , Solventes/química , Tensão Superficial
9.
Phys Chem Chem Phys ; 26(20): 14766-14776, 2024 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-38716816

RESUMO

Hybrid ionic fluids (HIFs) are newly emerging and fascinating sustainable solvent media, which are attracting a great deal of scientific interest in protecting the native structure of proteins. For a few decades, there has been a demand to consider ionic liquids (ILs) and deep eutectic solvents (DESs) as biocompatible solvent media for enzymes; however, in some cases, these solvent media also show limitations. Therefore, this work focuses on synthesising novel HIFs to intensify the properties of existing ILs and DESs by mixing them. Herein, HIFs have been synthesised by the amalgamation of a deep eutectic solvent (DES) and an ionic liquid (IL) with a common cation or anion. Later on, the stability and activity of hen's egg white lysozyme (Lyz) in the presence of biocompatible solvent media and HIFs were studied by various techniques such as UV-vis, steady-state fluorescence, circular dichroism (CD), Fourier transform infrared spectroscopy (FT-IR) and dynamic light scattering (DLS) measurements. This work emphasises the effect of a DES (synthesised using 1 : 2 choline chloride and malonic acid) [Maline], ILs (1-butyl-3-methylimidazolium chloride [BMIM]Cl or choline acetate [Chn][Ac]) and their corresponding HIFs on the structure and functionality of Lyz. Moreover, we also studied the secondary structure, thermal stability, enzymatic activity and thermodynamic profile of Lyz at pH = 7 in the presence of varying concentrations (0.1 to 0.5 M) of [BMIM]Cl and [Chn][Ac] ILs, Maline as a DES, and Maline [BMIM]Cl (HIF1) and Maline [Chn][Ac] (HIF2). Spectroscopic results elucidate that ILs affect the activity and structural stability of Lyz. In contrast, the stability and activity are inhibited by DES and are enhanced by HIFs at all the studied concentrations. Overall, the experimental results studied explicitly elucidate that the structure and stability of Lyz are maintained in the presence of HIF1 while these properties are intensified in HIF2. This study shows various applications in biocompatible green solvents, particularly in the stability and functionality of proteins, due to their unique combination where the properties counteract the negative effect of either DESs or ILs in HIFs.


Assuntos
Solventes Eutéticos Profundos , Estabilidade Enzimática , Líquidos Iônicos , Muramidase , Líquidos Iônicos/química , Muramidase/química , Muramidase/metabolismo , Solventes Eutéticos Profundos/química , Solventes/química , Animais , Galinhas , Colina/química
10.
J Chromatogr A ; 1726: 464960, 2024 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-38718695

RESUMO

Mass transport through the mesopore space of a reversed-phase liquid chromatography (RPLC) column depends on the properties of the chromatographic interface, particularly on the extent of the organic-solvent ditch that favors the analyte surface diffusivity. Through molecular dynamics simulations in cylindrical RPLC mesopore models with pore diameters between 6 and 12 nm we systematically trace the evolution of organic-solvent ditch overlap due to spatial confinement in the mesopore space of RPLC columns for small-molecule separations. Each pore model of a silica-based, endcapped, C18-stationary phase is equilibrated with two mobile phases of comparable elution strength, namely 70/30 (v/v) water/acetonitrile and 60/40 (v/v) water/methanol, to consider the influence of the mobile-phase composition on the onset of organic-solvent ditch overlap. The simulations show that, as the pore diameter decreases from 9 to 6 nm, the bonded-phase density extends and compacts towards the pore center, which leads to increased accumulation of organic-solvent excess and thus enhanced organic-solvent diffusivity in the ditch. Because the acetonitrile ditch is more pronounced than the methanol ditch, acetonitrile ditch overlap sets in at less severe spatial confinement than methanol ditch overlap. The pore-averaged methanol and acetonitrile diffusivities are considerably raised by ditch overlap in the 6 nm-diameter pore, but also benefit from the ditch (without overlap) in the 7 to 12 nm-diameter pores, whereby local and pore-averaged effects are generally larger for acetonitrile than methanol.


Assuntos
Acetonitrilas , Cromatografia de Fase Reversa , Metanol , Simulação de Dinâmica Molecular , Solventes , Cromatografia de Fase Reversa/métodos , Acetonitrilas/química , Solventes/química , Metanol/química , Porosidade , Difusão , Dióxido de Silício/química , Água/química
11.
J Pharm Biomed Anal ; 245: 116200, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-38723557

RESUMO

A high-performance liquid chromatography (HPLC) method was developed for the analysis of Allopurinol and its Ph.Eur. impurities using a porous graphitic carbon (PGC) stationary phase. Retention behavior of solutes was studied across a wide temperature range (30-90 °C) and various gradient times (5-20 min). Analysis of the data revealed distinct retention mechanisms between reversed-phase and PGC phases. However, it was proved that the retention of Allopurinol and its Ph.Eur. impurities on PGC stationary phase can be effectively modeled using the linear solvent strength (LSS) theory. This allows for the utilization of LSS-based method development software to optimize methods under these conditions. By using commercial chromatographic modeling software, separation of Allopurinol and Ph.Eur. impurities was optimized within a large design space. At the optimized operating conditions (pH = 2.0, tG = 6 min, T = 60 °C), all solutes were separated within 6 min with baseline resolution. Comparison between predicted and experimentally measured chromatograms further confirmed the applicability of LSS theory in developing analytical methods for PGC-based HPLC systems. The presented approach offers a general framework for method development on PGC phases.


Assuntos
Alopurinol , Grafite , Solventes , Cromatografia Líquida de Alta Pressão/métodos , Grafite/química , Solventes/química , Alopurinol/química , Alopurinol/análise , Porosidade , Temperatura , Contaminação de Medicamentos/prevenção & controle , Temperatura Alta
12.
Phys Chem Chem Phys ; 26(20): 14970-14979, 2024 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-38739372

RESUMO

Curcumin is a medicinal agent that exhibits anti-cancer and anti-Alzheimer's disease properties. It has a keto-enol moiety that gives rise to many of its chemical properties including metal complexation and acid-base equilibria. A previous study has shown that keto-enol tautomerization at this moiety is implicated in the anti-Alzheimer's disease effect of curcumin, highlighting the importance of this process. In this study, tautomerization of curcumin in methanol, acetone and acetonitrile was investigated using time-resolved 1H nuclear magnetic resonance spectroscopy. Curcumin undergoes hydrogen-deuterium exchange with the solvents and the proton resonance peak corresponding to the hydrogen at the α-carbon position (Cα) decays as a function of time, signifying deuteration at this position. Because tautomerization is the rate limiting step in the deuteration of curcumin at the Cα position, the rate of tautomerization is inferred from the rate of deuteration. The rate constant of tautomerization of curcumin shows a temperature dependence and analysis using the Arrhenius equation revealed activation energies (Ea) of tautomerization of (80.1 ± 5.9), (64.1 ± 1.0) and (68.3 ± 5.5) kJ mol-1 in methanol, D2O/acetone and D2O/acetonitrile, respectively. Insight into the role of water in tautomerization of curcumin was further offered by density functional theory studies. The transition state of tautomerization was optimized in the presence of water molecules. The results show a hydrogen-bonded solvent bridge between the diketo moiety and Cα of curcumin. The Ea of tautomerization of curcumin shows a strong dependence on the number of water molecules in the solvent bridge, indicating the critical role played by the solvent bridge in catalyzing tautomerization of curcumin.


Assuntos
Curcumina , Curcumina/química , Metanol/química , Acetonitrilas/química , Acetona/química , Isomerismo , Termodinâmica , Solventes/química
13.
Front Public Health ; 12: 1370767, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38756897

RESUMO

Background: While overall head and neck cancer incidence decreases due to reduced tobacco and alcohol consumption, the incidence of HPV negative oral cavity squamous cell carcinoma (SCC) is raising in several industrialized countries, especially in non-smoking and non-drinking patients. Case presentation: We document a case of gingiva SCC in a 56 years old never-smoker patient reporting low alcohol consumption and unusual occupational solvent exposure. The HPV-negative lesion was surgically removed in 2018, and the patient remains in complete remission 4 years after recurrent surgery in 2019. In 2021, the patient was referred to the occupational cancer consultation. The patient worked as screen printer for 18 years. He reported mouth siphoning every 2-3 days to transfer organic solvents (mainly aromatic hydrocarbons and ketones) from containers into smaller recipients, with regular passage of solvents into his mouth. Conclusion: According to the literature, the frequency of solvent siphoning using mouth is likely to be underestimated. While our review did not find studies reporting longterm consequences to the oral cavity of mouth siphoning, current evidence supports a positive association of upper aero digestive tract SCC with occupational exposures to organic solvents and printing processes. In absence of major extraprofessional factors, the HPV-negative gingiva SCC of this patient might be attributable to the regular occupational oral solvent exposure. While the available evidence remains limited to formally establish a causal relationship, clinicians should investigate this hazardous work practice in patients with OSCC and history of solvent exposures.


Assuntos
Carcinoma de Células Escamosas , Exposição Ocupacional , Solventes , Humanos , Pessoa de Meia-Idade , Masculino , Exposição Ocupacional/efeitos adversos , Neoplasias Gengivais , Gengiva/patologia
14.
Food Res Int ; 187: 114368, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38763647

RESUMO

This study aimed to extract bamboo shoot protein (BSP) using different extraction approaches and compare their functional and physicochemical properties with commercial protein ingredients, including whey protein and soy protein isolates. The extraction methods including alkali extraction (AE), salt extraction (SE), and phosphate-aided ethanol precipitation (PE) were used. An enhanced solvent extraction method was utilized in combination, resulting in a significant improvement in the protein purity, which reached 81.59 %, 87.36 %, and 67.08 % respectively. The extraction methods had significant effects on the amino acid composition, molecular weight distribution, and functional properties of the proteins. SE exhibited the best solubility and emulsification properties. Its solubility reached up to 93.38 % under alkaline conditions, and the emulsion stabilized by SE with enhanced solvent extraction retained 60.95 % stability after 120 min, which could be attributed to its higher protein content, higher surface hydrophobicity, and relative more stable and organized protein structure. All three BSP samples demonstrated better oil holding capacity, while the SE sample showed comparable functional properties to soy protein such as foaming and emulsifying properties. These findings indicate the potential of BSP as an alternative plant protein ingredient in the food industry.


Assuntos
Interações Hidrofóbicas e Hidrofílicas , Proteínas de Plantas , Brotos de Planta , Solubilidade , Proteínas de Plantas/química , Proteínas de Plantas/isolamento & purificação , Brotos de Planta/química , Emulsões/química , Aminoácidos/química , Aminoácidos/análise , Peso Molecular , Proteínas do Soro do Leite/química , Proteínas de Soja/química , Solventes/química
15.
Pak J Pharm Sci ; 37(2): 315-320, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38767098

RESUMO

The present study was designed to assess Tradescantia spathacea's antidiabetic ability, as well as the antiulcer activity of the entire plant extract. The diabetic condition was evaluated using Streptozotocin's oral glucose tolerance test, diabetes-alloxan and diabetes-models. Antiulcer activities were observed in rats where gastric ulcers were either caused by oral administration of ethanol, or pyloric ligation. Standards include ranitidine, glibenclamide and sucralfate. In all models, the blood glucose levels of animals treated with the test extract were found to be significantly lower compared to diabetic care. Similarly, in all models, the ulcer index in the animals treated with the test extract was found to be significantly lower relative to the animals under vehicle supervision. Our findings say T. Spathacea extract has essential anti-diabetic properties, as well as antiulcer properties.


Assuntos
Antiulcerosos , Glicemia , Diabetes Mellitus Experimental , Hipoglicemiantes , Extratos Vegetais , Ratos Wistar , Úlcera Gástrica , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/isolamento & purificação , Antiulcerosos/farmacologia , Antiulcerosos/isolamento & purificação , Diabetes Mellitus Experimental/tratamento farmacológico , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Úlcera Gástrica/patologia , Úlcera Gástrica/induzido quimicamente , Masculino , Ratos , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Metanol/química , Teste de Tolerância a Glucose , Solventes/química , Fitoterapia
16.
J Sep Sci ; 47(9-10): e2300925, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38726740

RESUMO

Deep eutectic solvents (DESs), as a new type of eco-friendly solvent, have attracted increasing attention on the extraction and separation of flavonoid compounds from various samples, owing to their excellent properties such as biodegradability and ease of handling with very low toxicity. This article provides a status review of the applications of DESs in the extraction of flavonoids, including the introduction of flavonoid compounds, the properties and superiority of DESs, and extraction methods (ultrasonic-assisted extraction, heating reflux extraction, matrix solid-phase dispersion, and solid-phase extraction). Finally, prospects and challenges in the application of DESs on extraction and separation are extensively elucidated and critically reviewed.


Assuntos
Solventes Eutéticos Profundos , Flavonoides , Extração em Fase Sólida , Flavonoides/isolamento & purificação , Flavonoides/química , Solventes Eutéticos Profundos/química , Solventes/química
17.
AAPS PharmSciTech ; 25(5): 93, 2024 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-38693316

RESUMO

Tolterodine tartrate (TOTA) is associated with adverse effect, high hepatic access, varied bioavailability, slight aqueous solubility, and short half-life after oral delivery. Hansen solubility parameters (HSP, HSPiP program), experimental solubility (T = 298.2 to 318.2 K and p = 0.1 MPa), computational (van't Hoff and Apelblat models), and thermodynamic models were used to the select solvent(s). HSPiP predicted PEG400 as the most suitable co-solvent based on HSP values (δd = 17.88, δp = 4.0, and δh = 8.8 of PEG400) and comparable to the drug (δd = 17.6, δp = 2.4, and δh = 4.6 of TOTA). The experimental mole fraction solubility of TOTA was maximum (xe = 0.0852) in PEG400 confirming the best fit of the prediction. The observed highest solubility was attributed to the δp and δh interacting forces. The activity coefficient (ϒi) was found to be increased with temperature. The higher values of r2 (linear regression coefficient) and low RMSD (root mean square deviation) indicated a good correlation between the generated "xe" data for crystalline TOTA and the explored models (modified Apelblat and van't Hoff models). TOTA solubility in "PEG400 + water mixture" was endothermic and entropy-driven. IR (immediate release product) formulation can be tailored using 60% PEG400 in buffer solution for 2 mg of TOTA in 0.25 mL (dosing volume). The isotonic binary solution was associated with a pH of 7.2 suitable for sub-Q delivery. The approach would be a promising alternative with ease of delivery to children and aged patients.


Assuntos
Solubilidade , Solventes , Termodinâmica , Tartarato de Tolterodina , Humanos , Tartarato de Tolterodina/administração & dosagem , Tartarato de Tolterodina/química , Tartarato de Tolterodina/farmacocinética , Solventes/química , Polietilenoglicóis/química , Disponibilidade Biológica , Química Farmacêutica/métodos , Injeções Subcutâneas , Sistemas de Liberação de Medicamentos/métodos
18.
Cryo Letters ; 45(3): 158-167, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38709187

RESUMO

BACKGROUND: Aquaporins (AQPs) are essential proteins that facilitate the rapid movement of water and cryoprotective agents (CPAs) during the cryopreservation process, and ensure the cryo-tolerance of sperm cells. OBJECTIVE: This study evaluated the preservation of aquaporin levels in human sperm after undergoing freezing using natural deep eutectic solvents (NADES) as CPAs for cryoprotection. MATERIALS AND METHODS: From June 2021 to October 2022, 35 semen samples with normal sperm parameters were acquired from the Mehr Infertility Treatment Institute in Rasht, Iran. The samples were divided into several groups for analysis: control group (not frozen), group frozen with SpermFreeze Solution, and groups frozen with different NADESs, including ChS, ChX, ChU, ChG, GlyP, and EtP. After thawing, various aspects for each group were assessed, including the integrity and condensation of sperm chromatin, viability, motility, integrity of acrosome, and the expression of AQP1, AQP3, AQP7, AQP8, and AQP9 genes. RESULTS: The analysis of gene expression revealed that freezing with ChS and GlyP preserved the expression of the AQP1 and AQP3 genes compared to the control group. Regarding AQP7 and AQP8, significant differences were not observed in expression levels between certain NADES groups (e.g., ChS, ChU, and GlyP) and the control group. Additionally, samples frozen with specific NADESs, such as ChS, ChG, EtP, and GlyP, exhibited preserved levels of AQP9 expression when compared to the control group. CONCLUSION: These findings emphasize the importance of NADES in preserving the expression of aquaporins in cryopreserved human sperm and their important fertility parameters. Doi.org/10.54680/fr24310110512.


Assuntos
Aquaporinas , Criopreservação , Crioprotetores , Preservação do Sêmen , Motilidade dos Espermatozoides , Espermatozoides , Humanos , Masculino , Criopreservação/métodos , Aquaporinas/genética , Aquaporinas/metabolismo , Espermatozoides/metabolismo , Espermatozoides/efeitos dos fármacos , Crioprotetores/farmacologia , Motilidade dos Espermatozoides/efeitos dos fármacos , Preservação do Sêmen/métodos , Solventes/química , Adulto , Sobrevivência Celular/efeitos dos fármacos
19.
Luminescence ; 39(5): e4759, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38693721

RESUMO

Colloidal semiconductor quantum dots have many potential optical applications, including quantum dot light-emitting diodes, single-photon sources, or biological luminescent markers. The optical properties of colloidal quantum dots can be affected by their dielectric environment. This study investigated the photoluminescence (PL) decay of thick-shell gradient-alloyed colloidal semiconductor quantum dots as a function of solvent refractive index. These measurements were conducted in a wide range of delay times to account for both the initial spontaneous decay of excitons and the delayed emission of excitons that has the form of a power law. It is shown that whereas the initial spontaneous PL decay is very sensitive to the refractive index of the solvent, the power-law delayed emission of excitons is not. Our results seem to exclude the possibility of carrier self-trapping in the considered solvents and suggest the existence of trap states inside the quantum dots. Finally, our data show that the average exciton lifetime significantly decreases as a function of the solvent refractive index. The change in exciton lifetime is qualitatively modeled and discussed.


Assuntos
Coloides , Luminescência , Pontos Quânticos , Solventes , Pontos Quânticos/química , Solventes/química , Coloides/química , Refratometria , Medições Luminescentes , Semicondutores , Fatores de Tempo
20.
Medicine (Baltimore) ; 103(18): e38039, 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38701291

RESUMO

As a result of increasing drug resistance, crossover resistance development, prolonged therapy, and the absence of different agents with innovative methods for implementation, the efficacy of recent antileishmanial medications is severely declining. So, it is vital to look for other medications from botanical remedies that have antileishmanial activity. The latex of Euphorbia abyssinica (E abyssinica) and the leaves of Clematis simensis fresen (C simensis) were macerated in methanol (80%). In vitro antileishmanial activity of the preparation was tried on promastigotes of Leishmania aethiopica (L aethiopica) and Leishmania donovani (L donovani) using resazurin assay, and fluorescence intensity was measured. One percent of dimethyl sulfoxide (DMSO) and media as negative control and amphotericin B as positive control were used. Additionally, hemolytic & phytochemical tests of the preparation were done. The mean and standard errors of each extract were evaluated and interpreted for statistical significance using one-way analysis of variance. From sigmoidal dose-response curves of % inhibition, half maximal inhibitory concentration (IC50) values were determined by GraphPad Prism and Microsoft Excel; outcomes were presented as mean ±â€…standard error of mean of triplicate trials. P < .05 was statistical significance. The phytochemical screening of C simensis and E abyssinica confirmed the existence of steroids, phenols, tannins, saponins, alkaloids, terpenoids, flavonoids and glycosides. C simensis possesses antileishmanial activity with IC50 outcomes of 46.12 ±â€…0.03 and 8.18 ±â€…0.10 µg/mL on the promastigotes of L aethiopica and L donovani, respectively. However, E abyssinica showed stronger activity with IC50 outcomes of 16.07 ±â€…0.05 µg/mL and 4.82 ±â€…0.07 µg/mL on L aethiopica and L donovani, respectively. C simensis and E abyssinica have a less hemolytic effect on human red blood cells at low concentrations. The outcomes from this investigation demonstrated that the preparation of C simensis and E abyssinica indicated significant antileishmanial activity. Therefore, further in vivo assessment of antileishmanial, cytotoxicity activity and quantitative identification of secondary metabolites are highly recommended.


Assuntos
Antiprotozoários , Euphorbia , Látex , Extratos Vegetais , Folhas de Planta , Extratos Vegetais/farmacologia , Euphorbia/química , Látex/farmacologia , Látex/química , Antiprotozoários/farmacologia , Folhas de Planta/química , Humanos , Leishmania donovani/efeitos dos fármacos , Concentração Inibidora 50 , Leishmania/efeitos dos fármacos , Metanol , Solventes , Hemólise/efeitos dos fármacos
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