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Science China Chemistry 2024年第7期67卷 2199-2205页

作者： Hongyan Long Sha Zhao Chunyan Jian Xiuli Wu Fengfei Lu Minghong Liao Fengrui Che Xingxing Wu Yonggui Robin Chi State Key laboratory of Green Pesticide Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationGuizhou UniversityGuiyang 550025China School of Chemistry Chemical Engineeringand BiotechnologyNanyang Technological UniversitySingapore 637371Singapore

Organoseleniums exhibit a diverse set of biological activities that are pivotal for drug discovery and are widely explored in synthetic chemistry and material *** many transformations have been developed for non-enantioselective C–Se bond formations,the catalyst-controlled stereoselective preparation of chiral organoseleniums continues to be of considerable *** particular,there are limited studies on the enantioselective seleno-Michael addition reactions to access chiral selenium functional ***,we disclose a carbene-catalyzed highly enantioselective nucleophilic C–Se bond construction through formal[3+3]annulations between selenocarboxamides and bromoenals,affording seleno-thiazinone products with good yields and excellent *** choice of a weak inorganic base was pivotal to suppressing the unproductive racemization and decomposition of the selenium ***,the catalytically generated chiral selenium-containing heterocyclic products feature remarkable antimicrobial activities that could serve as promising lead scaffolds for further agrochemical development.

关键词： seleno-Michael addition organocatalysis N-heterocyclic carbene seleno-heterocycles antimicrobial activity

Biosafe,rapid,and ultrahigh-capacity endotoxin purification in blood by a sustainable and recyclable MOF-functionalized chitin microsphere adsorbent

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SusMat 2024年第5期4卷 163-177页

作者： Anxiong Liu Lu Chen Luhe Qi Jing Huang Yongkang Zou Zhiwen Hu Le Yu Zibiao Zhong Qifa Ye Chaoji Chen National Quality Control Center for Donated Organ Procurement Hubei Key Laboratory of Medical Technology on TransplantationHubei Clinical Research Center for Natural Polymer Biological LiverHubei Engineering Center of Natural Polymer-Based Medical MaterialsZhongnan Hospital of Wuhan UniversityInstitute of Hepatobiliary Diseases ofWuhan UniversityTransplant Center of Wuhan UniversityWuhanChina School of Resource and Environmental Science Hubei Biomass-Resource Chemistry and Environmental Biotechnology Key LaboratoryWuhan UniversityWuhanChina

Sepsis is responsible for approximately 5.3 million deaths globally each ***,we constructed hierarchical chitin microspheres loaded with MOF-919(Ch/metal–organic frameworks[MOFs])for the rapid and efficient removal of lipopolysaccharide(LPS)in complex blood ***,abun-dant active sites on MOF-919(Sc)also enable a record-high adsorption capacity of 9.56 mg/g in biomass-based adsorbents due to the coordination interactions between endotoxin and MOF-919(Sc).The LPS level of sepsis rabbits was less than 2 EU/mL(clearance rate>95%)after 90-min hemoperfusion,showing no adverse effect on the rabbit ***,compared to the commonly used LPS scrubber Toraymyxin(polymethyl methacrylate),the chitin adsorbent is significantly more cost-effective and environmentally *** prepara-tion strategy for hierarchical porous microspheres offers notable advantages in designability,recyclability,and renewability,providing a new approach to sepsis treatment and promising prospects for the biomedical application of sustainable biomass materials.

关键词： biomass blood purification chitin endotoxin removal hemoperfusion metal–organic frameworks

A chromatographic method for pursuing potential GPCR ligands with the capacity to characterize their intrinsic activities of regulating downstream signaling pathway

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Chinese Chemical Letters 2024年第10期35卷 425-429页

作者： Ting Li Xinxin Zheng Lejing Qu Yuanyuan Ou Sai Qiao Xue Zhao Yajun Zhang Xinfeng Zhao Qian Li Key laboratory of Resource Biology and biotechnology in Western China Ministry of EducationCollege of Life SciencesNorthwest UniversityXi'an 710069China

GPCRs are dominant targets for approved drugs and the discovery of lead compound targeting them is still ***-based screening technique is a promising platform to uncover GPCR ***,the intrinsic activities of them are seldom simultaneously determined during the *** beta2-adrenoceptor(β2AR)as a probe,this work created a strategy for screening GPCR ligands with simultaneous characterization of their downstream G protein binding responses associated with *** strategy included(i)the design and expression of a protein miniature formed byβ2AR and G proteinα-subunit(Gαs)using circularly permuted HaloTag(cpHalo)as a flexible linker;(ii)immobilization of the miniature onto silica gel by a click dehalogenation reaction;(iii)systematic characterization of the immobilized miniature by fluorescent and chromatographic studies,and(iv)simulating of ligand-inducedβ2AR-Gαs signaling cascade by chromatographic assays using GTP as an *** immobilized miniature exhibited specificity toβ2AR and Gαs antibodies and *** specificity is stable at least within fifteen days with the variation less than 1%.The intrinsic activities ofβ2AR ligands were distinguished by the changes of GTP chromatographic behaviors on Gαs-cpHalo-β2AR *** strengthened the binding affinity and kinetics of GTP with Gαs,while antagonist did not give any effect on *** the intrinsic activity evaluation,we believe,it will improve the attributes of chromatographic methods for drug discovery efforts with minimizing false-positive results.

关键词： Intrinsic efficacy GPCR-G protein miniature Circularly permuted HaloTag High-performance receptor chromatography GTP binding Agonist/antagonist

Development of a cell-permeable adenine-derived probe for capture of nucleotide-binding proteins in living cells

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Chinese Chemical Letters 2024年第3期35卷 243-246页

作者： Lihong Liu Rui Chen Gang Xue Chenzhou Hao Weizhi Weng Zhengying Pan State Key laboratory of Chemical Oncogenomics School of Chemical Biology and BiotechnologyPeking University Shenzhen Graduate SchoolShenzhen 518055China

Adenine is an essential building block of genetic material and a range of *** probes containing an adenine moiety have been used in kinase profiling studies in cell *** we report that adenine-derived small-molecule probes with an activated ester reactive group can covalently modify a conserved lysine residue of protein kinases and capture a number of nucleotide-binding proteins within living cells.

关键词： Adenine-derived probe Cell-permeable Lysine residue Protein kinases Nucleotide-binding proteins

An Update on the Clinical Pipelines of New Antibacterial Drugs Developed in China

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Engineering 2024年第7期38卷 52-68页

作者： Xinyi Yang Congran Li Xiukun Wang Zhonghui Zheng Peiyi Sun Chunjie Xu Luni Chen Jiandong Jiang Staffan Normark Birgitta Henriques-Normark Xuefu You Beijing Key laboratory of Antimicrobial Agents/laboratory of Pharmacology Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Division for Medicinal Microorganism-Related Strains CAMS Collection Center of Pathogenic MicroorganismsChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China State Key laboratory of Bioactive Substances and Functions of natural Medicines Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Shandong Xinhua Pharmaceutical Co. Ltd.Zibo 255005China Department of Microbiology Tumor and Cell BiologyKarolinska InstitutetStockholm SE-17177Sweden State Key laboratory of Bioactive Substances and Function of natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Institute of Medicinal biotechnology Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Clinical Microbiology Karolinska University HospitalBioclinicumStockholm SE-17176Sweden

Antibacterial resistance is a global health threat that requires further concrete action on the part of all *** this context,one of the biggest concerns is whether enough new antibacterial drugs are being discovered and *** several high-quality reviews on clinical antibacterial drug pipelines from a global perspective were published recently,none provides comprehensive information on original antibacterial drugs at clinical stages in *** this review,we summarize the latest progress of novel antibacterial drugs approved for marketing and under clinical evaluation in China since *** was obtained by consulting official websites,searching commercial databases,retrieving literature,asking personnel from institutions or companies,and other means,and a considerable part of the data covered here has not been included in other *** of June 30,2023,a total of 20 antibacterial projects from 17 Chinese pharmaceutical companies or developers were identified and *** them,two new antibacterial drugs that belong to traditional antibiotic classes were approved by the National Medical Products Administration(NMPA)in China in 2019 and 2021,respectively,and 18 antibacterial agents are in clinical development,with one under regulatory evaluation,five in phase-3,six in phase-2,and six in *** of the clinical candidates are new analogs or monocomponents of traditional antibacterial pharmacophore types,including two dual-acting hybrid antibiotics and a recombinant antibacterial ***,despite there being 17 antibacterial clinical candidates,our analysis indicates that there are still relatively few clinically differentiated antibacterial agents in stages of clinical development in ***,Chinese pharmaceutical companies and institutions will develop more innovative and clinically differentiated candidates with good market potential in the future research and development(R&D)of original antibacterial drugs.

关键词： Antimicrobial resistance New antibiotics Clinical pipelines WHO priority pathogens National Mega-Project for Innovative Drugs

Lignocellulose-Based Optical Biofilter with High Near-Infrared Transmittance via Lignin Capturing–Fusing Approach

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Research 2024年第3期2023卷 139-149页

作者： Shixu Yu Yifang Zhou Meixue Gan Lu Chen Yimin Xie Yuning Zhong Qinghua Feng Chaoji Chen Hubei Provincial Key laboratory of Green Materials for Light Industry Hubei University of TechnologyWuhan 430068China.Hubei Biomass-Resource Chemistry and Environmental Biotechnology Key LaboratorySchool of Resource and Environmental SciencesWuhan UniversityWuhan 430079China Hubei Biomass-Resource Chemistry and Environmental biotechnology Key laboratory School of Resource and Environmental SciencesWuhan UniversityWuhan 430079China Hubei Open University Wuhan 430074China.

Near-infrared (NIR) transparent optical filters show great promise in night vision and receiving windows. However, NIR optical filters are generally prepared by laborious, environmentally unfriendly processes that involve metal oxides or petroleum-based polymers. We propose a lignin capturing–fusing approach to manufacturing optical biofilters based on molecular collaboration between lignin and cellulose from waste agricultural biomass. In this process, lignin is captured via self-assembly in a cellulose network;then, the lignin is fused to fill gaps and hold the cellulose fibers tightly. The resulting optical biofilter featured a dense structure and smooth surface with NIR transmittance of ~90%, ultralow haze of close to 0%, strong ultraviolet-visible light blocking (~100% at 400 nm and 57.58% to 98.59% at 550 nm). Further, the optical biofilter has comprehensive stability, including water stability, solvent stability, thermal stability, and environmental stability. Because of its unique properties, the optical biofilter demonstrates potential applications in the NIR region, such as an NIR-transmitting window, NIR night vision, and privacy protection. These applications represent a promising route to produce NIR transparent optical filters starting from lignocellulose biomass waste.

关键词： transparent starting waste

Access to Axially Chiral Aryl Aldehydes via Carbene-Catalyzed Nitrile Formation and Desymmetrization Reaction

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Research 2024年第3期2024卷 715-721页

作者： Yuanlin Cai Ya Lv Liangzhen Shu Zhichao Jin Yonggui Robin Chi Tingting Li National Key laboratory of Green Pesticide Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationGuizhou UniversityGuiyang 550025China School of Chemistry Chemical Engineeringand BiotechnologyNanyang Technological UniversitySingapore 637371Singapore.

An approach utilizing N-heterocyclic carbene for nitrile formation and desymmetrization reaction is developed. The process involves kinetic resolution, with the axially chiral aryl monoaldehydes obtained in moderate yields with excellent optical purities. These axially chiral aryl monoaldehydes can be conveniently transformed into functionalized molecules, showing great potential as catalysts in organic chemistry.

关键词： chemistry. aldehydes chiral

OsPPG encodes a pseudouridine-5'-phosphate glycosidase and regulates rice spikelet development

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The Crop Journal 2024年第3期12卷 698-708页

作者： Rui Chen Dagang Tian Yarong Lin Jiaqing Huang Qinqin Yang Yupei Li Huaqing Liu Shaohua Yang Jingyang Chen Shufen Zhou Feng Wang Shubiao Zhang Key laboratory of Genetics Breeding and Multiple Utilization of CropsMinistry of Education/Key Laboratory of Biological Breeding for Fujian and Taiwan CropsMinistry of Agriculture and Rural AffairsFujian Agriculture and Forestry UniversityFuzhou 350002FujianChina Fujian Key laboratory of Genetic Engineering for Agriculture Biotechnology Research InstituteFujian Academy of Agricultural SciencesFuzhou 350003FujianChina Institute of resources Environment and Soil FertilizerFujian Academy of Agricultural SciencesFuzhou 350013FujianChina

Florets are the basic structural units of spikelets,and their morphogenesis determines the yield and quality of rice ***,whether and how pseudouridine-5’-phosphate glycosidase participates in rice spikelet development remains an open *** this study,we identified a novel gene,OsPPG,which encodes a peroxisome-localized pseudouridine-5’-phosphate glycosidase and regulates the development of rice *** mutants exhibited abnormal sterile lemma,lemma,palea,lodicule,stamens,and pistils;male sterility;shorter panicles;and reduced plant *** was found to regulate several OsMADS genes,thereby affecting the morphogenesis of rice ***,metabolomics revealed that the OsPPG gene was involved in the decomposition of pseudouridine via the pyrimidine metabolism pathway and may affect the jasmonic acid signaling *** results suggest that OsPPG is a key regulator of rice spikelet development.

关键词： OsPPG Reproductive regulation Spikelet development Rice

Overexpression of wild-type HRAS drives non-alcoholic steatohepatitis to hepatocellular carcinoma in mice

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Zoological Research 2024年第3期45卷 551-566页

作者： Chen Ling Su-Su Liu Yu-Ya Wang Gui-Tao Huo Yan-Wei Yang Nan Xu Hong Wang Yong Wu Yu-Fa Miao Rui Fu Yu-Wei Zhao Chang-Fa Fan College of Life Sciences Northwest UniversityProvincial Key Laboratory of Biotechnology of Shaanxi ProvinceXi’anShaanxi 710069China Division of Animal Model Research Institute for Laboratory Animal ResourcesNational Institutes for Food and Drug Control(NIFDC)Beijing 102629China National Center for Safety Evaluation of Drugs National Institutes for Food and Drug Control(NIFDC)Beijing 100176China Division of HIV/AIDS and Sexually Transmitted Virus Vaccines Institute for Biological Products ControlNational Institutes for Food and Drug Control(NIFDC)Beijing 102629China Division of laboratory Animal Monitoring Institute for Laboratory Animal ResourcesNational Institutes for Food and Drug Control(NIFDC)Beijing 102629China

Hepatocellular carcinoma(HCC),a prevalent solid carcinoma of significant concern,is an aggressive and often fatal disease with increasing global incidence rates and poor therapeutic *** etiology and pathological progression of non-alcoholic steatohepatitis(NASH)-related HCC is multifactorial and ***,no single animal model can accurately mimic the full NASH-related HCC pathological progression,posing considerable challenges to transition and mechanistic ***,a novel conditional inducible wild-type human HRAS overexpressed mouse model(HRAS-HCC)was established,demonstrating 100%morbidity and mortality within approximately one month under normal dietary and lifestyle *** symptoms of HCC such as ascites,thrombus,internal hemorrhage,jaundice,and lung metastasis were successfully replicated in ***-depth pathological features of NASH-related HCC were demonstrated by pathological staining,biochemical analyses,and typical marker gene *** murine anti-PD-1 and sorafenib treatment effectively prolonged mouse survival,further confirming the accuracy and reliability of the *** on protein-protein interaction(PPI)network and RNA sequencing analyses,we speculated that overexpression of HRAS may initiate the THBS1-COL4A3 axis to induce NASH with severe fibrosis,with subsequent progression to ***,our study successfully duplicated natural sequential progression in a single murine model over a very short period,providing an accurate and reliable preclinical tool for therapeutic evaluations targeting the NASH to HCC continuum.

关键词： HRAS THBS1 HCC driver factor NASH Fibrosis Cirrhosis HCC Treatment evaluation

Application of Polygonum minus Extract in Enhancing Drought Tolerance in Maize by Regulating Osmotic and Antioxidant System

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Phyton-International Journal of Experimental Botany 2024年第2期93卷 213-226页

作者： Mingzhao Han Susilawati Kasim Zhongming Yang Xi Deng Md Kamal Uddin Noor Baity Saidi Effyanti Mohd Shuib Department of Land Management Faculty of AgricultureUniversiti Putra MalaysiaSerdang43400Malaysia natural Medicines and Products Research laboratory Institute of BioscienceUniversiti Putra MalaysiaSerdang43400Malaysia Department of Cell and Molecular Biology Faculty of Biotechnology and Biomolecular SciencesUniversiti Putra MalaysiaSerdang43400Malaysia

Drought stress is a major factor affecting plant growth and crop yield *** extracts as natural biostimulants hold great potential to strengthen plants to overcome drought *** explore the effect of Polygonum minus extract(PME)in enhancing drought tolerance in plants,a study was set up in a glasshouse environment using 10 different treatment *** foliar application were designed in CRD and effects were closely observed related to the growth,physiology,and antioxidant system changes in maize(Zea mays L.)under well-watered and drought *** seaweed extract(SWE)was used as a *** subjected to drought stress exhibited a significant reduction in fresh weight,dry weight,relative water content(RWC),and soluble sugar,but they stimulated the phenolic,flavonoid,proline,glutathione(GSH),malondialdehyde(MDA)and antioxidant enzyme(catalase,CAT;peroxidase,POD;superoxide dismutase,SOD)*** application of PME improved fresh and dry weight(FW:33.1%~41.4%;DW:48.0%~43.1%),chlorophyll content(Chl b:87.9%~100.76%),soluble sugar(23.6%~49.3%),and soluble protein(48.6%~56.9%)as well as antioxidant enzyme activities(CAT and POD)compared to CK under drought *** decreasing the level of ***,the mitigating effect of PME application with high concentration was more effective than those of *** study reveals that PME could alleviate drought stress by regulating osmoprotectant content and antioxidant defense system and can be used as an economical and environmentally friendly biostimulants for promoting maize growth under drought stress.

关键词： Drought biostimulants photosynthesis osmoprotectants antioxidants maize