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1.
Org Lett ; 2024 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-39465911

RESUMO

Herein, we describe a dual catalytic strategy that employs dihydroquinazolinones, derived from ketone analogs, as versatile intermediates for acylation via α C-C cleavage with 2-pyridyl esters, facilitating the efficient synthesis of a variety of ketones. The reaction accommodates a wide range of ketones and carboxylic acids, showing tolerance to various functional groups. The versatility of this synthetic technique is further highlighted through its application in the late-stage modification of pharmaceuticals and biologically active natural products.

2.
Foods ; 13(17)2024 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-39272541

RESUMO

Post-harvest selection of high-quality Sichuan pepper is a critical step in the production process. To achieve this, a visual system needs to analyze Sichuan pepper with varying postures and maturity levels. To quickly and accurately sort high-quality fresh Sichuan pepper, this study proposes a multi-scale frequency domain feature fusion module (MSF3M) and a multi-scale dual-domain feature fusion module (MS-DFFM) to construct a multi-scale, multi-domain fusion algorithm for feature fusion of Sichuan pepper images. The MultiDomain YOLOv8 Model network is then built to segment and classify the target Sichuan pepper, distinguishing the maturity level of individual Sichuan peppercorns. A selection method based on the average local pixel value difference is proposed for sorting high-quality fresh Sichuan pepper. Experimental results show that the MultiDomain YOLOv8-seg achieves an mAP50 of 88.8% for the segmentation of fresh Sichuan pepper, with a model size of only 5.84 MB. The MultiDomain YOLOv8-cls excels in Sichuan pepper maturity classification, with an accuracy of 98.34%. Compared to the YOLOv8 baseline model, the MultiDomain YOLOv8 model offers higher accuracy and a more lightweight structure, making it highly effective in reducing misjudgments and enhancing post-harvest processing efficiency in agricultural applications, ultimately increasing producer profits.

3.
Org Lett ; 26(38): 8063-8068, 2024 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-39283009

RESUMO

Pyridines and cyclopropanes are important structural units in chemistry. Herein, we introduce a photoredox-catalyzed approach for the ring opening and 1,3-oxypyridylation of aryl cyclopropanes using 4-cyanopyridines and carboxylic acids. This sequential process involves single-electron oxidation of the aryl cyclopropane, leading to nucleophilic ring opening and radical pyridylation at the benzylic position. The redox-neutral reaction exhibits high regioselectivity under mild reaction conditions, offering a broad substrate scope and wide applicability.

4.
ACS Omega ; 9(37): 38970-38988, 2024 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-39310156

RESUMO

Electrohydrodynamic atomization coating technology is well-suited for micro-/nanoscale thin-film additive manufacturing. However, there are still some challenges in quality control and parameter adjustment during the coating process. Especially when coating on nonconductive and nonhydrophilic substrates, film quality and thickness uniformity are difficult to control. This paper proposes an optimization strategy for enhancing the efficiency and quality of thin-film manufacturing on nonconductive, nonhydrophilic glass substrates. In this paper, a visual inspection system was developed for in situ inspection and identification of droplet deposition states in the substrate surface. Then, the statistical relationship between the operating parameters and the quality of the deposition state was analyzed by response surface methodology. On this basis, machine learning models and intelligent recommendation frameworks for small data sets were developed to rapidly optimize operating parameters and improve the quality of thin-film coating. Optimization strategy developed by applying the principles of statistical modeling, analysis of variance, and global optimization are more efficient and less costly than traditional parameter screening methods. The experimental results show that optimum deposition quality can be obtained with the recommended operating parameters. And, validation results show a 12.8% improvement in film thickness uniformity. At the same time, no mura defects appeared on the thin-film surface. The proposed optimization strategy can improve the efficiency and quality of additive manufacturing of micro and nano thin films and is beneficial for advancing industrial applications of the electrohydrodynamic atomization coating.

5.
Comput Biol Med ; 182: 109151, 2024 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-39332119

RESUMO

Detecting and segmenting unstained living adherent cells in differential interference contrast (DIC) images is crucial in biomedical research, such as cell microinjection, cell tracking, cell activity characterization, and revealing cell phenotypic transition dynamics. We present a robust approach, starting with dataset transformation. We curated 520 pairs of DIC images, containing 12,198 HepG2 cells, with ground truth annotations. The original dataset was randomly split into training, validation, and test sets. Rotations were applied to images in the training set, creating an interim "α set." Similar transformations formed "ß" and "γ sets" for validation and test data. The α set trained a Mask R-CNN, while the ß set produced predictions, subsequently filtered and categorized. A residual network (ResNet) classifier determined mask retention. The γ set underwent iterative processing, yielding final segmentation. Our method achieved a weighted average of 0.567 in average precision (AP)0.75bbox and 0.673 in AP0.75segm, both outperforming major algorithms for cell detection and segmentation. Visualization also revealed that our method excels in practicality, accurately capturing nearly every cell, a marked improvement over alternatives.

6.
Small ; : e2402564, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-39087370

RESUMO

For materials with coexisting phases, the transition from a random to an ordered distribution of materials often generates new mechanisms. Although the magnetic confinement effect has improved the electromagnetic (EM) performance, the transition from random to ordered magnetic confinement positions remains a synthetic challenge, and the underlying mechanisms are still unclear. Herein, precise control of magnetic nanoparticles is achieved through a spatial confinement growth strategy, preparing five different modalities of magnetic confined carbon fiber materials, effectively inhibiting magnetic agglomeration. Systematic studies have shown that the magnetic confinement network can refine CoNi NPs size and enhance strong magnetic coupling interactions. Compared to CoNi@HCNFs on the hollow carbon fibers (HCNFs) outer surface, HCNFs@CoNi constructed on the inner surface induce stronger spatial charge polarization relaxation at the interface and exhibit stronger magnetic coupling interactions at the inner surface due to the high-density magnetic coupling units at the micro/nanoscale, thereby respectively enhancing dielectric and magnetic losses. Remarkably, they achieve a minimum reflection loss (RLmin) of -64.54 dB and an absorption bandwidth of 5.60 GHz at a thickness of 1.77 mm. This work reveals the microscale mechanism of magnetic confinement-induced different polarization relaxation and magnetic response, providing a new strategy for designing magnetic materials.

7.
Food Chem ; 461: 140851, 2024 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-39167945

RESUMO

Reducing the allergenicity of edible insects is crucial for the comprehensive utilization of insect resources. Phospholipase A2 (PLA2) exists in various edible insects and mammalian tissues, which can cause serious allergic reactions. Herein, we constructed a magnetic nanocomposite with photo/chemical synergistic capability to mitigate the allergenicity of PLA2. The formation of prepared nanocomposite was systematically confirmed using various techniques. The nanocomposite exhibited uniform diameters, abundant functional groups, excellent magnetic capabilities. An effective photo/chemical method was established to reduce the allergenicity of PLA2 in vitro. The feasibility of the method was demonstrated through circular dichroism, fluorescence spectrum and IgE-binding analysis. The allergenicity and IgE-binding effect of PLA2 were significantly reduced due to conformational changes after nanomaterial treatment. These results demonstrate the sensitivity and effectiveness a strategy for reducing PLA2 allergenicity, providing a basis for development of nanomaterials to reduce the risk of novel food allergies in response to edible insect products.


Assuntos
Alérgenos , Fosfolipases A2 , Fosfolipases A2/química , Fosfolipases A2/imunologia , Alérgenos/imunologia , Alérgenos/química , Animais , Humanos , Hipersensibilidade Alimentar/imunologia , Hipersensibilidade Alimentar/prevenção & controle , Nanoestruturas/química , Imunoglobulina E/imunologia , Proteínas de Insetos/imunologia , Proteínas de Insetos/química , Nanocompostos/química , Insetos Comestíveis/química , Insetos Comestíveis/imunologia
8.
Carbohydr Polym ; 343: 122445, 2024 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-39174125

RESUMO

The application of novel insect proteins as future food resources in the food field has attracted more and more attention. In this study, a biodegradable antibacterial food packaging material with beneficial mechanical properties was developed using Tenebrio molitor larvae protein (TMP), chitosan (CS) and propolis ethanol extract (PEE) as raw materials. PEE was uniformly dispersed in the film matrix and the composite films showed excellent homogeneity and compatibility. There are strong intermolecular hydrogen bond interactions between CS, TMP, and PEE in the films, which exhibit the structure characteristics of amorphous materials. Compared with CS/TMP film, the addition of 3 % PEE significantly enhanced the elongation at break (34.23 %), water vapor barrier property (22.94 %), thermal stability (45.84 %), surface hydrophobicity (20.25 %), and biodegradability of the composite film. The composite film has strong antioxidant and antimicrobial properties, which were enhanced with the increase of PEE content. These biodegradable films offer an eco-friendly end-of-life option when buried in soil. Composite films can effectively delay the spoilage of strawberries and extend the shelf life of strawberries. Biodegradable active packaging film developed with insect protein and chitosan can be used as a substitute for petroleum-based packaging materials, and has broad application prospects in the field of fruits preservation.


Assuntos
Quitosana , Embalagem de Alimentos , Proteínas de Insetos , Larva , Própole , Tenebrio , Quitosana/química , Quitosana/farmacologia , Embalagem de Alimentos/métodos , Animais , Tenebrio/química , Própole/química , Própole/farmacologia , Larva/efeitos dos fármacos , Proteínas de Insetos/química , Antibacterianos/farmacologia , Antibacterianos/química , Etanol/química , Antioxidantes/química , Antioxidantes/farmacologia , Interações Hidrofóbicas e Hidrofílicas
9.
Front Biosci (Landmark Ed) ; 29(8): 283, 2024 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-39206889

RESUMO

BACKGROUND: Humankind have been struggling with colorectal cancer (CRC) for long period with its rapid progression and invasive metastasis. By hyperactivating IL-6/STAT3 signaling, CRC facilitates the capacity of angiogenesis to plunder massive nutrients and develops gradually under harsh condition. METHODS: The Cancer Genome Atlas database was analyzed for acquiring interferon-γ inducible protein 10 (IFITM10) expression levels and their correlation with clinical outcomes. The cell angiogenic ability were assessed by Cell Counting Kit-8 (CCK-8) and tube formation assay. Immunofluorescence, Western blot, and enzyme-linked immunosorbent assay (ELISA) assay were using to assess potential mechanism. RESULTS: In our study, we find that IFITM10 is upregulated in CRC and is positively related with tumor angiogenesis. We also find that IFITM inhibition decreased STAT3 phosphorylation level and IFITM10-mediated angiogenesis depends on STAT3 activation. Furthermore, our data suggests that IFITM10 may be a key prognostic biomarker in colorectal cancer. CONCLUSION: Together, our study suggests that IFITM10 enhance angiogenesis through STAT3 activation during CRC progression, which highlighting its potency as a therapeutic target for colorectal cancer.


Assuntos
Neoplasias Colorretais , Progressão da Doença , Neovascularização Patológica , Fator de Transcrição STAT3 , Fator de Transcrição STAT3/metabolismo , Humanos , Neovascularização Patológica/metabolismo , Neovascularização Patológica/genética , Neoplasias Colorretais/patologia , Neoplasias Colorretais/metabolismo , Neoplasias Colorretais/genética , Neoplasias Colorretais/irrigação sanguínea , Linhagem Celular Tumoral , Transdução de Sinais , Regulação Neoplásica da Expressão Gênica , Células Endoteliais da Veia Umbilical Humana/metabolismo , Fosforilação , Prognóstico , Biomarcadores Tumorais/metabolismo , Biomarcadores Tumorais/genética , Angiogênese , Antígenos de Diferenciação
10.
Nano Lett ; 24(35): 10883-10891, 2024 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-39172995

RESUMO

The development of electronic skin (e-skin) emulating the human skin's three essential functions (perception, protection, and thermoregulation) has great potential for human-machine interfaces and intelligent robotics. However, existing studies mainly focus on perception. This study presents a novel, eco-friendly, mechanically robust e-skin replicating human skin's three essential functions. The e-skin is composed of Ti3C2Tx MXene, polypyrrole, and bacterial cellulose nanofibers, where the MXene nanoflakes form the matrix, the bacterial cellulose nanofibers act as the filler, and the polypyrrole serves as a conductive "cross-linker". This design allows customization of the electrical conductivity, microarchitecture, and mechanical properties, integrating sensing (perception), EMI shielding (protection), and thermal management (thermoregulation). The optimal e-skin can effectively sense various motions (including minuscule artery pulses), achieve an EMI shielding efficiency of 63.32 dB at 78 µm thickness, and regulate temperature up to 129 °C in 30 s at 2.4 V, demonstrating its potential for smart robotics in complex scenarios.


Assuntos
Condutividade Elétrica , Polímeros , Dispositivos Eletrônicos Vestíveis , Humanos , Polímeros/química , Pirróis/química , Nanofibras/química , Celulose/química , Pele/química , Regulação da Temperatura Corporal , Titânio/química , Robótica
11.
Food Chem ; 460(Pt 3): 140767, 2024 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-39142206

RESUMO

Developing highland barley products is complex, possibly due to the presence of ß-glucan in highland barley. This study aims to investigate the impact of ß-glucan on the physicochemical properties, microstructure, and molecular interactions of highland barley starch (HBS) during gelatinization and aging. Increasing the ß-glucan content significantly reduced peak viscosity, setback viscosity, and breakdown viscosity, indicating altered gelatinization behavior. The ß-glucan content increase caused a significant drop in peak viscosity. With 20% ß-glucan addition, it reduced by 883 mPa·s, nearly 38%. Rheological analysis showed a transition from a solid-like to a liquid-like texture or quality, ultimately leading to a shear-thinning behavior. Fourier-transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD) confirmed the interaction between HBS and ß-glucan via intermolecular hydrogen bonding, promoting the formation of double helical structures in starch. These findings provide a deeper understanding of the role of ß-glucan in the processing of highland barley, highlighting its influence on the starch's properties.


Assuntos
Hordeum , Reologia , Amido , beta-Glucanas , Hordeum/química , beta-Glucanas/química , Amido/química , Viscosidade , Difração de Raios X , Espectroscopia de Infravermelho com Transformada de Fourier , Ligação de Hidrogênio
12.
Front Plant Sci ; 15: 1415884, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39119504

RESUMO

The pollination process of kiwifruit flowers plays a crucial role in kiwifruit yield. Achieving accurate and rapid identification of the four stages of kiwifruit flowers is essential for enhancing pollination efficiency. In this study, to improve the efficiency of kiwifruit pollination, we propose a novel full-stage kiwifruit flower pollination detection algorithm named KIWI-YOLO, based on the fusion of frequency-domain features. Our algorithm leverages frequency-domain and spatial-domain information to improve recognition of contour-detailed features and integrates decision-making with contextual information. Additionally, we incorporate the Bi-Level Routing Attention (BRA) mechanism with C3 to enhance the algorithm's focus on critical areas, resulting in accurate, lightweight, and fast detection. The algorithm achieves a m A P 0.5 of 91.6% with only 1.8M parameters, the AP of the Female class and the Male class reaches 95% and 93.5%, which is an improvement of 3.8%, 1.2%, and 6.2% compared with the original algorithm. Furthermore, the Recall and F1-score of the algorithm are enhanced by 5.5% and 3.1%, respectively. Moreover, our model demonstrates significant advantages in detection speed, taking only 0.016s to process an image. The experimental results show that the algorithmic model proposed in this study can better assist the pollination of kiwifruit in the process of precision agriculture production and help the development of the kiwifruit industry.

13.
Food Chem ; 461: 140858, 2024 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-39173258

RESUMO

Thaumatin-like proteins (TLP), existing in various fruits, have allergenic and pro-inflammatory activities. The current research attempts to reduce the pro-inflammatory activity of litchi TLP (LcTLP) through high hydrostatic pressure (HHP). This study demonstrated that HHP (250-500 MPa, 5-10 min) was a potential technique to reduce the pro-inflammatory activity of LcTLP, which was attributed to the irreversible destruction of the active domain, ie., V-cleft. SDS-PAGE showed no change in the protein profile. Continuous HHP treatment promoted LcTLP unfolding and then reassembling (400 MPa was the transition pressure), and the content of ß-sheets decreased from 35.4% to 31.1%. HHP treatment could mitigate inflammatory responses of LcTLP, as confirmed by ELISA and western blot. Molecular dynamics simulations showed significant changes in the residue network under HHP, thereby affecting the V-cleft. These findings provide a theoretical explanation and structural insights into the HHP-induced reduction of pro-inflammatory activity of LcTLP.


Assuntos
Pressão Hidrostática , Inflamação , Litchi , Proteínas de Plantas , Proteínas de Plantas/química , Proteínas de Plantas/imunologia , Litchi/química , Inflamação/imunologia , Animais , Camundongos , Simulação de Dinâmica Molecular , Frutas/química , Frutas/imunologia , Células RAW 264.7 , Domínios Proteicos , Humanos
14.
Heliyon ; 10(14): e34527, 2024 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-39130435

RESUMO

Colorectal cancer (CRC) is the third leading cancer type worldwide and accounts for the second highest rate of cancer-related mortality. Liver metastasis significantly contributes to the mortality associated with CRC, but the fundamental mechanisms behind it remain unclear. Signal-induced proliferation-associated protein 1 (SIPA1), a GTPase activating protein, has been shown to promote metastasis in breast cancer. In this study, our objective was to explore the role of SIPA1 in regulating epithelial-mesenchymal transition (EMT) in CRC. The analysis of The Cancer Genome Atlas (TCGA) database revealed that the expression level of SIPA1 mRNA was notably upregulated and exhibited a positively correlated with EMT and STAT3 signaling pathways in CRC. Knockdown of SIPA1 impairs CRC cell proliferation and migration. Further studies on the reliance of SIPA1 on STAT3 signaling for EMT regulation have shown that SIPA1 stimulates the activation of STAT3, resulting in its nuclear translocation. The co-treatment of overexpressed SIPA1 with the STAT3 inhibitor STTITA has shown that SIPA1 regulates the expression of EMT-related markers through STAT3. Our study indicate that SIPA1 promotes CRC metastasis by activating the STAT3 signaling pathway, underscoring the potential of SIPA1 as a therapeutic target for metastatic CRC patients.

15.
Foods ; 13(14)2024 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-39063263

RESUMO

Lentinula edodes (L. edodes) is a globally popular edible mushroom because of its characteristic sulfur-containing flavor compounds. However, the formation of the volatile sulfur-containing compounds in the mycelium of L. edodes has not been studied. We found that there were also sulfur-containing aroma compounds in the mycelium of L. edodes, and the content and composition varied at different stages of mycelial growth and development. The γ-glutamyl-transpeptidase (GGT) and cysteine sulfoxide lyase (C-S lyase) related to the generation of sulfur compounds showed the highest activities in the 15-day sample. Candidate genes for the metabolism of volatile sulfur compounds in mycelium were screened using transcriptome analysis, including encoding the GGT enzyme, C-S lyase, fatty acid oxidase, HSP20, and P450 genes. The expression patterns of Leggt3 and Leccsl3 genes were consistent with the measured activities of GGT and C-S lyase during the cultivation of mycelium and molecular dynamics simulations showed that they could stably bind to the substrate. Our findings provide insights into the formation of sulfur-containing flavor compounds in L. edodes. The mycelium of L. edodes is suggested for use as material for the production of sulfur-containing flavor compounds.

16.
Nat Commun ; 15(1): 6138, 2024 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-39033166

RESUMO

Integration of functional fillers into liquid metals (LM) induces rheology modification, enabling the free-form shaping of LM at the micrometer scale. However, integrating non-chemically modified low-dimensional materials with LM to form stable and uniform dispersions remain a great challenge. Herein, we propose a solvent-assisted dispersion (SAD) method that utilizes the fragmentation and reintegration of LM in volatile solvents to engulf and disperse fillers. This method successfully integrates MXene uniformly into LM, achieving better internal connectivity than the conventional dry powder mixing (DPM) method. Consequently, the MXene/LM (MLM) coating exhibits high electromagnetic interference (EMI) shielding performance (105 dB at 20 µm, which is 1.6 times that of coatings prepared by DPM). Moreover, the rheological characteristic of MLM render it malleable and facilitates direct printing and adaptation to diverse structures. This study offers a convenient method for assembling LM with low-dimensional materials, paving the way for the development of multifunctional soft devices.

17.
ACS Appl Mater Interfaces ; 16(28): 37122-37130, 2024 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-38953852

RESUMO

Light weight, thinness, transparency, flexibility, and insulation are the key indicators for flexible electronic device substrates. The common flexible substrates are usually polymer materials, but their recycling is an overwhelming challenge. Meanwhile, paper substrates are limited in practical applications because of their poor mechanical and thermal stability. However, natural biomaterials have excellent mechanical properties and versatility thanks to their organic-inorganic multiscale structures, which inspired us to design an organic-inorganic nanocomposite film. For this purpose, a bio-inspired multiscale film was developed using cellulose nanofibers with abundant hydrophilic functional groups to assist in dispersing hydroxyapatite nanowires. The thickness of the biosustainable film is only 40 µm, and it incorporates distinctive mechanical properties (strength: 52.8 MPa; toughness: 0.88 MJ m-3) and excellent optical properties (transmittance: 80.0%; haze: 71.2%). Consequently, this film is optimal as a substrate employed for flexible sensors, which can transmit capacitance and resistance signals through wireless Bluetooth, showing an ultrasensitive response to pressure and humidity (for example, responding to finger pressing with 5000% signal change and exhaled water vapor with 4000% signal change). Therefore, the comprehensive performance of the biomimetic multiscale organic-inorganic composite film confers a prominent prospect in flexible electronics devices, food packaging, and plastic substitution.

19.
Int J Biol Macromol ; 275(Pt 1): 133675, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38971287

RESUMO

With growing concerns about postharvest spoilage of fruits, higher requirements have been placed on high-performance and sustainable active packaging materials. In this study, we prepared curcumin-based functional composite films using chitosan (CS) and Tenebrio molitor larvae protein (TMP) as the substrates. The effects of curcumin concentration on the structural and physicochemical properties of the composite films were determined. Curcumin was equally distributed in the polymer film through physical interactions. Furthermore, the curcumin composite film with 0.3 % addition exhibited a 27.39 % increase in elongation at break (EBA), a 37.04 % increase in the water vapor barrier, and strong UV-blocking properties and antioxidant activity compared with the control film (CS/TMP). The degradation experiment of the composite film on natural soil revealed that the composite film exhibited good biodegradability and environmental protection. Furthermore, the applicability of functional composite films for preserving blueberries was investigated. Compared with the control film and polyethylene (PE) films, the prepared composite films packaging treatment reduced the decay rate and weight loss rate of blueberries during storage, delayed softening and aging, and maintained the quality of blueberries. Using sustainable protein resources (TMP) and natural polysaccharides as packaging materials provides an economically, feasible and sustainable way to achieve the functional preservation of biomass materials.


Assuntos
Antioxidantes , Mirtilos Azuis (Planta) , Quitosana , Curcumina , Embalagem de Alimentos , Conservação de Alimentos , Larva , Tenebrio , Animais , Quitosana/química , Quitosana/farmacologia , Curcumina/química , Curcumina/farmacologia , Tenebrio/química , Tenebrio/efeitos dos fármacos , Embalagem de Alimentos/métodos , Mirtilos Azuis (Planta)/química , Antioxidantes/farmacologia , Antioxidantes/química , Conservação de Alimentos/métodos , Larva/efeitos dos fármacos , Proteínas de Insetos/química
20.
Colloids Surf B Biointerfaces ; 241: 113992, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38833960

RESUMO

In order to reduce the cardiotoxicity of doxorubicin (DOX) and improve its antitumor effect, dihydroartemisinin (DHA) and DOX prodrug (DOX-S-DHA) synthesized via a single sulfur bond was used with TEPP-46 to prepare nano-liposomes (DOX-S-DHA@TEPP-46 Lips). In which, TEPP-46 was expected to exert p53 bidirectional regulation to promote the synergistic antitumor effect of DOX and DHA while reducing cardiotoxicity. DOX-S-DHA@TEPP-46 Lips exhibited uniform particle size, good stability, and excellent redox-responsive activity. DOX-S-DHA@TEPP-46 Lips could significantly inhibit the proliferation of tumor cells, but had less cytotoxicity on normal cells. The presence of TEPP-46 increased the content of p53 protein, which further induced tumor cell apoptosis. DOX-S-DHA@TEPP-46 Lips had satisfactory long circulation to enhance the antitumor efficacy and reversed the cardiotoxicity of DOX in B16-F10 tumor-bearing mice. In conclusion, DOX-S-DHA@TEPP-46 Lips provides a new insight on creating sophisticated redox-sensitive nano-liposomes for cancer therapy as well as the decreased cardiotoxicity of DOX.


Assuntos
Artemisininas , Cardiotoxicidade , Doxorrubicina , Lipossomos , Pró-Fármacos , Animais , Artemisininas/química , Artemisininas/farmacologia , Artemisininas/administração & dosagem , Doxorrubicina/farmacologia , Doxorrubicina/química , Doxorrubicina/administração & dosagem , Pró-Fármacos/química , Pró-Fármacos/farmacologia , Camundongos , Lipossomos/química , Cardiotoxicidade/prevenção & controle , Proliferação de Células/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/administração & dosagem , Tamanho da Partícula , Nanopartículas/química , Sistemas de Liberação de Medicamentos , Camundongos Endogâmicos C57BL , Melanoma Experimental/tratamento farmacológico , Melanoma Experimental/patologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Linhagem Celular Tumoral
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