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1.
Heliyon ; 10(1): e23223, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38148798

RESUMO

Macrophages play a crucial role in regulating inflammation and innate immune responses, and their polarization into distinct phenotypes, such as M1 and M2, is involved in various diseases. However, the specific role of CD163, a scavenger receptor expressed by macrophages, in the transformation of M2 to M1 macrophages remains unclear. Here, dexamethasone-induced M2 macrophages were treated with lipopolysaccharide (LPS) to induce the transformation of M2 to M1 macrophages. We found that treatment with lipopolysaccharide (LPS) induced the transformation of M2-like macrophages to an M1-like phenotype, as evidenced by increased mRNA levels of Il1b and Tnf, decreased mRNA levels of Cd206 and Il10, and increased TNF-α secretion. Knockdown of CD163 enhanced the phenotypic features of M1 macrophages, while treatment with recombinant CD163 protein (rmCD163) inhibited the LPS-induced M2-to-M1 transformation. Furthermore, LPS stimulation resulted in the activation of P38, ERK, JNK, and NF-κB P65 signaling pathways, and this activation was increased after CD163 knockdown and suppressed after rmCD163 treatment during macrophage transformation. Additionally, we observed that LPS treatment reduced the expression of CD163 in dexamethasone-induced M2 macrophages, leading to a decrease in the CD163-TWEAK complex and an increase in the interaction between TWEAK and Fn14. Overall, our findings suggest that rmCD163 can inhibit the LPS-induced transformation of M2 macrophages to M1 by disrupting the TWEAK-Fn14 interaction and modulating the MAPK-NF-κB pathway.

2.
Bioorg Med Chem Lett ; 26(15): 3598-602, 2016 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-27311893

RESUMO

Novel water-soluble paclitaxel prodrugs were designed and synthesized by introducing morpholino groups through different linkers. These derivatives showed 400-20,000-times greater water solubility than paclitaxel as well as comparable activity in MCF-7 and HeLa cell lines. The prodrug PM4 was tested in the S-180 tumor mouse model, with paclitaxel as the positive control. The results showed that PM4 had comparable antitumor activity as paclitaxel, with tumor inhibition of 54% versus 56%, and remarkably decreased toxicity. The survival rate of treated mice was 8/8 in the PM4 group, compared to 3/8 in the paclitaxel group.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Desenho de Fármacos , Morfolinos/farmacologia , Paclitaxel/farmacologia , Pró-Fármacos/farmacologia , Animais , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Células MCF-7 , Camundongos , Estrutura Molecular , Morfolinos/química , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/patologia , Paclitaxel/química , Pró-Fármacos/síntese química , Pró-Fármacos/química , Solubilidade , Relação Estrutura-Atividade , Água/química
3.
Opt Express ; 22 Suppl 2: A359-64, 2014 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-24922245

RESUMO

A type II GaSb quantum ring solar cell is fabricated and measured under the concentrated sunlight. The external quantum efficiency confirms the extended absorption from the quantum rings at long wavelength coinciding with the photoluminescence results. The short-circuit current of the quantum ring devices is 5.1% to 9.9% more than the GaAs reference's under various concentrations. While the quantum ring solar cell does not exceed its GaAs counterpart in efficiency under one-sun, the recovery of the open-circuit voltages at higher concentration helps to reverse the situation. A slightly higher efficiency (10.31% vs. 10.29%) is reported for the quantum ring device against the GaAs one.

4.
Opt Express ; 22(5): A359-64, 2014 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-24800292

RESUMO

A type II GaSb quantum ring solar cell is fabricated and measured under the concentrated sunlight. The external quantum efficiency confirms the extended absorption from the quantum rings at long wavelength coinciding with the photoluminescence results. The short-circuit current of the quantum ring devices is 5.1% to 9.9% more than the GaAs reference's under various concentrations. While the quantum ring solar cell does not exceed its GaAs counterpart in efficiency under one-sun, the recovery of the open-circuit voltages at higher concentration helps to reverse the situation. A slightly higher efficiency (10.31% vs. 10.29%) is reported for the quantum ring device against the GaAs one.

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