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1.
Front Genet ; 15: 1376486, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38655048

RESUMEN

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.
Artículo en Inglés | MEDLINE | ID: mdl-38328372

RESUMEN

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.
Artículo en Inglés | MEDLINE | ID: mdl-30576910

RESUMEN

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.


Asunto(s)
Antineoplásicos/síntesis química , Monoterpenos Bicíclicos/química , Diseño de Fármacos , Mitocondrias/metabolismo , Tiazoles/química , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Citocromos c/metabolismo , Ensayos de Selección de Medicamentos Antitumorales , Puntos de Control de la Fase G1 del Ciclo Celular/efectos de los fármacos , Humanos , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Mitocondrias/efectos de los fármacos , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Tiazoles/farmacología
4.
Bioorg Med Chem Lett ; 27(11): 2360-2363, 2017 06 01.
Artículo en Inglés | MEDLINE | ID: mdl-28431878

RESUMEN

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.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Hidrocarburos Aromáticos con Puentes/farmacología , Tiosemicarbazonas/química , Tiosemicarbazonas/farmacología , Antineoplásicos/síntesis química , Hidrocarburos Aromáticos con Puentes/síntesis química , Hidrocarburos Aromáticos con Puentes/química , Espectroscopía de Resonancia Magnética con Carbono-13 , Línea Celular Tumoral , Diseño de Fármacos , Humanos , Espectrometría de Masas , Espectroscopía de Protones por Resonancia Magnética , Tiosemicarbazonas/síntesis química
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