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Sugarcane, a globally cultivated crop constituting nearly 80% of total sugar production, yields residues from harvesting and sugar production known for their renewable bioactive compounds with health-promoting properties. Despite previous studies, the intricate interplay of extracts from diverse sugarcane byproducts and their biological attributes remains underexplored. This study focused on extracting the lipid fraction from a blend of selected sugarcane byproducts (straw, bagasse, and filter cake) using ethanol. The resulting extract underwent comprehensive characterization, including physicochemical analysis (FT-IR, DSC, particle size distribution, and color) and chemical composition assessment (GC-MS). The biological properties were evaluated through antihypertensive (ACE), anticholesterolemic (HMG-CoA reductase), and antidiabetic (alpha-glucosidase and Dipeptidyl Peptidase-IV) assays, alongside in vitro biocompatibility assessments in Caco-2 and Hep G2 cells. The phytochemicals identified, such as ß-sitosterol and 1-octacosanol, likely contribute to the extract's antidiabetic, anticholesterolemic, and antihypertensive potential, given their association with various beneficial bioactivities. The extract exhibited substantial antidiabetic effects, inhibiting α-glucosidase (5-60%) and DPP-IV activity (25-100%), anticholesterolemic potential with HMG-CoA reductase inhibition (11.4-63.2%), and antihypertensive properties through ACE inhibition (24.0-27.3%). These findings lay the groundwork for incorporating these ingredients into the development of food supplements or nutraceuticals, offering potential for preventing and managing metabolic syndrome-associated conditions.
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Saccharum , Humanos , Saccharum/metabolismo , Células CACO-2 , Antihipertensivos/farmacología , alfa-Glucosidasas/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Azúcares , Lípidos , Extractos Vegetales/farmacología , Extractos Vegetales/químicaRESUMEN
Biosynthetic gold nanoparticles (bAuNPs) present a promising avenue for enhancing bio-compatibility and offering an economically and environmentally responsible alternative to traditional production methods, achieved through a reduction in the use of hazardous chemicals. While the potential of bAuNPs as anticancer agents has been explored, there is a limited body of research focusing on the crucial physicochemical conditions influencing bAuNP production. In this study, we aim to identify the optimal growth phase of Pseudomonas aeruginosa cultures that maximizes the redox potential and coordinates the formation of bAuNPs with increased efficiency. The investigation employs 2,6-dichlorophenolindophenol (DCIP) as a redox indicator. Simultaneously, we explore the impact of temperature, pH, and incubation duration on the biosynthesis of bAuNPs, with a specific emphasis on their potential application as antitumor agents. Characterization of the resulting bAuNPs is conducted using ATR-FT-IR, TEM, and UV-Vis spectroscopy. To gain insights into the anticancer potential of bAuNPs, an experimental model is employed, utilizing both non-neoplastic (HPEpiC) and neoplastic (PC3) epithelial cell lines. Notably, P. aeruginosa cultures at 9 h/OD600 = 1, combined with biosynthesis at pH 9.0 for 24 h at 58 °C, produce bAuNPs that exhibit smaller, more spherical, and less aggregated characteristics. Crucially, these nanoparticles demonstrate negligible effects on HPEpiC cells while significantly impacting PC3 cells, resulting in reduced viability, migration, and lower IL-6 levels. This research lays the groundwork for the development of more specialized, economical, and ecologically friendly treatment modalities.
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Antineoplásicos , Nanopartículas del Metal , Neoplasias de la Próstata , Humanos , Masculino , Antibacterianos/química , Oro/química , Espectroscopía Infrarroja por Transformada de Fourier , Nanopartículas del Metal/uso terapéutico , Nanopartículas del Metal/química , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Neoplasias de la Próstata/tratamiento farmacológico , Tecnología Química Verde/métodos , Extractos Vegetales/químicaRESUMEN
INTRODUCTION: Studies prove that the use of medicinal plants is a custom carried out by man since ancient times, the evolution of the pharmaceutical industry makes more people consume more natural products. Currently, we can observe that mouthwashes containing natural compounds have shown a growth in demand in the markets and in the professional community. OBJECTIVE: The present study aims to carry out the chemical characterization and microbiological potential of Piper mikanianum (Kunth) Steud essential oil (EOPm), providing data that allows the development of a low-cost mouthwash formulation aimed at vulnerable communities. METHODS: The evaluation of the antibacterial activity and modulator of bacterial resistance was performed by the microdilution method to determine the minimum inhibitory concentration (MIC). The chemical components were characterized by gas chromatography coupled to mass spectrometry, identified 28 constituents, in which Safrole Phenylpropanoid is the major compound, representing 72.6 % of the total composition, followed by α-pinene (10.7 %), Limonene (2 %), ß-caryophyllene (2 %), E-nerolidol (1.9 %), spathulenol (1.3 %) and camphene (1.1 %). RESULTS: The EOPm showed a MIC minimum inhibitory concentration≥1024â µg/mL for all bacterial strains used in the tests. When the EOPm modulating activity combined with chlorhexidine, mouthwash, ampicillin, gentamicin and penicillin G was evaluated against bacterial resistance, the oil showed significant synergistic activity, reducing the MIC of the products tested in combination, in percentage between 20.6 % to 98 .4 %. CONCLUSIONS: We recommend the expansion of tests with greater variation of EOPm concentration combinations and the products used in this study, as well as toxicity evaluation and inâ vivo tests, seeking the development of a possible low-cost mouthwash formulation accessible to the most vulnerable population.
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Aceites Volátiles , Piper , Humanos , Aceites Volátiles/farmacología , Aceites Volátiles/química , Antisépticos Bucales/farmacología , Piper/química , Cromatografía de Gases y Espectrometría de Masas , Antibacterianos/farmacología , Antibacterianos/química , Pruebas de Sensibilidad MicrobianaRESUMEN
To better use the Lecythis pisonis Cambess. biomass, this study investigates whether Sapucaia seed coats present wound healing properties. We analyzed the antibacterial, antioxidant, and wound healing-promoting potentials, plus cytotoxicity and stimulation of vascular endothelial growth factor-A. The chemical composition was analyzed by positive ion mode electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry. A total of 19 compounds were identified, such as proanthocyanidin A1, procyanidins A1, B2, and C1, epigallocatechin, and kaempferol (p-coumaroyl) glycoside. Potent antioxidant strength/index was verified for 2,2-diphenyl-1-picrylhydrazyl radical (IC50 = 0.99 µg/mL) and ferric reducing antioxidant power (IC50 = 1.09 µg/mL). The extract did not present cytotoxicity and promoted significant cell migration and/or proliferation of fibroblasts (p < 0.05). Vascular endothelial growth factor-A was stimulated dose-dependently at 6 µg/mL (167.13 ± 8.30 pg/mL), 12.5 µg/mL (210.3 ± 14.2 pg/mL), and 25 µg/mL (411.6 ± 29.4 pg/mL). Platelet-derived growth factor (PDGF) (0.002 µg/mL) was stimulated at 215.98 pg/mL. Staphylococcus aureus was susceptible to the extract, with a minimum inhibitory concentration of 31.25 µg/mL. The identified compounds benefit the antioxidant activity, promoting hemostasis for the wound healing process, indicating that this extract has the potential for use in dermatological cosmetics.
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Antioxidantes , Polifenoles , Antioxidantes/química , Polifenoles/farmacología , Polifenoles/análisis , Factor A de Crecimiento Endotelial Vascular/análisis , Semillas/química , Cicatrización de Heridas , Extractos Vegetales/químicaRESUMEN
Punica granatum Linn has been known for its nutritional and medicinal value since ancient times and is used in the treatment of various pathologies owing to its antibacterial properties. This review reports the results of the most recent studies on the antibacterial effects of P. granatum and its isolated compounds on bacteria of clinical interest. A search in the PubMed, Scopus, Science Direct, and Science Citation Index Expanded (Web of Science) databases was performed, which included articles that evaluated the antibacterial activity of P. granatum extracts and excluded articles that analyzed other microorganisms or nonpathogenic bacteria, as well as theses, dissertations, duplicate articles, and those not fully available. The literature suggests that P. granatum extracts can act on bacteria, such as methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant S. aureus (MRSA), Streptococcus mutans, Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae. In addition, fruit peel was the most commonly used pharmacogen and methanol, ethanol, and water were the most common solvents for the extraction of bioactive compounds. The antibacterial potential of the methanolic extract of pomegranate peel could be attributed to the presence of active compounds, such as 5-hydroxymethylfurfural, punicic acid, gallic acid, and punicalagin. Thus, there is evidence that these plant extracts, having high polyphenol content, can disrupt the bacterial plasma membrane and inhibit the action of proteins related to antimicrobial resistance. P. granatum shows antibacterial activity against Gram-positive and Gram-negative bacteria, with great potential against multidrug-resistant strains. Further research is needed to clarify the mechanism of action related to this biological activity and investigate the isolated substances that may be responsible for the antibacterial effects.
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Uncaria species are used in traditional medicine and are considered of high therapeutic value and economic importance. This work describes the assembly and annotation of the chloroplast genomes of U. guianensis and U. tomentosa, as well as a comparative analysis. The genomes were sequenced on MiSeq Illumina, assembled with NovoPlasty, and annotated using CHLOROBOX GeSeq. Addictionaly, comparative analysis were performed with six species from NCBI databases and primers were designed in Primer3 for hypervariable regions based on the consensus sequence of 16 species of the Rubiaceae family and validated on an in-silico PCR in OpenPrimeR. The genome size of U. guianensis and U. tomentosa was 155,505 bp and 156,390 bp, respectively. Both Species have 131 genes and GC content of 37.50%. The regions rpl32-ccsA, ycf1, and ndhF-ccsA showed the three highest values of nucleotide diversity within the species of the Rubiaceae family and within the Uncaria genus, these regions were trnH-psbA, psbM-trnY, and rps16-psbK. Our results indicates that the primer of the region ndhA had an amplification success for all species tested and can be promising for usage in the Rubiaceae family. The phylogenetic analysis recovered a congruent topology to APG IV. The gene content and the chloroplast genome structure of the analyzed species are conserved and most of the genes are under negative selection. We provide the cpDNA of Neotropical Uncaria species, an important genomic resource for evolutionary studies of the group.
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Uña de Gato , Genoma del Cloroplasto , Rubiaceae , Uncaria , FilogeniaRESUMEN
This study assessed the effect of zerumbone (ZER) against fluconazole-resistant (CaR) and -susceptible Candida albicans (CaS) biofilms and verified the influence of ZER on extracellular matrix components. Initially, to determine the treatment conditions, the minimum inhibitory concentration (MIC), the minimum fungicidal concentration (MFC) and the survival curve were evaluated. Biofilms were formed for 48 h and exposed to ZER at concentrations of 128 and 256 µg/mL for 5, 10 and 20 min (n = 12). One group of biofilms did not receive the treatment in order to monitor the effects. The biofilms were evaluated to determine the microbial population (CFU/mL), and the extracellular matrix components (water-soluble polysaccharides (WSP), alkali-soluble polysaccharides (ASPs), proteins and extracellular DNA (eDNA), as well as the biomass (total and insoluble) were quantified. The MIC value of ZER for CaS was 256 µg/mL, and for CaR, it was 64 µg/mL. The survival curve and the MFC value coincided for CaS (256 µg/mL) and CaR (128 µg/mL). ZER reduced the cellular viability by 38.51% for CaS and by 36.99% for CaR. ZER at 256 µg/mL also reduced the total biomass (57%), insoluble biomass (45%), WSP (65%), proteins (18%) and eDNA (78%) of CaS biofilms. In addition, a reduction in insoluble biomass (13%), proteins (18%), WSP (65%), ASP (10%) and eDNA (23%) was also observed in the CaR biofilms. ZER was effective against fluconazole-resistant and -susceptible C. albicans biofilms and disturbed the extracellular matrix.
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Objectives: Medicinal plants and herbal medicines are widely used worldwide. However, patients with chronic health conditions or their caregivers do not often disclose these practices to their healthcare providers, leading to potentially severe interactions with current treatments, especially in children. We aimed to describe the prevalence of the use of medicinal plants and herbal medicines by children and adolescents with chronic health conditions and whether their physicians were informed about it. Methods: We conducted a cross-sectional electronic survey on parents and caregivers of children and adolescents with chronic health conditions seen at a university, tertiary-care pediatric outpatient clinic. The common names of the plants cited by respondents were reviewed and Latin names of the species were provided whenever possible. Results: From 20,213 text messages sent in May and June 2021, 521 valid responses were obtained. The prevalence of the use of medicinal plants and herbal medicines was 34.6%, most without a medical prescription (self-medication), and few physicians (4.0%) were aware of it. The five most used species were: Mentha spicata L. (mint), Foeniculum vulgare Mill. (fennel), "cidreira" (a common name possibly corresponding to Cymbopogon citratus (DC.) Stapf, Melissa officinalis L. or Lippia alba (Mill.) N.E. Br. ex Britton & Wilson, P.), Matricaria chamomilla L. (German chamomile), and Plectranthus barbatus Andrews (boldo). Conclusions: The prevalence of the use of medicinal plants and herbal medicines by children and adolescents with chronic health conditions in a tertiary-care outpatient clinic was 34.6%, and only a few physicians were aware of it (AU).
Objetivos: Plantas medicinais e seus derivados são amplamente utilizados no mundo todo. Entretanto, pacientes com condições crônicas de saúde ou seus cuidadores frequentemente não informam essas práticas para seus profissionais de saúde, levando a interações potencialmente graves com os demais tratamentos, especialmente em crianças. Nós objetivamos descrever a prevalência do uso de plantas medicinais e derivados por crianças e adolescentes com condições crônicas de saúde, e se seus médicos foram informados sobre isto. MeÌtodos: Levantamento eletrônico transversal junto a pais e cuidadores de crianças e adolescentes com condições crônicas de saúde atendidos em um serviço ambulatorial pediátrico universitário terciário. Os nomes comuns das plantas citadas pelos participantes foram revisados e os nomes latinos das espécies foram identificados, sempre que possível. Resultados: De 20.213 mensagens de texto enviadas em maio e junho de 2021, 521 respostas válidas foram obtidas. A prevalência de utilização de plantas medicinais e derivados foi de 34,6%, sendo a maioria sem prescrição médica (automedicação), e poucos médicos (4,0%) estavam cientes disto. As cinco plantas mais comumente utilizadas foram: Mentha spicata L. (hortelã), Foeniculum vulgare Mill. (funcho), "cidreira" (possivelmente correspondendo a Cymbopogon citratus (DC.) Stapf, Melissa officinalis L. ou Lippia alba (Mill.) N.E. Br. ex Britton & Wilson, P.), Matricaria chamomilla L. (camomila) e Plectranthus barbatus Andrews (boldo nacional). Conclusões: A prevalência de uso de plantas medicinais e derivados por crianças e adolescentes com condições crônicas de saúde em um serviço ambulatorial pediátrico terciário foi de 34,6%, com grande potencial para interações, e somente poucos médicos estavam cientes disto
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Humanos , Niño , Adolescente , Plantas Medicinales , Enfermedad Crónica/terapia , Medicina de Hierbas , FitoterapiaRESUMEN
Alpha-terpineol is a monoterpene alcohol found in essential oils from medicinal plants with some well-known pharmacological activities and widely used in cosmetics. However, the toxicological effects and additional pharmacological activities need to be clarified. Thus, the study evaluated the toxic, cytotoxic, genotoxic, hemolytic, and oxidative potential of alpha-terpineol in non-clinical bioassays. Different concentrations of alpha-terpineol were used in bioassays, including MTT (50, 100, 200, and 400 µg/mL), Artemia salina (6.25-400 µg/mL), Allium cepa (10, 50, and 100 µg/mL), comet assay (100, 200, and 500 µg/mL), cytokinesis-block micronucleus (100, 250, and 500 µg/mL), confocal microscopy for apoptosis quantification (100 and 500 µg/mL), hemolysis and Saccharomyces cerevisiae central disk test (10, 35, and 75 µg/mL). For the MTT test, alpha-terpineol was more cytotoxic on melanoma murine B16-F10 cells rather than macrophages. For A. salina test, alpha-terpineol showed LC50 of 68.29 and 76.36 µg/mL for 24 h and 48 h of exposure time, respectively. Meanwhile, alpha-terpineol was also cytotoxic to meristematic cells, which revealed inhibition of cellular division and mutagenic action by formation of bridges and delayed anaphases. The compound increased damage index and frequency of damage corroborated by the presence of micronuclei, bridges and nuclear buds at 500 µg/mL, but it caused neither hemolysis, oxidative damage on the S. cerevisiae nor cell death in normal fibroblasts. The findings indicate alpha-terpineol has cytotoxic potential by cytogenetic and molecular mechanisms associated with apoptosis and probable target effects against melanoma cells.
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Large amounts of vine shoots are generated every year during vine pruning. This residue still presents many of the compounds found in the original plant, including low molecular weight phenolic compounds and structural compounds such as cellulose, hemicellulose, and lignin. For wine-producing regions, the challenge is to develop alternatives that will increase the value of this residue. This work proposes the full valorization of vine shoots, focusing on the extraction of lignin by mild acidolysis for the preparation of nanoparticles. The effect of the pretreatment solvents (ethanol/toluene, E/T, and water/ethanol, W/E), on the chemical and structural features of lignin, was evaluated. The chemical analysis suggests similar composition and structure regardless of the pretreatment solvent, although lignin isolated after pretreatment of biomass with E/T showed a higher content of proanthocyanidins (11%) compared with W/E (5%). Lignin nanoparticles (LNPs) presented an average size ranging from 130-200 nm and showed good stability for 30 days. Lignin and LNPs showed excellent antioxidant properties (half maximal inhibitory concentration, IC50 0.016-0.031 mg/mL) when compared to commercial antioxidants. In addition, extracts resulting from biomass pretreatment showed antioxidant activity, with W/E presenting a lower IC50 (0.170 mg/mL) than E/T (0.270 mg/mL), correlated with the higher polyphenol content of W/E, with (+)-catechin and (-)-epicatechin being the main compounds detected. Overall, this work shows that the pre-treatment of vine shoots with green solvents can yield (i) the production of high-purity lignin samples with antioxidant properties and (ii) phenolic-rich extracts, promoting the integral reuse of this byproduct and contributing to sustainability.
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Antioxidantes , Lignina , Lignina/química , Antioxidantes/farmacología , Extractos Vegetales/química , Fenoles/análisis , Etanol , SolventesRESUMEN
Arabinogalactan-proteins (AGPs) are hydroxyproline-rich glycoproteins containing a high sugar content and are widely distributed in the plant kingdom. AGPs have long been suggested to play important roles in sexual plant reproduction. The synthesis of their complex carbohydrates is initiated by a family of hydroxyproline galactosyltransferase (Hyp-GALT) enzymes which add the first galactose to Hyp residues in the protein backbone. Eight Hyp-GALT enzymes have been identified so far, and in the present work a mutant affecting five of these enzymes (galt2galt5galt7galt8galt9) was analyzed regarding the reproductive process. The galt25789 mutant presented a low seed set, and reciprocal crosses indicated a significant female gametophytic contribution to this mutant phenotype. Mutant ovules revealed abnormal callose accumulation inside the embryo sac and integument defects at the micropylar region culminating in defects in pollen tube reception. In addition, immunolocalization and biochemical analyses allowed the detection of a reduction in the amount of glucuronic acid in mutant ovary AGPs. Dramatically low amounts of high-molecular-weight Hyp-O-glycosides obtained following size exclusion chromatography of base-hydrolyzed mutant AGPs compared to the wild type indicated the presence of underglycosylated AGPs in the galt25789 mutant, while the monosaccharide composition of these Hyp-O-glycosides displayed no significant changes compared to the wild-type Hyp-O-glycosides. The present work demonstrates the functional importance of the carbohydrate moieties of AGPs in ovule development and pollen-pistil interactions.
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Arabidopsis , Arabidopsis/genética , Hidroxiprolina/metabolismo , Galactosiltransferasas/genética , Galactosiltransferasas/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Mucoproteínas/genética , Mucoproteínas/metabolismo , Flores/genética , Polen/metabolismo , Glicósidos/metabolismoRESUMEN
The aim of this study was to determine the oxidative/antioxidative effects, modulatory and selective potential of α-tocopherol (vitamin E) on antineoplastic drug-induced toxicogenetic damage. The toxicity, cytotoxicity and genotoxicity induced by antineoplastic agents cyclophosphamide (CPA) and doxorubicin (DOX) was examined utilizing as models Saccharomyces cerevisiae, Allium cepa, Artemia salina and human peripheral blood mononuclear cells (PBMCs) in the presence of α-tocopherol. For these tests, concentrations of α- tocopherol 100 IU/ml (67mg/ml), CPA 20 µg/ml, DOX 2 µg/ml were used. The selectivity of α-tocopherol was assessed by the MTT test using human mammary gland non-tumor (MCF10A) and tumor (MCF-7) cell lines. Data showed cytoplasmic and mitochondrial oxidative damage induced by CPA or DOX was significantly diminished by α-tocopherol in S. cerevisiae. In addition, the toxic effects on A. salina and cytotoxic and mutagenic effects on A. cepa were significantly reduced by α-tocopherol. In PBMCs, α-tocopherol alone did not markedly affect these cells, and when treated in conjunction with CPA or DOX, α-tocopherol reduced the toxicogenetic effects noted after antineoplastic drug administration as evidenced by decreased chromosomal alterations and lowered cell death rate. In human mammary gland non-tumor and tumor cell lines, α-tocopherol produced selective cytotoxicity with 2-fold higher effect in tumor cells. Evidence indicates that vitamin E (1) produced anti-cytotoxic and anti-mutagenic effects against CPA and DOX (2) increased higher selectivity toward tumor cells, and (3) presented chemoprotective activity in PBMCs.
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Antineoplásicos , alfa-Tocoferol , Humanos , alfa-Tocoferol/farmacología , Saccharomyces cerevisiae , Leucocitos Mononucleares , Antineoplásicos/toxicidad , Antineoplásicos/uso terapéutico , Doxorrubicina/toxicidad , Ciclofosfamida/toxicidad , Vitamina ERESUMEN
Clinical auditory alarms are often found in hospital wards and operating rooms. In these environments, regular daily tasks can result in having a multitude of concurrent sounds (from staff and patients, building systems, carts, cleaning devices, and importantly, patient monitoring devices) which easily amount to a prevalent cacophony. The negative impact of this soundscape on staff and patients' health and well-being, as well as in their performance, demand for accordingly designed sound alarms. The recently updated IEC60601-1-8 standard, in guidance for medical equipment auditory alarms, proposed a set of pointers to distinctly convey medium or high levels of priority (urgency). However, conveying priority without compromising other features, such as ease of learnability and detectability, is an ongoing challenge. Electroencephalography, a non-invasive technique for measuring the brain response to a given stimulus, suggests that certain Event-Related Potentials (ERPs) components such as the Mismatch Negativity (MMN) and P3a may be the key to uncovering how sounds are processed at the pre-attentional level and how they may capture our attention. In this study, the brain dynamics in response to the priority pulses of the updated IEC60601-1-8 standard was studied via ERPs (MMN and P3a), for a soundscape characterised by the repetition of a sound (generic SpO2 "beep"), usually present in operating and recovery rooms. Additional behavioural experiments assessed the behavioural response to these priority pulses. Results showed that the Medium Priority pulse elicits a larger MMN and P3a peak amplitude when compared to the High Priority pulse. This suggests that, at least for the applied soundscape, the Medium Priority pulse is more easily detected and attended at the neural level. Behavioural data supports this indication, showing significantly shorter reaction times for the Medium Priority pulse. The results pose the possibility that priority pointers of the updated IEC60601-1-8 standard may not be successfully conveying their intended priority levels, which may not only be due to design properties but also to the soundscape in which these clinical alarms are deployed. This study highlights the need for intervention in both hospital soundscapes and auditory alarm design settings.
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Alarmas Clínicas , Humanos , Potenciales Evocados/fisiología , Atención/fisiología , Electroencefalografía/métodos , Tiempo de Reacción/fisiología , Potenciales Evocados Auditivos/fisiología , Estimulación Acústica , Percepción Auditiva/fisiologíaRESUMEN
Obesity is associated with complex adipose tissue energy metabolism remodeling. Whether AT metabolic reprogramming differs according to body mass index (BMI) and across different obesity classes is unknown. This study's purpose was to evaluate and compare bioenergetics and energy substrate preference of visceral adipose tissue (VAT) pertaining to individuals with obesity class 2 and class 3. VAT obtained from patients with obesity (n = 15) class 2 (n = 7; BMI 37.53 ± 0.58 kg/m2) or class 3 (n = 8; BMI 47.79 ± 1.52 kg/m2) was used to assess oxygen consumption rate (OCR) bioenergetics and mitochondrial substrate preferences. VAT of patients with obesity class 3 presented significantly higher non-mitochondrial oxygen consumption (p < 0.05). In VAT of patients with obesity class 2, inhibition of pyruvate and glutamine metabolism significantly decreased maximal respiration and spare respiratory capacity (p < 0.05), while pyruvate and fatty acid metabolism inhibition, which renders glutamine the only available substrate, increased the proton leak with a protective role against oxidative stress (p < 0.05). In conclusion, VAT bioenergetics of patients with obesity class 2 depicts a greater dependence on glucose/pyruvate and glutamine metabolism, suggesting that patients within this BMI range are more likely to be responsive to interventions based on energetic substrate modulation for obesity treatment.
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Glutamina , Grasa Intraabdominal , Humanos , Glutamina/metabolismo , Grasa Intraabdominal/metabolismo , Obesidad/metabolismo , Metabolismo Energético , Piruvatos/metabolismo , Tejido Adiposo/metabolismoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Stachytarpheta cayennensis (Verbenaceae) has been used in Brazilian traditional medicine to treat asthma and other respiratory diseases. AIMS OF THE STUDY: To investigate the effects of different doses of standardized hydro-ethanolic (SCH) and aqueous (SCA) extracts of aerial parts of S. cayennensis using a murine ovalbumin (OVA)-induced asthma model. MATERIALS AND METHODS: The major constituents of the plant extracts were identified and standardized by ultra-performance liquid chromatography coupled with mass spectrometry. Balb/c mice were challenged with OVA solution and treated concomitantly by intraperitoneal injection of standardized SCH or SCA extracts at 50, 100, and 200 mg/kg concentrations. OVA-challenged control animals were treated with either dexamethasone (OVA-DEX) or saline solution (OVA-SAL). After challenge, we assessed in vivo bronchial hyperresponsiveness, airway inflammation (number of cells), peribronchial inflammation (histological analysis) and production of OVA-specific IgE and interleukin (IL)-4, IL-5, and IL-13 (ELISA). RESULTS: Acteoside, isoacteoside, and ipolamiide were the major constituents of SCH and SCA. The respective concentrations of acteoside in SCH and SCA were 78 and 98 µg/mL, while those of ipolamiide were 30 and 19 µg/mL. Treatment with 200 mg/kg of SCH or SCA decreased IL-4, IL-5, and IL-13 in lung homogenates. These reductions were accompanied by a lower influx of inflammatory cells (eosinophils, lymphocytes, and macrophages) to the airways and lungs. In addition to the anti-inflammatory effects, administration of SCA, but not SCH, ameliorated the parameters of bronchial hyperresponsiveness and decreased levels of circulating OVA-specific IgE. CONCLUSION: The results presented herein demonstrate for the first time the anti-asthmatic activity of S. cayennensis extracts in a murine model, thereby supporting the ethnopharmacological uses of the plant.
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Antiasmáticos , Hiperreactividad Bronquial , Verbenaceae , Ratones , Animales , Antiasmáticos/efectos adversos , Interleucina-13 , Modelos Animales de Enfermedad , Interleucina-5 , Líquido del Lavado Bronquioalveolar , Hiperreactividad Bronquial/tratamiento farmacológico , Ovalbúmina/farmacología , Ratones Endogámicos BALB C , Pulmón , Inmunoglobulina E , Inflamación/tratamiento farmacológico , Citocinas/farmacologíaRESUMEN
BACKGROUND: Compounds from vegetal matter have therapeutic potential to control highly prevalent microorganisms that are resistant to commonly used antimicrobial drugs. Dynamization of compounds can either maintain or improve their therapeutic effects, and make their use safer, especially those compounds whose therapeutic dose is close to the toxic limit. Aloysia polystachya (Griseb.) stands out among aromatic plants with antimicrobial potential. OBJECTIVE: The aim of this study was to evaluate the antimicrobial activity of dynamized and crude forms of A. polystachya essential oil against Candida albicans, Escherichia coli and Staphylococcus aureus. METHODS: Essential oil was extracted from A. polystachya dry leaves, solubilized, and dynamized at 1 cH potency as recommended by the Brazilian Homeopathic Pharmacopoeia. Antimicrobial activity against C. albicans, E. coli and S. aureus of the samples was assayed using the plate microdilution method. RESULTS: Dynamized A. polystachya essential oil at the concentration of 1 µg/mL inhibited the growth of all the microbial species analyzed. The minimum inhibitory concentration of dynamized essential oil was smaller than crude essential oil for S. aureus, E. coli and C. albicans. CONCLUSION: It is reported for the first time that A. polystachya dynamized essential oil can effectively suppress microbial growth, and it is a promising adjuvant to treat infections with pathogenic S. aureus, E. coli and C. albicans.
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Antiinfecciosos , Homeopatía , Aceites Volátiles , Aceites Volátiles/farmacología , Escherichia coli , Staphylococcus aureus , Antiinfecciosos/farmacología , Candida albicans , Pruebas de Sensibilidad MicrobianaRESUMEN
Abstract Bauhinia forficata Link aqueous extract is usually recommended as a phytomedicine to reduce blood glucose levels and its biological activity has been linked to the presence of phenolic compounds from B. forficata preparations. Several drying processes are used in the production of dry herbal extracts, which may influence the chemical composition and efficacy of final herbal medicines. Due to significant chemical changes, defining appropriate drying processes is essential for phytopharmaceutical drug development. In view of this, we analyzed dried B. forficata leaf infusion (BFLI) extracts by HPLC-UV-MSn, followed by molecular networking analysis to evaluate the chemical profiles from dried extracts yielded by freeze-and spray-drying processes. The main metabolites detected included 11 ferulic/isoferulic acid derivatives and 13 glycosylated flavonoids. The qualitative chemical profiles were alike for both drying processes, whereas the relative abundance of some flavonoids was higher using spray-drying. Taken together, our results showed that freeze-and spray-drying preserved the phenolic profile of BFLI and suggested that spray-drying may be the most suitable to obtain its dried products. Along with studying the chemical profiles of dried herbal extracts, evaluating the influence of drying processes on the quality and chemical profiles of final products is pivotal and may benefit future research.
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Hojas de la Planta/clasificación , Bauhinia/efectos adversos , Compuestos Fenólicos , Fabaceae/clasificación , Flavonoides/agonistas , Cromatografía Líquida de Alta Presión/métodos , Gestión de la Calidad Total/organización & administración , Medicina de Hierbas/tendencias , Desarrollo de Medicamentos/instrumentaciónRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Hancornia speciosa Gomes (Apocynaceae) is a tree found in the Brazilian savannah, traditionally used to treat several diseases, including diabetes and hypertension. The anti-hypertensive activity of H. speciosa leaves (HSL) has been demonstrated in different models and is credited to the vasodilator effect and ACE (angiotensin-converting enzyme) inhibition. The hypoglycemic effect of HSL has been also reported. AIM OF THE STUDY: To establish correlations between the biological activities elicited by H. speciosa extracts and the contents of their major compounds, aiming to define chemical markers related to the potential antihypertensive and antidiabetic effects of the species. Additionally, it aimed to isolate and characterize the chemical structure of a marker related to the α-glucosidase inhibitory effect. MATERIALS AND METHODS: Extracts of a single batch of H. speciosa leaves were prepared by extraction with distinct solvents (ethanol/water in different proportions; methanol/ethyl acetate), employing percolation or static maceration as extraction techniques, at different time intervals. The contents of chlorogenic acid, rutin and FlavHS (a tri-O-glycoside of quercetin) were quantified by a developed and validated HPLC-PDA method. Bornesitol was determined by HPLC-PDA after derivatization with tosyl chloride, whereas total flavonoids were measured spectrophotometrically. Identification of other constituents in the extracts was performed by UPLC-DAD-ESI-MS/MS analysis. The vasorelaxant activity was assayed in rat aortic rings precontracted with phenylephrine, and α-glucosidase inhibition was tested in vitro. Principal component analysis (PCA) was employed to evaluate the contribution of each marker to the biological responses. Isolation of compound 1 was carried out by column chromatography and structure characterization was accomplished by NMR and UPLC-DAD-ESI-MS/MS analyses. RESULTS: The contents of the chemical markers (mean ± s.d. % w/w) varied significantly among the extracts, including total flavonoids (2.68 ± 0.14 to 5.28 ± 0.29), bornesitol (5.11 ± 0.26 to 7.75 ± 0.78), rutin (1.46 ± 0.06 to 1.97 ± 0.02), FlavHS (0.72 ± 0.05 to 0.94 ± 0.14) and chlorogenic acid (0.67 ± 0.09 to 0.91 ± 0.02). All extracts elicited vasorelaxant effect (pIC50 between 4.97 ± 0.22 to 6.48 ± 0.10) and α-glucosidase inhibition (pIC50 between 3.49 ± 0.21 to 4.03 ± 0.10). PCA disclosed positive correlations between the vasorelaxant effect and the contents of chlorogenic acid, rutin, total flavonoids, and FlavHS, whereas a negative correlation was found with bornesitol concentration. No significant correlation between α-glucosidase inhibition and the contents of the above-mentioned compounds was found. On the other hand, PCA carried out with the areas of the ten major peaks from the chromatograms disclosed positive correlations between a peak ascribed to co-eluted triterpenes and α-glucosidase inhibition. A triterpene was isolated and identified as 3-O-ß-(3'-R-hydroxy)-hexadecanoil-lupeol. CONCLUSION: According to PCA results, the vasorelaxant activity of H. speciosa extracts is related to flavonoids and chlorogenic acid, whereas the α-glucosidase inhibition is associated with lipophilic compounds, including esters of lupeol like 3-O-ß-(3'-R-hydroxy)-hexadecanoil-lupeol, described for the first time for the species. These compounds can be selected as chemical markers for the quality control of H. speciosa plant drug and derived extracts.
Asunto(s)
Apocynaceae , Inhibidores de Glicósido Hidrolasas , Extractos Vegetales , Angiotensinas/análisis , Animales , Antihipertensivos/análisis , Apocynaceae/química , Quimiometría , Ácido Clorogénico , Etanol , Flavonoides/análisis , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Glicósidos/análisis , Hipoglucemiantes/análisis , Hipoglucemiantes/farmacología , Metanol , Triterpenos Pentacíclicos , Fenilefrina , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Quercetina/análisis , Ratas , Rutina/farmacología , Solventes , Espectrometría de Masas en Tándem , Vasodilatadores/química , Vasodilatadores/farmacología , alfa-GlucosidasasRESUMEN
BACKGROUND: Pyrostegia venusta (Ker Gawl.) Miers occurs in threatened biodiversity hotspots of Cerrado and Atlantic forest biomes in Brazil and is used in traditional medicine to treat various respiratory and skin diseases. METHODS AND RESULTS: This study (i) examined the genetic diversity and structure of six natural populations of P. venusta from different Brazilian regions using sequence-related amplified polymorphism (SRAP) markers; and (ii) compared the intra- and inter-populational levels of the bioactive component verbascoside using high-performance liquid chromatography. The population from Nova Mutum, Mato Grosso, presented the highest genetic variability (Nei index H = 0.2759; Shannon index I = 0.4170; 85.14% polymorphic loci), whereas the population from Araxá, Minas Gerais, presented the lowest genetic variability (H = 0.1811; I = 0.2820; 70.27% polymorphic loci). The intra-populational variability (79%) was significantly higher (p = 0.001) than the inter-populational variability (21%). The populations were clustered into two groups but their genetic differentiation was not associated with geographical origin (Mantel test, r = 0.328; p > 0.05). The verbascoside content significantly differed (p > 0.05) among the six populations and between the individuals from each population. The highest verbascoside levels (> 200 µg/mg extract) were detected in populations from Araxá and Serrana, while the lowest verbacoside levels were detected in populations from Paranaíta and Sinop. CONCLUSIONS: This is the first report on the use of SRAP markers to analyze genetic variability in the family Bignoniaceae. Our findings shall help to better understand the genetic and chemical diversity of P. venusta populations, as well as provide useful information to select the most appropriate individuals to prepare phytomedicines.
Asunto(s)
Bignoniaceae , Bignoniaceae/química , Bignoniaceae/genética , Variación Genética , Glucósidos , Fenoles , PolifenolesRESUMEN
Collaborative models (CM) focused on intrapartum care shared between both midwives and obstetricians have been proposed as a strategy to reduce these rates. Our aim was to compare use of evidence-based practices, obstetric interventions and c-section rates in two settings: a maternity hospital that applies a CM of care (MRJ) and data from a pool of maternity hospitals included in the Birth in Brazil Survey (NB) that do not adopt a CM. Data was abstracted from medical and administrative records in MRJ and from medical records and face-to-face interviews in NB. Differences were compared using chi-square test, with significance level set at p<0.05. MRJ showed a higher frequency of labour companionship, labour care provided by nurse midwives, non-pharmacological pain relief methods, food intake during labour, and less use of oxytocin, analgesia and amniotomy. More women also had second stage assisted by a nurse midwife and in a vertical position, as well as lower use of episiotomies and vacuum-extractor/forceps. The c-section rate was lower at MRJ. Shared care between midwives and obstetricians can be an effective strategy to improve quality of intrapartum care.