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1.
Front Genet ; 15: 1376486, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38655048

RESUMO

Cancer, a significant global public health issue, resulted in about 10 million deaths in 2022. Anticancer peptides (ACPs), as a category of bioactive peptides, have emerged as a focal point in clinical cancer research due to their potential to inhibit tumor cell proliferation with minimal side effects. However, the recognition of ACPs through wet-lab experiments still faces challenges of low efficiency and high cost. Our work proposes a recognition method for ACPs named ACP-DRL based on deep representation learning, to address the challenges associated with the recognition of ACPs in wet-lab experiments. ACP-DRL marks initial exploration of integrating protein language models into ACPs recognition, employing in-domain further pre-training to enhance the development of deep representation learning. Simultaneously, it employs bidirectional long short-term memory networks to extract amino acid features from sequences. Consequently, ACP-DRL eliminates constraints on sequence length and the dependence on manual features, showcasing remarkable competitiveness in comparison with existing methods.

2.
Front Psychol ; 15: 1279872, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38328372

RESUMO

To investigate whether bullying and psychological conditions are correlated, this study analyzed a survey of primary and secondary school students from Zigong City, Sichuan Province. A total of 95,545 students completed a personal information questionnaire, the Multidimensional Peer-Victimization Scale (MPVS), and eight other scales pertaining to various psychological problems. The data showed that 68,315 (71.5%) participants experienced school bullying at varying degrees, indicating the prevalence of bullying among adolescents. The chi-square tests revealed a strong correlation between school bullying and psychological conditions. This correlation was further explored through multivariate logistic regression, showing that students who experienced mild bullying had a 3.10 times higher probability of emotional and behavioral problems, 4.06 times higher probability of experiencing prodromal symptoms of mental illness, 4.72 times higher probability of anxiety, 3.28 times higher probability of developing post-traumatic stress disorder (PTSD), 4.07 times higher probability of poor sleep quality, 3.13 times higher probability of internet addiction, 2.18 times higher probability of poor mental health, and 3.64 times higher probability of depression than students who did not experience bullying. The corresponding probabilities for students who experienced severe bullying were 11.35, 17.35, 18.52, 12.59, 11.67, 12.03, 4.64, and 5.34 times higher, respectively. In conclusion, school bullying and psychological conditions are significantly correlated among primary and secondary school students, and the more severe the bullying, the higher the probability to suffer from psychological problems.

3.
Bioorg Chem ; 84: 468-477, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30576910

RESUMO

A series of novel ß-pinene-based thiazole derivatives were synthesized and characterized by HRMS, 1H NMR, and 13C NMR analyses as potential antineoplastic agents. Derivatives were evaluated for their anticancer activities in vitro, and the data manifested that most target compounds showed potent anti-proliferative activities against three human cancer cell lines. Especially, compound 5g displayed excellent cytotoxic activity against Hela, CT-26, and SMMC-7721 cell lines with IC50 values of 3.48 ±â€¯0.14, 8.84 ±â€¯0.16, and 6.69 ±â€¯0.15 µM, respectively. To determine the underlying mechanism of compound 5g on cell viability, DAPI staining, Annexin-V/PI staining, JC-1 staining, DCFDA staining, and Western blot analysis were performed. Our data showed that compound 5g inhibited cell proliferation by inducing apoptosis and cell cycle arrest of Hela cells at the G0/G1 phase in a dose dependent manner. Further studies revealed that compound 5g enhanced levels of reactive oxygen species (ROS), caused a decrease in mitochondrial membrane potential, increased the release of mitochondrial cytochrome C, and affected the expression of Bax, Bcl-2, caspase-3 and caspase-9. Thus, our findings indicated that compound 5g induced apoptosis in Hela through ROS-mediated mitochondrial dysfunction signaling pathways.


Assuntos
Antineoplásicos/síntese química , Monoterpenos Bicíclicos/química , Desenho de Fármacos , Mitocôndrias/metabolismo , Tiazóis/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Citocromos c/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Tiazóis/farmacologia
4.
Bioorg Med Chem Lett ; 27(11): 2360-2363, 2017 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-28431878

RESUMO

A series of new nopinone-based thiosemicarbazone derivatives were designed and synthesized as potent anticancer agents. All these compounds were identified by 1H NMR, 13C NMR, HR-MS spectra analyses. In the in vitro anticancer activity, most derivatives showed considerable cytotoxic activity against three human cancer cell lines (MDA-MB-231, SMMC-7721 and Hela). Among them, compound 4i exhibited most potent antitumor activity against three cancer cell lines with the IC50 values of 2.79±0.38, 2.64±0.17 and 3.64±0.13µM, respectively. Furthermore, the cell cycle analysis indicated that compound 4i caused cell cycle arrest of MDA-MB-231 cells at G2/M phase. The Annexin V-FITC/7-AAD dual staining assay also revealed that compound 4i induced the early apoptosis of MDA-MB-231 cells.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Hidrocarbonetos Aromáticos com Pontes/farmacologia , Tiossemicarbazonas/química , Tiossemicarbazonas/farmacologia , Antineoplásicos/síntese química , Hidrocarbonetos Aromáticos com Pontes/síntese química , Hidrocarbonetos Aromáticos com Pontes/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Linhagem Celular Tumoral , Desenho de Fármacos , Humanos , Espectrometria de Massas , Espectroscopia de Prótons por Ressonância Magnética , Tiossemicarbazonas/síntese química
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