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Pyridine, a compound with a heterocyclic structure, is a key player in medicinal chemistry and drug design. It is widely used as a framework for the design of biologically active molecules and is the second most common heterocycle in FDA-approved drugs. Pyridine is known for its diverse biological activity, including antituberculosis, antitumor, anticoagulant, antiviral, antimalarial, antileishmania, anti-inflammatory, anti-Alzheimer's, antitrypanosomal, antimalarial, vasodilatory, antioxidant, antimicrobial, and antiproliferative effects. This review, spanning from 2022 to 2012, involved the meticulous identification of pyridine derivatives with antiproliferative activity, as indicated by their minimum inhibitory concentration values (IC50) against various cancerous cell lines. The aim was to determine the most favorable structural characteristics for their antiproliferative activity. Using computer programs, we constructed and calculated the molecular descriptors and analyzed the electrostatic potential maps of the selected pyridine derivatives. The study found that the presence and positions of the -OMe, -OH, -C=O, and NH2 groups in the pyridine derivatives enhanced their antiproliferative activity over the cancerous cellular lines studied. Conversely, pyridine derivatives with halogen atoms or bulky groups in their structures exhibited lower antiproliferative activity.
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Antineoplásicos , Proliferación Celular , Piridinas , Piridinas/química , Piridinas/farmacología , Humanos , Proliferación Celular/efectos de los fármacos , Antineoplásicos/farmacología , Antineoplásicos/química , Relación Estructura-Actividad , Línea Celular TumoralRESUMEN
Uropathogenic Escherichia coli (UPEC) is the main cause of urinary tract infections (UTIs) and carries virulence and resistance factors often found in mobilizable genetic elements, such as plasmids or pathogenicity islands (PAIs). UPEC is part of the extraintestinal pathogenic E. coli (ExPEC), but hybrid strains possessing both diarrheagenic E. coli (DEC) and ExPEC traits, termed "hypervirulent", present a significant health threat. This study assessed the prevalence of UPEC PAIs, ExPEC sequence types (ST), DEC genes, carbapenemase and extended-spectrum ß-lactamase (ESBL) phenotypes, resistance genotypes, and plasmids in 40 clinical isolates of UPEC. Results showed that 72.5% of isolates had PAIs, mainly PAI IV536 (53%). ESBL phenotypes were found in 65% of ß-lactam-resistant isolates, with 100% of carbapenem-resistant isolates producing carbapenemase. The predominant ESBL gene was blaCTX-M-2 (60%), and the most common resistance gene in fluoroquinolone and aminoglycoside-resistant isolates was aac(6')Ib (93%). Plasmids were present in 57% of isolates, and 70% belonged to the ST131 clonal group. Molecular markers for DEC pathotypes were detected in 20 isolates, with 60% classified as hybrid pathotypes. These findings indicate significant pathogenic potential and the presence of hybrid pathotypes in E. coli UTI clinical isolates in the Mexican population.
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Introduction. Leclercia adecarboxylata is a member of Enterobacterales, often considered an opportunistic pathogen. Recent reports have highlighted L. adecarboxylata as an emerging pathogen harbouring virulence and resistance determinants.Gap statement. Little information exists on virulence and resistance determinants in L. adecarboxylata strains isolated from environmental, food, and clinical samples.Aim. To determine the presence of resistance and virulence determinants and plasmid features in L. adecarboxylata strains isolated from environmental, food, and clinical samples, as well as their phylogenetic relationship.Results. All strains tested showed resistance to ß-lactams and quinolones but were sensitive to aminoglycosides and nitrofurans. However, even though fosfomycin resistance is considered a characteristic trait of L. adecarboxylata, the resistance phenotype was only observed in 50â% of the strains; bla TEM was the most prevalent BLEE gene (70â%), while the quinolone qnrB gene was observed in 60â% of the strains. Virulence genes were differentially observed in the strains, with adhesion-related genes being the most abundant, followed by toxin genes. Finally, all strains carried one to seven plasmid bands ranging from 7 to 125 kbps and harboured several plasmid addiction systems, such as ParDE, VagCD, and CcdAB in 80â% of the strains.Conclusions. L. adecarboxylata is an important emerging pathogen that may harbour resistance and virulence genes. Additionally, it has mobilizable genetic elements that may contribute to the dissemination of genetic determinants to other bacterial genera.
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Antibacterianos , Enterobacteriaceae , Pruebas de Sensibilidad Microbiana , Filogenia , Plásmidos , Factores de Virulencia , Antibacterianos/farmacología , Plásmidos/genética , Virulencia/genética , Enterobacteriaceae/genética , Enterobacteriaceae/efectos de los fármacos , Enterobacteriaceae/patogenicidad , Enterobacteriaceae/aislamiento & purificación , Enterobacteriaceae/clasificación , Factores de Virulencia/genética , Humanos , Infecciones por Enterobacteriaceae/microbiología , Fenotipo , Farmacorresistencia Bacteriana/genética , Quinolonas/farmacología , beta-Lactamas/farmacología , Farmacorresistencia Bacteriana Múltiple/genética , Microbiología de AlimentosRESUMEN
Kodamaea ohmeri is an environmental yeast considered a rare emerging pathogen. In clinical settings, the correct identification of this yeast is relevant because some isolates are associated with resistance to antifungals. There is a lack of available data regarding the geographical distribution, virulence, and drug resistance profile of K. ohmeri. To contribute to the knowledge of this yeast, this study aimed to describe in depth three isolates of K. ohmeri associated with fungemia in Honduras. The identification of the isolates was carried out by sequencing the ribosomal ITS region. In addition, the susceptibility profile to antifungals was determined, and some properties associated with virulence were evaluated (exoenzyme production, biofilm formation, cell adhesion, and invasion). The isolates showed strong protease, phospholipase, and hemolysin activity, in addition to being biofilm producers. Adherence and invasion capacity were evident in the HeLa and Raw 264.7 cell lines, respectively. This study expands the understanding of the underlying biological traits associated with virulence in K. ohmeri, and it is the first report of the detection and identification of K. ohmeri in Honduras as a cause of human infection.
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Urinary tract infections are commonly caused by uropathogenic Escherichia coli (UPEC), which usually presents multiple virulence and resistance mechanisms, making it difficult to treat. It has been demonstrated that silver and polymeric nanoparticles had potential against these pathogens. In this study, we synthesized thiol chitosan-coated silver nanoparticles (SH-Cs-AgNPs) and evaluated their antibacterial, antibiofilm and antiadherence activity against clinical isolates of UPEC. The SH-Cs-AgNPs showed a spherical shape with a size of 17.80 ± 2.67 nm and zeta potential of 18 ± 2 mV. We observed a potent antibacterial and antibiofilm activity as low as 12.5 µg/mL, as well as a reduction in the adherence of UPEC to mammalian cells at concentrations of 1.06 and 0.53 µg/mL. These findings demonstrate that SH-Cs-AgNPs have potential as a new therapeutic compound against infections caused by UPEC.
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Quitosano , Nanopartículas del Metal , Escherichia coli Uropatógena , Animales , Plata/farmacología , Quitosano/farmacología , Antibacterianos/farmacología , Biopelículas , MamíferosRESUMEN
Biological properties of Sonoran propolis (SP) are influenced by harvest time. Caborca propolis showed cellular protective capacity against reactive oxygen species, which might be implicated in anti-inflammatory effects. However, the anti-inflammatory activity of SP has not been investigated so far. This study investigated the anti-inflammatory activity of previously characterized seasonal SP extracts (SPE) and some of their main constituents (SPC). The anti-inflammatory activity of SPE and SPC was evaluated by measuring nitric oxide (NO) production, protein denaturation inhibition, heat-induced hemolysis inhibition, and hypotonicity-induced hemolysis inhibition. SPE from spring, autumn, and winter showed a higher cytotoxic effect on RAW 264.7 cells (IC50: 26.6 to 30.2 µg/mL) compared with summer extract (IC50: 49.4 µg/mL). SPE from spring reduced the NO secretion to basal levels at the lowest concentration tested (5 µg/mL). SPE inhibited the protein denaturation by 79% to 100%, and autumn showed the highest inhibitory activity. SPE stabilized erythrocyte membrane against heat-induced and hypotonicity-induced hemolysis in a concentration-dependent manner. Results indicate that the flavonoids chrysin, galangin, and pinocembrin could contribute to the anti-inflammatory activity of SPE and that the harvest time influences such a property. This study presents evidence of SPE pharmacological potential and some of their constituents.
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Própolis , Humanos , Própolis/farmacología , Hemólisis , Estaciones del Año , Óxido Nítrico , Antiinflamatorios/farmacologíaRESUMEN
This investigation aimed to determine the effect of high-power ultrasonic pulses on the antioxidant, antibacterial, and antiproliferative activity of sorghum (Sorghum bicolor) lignin. A lignin yield of 7.35% was obtained using the organosolv method. Additionally, the best conditions of the ultrasonic pulses were optimized to obtain a more significant increase in antioxidant capacity, resulting in 10 min for all treatments, with amplitudes of 20% for DPPH and FRAP, 18% for ABTS, and 14% for total phenols. The effect of ultrasonic pulses was mainly observed with FRAP (1694.88 µmol TE/g), indicating that the main antioxidant mechanism of lignin is through electron transport. Sorghum lignin with and without ultrasonic pulses showed high percentages of hemolysis inhibition (>80%) at concentrations of 0.003 to 0.33 mg/mL. The AB blood group and, in general, all Rh- groups are the most susceptible to hemolysis. Lignin showed high anti-inflammatory potential due to heat and hypotonicity (>82%). A higher antimicrobial activity of lignin on Escherichia coli bacteria was observed. The lignins evaluated without sonication and sonication presented higher activity in the cell line PC-3. No effect was observed on the lignin structure with the FT-IR technique between sonication and non-sonication; however, the organosolv method helped extract pure lignin according to HPLC.
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BACKGROUND: Urinary tract infections (UTI) are one of the most common pathologies in Mexico and the majority are caused by uropathogenic Escherichia coli (UPEC). UPEC possesses virulence and resistance determinants that promote UTI development and affect diagnosis and treatment. This study aims to systematically review published reports of virulence genes, antibiotic resistance, and phylogenetic groups prevalent in clinical isolates of UPEC in the Mexican population. METHODS: Systematic review with meta-analysis was performed following PRISMA guidelines. Articles in both English and Spanish were included. Total prevalence with a 95% confidence interval of each characteristic was calculated. Heterogeneity between studies and geographical areas was assessed by the Cochran Q test (Q), I-square (I2), and H-square (H2). Egger's test was used for risk of bias in publications and asymmetry evaluations. RESULTS: Forty-two articles were analyzed. The most prevalent virulence genes were ecp (97.25%; n = 364) and fimH (82.34%; n = 1,422), which are associated with lower UTI, followed by papGII (40.98%; n = 810), fliC (38.87%; n = 319), hlyA (23.55%; n = 1,521), responsible for with upper UTI. More than 78.13% (n = 1,893) of the isolates were classified as multidrug-resistant, with a higher prevalence of resistance to those antibiotics that are implemented in the basic regimen in Mexico. The most frequently reported Extended Spectrum ß-Lactamase (ESBL) was CTX-M-1 (55.61%; n = 392), and the predominant phylogroup was B2 (35.94%; n = 1,725). CONCLUSION: UPEC strains are responsible for a large portion of both lower and upper UTI in Mexico, and their multi-drug resistance drastically reduces the number of therapeutic options available.
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Infecciones por Escherichia coli , Infecciones Urinarias , Escherichia coli Uropatógena , Humanos , Virulencia/genética , Escherichia coli Uropatógena/genética , Infecciones por Escherichia coli/tratamiento farmacológico , Infecciones por Escherichia coli/epidemiología , Factores de Virulencia/genética , Factores de Virulencia/uso terapéutico , México/epidemiología , Filogenia , Antibacterianos/uso terapéutico , Infecciones Urinarias/tratamiento farmacológico , Infecciones Urinarias/epidemiologíaRESUMEN
Multi-drug resistant (MDR) bacteria have gained importance as a health problem worldwide, and novel antibacterial agents are needed to combat them. Silver nanoparticles (AgNPs) have been studied as a potent antimicrobial agent, capable of countering MDR bacteria; nevertheless, their conventional synthesis methods can produce cytotoxicity and environmental hazards. Biosynthesis of silver nanoparticles has emerged as an alternative to reduce the cytotoxic and environmental problems derived from their chemical synthesis, using natural products as a reducing and stabilizing agent. Sonoran Desert propolis (SP) is a poplar-type propolis rich in polyphenolic compounds with remarkable biological activities, such as being antioxidant, antiproliferative, and antimicrobial, and is a suitable candidate for synthesis of AgNPs. In this study, we synthesized AgNPs using SP methanolic extract (SP-AgNPs) and evaluated the reduction capacity of their seasonal samples and main chemical constituents. Their cytotoxicity against mammalian cell lines and antibacterial activity against multi-drug resistant bacteria were assessed. Quercetin and galangin showed the best-reduction capacity for synthesizing AgNPs, as well as the seasonal sample from winter (SPw-AgNPs). The SPw-AgNPs had a mean size of around 16.5 ± 5.3 nm, were stable in different culture media, and the presence of propolis constituents was confirmed by FT-IR and HPLC assays. The SPw-AgNPs were non-cytotoxic to ARPE-19 and HeLa cell lines and presented remarkable antibacterial and antibiofilm activity against multi-drug resistant clinical isolates, with E. coli 34 and ATCC 25922 being the most susceptible (MBC = 25 µg/mL), followed by E. coli 2, 29, 37 and PNG (MBC = 50 µg/mL), and finally E. coli 37 and S. aureus ATCC 25923 (MBC = 100 µg/mL). These results demonstrated the efficacy of SP as a reducing and stabilizing agent for synthesis of AgNPs and their capacity as an antibacterial agent.
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Escherichia coli is a well-recognized inhabitant of the animal and human gut. Its presence represents an essential component of the microbiome. There are six pathogenic variants of E. coli associated with diarrheal processes, known as pathotypes. These harbor genetic determinants that allow them to be classified as such. In this work, we report the presence of diarrheagenic pathotypes of E. coli strains isolated from healthy donors. Ninety E. coli strains were analyzed, of which forty-six (51%) harbored virulence markers specifics for diarrheagenic pathotypes, including four hybrids (one of them with genetic determinants of three DEC pathotypes). We also identified phylogenetic groups with a higher prevalence of B2 (45.6%) and A (17.8%). In addition, resistance to sulfonamides (100%), and aminoglycosides (100%) was found in 100% of the strains, with a lower prevalence of resistance to cefotaxime (13.3%), ceftriaxone (12.2%), fosfomycin (10%), and meropenem (0%). All analyzed strains were classified as multidrug resistant. Virulence genes were also investigated, which led us to propose three new virotypes. Among the virulence traits observed, the ability to form biofilms stands out, which was superior to that of the E. coli and Staphylococcus aureus strains used as positive controls.
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Sonoran propolis (SP) exerts remarkable biological activities attributed to its polyphenolic composition, mostly described as poplar-type flavonoids. It is known that polyphenols present low bioavailability derived of their molecular weight, glycosylation level, metabolic conversion, as well as interaction with the intestinal microbiota, affording limitations for possible in vivo applications. The aim of this work was to synthesize Poly-(lactide-co-glycolide) acid (PLGA) nanoparticles for encapsulation of SP, as a matrix to increase solubility of their polyphenolic compounds and improve delivery, for the evaluation of its antiproliferative activity on cancer cells. The Sonoran propolis-loaded PLGA nanoparticles (SP-PLGA NPs) were synthesized (by nanoprecipitation), and their physicochemical parameters were determined (size, morphology, zeta potential, stability, and drug release). Additionally, the antiproliferative activity of SP-PLGA nanoparticles was evaluated in vitro against murine (M12.C3.F6) and human (HeLa) cancer cell lines, including a non-cancer human cell line (ARPE-19) as control. SP-PLGA NPs presented a mean size of 152.6 ± 7.1 nm with an average negative charge of - 21.2 ± 0.7 mV. The encapsulation yield of SP into PLGA system was approximately 68.2 ± 6.0% with an in vitro release of 45% of propolis content at 48 h. SP-PLGA NPs presented antiproliferative activity against both cancer cell lines tested, with lower IC50 values in M12.C3.F6 and HeLa cell lines (7.8 ± 0.4 and 3.8 ± 0.4 µg/mL, respectively) compared to SP (24.0 ± 4.3 and 7.4 ± 0.4 µg/mL, respectively). In contrast, the IC50 of SP-PLGA NPs and SP against ARPE-19 was higher than 50 µg/mL. Cancer cells treated with SP and SP-PLGA NPs presented morphological features characteristic of apoptosis (cellular shrinkage and membrane blebs), as well as elongated cells, effect previously reported for SP, meanwhile, no morphological changes were observed with ARPE-19 cells. The obtained delivery system demonstrates appropriate encapsulation characteristics and antiproliferative activity to be used in the field of nanomedicine, therefore SP could be potentially used in antitumoral in vivo assays upon its encapsulation into PLGA nanoparticles.
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Nanopartículas , Neoplasias , Própolis , Animales , Portadores de Fármacos/química , Liberación de Fármacos , Células HeLa , Humanos , Ratones , Nanomedicina , Nanopartículas/química , Própolis/químicaRESUMEN
Argentina has the second highest mortality rate for breast cancer (BC) in South America. The age-standardized incidence of BC in Argentina is 73 per 100,000. Despite the availability of early detection services, 30% of BCs are diagnosed at advanced disease stages. The National Cancer Institute (NCI) of Argentina and the National Program for Control of Breast Cancer (NPCBC) focus on two main objectives: guaranteeing adequate and timely BC treatment and reducing BC mortality in Argentina. These objectives are addressed by maintaining three core concepts: quality control, disease monitoring, and wide coverage of available early detection and treatment services. The NPCBC is currently implementing the "Time 1 Survey Study." Time 1 is defined as the time from the first appearance of BC signs or symptoms to the first consult within the public healthcare system. This timeframe is important in Argentina because it is outside of the health timeframes and data parameters monitored by the national cancer data registry system. The Time 1 Survey study has the potential to serve as an informational tool for BC patient navigation efforts in Argentina because it can be used to identify and characterize the barriers and delays that women face during Time 1. Lessons and experiences included in this study could be translated to other Latin American and middle-income countries for developing cancer control programs that can lead to improving treatment and reducing mortality through patient navigation and cancer education efforts for the public, health professionals, and patients.
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Neoplasias de la Mama , Navegación de Pacientes , Humanos , Femenino , Neoplasias de la Mama/diagnóstico , Neoplasias de la Mama/prevención & control , Argentina/epidemiología , Renta , IncidenciaRESUMEN
Urinary tract infections (UTIs) belong to the most common pathologies in Mexico and are mainly caused by Uropathogenic Escherichia coli (UPEC). UPEC possesses a wide diversity of virulence factors that allow it to carry out its pathogenesis mechanism in the urinary tract (UT). The development of morphotypes in UT represents an important feature of UPEC because it is associated with complications in diagnosis of UTI. The aim of this study was to determine the presence of bacterial morphotypes, virulence genes, virulence phenotypes, antibiotic resistant, and phylogenetic groups in clinical isolates of UPEC obtained from women in Sonora, Mexico. Forty UPEC isolates were obtained, and urine morphotypes were observed in 65% of the urine samples from where E. coli was isolated. Phylogenetic group B2 was the most prevalent. The most frequent virulence genes were fimH (100%), fliCD (90%), and sfaD/focC (72%). Biofilm formation (100%) and motility (98%) were the most prevalent phenotypes. Clinical isolates showed high resistance to aminoglycosides and ß-lactams antibiotics. These data suggest that the search for morphotypes in urine sediment must be incorporated in the urinalysis procedure and also that clinical isolates of UPEC in this study can cause upper, lower, and recurrent UTI.
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BACKGROUND: Existing studies show that consuming food consistent with one's culture reduces cardiometabolic risk. However, few studies have assessed whether these dietary choices influence sleep health. Accordingly, this study assessed how Mexican food consumption by individuals of Mexican descent residing at the US-Mexico border, was associated with various measures of sleep, after accounting for acculturation. METHODS: Data were provided by 100 adults between the ages of 18-60, in the city of Nogales, AZ. Questionnaires were provided in either Spanish or English. Acculturation was assessed with the Acculturation Scale for Mexican-Americans (ARSMA-II), with an additional question, asking how often "my family cooks Mexican foods." Frequency of cooking Mexican food was coded as either "yes" or "no." Sleep was assessed, using validated measures that include the Insomnia Severity Index (ISI), the Epworth Sleepiness Scale (ESS), the Pittsburgh Sleep Quality Index (PSQI), and sleep duration with the item "how many hours of actual sleep did you get at night?" Regression models estimated the associations between sleep health variables as outcomes and consumption of Mexican food as the independent variable. Covariates included age, sex, and acculturation scores. Parental education level was also included, as an indicator of childhood socioeconomic status and since food culture likely involves parents. RESULT: We found that among individuals who identified as Mexican-Americans who consumed culturally-consistent foods, was associated with, on average, 1.41 more hours of sleep (95% CI 0.19, 2.62; p = 0.024) and were less likely to report snoring (OR: 0.25; 95% CI 0.07, 0.93; p = 0.039). Consuming Mexican food was not associated with sleep quality, insomnia severity or sleepiness. CONCLUSION: Individuals of Mexican descent residing at the US-Mexico border who regularly consumed Mexican food, reported more sleep and less snoring. Mexican acculturation has been shown previously to improve sleep health. This is likely due to consumption of a culturally- consistent diet. Future studies should examine the role of acculturation in sleep health, dietary choices, and subsequent cardiometabolic risk.
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The main chemical composition and pharmacological potential of propolis from arid and semi-arid regions of the Sonoran Desert have been previously reported. Caborca propolis (CP), from an arid zone of the Sonoran Desert, has shown a polyphenolic profile that suggests a mixed plant origin, presenting poplar-type markers, as well as a 6-methoxylated flavonoid, xanthomicrol, characteristic of Asteraceae plants. In addition, CP has shown significant antioxidant properties and antiproliferative activity on cancer cells. In this study, we analyzed the influence of collection time on the chemical constitution, antiproliferative activity and protective capacity of CP against reactive oxygen species (ROS), by using HPLC-UV-diode array detection (DAD) analysis, 3-(4,5-dimethylthiazol-2-yl)-2,5-Dimethyltetrazoliumbromide (MTT) and 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assays, as well as cellular antioxidant activity (CAA) assay on murine B-cell lymphoma M12.C3.F6 cells. HPLC-UV-DAD analyses of seasonally collected CP (one-year period) revealed quantitative differences among the most abundant CP constituents: pinocembrin, galangin, chrysin and pinobanksin-3-O-acetate. Though all seasonal samples of CP induced an antiproliferative effect in M12.C3.F6 cells, CP from autumn showed the highest inhibitory activity (IC50: 5.9 ± 0.6 µg/mL). The DPPH assay pointed out that CP collected in autumn presented the highest antioxidant potential (IC50: 58.8 ± 6.7 µg/mL), followed by winter (65.7 ± 12.2 µg/mL) and spring (67.0 ± 7.5 µg/mL); meanwhile, the summer sample showed a lesser antioxidant capacity (IC50: 98.7 ± 2.5 µg/mL). The CAA assay demonstrated that CP induced a significant protective effect against ROS production elicited by H2O2 in M12.C3.F6 cells. Pretreatment of M12.C3.F6 cells with CP from spring and autumn (25 and 50 µg/mL for 1 h) showed the highest reduction in intracellular ROS induced by H2O2 (1 and 5 mM). These results indicate that the antiproliferative effect and cellular antioxidant activity of CP are modulated by quantitative fluctuations in its polyphenolic profile due to its collection time.
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La medicina tradicional y estudios realizados a diferentes especies del género Prosopis, del desierto sonorense, indican que es una fuente para la cualificación de compuestos bioactivos, con poder antioxidante y ácidos grasos (linoleico y linolénico) de la semilla. La actividad biológica, es atribuible a alcaloides, flavonoides, terpenos y compuestos fenólicos, para lo cual, se realizó el perfil fitoquímico en los extractos acuoso, etanólico, hexanico y clorofórmico (mediante técnicas colorimétricas), actividad antioxidante (método: 1,1-difenil-2-picrilhidrazil (DPPH)), fenoles totales (utilizando el reactivo de Folin-Ciocalteau) y perfil de ácidos grasos (cromatografía de gases) de la semilla de Prosopis spp. La extracción del aceite se realizó mediante Soxhlet. Se encontraron saponinas en todos los extractos, mientras que, en el etanólico, hexanico y clorofórmico, terpenos y esteroles. En el extracto etanólico se encontraron quinonas y en el acuoso aminoácidos libres. El valor más alto de la actividad antioxidante de EC50 fue de 3.272,41 ± 5,97, para el extracto etanólico, indicando su potencial como antioxidante. El contenido de fenoles totales, fue hexano> etanol > cloroformo> acuoso (81,95; 119,83; 125,18 y 127,57 mg equivalentes de ácido gálico/g de extracto seco). Los ácidos grasos en mayor proporción fueron los insaturados con 71,41 % (ácido linoleico: 42,68 %; oleico: 28.73 %) y ácidos grasos saturados: ácido palmítico (13.42 %) y estérico (4,73 %). Se concluye que este tipo de extractos presentan metabolitos importantes para la dieta, presentan actividad antioxidante y ácidos grasos esenciales para el organismo(AU)
Traditional medicine and studies with different species of the Prosopis genus, from the Sonoran Desert, is a source for the qualification of bioactive compounds, with antioxidant power and fatty acids (linoleic and linolenic) of the seed. The biological activity is attributable to alkaloids, flavonoids, terpenes and phenolic compounds, for which, the phytochemical profile was performed in the aqueous, ethanolic, hexane and chloroform extracts (using colorimetric techniques), antioxidant activity (method: 1,1-diphenyl-2-picrilhidrazil (DPPH)), total phenols (using the Folin-Ciocalteau reagent) and fatty acid profile (gas chromatography). The oil was extracted using Soxhlet. Saponins were found in all extracts, while, in ethanolic, hexanic and chloroform, terpenes and sterols. In the ethanolic extract quinones were found and in the aqueous free amino acids. The highest value of the antioxidant activity of EC50 was 3,272.41 ± 5.97, for the ethanolic extract, indicating its potential as an antioxidant. The total phenolic content was hexane> ethanol> chloroform> aqueous (81.95, 119.83, 125.18 and 127.57 mg equivalent of gallic acid / g of dry extract). The fatty acids in greater proportion were unsaturated with 71.41 % (linoleic acid: 42.68 %; oleic: 28.73 %) and saturated fatty acids: palmitic acid (13.42 %) and stearic (4.73 %). It is concluded that this type of extracts have important metabolites for the diet, have antioxidant activity and essential fatty acids for the body(AU)
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Prosopis , Compuestos Fenólicos , Ácidos Grasos , Fitoquímicos , Semillas , Flavonoides/análisis , Alcaloides/análisisRESUMEN
The main chemical composition of Sonoran propolis (SP), as well as its antiproliferative activity on cancer cells through apoptosis induction, has been reported. The chemical constitution of SP remained qualitatively similar throughout the year, whereas the antiproliferative effect on cancer cells exhibited significant differences amongst seasonal samples. The main goal of this study was to provide phytochemical and pharmacological evidence for the botanical source of SP and its antiproliferative constituents. A chemical comparative analysis of SP and plant resins of species found in the surrounding areas of the beehives was carried out by HPLC-UV-DAD, as well as by 1H NMR experiments. The antiproliferative activity on cancerous (M12.C3.F6, HeLa, A549, PC-3) and normal cell lines (L-929; ARPE-19) was assessed through MTT assays. Here, the main polyphenolic profile of SP resulted to be qualitatively similar to Populus fremontii resins (PFR). However, the antiproliferative activity of PFR on cancer cells did not consistently match that exhibited by SP throughout the year. Additionally, SP induced morphological modifications on treated cells characterised by elongation, similar to those induced by colchicine, and different to those observed with PFR treatment. These results suggest that P. fremontii is the main botanical source of SP along the year. Nevertheless, the antiproliferative constituents of SP that induce that characteristic morphological elongation on treated cells are not obtained from PFR. Moreover, the presence of kaempferol-3-methyl-ether in SP could point Ambrosia ambrosioides as a secondary plant source. In conclusion, SP is a bioactive poplar-type propolis from semi-arid zones, in which chemical compounds derived from other semi-arid plant sources than poplar contribute to its antiproliferative activity.
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Própolis/química , Própolis/farmacología , Células A549 , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Clima Desértico , Células HeLa , Humanos , Populus/químicaRESUMEN
Propolis is a resinous substance produced by honeybees (Apis mellifera) from the selective collection of exudates and bud secretions from several plants. In previous works, we reported the antiproliferative activity of Sonoran propolis (SP) on cancer cells; in addition we suggested the induction of apoptosis after treatment with SP due to the presence of morphological changes and a characteristic DNA fragmentation pattern. Herein, in this study we demonstrated that the antiproliferative effect of SP is induced through apoptosis in a B-cell lymphoma cancer cell line, M12.C3.F6, by an annexin V-FITC/Propidium iodide double labeling. This apoptotic effect of SP resulted to be mediated by modulations in the loss of mitochondrial membrane potential (ΔΨm) and through activation of caspases signaling pathway (3, 8 and 9). Afterward, in order to characterize the chemical constituents of SP that induce apoptosis in cancer cells, an HPLC-PDA-ESI-MS/MS method followed by a preparative isolation procedure and NMR spectroscopy analysis have been used. Eighteen flavonoids, commonly described in propolis from temperate regions, were characterized. Chrysin, pinocembrin, pinobanksin and its ester derivatives are the main constituents of SP and some of them have never been reported in SP. In addition, two esters of pinobanksin (8 and 13) are described by first time in propolis samples in general. The antiproliferative activity on M12.C3.F6 cells through apoptosis induction was exhibited by pinobanksin (4), pinobanksin-3-O-propanoate (14), pinobanksin-3-O-butyrate (16), pinobanksin-3-O-pentanoate (17), and the already reported galangin (11), chrysin (9) and CAPE. To our knowledge this is the first report of bioactivity of pinobanksin and some of its ester derivatives as apoptosis inducers. Further studies are needed to advance in the understanding of the molecular basis of apoptosis induction by SP and its constituents, as well as the structure-activity relationship of them.
Asunto(s)
Apoptosis/efectos de los fármacos , Flavanonas/farmacología , Linfoma de Células B/tratamiento farmacológico , Própolis/química , Animales , Caspasas/metabolismo , Línea Celular Tumoral/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Ésteres/química , Flavanonas/química , Linfoma de Células B/patología , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ratones , Estructura Molecular , Própolis/análisis , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
The aim of the present study was to evaluate the anti-Vibrio activity of propolis collected from three different areas of the Sonoran Desert in northwestern, Mexico [Pueblo de Alamos (PAP), Ures (UP), and Caborca (CP)]. The anti-Vibrio spp. activity of Sonoran propolis was determined by the broth microdilution method. UP propolis showed the highest antibacterial activity [minimal inhibitory concentration (MIC(50))<50 µg mL(-1)] against Vibrio spp. (UP>CP>PAP). UP propolis significantly inhibited the growth of Vibrio cholerae O1 serotype Inaba (MIC(50)<50 µg mL(-1)), V. cholerae non-O1 (MIC(50)<50 µg mL(-1)), V. vulnificus (MIC(50)<50 µg mL(-1)), and V. cholerae O1 serotype Ogawa (MIC(50) 100 µg mL(-1)), in a concentration-dependent manner. The UP propolis constituents, galangin and caffeic acid phenethyl ester (CAPE), exhibited a potent growth inhibitory activity (MIC(50) 0.05-0.1 mmol l(-1)) against V. cholerae strains (non-O1 and serotype Ogawa). The strong anti-Vibrio activity of Sonoran propolis and some of its chemical constituents (galangin and CAPE) support further studies on the clinical applications of this natural bee product against different Vibrio spp., mainly V. cholerae.
Asunto(s)
Antibacterianos/farmacología , Própolis/farmacología , Vibrio cholerae O1/efectos de los fármacos , Vibrio/efectos de los fármacos , Ácidos Cafeicos/farmacología , Flavonoides/farmacología , México , Pruebas de Sensibilidad Microbiana , Alcohol Feniletílico/análogos & derivados , Alcohol Feniletílico/farmacologíaRESUMEN
Introducción: El síndrome de leucoencefalopatía posterior reversible (SLPR) se caracteriza por la presentación aguda o subaguda y habitualmente transitoria de cefalea, trastornos visuales, alteraciones de la conciencia y convulsiones asociadas a edema cerebral en las regiones posteriores del cerebro. Se ha descrito su asociación con múltiples procesos y eventualmente con el shock séptico (SS). Se presenta un nuevo caso de SLPR en el contexto de un SS. Caso clínico: Mujer de 52 años, quien después de colecistectomía desarrolló SS con falla respiratoria aguda por lo que es sometida a ventilación mecánica (VM). Cinco días después de suspender VM y sedación la paciente persistió con trastorno del estado de conciencia. La resonancia magnética (RM) cerebral mostró múltiples lesiones bilaterales, hiperintensas en FLAIR (fluid-attenuated inversion recovery) localizadas en sustancia blanca de los lóbulos parietales y occipitales. Dos días después se realizó una nueva RM que mostró una remisión de las lesiones. La recuperación clínica fue rápidamente progresiva en las dos semanas siguientes al diagnóstico. Conclusiones: El SLPR es una complicación aguda o subaguda que cursa con edema cerebral vasogénico detectable por RM. Esta entidad puede presentase en el curso del SS y su patogenia aun no es claramente conocida. En el caso presentado es posible que la injuria endotelial producida en el curso del SS hayan contribuido a su desarrollo.
Introduction: Reversible posterior leukoencephalopathy syndrome (RPLS) is characterized by acute or subacutepresentation, usually transient, ofheadache, visual disturbances, impaired consciousness and convulsions associated with alterations in the posterior region ofthe brain. It has been described in association with multiple processes including septic shock (SS). Wepresent a new case ofRPLS in the context of a SS. Case report: A woman of 52 years, developed SS after cholecystectomy with acute respiratory failure and was pot in mechanical ventilation (MV). Five days after stopping the VM and sedation, patient persisted with the state of consciousness disorder. Magnetic resonance imaging (MRI) brain showed multiple bilaterallesions, hyperintense on FLAIR (fluid-attenuated inversion recovery) located in the white matterof the parietal and occipitallobes. Two days later a new MRI was performed which showed a remission of the lesions. Clinical recovery was rapid and progresive in the two weeks following the diagnosis. Conclusions: The RPLS is an acute or subacute complication that is accompanied with brain vasogenic edema detectable by MRI. This entity can occur in the course ofthe SS and its pathogenesis is still not clearly. In this case it is possible that endothelial injury caused in the course of the SShave contributed to its development.