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Discovery of GluN2A subtype-selective N-methyl-d-aspartate(NMDA)receptor ligands

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Acta Pharmaceutica Sinica B 2024年第5期14卷 1987-2005页

作者： Liyang Jiang Na Liu Fabao Zhao Boshi Huang 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 UniversityJinan 250012China

The N-methyl-d-aspartate(NMDA)receptors,which belong to the ionotropic Glutamate receptors,constitute a family of ligand-gated ion *** the various subtypes of NMDA receptors,the GluN1/2A subtype plays a significant role in central nervous system(CNS)*** present article aims to provide a comprehensive review of ligands targeting GluN2A-containing NMDA receptors,encompassing negative allosteric modulators(NAMs),positive allosteric modulators(PAMs)and competitive ***,the ligands’structure–activity relationships(SARs)and the binding models of representative ligands are also discussed,providing valuable insights for the clinical rational design of effective drugs targeting CNS diseases.

关键词： NMDA receptors GluN2A subtype Subtype-selective ligands SARs Protein ligand interactions

1,6-Conjugate addition of para-quinone methides using gem-diborylcarbanions: Practical access to gem-diborylalkanes bearing vicinal tertiary/quaternary stereocenters

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Green Synthesis and Catalysis 2024年第1期5卷 68-72页

作者： Pu-Zhang Zi Xing-Bang Liu Quan-Hong Zhao Min He Yuan Huang department of medicinal Chemistry School of PharmacyXi'an Jiaotong UniversityXi'an710061China

A novel,efficient and pragmatic method to prepare gem-diboron products with vicinal tertiary/quaternary stereocenters using LiTMP-mediated 1,6-conjugate addition of gem-diborylalkanes to para-quinone methides was described for the first *** results showed that various gem-diboron products with vicinal tertiary and quaternary stereocenters could be formed within 15 min at ambient *** simple protocol has also been applied for the efficient synthesis of the analogue of Bedaquiline.

关键词： gem-Diborylalkanes Quaternary stereocenter Conjugate addition para-Quinone methides Organoboron compounds

MKK4 inhibitor:the hope for liver failure prevention and potential small liver graft transplantation

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Chinese Journal of Natural Medicines 2024年第6期22卷 483-485页

作者： ZHANG Yanqiu ZHANG Hao Jiangsu Key Laboratory of Bioactive Natural Product Research Department of Natural Medicinal ChemistryChina Pharmaceutical UniversityNanjing 210009China

Liver regeneration represents a fascinating concept that spans from ancient mythology to modern medical *** Greek mythology,Prometheus,a hero who defied Zeus by stealing fire and giving it to humanity,was subjected to a severe *** was bound to a rock where,each day,an eagle would feast on his liver,which would then miracu-lously regenerate *** myth underscores the liver’s unique regenerative abilities,a feature that is not just le-gendary but also scientifically recognized.

关键词： Liver regeneration Partial hepatectomy MKK4 Drug discovery and development First-in-human phase I trial

Drosophila X virus-like particles as delivery carriers for improved oral insecticidal efficacy of scorpion Androctonus australis peptide against the invasive fruit fly,Drosophila suzukii

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Insect Science 2024年第3期31卷 847-858页

作者： Qi Xue Luc Swevers Clauvis Nji Tizi Taning Faculty of Bioscience Engineering Department of Plants and CropsGhent UniversityGhentBelgium Insect Molecular Genetics and Biotechnology Institute of Biosciences and ApplicationsNational Centre for Scientific Research"Demokritos"AthensGreece

Insect-specific neurotoxic peptides derived from the venoms of scorpions and spiders can cause acute paralysis and death when injected into insects,offering a promising insecticidal component for insect pest ***,effective delivery systems are required to help neurotoxic peptides pass through the gut barrier into the hemolymph,where they can ***,we investigated the potential of a novel nanocarrier,Drosophila X virus-like particle(DXV-VLP),for delivering a neurotoxin from the scorpion Androctonus australis Hector(AaIT)against the invasive pest fruit fly,Drosophila *** results show that the fusion proteins of DXV polyproteins with AalT peptide at their Ctermini could be sufficiently produced in Lepidoptera Hi5 cells in a soluble form using the recombinant baculovirus expression system,and could self-assemble into VLPs with similar particle morphology and size to authentic DXV *** addition,the AalT peptides displayed on DXV-VLPs retained their toxicity,as demonstrated in injection bioassays that resulted in severe mortality(72%)in adults after 72 *** fed to adults,mild mortality was observed in the group treated with DXV-AalT(38%),while no mortality occurred in the group treated with AaIT peptide,thus indicating the significant role of DXV-VLPs in delivering AalT ***,this proof-of-concept study demonstrates for the first time that VLPs can be exploited to enhance oral delivery of insect-specific neurotoxic peptides in the context of pest ***,it provides insights for further improvements and potentially the development of neurotoxin-based bioinsecticides and/or transgenic crops for insect pest control.

关键词： AalT Drosophila suzuki nanocarrier neurotoxic peptides pest control virus-like particle(VLP)

Contemporary strategies and approaches for characterizing composition and enhancing biofilm penetration targeting bacterial extracellular polymeric substances

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Journal of Pharmaceutical Analysis 2024年第4期14卷 506-524页

作者： Lan Lu Yuting Zhao Mingxing Li Xiaobo Wang Jie Zhu Li Liao Jingya Wang Key Laboratory of medicinal and Edible Plants Resources Development of Sichuan Education department Sichuan Industrial Institute of AntibioticsSchool of PharmacyChengdu UniversityChengdu610000China Meishan Pharmaceutical Vocational College School of PharmacyMeishanSichuan620200China Laboratory of Molecular Pharmacology Department of PharmacologySchool of PharmacySouthwest Medical UniversityLuzhouSichuan646000China Hepatobiliary Surgery Langzhong People's HospitalLangzhongSichuan646000China

Extracellular polymeric substances(EPS)constitutes crucial elements within bacterial biofilms,facili-tating accelerated antimicrobial resistance and conferring defense against the host's immune *** precise and effective antibiofilm approaches and strategies,tailored to the specific charac-teristics of EPS composition,can offer valuable insights for the creation of novel antimicrobial ***,in turn,holds the potential to mitigate the alarming issue of bacterial drug *** analysis of EPS compositions relies heavily on colorimetric approaches with a significant bias,which is likely due to the selection of a standard compound and the cross-interference of various EPS *** the pivotal role of EPS in biofilm functionality,it is imperative for EPS research to delve deeper into the analysis of intricate compositions,moving beyond the current focus on polymeric *** ne-cessitates a shift from heavy reliance on colorimetric analytic methods to more comprehensive and nuanced analytical *** this study,we have provided a comprehensive summary of existing analytical methods utilized in the characterization of EPS ***,novel strategies aimed at targeting EPS to enhance biofilm penetration were explored,with a specific focus on high-lighting the limitations associated with colorimetric ***,we have outlined the challenges faced in identifying additional components of EPS and propose a prospective research plan to address these *** review has the potential to guide future researchers in the search for novel compounds capable of suppressing EPS,thereby inhibiting biofilm *** insight opens up a new avenue for exploration within this research domain.

关键词： Analytic strategies and approaches Composition characterization Extracellular polymeric substances(EPS) Promoting biofilm penetration

CsRAXs negatively regulate leaf size and fruiting ability through auxin glycosylation in cucumber

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Journal of Integrative Plant Biology 2024年第5期66卷 1024-1037页

作者： Jiacai Chen Liu Liu Guangxin Chen Shaoyun Wang Ye Liu Zeqin Zhang Hongfei Li Liming Wang Zhaoyang Zhou Jianyu Zhao Xiaolan Zhang Beijing Key Laboratory of Growth and Developmental Regulation for Protected Vegetable crops Department of Vegetable SciencesBeijing key Laboratoy of Growtn and Developmental Regul China Agricultural UniversityBeijing 100193China

Leaves are the main photosynthesis organ that directly determines crop yield and *** the regulatory mechanism of leaf development is crucial for food security and ecosystem ***,we identified the novel function of R2R3-MYB transcription factors CsRAXs in regulating cucumber leaf size and fruiting ***5 single mutant exhibited enlarged leaf size and stem diameter,and Csrax1/2/5 triple mutant displayed further enlargement *** of CsRAX1 or CsRAX5 gave rise to smaller leaf and thinner *** fruiting ability of Csrax1/2/5 plants was significantly enhanced,while that of CsRAX5 overexpression lines was greatly ***,cell number and free auxin level were elevated in mutant plants while decreased in overexpression *** data indicated that CsRAX1/5 directly promoted the expression of auxin glucosyltransferase gene ***,our data suggested that CsRAXs function as repressors for leaf size development by promoting auxin glycosylation to decrease free auxin level and cell division in *** findings provide new gene targets for cucumber breeding with increased leaf size and crop yield.

关键词： auxin glycosylation CsRAXs CsUGT74E2 fruiting ability leaf size

A new tetracyclic triterpenoid from endophytic fungus Fusarium sporotrichioides

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Chinese Herbal Medicines 2024年第2期16卷 231-234页

作者： Yajing Wang Chunyue Liu Yihui Yang Chang Li Yuehu Pei department of medicinal Chemistry and Natural Medicine Chemistry College of PharmacyHarbin Medical UniversityHarbin 150081China

Objective: To isolate bioactive compounds from the endophytic fungus Fusarium sporotrichioides isolated from Rauwolfia yunnanensis, and investigate their pharmacological ***: The chemical constituents were isolated and purified by combining with ODS column chromatography, silica gel column chromatography and by performing semipreparative HPLC. Their structures were established on the basis of 1D NMR(1H-NMR and13C-NMR) and 2D NMR(1H–1H COSY,HSQC, HMBC and NOESY), as well as HRESIMS and comparison with literature data. In addition, the absolute configuration of compound 1 was determined by calculated ECD ***: One previously undescribed tetracyclic triterpenoid derivative, named as integracide L(1), 12aacetoxy-4,4-dimethyl-24-methylene-5a-cholesta-8,14-diene-2a,3β,11β-triol(2), 12a-acetoxy-4,4-dime thyl-24-methylene-5a-cholesta-8-momoene-2a,3β,11β-triol(3), 12a-acetoxy-4,4-dimethyl-24-methy lene-5a-cholesta-8,14-diene-3β,11β-triol(4), and 12a-acetoxy-4,4-dimethyl-24-methylene-5acholesta-8-momoene-3β,11β-triol(5) were isolated from F. sporotrichioide. Moreover, compound 1 was rare tetracyclic triterpenoid with single methyl replacement at C-4 ***: Compound 1 was a new tetracyclic triterpenoid isolated from the endophytic fungus ***. In addition, compound 2 could inhibit the growth of three different human cancer cells significantly. Compounds 3 and 5 were found to possess better cytotoxic activities on Hep G-2 cells than the other compounds, with IC50values of(2.8 ± 0.1) and(6.3 ± 0.3) μmol/L respectively.

关键词： antitumor Fusarium sporotrichioides integracide L tetracyclic triterpenoid 12a-acetoxy-4,4-dimethyl-24-methylene5a-cholesta-814-diene-2a,3b,11b-triol 12a-acetoxy-4,4-dimethyl-24-methylene5a-cholesta-8-momoene-2a,3b,11b-triol 12a-acetoxy-4,4-dimethyl-24-methylene5a-cholesta-8-momoene-3b,11b-triol

Targeted mutations of BnPAP2 lead to a yellow seed coat in Brassica napus L.

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Journal of Integrative Agriculture 2024年第2期23卷 724-730页

作者： Wei Huang Ruyu Jiao Hongtao Cheng Shengli Cai Jia Liu Qiong Hu Lili Liu Bao Li Tonghua Wang Mei Li Dawei Zhang Mingli Yan Hunan Research Center of Heterosis Utilization in Rapeseed/Crop Research Institute Hunan Academy of Agricultural SciencesChangsha 410125China Hunan Key Laboratory of Economic crops Genetic Improvement and Integrated Utilization/School of Life and Health Science Hunan University of Science and TechnologyXiangtan 411201China Key Laboratory of Biology and Genetic Improvement of Oil crops Ministry of Agriculture and Rural Affairs/Oil Crops Research InstituteChinese Academy of Agricultural SciencesWuhan 430062China

The yellow seed trait is preferred by breeders for its potential to improve the seed quality and commercial value of Brassica *** the present study,we produced yellow seed mutants using a CRISPR/Cas9 system when the two BnPAP2 homologs were knocked *** staining of the seed coat demonstrated that proanthocyanidin accumulation was significantly reduced in the pap2 double mutants and decreased specifically in the endothelial and palisade layer cells of the seed *** and metabolite profiling analysis suggested that disruption of the BnPAP2 genes could reduce the expression of structural and regulated genes in the phenylpropanoid and flavonoid biosynthetic *** broad suppression of these genes might hinder proanthocyanidin accumulation during seed development,and thereby causing the yellow seed trait in *** results indicate that BnPAP2 might play a vital role in the regulatory network controlling proanthocyanidin accumulation.

关键词： yellow seed BnPAP2 proanthocyanidins CRISPR/Cas9

Enhancing Canola Yield and Photosynthesis under Water Stress with Hydrogel Polymers

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Phyton-International Journal of Experimental Botany 2024年第7期93卷 1623-1645页

作者： Elham A.Badr Gehan Sh.Bakhoum Mervat Sh.Sadak Ibrahim Al-Ashkar Mohammad Sohidul Islam Ayman El Sabagh Magdi T.Abdelhamid Field crops Research department National Research CentreCairo12622Egypt Botany department National Research CentreCairo12622Egypt Plant Production department College of Food and Agriculture SciencesKing Saud UniversityRiyadh12271Saudi Arabia department of Agronomy Hajee Mohammad Danesh Science and Technology UniversityDinajpur5200Bangladesh department of Field crops Faculty of AgricultureSiirt UniversitySiirt56100Turkey department of Agronomy Faculty of AgricultureKafrelsheikh UniversityKafrelsheikh33516Egypt department of Research Centers Montana State UniversityBozemanMT 59717USA

While Egypt’s canola production per unit area has recently grown,productivity remains low,necessitating increased *** are water-absorbent polymer compounds that can optimize irrigation schedules by increasing the soil’s ability to retain ***,twoﬁeld experiments were conducted to examine hydrogel application to sandy soil on canola growth,biochemical aspects,yield,yield traits,and nutritional quality of yielded seeds grown under water deﬁcit stress *** experiments were conducted by arranging a split-plot layout in a randomized complete block design(RCBD)with three times replications of each *** water stress at 75%or 50%of crop evapotranspiration(ETc)lowered chlorophyll a,chlorophyll b,caro-tenoids,and total pigments content,indole-3-acetic acid,plant development,seed yield,and oil and total carbo-hydrates of seed yield,hydrogel treatment enhanced all of the traits mentioned ***,hydrogel enhanced to gather compatible solutes(proline,amino acids,total soluble sugars),phenolics content in leaves,seed protein,and crop water productivity,which increased while the plants were under water *** results revealed that the full irrigation(100%ETc)along with hydrogel compared to water-stressed(50%ETc)led to enhanced seed yield(kg ha^(-1)),Oil(%),and Total carbohydrates(%)of rapeseed by 57.1%,11.1%and 15.7%,***,under water-stressed plots with hydrogel exhibited enhancement by 10.0%,3.2%and 5.1%in seed yield(kg ha^(-1)),oil(%),and total carbohydrates(%)of rapeseed by 57.1%,11.1%and 15.7%,respec-tively compared to *** a result,the use of hydrogel polymer will be a viable and practical solution for increasing agricultural output under water deﬁcit stress situations.

关键词： Hydrogel oil osmolytes rapeseed yield water stress