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1.
Nature ; 626(7998): 288-293, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38326594

RESUMO

The microscopic origin of high-temperature superconductivity in cuprates remains unknown. It is widely believed that substantial progress could be achieved by better understanding of the pseudogap phase, a normal non-superconducting state of cuprates1,2. In particular, a central issue is whether the pseudogap could originate from strong pairing fluctuations3. Unitary Fermi gases4,5, in which the pseudogap-if it exists-necessarily arises from many-body pairing, offer ideal quantum simulators to address this question. Here we report the observation of a pair-fluctuation-driven pseudogap in homogeneous unitary Fermi gases of lithium-6 atoms, by precisely measuring the fermion spectral function through momentum-resolved microwave spectroscopy and without spurious effects from final-state interactions. The temperature dependence of the pairing gap, inverse pair lifetime and single-particle scattering rate are quantitatively determined by analysing the spectra. We find a large pseudogap above the superfluid transition temperature. The inverse pair lifetime exhibits a thermally activated exponential behaviour, uncovering the microscopic virtual pair breaking and recombination mechanism. The obtained large, temperature-independent single-particle scattering rate is comparable with that set by the Planckian limit6. Our findings quantitatively characterize the pseudogap in strongly interacting Fermi gases and they lend support for the role of preformed pairing as a precursor to superfluidity.

2.
Nature ; 589(7841): 214-219, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-33408416

RESUMO

Quantum key distribution (QKD)1,2 has the potential to enable secure communication and information transfer3. In the laboratory, the feasibility of point-to-point QKD is evident from the early proof-of-concept demonstration in the laboratory over 32 centimetres4; this distance was later extended to the 100-kilometre scale5,6 with decoy-state QKD and more recently to the 500-kilometre scale7-10 with measurement-device-independent QKD. Several small-scale QKD networks have also been tested outside the laboratory11-14. However, a global QKD network requires a practically (not just theoretically) secure and reliable QKD network that can be used by a large number of users distributed over a wide area15. Quantum repeaters16,17 could in principle provide a viable option for such a global network, but they cannot be deployed using current technology18. Here we demonstrate an integrated space-to-ground quantum communication network that combines a large-scale fibre network of more than 700 fibre QKD links and two high-speed satellite-to-ground free-space QKD links. Using a trusted relay structure, the fibre network on the ground covers more than 2,000 kilometres, provides practical security against the imperfections of realistic devices, and maintains long-term reliability and stability. The satellite-to-ground QKD achieves an average secret-key rate of 47.8 kilobits per second for a typical satellite pass-more than 40 times higher than achieved previously. Moreover, its channel loss is comparable to that between a geostationary satellite and the ground, making the construction of more versatile and ultralong quantum links via geosynchronous satellites feasible. Finally, by integrating the fibre and free-space QKD links, the QKD network is extended to a remote node more than 2,600 kilometres away, enabling any user in the network to communicate with any other, up to a total distance of 4,600 kilometres.

3.
Nature ; 582(7813): 501-505, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32541968

RESUMO

Quantum key distribution (QKD)1-3 is a theoretically secure way of sharing secret keys between remote users. It has been demonstrated in a laboratory over a coiled optical fibre up to 404 kilometres long4-7. In the field, point-to-point QKD has been achieved from a satellite to a ground station up to 1,200 kilometres away8-10. However, real-world QKD-based cryptography targets physically separated users on the Earth, for which the maximum distance has been about 100 kilometres11,12. The use of trusted relays can extend these distances from across a typical metropolitan area13-16 to intercity17 and even intercontinental distances18. However, relays pose security risks, which can be avoided by using entanglement-based QKD, which has inherent source-independent security19,20. Long-distance entanglement distribution can be realized using quantum repeaters21, but the related technology is still immature for practical implementations22. The obvious alternative for extending the range of quantum communication without compromising its security is satellite-based QKD, but so far satellite-based entanglement distribution has not been efficient23 enough to support QKD. Here we demonstrate entanglement-based QKD between two ground stations separated by 1,120 kilometres at a finite secret-key rate of 0.12 bits per second, without the need for trusted relays. Entangled photon pairs were distributed via two bidirectional downlinks from the Micius satellite to two ground observatories in Delingha and Nanshan in China. The development of a high-efficiency telescope and follow-up optics crucially improved the link efficiency. The generated keys are secure for realistic devices, because our ground receivers were carefully designed to guarantee fair sampling and immunity to all known side channels24,25. Our method not only increases the secure distance on the ground tenfold but also increases the practical security of QKD to an unprecedented level.

4.
Proc Natl Acad Sci U S A ; 120(22): e2212323120, 2023 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-37216545

RESUMO

An independent set (IS) is a set of vertices in a graph such that no edge connects any two vertices. In adiabatic quantum computation [E. Farhi, et al., Science 292, 472-475 (2001); A. Das, B. K. Chakrabarti, Rev. Mod. Phys. 80, 1061-1081 (2008)], a given graph G(V, E) can be naturally mapped onto a many-body Hamiltonian [Formula: see text], with edges [Formula: see text] being the two-body interactions between adjacent vertices [Formula: see text]. Thus, solving the IS problem is equivalent to finding all the computational basis ground states of [Formula: see text]. Very recently, non-Abelian adiabatic mixing (NAAM) has been proposed to address this task, exploiting an emergent non-Abelian gauge symmetry of [Formula: see text] [B. Wu, H. Yu, F. Wilczek, Phys. Rev. A 101, 012318 (2020)]. Here, we solve a representative IS problem [Formula: see text] by simulating the NAAM digitally using a linear optical quantum network, consisting of three C-Phase gates, four deterministic two-qubit gate arrays (DGA), and ten single rotation gates. The maximum IS has been successfully identified with sufficient Trotterization steps and a carefully chosen evolution path. Remarkably, we find IS with a total probability of 0.875(16), among which the nontrivial ones have a considerable weight of about 31.4%. Our experiment demonstrates the potential advantage of NAAM for solving IS-equivalent problems.

5.
Phys Rev Lett ; 132(6): 063401, 2024 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-38394555

RESUMO

We report an extensive experimental investigation on the transition from flat-band localization (FBL) to Anderson localization (AL) in a one-dimensional synthetic lattice in the momentum dimension. By driving multiple Bragg processes between designated momentum states, an effective one-dimensional Tasaki lattice is implemented with highly tunable parameters, including nearest-neighbor and next-nearest-neighbor coupling coefficients and onsite energy potentials. With that, a flat-band localization phase is realized and demonstrated via the evolution dynamics of the particle population over different momentum states. The localization effect is undermined when a moderate disorder is introduced to the onsite potential and restored under a strong disorder. We find clear signatures of the FBL-AL transition in the density profile evolution, the inverse participation ratio, and the von Neumann entropy, where good agreement is obtained with theoretical predictions.

6.
J Org Chem ; 89(9): 6149-6158, 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38635972

RESUMO

The detailed mechanism of transition metal-free-catalyzed monomethylation of 2-naphthyl acetonitrile (1a) with CO2 in the presence of triazabicyclodecene (TBD) and BH3NMe3 was investigated using density functional theory. The C-methylation process proved to generate formaldehyde followed by the formation of the product via an alcohol rather than a methoxyborane intermediate. During the reaction, CO2 is activated to form the TBD-CO2 adduct and BH3NMe3 is changed into TBD-BH2 (IM2) in the presence of TBD. IM2 plays a real reducing role within the system due to the unique coordination capability of the B atom. In addition to enhancing the nucleophilicity of 1a through deprotonation by tBuOK, our research also indicates that the generated tBuOH not only assists in proton transfer to generate an alcohol intermediate but also promotes the regeneration of TBD.

7.
Arch Virol ; 169(5): 114, 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38700535

RESUMO

OBJECTIVE: Epstein-Barr virus (EBV)-associated gastric cancer (EBVaGC) is a distinct molecular subtype of gastric cancer (GC). At present, the clinical characteristics and prognostic implications of EBV infection and the potential clinical benefits of immune checkpoint blockade in GC remain to be clarified. Hence, this study was designed to analyze the clinical and pathological characteristics of GC patients with varying EBV infection states and compare their overall survival (OS). METHODS: A retrospective study was performed on 1031 consecutive GC patients who underwent gastrectomy at the Affiliated Hospital of Xuzhou Medical University from February 2018 to November 2022. EBV-encoded RNA (EBER) in situ hybridization (ISH) was used for EBV assessment, and immunohistochemical staining was used for evaluation of human epidermal growth factor receptor 2 (HER2), programmed death ligand 1 (PD-L1), and Ki67 expression. EBVaGC was defined as tumors with EBV positivity. In addition, EBV-negative GC (EBVnGC) patients were matched with EBVaGC patients based on seven clinicopathological parameters (age, gender, anatomic subsite, tumor size, Lauren classification, degree of differentiation, and tumor-node-metastasis [TNM] stage). The correlations of clinical features with HER2, PD-L1, and Ki67 expression were evaluated statistically. The survival of patients was assessed through medical records, telephone, or WeChat communication, and prognostic analysis was performed using the logrank test as well as univariable and multivariable regression analysis. RESULTS: Out of 1031 GC patients tested, 35 (3.4%) were diagnosed with EBVaGC. Notably, the EBVaGC group exhibited a distinct predominance of males and younger patients, significantly higher Ki67 and PD-L1 expression levels, and a lower prevalence of pericancerous nerve invasion than the EBVnGC group (P < 0.01). In the 35 EBVaGC cases, Ki67 expression was negatively correlated with age (P < 0.05), suggesting that a younger onset age was associated with higher Ki67 expression. In addition, PD-L1 expression was correlated with the degree of differentiation, T-stage, and clinical stage of the patient. Furthermore, PD-L1 expression was elevated in tumors with lower differentiation or at later stages (P < 0.05). Using univariate analysis, Ki67, PD-L1, and clinical stage were identified as significant factors influencing the overall survival (OS) of EBVaGC patients (P < 0.05). Moreover, multivariate survival analysis revealed that clinical stage and Ki67 expression were independent risk factors for the OS of the patients (P < 0.05), and the three-year OS rate of EBVaGC patients was 64.2%. CONCLUSION: EBV-ISH is a practical and valuable method to identify EBVaGC. Owing to its unique etiological, pathological, and clinical characteristics, patients with EBVaGC might benefit from immune checkpoint blockade therapy.


Assuntos
Infecções por Vírus Epstein-Barr , Herpesvirus Humano 4 , Neoplasias Gástricas , Humanos , Neoplasias Gástricas/virologia , Neoplasias Gástricas/patologia , Masculino , Feminino , Infecções por Vírus Epstein-Barr/virologia , Infecções por Vírus Epstein-Barr/complicações , Infecções por Vírus Epstein-Barr/mortalidade , Pessoa de Meia-Idade , Herpesvirus Humano 4/genética , Prognóstico , Estudos Retrospectivos , Idoso , Adulto , Antígeno B7-H1/metabolismo , Antígeno B7-H1/genética , Receptor ErbB-2/metabolismo , Receptor ErbB-2/genética , Antígeno Ki-67/metabolismo , RNA Viral/genética , Gastrectomia
8.
Phys Rev Lett ; 130(3): 030801, 2023 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-36763392

RESUMO

In the past two decades, quantum key distribution networks based on telecom fibers have been implemented on metropolitan and intercity scales. One of the bottlenecks lies in the exponential decay of the key rate with respect to the transmission distance. Recently proposed schemes mainly focus on achieving longer distances by creating a long-arm single-photon interferometer over two communication parties. Despite their advantageous performance over long communication distances, the requirement of phase locking between two remote lasers is technically challenging. By adopting the recently proposed mode-pairing idea, we realize high-performance quantum key distribution without global phase locking. Using two independent off-the-shelf lasers, we show a quadratic key-rate improvement over the conventional measurement-device-independent schemes in the regime of metropolitan and intercity distances. For longer distances, we also boost the key rate performance by 3 orders of magnitude via 304 km commercial fiber and 407 km ultralow-loss fiber. We expect this ready-to-implement high-performance scheme to be widely used in future intercity quantum communication networks.

9.
Phys Rev Lett ; 130(12): 120802, 2023 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-37027851

RESUMO

Quantum sensing can provide the superior sensitivity for sensing a physical quantity beyond the shot-noise limit. In practice, however, this technique has been limited to the issues of phase ambiguity and low sensitivity for small-scale probe states. Here, we propose and demonstrate a full-period quantum phase estimation approach by adopting the Kitaev's phase estimation algorithm to eliminate the phase ambiguity and using the GHZ states to obtain phase value, simultaneously. For an N-party entangled state, our approach can achieve an upper bound of sensitivity of δθ=sqrt[3/(N^{2}+2N)], which beats the limit of adaptive Bayesian estimation. By performing an eight-photon experiment, we demonstrate the estimation of unknown phases in a full period, and observe the phase superresolution and sensitivity beyond the shot-noise limit. Our Letter provides a new way for quantum sensing and represents a solid step towards its general applications.

10.
Inorg Chem ; 62(23): 9158-9167, 2023 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-37243623

RESUMO

Photocatalytic degradation of organic pollutants via semiconductors with high visible light response and effective carrier separation is an economical and green route to greatly achieve environmental remediation. Herein, an efficient BiOI/Bi2MoO6 p-n heterojunction was in situ fabricated through hydrothermal method by substituting Mo7O246- species for I ions. The characteristic p-n heterojunction exhibited a strongly enhanced visible light responsive absorption from 500 to 700 nm owing to the narrow band gap of BiOI and a greatly effective separation of photoexcited carriers because of the built-in electric field on the interface between BiOI and Bi2MoO6. Moreover, the flower-like microstructure also promoted the adsorption of organic pollutants owing to the large surface area (about 10.36 m2/g), good for further photocatalytic degradation. As a result, BiOI/Bi2MoO6 p-n heterojunction showed an excellent photocatalytic activity of RhB of almost 95% in a short time of 90 min under wavelength longer than 420 nm, 2.3 and 2.7 times higher compared with single BiOI and Bi2MoO6, respectively. This work offers a promising approach to purify the environment through the utilization of solar energy by constructing efficient p-n junction photocatalysts.

11.
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.

12.
Nature ; 549(7670): 70-73, 2017 09 07.
Artigo em Inglês | MEDLINE | ID: mdl-28825708

RESUMO

An arbitrary unknown quantum state cannot be measured precisely or replicated perfectly. However, quantum teleportation enables unknown quantum states to be transferred reliably from one object to another over long distances, without physical travelling of the object itself. Long-distance teleportation is a fundamental element of protocols such as large-scale quantum networks and distributed quantum computation. But the distances over which transmission was achieved in previous teleportation experiments, which used optical fibres and terrestrial free-space channels, were limited to about 100 kilometres, owing to the photon loss of these channels. To realize a global-scale 'quantum internet' the range of quantum teleportation needs to be greatly extended. A promising way of doing so involves using satellite platforms and space-based links, which can connect two remote points on Earth with greatly reduced channel loss because most of the propagation path of the photons is in empty space. Here we report quantum teleportation of independent single-photon qubits from a ground observatory to a low-Earth-orbit satellite, through an uplink channel, over distances of up to 1,400 kilometres. To optimize the efficiency of the link and to counter the atmospheric turbulence in the uplink, we use a compact ultra-bright source of entangled photons, a narrow beam divergence and high-bandwidth and high-accuracy acquiring, pointing and tracking. We demonstrate successful quantum teleportation of six input states in mutually unbiased bases with an average fidelity of 0.80 ± 0.01, well above the optimal state-estimation fidelity on a single copy of a qubit (the classical limit). Our demonstration of a ground-to-satellite uplink for reliable and ultra-long-distance quantum teleportation is an essential step towards a global-scale quantum internet.

13.
Phys Rev Lett ; 129(16): 163602, 2022 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-36306767

RESUMO

We systematically study the decay of quasi-two-dimensional vortices in an oblate strongly interacting Fermi gas over a wide interaction range and observe that, as the system temperature is lowered, the vortex lifetime increases in the Bose-Einstein condensate (BEC) regime but decreases at unitarity and in the Bardeen-Cooper-Schrieffer (BCS) regime. The observations can be qualitatively captured by a phenomenological model simply involving diffusion and two-body collisional loss, in which the vortex lifetime is mostly determined by the slower process of the two. In particular, the counterintuitive vortex decay in the BCS regime can be interpreted by considering the competition between the temperature dependence of the vortex annihilation rate and that of unpaired fermions. Our results suggest a competing mechanism for the complex vortex decay dynamics in the BCS-BEC crossover for the fermionic superfluids.

14.
Phys Rev Lett ; 128(11): 110501, 2022 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-35363009

RESUMO

The recognition of entanglement states is a notoriously difficult problem when no prior information is available. Here, we propose an efficient quantum adversarial bipartite entanglement detection scheme to address this issue. Our proposal reformulates the bipartite entanglement detection as a two-player zero-sum game completed by parameterized quantum circuits, where a two-outcome measurement can be used to query a classical binary result about whether the input state is bipartite entangled or not. In principle, for an N-qubit quantum state, the runtime complexity of our proposal is O(poly(N)T) with T being the number of iterations. We experimentally implement our protocol on a linear optical network and exhibit its effectiveness to accomplish the bipartite entanglement detection for 5-qubit quantum pure states and 2-qubit quantum mixed states. Our work paves the way for using near-term quantum machines to tackle entanglement detection on multipartite entangled quantum systems.

15.
Phys Rev Lett ; 128(17): 170501, 2022 Apr 29.
Artigo em Inglês | MEDLINE | ID: mdl-35570417

RESUMO

Long-distance quantum state transfer (QST), which can be achieved with the help of quantum teleportation, is a core element of important quantum protocols. A typical situation for QST based on teleportation is one in which two remote communication partners (Alice and Bob) are far from the entanglement source (Charlie). Because of the atmospheric turbulence, it is challenging to implement the Bell-state measurement after photons propagate in atmospheric channels. In previous long-distance free-space experiments, Alice and Charlie always perform local Bell-state measurement before the entanglement distribution process is completed. Here, by developing a highly stable interferometer to project the photon into a hybrid path-polarization dimension and utilizing the satellite-borne entangled photon source, we demonstrate proof-of-principle QST at the distance of over 1200 km assisted by prior quantum entanglement shared between two distant ground stations with the satellite Micius. The average fidelity of transferred six distinct quantum states is 0.82±0.01, exceeding the classical limit of 2/3 on a single copy of a qubit.

16.
Biomacromolecules ; 23(5): 2064-2074, 2022 05 09.
Artigo em Inglês | MEDLINE | ID: mdl-35394757

RESUMO

Acute kidney injury (AKI) is a global healthcare burden characterized by rapid loss of renal function and high morbidity and mortality. Chemokine receptor CXCR4 participates in the renal infiltration of immune cells following injury and in local inflammatory enhancement. Injured renal tubule cells overexpress CXCR4, which could be used as a target for improved drug delivery in AKI. Plerixafor is a small-molecule CXCR4 antagonist that has shown beneficial effects against AKI and has been previously developed into a polymeric analog (polymeric plerixafor, PP). With the goal of gaining a better understanding of how overall charge and hydrophilicity affect renal accumulation of PP, we have synthesized PP copolymers containing hydroxyl, carboxyl, primary amine, and alkyl moieties using Michael-type addition copolymerization. All synthesized copolymers showed excellent CXCR4-binding and inhibiting ability in vitro and improved cellular uptake in hypoxia-reoxygenation stimulated mouse tubule cells. Analysis of serum protein binding revealed that polymers with hydroxyl group modification showed the least amount of protein binding. Biodistribution of the polymers was tested in a unilateral ischemia reperfusion-induced AKI mouse model. The results showed significant differences in accumulation in the injured kidneys depending on the net charge and hydrophilicity of the polymers. The findings of this study will guide the development of polymeric drug carriers for targeted delivery to injured kidneys for better AKI therapy.


Assuntos
Injúria Renal Aguda , Compostos Heterocíclicos , Traumatismo por Reperfusão , Injúria Renal Aguda/tratamento farmacológico , Injúria Renal Aguda/metabolismo , Animais , Feminino , Mobilização de Células-Tronco Hematopoéticas , Humanos , Rim/metabolismo , Masculino , Camundongos , Polieletrólitos , Polímeros/metabolismo , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/metabolismo , Distribuição Tecidual
17.
Cardiovasc Drugs Ther ; 36(6): 1075-1089, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-34436706

RESUMO

PURPOSE: Anti-inflammatory therapy is important for reducing myocardial injury after acute myocardial infarction (MI). New anti-inflammatory drugs and their mechanism are necessary to be explored to improve clinical efficacy. We aimed to improve the efficacy of colchicine on attenuating MI injury by nano-drug delivery systems and to investigate the mechanism of anti-inflammatory. METHODS: A colchicine-containing delivery system based on calcium carbonate nanoparticles (ColCaNPs) was synthesized. The protection against MI by ColCaNPs was evaluated using an in vivo rat model established by ligating the left anterior descending coronary artery. Macrophage polarization and the levels of inflammatory cytokines were determined using immunohistochemistry, Western blot, and ELISA analysis. RESULTS: ColCaNP treatment showed about a 45% reduction in myocardial infarct size and attenuating myocardial fibrosis compared with groups without drug intervention after MI. Furthermore, ColCaNPs significantly decreased the levels of CRP, TNF-α, and IL-1ß in serum and the expression of proinflammatory cytokine in myocardial tissues after MI (p < 0.05). We also found that ColCaNPs notably restrained pyroptosis and inhibited inflammatory response by modulating on M1/M2 macrophage polarization and suppressing TLR4/NFκB/NLRP3 signal pathway. CONCLUSION: Colchicine-containing nanoparticles can protect against MI injury in a clinically relevant rat model by reducing inflammation. In addition, calcium carbonate nanoparticles can increase the cardioprotective effects of colchicine.


Assuntos
Infarto do Miocárdio , Nanopartículas , Ratos , Animais , Colchicina/farmacologia , Colchicina/uso terapêutico , Modelos Animais de Doenças , Infarto do Miocárdio/tratamento farmacológico , Infarto do Miocárdio/prevenção & controle , Infarto do Miocárdio/metabolismo , Inflamação/tratamento farmacológico , Inflamação/prevenção & controle , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Citocinas , Nanopartículas/uso terapêutico , Carbonato de Cálcio/uso terapêutico
18.
Molecules ; 27(8)2022 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-35458639

RESUMO

Conformationally restrained polyamine analog PG11047 is a well-known drug candidate that modulates polyamine metabolism and inhibits cancer cell growth in a broad spectrum of cancers. Here, we report a structure-activity relationship study of the PG11047 analogs (HPGs) containing alkyl chains of varying length, while keeping the unsaturated spermine backbone unchanged. Synthesis of higher symmetrical homologues was achieved through a synthetic route with fewer steps than the previous route to PG11047. The amphiphilic HPG analogs underwent self-assembly and formed spherically shaped nanoparticles whose size increased with the hydrophobic alkyl group's increasing chain length. Assessment of the in vitro anticancer activity showed more than an eight-fold increase in the cancer cell inhibition activity of the analogs with longer alkyl chains compared to PG11047 in human colon cancer cell line HCT116, and a more than ten-fold increase in human lung cancer cell line A549. Evaluation of the inhibition of spermine oxidase (SMOX) showed no activity for PG11047, but activity was observed for its higher symmetrical homologues. Comparison with a reference SMOX inhibitor MDL72527 showed nine-fold better activity for the best performing HPG analog.


Assuntos
Antineoplásicos , Neoplasias Pulmonares , Nanopartículas , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Humanos , Poliaminas/química , Espermina/farmacologia
19.
Pharm Biol ; 60(1): 1-8, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34860644

RESUMO

CONTEXT: As an inhibitor cytochrome P450 family 2 subfamily C polypeptide 8 (CYP2C8), quercetin is a naturally occurring flavonoid with its glycosides consumed at least 100 mg per day in food. However, it is still unknown whether quercetin and selexipag interact. OBJECTIVE: The study investigated the effect of quercetin on the pharmacokinetics of selexipag and ACT-333679 in beagles. MATERIALS AND METHODS: The ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was used to investigate the pharmacokinetics of orally administered selexipag (2 mg/kg) with and without quercetin (2 mg/kg/day for 7 days) pre-treatment in beagles. The effect of quercetin on the pharmacokinetics of selexipag and its potential mechanism was studied through the pharmacokinetic parameters. RESULTS: The assay method was validated for selexipag and ACT-333679, and the lower limit of quantification for both was 1 ng/mL. The recovery and the matrix effect of selexipag were 84.5-91.58% and 94.98-99.67%, while for ACT-333679 were 81.21-93.90% and 93.17-99.23%. The UPLC-MS/MS method was sensitive, accurate and precise, and had been applied to the herb-drug interaction study of quercetin with selexipag and ACT-333679. Treatment with quercetin led to an increased in Cmax and AUC0-t of selexipag by about 43.08% and 26.92%, respectively. While the ACT-333679 was about 11.11% and 18.87%, respectively. DISCUSSION AND CONCLUSION: The study indicated that quercetin could inhibit the metabolism of selexipag and ACT-333679 when co-administration. Therefore, the clinical dose of selexipag should be used with caution when co-administered with foods high in quercetin.


Assuntos
Acetamidas/farmacocinética , Acetatos/farmacocinética , Inibidores do Citocromo P-450 CYP2C8/farmacologia , Pirazinas/farmacocinética , Quercetina/farmacologia , Animais , Anti-Hipertensivos/farmacocinética , Área Sob a Curva , Cromatografia Líquida de Alta Pressão , Cães , Feminino , Interações Ervas-Drogas , Masculino , Espectrometria de Massas em Tandem
20.
Phys Rev Lett ; 127(10): 103601, 2021 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-34533368

RESUMO

Interferometers are widely used in imaging technologies to achieve enhanced spatial resolution, but require that the incoming photons be indistinguishable. In previous work, we built and analyzed color erasure detectors, which expand the scope of intensity interferometry to accommodate sources of different colors. Here we demonstrate experimentally how color erasure detectors can achieve improved spatial resolution in an imaging task, well beyond the diffraction limit. Utilizing two 10.9-mm-aperture telescopes and a 0.8 m baseline, we measure the distance between a 1063.6 and a 1064.4 nm source separated by 4.2 mm at a distance of 1.43 km, which surpasses the diffraction limit of a single telescope by about 40 times. Moreover, chromatic intensity interferometry allows us to recover the phase of the Fourier transform of the imaged objects-a quantity that is, in the presence of modest noise, inaccessible to conventional intensity interferometry.

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