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1.
New Phytol ; 2024 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-38922886

RESUMO

Acyl-CoA-Binding Proteins (ACBPs) bind acyl-CoA esters and function in lipid metabolism. Although acbp3-1, the ACBP3 mutant in Arabidopsis thaliana ecotype Col-0, displays normal floral development, the acbp3-2 mutant from ecotype Ler-0 characterized herein exhibits defective adaxial anther lobes and improper sporocyte formation. To understand these differences and identify the role of ERECTA in ACBP3 function, the acbp3 mutants and acbp3-erecta (er) lines were analyzed by microscopy for anther morphology and high-performance liquid chromatography for lipid composition. Defects in Landsberg anther development were related to the ERECTA-mediated pathway because the progenies of acbp3-2 × La-0 and acbp3-1 × er-1 in Col-0 showed normal anthers, contrasting to that of acbp3-2 in Ler-0. Polymorphism in the regulatory region of ACBP3 enabled its function in anther development in Ler-0 but not Col-0 which harbored an AT-repeat insertion. ACBP3 expression and anther development in acbp3-2 were restored using ACBP3pro (Ler)::ACBP3 not ACBP3pro (Col)::ACBP3. SPOROCYTELESS (SPL), a sporocyte formation regulator activated ACBP3 transcription in Ler-0 but not Col-0. For anther development, the ERECTA-related role of ACBP3 is required in Ler-0, but not Col-0. The disrupted promoter regulatory region for SPL binding in Col-0 eliminates the role of ACBP3 in anther development.

2.
Nature ; 549(7670): 43-47, 2017 09 07.
Artigo em Inglês | MEDLINE | ID: mdl-28825707

RESUMO

Quantum key distribution (QKD) uses individual light quanta in quantum superposition states to guarantee unconditional communication security between distant parties. However, the distance over which QKD is achievable has been limited to a few hundred kilometres, owing to the channel loss that occurs when using optical fibres or terrestrial free space that exponentially reduces the photon transmission rate. Satellite-based QKD has the potential to help to establish a global-scale quantum network, owing to the negligible photon loss and decoherence experienced in empty space. Here we report the development and launch of a low-Earth-orbit satellite for implementing decoy-state QKD-a form of QKD that uses weak coherent pulses at high channel loss and is secure because photon-number-splitting eavesdropping can be detected. We achieve a kilohertz key rate from the satellite to the ground over a distance of up to 1,200 kilometres. This key rate is around 20 orders of magnitudes greater than that expected using an optical fibre of the same length. The establishment of a reliable and efficient space-to-ground link for quantum-state transmission paves the way to global-scale quantum networks.

3.
Sensors (Basel) ; 23(10)2023 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-37430637

RESUMO

Telemetry data are the most important basis for ground operators to assess the status of satellites in orbit, and telemetry data-based anomaly detection has become a key tool to improve the reliability and safety of spacecrafts. Recent research on anomaly detection focuses on constructing a normal profile of telemetry data using deep learning methods. However, these methods cannot effectively capture the complex correlations between the various dimensions of telemetry data, and thus cannot accurately model the normal profile of telemetry data, resulting in poor anomaly detection performance. This paper presents CLPNM-AD, contrastive learning with prototype-based negative mixing for correlation anomaly detection. The CLPNM-AD framework first employs an augmentation process with random feature corruption to generate augmented samples. Following that, a consistency strategy is employed to capture the prototype of samples, and then prototype-based negative mixing contrastive learning is used to build a normal profile. Finally, a prototype-based anomaly score function is proposed for anomaly decision-making. Experimental results on public datasets and datasets from the actual scientific satellite mission show that CLPNM-AD outperforms the baseline methods, achieves up to 11.5% improvement based on the standard F1 score and is more robust against noise.

4.
Phys Rev Lett ; 120(3): 030501, 2018 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-29400544

RESUMO

We perform decoy-state quantum key distribution between a low-Earth-orbit satellite and multiple ground stations located in Xinglong, Nanshan, and Graz, which establish satellite-to-ground secure keys with ∼kHz rate per passage of the satellite Micius over a ground station. The satellite thus establishes a secure key between itself and, say, Xinglong, and another key between itself and, say, Graz. Then, upon request from the ground command, Micius acts as a trusted relay. It performs bitwise exclusive or operations between the two keys and relays the result to one of the ground stations. That way, a secret key is created between China and Europe at locations separated by 7600 km on Earth. These keys are then used for intercontinental quantum-secured communication. This was, on the one hand, the transmission of images in a one-time pad configuration from China to Austria as well as from Austria to China. Also, a video conference was performed between the Austrian Academy of Sciences and the Chinese Academy of Sciences, which also included a 280 km optical ground connection between Xinglong and Beijing. Our work clearly confirms the Micius satellite as a robust platform for quantum key distribution with different ground stations on Earth, and points towards an efficient solution for an ultralong-distance global quantum network.

5.
Bioorg Chem ; 71: 299-304, 2017 04.
Artigo em Inglês | MEDLINE | ID: mdl-28267982

RESUMO

A series of 2-morpholinetetraphenylporphyrins functionalized with various substituents (Cl, Me, MeO group) at 4-phenyl position were prepared via nucleophilic substitution of 2-nitroporphyrin copper derivatives with morpholine by refluxing under a nitrogen atmosphere and then demetalization. Their basic photophysical properties, intracellular localization, cytotoxicities in vitro and in vivo were also investigated. All synthesized photosensitizers exhibited longer maxima absorption wavelengths than Hematoporphyrin monomethyl ether (HMME). They showed low dark cytotoxicity compared with that of HMME and were more phototoxic than HMME against Eca-109 cells in vitro. M3 also exhibited better photodynamic antitumor efficacy on BALB/c nude mice at a lower concentration. Therefore, M3 is a promising antitumor photosensitizer in photodynamic therapy application.


Assuntos
Morfolinas/química , Morfolinas/uso terapêutico , Neoplasias/tratamento farmacológico , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/uso terapêutico , Porfirinas/química , Porfirinas/uso terapêutico , Animais , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Feminino , Hematoporfirinas/farmacologia , Humanos , Camundongos Endogâmicos BALB C , Camundongos Nus , Morfolinas/síntese química , Morfolinas/farmacologia , Fotoquimioterapia , Fármacos Fotossensibilizantes/síntese química , Fármacos Fotossensibilizantes/farmacologia , Porfirinas/síntese química , Porfirinas/farmacologia
6.
Biol Pharm Bull ; 40(12): 2088-2095, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29199233

RESUMO

This study aimed to investigate the effect of hematoporphyrin dimethylether (HDME)-mediated photodynamic therapy for laser-induced choroidal neovascularization (CNV) in adult Brown Norway rats. HDME was administered via tail vein at 14 d after the laser photocoagulation, and the rats received irradiance with a laser light at 570 nm at 15 min after injection. CNV was evaluated by fundus photography, fundus fluorescein angiography, optical coherence tomography, and hematoxylin and eosin staining. We found that CNV was occurred at 7 d after photocoagulation and reaching peak activity at 14 d after photocoagulation. There is a significant reduction in the total area of the fluorescein leakage and the number of strong fluorescein leakage spots on 7 d after HDME-mediated photodynamic therapy (PDT). The results suggest that HDME-mediated PDT inhibits laser-induced CNV in rats, representing a promising therapy for wet age-related macular degeneration.


Assuntos
Neovascularização de Coroide/tratamento farmacológico , Hematoporfirinas/uso terapêutico , Éteres Metílicos/uso terapêutico , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/uso terapêutico , Animais , Permeabilidade Capilar , Neovascularização de Coroide/diagnóstico por imagem , Neovascularização de Coroide/etiologia , Modelos Animais de Doenças , Angiofluoresceinografia , Fundo de Olho , Hematoporfirinas/química , Humanos , Lasers/efeitos adversos , Masculino , Éteres Metílicos/química , Fármacos Fotossensibilizantes/química , Ratos , Ratos Endogâmicos BN
7.
Plant Mol Biol ; 92(6): 717-730, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27645136

RESUMO

Arabidopsis thaliana ACYL-COA-BINDING PROTEIN6 (AtACBP6) encodes a cytosolic 10-kDa AtACBP. It confers freezing tolerance in transgenic Arabidopsis, possibly by its interaction with lipids as indicated by the binding of acyl-CoA esters and phosphatidylcholine to recombinant AtACBP6. Herein, transgenic Arabidopsis transformed with an AtACBP6 promoter-driven ß-glucuronidase (GUS) construct exhibited strong GUS activity in the vascular tissues. Immunoelectron microscopy using anti-AtACBP6 antibodies showed AtACBP6 localization in the phloem especially in the companion cells and sieve elements. Also, the presence of gold grains in the plasmodesmata indicated its potential role in systemic trafficking. The AtACBP6 protein, but not its mRNA, was found in phloem exudate of wild-type Arabidopsis. Fatty acid profiling using gas chromatography-mass spectrometry revealed an increase in the jasmonic acid (JA) precursor, 12-oxo-cis,cis-10,15-phytodienoic acid (cis-OPDA), and a reduction in JA and/or its derivatives in acbp6 phloem exudates in comparison to the wild type. Quantitative real-time PCR showed down-regulation of COMATOSE (CTS) in acbp6 rosettes suggesting that AtACBP6 affects CTS function. AtACBP6 appeared to affect the content of JA and/or its derivatives in the sieve tubes, which is consistent with its role in pathogen-defense and in its wound-inducibility of AtACBP6pro::GUS. Taken together, our results suggest the involvement of AtACBP6 in JA-biosynthesis in Arabidopsis phloem tissues.


Assuntos
Proteínas de Arabidopsis/metabolismo , Arabidopsis/metabolismo , Proteínas de Transporte/metabolismo , Ciclopentanos/metabolismo , Oxilipinas/metabolismo , Floema/metabolismo , Arabidopsis/genética , Proteínas de Arabidopsis/genética , Proteínas de Transporte/genética
8.
World J Surg Oncol ; 14(1): 10, 2016 Jan 14.
Artigo em Inglês | MEDLINE | ID: mdl-26762567

RESUMO

BACKGROUND: The invasion of colon cancer is associated with the tumor angiogenesis. Endostatin is an important anti-angiogenic agent, and the additive effect of endostatin with a chemotherapeutic agent, cyclophosphamide, on micrangium has not been established. METHODS: Male BALB/c strain nude mice were injected with human colorectal carcinoma cells (HCT-116). The mice were divided into four groups (n=15, each group) and were treated with different concentrations of endostatin (15, 10, and 5 mg/kg/day), cyclophosphamide (20, 10, and 5 mg/kg/day), and combination of endostatin/cyclophosphamide (15+20, 15+10, and 15+5 mg/kg/day). The tumor inhibition rate was evaluated, followed by the quantification of messenger ribonucleic acid (mRNA) and protein expression of notch signaling components NOTCH-1, NOTCH-3, NOTCH-4, JAG-1, DLL-4, Hes-1, and Hey-1 using quantitative polymerase chain reaction (qPCR). The protein expression of NOTCH-3, JAG-1, and DLL-4 was confirmed using western blotting. Microvessel density (MVD) was evaluated to detect micrangium following the treatment. RESULTS: The endostatin/cyclophosphamide-treated samples exhibited an additive effect on the tumor inhibition rate and the microvessel count. NOTCH-1, NOTCH-3, NOTCH-4, JAG-1, Hes-1, and Hey-1 expression levels were highly correlated and downregulated in the treated samples, whereas DLL-4 expression was upregulated that accounted for its anti-angiogenic property. CONCLUSIONS: The combination treatment of colon cancer with endostatin and a chemotherapeutic agent, cyclophosphamide proves to be an efficient therapeutic strategy to inhibit the rapid vasculature formation confirmed by the differential expression of notch signaling components.


Assuntos
Antineoplásicos/farmacologia , Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Neoplasias do Colo/tratamento farmacológico , Ciclofosfamida/farmacologia , Endostatinas/farmacologia , Microvasos/efeitos dos fármacos , Neovascularização Patológica/tratamento farmacológico , Animais , Antineoplásicos/uso terapêutico , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Biomarcadores Tumorais/metabolismo , Western Blotting , Linhagem Celular Tumoral , Neoplasias do Colo/metabolismo , Neoplasias do Colo/patologia , Ciclofosfamida/uso terapêutico , Relação Dose-Resposta a Droga , Esquema de Medicação , Endostatinas/uso terapêutico , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Reação em Cadeia da Polimerase , Distribuição Aleatória , Receptores Notch/metabolismo , Transdução de Sinais/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto
9.
Appl Microbiol Biotechnol ; 99(3): 1485-97, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25261128

RESUMO

This study investigated methanogenic communities involved in degradation of tetramethylammonium hydroxide (TMAH) in three full-scale bioreactors treating TMAH-containing wastewater. Based on the results of terminal-restriction fragment-length polymorphism (T-RFLP) and quantitative PCR analyses targeting the methyl-coenzyme M reductase alpha subunit (mcrA) genes retrieved from three bioreactors, Methanomethylovorans and Methanosarcina were the dominant methanogens involved in the methanogenic degradation of TMAH in the bioreactors. Furthermore, batch experiments were conducted to evaluate mcrA messenger RNA (mRNA) expression during methanogenic TMAH degradation, and the results indicated that a higher level of TMAH favored mcrA mRNA expression by Methansarcina, while Methanomethylovorans could only express considerable amount of mcrA mRNA at a lower level of TMAH. These results suggest that Methansarcina is responsible for methanogenic TMAH degradation at higher TMAH concentrations, while Methanomethylovorans may be important at a lower TMAH condition.


Assuntos
Bactérias/metabolismo , Reatores Biológicos/microbiologia , Metano/metabolismo , Compostos de Amônio Quaternário/metabolismo , Bactérias/classificação , Bactérias/genética , Bactérias/isolamento & purificação , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Polimorfismo de Fragmento de Restrição , Esgotos/microbiologia
10.
Chem Biol Interact ; 395: 111013, 2024 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-38663798

RESUMO

Ulcerative colitis is a chronic disease with colonic mucosa injury. Nitazoxanide is an antiprotozoal drug in clinic. Nitazoxanide and its metabolite tizoxanide have been demonstrated to activate AMPK and inhibit inflammation, therefore, the aim of the present study is to investigate the effect of nitazoxanide on dextran sulfate sodium (DSS)-induced colitis and the underlying mechanism. Oral administration of nitazoxanide ameliorated the symptoms of mice with DSS-induced colitis, as evidenced by improving the increased disease activity index (DAI), the decreased body weight, and the shortened colon length. Oral administration of nitazoxanide ameliorated DSS-induced intestinal barrier dysfunction and reduced IL-6 and IL-17 expression in colon tissues. Mechanistically, nitazoxanide and its metabolite tizoxanide treatment activated AMPK and inhibited JAK2/STAT3 signals. Nitazoxanide and tizoxanide treatment increased caudal type homeobox 2 (CDX2) expression, increased alkaline phosphatase (ALP) activity and promoted tight junctions in Caco-2 cells. Nitazoxanide and tizoxanide treatment restored the decreased zonula occludens-1(ZO-1) and occludin protein levels induced by LPS or IL-6 in Caco-2 cells. On the other hand, nitazoxanide and tizoxanide regulated macrophage bias toward M2 polarization, as evidenced by the increased arginase-1expression in bone marrow-derived macrophages (BMDM). Nitazoxanide and tizoxanide reduced the increased IL-6, iNOS and CCL2 pro-inflammatory gene expressions and inhibited JAK2/STAT3 activation in BMDM induced by LPS. In conclusion, nitazoxanide protects against DSS-induced ulcerative colitis in mice through improving intestinal barrier and inhibiting inflammation and the underlying mechanism involves AMPK activation and JAK2/STAT3 inhibition.


Assuntos
Colite Ulcerativa , Sulfato de Dextrana , Mucosa Intestinal , Nitrocompostos , Fator de Transcrição STAT3 , Tiazóis , Animais , Tiazóis/farmacologia , Tiazóis/uso terapêutico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/patologia , Colite Ulcerativa/metabolismo , Nitrocompostos/farmacologia , Camundongos , Humanos , Células CACO-2 , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Mucosa Intestinal/patologia , Sulfato de Dextrana/toxicidade , Fator de Transcrição STAT3/metabolismo , Masculino , Janus Quinase 2/metabolismo , Proteínas Quinases Ativadas por AMP/metabolismo , Inflamação/tratamento farmacológico , Colo/efeitos dos fármacos , Colo/patologia , Colo/metabolismo , Camundongos Endogâmicos C57BL , Transdução de Sinais/efeitos dos fármacos , Óxido Nítrico Sintase Tipo II/metabolismo , Interleucina-6/metabolismo , Modelos Animais de Doenças
11.
Heliyon ; 9(4): e14812, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37025849

RESUMO

Economic resilience has been a popular issue in recent years. Along with the consideration of severe shocks caused by the financial crisis of 2007-2008 and globalization of industry and the upgradation of knowledge and technology, economic resilience has brought in much attention. About 50 years of development of planned industrial parks in Taiwan has resulted in considerable economic scale; however, due to changes in interior demands and the exterior environment with time, rearrangement and industrial transformation have made the development of industrial parks difficult. Accordingly, the resilience of planned industrial parks in Taiwan, when encountering a variety of shocks, need to be reviewed and examined. This study selects 12 planned industrial parks from Tainan and Kaohsiung, in southern Taiwan, as subjects and had a complete understanding of economic resilience and factors that influence economic resilience from literature reviews. Four quadrant model constituted by the indicators of economic resistance and recovery as well as discriminant analysis are implemented to analyze the resilience of industrial parks with different backgrounds and various shocks, as well as the elements influencing the resilience. Analytical results indicate that planned industrial parks with industrial structures based on specialized variety or with a steady input of knowledge and innovation to research and development benefited the industrial parks in better resilience, while complete infrastructure planning and governance are fundamental conditions for resilience.

12.
Front Plant Sci ; 12: 632503, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33664761

RESUMO

[This corrects the article DOI: 10.3389/fpls.2018.00002.].

13.
J Am Chem Soc ; 132(9): 3063-77, 2010 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-20148556

RESUMO

The fundamental role played by actin in the regulation of eukaryotic cell maintenance and motility renders it a primary target for small-molecule intervention. In this arena, a class of potent cytotoxic cyclodepsipeptide natural products has emerged over the last quarter-century to stimulate the fields of biology and chemistry with their unique actin-stabilizing properties and complex peptide-polyketide hybrid structures. Despite considerable research effort, a structural basis for the activity of these secondary metabolites remains elusive, not least for the lack of high-resolution structural data and a reliable synthetic route to diverse compound libraries. In response to this, an efficient solid-phase approach has been developed and successfully applied to the total synthesis of jasplakinolide and chondramide C and diverse analogues. The key macrocylization step was realized using ruthenium-catalyzed ring-closing metathesis (RCM) that in the course of a library synthesis produced discernible trends in metathesis reactivity and E/Z-selectivity. After optimization, the RCM step could be operated under mild conditions, a result that promises to facilitate the synthesis of more extensive analogue libraries for structure-function studies. The growth inhibitory effects of the synthesized compounds were quantified and structure-activity correlations established which appear to be in good alignment with relevant biological data from natural products. In this way a number of potent unnatural and simplified analogues have been found. Furthermore, potentially important stereochemical and structural components of a common pharmacophore have been identified and rationalized using molecular modeling. These data will guide in-depth mode-of-action studies, especially into the relationship between the cytotoxicity of these compounds and their actin-perturbing properties, and should inform the future design of simplified and functionalized actin stabilizers as well.


Assuntos
Actinas/química , Antineoplásicos/farmacologia , Proteínas de Bactérias/farmacologia , Fatores Biológicos/farmacologia , Depsipeptídeos/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Proteínas de Bactérias/síntese química , Proteínas de Bactérias/química , Fatores Biológicos/síntese química , Fatores Biológicos/química , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Depsipeptídeos/síntese química , Depsipeptídeos/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Camundongos , Modelos Moleculares , Conformação Molecular , Estabilidade Proteica/efeitos dos fármacos , Estereoisomerismo , Relação Estrutura-Atividade
14.
Am J Physiol Endocrinol Metab ; 297(2): E525-31, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19531636

RESUMO

Sonic hedgehog (SHH) plays an important role in postnatal tissue repair. The present study tested the hypothesis that impaired SHH pathway results in delayed wound healing by suppressing cutaneous nitric oxide (NO) function in type 1 diabetes. Adult male C57/B6 mice and streptozotocin (STZ)-induced type 1 diabetic mice were used. Although cutaneous SHH and Patched-1 (Ptc-1 encoded by PTCH, PTCH 1) proteins were increased significantly on day 4 after wounding compared with day 0 in normal mice, both were decreased significantly in STZ-induced diabetic mice. Topical application of SHH restored wound healing delay in STZ-induced diabetic mice, with a concomitant augmentation of both cutaneous constitutive nitric oxide synthase (NOS) activity and nitrite level. The effects of SHH on wound healing and cutaneous NO function were markedly inhibited by SHH receptor inhibitor cyclopamine. After 24-h treatment in vitro, SHH (5-20 microg/ml) significantly increased cutaneous endothelial NOS protein expression, NOS activity and NO level in normal mice and STZ-induced diabetic mice in a concentration-dependent manner, an effect that was blunted by cyclopamine and NOS inhibitor N(omega)-nitro-L-arginine methyl ester. The phosphatidylinositol 3-kinase inhibitor LY-294002 significantly blunted the increase of NOS activity and NO level induced by SHH treatment in human umbilican vein endothelial cells. These results demonstrate that the SHH pathway is activated in a normal wound, and its reduction results in impaired NO function and wound healing in diabetes. Strategies aimed at augmenting the endogenous SHH pathway may provide an effective means in ameliorating delayed diabetic wound healing.


Assuntos
Diabetes Mellitus Experimental/complicações , Proteínas Hedgehog/farmacologia , Óxido Nítrico/fisiologia , Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos , Animais , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Avaliação Pré-Clínica de Medicamentos , Proteínas Hedgehog/metabolismo , Proteínas Hedgehog/uso terapêutico , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Receptores Patched , Receptor Patched-1 , Receptores de Superfície Celular/metabolismo , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Pele/lesões , Pele/metabolismo , Dermatopatias/tratamento farmacológico , Dermatopatias/etiologia , Estreptozocina , Fatores de Tempo
15.
Chem Commun (Camb) ; (12): 1493-5, 2009 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-19277367

RESUMO

The study of classical ring-closing metathesis and relay ring-closing metathesis in a total synthesis of Jasplakinolide and its desbromo analog is described.


Assuntos
Depsipeptídeos/síntese química , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Cromatografia Líquida de Alta Pressão , Ciclização , Depsipeptídeos/química , Estrutura Molecular
16.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 6): m647, 2009 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-21583013

RESUMO

In the title mononuclear complex, [Ni(C(3)H(2)O(4))(C(15)H(10)N(4))(H(2)O)]·3H(2)O, the metal center is coordinated in a distorted NiN(3)O(3) geometry. In the crystal structure, inter-molecular O-H⋯O hydrogen bonds link the components into a two-dimensional network. In addition, there are weak π-π stacking inter-actions between symmetry-related phenanthroline rings, with a centroid-centroid distance of 3.6253 (17) Å.

17.
Zhonghua Gan Zang Bing Za Zhi ; 17(3): 171-4, 2009 Mar.
Artigo em Zh | MEDLINE | ID: mdl-19335977

RESUMO

OBJECTIVE: To explore the strategy for the treatment of chronic hepatitis B with YMDD mutation. METHODS: A total of 120 chronic hepatitis B patients with YMDD mutation were randomly assigned into four groups. In group A, patients received adefovir dipivoxil for 48 weeks. In group B, patients received adefovir dipivoxil in combination with lamivudine during the first 12 weeks and adefovir dipivoxil only for the following 36 weeks. In group C, patients received adefovir dipivoxil in combination with lamivudine for 48 weeks. In group D, patients received entecavir for 48 weeks. RESULTS: The rate of rebound of alanine aminotransferase (ALT) was 30.0% (9/30), 10.0% (3/30), 6.7% (2/30), 10.0% (3/30) (P < 0.05) during the first 12 weeks, and one patient with severe hepatitis was found in group A. The positive rate of YMDD mutation was 17.9%, 0, 0, 0 at week 12. There was no significant difference in the level of ALT and the rate of HBeAg seroconversion after 48-week treatment (P > 0.05). At week 48, there was significant difference in the ALT normalization rate and undetectable HBV DNA rate between group C and group A, and also between group D and group A, and the rate of drug resistant genotype was 6.9%, 6.7%, 0, 0. Two patients had rtN236T mutation in group A, and one patient had rtN236T mutation and another one had rtA181V mutation in group B. CONCLUSION: Adefovir dipivoxil in combination with lamivudine or entecavir are safe and effective therapies for chronic hepatitis B patients with YMDD mutation.


Assuntos
Antivirais/uso terapêutico , DNA Viral/sangue , Vírus da Hepatite B/genética , Hepatite B Crônica/tratamento farmacológico , Hepatite B Crônica/virologia , Adenina/administração & dosagem , Adenina/análogos & derivados , Adenina/uso terapêutico , Adulto , Alanina Transaminase/sangue , Antivirais/administração & dosagem , Farmacorresistência Viral , Quimioterapia Combinada/métodos , Feminino , Seguimentos , Guanina/administração & dosagem , Guanina/análogos & derivados , Guanina/uso terapêutico , Antígenos E da Hepatite B/sangue , Vírus da Hepatite B/efeitos dos fármacos , Humanos , Lamivudina/administração & dosagem , Lamivudina/uso terapêutico , Masculino , Pessoa de Meia-Idade , Mutação , Organofosfonatos/administração & dosagem , Organofosfonatos/uso terapêutico , Inibidores da Transcriptase Reversa/administração & dosagem , Inibidores da Transcriptase Reversa/uso terapêutico , Adulto Jovem
18.
Chem Commun (Camb) ; 55(81): 12172-12175, 2019 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-31544179

RESUMO

Phthalimide-based "D-N-A" emitters o-AI-Cz, m-AI-Cz and p-AI-Cz showed TADF and RTP properties due to their small ΔEST in both film and crystalline states. In particular, o-AI-Cz exhibited an ultralong RTP with a lifetime of 602 ms in air and remarkable afterglow, which could allow it to be used as a security ink for application in anti-counterfeiting materials. Moreover, o-AI-Cz showed intense intramolecular interaction between the donor and the acceptor subunits, while p-AI-Cz could form regular hexagonal pores with a diameter of 13.171 Å in the solid state, which might result in their different RTP properties.

19.
Sci Rep ; 9(1): 15838, 2019 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-31676873

RESUMO

This study aimed to assess the prevalence and related factors of obesity-related hypertension among adults aged 40 to 79 years in Southwest China. From September 2013 to March 2014, a multi-stage, stratified sampling method was conducted on 10,589 people aged 40 to 79 years and living in Chengdu and Chongqing investigated by using a questionnaire and performing physical and biochemical measurements. The prevalence of obesity-related hypertension and hypertension overall (systolic ≥130 mmHg and/or diastolic ≥80 mmHg or treated hypertension) was 22.8% and 57.4%, respectively, among all participants. For obesity-related hypertension, the prevalence was higher in women than in men (24.7% versus 19.4%, p < 0.001). For people in the age ranges of 40-49, 50-59, 60-69, and ≥70, the prevalence of obesity-related hypertension were 11.8%, 22.6%, 30.7%, and 36.6%, respectively. Participants with obesity-related hypertension as opposed to those with non-obesity-related hypertension had a higher prevalence of hypertriglyceridemia, high low-density lipoprotein cholesterolemia, diabetes, and hyperuricemia (all p < 0.05). Multivariate logistic regression analysis showed that age, female gender, current smoking, hypertriglyceridemia, diabetes and family history of hypertension were all positively correlated with obesity-related hypertension, whereas higher education level and having spouse were negatively correlated with obesity-related hypertension. The prevalence of obesity-related hypertension was high among adults aged 40 to 79 years in Southwest China. Cardiometabolic abnormalities among participants with obesity-related hypertension were more serious and frequently present than in those with non-obesity-related hypertension. Aggressive and holistic strategies aiming at the prevention and treatment of obesity-related hypertension are needed.


Assuntos
Hipertensão , Obesidade , Adulto , Fatores Etários , Idoso , China/epidemiologia , Feminino , Humanos , Hipertensão/epidemiologia , Hipertensão/fisiopatologia , Masculino , Pessoa de Meia-Idade , Obesidade/epidemiologia , Obesidade/fisiopatologia , Prevalência , Fatores Sexuais
20.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 6): m769, 2008 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-21202461

RESUMO

In the title complex, [Ni(NCS)(2)(C(14)H(13)N(3))(2)]·2CH(3)OH, the Ni(II) atom lies on a crystallographic twofold rotation axis and is in a slightly distorted octa-hedral NiN(6) coordination environment. The crystal structure is stabilized by a combination of weak π-π stacking inter-actions between symmetry-related 1,10-phenanthroline ligands [centroi-centroid distance between benzene rings = 3.5936 (18) Å] and weak O-H⋯S, C-H⋯O and C-H⋯S hydrogen bonds between methanol and complex mol-ecules.

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