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1.
Nat Nanotechnol ; 18(7): 721-726, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37169896

RESUMO

Electron flying qubits are envisioned as potential information links within a quantum computer, but also promise-like photonic approaches-to serve as self-standing quantum processing units. In contrast to their photonic counterparts, electron-quantum-optics implementations are subject to Coulomb interactions, which provide a direct route to entangle the orbital or spin degree of freedom. However, controlled interaction of flying electrons at the single-particle level has not yet been established experimentally. Here we report antibunching of a pair of single electrons that is synchronously shuttled through a circuit of coupled quantum rails by means of a surface acoustic wave. The in-flight partitioning process exhibits a reciprocal gating effect which allows us to ascribe the observed repulsion predominantly to Coulomb interaction. Our single-shot experiment marks an important milestone on the route to realize a controlled-phase gate for in-flight quantum manipulations.

2.
Nano Lett ; 22(23): 9313-9318, 2022 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-36442504

RESUMO

Single-electron sources, formed by a quantum dot (QD), are key elements for realizing electron analogue of quantum optics. We develop a new type of single-electron source with functionalities that are absent in existing sources. This source couples with only one lead. By an AC rf drive, it successively emits holes and electrons cotraveling in the lead, as in the mesoscopic capacitor. Thanks to the considerable charging energy of the QD, however, emitted electrons have energy levels a few tens of millielectronvolts above the Fermi level, so that emitted holes and electrons are split by a potential barrier on demand, resulting in a rectified quantized current. The resulting pump map exhibits quantized triangular islands, in good agreement with our theory. We also demonstrate that the source can be operated with another tunable-barrier single-electron source in a series double QD geometry, showing parallel electron pumping by a common gate driving.

3.
J Microbiol Biotechnol ; 27(8): 1457-1460, 2017 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-28621108

RESUMO

Seven flavonoids were isolated from Spatholobus suberectus via repetitive column chromatography and high-performance liquid chromatography. The chemical structures of these compounds were identified by spectroscopic analysis and comparison with values reported in the literature. Among the flavonoids tested, 7-hydroxy-6-methoxyflavanone (1) and formononetin (4) exhibited strong inhibitory activity against Streptococcus mutans SrtA, with IC50 values of 46.1 and 41.8 µM, respectively, but did not affect cell viability. The onset and magnitude of inhibition of saliva-induced aggregation in S. mutans treated with compounds 1 and 4 were comparable to the behavior of a srtA-deletion mutant without treatment.


Assuntos
Aminoaciltransferases/antagonistas & inibidores , Aderência Bacteriana/efeitos dos fármacos , Proteínas de Bactérias/antagonistas & inibidores , Inibidores Enzimáticos/isolamento & purificação , Fabaceae/química , Flavonoides/isolamento & purificação , Streptococcus mutans/efeitos dos fármacos , Cromatografia Líquida , Cisteína Endopeptidases , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Flavonoides/química , Flavonoides/metabolismo , Concentração Inibidora 50 , Viabilidade Microbiana/efeitos dos fármacos , Estrutura Molecular , Análise Espectral , Streptococcus mutans/enzimologia , Streptococcus mutans/fisiologia
4.
Mar Drugs ; 15(6)2017 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-28587270

RESUMO

Chemical investigation of a halophilic actinomycete strain belonging to the genus Nocardiopsis inhabiting a hypersaline saltern led to the discovery of new 18-membered macrolides with nitrile functionality, borrelidins C-E (1-3), along with a previously reported borrelidin (4). The planar structures of borrelidins C-E, which are new members of the rare borrelidin class of antibiotics, were elucidated by NMR, mass, IR, and UV spectroscopic analyses. The configurations of borrelidines C-E were determined by the interpretation of ROESY NMR spectra, J-based configuration analysis, a modified Mosher's method, and CD spectroscopic analysis. Borrelidins C and D displayed inhibitory activity, particularly against the Gram-negative pathogen Salmonella enterica, and moderate cytotoxicity against the SNU638 and K562 carcinoma cell lines.


Assuntos
Actinobacteria/química , Antibacterianos/química , Macrolídeos/química , Antibacterianos/farmacologia , Linhagem Celular Tumoral , Álcoois Graxos/química , Álcoois Graxos/farmacologia , Humanos , Células K562 , Macrolídeos/farmacologia , Salmonella enterica/efeitos dos fármacos , Análise Espectral/métodos
5.
Biochem Biophys Res Commun ; 490(3): 664-669, 2017 08 26.
Artigo em Inglês | MEDLINE | ID: mdl-28634080

RESUMO

Many factors regulate the expression of specialised secondary metabolite biosynthetic gene clusters, which have been recognised as important for the discovery of novel microbial natural products. A cosmid library based on genomic DNA of the marine-derived Streptomyces puniceus Act1085 was constructed and screened to identify a short gene cluster similar to the nonactin biosynthetic cluster. The ORFs of the gene cluster isolated had high amino acid sequence identity, from 82% to 96%, with corresponding ORFs of the nonactin biosynthetic gene cluster from S. griseus subsp. griseus ETH A7796. Despite the expectation that nonactin or its derivatives would be made from heterologous expression of the gene cluster found in S. albus J1074, nocardamine was isolated. The heterologous expression data indicate that the production of nocardamine in S. albus J1074 is due to an ortholog of nonG, a TetR family transcriptional regulator, from S. puniceus Act1085.


Assuntos
Vias Biossintéticas , Genes Bacterianos , Família Multigênica , Peptídeos Cíclicos/metabolismo , Streptomyces/genética , Clonagem Molecular , Expressão Gênica , Macrolídeos/metabolismo , Peptídeos Cíclicos/genética , Streptomyces/metabolismo
6.
FEBS Lett ; 591(9): 1225-1235, 2017 05.
Artigo em Inglês | MEDLINE | ID: mdl-28369931

RESUMO

Candida albicans hyphal formation is inhibited by a quorum-sensing molecule, farnesoic acid, which accumulates in the medium as the cells proliferate. We recently showed that Pho81 is essential for the inhibition of hyphal growth by farnesoic acid. Here, we describe a newly identified regulator, Hot1, which increases the expression of PHO81. The binding site of Hot1 in the PHO81 promoter region was identified by DNase I protection assay. The hot1Δ mutant grows extensively as filaments. Furthermore, the inhibition of hyphal formation and the repression of major signaling pathway components in response to farnesoic acid are defective in hot1Δ mutant cells. These data suggest an important role for HOT1 in the inhibition of hyphal development by farnesoic acid in this fungus.


Assuntos
Candida albicans/metabolismo , Ácidos Graxos Insaturados/farmacologia , Proteínas Fúngicas/genética , Hifas/genética , Fatores de Transcrição/genética , Sequência de Aminoácidos , Sítios de Ligação/genética , Candida albicans/genética , Candida albicans/crescimento & desenvolvimento , Eletroforese em Gel de Poliacrilamida , Proteínas Fúngicas/metabolismo , Regulação Fúngica da Expressão Gênica/efeitos dos fármacos , Hifas/crescimento & desenvolvimento , Hifas/metabolismo , Morfogênese/efeitos dos fármacos , Morfogênese/genética , Mutação , Regiões Promotoras Genéticas/genética , Proteínas Repressoras/genética , Proteínas Repressoras/metabolismo , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Homologia de Sequência de Aminoácidos , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/genética , Fatores de Transcrição/metabolismo
7.
Mar Drugs ; 13(3): 1290-303, 2015 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-25775424

RESUMO

Terrelumamides A (1) and B (2), two new lumazine-containing peptides, were isolated from the culture broth of the marine-derived fungus Aspergillus terreus. From the results of combined spectroscopic and chemical analyses, the structures of these compounds were determined to be linear assemblies of 1-methyllumazine-6-carboxylic acid, an amino acid residue and anthranilic acid methyl ester connected by peptide bonds. These new compounds exhibited pharmacological activity by improving insulin sensitivity, which was evaluated in an adipogenesis model using human bone marrow mesenchymal stem cells. In addition, the compounds exhibited fluorescence changes upon binding to DNA, demonstrating their potential applications to DNA sequence recognition.


Assuntos
Aspergillus/química , Células-Tronco Mesenquimais/efeitos dos fármacos , Peptídeos/farmacologia , Pteridinas/farmacologia , Adipogenia/efeitos dos fármacos , DNA/metabolismo , Fluorescência , Humanos , Células-Tronco Mesenquimais/metabolismo , Peptídeos/química , Peptídeos/isolamento & purificação , Pteridinas/química , Pteridinas/isolamento & purificação , Análise Espectral
8.
J Nat Prod ; 77(2): 406-10, 2014 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-24437979

RESUMO

Penicillipyrones A (1) and B (2), two novel meroterpenoids, were isolated from the marine-derived fungus Penicillium sp. On the basis of the results of combined spectroscopic analyses, these compounds were structurally elucidated to be sesquiterpene γ-pyrones from a new skeletal class derived from a unique linkage pattern between the drimane sesquiterpene and pyrone moieties. Compound 2 elicited significant induction of quinone reductase.


Assuntos
Penicillium/química , Sesquiterpenos/isolamento & purificação , Animais , Biologia Marinha , Camundongos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Pironas/química , Pironas/isolamento & purificação , Pironas/farmacologia , Quinona Redutases/efeitos dos fármacos , Sesquiterpenos/química , Sesquiterpenos/farmacologia
9.
Org Lett ; 15(6): 1286-9, 2013 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-23431962

RESUMO

Herqueiazole (1), herqueioxazole (2), and herqueidiketal (3), polyaromatic metabolites with a novel skeletal class, were isolated from the marine-derived fungus Penicillium sp. Based on the combined spectroscopic analyses, the structures of 1 and 2 were determined to be the first examples of pyrrole- and oxazole-containing phenalenone compounds, respectively, whereas 3 possessed a novel skeleton with a highly oxidized naphthoquinone moiety. Compound 3 exhibited moderate cytotoxicity and significant inhibitory activity against sortase A.


Assuntos
Antibacterianos/isolamento & purificação , Compostos Heterocíclicos de 4 ou mais Anéis/isolamento & purificação , Penicillium/química , Antibacterianos/química , Antibacterianos/farmacologia , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Biologia Marinha , Testes de Sensibilidade Microbiana , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacos
10.
Biol Pharm Bull ; 35(3): 428-32, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22382332

RESUMO

Na(+)/K(+)-adenosine triphosphatase (ATPase) inhibitors have considerable therapeutic potential against some heart diseases like congestive heart failure and cardiac arrhythmias. Through bioassay-guided separation of the leaf extract of Laurus nobilis, six acylated kaempferol glycosides (compounds 1-6) were isolated. Their structures were determined on the basis of spectroscopic analysis and comparison with reported data. All the isolates were subjected to in vitro bioassays to evaluate their inhibitory activities against Na(+)/K(+)-ATPase from porcine cerebral cortex and bacterial growth. These studies led to the identification of compounds 1-6 as potent Na(+)/K(+)-ATPase inhibitors, with IC(50) values in the range of 4.0 ± 0.1-10.4 ± 0.6 µM. These compounds also exhibited a broad spectrum of antibacterial activity. In particular, compounds 4 and 6 showed potent inhibitory activities against several bacterial strains, except Escherichia coli, with minimum inhibitory concentration (MIC) values in the range of 0.65-2.08 µg/mL. Thus, L. nobilis-derived acylated kaempferol glycosides may have a potential to be leads for the development of Na(+)/K(+) ATPase inhibitors (1-6) and antibacterial agents (4, 6).


Assuntos
Antibacterianos/farmacologia , Inibidores Enzimáticos/farmacologia , Glicosídeos/farmacologia , Quempferóis/farmacologia , ATPase Trocadora de Sódio-Potássio/antagonistas & inibidores , Acilação , Animais , Antibacterianos/isolamento & purificação , Bactérias/efeitos dos fármacos , Córtex Cerebral/enzimologia , Inibidores Enzimáticos/isolamento & purificação , Glicosídeos/isolamento & purificação , Quempferóis/isolamento & purificação , Laurus/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Folhas de Planta/química , ATPase Trocadora de Sódio-Potássio/metabolismo , Suínos
11.
Bioorg Med Chem Lett ; 21(11): 3198-201, 2011 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-21550239

RESUMO

Oxazole-containing macrolides (1-5) isolated from the marine sponge Chondrosia corticata were evaluated for their actin depolymerizing activities by monitoring fluorescent intensity of pyrene F-actin. These studies led to the identification of (19Z)-halichondramide (5) as a new actin depolymerizing agent. The actin depolymerizing activity by (19Z)-halichondramide (5) was four times more potent than that of halichondramide (1). Compounds 1 and 5 also have potent antifungal activity. The preliminary structure-activity relationship of these compounds is described to elucidate the essential structural requirements.


Assuntos
Macrolídeos/química , Oxazóis/química , Poríferos/química , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Aspergillus fumigatus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Fluorescência , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Macrolídeos/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oxazóis/farmacologia , Polimerização/efeitos dos fármacos , Relação Estrutura-Atividade
12.
Bioorg Med Chem Lett ; 20(23): 6882-5, 2010 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-21035332

RESUMO

Guided by the inhibitory activities of indole-containing natural products against isocitrate lyase (ICL) from Candida albicans and sortase A (SrtA) from Staphylococcus aureus, a series of compounds structurally analogous to natural products were synthesized. Eight SrtA inhibitors and an ICL inhibitor having higher activities than the natural products were discovered by screening the enzyme inhibitory activities of synthesized compounds. Among the SrtA inhibitors discovered, six exhibited higher activities than p-hydroxymercuribenzoic acid, which suggests that these compounds have great potential as alternative antibacterial agents.


Assuntos
Aminoaciltransferases/antagonistas & inibidores , Antibacterianos/química , Proteínas de Bactérias/antagonistas & inibidores , Produtos Biológicos/química , Indóis/química , Isocitrato Liase/antagonistas & inibidores , Antibacterianos/farmacologia , Candida albicans/enzimologia , Cisteína Endopeptidases , Avaliação Pré-Clínica de Medicamentos/métodos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Indóis/síntese química , Indóis/farmacologia , Staphylococcus aureus/enzimologia , Relação Estrutura-Atividade
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