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1.
RSC Adv ; 14(29): 20714-20734, 2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-38952936

RESUMO

Presently, excessive carbon dioxide emissions represent a critical environmental challenge. Thus, urgent efforts are required to develop environmentally friendly and low-energy technologies for carbon dioxide treatment. In this case, membrane separation technology stands out as a promising avenue for CO2 separation, with selective membrane materials of high permeability playing a pivotal role in this process. Herein, we categorize CO2 separation membranes into three groups: inorganic membranes, organic membranes, and emerging membranes. Moreover, representative high-performance membranes are introduced and their synthesis methods, gas separation performances, and applications are examined. Furthermore, a brief analysis of the challenges encountered by carbon dioxide separation membrane materials is provided together with a discussion on the future research direction. It is expected that this review will provide some potential insights and guidance for the future development of CO2 separation membranes, which can promote their development.

2.
Huan Jing Ke Xue ; 45(5): 2828-2839, 2024 May 08.
Artigo em Chinês | MEDLINE | ID: mdl-38629545

RESUMO

It is of great practical significance for regional sustainable development and ecological construction to quantitatively analyze the impact of construction land expansion on terrestrial ecosystem carbon storage and to explore the optimization scheme of simulating construction land expansion to improve future ecosystem carbon storage. Based on the land use and cover change (LUCC) and other geospatial data of the Beijing-Tianjin-Hebei Urban Agglomeration from 2000 to 2020, this study utilized the Integrated Valuation of Ecosystem Services and Tradeoffs (InVEST) model and the patch-generating land-use simulation (PLUS) model to assess and analyze the changes in ecosystem carbon stocks and spatial patterns regionally. In this study, we performed linear regression analysis to investigate the relationship between urban land expansion and changes in ecosystem carbon stocks for varying urban land proportion levels during two distinct time intervals, 2000-2010 and 2010-2020, which was conducted at a spatial resolution of 2 km. Three distinct urban land expansion scenarios were subjected to simulation to forecast the prospective land use pattern by 2030. Subsequently, we quantified the ramifications of these scenarios on ecosystem carbon stocks during the period from 2020 to 2030. The results were as follows:① In the Beijing-Tianjin-Hebei Urban Agglomeration, the ecosystem carbon stocks exhibited notable variations over the study period, with values of 2 088.02, 2 106.78, and 2 121.25 Tg recorded for the years 2000, 2010, and 2020, respectively, resulting in a cumulative carbon sequestration of 33.23 Tg C during the study duration. It is noteworthy that forest carbon storage emerged as the dominant contributor, with an increase from 1 010.17 Tg in 2000 to 1 136.53 Tg in 2020. Throughout the study period, the spatial distribution of carbon stocks displayed relative stability. Regions characterized by lower carbon content were concentrated in the vicinity of the Bohai Rim region and in proximity to cities such as Beijing, Tianjin, and Shijiazhuang, as well as rural settlements. In contrast, grid units with moderate and high carbon stocks were predominantly situated in the western Taihang Mountain and the northern Yanshan Mountain. Additionally, there was a tendency of increasing carbon stocks in the Taihang Mountain and Yanshan Mountain region, whereas those surrounding major urban centers such as Beijing, Tianjin, Shijiazhuang, and Tangshan experienced a notable decline in carbon stocks. Such reductions were most pronounced in regions undergoing urban land expansion during the study period. ② In grid units with an urban land proportion exceeding 10% at each level, a strong correlation was observed between urban land expansion and changes in carbon stocks during both the 2000-2010 and 2010-2020 periods. The changes in urban land proportion adequately explained the variations in carbon stocks. However, the explanatory power of urban land on carbon stocks decreased during the 2010-2020 period, indicating that other factors played a more substantial role in influencing carbon stocks during this time. The regression coefficients for both periods exhibited a fluctuating upward trend. In comparison to that during the 2000-2010 period, the impact of urban land expansion on carbon stocks was relatively smaller during 2010-2020, indicating a weakening influence. ③ In light of three distinct development scenarios, namely natural development (Scenario Ⅰ), a 15% reduction in the rate of urban land expansion (Scenario Ⅱ), and a 30% reduction in the rate of urban land expansion (Scenario Ⅲ), the projected ecosystem carbon stocks for the Beijing-Tianjin-Hebei Urban Agglomeration in the year 2030 were estimated to be 2 129.12, 2 133.55, and 2 139.10 Tg, respectively. These projections indicated an increase of 7.88, 12.30, and 17.85 Tg in comparison to the current carbon stocks. All scenarios demonstrated that the terrestrial ecosystem would play a role of carbon sink, particularly with the greatest carbon sink observed in the scenario with a 30% reduction in urban land expansion. The fit performance between urban land expansion and carbon stock changes during the 2020-2030 period was significantly better than that during the 2000-2010 and 2010-2020 periods, and the regression coefficients showed a fluctuating increase with an increase in urban land proportion. Across grid units with different urban land proportion levels, the regression coefficients exhibited the order of Scenario Ⅰ < Scenario Ⅱ < Scenario Ⅲ. In pursuit of the carbon peaking and carbon neutrality goals, the Beijing-Tianjin-Hebei Urban Agglomeration should prioritize scenarios with reduced rates of urban land expansion, especially in regions with higher urban land proportions.

3.
ACS Omega ; 9(2): 2752-2757, 2024 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-38250410

RESUMO

A catalyst with a simple synthetic process and good catalytic performance was prepared using Na2CO3 as the active component and ZSM-5 as the carrier for the resource utilization of waste cooking oil. The structure of Na2CO3/ZSM-5 was characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy, and the effects of parameters such as Na2CO3 loading, catalyst percentage, and reaction time on the yield of fatty acid methyl esters were investigated. The results showed that the conversion of waste cooking oil to fatty acid methyl esters yielded up to 96.89% when the Na2CO3 loading was 35%, the reaction temperature was 65 °C, the reaction time was 2 h, and the catalyst percentage was 1 wt %. The Na2CO3/ZSM-5 catalyst could be used to replace H2SO4 or NaOCH3 in the industrial treatment of waste cooking oil for its resource utilization.

4.
Carbohydr Res ; 536: 109009, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38211450

RESUMO

This article introduces the synthesis optimization of carboxymethyl inulin using response surface methodology. The important factors affecting the degree of substitution (DS) were determined by Plackett-Burman design, including sodium hydroxide concentration, monochloroacetic concentration, and etherification temperature. Further optimization was conducted using the Box-Behnken response surface design. The coefficient of determination (R2) of the response surface model was 0.9827, and the adjusted R2 value was 0.9516, which proved the significance of the model. The optimized results of the predicted response showed that the molar ratios of sodium hydroxide to monochloroacetic acid and fructose to furan were 3.67 and 2.21, respectively. The maximum DS of 1.67 was obtained at 30 °C alkalization for 30 min and 50.30 °C etherification for 4 h, and the reaction efficiency (RE) reached 76.01 %. Under the optimized conditions, the Experimental DS was 1.68, suggesting that the experimental and predicted values of DS were in good agreement. The characterization results confirmed the synthesis of CMI. In this work, we have provided an effective method for the preparation of moderately to highly substituted CMI in 95 % ethanol.


Assuntos
Inulina , Hidróxido de Sódio , Temperatura
5.
Spectrochim Acta A Mol Biomol Spectrosc ; 303: 123203, 2023 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-37523848

RESUMO

A water-soluble turn-on fluorescent probe PNAP for pH has been designed and synthesized. PNAP was consist of pyrene as fluorophore and morpholine as receptor. Owing to the photoinduced electron transfer (PET) effect, the fluorescence of PNAP was quenched, while PNAP exhibited a remarkable "turn-on" fluorescence with the increase of acidity. Notably for its pKa of 2.15, PNAP was one of the pH fluorescent probes used in extremely acidic environments. Furthermore, PNAP also displayed good repeatability, strong anti-ion interference ability, high sensitivity and selectivity toward pH. In addition, PNAP has been successfully applied to the test strips and monitor the pH of environment water samples and realistic samples, showing its good promising prospect.

6.
J Org Chem ; 88(13): 8034-8041, 2023 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-37319302

RESUMO

A tandem reaction for the synthesis of phenanthrenes from arynes and α-(bromomethyl)styrenes is reported. The transformation proceeds via an ene reaction of α-(bromomethyl)styrenes with arynes, followed by a [4 + 2] cycloaddition reaction. The reaction generates 9-benzylphenanthrene derivatives in moderate to excellent yields.


Assuntos
Fenantrenos , Estirenos , Reação de Cicloadição , Ciclização
7.
Spectrochim Acta A Mol Biomol Spectrosc ; 289: 122245, 2023 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-36535222

RESUMO

A probe 3 (2-ethoxy-N-(2-(2-(2-hydroxyethoxy)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de] isoquinolin-6-yl)benzamide) that could selectively respond to Cr2O72- and Fe3+ was reported in this paper. The selectivity, pH titration, concentration titration, detection limit, time dependence, quenching constant and recognition mechanism of probe 3 for Cr2O72- and Fe3+ were studied in CH3CN/HEPES buffer solution. The results showed that Cr2O72- and Fe3+ could rapidly quench the fluorescence of probe 3 through the inner filter effect (IFE). The quenching kept constant after 30 s, and the quenching constants were 7.99 × 103 L.mol-1 and 4.13 × 103 L.mol-1, respectively. The detection limits of probe 3 for Cr2O72- and Fe3+ were 1.15 µmol.L-1 and 1.95 µmol.L-1, respectively, which were lower than the maximum allowable concentrations in drinking water stipulated by EPA. The determination results of Cr2O72- and Fe3+ in water samples indicated that probe 3 could be used as a potential detection tool in practical applications.


Assuntos
Água Potável , Corantes Fluorescentes , Naftalimidas , Fluorescência
8.
RSC Adv ; 12(51): 33260-33263, 2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36425163

RESUMO

A transition-metal-free intramolecular redox cyclization reaction for the synthesis of cinnolines has been developed from 2-nitrobenzyl alcohol and benzylamine. Mechanistic investigations disclosed the involvement of a key intramolecular redox reaction, followed by condensation, azo isomerization to hydrazone, cyclization, and aromatization to form the desired products. Notably, the formation of intermediate 2-nitrosobenzaldehyde and (E)-2-(2-benzylidenehydrazineyl) benzaldehyde plays an important role in this transformation.

9.
Arch Med Res ; 52(5): 461-470, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33551225

RESUMO

OBJECTIVE: This research was designed to investigate the function of miR-1275 in hypoxia/reoxygenation (H/R)-induced myocardial injury and its in-depth mechanism. METHODS: Firstly, the differential expression of miR-1275 in patients with heart failure and healthy control were analyzed based on Gene Expression Omnibus (GEO) database. Then H/R model was constructed in vitro with AC16 cells. The qRT-PCR assay was performed to analyze the expression of miR-1275 in H/R-treated cells. Afterwards, CCK-8 assay and flow cytometry assay were carried out to detect the cells viability and apoptosis. Bioinformatics prediction, western blotting and dual-luciferase reporter assays were set to check the target gene of miR-1275. Finally, we used an Elisa to test the effect of miR-1275/HK2 axis on inflammatory factors. RESULTS: We found that miR-1275 was highly expressed in patients with heart failure and H/R treated AC16 cells than that in control group, and inhibition of miR-1275 can alleviate induced-decrease of cell viability. Subsequently, we revealed that HK2 was a downstream target gene of miR-1275, which was lowly expressed in patients with heart failure. Furthermore, our data also suggested that inhibition of miR-1275 can significantly alleviate H/R-induced myocardial injury, which can also markedly decrease the concentration of pro-inflammatory factors TNF-α, IL-1 ß and increase the concentration of anti-inflammatory factors IL-10 in H/R-treated AC16 cells, while knockdown of HK2 canceled the effect caused by miR-1275 deletion. CONCLUSIONS: In summing, our results illustrated that miR-1275/HK2 axis act as a potential regulator to against H/R-induced AC16 cells injury through anti-inflammatory effect.


Assuntos
Insuficiência Cardíaca/fisiopatologia , Hipóxia , MicroRNAs , Apoptose , Hipóxia Celular , Linhagem Celular , Insuficiência Cardíaca/genética , Humanos , Hipóxia/metabolismo , MicroRNAs/genética , MicroRNAs/metabolismo , Miócitos Cardíacos/metabolismo
10.
RSC Adv ; 11(47): 29632-29660, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-35479541

RESUMO

Cadmium is a heavy metal which exists widely in industrial and agricultural production and can induce a variety of diseases in organisms. Therefore, its detection is of great significance in the fields of biology, environment and medicine. Fluorescent probe has been a powerful tool for cadmium detection because of its convenience, sensitivity, and bioimaging capability. In this paper, we reviewed 98 literatures on cadmium fluorescent sensors reported from 2017 to 2021, classified them according to different fluorophores, elaborated the probe design, application characteristics and recognition mode, summarized and prospected the development of cadmium fluorescent and colorimetric probes. We hope to provide some help for researchers to design cadmium fluorescent probes with higher selectivity, sensitivity and practicability.

11.
Dalton Trans ; 49(48): 17511-17519, 2020 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-33206738

RESUMO

In the past few decades, the construction of discrete supramolecular double-metallacycles has attracted wide interest because of their unique structures and their potential applications in photoelectric materials. Since some progress has been made in this area, it is time to summarize the progress of discrete supramolecular double-metallacycles. In this review, we will briefly introduce the synthetic strategy of discrete supramolecular double-metallacycles. In addition, we will discuss the design principles, preparation methods, optical properties, and functions of these discrete supramolecular double-metallacycles.

12.
Urol Oncol ; 37(2): 150-157, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30455080

RESUMO

OBJECTIVE: MicroRNA-93 (miR-93) is upregulated in the urine of patients with bladder cancer (BC). Here, we investigated the role of miR-93 in BC progression and explored the underlying mechanism. METHODS: miR-93 expression in BC tissues and cells was detected by real time-polymerase chain reaction. The effects of miR-93 and pigment epithelium-derived factor (PEDF) on cell proliferation and invasion were assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and Transwell assays. The binding of miR-93 to the 3'-untranslated region of PEDF was identified by the luciferase reporter assay. RESULTS: miR-93 expression was higher in BC tissues than in normal controls, and its expression was associated with tumor stage and node stage. Inhibition of miR-93 suppressed the proliferation and invasion of BC cells. PEDF was identified as a target of miR-93 and shown to mediate the effect of miR-93 on cell proliferation and invasion. CONCLUSIONS: The present data suggested that miR-93 promoted BC cell proliferation and invasion by targeting PEDF, providing new biomarkers and targets for BC diagnosis and treatment.


Assuntos
Biomarcadores Tumorais/metabolismo , Proliferação de Células , Proteínas do Olho/metabolismo , Regulação Neoplásica da Expressão Gênica , MicroRNAs/genética , Fatores de Crescimento Neural/metabolismo , Serpinas/metabolismo , Neoplasias da Bexiga Urinária/patologia , Biomarcadores Tumorais/genética , Estudos de Casos e Controles , Movimento Celular , Proteínas do Olho/genética , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Invasividade Neoplásica , Fatores de Crescimento Neural/genética , Prognóstico , Serpinas/genética , Células Tumorais Cultivadas , Neoplasias da Bexiga Urinária/genética , Neoplasias da Bexiga Urinária/metabolismo
13.
Luminescence ; 31(1): 88-95, 2016 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25991384

RESUMO

The interactions between the three kinds of naphthalimide-based anti-tumor drugs (NADA, NADB, NADC) and human serum albumin (HSA) under simulated physiological conditions were investigated by fluorescence spectroscopy, circular dichroism spectroscopy and molecular modeling. The results of the fluorescence quenching spectroscopy showed that the quenching mechanisms for different drugs were static and their affinity was in a descending order of NADA > NADB > NADC. The relative thermodynamic parameters indicated that hydrophobic force was the predominant intermolecular force in the binding of NAD to HSA, while van der Waals interactions and hydrogen bonds could not be ignored. The results of site marker competitive experiment confirmed that the binding site of HSA primarily took place in site I. Furthermore, the molecular modeling study was consistent with these results. The study of circular dichroism spectra demonstrated that the presence of NADs decreased the α-helical content of HSA and induced the change of the secondary structure of HSA.


Assuntos
Antineoplásicos/química , Modelos Moleculares , Naftalimidas/química , Albumina Sérica/química , Dicroísmo Circular , Humanos , Interações Hidrofóbicas e Hidrofílicas , Estrutura Molecular , Espectrometria de Fluorescência , Termodinâmica
14.
Chem Biol Drug Des ; 78(6): 941-7, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21958160

RESUMO

A series of novel naphthalimide derivatives with 4-[4-(3,3-diphenylallyl)piperazin-1-yl]benzoic acid as side chain were designed and synthesized. Their antitumor activities were evaluated against a variety of cancer cell lines in vitro. Preliminary results showed that most of the derivatives had cytotoxic activity comparable with that of amonafide, with IC50 values of 10⁻6-10⁻5 M. Interestingly, compound 12e had the unique antitumor activity against MCF-7 among the cancer cell lines tested. More importantly, flow cytometric analysis indicated that compared with amonafide, the target compounds could effectively induce G2/M arrest and progress to apoptosis in HL-60 cells after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potential apoptosis-inducing and improved antitumor activity for further optimization.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/toxicidade , Ácido Benzoico/síntese química , Ácido Benzoico/toxicidade , Naftalimidas/síntese química , Naftalimidas/toxicidade , Adenina , Antineoplásicos/química , Apoptose , Ácido Benzoico/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Naftalimidas/química , Naftalimidas/farmacologia , Organofosfonatos , Relação Estrutura-Atividade
15.
Invest New Drugs ; 29(4): 646-58, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20179988

RESUMO

In the course of screening for novel anticancer compounds, B1 (N-(2-(Dimethylamino)ethyl)-2-aminothiazonaphthalimide), a novel naphthalimide-based DNA intercalator, was generated as a new anticancer candidate. For the first time, our investigation demonstrates that B1 inhibited the growth of HeLa cells by the induction of cell cycle arrest and apoptosis. Analysis of flow cytometry and western blots of HeLa cells treated with B1 revealed an appreciable cell cycle arrest and apoptotic induction in dose and time-dependent manner via the p53-dependent pathway. Furthermore, the release of cytochrome c from mitochondria was detected using confocal microscopy in HeLa cells treated with B1. Accordingly, these data demonstrate that the anticancer activity of B1 is associated with the activation of p53 and the release of cytochrome c, which suggest that B1 might have therapeutic potential against cervix carcinoma as an effective lead compound.


Assuntos
Apoptose/efeitos dos fármacos , Benzotiazóis/farmacologia , Ciclo Celular/efeitos dos fármacos , DNA de Neoplasias/metabolismo , Substâncias Intercalantes/farmacologia , Naftalimidas/farmacologia , Proteína Supressora de Tumor p53/metabolismo , Adenina , Benzotiazóis/química , Caspases/metabolismo , Ciclo Celular/genética , Proteínas de Ciclo Celular/genética , Proteínas de Ciclo Celular/metabolismo , Proliferação de Células/efeitos dos fármacos , Forma Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocromos c/metabolismo , Relação Dose-Resposta a Droga , Citometria de Fluxo , Fluorescência , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HeLa , Humanos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Naftalimidas/química , Necrose , Organofosfonatos , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , RNA Interferente Pequeno/metabolismo , Coloração e Rotulagem , Fatores de Tempo , Ensaio Tumoral de Célula-Tronco
16.
Eur J Med Chem ; 44(11): 4674-80, 2009 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-19643513

RESUMO

A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had comparable antitumor activities over Amonafide with the IC(50) values of 10(-6) to 10(-5)M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G(2)/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Naftalimidas/química , Naftalimidas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Fase G2/efeitos dos fármacos , Células HL-60 , Humanos
17.
Cancer Lett ; 283(2): 193-202, 2009 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-19435648

RESUMO

Amonafide, a naphthalimide derivative, although selected for exploratory clinical trials for its potent anticancer activity, has long been challenged by its unpredictable side effects. In the present study, a novel amonafide analogue, M(2)-A 2-(2-(dimethylamino)ethyl)-6-(thiophene-2-ylmethylamino)-1H-benzo[de]isoquinoline-1,3(2H)-dione was ascribed to its potent effects on topoisomerase IIalpha. Moreover, our investigation indicates that M(2)-A induces G(2)/M phase growth arrest through inhibiting PI3K/Akt pathway. M(2)-A inhibits proliferation of HeLa, HL60, HCT-8, A375, MCF-7 and MRC-5 cells, especially inhibits proliferation of HL60 with an IC(50) value of 18.86 microM. M(2)-A can not only induce DNA fragmentation, but also enhance Annexin V-FITC binding of the cells. On the one hand the expression levels of protein Cyclin B1, Cdk1 changed in response to M(2)-A treatment in HL60 cells. On the other hand we observed the inhibition of NF-kappaB nuclear translocation, up-regulation of Bax and down-regulation of Bcl-2, the caspase -3, -9 activity increase in HL60 cells after treated with M(2)-A, which indicated that the mitochondrial pathway was involved in the apoptosis signal pathway. Our results showed that the phosphorylation of p85/PI3K and Akt decreased following M(2)-A treatment. In summary, M(2)-A displayed a significant anti-tumor effect through cell cycle arrest and apoptotic induction in HL60 cells, which suggested that M(2)-A might have therapeutic potential against leukaemia.


Assuntos
Antineoplásicos/farmacologia , Naftalimidas/química , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Adenina , Apoptose/efeitos dos fármacos , Western Blotting , Linhagem Celular Tumoral , Fragmentação do DNA , Citometria de Fluxo , Fase G2/efeitos dos fármacos , Células HL-60 , Humanos , Microscopia de Fluorescência , Naftalimidas/farmacologia , Organofosfonatos , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Transdução de Sinais/fisiologia
18.
Bioorg Med Chem ; 17(2): 592-9, 2009 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-19109022

RESUMO

A series of novel naphthalimide derivatives with flexible leucine side chains were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had moderate antitumor activities with the IC(50) values of 10(-6)-10(-5) M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.


Assuntos
Aminoácidos/química , Antineoplásicos/síntese química , Naftalimidas/química , Aminoácidos/farmacologia , Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Desenho de Fármacos , Feminino , Humanos , Concentração Inibidora 50 , Substâncias Intercalantes , Leucina , Naftalimidas/farmacologia , Relação Estrutura-Atividade
19.
Blood ; 102(12): 4143-5, 2003 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-12893774

RESUMO

In mammals, it is well documented that observable circadian rhythms are controlled by a central oscillator that is organized in transcriptional and translational feedback loops involving several clock genes. Although recent studies have demonstrated that clock genes oscillate in many peripheral tissues, their characteristics in the human immune system remain unknown. The present study investigates whether circadian clock genes function in human peripheral blood mononuclear cells. On the basis of studies derived from 3 human subjects under controlled conditions, circadian clock genes hPer1, hPer2, hPer3, and hDec1 are expressed in a circadian manner in human peripheral blood mononuclear cells (PBMCs), with the peak level occurring during the habitual time of activity. The demonstration of functional circadian machinery in human PBMCs suggests that peripheral blood cells may be useful for the investigation of human circadian rhythms and their associated disorders.


Assuntos
Ritmo Circadiano/genética , Regulação da Expressão Gênica , Leucócitos Mononucleares/fisiologia , Atividades Cotidianas , Fatores de Transcrição Hélice-Alça-Hélice Básicos , Células Sanguíneas , Proteínas de Ciclo Celular , Hábitos , Proteínas de Homeodomínio/biossíntese , Proteínas de Homeodomínio/genética , Humanos , Leucócitos Mononucleares/metabolismo , Proteínas Nucleares/biossíntese , Proteínas Nucleares/genética , Proteínas Circadianas Period , Proteínas , Fatores de Tempo , Fatores de Transcrição
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