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Identification and semisynthesis of(-)-anisomelic acid as oral agent against SARS-CoV-2 in mice

National Science Review 2022年第11期9卷 29-36页

作者： Hai-Xin Yu Nan Zheng Chi-Tai Yeh Chien-Ming Lee Qi Zhang wen-lv Zheng Qing Chang Yuan-He Li Yu-Jun Li Gui-Zhen Wu Jun-Min Quan Lin-Qi Zhang Yew-Min Tzeng Zhen Yang Laboratory of Chemical Genomics School of Chemical Biology and Biotechnology Peking University Shenzhen Graduate School Department of Medicinal Research and Education Taipei Medical University-Shuang Ho Hospital Department of Applied Science Taitung University Center for Global Health and Infectious Diseases Comprehensive AIDS Research Center and Beijing Advanced Innovation Center for Structural Biology School of Medicine Tsinghua University Lanzhou Institute of Separation Science State Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education and Beijing National Laboratory for Molecular Science(BNLMS) College of Chemistry and Molecular EngineeringPeking University Shenzhen Bay Laboratory NHC Key Laboratory of Biosafety National Institute for Viral Disease Control and Prevention Chinese Center for Disease Control and Prevention Department of Applied Chemistry Chaoyang University of Technology

(-)-Anisomelic acid, isolated from Anisomeles indica(L.) Kuntze(Labiatae) leaves, is a macrocyclic cembranolide with a trans-fused α-methylene-γ-lactone motif. Anisomelic acid effectively inhibits SARS-Co V-2 replication and viral-induced cytopathic effects with an EC50 of 1.1 and 4.3 μM, *** studies of SARS-CoV-2-infected K18-hACE2 mice showed that oral administration of anisomelic acid and subcutaneous dosing of remdesivir can both reduce the viral titers in the lung tissue at the same level. To facilitate drug discovery, we used a semisynthetic approach to shorten the project timelines. The enantioselective semisynthesis of anisomelic acid from the naturally enriched and commercially available starting material(+)-costunolide was achieved in five steps with a 27% overall *** developed chemistry provides opportunities for developing anisomelic-acid-based novel ligands for selectively targeting proteins involved in viral infections.

关键词： identification enantioselective semisynthesis (−)-anisomelic acid oral agent anti-SARS-CoV-2

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Mechanism research progress on transition metal compound electrode materials for supercapacitors

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Rare Metals 2024年第9期43卷 4076-4098页

作者： Zhi-Hui Xu Xue-Lei Li Qing-wen Li Kai lv Jing-Shun Liu Xiu-Kun Hang Aruuhan Bayaguud School of Materials Science and Engineering Inner Mongolia University of Technology School of Materials Science and Engineering Tianjin University of Technology College of Chemistry and Chemical Engineering Inner Mongolia University

Supercapacitors(SCs) have remarkable energy storage capabilities and have garnered considerable interest due to their superior power densities and ultra-long cycling characteristics. However, their comparatively low energy density limits their extensive application in large-scale commercial applications. Electrode materials directly affect the performance of SCs. Thus, the development of cutting-edge electrode materials and modification of their morphological and structural properties are vital for advancing the performance of SCs. Transition metal compounds have a high specific capacity and good cycling durability, making them the most promising electrode active materials for high-energy density SCs. Nevertheless,their inadequate conductivity, unfavorable ion diffusion rates, substantial volume expansion and phase transitions during charging and discharging are obstacles to their stable and efficient integration into SCs. To address these challenges, this study provides a comprehensive summary of the current advancements in transition metal nanomaterials as electrode materials for SCs, an overview of the current research status, and the prevailing ***, this study highlights synthetic techniques and management strategies for electrode materials derived from transition metal compounds, targeting the resolution of the aforementioned challenges. Finally, a concise discussion is provided on the future directions of SC development, with an emphasis on the utilization of transition metal compound electrode materials.

关键词： Electrodes

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In-situ SEM characterization of fracture mechanism of TiB/Ti-2Al-6Sn titanium matrix composites after electroshocking treatment

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Rare Metals 2024年第6期43卷 2805-2818页

作者： Ya-Ya Wu Jian Zhou Guo-Lei Han Yan wen Zhou Wang Li-Qiang Wang Wei-Jie lv Le-Chun Xie Lin Hua Hubei Key Laboratory of Advanced Technology for Automotive Components Wuhan University of TechnologyWuhan 430070China Hubei Collaborative Innovation Center for Automotive Components Technology Wuhan 430070China Faculty of Materials and Manufacturing Beijing University of TechnologyBeijing 100124China State Key Laboratory of Metal Matrix Composites School of Materials Science and EngineeringShanghai Jiao Tong UniversityShanghai 200240China

In this article,in-situ scanning electron microscope characterization of the tensile properties of TiB/Ti-2Al-6Sn titanium matrix composite(TMC)was conducted before and after electroshocking treatment(EST).After EST,the tensile strength increased by 113.2 *** effect of EST on the tensile strength and fracture behavior of TiB was investigated using in-situ characterization of the fracture morphology and crack propagation path of the matrix and *** EST,TiB fracture introduced cracks that extended into the matrix,resulting in material *** EST,the refined TiB improved the bearing capacity of the matrix,thereby improving TMC ***,after EST,the cracks were introduced into the matrix,and resulting the fracture of matrix *** an increase in the external load,cracks in the matrix were observed to propagate to TiB,and the refined TiB was fractured,detached,and pulled out,resulting in the formation of *** the propagation path of the main crack after EST showed that the deflection angle of the main crack *** micro structure of the fracture surface indicated that the fracture of the matrix was plastic,whereas that of TiB was *** EST,the size and area of the dimples increased,confirming the increase in *** results revealed that the comprehensive mechanical properties of TiB/Ti-2Al-6Sn improved after ***,EST is an efficient method for tailoring the micro structures and mechanical properties of TMCs.

关键词： TiB/Ti-2Al-6Sn In-situ microstructure characterization Tensile properties Reinforcement Electroshocking treatment(EST)

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Hypervalent iodine-mediated gem-difluorination of vinyl halides enabled by exclusive 1,2-halo migration

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Science China Chemistry 2021年第6期64卷 999-1003页

作者： Chenglong Li Yangzhen Liao Xuemei Tan Xiaozu Liu Peijun Liu wen-Xin lv Honggen Wang Key Laboratory of Biocatalysis&Chiral Drug Synthesis of Guizhou Province Generic Drug Research Center of Guizhou ProvinceSchool of PharmacyZunyi Medical UniversityZunyi 563000China Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education Zunyi Medical UniversityZunyi 563000China Guangdong Key Laboratory of Chiral Molecule and Drug Discovery School of Pharmaceutical SciencesSun Yat-sen UniversityGuangzhou 510006China

β-Difluorinated alkyl halides are of significant value in the modular synthesis of gem-difluorinated *** exclusive 1,2-halo migratory gem-difluorination of vinyl halides with in situ-generated PhIF_(2)·HF is *** protocol provides a general and practical approach towards a wide variety ofβ-difluorinated alkyl ***α-andβ-bromoalkyl alkenes are suitable substrates,leading to two distinct types of *** extension of this protocol to vinyl chloride and iodide are also *** synthetic versatility of this method has been highlighted by the late-stage modification of complex small molecules and further transformations of theβ-difluorinated alkyl halides to valuable CF_(2)-containing compounds.

关键词： gem-difluorination vinyl halides 1,2-halo migration hypervalent iodine late-stage modification

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Basilic vein variation encountered during surgery for arm vein port:A case report

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World Journal of Clinical Cases 2024年第12期12卷 2086-2091页

作者： Cheng-Da Hu Rui lv Ya-Xin Zhao Ming-Hao Zhang Hong-Dou Zeng Yi-wen Mao Department of Breast Surgery The Second Affiliated Hospital and Yuying Children’s Hospital of Wenzhou Medical UniversityWenzhou 325000Zhejiang ProvinceChina

BACKGROUND Venous variations are uncommon and usually hard to identify,and basilic vein variation is particularly *** vein variation usually presents without any clinical symptoms and is often regarded as a benign *** case was a patient with congenital basilic vein variation encountered during surgery for an infusion *** SUMMARY We documented and analyzed an uncommon anatomical variation in the basilic vein encountered during arm port *** peculiarity has hitherto remained undescribed in the *** offer remedial strategies for addressing this anomaly in the future and precautionary measures to circumvent its *** conducted a comprehensive review of analogous cases in the literature,offering pertinent therapeutic recommendations and solutions,with the aim of enhancing the efficacy and safety of future arm port *** Venous variation is rare and requires detailed intraoperative and postoperative examination to ensure accuracy,so as not to affect subsequent treatment.

关键词： Totally implantable venous access ports Arm ports Venous variation Postoperative breast cancer Systematic review Case report

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行政区划调整与边疆治理效能研究--以广西钦廉地区1000年、650年、50年的变迁为观察视角

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云南社会科学 2022年第1期 11-18,187页

作者：吕文利中国社会科学院大学中国社会科学院中国边疆研究所

宋代以降,围绕钦廉地区的归属问题,历代政府根据当时的情况不同而有所调整。宋朝成立了独立的高层政区--广南西路,其背景是交趾的独立,钦廉地区作为广南西路边防的前沿而受到重视。元朝把钦廉地区归为海北海南道,但在行省一级上,与广西... 详细信息

宋代以降,围绕钦廉地区的归属问题,历代政府根据当时的情况不同而有所调整。宋朝成立了独立的高层政区--广南西路,其背景是交趾的独立,钦廉地区作为广南西路边防的前沿而受到重视。元朝把钦廉地区归为海北海南道,但在行省一级上,与广西其他地区一起,统归于湖广行省管理。明朝基本继承了元末的行政建制,但把钦廉地区划归为广东行省,此项省一级行政区的调整,后历经清朝和民国,几无变化。而促成这样调整的,恰是明初与安南建立了较为稳定的宗藩关系,“防边”思维压倒了“边防”思维,由此历明、清、民国并未调整。中华人民共和国成立后,广西各民族进入了和睦相处、共同发展时期。1965年,经中央协调,把钦廉地区由广东划归广西。以1000年、650年、50年这三个视角考察钦廉地区的归属问题及治理效能,有助于理解在“行政区划标签”下的国家决策,对如何实现西南边疆稳定,如何促进西部大开发、促进区域发展,特别是对当代广西地区的治理,具有重要的参考价值和借鉴意义。

关键词：宋代广西钦廉地区归属治理效能

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Genome mining of sulfonated lanthipeptides reveals unique cyclic peptide sulfotransferases

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Acta Pharmaceutica Sinica B 2024年第6期14卷 2773-2785页

作者： Meng Wang wen-Wei Li Zhe Cao Jianong Sun Jiang Xiong Si-Qin Tao Tinghong lv Kun Gao Shangwen Luo Shi-Hui Dong State Key Laboratory of Applied Organic Chemistry College of Chemistry and Chemical EngineeringLanzhou UniversityLanzhou 730000China

Although sulfonation plays crucial roles in various biological processes and is frequently utilized in medicinal chemistry to improve water solubility and chemical diversity of drug leads,it is rare and underexplored in ribosomally synthesized and post-translationally modified peptides(RiPPs).Biosynthesis of RiPPs typically entails modification of hydrophilic residues,which substantially increases their chemical stability and bioactivity,albeit at the expense of reducing water *** explore sulfonated RiPPs that may have improved solubility,we conducted co-occurrence analysis of RiPP class-defining enzymes and sulfotransferase(ST),and discovered two distinctive biosynthetic gene clusters(BGCs)encoding both lanthipeptide synthetase(LanM)and *** expressing these BGCs,we characterized the structures of novel sulfonated lanthipeptides and determined the catalytic details of LanM and *** demonstrate that SslST-catalyzed sulfonation is leader-independent but relies on the presence of A ring formed by *** LanM and ST are promiscuous towards residues in the A ring,but ST displays strict regioselectivity toward *** recognition of cyclic peptide by ST was further *** evaluation underscores the significance of the ST-catalyzed *** study sets up the starting point to engineering the novel lanthipeptide STs as biocatalysts for hydrophobic lanthipeptides improvement.

关键词： Lanthipeptides Sulfotransferases Sulfonation Biosynthesis Genome mining

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Mechanism of active silica nanofluids based on interface-regulated effect during spontaneous imbibition

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Petroleum Science 2021年第3期18卷 883-894页

作者： Xu-Guang Song Ming-Wei Zhao Cai-Li Dai Xin-Ke Wang wen-Jiao lv Key Laboratory of Unconventional Oil and Gas Development Ministry of EducationSchool of Petroleum EngineeringChina University of Petroleum(East China)Qingdao 266580ShandongChina Shandong Key Laboratory of Oilfeld Chemistry School of Petroleum EngineeringChina University of Petroleum(East China)Qingdao 266580China

The ultra-low permeability reservoir is regarded as an important energy source for oil and gas resource development and is attracting more and more *** this work,the active silica nanofuids were prepared by modifed active silica nanoparticles and surfactant *** dispersion stability tests showed that the hydraulic radius of nanofuids was 58.59 nm and the zeta potential was−48.39 *** active nanofuids can simultaneously regulate liquid-liquid interface and solid-liquid *** nanofuids can reduce the oil/water interfacial tension(IFT)from 23.5 to 6.7 mN/m,and the oil/water/solid contact angle was altered from 42°to 145°.The spontaneous imbibition tests showed that the oil recovery of 0.1 wt%active nanofuids was 20.5%and 8.5%higher than that of 3 wt%NaCl solution and 0.1 wt%BSSB-12 ***,the efects of nanofuids on dynamic contact angle,dynamic interfacial tension and moduli were studied from the adsorption behavior of nanofuids at solid-liquid and liquid-liquid *** oil detaching and transporting are completed by synergistic efect of wettability alteration and interfacial tension *** fndings of this study can help in better understanding of active nanofuids for EOR in ultra-low permeability reservoirs.

关键词： Active nanofuids Regulate interface Ultra-low permeability Spontaneous imbibition

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Development of a new Cox model for predicting long-term survival in hepatitis cirrhosis patients underwent transjugular intrahepatic portosystemic shunts

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World Journal of Gastrointestinal Surgery 2024年第2期16卷 491-502页

作者： Yi-Fan lv Bing Zhu Ming-Ming Meng Yi-Fan Wu Cheng-Bin Dong Yu Zhang Bo-wen Liu Shao-Li You Sa lv Yong-Ping Yang Fu-Quan Liu Liver Disease Minimally Invasive Diagnosis and Treatment Center Beijing Shijitan HospitalCapital Medical UniversityBeijing 100038China Liver Vascular Disease Diagnosis and Treatment Center The Fifth Medical Center of Chinese People's Liberation Army General HospitalBeijing 100039China

BACKGROUND Transjugular intrahepatic portosystemic shunt(TIPS)placement is a procedure that can effectively treat complications of portal hypertension,such as variceal bleeding and refractory ***,there have been no specific studies on predicting long-term survival after TIPS *** To establish a model to predict long-term survival in patients with hepatitis cirrhosis after *** A retrospective analysis was conducted on a cohort of 224 patients who un-derwent TIPS *** univariate and multivariate Cox regression analyses,various factors were examined for their ability to predict survival at 6 years after ***,a composite score was formulated,encompassing the indication,shunt reasonability,portal venous pressure gradient(PPG)after TIPS,percentage decrease in portal venous pressure(PVP),indocyanine green retention rate at 15 min(ICGR15)and total bilirubin(Tbil)***,the performance of the newly developed Cox(NDC)model was evaluated in an in-ternal validation cohort and compared with that of a series of existing *** The indication(variceal bleeding or ascites),shunt reasonability(reasonable or unreasonable),ICGR15,post-operative PPG,percentage of PVP decrease and Tbil were found to be independent factors affecting long-term survival after TIPS *** NDC model incorporated these parameters and successfully identified patients at high risk,exhibiting a notably elevated mortality rate following the TIPS procedure,as observed in both the training and validation ***,in terms of predicting the long-term survival rate,the performance of the NDC model was significantly better than that of the other four models[Child-Pugh,model for end-stage liver disease(MELD),MELD-sodium and the Freiburg index of post-TIPS survival].CONCLUSION The NDC model can accurately predict long-term survival after the TIPS procedure in patients with hepatitis cirrhosis,help identify high-risk patients

关键词： Transjugular intrahepatic portosystemic shunt Long-term survival Predictive model

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Photo-triggered nucleus targeting for cancer drug delivery

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Nano Research 2021年第8期14卷 2630-2636页

作者： Yafei Li wen lv Lang Wang Yarning Zhang Lipeng Yang Tianyi Wang Linyong Zhu Yufeng Wang Weiping Wang Department of Pharmacology and Pharmacy Li Ka Shing Faculty of MedicineThe University of Hong KongHong KongChina Dr.Li Dak-Sum Research Centre The University of Hong KongHong KongChina Department of Chemistry The University of Hong Kong Hong Kong China School of Chemistry and Molecular Engineering East China University of Science and Technology Shanghai 200030China

Here,we report a strategy to deliver drug nanoparticles into cells with nucleus-targeting ability under a spatiotemporal *** nanoparticles were constructed through self-assembly of photoresponsive prodrugs and free *** incorporating a nucleus localization sequence in the system,drug nanoparticles could be delivered into nuclei upon visible light *** drug nanoparticles showed high drug loading capacity and specific nucleus-targeting ability,which efficiently killed cancer *** self-assembly strategy could be applied to other hydrophobic drugs and targeting ligands for photo-controlled organelle-targeted drug delivery.

关键词： phototargeting dePEGylation nucleus targeting coumarin photoresponsive prodrugs

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