RESUMEN
Double polymeric grafted layer is constructed by two steps of chemical reaction, in which two polymers had been used, respectively polydopamine (PDA) film and modified PASS (NH2-PASS) resin containing amine group, as the interphase in carbon fiber reinforced poly(arylene sulfide sulfone) (PASS) composite (CF/PASS) to work on enhancing the interfacial property. All the test results of chemical components and chemical structures on the carbon fiber surface show that the double polymeric grafted layer was constructed successfully with PDA and NH2-PASS chains. And obvious characteristics of thin PDA film and a polymer layer can be clearly seen in the morphology of modified carbon fiber. In addition to this, the obvious interphase and change in the thickness of interphase have been observed in the modulus distribution images of CF/PASS. The final superb performance is achieved by PASS composites with a double polymeric grafted layer, 27.2% and 198.6% superior to the original PASS composite for IFSS and ILSS, respectively. Moreover, the result also indicates that constructing a double polymeric grafted layer on a carbon fiber surface is a promising technique to modify carbon fiber for processing high-performance advanced thermoplastic composites and is more environmental friendly as well as convenient.
RESUMEN
RATIONALE: The aim of this study was to determine the effectiveness of intratumoral injection of chemotherapeutics in improving the quality of life and survival of patients with pancreatic carcinoma. PATIENT CONCERNS: We present a case series of 5 patients with unresectable pancreatic adenocarcinoma. DIAGNOSES: Patients diagnosed with unresectable poorly differentiated pancreatic ductal adenocarcinoma by intraoperative frozen biopsyor percutaneous biopsy. INTERVENTIONS: Five patients with unresectable pancreatic adenocarcinoma received a computed tomography-guided percutaneous intratumoral injection of gemcitabine plus cisplatin mixed with fibrin glue. OUTCOMES: Mean overall survival was 16.2â±â3.7 months. Local control rates were 100% and 80% at postoperative 3 and 6 months, respectively. Mean Visual Analogue Scale pain score decreased from 7.2â±â.84 preoperatively to 2â±â1.22 at postoperative 4 weeks. There were no complications associated with the procedure. LESSONS: Percutaneous intratumoral injection of gemcitabine plus cisplatin mixed with fibrin glue for advanced pancreatic may be safe and effective.
Asunto(s)
Adenocarcinoma/tratamiento farmacológico , Antineoplásicos/administración & dosificación , Protocolos de Quimioterapia Combinada Antineoplásica/administración & dosificación , Cisplatino/administración & dosificación , Desoxicitidina/análogos & derivados , Adhesivo de Tejido de Fibrina/administración & dosificación , Neoplasias Pancreáticas/tratamiento farmacológico , Adenocarcinoma/patología , Anciano , Desoxicitidina/administración & dosificación , Quimioterapia Combinada , Femenino , Humanos , Inyecciones Intralesiones , Masculino , Persona de Mediana Edad , Estadificación de Neoplasias , Neoplasias Pancreáticas/patología , GemcitabinaRESUMEN
Through a structure-based molecular hybridization approach, a series of novel quinazolinyl-diaryl urea derivatives were designed, synthesized, and screened for their in vitro antiproliferative activities against three cancer cell lines (HepG2, MGC-803, and A549). Six compounds (7 g, 7 m, 7 o, 8 e, 8 g, and 8 m) showed stronger activity against a certain cell line compared with the positive reference drugs sorafenib and gefitinib. Among the six compounds, 8 g exhibited the strongest activity. In particular, compound 8 g induced A549 apoptosis, arrested cell cycle at the G0/G1 phase, elevated intracellular reactive oxygen species level, and decreased mitochondrial membrane potential. This compound can also effectively regulate the expression of apoptosis- and cell cycle-related proteins, and influence the Raf/MEK/ERK pathway. Molecular docking and structure-activity relationship analyses revealed that it can bind well to the active site of the receptor c-Raf, which was consistent with the biological data. Therefore, compound 8 g may be a potent antitumor agent, representing a promising lead for further optimization.
Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Antineoplásicos/síntesis química , Apoptosis/efectos de los fármacos , Dominio Catalítico , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Técnicas de Química Sintética , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Células Hep G2/efectos de los fármacos , Humanos , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Simulación del Acoplamiento Molecular , Proteínas Proto-Oncogénicas c-raf/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Relación Estructura-Actividad , Urea/químicaRESUMEN
In this study, two series of 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives (compounds 5a-i and 6a-g) were synthesized. Their in vitro proliferation inhibitory activities against the A549 and NCI-H460 human non-small cell lung cancer (NSCLC) cell lines were evaluated. Their photophysical properties were measured. Among these target compounds, 5e exhibited the strongest antiproliferative activity by inducing apoptosis, arresting cell cycle, and elevating intracellular reactive oxygen species (ROS) level, suggesting that it may be a potent antitumor agent. In addition, compound 6g with very low cytotoxicity, demonstrated excellent fluorescence properties, which could be used as an effective fluorescence probe for biological imaging.