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1.
J Enzyme Inhib Med Chem ; 38(1): 2206581, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37144599

RESUMO

Pan-histone deacetylase (HDAC) inhibitors often have some toxic side effects. In this study, three series of novel polysubstituted N-alkyl acridone analogous were designed and synthesised as HDAC isoform-selective inhibitors. Among them, 11b and 11c exhibited selective inhibition of HDAC1, HDAC3, and HDAC10, with IC50 values ranging from 87 nM to 418 nM. However, these compounds showed no inhibitory effect against HDAC6 and HDAC8. Moreover, 11b and 11c displayed potent antiproliferative activity against leukaemia HL-60 cells and colon cancer HCT-116 cells, with IC50 values ranging from 0.56 µM to 4.21 µM. Molecular docking and energy scoring functions further analysed the differences in the binding modes of 11c with HDAC1/6. In vitro anticancer studies revealed that the hit compounds 11b and 11c effectively induced histone H3 acetylation, S-phase cell cycle arrest, and apoptosis in HL-60 cells in a concentration-dependent manner.


Assuntos
Antineoplásicos , Neoplasias , Humanos , Inibidores de Histona Desacetilases/farmacologia , Inibidores de Histona Desacetilases/química , Estrutura Molecular , Relação Estrutura-Atividade , Linhagem Celular Tumoral , Simulação de Acoplamento Molecular , Histona Desacetilases/metabolismo , Isoformas de Proteínas/metabolismo , Proliferação de Células , Antineoplásicos/farmacologia , Antineoplásicos/química , Histona Desacetilase 1/metabolismo , Histona Desacetilase 1/farmacologia , Proteínas Repressoras/metabolismo , Proteínas Repressoras/farmacologia
2.
J Relig Health ; 60(1): 458-474, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31894522

RESUMO

The aim of the study was to develop and psychometrically evaluate the Chinese Spiritual Coping Scale. The items in the questionnaire were written according to the study's theoretical conception and literature research. A sample of 415 participants with or without religious beliefs was used for exploratory factor analyses to select the items. In addition, another sample of 207 participants was used to cross-validate the factor structure and examine the internal consistency. The results supported the four-factor structure of the Chinese Spiritual Coping Scale (17 items, four dimensions: Mystical Experience, Moral Practice, Meaning Exploration, and Transcendent Attitude). The analyses demonstrated adequate internal consistency and construct validity. The overall psychometric evaluation of the Spiritual Coping Scale suggested that this could be a promising measure of spiritual coping for Chinese individuals.


Assuntos
Adaptação Psicológica , Psicometria , Espiritualidade , China , Humanos , Reprodutibilidade dos Testes , Inquéritos e Questionários
3.
Ying Yong Sheng Tai Xue Bao ; 17(5): 894-8, 2006 May.
Artigo em Chinês | MEDLINE | ID: mdl-16883822

RESUMO

Based on the water quality investigation data from August 2003 to August 2004, and by using single water quality parameter model, integrated water quality index model and eutrophication assessment model, this paper assessed the environmental quality of Guangzhou sea area. The results showed that the key pollutants were dissolved inorganic nitrogen (DIN), dissolved inorganic phosphorus, oil, Cu and Pb, with their annual average concentrations of 1.87 mg x L(-1), 0.049 mg x L(-1), 0.107 mg x L(-1), 6.07 microg x L(-1) and 1.43 microg x L(-1), respectively. Among the pollutants, DIN was the most important one. Its concentration exceeded the fourth standard of sea water quality, and decreased gradually from inner bay to outer bay. Under the effects of Pearl River water flow and land-based pollutants, most part of Guangzhou sea area was seriously polluted, and the annual averages of single parameter pollution index, integrated water quality index, and eutrophication index were 2.22, 6.80 and 48.44, respectively, which also decreased gradually from inner bay to outer bay, and from nearshore to offshore.


Assuntos
Monitoramento Ambiental , Nitratos/análise , Água do Mar/análise , Poluentes Químicos da Água/análise , China , Eutrofização , Sedimentos Geológicos/análise , Metais Pesados/análise , Controle de Qualidade
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