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AIMS: The aim of our work is to load Vinblastine drugs loaded on graphene quantum dots to improve its cytotoxicity on cancer cells and reduce it on the normal cell in the composites. Moreover, the GQDs-Vin composite significantly inhibited tumour growth in animals. METHODS: GQDs-Vin composites were prepared by homogenisation of GQDs and Vin solutions. The loading of Vin on GQDs in the composites was characterised by FTIR, PL, UV-vis spectra, and TEM. The cytotoxicity of GQDs, Vin, and GQDs-Vin composites was investigated on the Hela, HGC-27, A549, MCF-7, CCF-STTG1 cells and Vero by in vitro and in vivo methods. The difference in cellular structure and organelles in mice's livers in comparison between the control group and GQDs-Vin (1:5) groups was characterised by TEM. RESULTS: The diameter of the nanoparticles of GQDs-Vin composites in weight ratios 1:1, 1:3 and 1:5 w/w of 50-70 nm, 100-150 nm and â¼500nm, respectively, is larger than that of GQDs of 10-50nm. The in vitro results showed that GQDs not only improved the cytotoxicity of Vin to cancer cells but also decreased its cytotoxicity towards normal cells in the composites. The GQDs-Vin (1:5) composite exhibited a stronger tumour inhibition effect than Vin alone. The morphology of mice's livers showed the absence GQDs-Vin nanoparticles in the mice livers suggesting the lack of storage and the leakage from the liver without any toxicity. CONCLUSIONS: Results of the improved cytotoxicity of GQDs-Vin composite on cancer cells, its reduced cytotoxicity on normal cells and the significant inhibition on tumour growth of GQDs-Vin composite compared with Vin and GQDs alone may indicate a synergistic effect of Vin and GQDs in their composites for anticancer application.
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Grafite , Pontos Quânticos , Animais , Grafite/química , Grafite/farmacologia , Células HeLa , Humanos , Camundongos , Pontos Quânticos/química , VimblastinaRESUMO
1,4-Dihydroxy-2-naphthoic acid was used as a substrate for a straightforward five-step synthesis of 3-substituted 1H-benzo[g]isochromene-5,10-diones, with a Michael addition of N-acylmethylpyridinium ylides across 2-hydroxymethyl-1,4-naphthoquinone and a subsequent acid-mediated dehydratation of intermediate hemiacetals as the key steps. The obtained benzo[g]isochromene-5,10-diones were subsequently deployed for further synthetic elaboration to produce new 3,4-dihydrobenzo[g]isochromene-5,10-diones and (3,4-dihydro-)4a,10a-epoxybenzo[g]isochromene-5,10-diones. All compounds were screened for their cytotoxic and antimicrobial effects, revealing an interesting cytotoxic activity of 1H-benzo[g]isochromene-5,10-diones against different cancer cell lines.
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Compostos de Epóxi/síntese química , Compostos de Epóxi/farmacologia , Naftoquinonas/síntese química , Naftoquinonas/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Ácidos Carboxílicos/síntese química , Ácidos Carboxílicos/química , Ácidos Carboxílicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Compostos de Epóxi/química , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Naftalenos/síntese química , Naftalenos/química , Naftalenos/farmacologia , Naftoquinonas/química , Relação Estrutura-AtividadeRESUMO
In this Letter, the synthesis and the evaluation of the cytotoxicity of new hemiasterlin analogues were reported. The indole moiety was replaced respectively by benzofurane, naphthalene and 4-bromobenzene groups. Most of these derivatives possess strong cytotoxic activity on two human tumour cell lines (KB and Hep-G2), and some analogues showed comparable cytotoxic activity to that observed for paclitaxel and ellipticine, against KB and Hep-G2 cancer cell lines.
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Citotoxinas/química , Citotoxinas/toxicidade , Oligopeptídeos/química , Oligopeptídeos/toxicidade , Morte Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Células Hep G2 , Humanos , EstereoisomerismoRESUMO
Hydroxyapatite (HAp), a well-known biomaterial, has witnessed a remarkable evolution over the years, transforming from a simple biocompatible substance to an advanced functional material with a wide range of applications. This abstract provides an overview of the significant advancements in the field of HAp and its journey towards becoming a multifunctional material. Initially recognized for its exceptional biocompatibility and bioactivity, HAp gained prominence in the field of bone tissue engineering and dental applications. Its ability to integrate with surrounding tissues, promote cellular adhesion, and facilitate osseointegration made it an ideal candidate for various biomedical implants and coatings. As the understanding of HAp grew, researchers explored its potential beyond traditional biomaterial applications. With advances in material synthesis and engineering, HAp began to exhibit unique properties that extended its utility to other disciplines. Researchers successfully tailored the composition, morphology, and surface characteristics of HAp, leading to enhanced mechanical strength, controlled drug release capabilities, and improved biodegradability. These modifications enabled the utilization of HAp in drug delivery systems, biosensors, tissue engineering scaffolds, and regenerative medicine applications. Moreover, the exceptional biomineralization properties of HAp allowed for the incorporation of functional ions and molecules during synthesis, leading to the development of bioactive coatings and composites with specific therapeutic functionalities. These functionalized HAp materials have demonstrated promising results in antimicrobial coatings, controlled release systems for growth factors and therapeutic agents, and even as catalysts in chemical reactions. In recent years, HAp nanoparticles and nanostructured materials have emerged as a focal point of research due to their unique physicochemical properties and potential for targeted drug delivery, imaging, and theranostic applications. The ability to manipulate the size, shape, and surface chemistry of HAp at the nanoscale has paved the way for innovative approaches in personalized medicine and regenerative therapies. This abstract highlights the exceptional evolution of HAp, from a traditional biomaterial to an advanced functional material. The exploration of novel synthesis methods, surface modifications, and nanoengineering techniques has expanded the horizon of HAp applications, enabling its integration into diverse fields ranging from biomedicine to catalysis. Additionally, this manuscript discusses the emerging prospects of HAp-based materials in photocatalysis, sensing, and energy storage, showcasing its potential as an advanced functional material beyond the realm of biomedical applications. As research in this field progresses, the future holds tremendous potential for HAp-based materials to revolutionize medical treatments and contribute to the advancement of science and technology.
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Nanopartículas , Nanoestruturas , Materiais Biocompatíveis/farmacologia , Materiais Biocompatíveis/química , Durapatita/química , Nanopartículas/química , Osso e OssosRESUMO
Photoacoustic (PA) microscopy allows imaging of the soft biological tissue based on optical absorption contrast and spatial ultrasound resolution. One of the major applications of PA imaging is its characterization of microvasculature. However, the strong PA signal from skin layer overshadowed the subcutaneous blood vessels leading to indirectly reconstruct the PA images in human study. Addressing the present situation, we examined a deep learning (DL) automatic algorithm to achieve high-resolution and high-contrast segmentation for widening PA imaging applications. In this research, we propose a DL model based on modified U-Net for extracting the relationship features between amplitudes of the generated PA signal from skin and underlying vessels. This study illustrates the broader potential of hybrid complex network as an automatic segmentation tool for the in vivo PA imaging. With DL-infused solution, our result outperforms the previous studies with achieved real-time semantic segmentation on large-size high-resolution PA images.
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A reduced graphite oxide nanosheet electrode (RGOnS) was prepared as a sensor for amoxicillin (AMX) detection, an antibiotic commonly used in the livestock farm, by the square-wave adsorptive stripping voltammetry technique. Graphite oxide with nanosheet shape was produced from a graphite electrode by a chronoamperometry process at 5 V and then an electrochemical reduction process was carried out to form RGOnS with restored long-range conjugated networks and better conductivity. The electrodes were characterized by SEM, EDX, and FTIR spectroscopy. The RGOnS electrode prepared at an optimal reduction potential of -1 V for 120 s exhibits a larger electrochemical active surface area, and the obtained oxidation signal of AMX is approximately ten times higher than that of the pristine graphite electrode. The analytical conditions such as the pH of electrolyte and accumulation time were optimized. The calibration curve built under the optimal conditions provided a good linear relationship in the range of AMX concentration from 0.5-80 µM with the correlation coefficient of 0.9992. The limit of detection was calculated as 0.193 µM. Satisfactory results are obtained from the detection of the AMX in different samples using the prepared electrode.
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The present paper reports the fabrication of inverse opal photonic crystals (IOPCs) by using SiO2 spherical particles with a diameter of 300 nm as an opal photonic crystal template and poly(ethylene glycol) diacrylate (PEGDA) as an inverse opal material. Characteristics and fluorescence properties of the fabricated IOPCs were investigated by using the Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), reflection spectroscopy, and fluorescence microscopy. The results clearly showed that the IOPCs were formed comprising of air spheres with a diameter of â¼270 nm. The decrease in size led to a decrease in the average refractive indexes from 1.40 to 1.12, and a remarkable stopband blue shift for the IOPCs was thus achieved. In addition, the obtained results also showed a fluorescence enhancement over 7.7-fold for the Fluor® 488 dye infiltrated onto the IOPCs sample in comparison with onto the control sample.