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1.
J Cardiothorac Surg ; 19(1): 592, 2024 Oct 04.
Artículo en Inglés | MEDLINE | ID: mdl-39367427

RESUMEN

INTRODUCTION: Infection is a significant complication of cardiac implantable electronic device (CIED) therapy. The European TauroPace™ Registry investigates the safety and efficacy of TauroPace™ (TP), an antimicrobial solution containing taurolidine, designed to prevent CIED infections. METHODS: This multicenter study included patients undergoing CIED procedures at participating centers where TP was used as a disinfectant for external hardware surfaces and an antiseptic for irrigating surgical sites. All patients eligible for CIED placement with adjunctive TP as the standard of care were included. Other aspects of CIED procedures adhered to current guidelines. Data on CIED-related infective endocarditis, CIED pocket infection, device and procedure-related complications, adverse events, and all-cause mortality were prospectively collected for 12 months. In cases of revision, the previous procedure was censored, and a new procedure was created. Binomial and Kaplan-Meier statistics were employed to analyze event rates. RESULTS: From January 2020 to November 2022, TP was used in 822 out of 1170 CIED procedures. Among patients who completed the 3-month follow-up, no CIED pocket infections were observed, and one case of CIED-related infective endocarditis was reported. In the 12-month follow-up cohort, two additional local pocket CIED infections were observed, resulting in a total of three major CIED infections within 1 year after the CIED placement procedure. The 3-month and 12-month major CIED infection rates were 0.125% and 0.51%, respectively. During the observation a complication rate of 4.4% was reported. No adverse events related to TP were observed. CONCLUSIONS: TP appears to be effective and safe in preventing CIED infections. CLINICALTRIALS: gov Identifier: NCT04735666.


Asunto(s)
Desfibriladores Implantables , Marcapaso Artificial , Infecciones Relacionadas con Prótesis , Sistema de Registros , Taurina , Tiadiazinas , Humanos , Tiadiazinas/uso terapéutico , Taurina/análogos & derivados , Taurina/uso terapéutico , Masculino , Femenino , Infecciones Relacionadas con Prótesis/prevención & control , Anciano , Desfibriladores Implantables/efectos adversos , Marcapaso Artificial/efectos adversos , Persona de Mediana Edad , Europa (Continente) , Estudios Prospectivos , Antiinfecciosos Locales/uso terapéutico
2.
Curr Microbiol ; 81(10): 325, 2024 Aug 24.
Artículo en Inglés | MEDLINE | ID: mdl-39182011

RESUMEN

Antimicrobials fight microorganisms, preventing and treating infectious diseases. However, antimicrobial resistance (AMR) is a growing concern due to the inappropriate and excessive use of these drugs. Several mechanisms can lead to resistance, including efflux pumps such as the NorA pump in Staphylococcus aureus, which reduces the effectiveness of fluoroquinolones. Thiadiazines are heterocyclic compounds whose chemical structure resembles that of cephalosporins. Therefore, these compounds and their derivatives have been studied for their potential in combating increased bacterial resistance. To analyze this hypothesis, direct activity assays, antibiotic action-modifying activity, fluorescence assays to evaluate the retention of ethidium bromide inside bacteria, and molecular docking were carried out. These experiments involved serial dilutions in microplates against Staphylococcus aureus strain 1199B under the influence of six thiadiazine derivatives (IJ10, IJ11, IJ21, IJ22, IJ23, and IJ25). The tests revealed that, despite not showing effective direct activity, some thiadiazine derivatives (IJ11, IJ21, and IJ22) inhibited the function of the bromide pump both in microdilution tests and in fluorescence and docking assays. Particularly, the IJ11 compound stood out for its activity similar to efflux inhibitors, as well as its inhibition of the norfloxacin pump of this bacterium. Among the results of this study, it deserves to be highlighted for anchoring future experiments, as it represents the first investigation of this group of thiadiazine derivatives against the NorA pump.


Asunto(s)
Antibacterianos , Proteínas Bacterianas , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Proteínas Asociadas a Resistencia a Múltiples Medicamentos , Staphylococcus aureus , Tiadiazinas , Antibacterianos/farmacología , Antibacterianos/química , Staphylococcus aureus/efectos de los fármacos , Proteínas Bacterianas/metabolismo , Proteínas Bacterianas/química , Proteínas Bacterianas/genética , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/antagonistas & inhibidores , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/metabolismo , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/química , Tiadiazinas/farmacología , Tiadiazinas/química , Simulación por Computador
3.
Int J Mol Sci ; 25(16)2024 Aug 22.
Artículo en Inglés | MEDLINE | ID: mdl-39201791

RESUMEN

Alzheimer's disease (AD) is the most common neurodegenerative disorder, marked by cognitive impairment. Currently, the available treatment provides only symptomatic relief and there is a great need to design and formulate new drugs to stabilize AD. In the search for a new anti-Alzheimer's drug, 3,5-bis(2-hydroxyethyl)-1,3,5-thiadiazinane-2-thione (THTT), a tetrahydro-2H-1,3,5-thiadiazine-2-thione derivative, was investigated against a scopolamine-induced Alzheimer's model. The selected test compound was administered intraperitoneally in three doses (15 mg/kg, 30 mg/kg, and 45 mg/kg). The test compound exhibited an IC50 value of 69.41 µg/mL, indicating its ability to inhibit the acetylcholinesterase enzyme. An antioxidant DPPH assay revealed that the IC50 value of the test compound was 97.75 µg/mL, which shows that the test compound possesses antioxidant activity. The results of behavior tests including the Y-maze and elevated plus maze (EPM) show that the test compound improved short-term memory and spatial memory, respectively. Furthermore, in the Morris water maze (MWM) and light/dark model, the test compound shows improvements in learning and memory. Moreover, the results of histological studies show that the test compound can protect the brain against the harmful effects of scopolamine. Overall, the findings of our investigation suggest that our chosen test compound has disease-modifying and neuroprotective activities against the scopolamine-induced Alzheimer's model. The test compound may be beneficial, subject to further elaborate investigation for anti-amyloid disease-modifying properties in AD.


Asunto(s)
Enfermedad de Alzheimer , Aprendizaje por Laberinto , Escopolamina , Tiadiazinas , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/inducido químicamente , Animales , Tiadiazinas/farmacología , Tiadiazinas/uso terapéutico , Masculino , Aprendizaje por Laberinto/efectos de los fármacos , Modelos Animales de Enfermedad , Ratones , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Acetilcolinesterasa/metabolismo , Tionas/farmacología , Tionas/química , Tionas/uso terapéutico , Ratas
4.
Food Chem ; 460(Pt 3): 140779, 2024 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-39121778

RESUMEN

Buprofezin (BUP) is an insect growth regulator widely used in agriculture to control hemipteran pests, particularly the melon aphid, Aphis gossypii, due to its efficiency and low toxicity. Although approved by the Chinese government, its maximum residue limit (MRL) in food is strictly regulated, and conventional techniques for detecting BUP have several limitations. Our study reports successful BUP detection using a supramolecular fluorescent probe DP@ALB, constructed with chalcone-based fluorescent dye DP and albumin as the host. The probe offers advantages such as low cost, visual signal output with high fluorescence color variation, rapid response, and high sensitivity. Additionally, portable test strips enable convenient on-site BUP detection and simplifying field monitoring of spiked real samples. The study achieves precise qualitative and quantitative BUP analysis in grape fruit, groundwater, and soil with satisfactory recoveries. Further, the biological applicability of sensor for the in vitro detection of BUP in L929 living cells was demonstrated. This research breakthrough overcomes the limitations of traditional analytical methods, offering an efficient and reliable approach for food and environmental monitoring and pesticide residue detection.


Asunto(s)
Técnicas Biosensibles , Contaminación de Alimentos , Teléfono Inteligente , Tiadiazinas , Técnicas Biosensibles/instrumentación , Técnicas Biosensibles/métodos , Contaminación de Alimentos/análisis , Tiadiazinas/química , Tiadiazinas/análisis , Residuos de Plaguicidas/análisis , Vitis/química , Colorantes Fluorescentes/química , Insecticidas/análisis , Animales , Límite de Detección , Frutas/química
5.
J Hosp Infect ; 152: 56-65, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39004189

RESUMEN

BACKGROUND: Taurolidine-citrate(-heparin) lock solutions (TCHL) are suggested as a promising and safe method for the prevention of central-line-associated bloodstream infections (CLABSI). AIM: To investigate the efficacy of TCHL for the prevention of CLABSI in paediatric oncology patients. METHODS: An assessor-blinded randomized controlled trial at the Princess Máxima Centre for paediatric oncology, the Netherlands, was performed from 2020 to 2023. Paediatric oncology patients receiving a tunnelled central venous access device (CVAD) were eligible. A total of 462 patients were required to compare the TCHL to the heparin-only lock (HL). Patients were followed-up for the first 90 days after CVAD insertion. The primary outcome was the incidence of the first CLABSI from CVAD insertion until the end of follow-up. Intention-to-treat and per-protocol analyses were performed. FINDINGS: In total, 232 were randomized in the HL and 231 in the TCHL group. A total of 47 CLABSIs were observed. The intention-to-treat analysis showed that a CLABSI was observed in 26 (11.2%) of the HL group patients versus 21 (9.1%) of the TCHL group patients; incidence rate ratio (IRR) of 0.81 (95% confidence interval (CI): 0.46-1.45) in favour of the TCHL group. The per-protocol analysis showed that a CLABSI was observed in 10 (7.9%) of the HL group patients versus 6 (4.8%) of the TCHL group patients; IRR of 0.59 (95% CI: 0.21-1.62) in favour of the TCHL group. Adverse events were more common in the TCHL group but rarely reported. CONCLUSION: No difference was detected between the TCHL and HL in the incidence of CLABSI in paediatric oncology patients.


Asunto(s)
Infecciones Relacionadas con Catéteres , Cateterismo Venoso Central , Heparina , Taurina , Tiadiazinas , Humanos , Infecciones Relacionadas con Catéteres/prevención & control , Infecciones Relacionadas con Catéteres/epidemiología , Tiadiazinas/administración & dosificación , Tiadiazinas/uso terapéutico , Taurina/análogos & derivados , Taurina/administración & dosificación , Masculino , Femenino , Niño , Heparina/administración & dosificación , Preescolar , Países Bajos , Lactante , Cateterismo Venoso Central/efectos adversos , Neoplasias/complicaciones , Ácido Cítrico/administración & dosificación , Adolescente , Incidencia , Catéteres Venosos Centrales/efectos adversos , Resultado del Tratamiento
6.
Bull Exp Biol Med ; 177(1): 63-67, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38954300

RESUMEN

Compound L-36, a new derivative of 6H-1,3,4-thiadiazine, was studied in in vitro and in vivo experiments. This compound exhibits high antiplatelet and antithrombogenic activity. In in vitro experiments, compound L-36 by its antiplatelet activity (by IC50) was superior to acetylsalicylic acid by 9.4 times. In in vivo experiments, compound L-36 by its ED50 value was close to the comparison drug. On the model of pulmonary artery thrombosis, compound L-36 ensured better survival of experimental animals than acetylsalicylic acid. Morphological studies showed that compound L-36 effectively attenuated the thrombosis processes in the pulmonary tissue induced by intravenous injection of a thrombogenic mixture (epinephrine and collagen).


Asunto(s)
Aspirina , Fibrinolíticos , Inhibidores de Agregación Plaquetaria , Agregación Plaquetaria , Tiadiazinas , Animales , Inhibidores de Agregación Plaquetaria/farmacología , Inhibidores de Agregación Plaquetaria/química , Tiadiazinas/farmacología , Tiadiazinas/química , Fibrinolíticos/farmacología , Fibrinolíticos/química , Agregación Plaquetaria/efectos de los fármacos , Aspirina/farmacología , Masculino , Trombosis/tratamiento farmacológico , Trombosis/prevención & control , Ratas , Arteria Pulmonar/efectos de los fármacos , Colágeno , Epinefrina/farmacología , Ratones , Plaquetas/efectos de los fármacos
7.
Oncol Res ; 32(7): 1163-1172, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38948019

RESUMEN

Background: Osteosarcoma is the most common malignant primary bone tumor. The prognosis for patients with disseminated disease remains very poor despite recent advancements in chemotherapy. Moreover, current treatment regimens bear a significant risk of serious side effects. Thus, there is an unmet clinical need for effective therapies with improved safety profiles. Taurolidine is an antibacterial agent that has been shown to induce cell death in different types of cancer cell lines. Methods: In this study, we examined both the antineoplastic and antiangiogenic effects of taurolidine in animal models of osteosarcoma. K7M2 murine osteosarcoma cells were injected, both intramuscular and intraperitoneal, into 60 BALB/c mice on day zero. Animals were then randomized to receive treatment with taurolidine 2% (800 mg/kg), taurolidine 1% (400 mg/kg), or NaCl 0.9% control for seven days by intravenous or intraperitoneal administration. Results: After 35 days, mice were euthanized, and the tumors were harvested for analysis. Eighteen mice were excluded from the analysis due to complications. Body weight was significantly lower in the 2% taurolidine intraperitoneal treatment group from day 9 to 21, consistent with elevated mortality in this group. Intraperitoneal tumor weight was significantly lower in the 1% (p = 0.003) and 2% (p = 0.006) intraperitoneal taurolidine treatment groups compared to the control. No antineoplastic effects were observed on intramuscular tumors or for intravenous administration of taurolidine. There were no significant differences in microvessel density or mitotic rate between treatment groups. Reduced body weight and elevated mortality in the 2% taurolidine intraperitoneal group suggest that the lower 1% dose is preferable. Conclusions: In conclusion, there is no evidence of antiangiogenic activity, and the antitumor effects of taurolidine on osteosarcoma observed in this study are limited. Moreover, its toxic profile grants further evaluation. Given these observations, further research is necessary to refine the use of taurolidine in osteosarcoma treatment.


Asunto(s)
Neoplasias Óseas , Modelos Animales de Enfermedad , Osteosarcoma , Taurina , Tiadiazinas , Carga Tumoral , Animales , Taurina/análogos & derivados , Taurina/farmacología , Taurina/uso terapéutico , Tiadiazinas/farmacología , Tiadiazinas/uso terapéutico , Osteosarcoma/tratamiento farmacológico , Osteosarcoma/patología , Osteosarcoma/irrigación sanguínea , Ratones , Neoplasias Óseas/tratamiento farmacológico , Neoplasias Óseas/patología , Carga Tumoral/efectos de los fármacos , Densidad Microvascular/efectos de los fármacos , Ratones Endogámicos BALB C , Línea Celular Tumoral , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Inhibidores de la Angiogénesis/farmacología , Inhibidores de la Angiogénesis/uso terapéutico , Humanos , Neovascularización Patológica/tratamiento farmacológico
8.
Antimicrob Agents Chemother ; 68(7): e0038124, 2024 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-38864612

RESUMEN

Candida auris is an evolving and concerning global threat. Of particular concern are bloodstream infections related to central venous catheters. We evaluated the activity of taurolidine, a broad-spectrum antimicrobial in catheter lock solutions, against 106 C. auris isolates. Taurolidine was highly active with a MIC50/MIC90 of 512/512 mg/L, over 20-fold lower than lock solution concentrations of ≥13,500 mg/L. Our data demonstrate a theoretical basis for taurolidine-based lock solutions for prevention of C. auris catheter-associated infections.


Asunto(s)
Antifúngicos , Candida auris , Infecciones Relacionadas con Catéteres , Pruebas de Sensibilidad Microbiana , Taurina , Tiadiazinas , Tiadiazinas/farmacología , Taurina/análogos & derivados , Taurina/farmacología , Infecciones Relacionadas con Catéteres/microbiología , Infecciones Relacionadas con Catéteres/tratamiento farmacológico , Infecciones Relacionadas con Catéteres/prevención & control , Humanos , Antifúngicos/farmacología , Candida auris/efectos de los fármacos , Catéteres Venosos Centrales/microbiología , Catéteres Venosos Centrales/efectos adversos , Candidiasis/microbiología , Candidiasis/tratamiento farmacológico , Candidemia/microbiología , Candidemia/tratamiento farmacológico
9.
Pestic Biochem Physiol ; 202: 105953, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38879307

RESUMEN

The brown planthopper (Nilaparvata lugens) is a major destructive rice pest in Asia. High levels of insecticide resistance have been frequently reported, and the G932C mutation in the chitin synthase 1 (CHS1) gene has been found to mediate buprofezin resistance. However, there has been no direct evidence to confirm the functional significance of the single G932C substitution mutation leading to buprofezin resistance in N. lugens. Here, we successfully constructed a knock-in homozygous strain (Nl-G932C) of N. lugens using CRISPR/Cas9 coupled with homology-directed repair (HDR). Compared with the background strain susceptible to buprofezin (Nl-SS), the knock-in strain (Nl-G932C) showed a 94.9-fold resistance to buprofezin. Furthermore, resistant strains (Nl-932C) isolated from the field exhibited a 2078.8-fold resistance to buprofezin, indicating that there are other mechanisms contributing to buprofezin resistance in the field. Inheritance analysis showed that the resistance trait is incomplete dominance. In addition, the Nl-G932C strain had a relative fitness of 0.33 with a substantially decreased survival rate, emergence rate, and fecundity. This study provided in vivo functional evidence for the causality of G932C substitution mutation of CHS1 with buprofezin resistance and valuable information for facilitating the development of resistance management strategies in N. lugens. This is the first example of using CRISPR/Cas9 gene-editing technology in a hemipteran insect to directly confirm the role of a candidate target site mutation in insecticide resistance.


Asunto(s)
Sistemas CRISPR-Cas , Quitina Sintasa , Hemípteros , Resistencia a los Insecticidas , Insecticidas , Tiadiazinas , Animales , Hemípteros/genética , Resistencia a los Insecticidas/genética , Tiadiazinas/farmacología , Quitina Sintasa/genética , Insecticidas/farmacología , Mutación , Proteínas de Insectos/genética , Proteínas de Insectos/metabolismo , Técnicas de Sustitución del Gen , Femenino , Masculino
10.
Am J Ther ; 31(4): e398-e409, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38710029

RESUMEN

BACKGROUND: Chronic kidney disease can lead to end-stage renal disease, and the prevalence is increasing. Many patients starting hemodialysis require central venous catheters (CVCs). Catheter-related bloodstream infections (CRBSIs) are a common complication and lead to significant morbidity and mortality. Interventions to prevent CRBSI include antimicrobial lock therapy but concern for the development of antimicrobial resistance and adverse effects. Nonantimicrobial antiseptics as catheter lock solutions have also been used. Taurolidine and heparin catheter lock solution is first approved by the Food and Drug Administration for the prevention of CRBSI in patients on hemodialysis. Taurolidine has a unique mechanism of action and favorable safety profile. MECHANISM OF ACTION, PHARMACODYNAMICS, AND PHARMACOKINETICS: Taurolidine and heparin catheter lock solution have both antimicrobial and anticoagulant properties. Taurolidine is derivative of the amino acid taurine, and heparin is derived from porcine intestinal mucosa. Taurolidine not only damages microbial cell walls but also prevents the adherence of microorganisms to biological surfaces, preventing biofilm formation. Taurolidine and heparin catheter lock solution is intended to be used intraluminally within the catheter and should be aspirated. Because it is used locally, limited pharmacokinetic and pharmacodynamic data are available. CLINICAL TRIALS: The LOCK-IT-100 trial is a randomized, double-blind, phase 3 study, which included 795 end-stage renal disease patients on hemodialysis with CVC. Taurolidine and heparin was compared with the control heparin alone. The results of the study showed a 71% risk reduction in CRBSI for taurolidine and heparin arm (95% confident interval, 38%-86%, P = 0.0006). Other studies have also shown that taurolidine lock solution leads to decreased CRBSI episodes. Several systematic reviews and meta-analysis consisted of taurolidine in adult, and pediatric populations also showed reduction in the incidence of CRBSIs. THERAPEUTIC ADVANCE: Taurolidine and heparin lock solution represents a novel preventive strategy for those undergoing hemodialysis through a CVC by reducing the risk of CRBSI. This is significant progress because there are no other similar options available for patients for whom catheters are the only options for their life-saving treatment.


Asunto(s)
Anticoagulantes , Infecciones Relacionadas con Catéteres , Catéteres Venosos Centrales , Heparina , Diálisis Renal , Taurina , Tiadiazinas , Taurina/análogos & derivados , Taurina/farmacología , Taurina/administración & dosificación , Humanos , Heparina/administración & dosificación , Heparina/farmacología , Diálisis Renal/instrumentación , Diálisis Renal/métodos , Diálisis Renal/efectos adversos , Tiadiazinas/farmacología , Tiadiazinas/administración & dosificación , Catéteres Venosos Centrales/efectos adversos , Infecciones Relacionadas con Catéteres/prevención & control , Anticoagulantes/administración & dosificación , Anticoagulantes/farmacología , Cateterismo Venoso Central/efectos adversos , Ensayos Clínicos Controlados Aleatorios como Asunto , Fallo Renal Crónico/terapia , Antiinfecciosos Locales/administración & dosificación , Antiinfecciosos Locales/farmacología
11.
Nutr Hosp ; 41(3): 702-705, 2024 Jun 27.
Artículo en Español | MEDLINE | ID: mdl-38726617

RESUMEN

Introduction: Objectives: the prevention of central line-associated bloodstream infections is a critical aspect of care for patients with intestinal failure who are treated with parenteral nutrition. The use of taurolidine in this context is becoming increasingly popular, however there is a lack of standardization in its pediatric application. The objective of this work is to develop a guide to support its prescription. Methodology: the guide is based on a review of the literature and expert opinions from the Intestinal Failure Group of the SEGHNP. It was developed through a survey distributed to all its members, addressing aspects of usual practice with this lock solution. Results: this manuscript presents general recommendations concerning taurolidine indications, commercial presentations, appropriate forms of administration, use in special situations, adverse reactions, and contraindications in the pediatric population Conclusions: taurolidine is emerging as the primary lock solution used to prevent central line-associated bloodstream infections, proving to be safe and effective. This guide aims to optimize and standardize its use in pediatrics.


Introducción: Objetivo: la prevención de las infecciones asociadas a catéter ocupa un papel fundamental en los cuidados del paciente en situación de fracaso intestinal en tratamiento con nutrición parenteral. El empleo del sellado del catéter con taurolidina con ese fin se ha generalizado sin que exista una estandarización sobre su uso en población pediátrica. El objetivo de este trabajo es elaborar una guía clínica que sirva de apoyo en su utilización. Métodos: la guía se basa en una revisión de la literatura y en la opinión de expertos del Grupo de Trabajo de Fracaso Intestinal de la SEGHNP recogida a través de una encuesta realizada a todos sus integrantes sobre aspectos de la práctica habitual con este sellado. Resultados: este manuscrito expone unas recomendaciones en cuanto a las indicaciones, presentaciones comerciales disponibles, forma adecuada de administración, uso en situaciones especiales, reacciones adversas y contraindicaciones de la taurolidina en población pediátrica. Conclusiones: el sellado con taurolidina para la prevención de la infección asociada a catéter venoso central se ha mostrado como un tratamiento eficaz y seguro. La presente guía pretender optimizar y homogeneizar su uso en pediatría.


Asunto(s)
Insuficiencia Intestinal , Nutrición Parenteral , Taurina , Tiadiazinas , Humanos , Tiadiazinas/uso terapéutico , Tiadiazinas/efectos adversos , Niño , Taurina/análogos & derivados , Taurina/uso terapéutico , Nutrición Parenteral/normas , Nutrición Parenteral/métodos , Insuficiencia Intestinal/terapia , Infecciones Relacionadas con Catéteres/prevención & control , Cateterismo Venoso Central/efectos adversos , Antiinfecciosos/uso terapéutico , Lactante , Preescolar
12.
J Agric Food Chem ; 72(20): 11369-11380, 2024 May 22.
Artículo en Inglés | MEDLINE | ID: mdl-38727083

RESUMEN

In keeping with our investigation, a simple and practical synthesis of novel heterocyclic compounds with a sulfamoyl moiety that can be employed as insecticidal agents was reported. The compound 2-hydrazinyl-N-(4-sulfamoylphenyl)-2-thioxoacetamide 1 was coupled smoothly with triethylorthoformate or a variety of halo compounds, namely phenacyl chloride, chloroacetyl chloride, chloroacetaldehyde, chloroacetone, 1,3-dichloropropane, 1,2-dichloroethane, ethyl chloroformate, 2,3-dichloro-1,4-naphthoquinone, and chloroanil respectively, which afforded the 1,3,4-thiadiazole and 1,3,4-thiadiazine derivatives. The new products structure was determined using elemental and spectral analysis. Under laboratory conditions, the biological and toxicological effects of the synthetic compounds were also evaluated as insecticides against Spodoptera littoralis (Boisd.). Compounds 3 and 5 had LC50 values of 6.42 and 6.90 mg/L, respectively. The investigated compounds (from 2 to 11) had been undergoing molecular docking investigation for prediction of the optimal arrangement and strength of binding between the ligand (herein, the investigated compounds (from 2 to 11)) and a receptor (herein, the 2CH5) molecule. The binding affinity within docking score (S, kcal/mol) ranged between -8.23 (for compound 5), -8.12 (for compound 3) and -8.03 (for compound 9) to -6.01 (for compound 8). These compounds were shown to have a variety of binding interactions within the 2CH5 active site, as evidenced by protein-ligand docking configurations. This study gives evidence that those compounds have 2CH5-inhibitory capabilities and hence may be used for 2CH5-targeting development. Furthermore, the three top-ranked compounds (5, 3, and 9) and the standard buprofezin were subjected to density functional theory (DFT) analysis. The highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) energy difference (ΔE) of compounds 5, 3, and 9 was found to be comparable to that of buprofezin. These findings highlighted the potential and relevance of charge transfer at the molecular level.


Asunto(s)
Diseño de Fármacos , Insecticidas , Simulación del Acoplamiento Molecular , Spodoptera , Tiadiazinas , Tiadiazoles , Animales , Insecticidas/química , Insecticidas/síntesis química , Insecticidas/farmacología , Spodoptera/efectos de los fármacos , Tiadiazoles/química , Tiadiazoles/farmacología , Tiadiazoles/síntesis química , Tiadiazinas/química , Tiadiazinas/farmacología , Tiadiazinas/síntesis química , Relación Estructura-Actividad , Sulfonamidas/química , Sulfonamidas/farmacología , Sulfonamidas/síntesis química , Proteínas de Insectos/química , Bencenosulfonamidas , Estructura Molecular , Anhidrasa Carbónica II/antagonistas & inhibidores , Anhidrasa Carbónica II/metabolismo , Anhidrasa Carbónica II/química
13.
JPEN J Parenter Enteral Nutr ; 48(4): 486-494, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38605559

RESUMEN

BACKGROUND: Children with chronic IF require long-term home parenteral nutrition (HPN), administered through a central venous catheter. Catheter-related bloodstream infection (CRBSI) with Staphylococcus aureus is known to be a serious infection with a high mortality rate and risk of complications. A standardized protocol on the management of S aureus CRBSIs in children receiving HPN is lacking. The aim of this study is to evaluate the effectiveness and safety of the current management in an HPN expertise center in the Netherlands. METHODS: We performed a retrospective descriptive cohort study between 2013 and 2022 on children 0-18 years of age with chronic IF requiring long-term HPN. Our primary outcomes were the incidence of S aureus CRBSI per 1000 catheter days, catheter salvage attempt rate, and successful catheter salvage rate. Our secondary outcomes included complications and mortality. RESULTS: A total of 74 patients (39 male; 53%) were included, covering 327.8 catheter years. Twenty-eight patients (38%) had a total of 52 S aureus CRBSIs, with an incidence rate of 0.4 per 1000 catheter days. The catheter salvage attempt rate was 44% (23/52). The successful catheter salvage rate was 100%. No relapse occurred, and no removal was needed after catheter salvage. All complications that occurred were already present at admission before the decision to remove the catheter or not. No patients died because of an S aureus CRBSI. CONCLUSION: Catheter salvage in S aureus CRBSIs in children receiving HPN can be attempted after careful consideration by a multidisciplinary team in an HPN expertise center.


Asunto(s)
Infecciones Relacionadas con Catéteres , Insuficiencia Intestinal , Nutrición Parenteral en el Domicilio , Infecciones Estafilocócicas , Staphylococcus aureus , Taurina/análogos & derivados , Tiadiazinas , Humanos , Nutrición Parenteral en el Domicilio/métodos , Nutrición Parenteral en el Domicilio/efectos adversos , Masculino , Infecciones Relacionadas con Catéteres/prevención & control , Infecciones Relacionadas con Catéteres/microbiología , Infecciones Relacionadas con Catéteres/epidemiología , Estudios Retrospectivos , Femenino , Niño , Preescolar , Lactante , Infecciones Estafilocócicas/prevención & control , Adolescente , Países Bajos , Insuficiencia Intestinal/terapia , Recién Nacido , Catéteres Venosos Centrales/efectos adversos , Catéteres Venosos Centrales/microbiología , Enfermedad Crónica , Incidencia , Remoción de Dispositivos , Estudios de Cohortes , Cateterismo Venoso Central/efectos adversos , Catéteres de Permanencia/efectos adversos , Catéteres de Permanencia/microbiología , Bacteriemia/prevención & control , Bacteriemia/epidemiología , Bacteriemia/etiología
15.
Sci Rep ; 14(1): 5407, 2024 03 05.
Artículo en Inglés | MEDLINE | ID: mdl-38443552

RESUMEN

Dazomet is a dry powder formulation that releases toxic gas containing methyl isothiocyanate, which controls soil-borne pests and weeds, improving crop yields when applied to moist soils. To explore the efficacy of dazomet fumigation in the cultivation of the perennial herb Codonopsis pilosula, four typical cultivars (G1, G2, W1 and TCK) in Gansu Province were selected for seedling cultivation after soil fumigation (F) by dazomet, and non-fumigated soil was used as a control (CK). The experiments took 2 years to complete. The functional diversity of the soil enzymes and microorganisms, seedling emergence and physiological characteristics, and the quality and yield of Codonopsis seedlings and Radix were assessed. The results showed that the seed emergence rate, seedling re-green rate and several antioxidant enzymatic activities improved in the treatments involving soil fumigation with dazomet, and membrane lipid peroxidation in the seedlings decreased. On average, compared with those of the respective controls, the root viability and yield of the seedlings of the tested cultivars also increased by 34.87% and 42.4%, respectively, and the incidence of root rot in the seedlings was reduced by 83.9%, compared with their respective controls. After harvest, the yield increased by 23.9%, the incidence of root rot decreased by 61.3%, increase in yield and a 61.3% reduction in incidence, and the medicinal materials were determined to be safe and residue-free. The effects of fumigation were cultivar-specific and were especially prominent in G2. Therefore, soil fumigation with dazomet could improve the quality and productivity of Codonopsis pilosula seedlings. Taken together, these findings suggest that when herbs are bred by seedling transplantation, especially cultivars of good quality but poor resistance or species with rare germplasm resources, soil fumigation provides a way to improve cultivation effectiveness and, more importantly, ensures the probability of successfully breeding the species.


Asunto(s)
Codonopsis , Tiadiazinas , Fumigación , Plantones , Fitomejoramiento , Suelo
16.
Molecules ; 29(6)2024 Mar 16.
Artículo en Inglés | MEDLINE | ID: mdl-38542962

RESUMEN

This review article examines the synthetic pathways for triazolothiadiazine derivatives, such as triazolo[3,4-b]thiadiazines, triazolo[5,1-b]thiadiazines, and triazolo[4,3-c]thiadiazines, originating from triazole derivatives, thiadiazine derivatives, or thiocarbohydrazide. The triazolothiadiazine derivatives exhibit several biological actions, including antibacterial, anticancer, antiviral, antiproliferative, analgesic, anti-inflammatory, and antioxidant properties. The review article aims to assist researchers in creating new biologically active compounds for designing target-oriented triazolothiadiazine-based medicines to treat multifunctional disorders.


Asunto(s)
Tiadiazinas , Tiadiazinas/farmacología , Pruebas de Sensibilidad Microbiana , Antibacterianos/farmacología , Analgésicos/farmacología , Triazoles/farmacología
17.
Pestic Biochem Physiol ; 199: 105798, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38458668

RESUMEN

Spiders, the major predatory enemies of insect pests in fields, are vulnerable to insecticides. In this study, we observed that the recommended dose of buprofezin delayed the molting of the pond wolf spider Pardosa pseudoannulata, although it had no lethal effect on the spiders. Since buprofezin is an insect chitin biosynthesis inhibitor, we identified two chitin synthase genes (PpCHS1 and PpCHS2) in P. pseudoannulata. Tissue-specific expression profiling showed that PpCHS1 was most highly expressed in cuticle. In contrast, PpCHS2 showed highest mRNA levels in the midgut and fat body. RNAi knockdown of PpCHS1 significantly delayed the molting of 12-days old spiderlings, whereas no significant effect on the molting was observed in the PpCHS2-silencing spiderlings. The expression of PpCHS1 was significantly suppressed in the spiderlings treated with buprofezin, but rescued by exogenous ecdysteroid ponasterone A (PA). Consistent with this result, the molting delay caused by buprofezin was also rescued by PA. The results revealed that buprofezin delayed the molting of spiders by suppressing PpCHS1 expression, which will benefit the protection of P. pseudoannulate and related spider species.


Asunto(s)
Animales Ponzoñosos , Quitina Sintasa , Arañas , Tiadiazinas , Animales , Quitina Sintasa/genética , Quitina Sintasa/metabolismo , Muda/genética , Insectos , Arañas/genética , Arañas/metabolismo , Quitina/metabolismo
18.
Neotrop Entomol ; 53(2): 383-390, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38228816

RESUMEN

Reduced-risk insecticides and mirid predators have been used to control Bemisia tabaci (Gennadius) (Hemiptera: Aleyrodidae) in tomato crops. However, even when causing low mortality to the beneficial insects, these products might cause side effects. This study investigated the sublethal and transgenerational effects of buprofezin, cyantraniliprole, and spiromesifen on Macrolophus basicornis (Stal) (Hemiptera: Miridae). After 72 h of exposure of third-instar nymphs and adults to residues on tomato leaves, adult couples were formed and kept in cages with residue-free tomato leaves. The leaves were changed every 48 h and the offspring were assessed in 6 different periods. Body size was assessed by measuring the hind-tibia length of adults (F0) from exposed nymphs and in three different offspring groups. None of the insecticide residues caused a reduction on offspring populations or affected the body size of adults in generation F0. Regardless, buprofezin and spiromesifen reduced the tibia length of adults (F1) from exposed nymphs assayed in the third mating period. Cyantraniliprole did not affect any parameter and could be recommended for control of B. tabaci in association with M. basicornis releases. This study may contribute to future field assays of the compatibility of these insecticides with M. basicornis.


Asunto(s)
Hemípteros , Heterópteros , Insecticidas , Pirazoles , Solanum lycopersicum , Compuestos de Espiro , Tiadiazinas , ortoaminobenzoatos , Animales , Insecticidas/farmacología , Ninfa
19.
Toxicol Sci ; 198(2): 246-259, 2024 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-38237923

RESUMEN

Early developmental exposure to environmental toxicants may play a role in the risk for developing autism. A variety of pesticides have direct effects on retinoic acid (RA) signaling and as RA signaling has important roles in neurodevelopment, such compounds may cause developmental neurotoxicity through an overlapping adverse outcome pathway. It is hypothesized that a pesticide's embryonic effects on retinoid function may correspond with neurobehavioral disruption later in development. In the current studies, we determined the effects of RA-acting pesticides on neurobehavioral development in zebrafish. Buprofezin and imazalil caused generalized hypoactivity in the larval motility test, whereas chlorothalonil and endosulfan I led to selective hypoactivity and hyperactivity, respectively. With buprofezin, chlorothalonil, and imazalil, hypoactivity and/or novel anxiety-like behaviors persisted in adulthood and buprofezin additionally decreased social attraction responses in adulthood. Endosulfan I did not produce significant adult behavioral effects. Using qPCR analyses of adult brain tissue, we observed treatment-induced alterations in RA synthesis or catabolic genes, indicating persistent changes in RA homeostasis. These changes were compound-specific, with respect to expression directionality, and potential patterns of homeostatic disruption. Results suggest the likely persistence of disruptions in RA signaling well into adulthood and may represent compensatory mechanisms following early life stage exposures. This study demonstrates that early developmental exposure to environmental toxicants that interfere with RA signaling causes short as well as long-term behavioral disruption in a well-established zebrafish behavioral model and expand upon the meaning of the RA adverse outcome pathway, indicating that observed effects likely correspond with the nature of underlying homeostatic effects.


Asunto(s)
Nitrilos , Plaguicidas , Tiadiazinas , Pez Cebra , Animales , Tretinoina/toxicidad , Retinoides/farmacología , Plaguicidas/metabolismo , Endosulfano , Conducta Animal
20.
J Hosp Infect ; 143: 76-81, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-37972710

RESUMEN

BACKGROUND: Taurolidine lock, a technique used to prevent or treat catheter-related bloodstream infection (CRBSI), is effective in adult and paediatric patients but has been described rarely in neonates. The aim of this descriptive retrospective study, was to determine the feasibility and direct outcomes of prophylactic and therapeutic taurolidine locks in term and preterm neonates. METHODS: We implemented the use of therapeutic taurolidine lock in addition to antibiotic treatment with the aim of catheter salvage in critical neonates with difficult vascular access (group 1). In addition, we introduced taurolidine lock as a preventive measure in neonates with a central venous catheter (CVC) at high risk of developing CRBSI (group 2). Every 24 h (in the treatment group) a 2% taurolidine solution was injected and the catheter locked for at least 120 min, until infection clearance (group 1). In the preventive group, the catheter was locked for 30 min every 48 h until CVC removal (group 2). FINDINGS: Thirty-seven neonates who received taurolidine were included in this study. We did not observe any major adverse events. In group 1 (21 cases), clinical symptom disappearance and bacteraemia clearance were achieved without catheter removal in 18 cases (85.7%); in the other three neonates the catheter was removed shortly after the start of the locks as it was possible to replace the CVC. In group 2 (16 neonates), no CRBSI was observed during the duration of the catheter placement. CONCLUSIONS: In this retrospective study, taurolidine was successfully used in neonates both for prevention and treatment of CRBSI, without major undesired effects. A larger cohort and a randomized clinical trial is warranted in order to establish its efficacy and safety in neonates.


Asunto(s)
Bacteriemia , Infecciones Relacionadas con Catéteres , Cateterismo Venoso Central , Catéteres Venosos Centrales , Taurina/análogos & derivados , Tiadiazinas , Adulto , Recién Nacido , Humanos , Niño , Estudios de Factibilidad , Estudios Retrospectivos , Infecciones Relacionadas con Catéteres/tratamiento farmacológico , Infecciones Relacionadas con Catéteres/prevención & control , Infecciones Relacionadas con Catéteres/diagnóstico , Catéteres Venosos Centrales/efectos adversos , Cateterismo Venoso Central/efectos adversos , Bacteriemia/tratamiento farmacológico , Bacteriemia/prevención & control
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