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1.
Opt Lett ; 49(8): 1969-1972, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38621053

RESUMO

Photonic integrated circuits have garnered significant attention and experienced rapid development in recent years. To provide fundamental building blocks for scalable optical classical and quantum information processing, one important direction is to develop cryogenic compatible photonic integrated devices. Here, we prepare one optical filter on a lithium-niobate-on-insulator (LNOI) platform based on a multimode waveguide grating and verify its availability at temperature from 295 to 7 K. We find that the integrated optical filter still shows good quality under cryogenic conditions, and the shift of the working wavelength at different temperatures is well explained by the index variation of the material. These results advance LNOI integrated optical devices in applications under cryogenic conditions.

2.
Molecules ; 29(3)2024 Feb 02.
Artigo em Inglês | MEDLINE | ID: mdl-38338433

RESUMO

Natural bioactive compounds are valuable resources for drug discovery due to their diverse and unique structures. However, these compounds often lack optimal drug-like properties. Therefore, structural optimization is a crucial step in the drug development process. By employing medicinal chemistry principles, targeted molecular operations can be applied to natural products while considering their size and complexity. Various strategies, including structural fragmentation, elimination of redundant atoms or groups, and exploration of structure-activity relationships, are utilized. Furthermore, improvements in physicochemical properties, chemical and metabolic stability, biophysical properties, and pharmacokinetic properties are sought after. This article provides a concise analysis of the process of modifying a few marketed drugs as illustrative examples.


Assuntos
Produtos Biológicos , Desenho de Fármacos , Produtos Biológicos/farmacologia , Produtos Biológicos/química , Química Farmacêutica , Descoberta de Drogas , Relação Estrutura-Atividade
3.
Chem Rec ; 23(11): e202300173, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37401804

RESUMO

Enantiomerically enriched five- and six-membered benzo oxygen heterocycles are privileged architectures in functional organic molecules. Over the last several years, many effective methods have been established to access these compounds. However, comprehensive documents cover updated methodologies still in highly demand. In this review, recent transition metal catalyzed transformations lead to chiral five- and six-membered benzo oxygen heterocycles are presented. The mechanism and chirality transfer or control processes are also discussed in details.

4.
Front Bioeng Biotechnol ; 10: 1033514, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36324886

RESUMO

Nature is the source of human design inspiration. In order to adapt to the environment better, creatures in nature have formed various morphological structures during billions of years of evolution, among which the superhydrophobic characteristics of some animal and plant surface structures have attracted wide attention. At present, the preparation methods of bionic superhydrophobic surface based on the microstructure of animal and plant body surface include vapor deposition, etching modification, sol-gel method, template method, electrostatic spinning method and electrostatic spraying method, etc., which have been used in medical care, military industry, shipping, textile and other fields. Based on nature, this paper expounds the development history of superhydrophobic principle, summarizes the structure and wettability of superhydrophobic surfaces in nature, and introduces the characteristics differences and applications of different superhydrophobic surfaces in detail. Finally, the challenge of bionic superhydrophobic surface is discussed, and the future development direction of this field is prospected.

5.
Opt Express ; 30(22): 39911-39921, 2022 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-36298933

RESUMO

In chip-based quantum key distribution (QKD) systems, the non-ideal quantum state preparation due to the imperfect electro-optic phase modulators (EOPM) decreases the secret key rate and introduces potential vulnerabilities. We propose and implement an on-chip transmittance-invariant phase modulator (TIPM) to solve this problem. Simulated and experimental results show that TIPM can eliminate the correlation between phase, intensity, and polarization of quantum states caused by phase-dependent loss. The design can tolerate a significant fabrication mismatch and is universal to multi-material platforms. Furthermore, TIPM increases the modulation depth achievable by EOPMs in standard process design kit (PDK). The proposal of TIPM can improve the practical security and performance of the chip-based QKD systems.

6.
Polymers (Basel) ; 14(16)2022 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-36015621

RESUMO

Compared with other materials, polyethylene terephthalate (PET) has high transparency, excellent physical and mechanical properties in a wide temperature range and good hygiene and safety, so it is widely used in the packaging industry, especially in the packaging of beverages and foods. The optimization of PET bottles is mainly reflected in three aspects: material optimization, structure optimization and process optimization, among which there is much research on material optimization and process optimization, but there is no complete overview on structure optimization. A summary of structural optimization is necessary. Aiming at structural optimization, the finite element method is a useful supplement to the beverage packaging industry. By combining the computer-aided design technology and using finite element software for finite element simulation, researchers can replace the experimental test in the pre-research design stage, predict the effect and save cost. This review summarizes the development of PET bottles for beverage packaging, summarizes various optimization methods for preventing stress cracking in beverage packaging, and especially focuses on comparing and evaluating the effects of several optimization methods for packaging structure. Finally, the future development of all kinds of optimization based on structural optimization in the field of beverage packaging is comprehensively discussed, including personalized design, the combination of various methods and the introduction of actual impact factor calculation.

7.
Polymers (Basel) ; 14(14)2022 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-35890620

RESUMO

PET bottlesare often used as airtight containers for filling carbonated drinks. Because carbonated drinks contain large volumes of CO2 gas, the container needs to bear a tremendous pressure from the inside of the bottle.If the stress exceeds the bearing limit, the material will show the phenomenon of local cracking and liquid overflow.For the structural design, the method of manual adjustment before automatic adjustment was adopted. First, through manual optimization, the initial optimal parameter combination was as follows:the inner diameter of the bottle bottom was 17 mm, the dip angle of the valley bottom was 81°, the deepest part of the valley bottom was 25 mm, and the outer diameter was 27 mm. Comsol software was used for automatic optimization. Compared with the original bottle bottom, the total maximum principal stress and total elastic strain energy in the bottle bottom after manual-automatic double optimization decreased by 69.4% and 40.0%, respectively, and the displacement caused by deformation decreased by 0.60 mm (74.1%). The extremely high reduction ratio was caused by manual-automatic double optimization.

8.
Comput Intell Neurosci ; 2022: 6081680, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-38025495

RESUMO

Accurate monitoring of fire and smoke plays an irreplaceable role in preventing fires and safeguarding the safety of citizens' lives and property. The network structure of YOLOv5 is simple, but using convolution to extract features will lead to some problems such as limited receptive field, poor feature extraction ability, and insufficient feature integration. In view of the current defects of YOLOv5 target detection algorithm, a new algorithm model named Swin-YOLOv5 was proposed in this work. Swin transformation mechanism was introduced into YOLOv5 network, which enhanced the receptive field and feature extraction ability of the model without changing the depth of the model. In order to enrich the feature map splicing method of weighted Concat and enhance the feature fusion ability of model pairs, the feature splicing method of three output heads of feature fusion layer network was improved. The feature fusion module was further modified, and the weighted feature splicing method was introduced to improve the network feature fusion ability. Experiments showed that, compared with the original algorithm, the rising rate of mAP@0.5 (mean average precision, IoU=0.5) of the improved algorithm was 0.7%, the mAP@0.5:0.95 was increased by 4.5%, and the target detection speed with high accuracy was accelerated by 1.8 FPS (frames per second) under the same experimental dataset. The improved algorithm could more accurately detect the targets that were not detected or detected inaccurately by the original algorithm, which embodied the adaptability of real scene detection and had practical significance. This work provided an opportunity for the application of fire-smoke detection in forest and indoor scenes and also developed a feasible idea for feature extraction and fusion of YOLOv5.


Assuntos
Incêndios , Fumaça , Fumaça/efeitos adversos , Algoritmos
9.
Opt Lett ; 46(13): 3175-3178, 2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-34197409

RESUMO

To date, various quantum random number schemes have been demonstrated. However, the cost, size, and final random bit generation rate usually limits their wide application on-shelf. To overcome these limitations, we propose and demonstrate a compact, simple, and low-cost quantum random number generation based on a linear optocoupler. Its integrated structure consists mainly of a light emitting diode and a photodetector. Random bits are generated by directly measuring the intensity noise of the output light, which originates from the random recombination between holes of the p region and electrons of the n region in a light emitting diode. Moreover, our system is robust against fluctuation of the operating environment, and can be extended to a parallel structure, which will be of great significance for the practical and commercial application of quantum random number generation. After post-processing by the SHA-256 algorithm, a random number generation rate of 43 Mbps is obtained. Finally, the final random bit sequences have low autocorrelation coefficients with a standard deviation of 3.16×10-4 and pass the NIST-Statistical Test Suite test.

10.
Bioorg Chem ; 89: 102870, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31103493

RESUMO

Indoleamine 2,3-dioxygenase 1 (IDO1) is an attractive therapeutic target for the treatment of cancer, chronic viral infections and neurological disorders characterized by pathological immune stimulation. Herein, a series of known metal-chelating ubiquinone derivatives were designed, synthesized and evaluated for the IDO1 inhibiting activities. The docking studies showed that the compounds 11, 16, 18 and coenzyme-Q1 exhibited different binding modes to IDO1 protein. Among these compounds, the most active compound is 16d with an IC50 of 0.13 µM in enzymatic assay. The results reveal that a possible halogen bonding interaction between the bromine atom (3-Br) and Cys129 significantly enhances the inhibition activity against IDO1. This study provides structural insights of the interactions between ubiquinone analogues and IDO1 protein for the further modification and optimization.


Assuntos
Desenho de Fármacos , Inibidores Enzimáticos/síntese química , Indolamina-Pirrol 2,3,-Dioxigenase/antagonistas & inibidores , Ubiquinona/análogos & derivados , Sítios de Ligação , Domínio Catalítico , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Células HEK293 , Humanos , Indolamina-Pirrol 2,3,-Dioxigenase/metabolismo , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade , Ubiquinona/metabolismo , Ubiquinona/farmacologia
11.
Life Sci ; 200: 115-125, 2018 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-29555588

RESUMO

AIMS: This study aimed to evaluate the efficacy and mechanisms of Cappariloside A, a chemically synthesized compound, against virus and inflammation induced by influenza virus. MAIN METHODS: The inhibitory activity of Cappariloside A against influenza virus was determined by plaque assay and cytopathic effect inhibition assay. Quantitative real-time PCR, enzyme-linked immunosorbent assay and Bio-Plex methods were used to quantify cytokine and chemokine expression profiles. Effects of Cappariloside A were also evaluated in a mouse model of influenza virus infection. KEY FINDINGS: We successfully synthesized Cappariloside A, which could inhibit replication of a variety of viruses, including influenza viruses H1N1 and H3N2, PIV3 and ADV in vitro. Cappariloside A could also inhibit progeny virus replication at concentrations of 2 and 1 mg/mL. Simultaneously, it significantly reduced the expressions of IL-6, IP-10, MIG and RANTES/CCL-5 stimulated by A/PR/8/34 (H1N1) at a range of doses, even 0.5 mg/mL. Similar anti-inflammatory activity was detected in cells induced by avian influenza virus H9N2 or lipopolysaccharide. In addition, Cappariloside A clearly inhibited inflammatory response induced by mouse lung-adapted influenza strain PR8/H1N1. Furthermore, Cappariloside A strongly inhibited phosphorylated STAT1 levels and IFN-ß and IL-29 expressions induced by PR8/H1N1. Cappariloside A also inhibited IP-10 and CCL-5/RANTES expressions induced by exogenous human recombinant IFN-ß. SIGNIFICANCE: Cappariloside A not only shows broad-spectrum antiviral efficacy, but more effectively impairs the upregulations of pro-inflammatory factors in host cells induced by influenza virus. The potential antiviral mechanism of Cappariloside A is through inhibiting the activation of the host IFN signaling pathway.


Assuntos
Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , Vírus da Influenza A/fisiologia , Influenza Humana/tratamento farmacológico , Interferon beta/metabolismo , Transdução de Sinais/efeitos dos fármacos , Replicação Viral/efeitos dos fármacos , Células A549 , Animais , Quimiocinas/metabolismo , Chlorocebus aethiops , Cães , Humanos , Influenza Humana/metabolismo , Influenza Humana/patologia , Células Madin Darby de Rim Canino , Camundongos , Células RAW 264.7 , Células Vero
12.
Opt Express ; 25(22): 27923-27936, 2017 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-29092260

RESUMO

Polarization variations in the installed fibers are complex and volatile, and would severely affect the performances of polarization-sensitive quantum key distribution (QKD) systems. Based on the recorded data about polarization variations of different installed fibers, we establish an analytical methodology to quantitatively evaluate the influence of polarization variations on polarization-sensitive QKD systems. Using the increased quantum bit error rate induced by polarization variations as a key criteria, we propose two parameters - polarization drift time and required tracking speed - to characterize polarization variations. For field buried and aerial fibers with different length, we quantitatively evaluate the influence of polarization variations, and also provide requirements and suggestions for polarization basis alignment modules of QKD systems deployed in different kind of fibers.

13.
Opt Lett ; 42(6): 1023-1026, 2017 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-28295082

RESUMO

The calibration of the polarization basis between the transmitter and receiver is an important task in quantum key distribution. A continuously working polarization-basis tracking scheme (PBTS) will effectively promote the efficiency of the system and reduce the potential security risk when switching between the transmission and calibration modes. Here, we proposed a single-photon level continuously working PBTS using only sifted key bits revealed during an error correction procedure, without introducing additional reference light or interrupting the transmission of quantum signals. We applied the scheme to a polarization-encoding BB84 QKD system in a 50 km fiber channel, and obtained an average quantum bit error rate (QBER) of 2.32% and a standard derivation of 0.87% during 24 h of continuous operation. The stable and relatively low QBER validates the effectiveness of the scheme.

14.
Medchemcomm ; 8(9): 1806-1809, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-30108890

RESUMO

Based on structure modification and a high-throughput Jurkat-Lat cell screening model, we found that GIBH-LRA002, ethyl-2-amino-3-cyano-9-methyl-4-(trifluoromethyl)-4,9-dihydropyrano[2,3-b]indole-4-carboxylate, effectively reactivated the latent proviruses in a Jurkat-Lat cell line and primary CD4+ T cells from both chronic SIV-infected rhesus macaques and HIV-1 patients but without inducing systemic activation, making this compound attractive for potentially treating HIV-1 infection.

15.
Opt Lett ; 41(23): 5596-5599, 2016 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-27906248

RESUMO

Measurement-device-independent quantum key distribution (MDI QKD) is an efficient way to share secrets using untrusted measurement devices. However, the assumption on the characterizations of encoding states is still necessary in this promising protocol, which may lead to unnecessary complexity and potential loopholes in realistic implementations. Here, by using the mismatched-basis statistics, we present the first proof-of-principle experiment of MDI QKD with uncharacterized encoding sources. In this demonstration, the encoded states are only required to be constrained in a two-dimensional Hilbert space, and two distant parties (Alice and Bob) are resistant to state preparation flaws even if they have no idea about the detailed information of their encoding states. The positive final secure key rates of our system exhibit the feasibility of this novel protocol, and demonstrate its value for the application of secure communication with uncharacterized devices.

16.
Bioorg Med Chem Lett ; 25(14): 2744-8, 2015 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-26026363

RESUMO

A series of highly active C-aryl glucoside SGLT2 inhibitors containing a biphenyl motif were designed and synthesized for biological evaluation. Among the compounds tested, compound 16l demonstrated high inhibitory activity against SGLT2 (IC50=1.9 nM) with an excellent pharmacokinetic profile. Further study indicated that the in vivo efficacy of compound 16l was comparable to that of dapagliflozin, suggesting that further development would be worthwhile.


Assuntos
Compostos de Bifenilo/química , Glucosídeos/química , Hipoglicemiantes/química , Inibidores do Transportador 2 de Sódio-Glicose , Animais , Compostos de Bifenilo/síntese química , Compostos de Bifenilo/farmacocinética , Teste de Tolerância a Glucose , Glucosídeos/síntese química , Glucosídeos/farmacocinética , Meia-Vida , Humanos , Hipoglicemiantes/síntese química , Hipoglicemiantes/farmacocinética , Ligação Proteica , Ratos , Ratos Sprague-Dawley , Transportador 1 de Glucose-Sódio/antagonistas & inibidores , Transportador 1 de Glucose-Sódio/metabolismo , Transportador 2 de Glucose-Sódio/metabolismo , Relação Estrutura-Atividade
17.
Org Lett ; 17(3): 540-3, 2015 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-25594307

RESUMO

A highly enantioselective C2 Friedel-Crafts alkylation reaction of 3-substituted indoles to ß,γ-unsaturated α-ketimino esters has been developed. This reaction was efficiently catalyzed by a chiral phosphoric acid catalyst. The corresponding C2-substituted indole derivatives, bearing an α-ketimino ester motif, were obtained in moderate to high yields (up to 93%) and with high enantioselectivities (up to >99% ee).


Assuntos
Indóis/química , Cetonas/química , Ácidos Fosfóricos/química , Alquilação , Catálise , Ésteres , Estrutura Molecular , Estereoisomerismo
18.
Yao Xue Xue Bao ; 49(1): 61-7, 2014 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-24783507

RESUMO

Though all the marketed drugs of dipeptidyl peptidase IV inhibitors are structurally different, their inherent correlation is worthy of further investigation. Herein we rapidly discovered a novel DPP-IV inhibitor 8g (IC50 = 4.9 nmol.L-1) which exhibits as good activity and selectivity as the market drugs through scaffold hopping and drug splicing strategies based on alogliptin and linagliptin. This study demonstrated that the employment of classic medicinal chemistry strategy to the marketed drugs with specific target is an efficient approach to discover novel bioactive molecules.


Assuntos
Inibidores da Dipeptidil Peptidase IV/síntese química , Desenho de Fármacos , Descoberta de Drogas/métodos , Hipoglicemiantes/síntese química , Inibidores da Dipeptidil Peptidase IV/química , Humanos , Hipoglicemiantes/química , Linagliptina/síntese química , Linagliptina/química , Estrutura Molecular , Piperidinas/síntese química , Piperidinas/química , Relação Estrutura-Atividade , Uracila/análogos & derivados , Uracila/síntese química , Uracila/química
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