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Design and optimization of piperidinesubstituted thiophene[3,2-d]pyrimidine-based HIV-1 NNRTIs with improved drug resistance and pharmacokinetic profiles

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3110-3124页

作者： Yanying Sun Zhenzhen Zhou Zhongling Shi Fabao Zhao Minghui Xie Zongji Zhuo Erik De Clercq Christophe Pannecouqueb Dongwei Kang peng zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesShandong UniversityJinan 250012China Rega Institute for Medical Research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province Jinan 250012China

HIV-1 reverse transcriptase(RT)has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome(AIDS),but the inevitable drug resistance and side effects have always been major challenges faced by non-nucleoside reverse transcriptase inhibitors(NNRTIs).This work aimed to identify novel chemotypes of anti-HIV-1 agents with improved drugresistance profiles,reduced toxicity,and excellent druggability.A series of diarylpyrimidine(DAPY)derivatives were prepared via structural modifications of the leads K-5a2 and *** them,15a with dimethylphosphine oxide moiety showed the most prominent antiviral potency against all of the tested viral panel,being 1.6-fold(WT,EC_(50) Z 1.75 nmol/L),3.0-fold(L100I,EC_(50) Z 2.84 nmol/L),2.4-fold(K103N,EC_(50) Z 1.27 nmol/L),3.3-fold(Y181C,EC50 Z 5.38 nmol/L),2.9-fold(Y188L,EC_(50) Z 7.96 nmol/L),2.5-fold(E138K,EC_(50) Z 4.28 nmol/L),4.8-fold(F227L/V106A,EC_(50) Z 3.76 nmol/L)and 5.3-fold(RES056,EC_(50) Z 15.8 nmol/L)more effective than that of the marketed drug *** docking results illustrated the detailed interactions formed by compound 15a and WT,F227L/V106A,and RES056 ***,15a-HCl carried outstanding pharmacokinetic(t1/2 Z 1.32 h,F Z 40.8%)and safety profiles(LD_(50)>2000 mg/kg),which demonstrated that 15a HCl is a potential anti-HIV-1 drug candidate.

关键词： HIV-1 NNRTIs NNIBP Structural alert Anti-HIV-1 drug candidate

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Enhancing the Quality of Low-Light Printed Circuit Board Images through Hue, Saturation, and Value Channel Processing and Improved Multi-Scale Retinex

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Journal of Computer and Communications 2024年第1期12卷 1-10页

作者： Huichao shang penglei Li Xiangqian peng School of Mechanical and Electrical Engineering Zhongyuan University of Technology Zhengzhou China School of Mechanical and Electrical Engineering Hunan University of Science and Technology Xiangtan China

To address the issue of deteriorated PCB image quality in the quality inspection process due to insufficient or uneven lighting, we proposed an image enhancement fusion algorithm based on different color spaces. Firstly, an improved MSRCR method was employed for brightness enhancement of the original image. Next, the color space of the original image was transformed from RGB to HSV, followed by processing the S-channel image using bilateral filtering and contrast stretching algorithms. The V-channel image was subjected to brightness enhancement using adaptive Gamma and CLAHE algorithms. Subsequently, the processed image was transformed back to the RGB color space from HSV. Finally, the images processed by the two algorithms were fused to create a new RGB image, and color restoration was performed on the fused image. Comparative experiments with other methods indicated that the contrast of the image was optimized, texture features were more abundantly preserved, brightness levels were significantly improved, and color distortion was prevented effectively, thus enhancing the quality of low-lit PCB images.

关键词： Low-Lit PCB Images Spatial Transformation Image Enhancement Image Fusion HSV

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2-APQC,a small-molecule activator of Sirtuin-3(SIRT3),alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis

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Signal Transduction and Targeted Therapy 2024年第6期9卷 2748-2764页

作者： Fu peng Minru Liao Wenke Jin Wei Liu Zixiang Li Zhichao Fan Ling Zou Siwei Chen Lingjuan Zhu Qian Zhao Gu zhan Liang Ouyang Cheng peng Bo Han Jin zhang Leilei Fu West China School of Pharmacy and Department of Biotherapy Cancer Center and State Key Laboratory of BiotherapyWest China HospitalSichuan UniversityChengdu 610041China Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs School of Life Science and EngineeringSouthwest Jiaotong UniversityChengdu 610031China State Key Laboratory of Southwestern Chinese Medicine Resources Hospital of Chengdu University of Traditional Chinese MedicineSchool of PharmacyChengdu University of Traditional Chinese MedicineChengdu 611137China School of Pharmaceutical Sciences Health Science CenterShenzhen UniversityShenzhen 518060China School of Traditional Chinese Materia Medica Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China

Sirtuin 3(SIRT3)is well known as a conserved nicotinamide adenine dinucleotide^(+)(NAD^(+))-dependent deacetylase located in the mitochondria that may regulate oxidative stress,catabolism and ATP *** evidence has recently revealed that SIRT3 plays its critical roles in cardiac fibrosis,myocardial fibrosis and even heart failure(HF),through its deacetylation ***,discovery of SIRT3 activators and elucidating their underlying mechanisms of HF should be urgently ***,we identified a new small-molecule activator of SIRT3(named 2-APQC)by the structure-based drug designing strategy.2-APQC was shown to alleviate isoproterenol(ISO)-induced cardiac hypertrophy and myocardial fibrosis in vitro and in vivo rat ***,in SIRT3 knockout mice,2-APQC could not relieve HF,suggesting that 2-APQC is dependent on SIRT3 for its protective ***,2-APQC was found to inhibit the mammalian target of rapamycin(mTOR)-p70 ribosomal protein S6 kinase(p70S6K),c-jun N-terminal kinase(JNK)and transforming growth factor-β(TGF-β)/small mother against decapentaplegic 3(Smad3)pathways to improve ISO-induced cardiac hypertrophy and myocardial *** upon RNA-seq analyses,we demonstrated that SIRT3-pyrroline-5-carboxylate reductase 1(PYCR1)axis was closely assoiated with *** activating PYCR1,2-APQC was shown to enhance mitochondrial proline metabolism,inhibited reactive oxygen species(ROS)-p38 mitogen activated protein kinase(p38MAPK)pathway and thereby protecting against ISO-induced mitochondrialoxidative ***,activation of SIRT3 by 2-APQC could facilitate AMP-activated protein kinase(AMPK)-Parkin axis to inhibit ISO-induced ***,our results demonstrate that 2-APQC is a targeted SIRT3 activator that alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis,which may provide a new clue on exploiting a promising drug candidate for the future HF therapeutics.

关键词： SIRT3 homeostasis metabolism

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Babao Dan Inhibits Gastric Cancer Progression in vivo Through Multiple Signaling Pathways

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World Journal of Traditional Chinese Medicine 2024年第1期10卷 14-21页

作者： Hai-Xia shang Yi Fang Bin Guan Jian-Hua Guan Jun peng Jin-Yan Zhao Jiu-Mao Lin Institute of Oncology of Academy of Integrative Medicine Fujian University of Traditional Chinese MedicineFuzhouFujianChina Key Laboratory of Integrative Medicine of Fujian Province University Fujian University of Traditional Chinese MedicineFuzhouFujianChina Fujian Key Laboratory of Integrative Medicine on Geriatric Fujian University of Traditional Chinese MedicineFuzhouFujianChina Innovation and Transformation Center Fujian University of Traditional Chinese MedicineFuzhouFujianChina Xiamen Traditional Chinese Medicine Co. Ltd.XiamenFujianChina

Objective:The aim of this study was to explore the effects of Babao dan(BBD),a traditional Chinese medicine,on gastric cancer(GC)progression in *** and Methods:A subcutaneous xenograft mouse model of GC was established using MGC80-3 *** terminal deoxynucleotidyl transferase-mediated dUTP:2'-deoxyuridine 5'-triphosphate-biotin nick-end labeling method was adopted to detect cell apoptosis in *** expression levels of proteins associated with proliferation,apoptosis,and angiogenesis were measured by immunohistochemical staining or western blotting(WB).The activation and protein levels of p-c-Jun N-terminal kinase(JNK),p-p38,p-extracellular-regulated kinase 1/2,p-nuclear factor-κB(NF-κB),and p-STAT3 were examined by Bio-plex and ***:BBD significantly inhibited tumor growth in GC mouse models with no adverse effect on body weight or organ *** was also found that BBD significantly suppressed the proliferation of GC tumor cells,induced the apoptosis of tumor cells,and inhibited angiogenesis through inactivating with mitogen-activated protein kinase,NF-κB,and STAT3 ***:BBD exerts suppressive effects on GC tumor growth by regulating multiple pathways in vivo,which may provide a novel treatment option for GC therapy.

关键词： Babao dan gastric cancer multiple signaling pathways proliferation traditional Chinese medicine

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High-Value-Added Utilization of Turpentine:Screening of Anti-Influenza Virus Agents fromβ-Pinene Derivatives

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Journal of Renewable Materials 2024年第1期12卷 45-56页

作者： Yiwen Li Hongyan Si peng Wang Hai Luo Minggui Shen Xiaoping Rao zhanqian Song Shibin shang Zongde Wang Shengliang Liao East China Woody Fragrance and Flavor Engineering Research Center of National Forestry and Grassland Administration Camphor Engineering Research Center of National Forestry and Grassland AdministrationCollege of ForestryJiangxi Agricultural UniversityNanchang330045China Institute of Chemical Industry of Forestry Products China Academy of ForestryNational Engineering Laboratory for Biomass Chemical UtilizationKey and Open Laboratory of Forest Chemical EngineeringState Forestry AdministrationKey Laboratory of Biomass Energy and MaterialJiangsu ProvinceNanjing210042China College of Chemical Engineering Huaqiao UniversityXiamen361021China

Turpentine is a renewable and resourceful forest *** deep processing and utilization of turpentine,particularly its primary componentβ-pinene,has garnered widespread *** study aimed to synthesize 40 derivatives ofβ-pinene,including nopinone,3-cyanopyridines of nopinone,myrtanyl acid,myrtanyl acylthioureas,and myrtanyl *** assessed the antiviral activities of theseβ-pinene derivatives against influenza virus A/Puerto Rico/8/34(H1N1)using the 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide ***β-pinene derivatives were used before and after cellular infection with the influenza virus to evaluate their preventive and therapeutic effects against the H1N1 *** results showed that only compound 10o exhibited a preventive effect against the H1N1 virus with a half-maximal inhibitory concentration(IC50)value of 47.6μmol/*** the compounds,4e,4i,and 4l demonstrated therapeutic effects against cellular infection,with compound 4e displaying the most potent therapeutic effect(IC50=17.5μmol/L),comparable to the positive control *** findings indicated that certainβ-pinene derivatives exhibited in vitro antiviral activity against the H1N1 influenza A virus,warranting further investigation as potential anti-influenza agents.

关键词： Antiviral activity β-pinene derivative 3-cyanopyridine influenza virus

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Evolution of template-assisted two-dimensional porphyrin chiral grating structure by directed self-assembly using chiral second harmonic generation microscopy

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Chinese Chemical Letters 2024年第10期35卷 170-174页

作者： Changhui Yu peng shang Huihui Hu Yuening zhang Xujin Qin Linyu Han Caihe Liu Xiaohan Liu Minghua Liu Yuan Guo Zhen zhang Beijing National Laboratory for Molecular Sciences State Key Laboratory of Molecular Reaction DynamicsInstitute of ChemistryChinese Academy of SciencesBeijing 100190China University of Chinese Academy of Sciences Beijing 100049China Beijing National Laboratory for Molecular Science CAS Key Laboratory of ColloidInterface and Chemical ThermodynamicsInstitute of ChemistryChinese Academyof SciencesBeijing100190China

Directed self-assembly has been used to create micro-nano scale patterns,including chiral periodic structures of organic molecules,for potential applications in optics,photonics,metamaterials,and medical and sensing *** study presents a straightforward approach for fabricating large-scale chiral grating porphyrin assemblies through template-assisted *** solution of tetrakis(4-sulfonatophenyl)porphyrin(TPPS)was induced by chiral amino acids(L/D-arginine and L/D-serine)to selfassemble into highly ordered chiral grating structures with the assistance of sodium dodecyl sulfate(SDS).The structures show precise line widths(5.5μm)and gaps(18μm).Using in situ optical microscopy and second harmonic generation(SHG)microscopy,the chiral characteristics and dynamic evolution of the template-assisted self-assembly are *** is found that the chirality of amino acids induced TPPS self-assembled into chiral structures and the liquid contraction interface significantly enhanced the chirality of the *** study is significant for understanding the mechanism of chiral evolution and designing novel micro-nano materials with predetermined chiral properties.

关键词： Second harmonic generation microscopy Chiral assembly Porphyrin Chiral evolution Template-assisted self-assembly Micro-nano structure

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A potential giant gallium deposit hosted in the tailing dam of the Fankou Zn-Pb deposit in northern Guangdong Province, South China

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China Geology 2024年第1期7卷 157-160页

作者： peng-peng Yu Zhao-bin Hu Yi Zheng Lan-xuan Guo Shi-yuan Ouyang Gui-qiang Yuan shang-zhou Chen Cheng-ming Wang Xi Chen School of Earth Sciences and Geological Engineering Sun Yat-sen UniversityGuangzhou 510275China Guangdong Provincial Key Lab of Geological Process and Mineral Resources Survey Sun Yat-sen UniversityGuangzhou 510275China Southern Marine Science and Engineering Guangdong Laboratory(Zhuhai) Zhuhai 519000China Zhongjin Lingnan Nonfemet Co. LtdShenzhen 518000China

*** The Fankou giant zinc(Zn)-lead(Pb)deposit in Guangdong Province is well-known for its huge reserves of over 10 Mt(million ton)Zn+Pb metals and high ore-grade with Zn+Pb exceeding 15%(Guangdong Fankou Deposit Investigation Group,1980;Zhu XY et al.,2017).After 60 years of exploration and exploitation,the deposit has accumulated millions of tons of *** interesting question is that what components are hosted in these tailings,and whether some key and critical metals such as gallium and germanium are extremely enriched and worth further comprehensive *** motivated us to conduct an integrated set of field investigation,sampling,major-trace element analyses and reserve assessments about the Fankou *** this contribution,we discover that the tailings contain a variety of metal elements such as zinc,lead and gallium with comprehensive utilization *** data can act as a scientific guidance for further exploration and utilization of the Fankou tailings,and aid to enhance the utilization efficiency of the key mineral resource in *** study also provide demonstration for future green mine construction in China.

关键词： deposit comprehensive Guangdong

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Design,synthesis,and biological evaluation of benzo[4,5]thieno[2,3-d]pyrimidine derivatives as novel HIV-1 NNRTIs

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Chinese Chemical Letters 2024年第6期35卷 344-348页

作者： Bairu Meng Zongji Zhuo Han Yu Sining Tao Zixuan Chen Erik De Clercq Christophe Pannecouque Dongwei Kang peng zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJi’nan 250012China Laboratory of Virology and Chemotherapy Rega Institute for Medical ResearchK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province Ji’nan 250012China

Inspired by our previous studies to discover novel human immunodeficiency virus-1(HIV-1)nonnucleoside reverse transcriptase inhibitors(NNRTIs)by targeting the tolerant region II of the NNRTIs binding pocket(NNIBP),a series of novel benzo[4,5]thieno[2,3-d]pyrimidine derivatives were designed through structure-based drug design as novel potent HIV-1 *** results showed that compound16b was the most active inhibitor,exhibiting 50% effective concentration(EC50)values from 0.021μmol/L to 0.298μmol/L against wild-type(WT)and a panel of NNRTIs-resistant HIV-1 ***,16b was demonstrated with a significantly low 50% cytotoxicity concentration(CC_(50))value(>200μmol/L)and high selectivity index(SI)*** addition,16b yielded moderate reverse transcriptase(RT)enzyme inhibition with a 50% inhibition concentration(IC_(50))value of 0.183μmol/L,which demonstrated that it acted as HIV-1 *** binding mode of 16b with RT was also illustrated via molecular ***,this work provided a novel lead compound for developing potent HIV-1 NNRTIs.

关键词： HIV-1 NNRTIs DAPYs Tolerant regionⅡ Drug design

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Probing quantum causality with geometric asymmetry in spatial-temporal correlations

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Science China(Information Sciences) 2024年第9期67卷 294-305页

作者： Yu MENG Zheng-Hao LIU Zhikuan ZHAO peng YIN Yi-Tao WANG Wei LIU Zhi-peng LI Yuan-Ze YANG Zhao-An WANG Jin-Shi XU shang YU Jian-Shun TANG Chuan-Feng LI Guang-Can GUO CAS Key Laboratory of Quantum Information University of Science and Technology of China CAS Center for Excellence in Quantum Information and Quantum Physics University of Science and Technology of China Department of Computer Science Eidgen?ssische Technische Hochschule Zürich Hefei National Laboratory Department of Physics Imperial College London Research Center for Quantum Sensing Zhejiang Lab

Causation promotes the understanding of correlation to an advanced stage by elucidating its underlying mechanism. Although statisticians have specified the possible causal relations among correlations,inferring causal structures is impossible from only the observed correlations in the classical world. Quantum correlations encapsulating the most defining aspects of quantum physics have taken a new turn for the causal inference problem — the two-point spatial and temporal quantum correlations with observationally discernible characteristics correspond exactly to the two most basic causal structures. However, a direct causal interpretation for quantum correlations has only been established in very limited cases. Here, we explore to what extent quantum correlations promote causal inference. Theoretically, we have found that the distinguishable causal regime of two-point Pauli correlations can be expanded from a single value to an asymmetric interval, and the causal structures determining the quantum correlations can be interpreted by a simple distance criterion. Experimentally, we have devised and implemented a versatile non-unital quantum channel in an optical architecture to directly observe such an asymmetric interval. The setup enabled quantum causal inference without any requirement of active intervention, which is impossible in the classical realm. Our work facilitates the identification of causal links among quantum variables and provides insight into characterizing causation and spatial-temporal correlation in quantum mechanics.

关键词： causality quantum information quantum channel channel-state duality non-unital channel

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剩余污泥有机质资源回收利用原位驱动晚期垃圾渗滤液深度脱氮——一种具有显著能源优势的创新生物技术

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Engineering 2024年第3期34卷 120-132页

作者： Fangzhai zhang shang Ren Haoran Liang Zhaozhi Wang Ying Yan Jiahui Wang Yongzhen peng National Engineering Laboratory for Advanced Municipal Wastewater Treatment and Reuse Technology Engineering Research Center of BeijingBeijing University of TechnologyBeijing 100124China

The sustainable recovery and utilization of sludge bioenergy within a circular economy context has drawn increasing attention,but there is currently a shortage of reliable *** study presents an innovative biotechnology based on free nitrous acid(FNA)to realize sustainable organics recovery from waste activated sludge(WAS)in-situ,driving efficient nitrogen removal from ammonia rich mature landfill leachate by integrating partial nitrification,fermentation,and denitrification process(PN/DN-F/DN).First,ammonia((1708.5±142.9)mg·L^(-1))in mature landfill leachate is oxidized to nitrite in the aerobic stage of a partial nitrification coupling denitrification(PN/DN)sequencing batch reactor(SBR),with nitrite accumulation ratio of 95.4%±2.5%.Then,intermediate effluent(NO_(2)^(-)-N=(1196.9±184.2)mg·L^(-1))of the PN/DN-SBR,along with concentrated WAS(volatile solids(VSs)=(15119.8±2484.2)mg·L^(-1)),is fed into an anoxic reactor for fermentation coupling denitrification process(F/DN).FNA,the protonated form of nitrite,degrades organics in the WAS to the soluble fraction by the biocidal effect,and the released organics are utilized by denitrifiers to drive *** ultra-fast sludge reduction rate of 4.89 kg·m^(-3)·d^(-1) and nitrogen removal rate of 0.46 kg·m^(-3)·d^(-1) were realized in the ***,F/DN-SBR effluent containing organics is refluxed to PN/DN-SBR for secondary denitrification in the post anoxic *** 175 d operation,an average of 19350.6 mg chemical oxygen demand organics were recovered per operational cycle,with 95.2%nitrogen removal and 53.4%sludge ***/DN-F/DN is of great significance for promoting a paradigm transformation from energy consumption to energy neutral,specifically,the total benefit in equivalent terms of energy was 291.8 kW·h·t^(-1) total solid.

关键词： Waste activated sludge Bioresource recovery Simultaneous treatment of wastewater and sludge Mature landfill leachate Free nitrous acid

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