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1.
Bioorg Chem ; 97: 103670, 2020 04.
Artículo en Inglés | MEDLINE | ID: mdl-32088417

RESUMEN

Selective COX-2 inhibitor celecoxib was found directly inhibiting the growth of tested phytopathogenic fungi with the inhibitory rate ranging from 30 to 40% at 100 µg/ml. Lead optimization of celecoxib led to the identification of compound 12 among its derivatives as the most active antifungal candidate. The antifungal effect of compound 12 was supposed to be independent of COX-2 inhibition. Transcriptome profiling analysis of Fusarium graminearium (PH-1) treated with compound 12 brought about 406 up-regulated and 572 down-regulated differentially express genes (DEGs) respectively.


Asunto(s)
Celecoxib/análogos & derivados , Protección de Cultivos/métodos , Inhibidores de la Ciclooxigenasa 2/química , Fungicidas Industriales/química , Fusarium/efectos de los fármacos , Enfermedades de las Plantas/prevención & control , Celecoxib/toxicidad , Productos Agrícolas/microbiología , Inhibidores de la Ciclooxigenasa 2/toxicidad , Fungicidas Industriales/toxicidad , Fusarium/genética , Regulación Fúngica de la Expresión Génica/efectos de los fármacos , Enfermedades de las Plantas/microbiología , Transcriptoma/efectos de los fármacos
2.
ACS Appl Mater Interfaces ; 16(26): 33093-33105, 2024 Jul 03.
Artículo en Inglés | MEDLINE | ID: mdl-38884171

RESUMEN

The morphological features of materials significantly influence their interactions with cells, consequently affecting the cellular uptake of these materials. In this study, we examine the cellular uptake behavior of spherical metal-organic frameworks (MOFs) and petaloid MOFs, both possessing similar sizes and compositions. In comparison to spherical MOFs, dendritic cells (DCs) and macrophages exhibit superior phagocytic uptake of petaloid MOFs. Next, the results demonstrate that R848@petaloid MOFs more effectively promote the repolarization of tumor-associated macrophages (TAMs) from the M2 to M1 phenotype and the maturation of DCs. More importantly, the R848-loaded petaloid MOFs are found to significantly enhance the therapeutic effects of radiotherapy (RT) by eliciting antitumor responses. Furthermore, R848@petaloid MOFs combined with RT and αPD-L1 elicit a potent abscopal effect, effectively suppressing tumor metastasis. Therefore, this work proposes a new strategy to enhance the uptake of immunomodulators by immune cells through modulating the morphology of drug delivery carriers.


Asunto(s)
Imidazoles , Estructuras Metalorgánicas , Estructuras Metalorgánicas/química , Estructuras Metalorgánicas/farmacología , Ratones , Animales , Imidazoles/química , Imidazoles/farmacología , Células Dendríticas/efectos de los fármacos , Células Dendríticas/inmunología , Portadores de Fármacos/química , Antineoplásicos/química , Antineoplásicos/farmacología , Células RAW 264.7 , Línea Celular Tumoral , Ratones Endogámicos C57BL , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Macrófagos/inmunología , Femenino , Antígeno B7-H1/metabolismo , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Neoplasias/inmunología
3.
Biomimetics (Basel) ; 8(1)2023 Feb 06.
Artículo en Inglés | MEDLINE | ID: mdl-36810400

RESUMEN

In medical validation experiments, such as drug testing and clinical trials, 3D bioprinted biomimetic tissues, especially those containing blood vessels, can be used to replace animal models. The difficulty in the viability of printed biomimetic tissues, in general, lies in the provision of adequate oxygen and nutrients to the internal regions. This is to ensure normal cellular metabolic activity. The construction of a flow channel network in the tissue is an effective way to address this challenge by both allowing nutrients to diffuse and providing sufficient nutrients for internal cell growth and by removing metabolic waste in a timely manner. In this paper, a three-dimensional TPMS vascular flow channel network model was developed and simulated to analyse the effect of perfusion pressure on blood flow rate and vascular-like flow channel wall pressure when the perfusion pressure varies. Based on the simulation results, the in vitro perfusion culture parameters were optimised to improve the structure of the porous structure model of the vascular-like flow channel, avoiding perfusion failure due to unreasonable perfusion pressure settings or necrosis of cells without sufficient nutrients due to the lack of fluid passing through some of the channels, and the research work promotes the development of tissue engineering in vitro culture.

4.
Artículo en Inglés | MEDLINE | ID: mdl-35955016

RESUMEN

PURPOSE: To evaluate the impact of high-temperature environments on bus drivers' physiology and reaction times, and to provide a basis for driver occupational health management. METHODS: The physiological and reaction indexes of 24 bus drivers under different temperatures were investigated. The statistical analysis method was used to analyze the changes in drivers' physiological stress, the relationship between stress and response ability, and a safe driving time. The Kaplan-Meier survival function was used to analyze the survival rate of bus drivers under different temperatures and driving times. RESULTS: The results showed that body temperature, heart rate, physiological strain index (PSI), and reaction ability were significantly different among different compartment temperatures. PSI was positively correlated with reaction ability. The safe driving time was 80 min, 73 min, and 53 min, respectively, at 32 °C, 36 °C, and 40 °C. The survival rate decreased to less than 60% at 36 °C when driving continuously for 73 min; it decreased to 20% at 40 °C when driving for 53 min, and it was 0 for 75 min. CONCLUSIONS: High-temperature environments lead to heat stress of bus drivers, physiological indexes have changed significantly, and behavioral ability is also decreased. The higher the temperature, the lower the survival rate. Improvement measures can be taken from the aspects of convection, conduction, and behavior to ensure the bus driver's physiological health and driving safety under high temperatures and to improve the survival rate.


Asunto(s)
Conducción de Automóvil , Salud Laboral , Accidentes de Tránsito , Tiempo de Reacción , Tiempo (Meteorología)
5.
Ying Yong Sheng Tai Xue Bao ; 31(2): 493-500, 2020 Feb.
Artículo en Zh | MEDLINE | ID: mdl-32476342

RESUMEN

A split plot experiment was conducted in greenhouse to investigate the effects of irrigation lower limit and maize straw returning on the yield, quality, and water use efficiency (WUE) of tomato. Maize straw was applied for 1 (2018, A1), 2(2017, A2), and 3 (2016, A3) years at different amounts (0, 1.5×104, 3×104, 4.5×104 kg·hm-2) and different irrigation lower limits (50%θf, 60%θf, 70%θf, 80%θf, θf was the field water capacity). Variance analysis, entropy-weight and TOPSIS methods were used to examine the responses of yield, quality and water use efficiency (WUE) of tomato. The results showed that tomato yield was enhanced by the increases of irrigation lower limit. The maximum value of yield was observed in the 80%θf treatments, with the maximum average yield of 93.55 t·hm-2 in A1, 87.23 t·hm-2 in A2, and 99.34 t·hm-2 in A3, respectively. WUE and quality of tomato decreased with increasing irrigation lower limit. In the first year of straw returning, the maximum average yield of tomato was 99.60 t·hm-2 in straw returning 1.5×104 kg·hm-2 . In the second and third years, 4.5×104 kg·hm-2 straw returning had the highest average yield of tomato, which was 92.50 and 107.75 t·hm-2, respectively. The maximum WUE was observed with the straw returning of 1.5×104 kg·hm-2 in A1 and A2, while in the A3 treatment it happened in straw returning of 4.5×104 kg·hm-2. The quality index of tomato showed different trends with the increases of straw returning years and amount.


Asunto(s)
Solanum lycopersicum , Agua , Riego Agrícola , Agricultura , Fertilizantes , Suelo , Zea mays
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