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1.
Nat Nanotechnol ; 18(7): 721-726, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37169896

ABSTRACT

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.
Article in English | MEDLINE | ID: mdl-36442504

ABSTRACT

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.
Article in English | MEDLINE | ID: mdl-28621108

ABSTRACT

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.


Subject(s)
Aminoacyltransferases/antagonists & inhibitors , Bacterial Adhesion/drug effects , Bacterial Proteins/antagonists & inhibitors , Enzyme Inhibitors/isolation & purification , Fabaceae/chemistry , Flavonoids/isolation & purification , Streptococcus mutans/drug effects , Chromatography, Liquid , Cysteine Endopeptidases , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/metabolism , Flavonoids/chemistry , Flavonoids/metabolism , Inhibitory Concentration 50 , Microbial Viability/drug effects , Molecular Structure , Spectrum Analysis , Streptococcus mutans/enzymology , Streptococcus mutans/physiology
4.
Mar Drugs ; 15(6)2017 Jun 06.
Article in English | MEDLINE | ID: mdl-28587270

ABSTRACT

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.


Subject(s)
Actinobacteria/chemistry , Anti-Bacterial Agents/chemistry , Macrolides/chemistry , Anti-Bacterial Agents/pharmacology , Cell Line, Tumor , Fatty Alcohols/chemistry , Fatty Alcohols/pharmacology , Humans , K562 Cells , Macrolides/pharmacology , Salmonella enterica/drug effects , Spectrum Analysis/methods
5.
Biochem Biophys Res Commun ; 490(3): 664-669, 2017 08 26.
Article in English | MEDLINE | ID: mdl-28634080

ABSTRACT

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.


Subject(s)
Biosynthetic Pathways , Genes, Bacterial , Multigene Family , Peptides, Cyclic/metabolism , Streptomyces/genetics , Cloning, Molecular , Gene Expression , Macrolides/metabolism , Peptides, Cyclic/genetics , Streptomyces/metabolism
6.
FEBS Lett ; 591(9): 1225-1235, 2017 05.
Article in English | MEDLINE | ID: mdl-28369931

ABSTRACT

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.


Subject(s)
Candida albicans/metabolism , Fatty Acids, Unsaturated/pharmacology , Fungal Proteins/genetics , Hyphae/genetics , Transcription Factors/genetics , Amino Acid Sequence , Binding Sites/genetics , Candida albicans/genetics , Candida albicans/growth & development , Electrophoresis, Polyacrylamide Gel , Fungal Proteins/metabolism , Gene Expression Regulation, Fungal/drug effects , Hyphae/growth & development , Hyphae/metabolism , Morphogenesis/drug effects , Morphogenesis/genetics , Mutation , Promoter Regions, Genetic/genetics , Repressor Proteins/genetics , Repressor Proteins/metabolism , Reverse Transcriptase Polymerase Chain Reaction , Sequence Homology, Amino Acid , Signal Transduction/drug effects , Signal Transduction/genetics , Transcription Factors/metabolism
7.
Mar Drugs ; 13(3): 1290-303, 2015 Mar 12.
Article in English | MEDLINE | ID: mdl-25775424

ABSTRACT

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.


Subject(s)
Aspergillus/chemistry , Mesenchymal Stem Cells/drug effects , Peptides/pharmacology , Pteridines/pharmacology , Adipogenesis/drug effects , DNA/metabolism , Fluorescence , Humans , Mesenchymal Stem Cells/metabolism , Peptides/chemistry , Peptides/isolation & purification , Pteridines/chemistry , Pteridines/isolation & purification , Spectrum Analysis
8.
J Nat Prod ; 77(2): 406-10, 2014 Feb 28.
Article in English | MEDLINE | ID: mdl-24437979

ABSTRACT

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.


Subject(s)
Penicillium/chemistry , Sesquiterpenes/isolation & purification , Animals , Marine Biology , Mice , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Pyrones/chemistry , Pyrones/isolation & purification , Pyrones/pharmacology , Quinone Reductases/drug effects , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology
9.
Org Lett ; 15(6): 1286-9, 2013 Mar 15.
Article in English | MEDLINE | ID: mdl-23431962

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/isolation & purification , Heterocyclic Compounds, 4 or More Rings/isolation & purification , Penicillium/chemistry , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Heterocyclic Compounds, 4 or More Rings/chemistry , Heterocyclic Compounds, 4 or More Rings/pharmacology , Marine Biology , Microbial Sensitivity Tests , Molecular Structure , Staphylococcus aureus/drug effects
10.
Biol Pharm Bull ; 35(3): 428-32, 2012.
Article in English | MEDLINE | ID: mdl-22382332

ABSTRACT

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).


Subject(s)
Anti-Bacterial Agents/pharmacology , Enzyme Inhibitors/pharmacology , Glycosides/pharmacology , Kaempferols/pharmacology , Sodium-Potassium-Exchanging ATPase/antagonists & inhibitors , Acylation , Animals , Anti-Bacterial Agents/isolation & purification , Bacteria/drug effects , Cerebral Cortex/enzymology , Enzyme Inhibitors/isolation & purification , Glycosides/isolation & purification , Kaempferols/isolation & purification , Laurus/chemistry , Microbial Sensitivity Tests , Plant Extracts/chemistry , Plant Leaves/chemistry , Sodium-Potassium-Exchanging ATPase/metabolism , Swine
11.
Bioorg Med Chem Lett ; 21(11): 3198-201, 2011 Jun 01.
Article in English | MEDLINE | ID: mdl-21550239

ABSTRACT

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.


Subject(s)
Macrolides/chemistry , Oxazoles/chemistry , Porifera/chemistry , Animals , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Aspergillus fumigatus/drug effects , Candida albicans/drug effects , Fluorescence , Heterocyclic Compounds, 4 or More Rings/chemistry , Heterocyclic Compounds, 4 or More Rings/pharmacology , Macrolides/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Oxazoles/pharmacology , Polymerization/drug effects , Structure-Activity Relationship
12.
Bioorg Med Chem Lett ; 20(23): 6882-5, 2010 Dec 01.
Article in English | MEDLINE | ID: mdl-21035332

ABSTRACT

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.


Subject(s)
Aminoacyltransferases/antagonists & inhibitors , Anti-Bacterial Agents/chemistry , Bacterial Proteins/antagonists & inhibitors , Biological Products/chemistry , Indoles/chemistry , Isocitrate Lyase/antagonists & inhibitors , Anti-Bacterial Agents/pharmacology , Candida albicans/enzymology , Cysteine Endopeptidases , Drug Evaluation, Preclinical/methods , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Indoles/chemical synthesis , Indoles/pharmacology , Staphylococcus aureus/enzymology , Structure-Activity Relationship
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