RESUMEN
In this study, a series of compounds with 1,2,4-oxadiazole core was designed and synthesized for the optimization of JC01, an anti-inflammatory hit identified from our in-house compound library using NF-κB pathway luciferase assay and NO production assay. All the synthetic compounds 1-29 have been screened for their anti-inflammatory effects by evaluating their inhibition against LPS-induced NO release, and compound 17 exhibited the highest activity. Western blotting and immunofluorescence analysis revealed that 17 prominently inhibited LPS-induced activation of NF-κB in RAW264.7 cells and blocked the phosphorylation of p65. Consistent with these results, it was found that 17 prevented the nuclear translocation of NF-κB induced by LPS. These data highlighted 17 as a promising anti-inflammatory agent by inhibiting NF-κB activity.
Asunto(s)
Antiinflamatorios/farmacología , Oxadiazoles/química , Transducción de Señal/efectos de los fármacos , Animales , Antiinflamatorios/síntesis química , Supervivencia Celular , Diseño de Fármacos , Interleucina-6/genética , Interleucina-6/metabolismo , Lipopolisacáridos/farmacología , Macrófagos/citología , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , FN-kappa B/metabolismo , Óxido Nítrico/metabolismo , Oxadiazoles/síntesis química , Oxadiazoles/farmacología , Fosforilación/efectos de los fármacos , Células RAW 264.7 , Relación Estructura-Actividad , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
The addition of toxic substances and poor durability severely limit the market applications of superhydrophobic coatings in the oil−water-separation industry, anti-icing, and self-cleaning surfaces. In order to solve the above problems, a stable, strong, fluorine-free superhydrophobic coating was prepared according to natural inspiration. In this study, polydivinylbenzene (PDVB) was produced by the hydrothermal method, and micro-nanoparticle clusters composed of PDVB particles of different sizes were prepared by controlling the ratio of raw materials, which was then attached to the substrate surface by a simple spraying technique. A rough coating with a lotus-leaf-like layered protruding structure was constructed by depositing particle clusters of different sizes. In the end, the prepared coating showed attractive superhydrophobicity, with a maximum contact angle (CA) that reached up to 160°. In addition, the coating had long-lasting superhydrophobic properties in various environments, such as common liquid and acidic and alkaline solutions. Moreover, in the oil−water-separation process, the superhydrophobic filter paper was still able to obtain a separation efficiency of more than 85% after being used 50 times, and it maintained a contact angle of >150°. At the same time, the coating had excellent dye resistance and self-cleaning performance.
RESUMEN
Cellulose has shown encouraging properties in many applications, such as energy storage, optical instrument and catalysis. In particular, cellulose films have shown potential applications in flexible transparent devices and are expected to replace indium-tin oxide (ITO). However, cellulose is highly hydrophilic and electrically insulating, which limits its scope of application. In this study, the conductivity (R s = 40.3 Ω sq-1), transparency (81.4%) and superhydrophobicity (static contact angle = 153.2°, sliding angle = 4.1°) of cellulose film (CTSC-P) are reported. First, before suction filtration to prepare the film, cellulose was oxidized to improve dispersibility and mechanical strength. Then, the obtained film was hydrophobically modified by grafting long-chain silanes on the surface, followed by electrospinning and electroless plating. In general, the design is an ingenious way to manufacture transparent, conductive, and super-hydrophobic films in the future, and is transformed into a flexible electronic technically feasible device.
RESUMEN
This study cloned the hemoglobin α1 from the marine teleost, the half-smooth tongue sole (Cynoglossus semilaevis), and then examined its expression under hypoxia exposure. The full-length of CsHb-α1 (594 bp) cDNA contains an open reading frame encoding 144 amino acids. Sequence analysis shows that the predicted CsHb-α1 amino acids shares high identities with that of other species. Real-time PCR showed that CsHb-α1 was highly expressed in the heart, liver, spleen, kidney and blood. Five to 120 min esposure and long-term (36 h) exposure to hypoxia (1.0 mg/L) significantly increased CsHb-α1 mRNA expression in most tissues compared to those fish held in normoxic conditions (dissolved oxygen (DO): 6.2 mg/L). These results suggested that the up-regulation of Hb-α1 is an important component for adaptation of half-smooth tongue sole to short-term hypoxia.