RESUMEN
The neem tree (Azadirachta indica A. Juss) is grown mainly for shade, fuel, and numerous non-timber forest products using its leaves, fruit, and bark. It produces an essential oil that is used as a source for obtaining bioinsecticides, with a broad spectrum of action in agricultural production. Its bioinsecticidal activity is due to the presence of triterpenes, such as azadirachtin, a product in continued growth of the global biopesticide market. Optimal conditions for neem oil extraction using response surface methodology (RSM) and microwave-assisted extraction (MAE) methods have been defined. However, the extraction conditions for these methods tend to consume high volumes of organic solvent and long extraction times. The aim of the present study is to determine the optimal conditions for the extraction of azadirachtin from neem seeds in a hydroalcoholic medium using MAE and RSM with a Box-Behnken design (BBD). A BBD was applied to evaluate the effects of the factors, magnetron voltage (X1), extraction time (X2), and pH of the extraction medium (X3), on the yield of the azadirachtin extraction process. The effect of each variable on the extraction yield was studied independently, considering the pure coefficients (linear and quadratic) on the three levels that were studied in the experiments. Moreover, the study experiments were conducted in triplicate, data were presented as mean and standard deviation, homogeneity of variances was estimated using Levene's test, and a two-way ANOVA with Tukey's post hoc analysis was performed to identify the experimental conditions that allowed us to find the highest extraction yield and to analyze whether the response surface model adequately described our data. The most significant effects of the model correspond to quadratic and interaction effects (p < 0.0001); the quadratic terms voltage (X1), extraction time (X2), and pH (X3); and the interaction effects between voltage-pH (X1*X3) and time-pH (X2*X3), which had a significant influence on the model. Moreover, a canonical analysis was performed. The optimal conditions were as follows: 69.22 V, 6.89 min, and a pH value of 4.35, coinciding with the zones shown in the contour plots. Furthermore, the response obtained at the optimal conditions was 37.5 µg of azadirachtin per gram of pretreated seed.
RESUMEN
Arterial hypertension (AH) is a multifactorial and asymptomatic disease that affects vital organs such as the kidneys and heart. Considering its prevalence and the associated severe health repercussions, hypertension has become a disease of great relevance for public health across the globe. Conventionally, the classification of an individual as hypertensive or non-hypertensive is conducted through ambulatory blood pressure monitoring over a 24-h period. Although this method provides a reliable diagnosis, it has notable limitations, such as additional costs, intolerance experienced by some patients, and interferences derived from physical activities. Moreover, some patients with significant renal impairment may not present proteinuria. Accordingly, alternative methodologies are applied for the classification of individuals as hypertensive or non-hypertensive, such as the detection of metabolites in urine samples through liquid chromatography or mass spectrometry. However, the high cost of these techniques limits their applicability for clinical use. Consequently, an alternative methodology was developed for the detection of molecular patterns in urine collected from hypertension patients. This study generated a direct discrimination model for hypertensive and non-hypertensive individuals through the amplification of Raman signals in urine samples based on gold nanoparticles and supported by chemometric techniques such as partial least squares-discriminant analysis (PLS-DA). Specifically, 162 patient urine samples were used to create a PLS-DA model. These samples included 87 urine samples from patients diagnosed with hypertension and 75 samples from non-hypertensive volunteers. In the AH group, 35 patients were diagnosed with kidney damage and were further classified into a subgroup termed (RAH). The PLS-DA model with 4 latent variables (LV) was used to classify the hypertensive patients with external validation prediction (P) sensitivity of 86.4%, P specificity of 77.8%, and P accuracy of 82.5%. This study demonstrates the ability of surface-enhanced Raman spectroscopy to differentiate between hypertensive and non-hypertensive patients through urine samples, representing a significant advance in the detection and management of AH. Additionally, the same model was then used to discriminate only patients diagnosed with renal damage and controls with a P sensitivity of 100%, P specificity of 77.8%, and P accuracy of 82.5%.
Asunto(s)
Hipertensión , Enfermedades Renales , Nanopartículas del Metal , Humanos , Espectrometría Raman/métodos , Oro , Monitoreo Ambulatorio de la Presión Arterial , Nanopartículas del Metal/química , Enfermedades Renales/diagnóstico , Urinálisis/métodos , Hipertensión/orinaRESUMEN
The growing emergence of microbes resistant to commercially available antibiotic therapies poses a threat to healthcare systems worldwide. Multiple factors have been associated with the increasing incidence of hospital-acquired infections caused by antibiotic-resistant pathogens, including the indiscriminate use of broad-spectrum antibiotics, the massive application of antibiotics in hospitals as a prophylactic measure, self-medication, and nonadherence to pharmacological therapies by patients. In this study, we developed a novel treatment to mitigate the impact of microbial resistance. We synthesized a benzoporphyrin derivative, 5,10,15,20-tetrakis (4-ethylphenyl) porphyrin (TEtPP), with a reaction yield close to 50%. TEtPP exhibited excellent photophysical properties (Φf = 0.12 ± 0.04 and ΦΔ = 0.81 ± 0.23) and was thereby assessed as a potential agent for antibacterial photodynamic therapy. The photophysical properties of the synthesized porphyrin derivative were correlated with the assayed antimicrobial activity. TEtPP showed higher activity against the MRSA strain under irradiation than in the absence of irradiation (minimum inhibitory concentration (MIC) = 69.42 µg/mL vs. MIC = 109.30 µg/mL, p < 0.0001). Similar behavior was observed against P. aeruginosa (irradiated MIC = 54.71 µg/mL vs. nonirradiated MIC = 402.90 µg/mL, p < 0.0001). TEtPP exhibited high activity against S. aureus in both the irradiated and nonirradiated assays (MIC = 67.68 µg/mL vs. MIC = 58.26 µg/mL, p = 0.87).
RESUMEN
In this report 5 compounds were synthesized and structural and their photophysical characterization was performed (ΦΔ and Φf). Furthermore, in this in vitro study, their biological activity against Leishmania panamensis was evaluated. The photophysical behavior of these compounds was measured and high ΦΔ and low Φf was observed. Besides, DFT quantum calculations on the electronic structures were performed. Finally, the biological activity was determined by means of the compounds capacity to inhibit the viability of parasites using the MTT assay. The inclusion of the metal ions substantially modified the photophysical and biological properties in comparison with the free metal porphyrin (1). In fact, Zn2+ porphyrin derivative (2) showed a marked decrease of Φf and increase of ΦΔ. In this sense, using TDDFT approaches, a luminescent process for Sn4+ derivative (3) was described, where emissive states involve the ML-LCT transition. So, this led to a decrease in the singlet oxygen production (0.82-0.67). Biological results showed that all compounds inhibit the viability of L. panamensis with high efficiency; the decrease in the viability was greater as the concentration of exposure increased. Finally, under light irradiation the IC50 of L. panamensis against the Zn(II)-porphyrin (2) and V(IV)-porphyrin (5) was lower than the IC50 of the Glucantime control (IC50 = 2.2 and 6.95 µM Vs IC50 = 12.7 µM, respectively). We showed that the use of porphyrin and metalloporphyrin-type photosensitizers with exceptional photophysical properties can be successful in photodynamic therapy (PDT) against L. panamensis, being the diamagnetic ion Zn2+ a candidate for the preparation of metalloporphyrins with high singlet oxygen production.
Asunto(s)
Leishmania , Metaloporfirinas , Fotoquimioterapia , Porfirinas , Metaloporfirinas/química , Metaloporfirinas/farmacología , Metales , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/farmacología , Porfirinas/química , Porfirinas/farmacología , Oxígeno Singlete/química , Zinc/farmacologíaRESUMEN
Leptospirosis is an acute febrile disease that mainly affects developing countries with tropical climates. The complexity and magnitude of this disease is attributed to socioeconomic, climatic, and environmental conditions. In this study, in a 10-year period from 2008 to 2017, the relationship between human leptospirosis cases and climatic factors in Cartagena de Indias, Colombia were evaluated. Monthly leptospirosis cases, climatic variables, and macroclimatic phenomena (El Niño and La Niña) were obtained from public datasets. Local climatic factors included temperature (maximum, average, and minimum), relative humidity, precipitation, and the number of precipitation days. Time series graphs were drawn and correlations between cases of leptospirosis and climatic variables considering lags from 0 to 10 months were examined. A total of 360 cases of leptospirosis were reported in Cartagena during the study period, of which 192 (53.3%) were systematically notified between October and December. Several correlations were detected between the number of cases, local climatic variables, and macroclimatic phenomena. Mainly, the increase of cases correlated with increased precipitation and humidity during the La Niña periods. Herein, seasonal patterns and correlations suggest that the climate in Cartagena could favor the incidence of leptospirosis. Our findings suggest that prevention and control of human leptospirosis in Cartagena should be promoted and strengthened, especially in the last quarter of the year.
Asunto(s)
Leptospirosis , Colombia/epidemiología , El Niño Oscilación del Sur , Humanos , Humedad , Incidencia , Leptospirosis/epidemiología , TemperaturaRESUMEN
Background: Photodynamic therapy activity against different biological systems has been reported for porphyrins. Porphyrin modifications through peripheral groups and/or by metal insertion inside the ring are main alternatives for the improvement of its photo-physical properties. In this study, we synthesized and characterized 5,10,15,20-tetrakis(4-bromophenyl)porphyrin and the dicloro-5,10,15,20-tetrakis(4-bromophenyl)porphyrinato Sn(IV). Methods: Metal-free porphyrin was synthesized using the Alder method, while the Sn(IV)-porphyrin complex was prepared by combining metal-free porphyrin with stannous chloride in DMF; the reaction yields were 47% and 64% respectively. Metal-free porphyrin was characterized by UV-Vis, FT-IR, ESI-mass spectrometry and 13C-NMR. Additionally, the Sn(IV) -porphyrin complex was characterized using UV-Vis and FT-IR. Cyclic voltammetry tests in four different solvents. The fluorescence quantum yield (Φ f) was measured using fluorescein as a standard, the singlet oxygen quantum yield (Φ D) was estimated using the standard 5,10,15,20-(tetraphenyl)porphyrin (H2TPP) and the quencher of singlet oxygen 1,3-diphenylisobenzofuran (DPBF). Results: UV-Vis assay showed typical Q and Soret bands for porphyrin and its metallo-porphyrin complex. Compounds showed photoluminescence at the visible range of electromagnetic spectrum. The inclusion of the metal in the porphyrin core changed the Φ f from 0.15 to 0.05 and the Φ D increased from 0.55 to 0.59. Finally, the effect of the compounds on the viability of L. panamensis was evaluated by means of the MTT test. The results showed that both compounds decreased the viability of the parasite; this inhibitory activity was greater under light irradiation; the porphyrin compound had IC 50 of 16.5 µM and the Sn(IV)-porphyrin complex had IC 50 of 19.2 µM. Conclusion: The compounds were synthesized efficiently, their characterization was carried out by different spectroscopy techniques and their own signals were evidenced for both structures, both compounds decreased the cell viability of L. panamensis.
Asunto(s)
Leishmania , Fármacos Fotosensibilizantes , Supervivencia Celular , Fármacos Fotosensibilizantes/farmacología , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
COVID-19, caused by SARS-CoV-2, a new coronavirus, was first observed in Wuhan (China) in November 2019. In a short time, SARS-CoV-2 spread across the world, creating a pandemic. There is a need to know the current situation of each country and region and to generate strategies to contain and mitigate the impact on global health and the economy. To control COVID-19 in Cartagena and the Department of Bolívar, Colombia, a strategic network involving public health entities and higher education institutions has emerged. The network has been in place for six months, and 77,122 subjects have been tested in Cartagena and Bolívar Department, of whom 8,260 (10.71%) tested positive (RT-qPCR). Of those who tested positive, 51.4% were male (p>0.05), and 13.1% were health personnel (9.43% female, p < 0.05). The mortality rate was relatively low, 1.22%, with males being the most affected, accounting for 0.9% of deaths (p > 0.05). The daily case report showed upward and downward fluctuations by the mobility restrictions applied to the population, and from day 120 of the start of the pandemic, the epidemiological curve stabilized, and a logarithmic plateau was reached. COVID-19 spread in 39/46 municipalities of Bolívar; however, Bolívar and Cartagena had a low number of cases and deaths compared to other departments and city in Colombia. Cartagena and Bolívar have been given an economic opening with restrictions on crowding and mandatory use of a mouth cover until a vaccine is available. UNIMOL was the first laboratory in Cartagena, Bolívar and Colombia to receive approval from the National Institute of Health to process COVID-19 samples; thanks to the timely diagnosis of cases by UNIMOL, intensive care unit (ICU) occupancy did not exceed capacity, and population confinement was appropriately initiated.
RESUMEN
In this study, a family of porphyrins based on 5,10,15,20-Tetrakis(4-ethylphenyl)porphyrin (1, Ph) and six metallo-derivatives (Zn2+(2, Ph-Zn), Sn4+(3, Ph-Sn), Mn2+ (4, Ph-Mn), Ni2+ (5, Ph-Ni), Al3+ (6, Ph-Al), and V3+ (7, Ph-V)) were tested as photosensitizers for photodynamic therapy against Leishmania braziliensis and panamensis. The singlet oxygen quantum yield value (ΦΔ) for (1-7) was measured using 1,3-diphenylisobenzofuran (DPBF) as a singlet oxygen trapping agent and 5,10,15,20-(tetraphenyl)-porphyrin (H2TPP) as a reference standard; besides, parasite viability was estimated by the MTT assay. After metal insertion into the porphyrin core, the ΦΔ increased from 0.76-0.90 and cell viability changed considerably. The ΦΔ and metal type changed the cytotoxic activity. Finally, (2) showed both the highest ΦΔ (0.90) and the best photodynamic activity against the parasites studied (IC50 of 1.2 µM).
Asunto(s)
Leishmania braziliensis/efectos de los fármacos , Leishmania/efectos de los fármacos , Metaloporfirinas/química , Metaloporfirinas/toxicidad , Fármacos Fotosensibilizantes/química , Porfirinas/química , Oxígeno Singlete/química , Benzofuranos/química , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/efectos de la radiación , Concentración 50 Inhibidora , Leishmania/efectos de la radiación , Leishmania braziliensis/efectos de la radiación , Luz , Metaloporfirinas/síntesis química , Fotoquimioterapia , Porfirinas/síntesis química , Porfirinas/toxicidadRESUMEN
BACKGROUND: Adiponectin is a hormone secreted by adipose tissue. It regulates glycolysis and lipolysis and is involved in the pathophysiology of diabetes and related disorders. Its activity is mainly mediated by the transmembrane receptors AdipoR1 and AdipoR2, which are encoded by ADIPOR1 (1q32.1) and ADIPOR2 (12p13.33) genes, respectively. In genetic association studies, single nucleotide polymorphisms (SNPs) in or near these genes have been associated with metabolic alterations. However, these relationships are still controversial. AIM: The aim of this work was to analyze possible associations between ADIPOR1/2 and diabetes and other metabolic disorders. METHODS: A genetic association study was carried out in an admixed Latin American population. A sample of 200 adults was analyzed. Clinical and serum-biochemical characteristics were measured to diagnose obesity, abdominal obesity, hypertension, hyperglycemia, hypertriglyceridemia, low HDLc, insulin resistance (HOMA-IR), and diabetes. Three SNPs were genotyped in ADIPOR1 (rs10494839, rs12733285, and rs2275737) and ADIPOR2 (rs11061937, rs11612383, and rs2286383). For the association analysis, an additive model was assessed through logistic regression. An admixture adjustment was performed using a Monte-Carlo-Markov-Chain method, assuming a three-hybrid substructure (k = 3). RESULTS: Two SNPs in ADIPOR1 were associated with diabetes: rs10494839 (OR = 3.88, adjusted p < 0.03) and rs12733285 (OR = 4.72, adjusted p < 0.03). Additionally, rs10494839 was associated with hypertriglyceridemia (OR = 2.16, adjusted p < 0.01). None of the SNPs in ADIPOR2 were associated with metabolic disorders. CONCLUSIONS: ADIPOR1 was consistently associated with diabetes and hypertriglyceridemia. This association was maintained even after adjusting for genetic stratification. There were no significant associations involving ADIPOR2.