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1.
Materials (Basel) ; 16(14)2023 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-37512312

RESUMO

I-III-VI type QDs have unique optoelectronic properties such as low toxicity, tunable bandgaps, large Stokes shifts and a long photoluminescence lifetime, and their emission range can be continuously tuned in the visible to near-infrared light region by changing their chemical composition. Moreover, they can avoid the use of heavy metal elements such as Cd, Hg and Pb and highly toxic anions, i.e., Se, Te, P and As. These advantages make them promising candidates to replace traditional binary QDs in applications such as light-emitting diodes, solar cells, photodetectors, bioimaging fields, etc. Compared with binary QDs, multiple QDs contain many different types of metal ions. Therefore, the problem of different reaction rates between the metal ions arises, causing more defects inside the crystal and poor fluorescence properties of QDs, which can be effectively improved by doping metal ions (Zn2+, Mn2+ and Cu+) or surface coating. In this review, the luminous mechanism of I-III-VI type QDs based on their structure and composition is introduced. Meanwhile, we focus on the various synthesis methods and improvement strategies like metal ion doping and surface coating from recent years. The primary applications in the field of optoelectronics are also summarized. Finally, a perspective on the challenges and future perspectives of I-III-VI type QDs is proposed as well.

2.
Eur J Med Chem ; 135: 12-23, 2017 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-28426996

RESUMO

Based upon the modeling binding mode of marketed AZD9291 with T790M, a series of 5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline derivatives were designed and synthesized with the purpose to overcome the drug resistance resulted from T790M/L858R double mutations. The most potent compound 8 showed excellent enzyme inhibitory activities and selectivity with sub nanomolar IC50 values for both the single L858R and double T790M/L858R mutant EGFRs, and was more than 8-fold selective for wild type EGFR. Compound 8 exhibited good microsomes stabilities and pharmacokinetic properties and lower binding affinity to hERG ion channel than AZD9291 and displayed strong antiproliferative activity against the H1975 non-small cell lung cancer (NSCLC) cells bearing T790M/L858R and in vivo anticancer efficacy in a human NSCLC (H1975) xenograft mouse model.


Assuntos
Desenho de Fármacos , Receptores ErbB/antagonistas & inibidores , Animais , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Receptores ErbB/genética , Humanos , Masculino , Camundongos , Camundongos SCID , Estrutura Molecular , Mutação , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/patologia , Ratos , Ratos Sprague-Dawley , Relação Estrutura-Atividade
3.
Bioorg Med Chem Lett ; 26(8): 1958-62, 2016 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-26965867

RESUMO

A series of novel dipeptidyl boronic acid proteasome inhibitors constructed from αα- and αß-amino acids were designed and synthesized. Their structures were elucidated by (1)H NMR, (13)C NMR, LC-MS and HRMS. These compounds were evaluated for their ß5 subunit inhibitory activities of human proteasome. The results showed that dipeptidyl boronic acid inhibitors composed of αα-amino acids were as active as bortezomib. Interestingly, the activities of those derived from αß-amino acids lost completely. Of all the inhibitors, compound 22 (IC50=4.82 nM) was the most potent for the inhibition of proteasome activity. Compound 22 was also the most active against three MM cell lines with IC50 values less than 5 nM in inhibiting cell growth assays. Molecular docking studies displayed that 22 fitted very well in the ß5 subunit active pocket of proteasome.


Assuntos
Aminoácidos/química , Aminoácidos/farmacologia , Ácidos Borônicos/farmacologia , Dipeptídeos/farmacologia , Desenho de Fármacos , Simulação de Acoplamento Molecular , Complexo de Endopeptidases do Proteassoma/metabolismo , Inibidores de Proteassoma/síntese química , Inibidores de Proteassoma/farmacologia , Ácidos Borônicos/síntese química , Ácidos Borônicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Dipeptídeos/síntese química , Dipeptídeos/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Inibidores de Proteassoma/química , Relação Estrutura-Atividade
4.
Artigo em Chinês | MEDLINE | ID: mdl-25007667

RESUMO

OBJECTIVE: To investigate the postoperative application of nasopharyngeal airway (NPA) in rhinogenous obstructive sleep apnea hypopnea syndrome (OSAHS) patients, so that to observe the parameters including vital signs of the patients and evaluatethe value of clinical application and reliability of NPA. METHOD: A total of 216 patients diagnosed as rhinogenous OSAHS were randomly assigned to experimental group (setting NPA, 112 cases) and control group (not setting NPA, 104 cases) according to whether NPA was placed in the nasal cavity postoperatively. ECG, oxygen saturation and hemodynamics were monitored for 24 h postoperatively. The pharyngeal pain and discomfort, low oxygen saturation and hemodynamics were compared between these two groups. The subjective assessment and clinical symptoms were compared between the two groups using visual analogue scale (VAS). RESULT: The experimental group showed better relief of nasal obstruction, nasal pain, headache, dry pharynx, insomnia and pain while taking out nasal packing compared with control group, where the differences were statistically significant (P < 0.01). In the experimental group, the level of LSa2O2 (P < 0.05), HR (P < 0.01), SBP (P < 0.05), DBP (P < 0.01), MAP (P < 0.01) and RPP (P < 0.01) was significantly lower than in the control group. CONCLUSION: The postoperative application of nasopharyngeal airway in rhinogenous OSAHS patients could help to keep nasal patency and avoid the upper airway obstruction, which exhibited good safety and compliance. The nasopharyngeal airway can reduce patients' discomfort and improve hyoxemia, ensuring hemodynamic stability.


Assuntos
Respiração Artificial/métodos , Apneia Obstrutiva do Sono/terapia , Adolescente , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Nasofaringe , Cuidados Pós-Operatórios , Adulto Jovem
5.
Zhonghua Yi Xue Za Zhi ; 88(48): 3392-6, 2008 Dec 30.
Artigo em Chinês | MEDLINE | ID: mdl-19159567

RESUMO

OBJECTIVE: To investigate the significance of T cell immunoglobulin domain and mucin domain-1 (TIM-1) expression in helper T lymphocyte in allergic rhinitis (AR) patients. METHODS: Peripheral blood samples were collected from 20 AR patients, 9 males and 11 females, aged 31.4 (20-54), and 20 healthy persons, 12 males and 8 females, aged 38, 6 (18-60). Peripheral blood mononuclear cells (PBMNs) were isolated and magnetic cell sorting technique was used to purify the CD4+ T cells and CD4 + CD45RA + T cells. Immunofluorescence staining and flow cytometry were used to detect the percentage of CD4 + CD45RA + T cells positive in TIM-1, a helper T lymphocyte marker. Phytohemagglutinin (PHA) was added into the culture media to stimulate the TIM-1 positive helper T lymphocytes. Dendritic cells (DCs) thus induced and differentiated were conditioned by standardized allergen from dust mite (Dermatophagoides pteronyssinus) or lipopolysaccharide (LPS), and then co-cultured with CD4 T cells. The percentage of TIM-1 positive CD4 + CD45RA + T cells was counted. ELISA was used to detect the IL-4 and interferon (IFN)-gamma levels in the supernatants of the culture media of the dust mite and LPS groups. RESULTS: The percentage of TIM-1 positive CD4+ T cells of the AR patients was (9.48 +/- 1.51)%, significantly higher than that of the healthy controls [(3.12 +/- 0.32)%, P < 0.05], and the percentage of TIM-1 positive CD4 + T cells after PHA stimulation of the AR patients was (47.05 +/- 4.35)%, significantly higher than that of the healthy controls [(29.92 +/- 3.36)%, P < 0.05]. The percentage of TIM-1 positive CD4 + CD45RA + T cells of the AR patients was (26.34 +/- 4.0)%, significantly higher than that of the healthy controls [(18.4 +/- 8.1)%, P < 0.05], and the percentage of TIM-1 positive CD4 + CD45RA + T cells after PHA stimulation of the AR patients was (65.3 +/- 7.4)%, significantly higher than that of the healthy controls [(36.3 +/- 6.8)%, P < 0.05]. The percentage of TIM-1 positive CD4 + CD45RA + T cells co-cultured with the DCs conditioned by dust mite of the AR patients was (10.81 +/- 1.48)%, significantly higher than that of the LPS group [(6.08 +/- 1.45)%] and the blank control group [(1.56 +/- 2.30)%, both P < 0.05]. The IL-4 level of the DCs conditioned by dust mite allergen was (74.61 +/- 13.82) pg/ml, significantly higher than those of the LPS group and blank control group [(28.57 +/- 3.36) and (1.40 +/- 0.99) ng/ml respectively, both P < 0.05]. The IFN-gamma level of the DCs conditioned by dust mite allergen was (25.31 +/- 7.23) pg/ml, significantly lower than that of the LPS group [(163.41 +/- 82.37) pg/ml, P < 0.05], however, significantly higher than that of the blank control group [(1.58 +/- 0.53) pg/ml, P < 0.05]. CONCLUSION: The percentage of TIM-1 positive helper T lymphocytes of the AR patients are abnormally high. After stimulation of allergen The DCs increase the number of TIM-1 expressing naïve Th cells and promote them to differentiate into Th2 cells. Promoting naïve Th cells to differentiate into Th2 cells, TIM-1 expression induces Th2 cytokine-based immune responses.


Assuntos
Glicoproteínas de Membrana/metabolismo , Receptores Virais/metabolismo , Rinite Alérgica Perene/imunologia , Subpopulações de Linfócitos T/metabolismo , Células Th2/metabolismo , Adolescente , Adulto , Diferenciação Celular , Células Dendríticas/imunologia , Feminino , Citometria de Fluxo , Receptor Celular 1 do Vírus da Hepatite A , Humanos , Masculino , Pessoa de Meia-Idade , Rinite Alérgica Perene/metabolismo , Subpopulações de Linfócitos T/imunologia , Células Th2/imunologia
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