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1.
Inorg Chem ; 63(17): 7631-7639, 2024 Apr 29.
Artigo em Inglês | MEDLINE | ID: mdl-38625102

RESUMO

Two novel MoO42--templated luminescent silver alkynyl nanoclusters with 20-nuclearity ([(MoO42-)@Ag20(C≡CtBu)8(Ph2PO2)7(tfa)2]·(tfa-) (1)) and 18-nuclearity ([(MoO42-)@Ag18(C≡CtBu)8(Ph2PO2)7]·(OH) (2)) (tfa = trifluoroacetate) were synthesized with the green light maximum emissions at 507 and 516 nm, respectively. The nanoclusters were investigated and characterized by single-crystal X-ray crystallography, electrospray ionization mass spectrum (ESI-MS), X-ray photoelectron spectroscopy, thermogravimetry (TG), photoluminescence (PL), ultraviolet-visible (UV-vis) spectroscopy, and density functional theory calculations (DFT). The two nanoclusters differ in their structure by a supplementary [Ag2(tfa)2] organometallic surface motif, which significantly participates in the frontier molecular orbitals of 1, resulting in similar bonding patterns but different optical properties between the two clusters. Indeed, both nanoclusters show strong temperature-dependent photoluminescence properties, which make them potential candidates in the fields of optical devices for further applications.

2.
Opt Express ; 31(19): 30146-30159, 2023 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-37710563

RESUMO

Non-orthogonal multiple access (NOMA) has been studied as a promising multiple access technology for optical communication systems due to its superior spectral efficiency. However, the multi-user communication systems that employ NOMA with successive interference cancellation (SIC) suffer from error propagation (EP). Besides, the issue of non-ideal rise and fall time of the received signal can result in severe bit error rate (BER) degradation while decoding by the SIC technique. In this paper, we propose a straightforward two-stage program judgment filter (PJF) for signal reshaping and a SIC-free decoding method for NOMA. Based on the amplitude threshold (AT) decoding method, we demonstrate a real-time, two-user uplink underwater wireless optical communication (UWOC) system via field programmable gate arrays (FPGAs). With a power allocation ratio (PAR) of 2:1 (user 1: user 2), the established real-time NOMA-based UWOC system utilizing commercial light emitting diodes (LEDs) achieves a data rate of 30 Mbps for each user with BERs of 7.8 × 10-6 and 3 × 10-4 for user 1 and user 2, respectively. The results show that the AT-based NOMA can obtain a lower BER compared to the SIC-based NOMA, especially for user 2.

3.
Br J Neurosurg ; 37(5): 1292-1296, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33325256

RESUMO

BACKGROUND: Upper limb spasticity leads to different degrees of disabilities in cerebral palsy, which seriously affects the life of patients. Contralateral C7 nerve transfer has been shown to improve function and reduce spasticity in the affected upper limb with post-stroke hemiplegia. However, reports about the efficacy of this procedure in treating upper limb spasticity caused by hemiplegic cerebral palsy were limited. CASE DESCRIPTION: We reported two cases (a 23-year-old male and a 18-year-old female) who suffered from hemiplegic cerebral palsy with unilateral sustained upper limb spasticity and underwent contralateral C7 nerve transfer in adulthood. The scores of Fugel-Meyer and ROM of the affected upper limbs were observed before and after surgery. Compared with the preoperative, scores of the latest follow-up both were significantly improved. The muscle tension of the upper limbs decreased, and the symptoms of spasm were alleviated. CONCLUSIONS: Considering contralateral C7 nerve transfer could effectively relieve spasticity and improve upper limb activity, it can be recommended as one of the reliable methods to manage spasticity and dystonia of upper limbs in patients with hemiplegic cerebral palsy.


Assuntos
Paralisia Cerebral , Transferência de Nervo , Masculino , Feminino , Humanos , Adolescente , Adulto Jovem , Adulto , Paralisia Cerebral/complicações , Paralisia Cerebral/cirurgia , Transferência de Nervo/métodos , Hemiplegia/etiologia , Hemiplegia/cirurgia , Espasticidade Muscular/cirurgia , Espasticidade Muscular/complicações , Extremidade Superior/cirurgia
4.
Bioorg Med Chem Lett ; 25(12): 2540-4, 2015 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-25959813

RESUMO

A series of novel matrine-1H-1,2,3-triazole-chalcone conjugates was synthesized and their anticancer activity against A549, Bel-7402, Hela, and MCF-7 cancer cells was evaluated. Most of the conjugates displayed higher potency than their components. Compounds 6h and 6i exhibited more potent anticancer activity than 5-fluorouracil against the four tested human cancer cell lines and lower cytotoxicity to NIH3T3 normal cells. Flow cytometry tests demonstrated that compound 6h could induce apoptosis of A549 cells in a concentration-dependent manner. Moreover, 6h could efficiently suppress human tumor growth in mouse xenograft model without causing obvious toxicities.


Assuntos
Antineoplásicos/síntese química , Chalcona/química , Desenho de Fármacos , Alcaloides/química , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Fluoruracila/farmacologia , Células HeLa , Humanos , Células MCF-7 , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Células NIH 3T3 , Quinolizinas/química , Relação Estrutura-Atividade , Transplante Heterólogo , Triazóis/química , Matrinas
5.
Brain Inj ; 29(3): 396-402, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25671811

RESUMO

OBJECTIVE: To investigate whether electro-acupuncture can serve as a method of inducing brain ischaemic tolerance (BIT) by encouraging the expression of glutamate transporter-1 (GLT-1) and suppressing the release of glutamate (Glu). METHODS: Sprague-Dawley (SD) rats were divided into sham, ischaemia and EA groups. EA was performed on dazhui and baihui acupoints and the rat cerebral ischaemia model was achieved by occluding the middle cerebral artery (MCA) for 2 hours, followed by reperfusion. Dialysate was collected from the striatum in vivo to detect the concentration of Glu and the expression of Glutamate Transporter-1 (GLT-1) was examined. The changes of neurological deficit scores were evaluated at 24 hours after reperfusion, while the infarct volumes of brains were then measured with 2,3,5-triphenyltetrazolium chloride (TTC) staining. RESULTS: Compared with the ischaemia group, the concentration of Glu decreased and the expression of GLT-1 increased at most of the detective time points in the EA group; the neurological deficit scores were lower and the infarct volumes were smaller in the EA group. CONCLUSION: EA can up-regulate the expression of GLT-1 and inhibit the excessive release of Glu in the striatum in the process of subsequent ischaemic-reperfusion brain injury, which may be one of the mechanisms of inducing BIT and, thus, be neuroprotective for early ischaemic brain injury.


Assuntos
Terapia por Acupuntura/métodos , Isquemia Encefálica/patologia , Eletroacupuntura , Transportador 2 de Aminoácido Excitatório/metabolismo , Glutamatos/metabolismo , Animais , Modelos Animais de Doenças , Ratos , Ratos Sprague-Dawley , Regulação para Cima
6.
Zhong Yao Cai ; 38(6): 1230-6, 2015 Jun.
Artigo em Zh | MEDLINE | ID: mdl-26762065

RESUMO

OBJECTIVE: To explore the cardioprotective effect and its mechanism of total saponins of Panacis Majoris Rhizoma in myocardial infarction (MI) rats. METHODS: The MI model rats induced by ligating anterior descending branch of coronary artery were randomly divided into four group:model group, total saponins of Panacis Majoris Rhizoma (100 and 200 mg/kg) groups and compound Danshen dripping pills group. The rats were orally administrated with drugs once a day for four weeks. Another rats were selected as sham operation group. After four weeks intervention, cardiac function was examined, the serum levels of TNF-α, IL-1ß, IL-6 and IL-8 were measured by using ELISA, respectively. The myocardial hypertrophy index was investigated, the myocardial infarct size, degree of ventricular dilatation, myocardial interstitial collagen volume fraction and tissue morphology were investigated by HE, Masson, picric acid-sirius red staining and observing with alight microscope and electron microscope. Protein expressions of phosphorylation IκB-α( pIκB-α) and NF-κB p65 in heart tissue were detected by Western blotting. RESULTS: Total saponins of Panacis Majoris Rhizoma might significantly decrease the levels of serum TNF-α, IL-1ß, IL-6 and IL-8; decrease myocardial hypertrophy indexes, myocardial infarct size, degree of ventricular dilatation and myocardial interstitial collagen volume fraction; improve heart tissue morphology and cardiac function; downregulate protein expression of pIκB-α and NF-κBp65; and upregulate protein expression of SIRT1. The aforementioned action effects of total saponins of Panacis Majoris Rhizoma (200 mg/kg) were similar with compound Danshen dripping pills. CONCLUSION: Total saponins of Panacis Majoris Rhizoma possesses cardioprotective effect against ligating left anterior descending branch induced MI in rats. The mechanism may be related to strengthening SIRT1 expression, inhibiting the phosphorylation of IκB-α, and finally inhibiting the activation of NF-κB and proinflammatory production.


Assuntos
Cardiotônicos/química , Infarto do Miocárdio/tratamento farmacológico , Panax/química , Saponinas/química , Animais , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/química , Coração/efeitos dos fármacos , Proteínas I-kappa B/metabolismo , Interleucina-1beta/sangue , Interleucina-6/sangue , Interleucina-8/sangue , Miocárdio/patologia , Inibidor de NF-kappaB alfa , NF-kappa B , Ratos , Rizoma/química , Salvia miltiorrhiza , Fator de Transcrição RelA/metabolismo , Fator de Necrose Tumoral alfa/sangue
7.
J Stroke Cerebrovasc Dis ; 23(6): 1696-702, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24774439

RESUMO

Stroke is an acute cerebrovascular disease with high incidence, morbidity, and mortality. Preischemic treadmill training has been shown to be effective in improving behavioral and neuropathologic indices after cerebral ischemia. However, the exact neuroprotective mechanism of preischemic treadmill training against ischemic injury has not been elucidated clearly. The present study investigated whether preischemic treadmill training could protect the brain from ischemic injury via regulating cerebral blood flow (CBF) and endothelin 1 (ET-1). We analyzed the CBF by laser speckle imaging and ET-1 expression by an enzyme-linked immunosorbent assay using an ischemic rat model with preischemic treadmill training. Generally speaking, ET-1 expression decreased and CBF increased significantly in the pretreadmill group. It is worth noting that ET-1 expression is increased at 24 hours of reperfusion in the pretreadmill group compared with the level of the time after middle cerebral artery occlusion. These changes were followed by significant changes in neurologic deficits and cerebral infarct volume. This study indicated that preconditioning exercise protected brain from ischemic injury through the improvement of CBF and regulation of ET-1 expression, which may be a novel component of the neuroprotective mechanism of preischemic treadmill training against brain injury.


Assuntos
Isquemia Encefálica/fisiopatologia , Circulação Cerebrovascular/fisiologia , Endotelina-1/metabolismo , Precondicionamento Isquêmico/métodos , Condicionamento Físico Animal/fisiologia , Acidente Vascular Cerebral/fisiopatologia , Animais , Encéfalo/metabolismo , Encéfalo/patologia , Encéfalo/fisiopatologia , Isquemia Encefálica/metabolismo , Isquemia Encefálica/patologia , Modelos Animais de Doenças , Infarto da Artéria Cerebral Média/fisiopatologia , Masculino , Ratos , Ratos Sprague-Dawley , Acidente Vascular Cerebral/metabolismo , Acidente Vascular Cerebral/patologia
8.
Int J Mol Sci ; 15(3): 4453-63, 2014 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-24633199

RESUMO

Exercise training is a neuroprotective strategy in cerebral ischemic injury, but the underlying mechanisms are not yet clear. In the present study, we investigated the effects of treadmill exercise pretreatment on the expression of mitochondrial dynamic proteins. We examined the expression of OPA1/DLP1/MFF/Mfn1/Mfn2, which regulates mitochondrial fusion and fission, and cytochrome C oxidase subunits (COX subunits), which regulate mitochondrial functions, after middle cerebral artery occlusion (MCAO) in rats. T2-weighted magnetic resonance imaging (MRI) was evaluated as indices of brain edema after ischemia as well. Treadmill training pretreatment increased the expression levels of OPA1 and COXII/III/IV and alleviated brain edema, indicating that exercise pretreatment provided neuroprotection in cerebral ischemic injury via the regulation of mitochondrial dynamics and functions.


Assuntos
Isquemia Encefálica/metabolismo , GTP Fosfo-Hidrolases/metabolismo , Proteínas Mitocondriais/metabolismo , Condicionamento Físico Animal/fisiologia , Animais , Western Blotting , Encéfalo/irrigação sanguínea , Encéfalo/metabolismo , Encéfalo/patologia , Isquemia Encefálica/etiologia , Isquemia Encefálica/fisiopatologia , Dinaminas/metabolismo , Complexo IV da Cadeia de Transporte de Elétrons/metabolismo , Infarto da Artéria Cerebral Média/complicações , Infarto da Artéria Cerebral Média/metabolismo , Infarto da Artéria Cerebral Média/fisiopatologia , Imageamento por Ressonância Magnética , Masculino , Proteínas de Membrana/metabolismo , Dinâmica Mitocondrial/fisiologia , Ratos Sprague-Dawley , Fatores de Tempo
9.
Diagn Microbiol Infect Dis ; 109(2): 116264, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38493510

RESUMO

This study was performed to investigate the frequency of angiogenic T cells (CD4+ Tang cells) among CD4+ T cells in patients with hepatitis B-induced liver cirrhosis (HBV-LC) and to evaluate the predictive role of these cells in the clinical outcome. In total, 185 patients with HBV-LC were recruited to measure the frequency of CD4+ Tang cells and chemokine levels using flow cytometry. RESULTS: There was 11.4% of death after 3-momth follow-up. The AUC for the ability of the frequency of CD4+ Tang cell to predict death was 0.724 (higher than those for the MELD score, FIB-4 score, and Child-Pugh classification). Cox regression analysis revealed an association between the frequency of CD4+ Tang cells and a 3-month survival chance. CONCLUSIONS: The lower frequency of CD4+ T ang cells was correlated with the severity of HBV-LC and may serve as a prognostic predictor.


Assuntos
Linfócitos T CD4-Positivos , Cirrose Hepática , Humanos , Masculino , Feminino , Cirrose Hepática/virologia , Prognóstico , Pessoa de Meia-Idade , Linfócitos T CD4-Positivos/imunologia , Adulto , Hepatite B/complicações , Citometria de Fluxo , Quimiocinas/sangue , Hepatite B Crônica/complicações , Idoso
10.
Front Chem ; 12: 1384301, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38562527

RESUMO

Introduction: Cancer, a significant global health concern, necessitates innovative treatments. The pivotal role of chronic inflammation in cancer development underscores the urgency for novel therapeutic strategies. Benzothiazole derivatives exhibit promise due to their distinctive structures and broad spectrum of biological effects. This study aims to explore new anti-tumor small molecule drugs that simultaneously anti-inflammatory and anticancer based on the advantages of benzothiazole frameworks. Methods: The compounds were characterized by nuclear magnetic resonance (NMR), liquid chromatograph-mass spectrometer (LC-MS) and high performance liquid chromatography (HPLC) for structure as well as purity and other related physicochemical properties. The effects of the compounds on the proliferation of human epidermoid carcinoma cell line (A431) and human non-small cell lung cancer cell lines (A549, H1299) were evaluated by MTT method. The effect of compounds on the expression levels of inflammatory factors IL-6 and TNF-α in mouse monocyte macrophages (RAW264.7) was assessed using enzyme-linked immunosorbent assay (ELISA). The effect of compounds on apoptosis and cell cycle of A431 and A549 cells was evaluated by flow cytometry. The effect of compounds on A431 and A549 cell migration was evaluated by scratch wound healing assay. The effect of compounds on protein expression levels in A431 and A549 cells was assessed by Western Blot assay. The physicochemical parameters, pharmacokinetic properties, toxicity and drug similarity of the active compound were predicted using Swiss ADME and admetSAR web servers. Results: Twenty-five novel benzothiazole compounds were designed and synthesized, with their structures confirmed through spectrogram verification. The active compound 6-chloro-N-(4-nitrobenzyl) benzo[d] thiazol-2-amine (compound B7) was screened through a series of bioactivity assessments, which significantly inhibited the proliferation of A431, A549 and H1299 cancer cells, decreased the activity of IL-6 and TNF-α, and hindered cell migration. In addition, at concentrations of 1, 2, and 4 µM, B7 exhibited apoptosis-promoting and cell cycle-arresting effects similar to those of the lead compound 7-chloro-N-(2, 6-dichlorophenyl) benzo[d] thiazole-2-amine (compound 4i). Western blot analysis confirmed that B7 inhibited both AKT and ERK signaling pathways in A431 and A549 cells. The prediction results of ADMET indicated that B7 had good drug properties. Discussion: This study has innovatively developed a series of benzothiazole derivatives, with a focus on compound B7 due to its notable dual anticancer and anti-inflammatory activities. B7 stands out for its ability to significantly reduce cancer cell proliferation in A431, A549, and H1299 cell lines and lower the levels of inflammatory cytokines IL-6 and TNF-α. These results position B7B7 as a promising candidate for dual-action cancer therapy. The study's mechanistic exploration, highlighting B7's simultaneous inhibition of the AKT and ERK pathways, offers a novel strategy for addressing both the survival mechanisms of tumor cells and the inflammatory milieu facilitating cancer progression.

11.
Int J Mol Sci ; 13(8): 9447-9459, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22949807

RESUMO

Pre-ischemic treadmill training exerts cerebral protection in the prevention of cerebral ischemia by alleviating neurotoxicity induced by excessive glutamate release following ischemic stroke. However, the underlying mechanism of this process remains unclear. Cerebral ischemia-reperfusion injury was observed in a rat model after 2 weeks of pre-ischemic treadmill training. Cerebrospinal fluid was collected using the microdialysis sampling method, and the concentration of glutamate was determined every 40 min from the beginning of ischemia to 4 h after reperfusion with high-performance liquid chromatography (HPLC)-fluorescence detection. At 3, 12, 24, and 48 h after ischemia, the expression of the glutamate transporter-1 (GLT-1) protein in brain tissues was determined by Western blot respectively. The effect of pre-ischemic treadmill training on glutamate concentration and GLT-1 expression after cerebral ischemia in rats along with changes in neurobehavioral score and cerebral infarct volume after 24 h ischemia yields critical information necessary to understand the protection mechanism exhibited by pre-ischemic treadmill training. The results demonstrated that pre-ischemic treadmill training up-regulates GLT-1 expression, decreases extracellular glutamate concentration, reduces cerebral infarct volume, and improves neurobehavioral score. Pre-ischemic treadmill training is likely to induce neuroprotection after cerebral ischemia by regulating GLT-1 expression, which results in re-uptake of excessive glutamate.


Assuntos
Lesões Encefálicas/prevenção & controle , Isquemia Encefálica/prevenção & controle , Transportador 2 de Aminoácido Excitatório/metabolismo , Terapia por Exercício/métodos , Glutamatos/metabolismo , Infarto da Artéria Cerebral Média/prevenção & controle , Fármacos Neuroprotetores , Animais , Western Blotting , Lesões Encefálicas/metabolismo , Isquemia Encefálica/metabolismo , Terapia por Exercício/instrumentação , Infarto da Artéria Cerebral Média/metabolismo , Masculino , Microdiálise , Ratos , Ratos Sprague-Dawley
12.
ACS Omega ; 7(19): 16817-16826, 2022 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-35601319

RESUMO

g-C3N4-based materials show potential for photoreduction of CO2 to oxygenates but are subjected to fast recombination of photogenerated charge carriers. Here, a novel Cu-dispersive protonated g-C3N4 (PCN) metal-semiconductor (m-s) heterojunction from thermal reduction of a Cu2O/PCN precursor was prepared and characterized using in situ X-ray diffraction, scanning transmission electron microscopy, X-ray photoelectron spectroscopy, ultraviolet-visible (UV-vis) spectra, photoluminescence (PL) spectra, transient photocurrent response, and electrochemical impedance spectroscopy (EIS). The Cu amount in Cu/PCN and the reduction temperature affected the generation of CH3OH and C2H5OH from the photoreaction of CO2-aerated H2O. During calcination of Cu2O/PCN in N2 at 550 °C, Cu2O was completely reduced to Cu with even dispersion, and a m-s heterojunction was obtained. With thermal exfoliation, Cu/PCN showed a specific surface area and layer spacing larger than those of PCN. Cu/PCN-0.5 (12.8 wt % Cu) exhibited a total carbon yield of 25.0 µmol·g-1 under UV-vis irradiation for 4 h, higher than that of Cu2O/PCN (13.6 µmol·g-1) and PCN (6.0 µmol·g-1). The selectivity for CH3OH and C2H5OH was 51.42 and 46.14%, respectively. The PL spectra, transient photocurrent response, and EIS characterizations indicated that Cu/PCN heterojunction promotes the separation of electrons and holes and suppresses their recombination. The calculated conduction band position was more negative, which is conducive to the multielectron reactions for CH3OH and C2H5OH generation.

14.
Adv Mater ; 34(46): e2107262, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34677908

RESUMO

Perovskite-type oxides, characterized by excellent multifunctional physical and chemical properties, are widely used in ferroelectric, piezoelectric, energy conversion, and storage applications. It is shown here that the perovskite-type SrVO3 can achieve excellent electrochemical performance as lithium-ion battery anodes thanks to its high electrically and ionically conductivity. Conducting additive-free SrVO3 electrodes can deliver a high specific capacity of 324 mAh g-1 at a safe and low average working potential of ≈0.9 V vs Li/Li+ together with excellent high-rate performance. A high areal capacity of ≈5.4 mAh cm-2 is obtained using an ultrathick (≈120 µm) electrode. Moreover, the fully lithiated SrVO3 electrode exhibits only 2.3% volume expansion that is explained by a simple solid-solution Li+ -storage mechanism, resulting in good cycling stability of the electrode. This study highlights the perovskite-type SrVO3 as a promising Li+ -storage anode and provides opportunities for exploring a variety of perovskite oxides as next-generation metal-ion battery anodes.

15.
Sci Bull (Beijing) ; 67(22): 2305-2315, 2022 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-36546221

RESUMO

Perovskite SrVO3 has been investigated as a promising lithium storage anode where the V cation plays the role of the redox center, combining excellent cycle stability and safe operating potential versus Li metal plating, with limited capacity. Here, we demonstrate the possibility to boost the lithium storage properties, by reducing the non-redox active Sr cation content and fine-tuning the O anion vacancies while maintaining a non-stoichiometric SrxVO3-δ perovskite structure. Theoretical investigations suggest that Sr vacancy can work as favorable Li+ storage sites and preferential transport channels for guest Li+ ions, contributing to the increased specific capacity and rate performance. In contrast, inducing O anion vacancy in SrxVO3-δ can improve rate performance while compromising the specific capacity. Our experimental results confirm the enhancement of specific capacities by fine adjusting the Sr and O vacancies, with a maximum capacity of 444 mAh g-1 achieved with Sr0.63VO3-δ, which is a 37% increase versus stoichiometric SrVO3. Although rich defects have been induced, SrxVO3-δ electrodes maintain a stable perovskite structure during cycling versus a LiFePO4 cathode, and the full-cell could achieve more than 6000 discharge/charge cycles with 80% capacity retention. This result highlights the possibility to use the cation defective-based engineering approach to design high-capacity perovskite oxide anode materials.

16.
Wei Sheng Yan Jiu ; 40(6): 720-2, 2011 Nov.
Artigo em Zh | MEDLINE | ID: mdl-22279664

RESUMO

OBJECTIVE: To measure the energy expenditure of healthy adults engaged in light activities in southern China, and to provide reference database for revising Chinese RNI. METHODS: Thirty four healthy adults eligible for the energy metabolic experiment were selected. A 3-day recycled dietary prescription was designed. The food intake of all foods per person per meal were weighed and recorded, and the energy intake from diets was determined by chemical analysis. The energy expenditure was calculated by combining the change of body weight and dietary consumption. RESULTS: The average energy intake was (8424 +/- 1616) kJ/d [(2013 +/- 386) kcal/d], which was (9990 +/- 798) kJ/d [(2388 +/- 191) kcal/d] for men and (7032 +/- 384)kJ/d [(1681 +/- 92) kcal/d] for women. The average change of body weight of all subjects in 16 days was reduced 0.02 kg, the men increased 0.15 kg, and the women decreased 0.17 kg. According to the energy balance principle, the ultimate energy expenditure of healthy adults in southern China was (8468 +/- 1762) kJ/d [(2024 +/- 421) kcal/d], the men was (9680 +/- 1759) kJ/d [(2314 +/- 420) kcal/d], and the women was (7391 +/- 827) kJ/d [(1767 +/- 198) kcal/d]. CONCLUSIONS: The energy expenditure of healthy adult male engaged in light activities in southern China was 9680 +/- 1759 kJ/d [(2314 +/- 420 kcal/d)], and that of female was 7391 +/- 827 kJ/d [(1767 +/- 198 kcal/d)]. The energy expenditure of men and women measured in this study were 86kcal and 333kcal lower than the Chinese energy RNI (2400kcal and 2100 kcal) established in 2000.


Assuntos
Metabolismo Basal/fisiologia , Ingestão de Energia/fisiologia , Metabolismo Energético/fisiologia , Alimentos/normas , Adolescente , Adulto , Peso Corporal , China , Inquéritos sobre Dietas , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Atividade Motora/fisiologia , Adulto Jovem
17.
Biology (Basel) ; 10(7)2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-34203341

RESUMO

TGF-ß signaling plays a pivotal role in promoting tumor cell migration and cancer metastasis. ΔNp63α and TAp63α are two major isoforms of p53-related p63 protein. Our recent study has shown that TGF-ß1 promotes ΔNp63α protein degradation to facilitate cancer metastasis. However, whether TAp63α is involved in TGF-ß1-induced cancer metastasis remains unclear. In this study, we show that, in human pancreatic cancer MIA PaCa-2 cells harboring p53-R248W allele, TGF-ß1 can significantly inhibit TAp63α protein stability in a Smad pathway-independent manner. Lysosome inhibitor, chloroquine, but not proteasome inhibitor MG132, can rescue TGF-ß1-induced downregulation of TAp63α protein. In addition, we show that either TGF-ß1 treatment or silencing of TAp63α can dramatically increase migration of MIA PaCa-2 cells. Importantly, the restored expression of TAp63α can effectively block TGF-ß1-induced migration of MIA PaCa-2 cells. Mechanistically, we show that TGF-ß1 promotes TAp63α protein degradation, leading to upregulation of p53-R248W protein expression, and consequently resulting in elevated MIA PaCa-2 cell migration. Together, this study indicates that lysosomal degradation is an important way for regulating TAp63α protein fate and highlights that TGF-ß1-TAp63α-mutant p53 axis is critically important in pancreatic cancer metastasis.

18.
Eur J Med Chem ; 218: 113362, 2021 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-33774344

RESUMO

Signal transducer and activator of transcription 3 (STAT3) has been confirmed as an attractive therapeutic target for cancer therapy. Herein, we designed and synthesized a series of N-substituted Sulfamoylbenzamide STAT3 inhibitors based on small-molecule STAT3 inhibitor Niclosamide. Compound B12, the best active compound of this series, was identified as an inhibitor of IL-6/STAT3 signaling with an IC50 of 0.61-1.11 µM in MDA-MB-231, HCT-116 and SW480 tumor cell lines with STAT3 overexpression, by inhibiting the phosphorylation of STAT3 of Tyr705 residue and the expression of STAT3 downstream genes, inducing apoptosis and inhibiting the migration of cancer cells. Furthermore, in vivo study revealed that compound B12 suppressed the MDA-MB-231 xenograft tumor growth in nude mice at the dose of 30 mg/kg (i.g.), which has better antitumor activity than the positive control Niclosamide. More importantly, B12 is an orally bioavailable anticancer agent as a promising candidate for further development.


Assuntos
Benzamidas/farmacologia , Descoberta de Drogas , Niclosamida/farmacologia , Fator de Transcrição STAT3/antagonistas & inibidores , Benzamidas/síntese química , Benzamidas/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Niclosamida/síntese química , Niclosamida/química , Fator de Transcrição STAT3/metabolismo , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
19.
Br J Nutr ; 104(12): 1817-23, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-20804631

RESUMO

The objective of the present study is to measure basal energy expenditure (BEE) using the Cosmed K4b² portable metabolic system (Rome, Italy) and to develop a new predictive equation for BEE in southern Chinese adults. A total of 165 healthy Chinese adults aged 18-45 years with normal body weight were involved in the present study. BEE was measured by Cosmed K4b². Body composition was determined by body composition analysers (ImpediMed DF50, QLD, Australia). Multiple linear regression analysis and correlation analysis were applied to develop a new optimal equation for predicting BEE of southern healthy Chinese adults. Measured BEE (mBEE) of southern Chinese healthy adults was 5513 (sem 96) kJ/d, which was similar to the results predicted by the equation developed by of Liu 5579 (sem 57) kJ/d (P = 0·37) and significantly lower than those from equations developed by Henry (5763 (sem 54) kJ/d), Schofield (5898 (sem 58) kJ/d) and Harris-Benedict (HB; 5863 (sem 51) kJ/d) (all P = 0·001). The optimal equation developed by our data was BEE (kJ/d) = 277+89 weight (kg)+600 sex (male = 1 and female = 0) (r² = 0·48, n 165). For males, BEE (kJ/d) = 105 weight (kg) - 58 (r² = 0·27, n 79); for females, BEE (kJ/d) = 69 weight (kg)+1335 (r² = 0·24, n 86). In conclusion, the mBEE of southern Chinese healthy adults was 5513 (sem 96) kJ/d. The BMR of Chinese adults of normal weight is overestimated by widely used prediction equations developed by Henry, Schofield and HB. The equation developed in the present study (equation 7) can be used in predicting BEE for Chinese adults aged 18-45 years with normal body weight.


Assuntos
Povo Asiático , Metabolismo Basal/fisiologia , Adolescente , Adulto , Composição Corporal , Superfície Corporal , China , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Troca Gasosa Pulmonar , Adulto Jovem
20.
Clin Exp Pharmacol Physiol ; 37(2): 150-5, 2010 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-19566840

RESUMO

1. Resveratrol (RSV), a polyphenol in red wine, exhibits cardioprotective effects in vitro, such as inhibition of angiotensin II- or phenylephrine-induced cardiomyocyte hypertrophy in rat neonatal myocyte cultures and suppression of cardiac fibroblast proliferation. The aim of the present study was to investigate the protective effects of RSV against monocrotaline (MCT)-induced right ventricular (RV) hypertrophy in rats. 2. Male Sprague-Dawley rats were given a single injection of MCT (50 mg/kg, s.c.) and were then treated with either vehicle (normal saline) or RSV (10 and 30 mg/kg, i.g., twice daily) for 21 days. A separate group of control rats were not injected with MCT and were treated with normal saline for 21 days. At the end of the treatment period, all rats were subjected to echocardiography and haemodynamic measurements. In addition, after rats had been killed, the hearts were subjected to histopathological, untrastructural and immunohistochemical analyses. 3. In vehicle-treated rats, MCT injection resulted in 33% mortality, whereas mortality in RSV-treated MCT-injected rats was 0%. In vehicle-treated rats, MCT increased RV free wall thickness and RV systolic pressure and decreased pulmonary arterial acceleration time at the end of the experimental period. These dynamic changes were ameliorated by RSV in a dose-dependent manner. Histologically, MCT injection resulted in RV hypertrophy, swollen mitochrondria and cardiomyocyte apoptosis; all these morphological changes were dose-dependently improved in rats treated with RSV. 4. In conclusion, RSV inhibits the RV hypertrophy induced by MCT in rats and this effect is mediated by both a direct effect of RSV on cardiomyocytes and an indirect effect mediated via a reduction in pulmonary hypertension.


Assuntos
Cardiotônicos/administração & dosagem , Hipertrofia Ventricular Direita/prevenção & controle , Estilbenos/administração & dosagem , Animais , Apoptose/efeitos dos fármacos , Coração/anatomia & histologia , Coração/fisiopatologia , Hipertrofia Ventricular Direita/induzido quimicamente , Hipertrofia Ventricular Direita/fisiopatologia , Masculino , Monocrotalina/farmacologia , Miocárdio/patologia , Ratos , Ratos Sprague-Dawley , Resveratrol
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