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Journal of Chinese Pharmaceutical Sciences 2019年第12期28卷 878-884页

作者： Shuxiang Song state key laboratory of natural and biomimetic drugs School of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China

The state key laboratory of natural and biomimetic drugs was approved for a funding of nearly 100 million yuan specifically aimed at the purchase and maintenance of equipment and instruments from 2018 to 2020,which is a record *** laboratory focuses on two major directions of scientific research,the"basic scientific problems of drug resistance of complex components of natural products"and the"key biomimetic scientific problems of endogenous substances therapeutic functions".The selection of scientific instruments and equipment,trial production,upgrading,as well as high level of technical and management personnel allocation and other aspects are critical to meet the development needs of the key laboratory and to maintain the advantages and leading role in these two major directions of scientific research.

关键词： Instrument platform construction Optimization of resource allocation Scientific research service

Bifunctional organocatalyst-catalyzed dynamic kinetic resolution of hemiketals for synthesis of chiral ketals via hydrogen bonding control

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Chinese Chemical Letters 2025年第1期36卷 248-252页

作者： Meng Shan Yongmei Yu Mengli Sun Shuping Yang Mengqi Wang Bo Zhu Junbiao Chang state key laboratory of Antiviral drugs Pingyuan LaboratoryNMPA Key Laboratory for Research and Evaluation of Innovative DrugSchool of Chemistry and Chemical EngineeringHenan Normal UniversityXinxiang 453007China

Herein,we report the dynamic kinetic resolution asymmetric acylation ofγ-hydroxy-γ-perfluoroalkyl butenolides/phthalides catalyzed by amino acid-derived bifunctional organocatalysts,and a series of ketals were obtained in high yields(up to 95%)and excellent enantioselectivities(up to 99%).In terms of synthetic utility,the reaction can be performed on a gram scale,and the product can be converted into potential biological nucleoside analog.

关键词： Bifunctional organocatalyst Dynamic kinetic resolution Hemiketal Chiral ketals Hydrogen bonding

Recent advances,strategies,and future perspectives of peptide-based drugs in clinical applications

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Chinese Journal of natural Medicines 2025年第1期23卷 31-42页

作者： Qimeng Yang Zhipeng Hu Hongyu Jiang Jialing Wang Han Han Wei Shi Hai Qian Centre of Drug Discovery State Key Laboratory of Natural Medicines China Pharmaceutical University Jiangsu key laboratory of Drug Discovery for Metabolic Disease China Pharmaceutical University

Peptide-based therapies have attracted considerable interest in the treatment of cancer, diabetes, bacterial infections, and neurodegenerative diseases due to their promising therapeutic properties and enhanced safety profiles. This review provides a comprehensive overview of the major trends in peptide drug discovery and development, emphasizing preclinical strategies aimed at improving peptide stability, specificity, and pharmacokinetic properties. It assesses the current applications and challenges of peptide-based drugs in these diseases, illustrating the pharmaceutical areas where peptide-based drugs demonstrate significant potential. Furthermore, this review analyzes the obstacles that must be overcome in the future,aiming to provide valuable insights and references for the continued advancement of peptidebased drugs.

关键词： Antimicrobial peptides Diabetes Neurodegenerative diseases Oncology Peptide-based drugs

Total synthesis of(+)-taberdicatine B and(+)-tabernabovine B

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Chinese Chemical Letters 2025年第2期36卷 349-353页

作者： Tengfei Xuan Xinyu Zhang Wei Han Yidong Huang Weiwu Ren Molecular Synthesis Center&key laboratory of Marine drugs Chinese Ministry of EducationSchool of Medicine and PharmacyOcean University of China laboratory for Marine drugs and Bioproducts Laoshan Laboratory

The first total synthesis of(+)-taberdicatine B and(+)-tabernabovine B has been accomplished in 10steps with 26.9% overall yield and 15 steps with 7.3% overall yield, respectively. The prominent features of this efficient synthetic strategy include the following:(1)(+)-Taberdicatine B and(+)-tabernabovine B were accessed from common advanced intermediates by varying the substituents;(2) A one-pot asymmetric bromocyclization/hydrolysis was explored to assemble HPI skeleton;(3) Dieckmann condensation to form β-keto ester for the assembly of seven-membered ring;(4) An ester reduction/amide semireduction/cyclization sequence was applied to form the cage-like framework.

关键词： Asymmetric dearomatization Hexahydropyrrolo[2,3-b]indole Taberdicatine B Tabernabovine B Total synthesis

A comprehensive review on wedelolactone: natural sources, total synthesis, and pharmacological activities

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Chinese Journal of natural Medicines 2025年第02期23卷 169-181页

作者： Haiping Cai Yue Wu Xiaojin Zhang state key laboratory of natural Medicines Jiangsu Key Laboratory of Drug Design and Optimization and Department of Chemistry China Pharmaceutical University

Plant-derived natural products have long been a vital source for developing therapeutic drugs. Wedelolactone(WDL), a coumestan isolated from Eclipta prostrata, Wedelia calendulacea, Wedelia chinensis, and Sphagneticola trilobata, demonstrates a broad spectrum of therapeutic potential, including anticancer, anti-inflammatory, anti-obesity, anti-myotoxic,antimicrobial, anti-diabetic, and tissue-protective activities. This review synthesizes information on the isolation, total synthesis, pharmacological activity, underlying mechanisms, and pharmacokinetic properties of WDL. Additionally, it offers insights into potential clinical applications and future drug discovery avenues utilizing WDL or its derivatives, either independently or in combination with other pharmaceuticals.

关键词： Mechanism natural product Pharmacological activity Synthesis Wedelolactone

Synthesis of ordered mesoporous crystalline boron phosphate scaffold with double diamond surface structure

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Science China Chemistry 2025年第2期68卷 590-600页

作者： Chao Wang Wen-Duo Lu Jiao Wang Shunai Che An-Hui Lu Lu Han School of Chemical Science and Engineering Tongji UniversityShanghai 200092China state key laboratory of Fine Chemicals Liaoning Key Laboratory for Catalytic Conversion of Carbon ResourcesSchool of Chemical EngineeringDalian University of TechnologyDalian 116024China School of Chemistry and Chemical Engineering Frontiers Science Center for Transformative MoleculesState Key Laboratory of Metal Matrix CompositesShanghai Key Laboratory for Molecular Engineering of Chiral DrugsShanghai Jiao Tong UniversityShanghai 200240China

Ordered mesoporous materials have received great attention due to their well-defined pore structures and potential applications in catalysis,adsorption,separation,drug delivery,*** various compositions of mesoporous solids have been successfully prepared,the preparation of crystalline non-metallic oxyacid salts with ordered mesoporosity remains a major ***,we report the synthesis of a mesoporous solid acid crystalline boron phosphate(BPO_(4))catalyst with a bicontinuous shifted double diamond(SDD)hyperbolic surface *** BPO_(4) scaffold was obtained by synergistic selfassembly in a mixed solvent of water and tetrahydrofuran using the diblock copolymer poly(ethylene oxide)-block-polystyrene as template and phosphoric acid and orthoboric acid as inorganic *** structure consists of two sets of diamond networks adjacent to each other with a mesostructural scale tetragonal symmetry(space group I4_(1)/amd)with unit cell parameters of a=80 nm and c=113 nm,which affords the scaffold a specific surface area of 44 m^(2)/*** a solid acid catalytic material,the SDD BPO_(4) scaffold exhibited excellent catalytic activity at room temperature with a conversion of furfural to 2-(dimethoxymethyl)furan over 70%and can be reused after recovery without serious loss of *** the propane oxidative dehydrogenation reaction,SDD BPO_(4) demonstrated high olefin productivity and selectivity while maintaining high reaction *** study provides ideas for the preparation of ordered mesoporous crystalline catalytic materials and demonstrates their potential for practical applications.

关键词： boron phosphate mesoporous material self-assembly block copolymer catalyst

Protein nanoparticles as potent delivery vehicles for polycytosine RNA-binding protein one

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World Journal of Diabetes 2025年第1期16卷 222-225页

作者： Zi-Yu Zhao Pei-Li Luo Xia Guo Zheng-Wei Huang state key laboratory of Bioactive Molecules and Druggability Assessment Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative DrugsCollege of PharmacyJinan UniversityGuangzhou 511436Guangdong ProvinceChina

Ma et al recently reported in the World Journal of Diabetes that ferroptosis occurs in osteoblasts under high glucose conditions,reflecting diabetes *** condition could be protected by the upregulation of the gene encoding polycytosine RNA-binding protein 1(PCBP1).Additionally,Ma et al used a lentivirus infection system to express *** the authors’method of administration can be improved in terms of stability and cost,we propose delivering PCBP1 to treat type 2 diabetic osteoporosis by encapsulating it in protein ***,PCBP1 is small and ***,intravenous injection can help deliver PCBP1 across the mucosa while avoiding acid and enzyme-catalyzed ***,incorporating PCBP1 into nanoparticles prevents its interaction with water or oxygen and protects PCBP1’s structure and ***,the safety of the protein materials and the industrialization techniques for large-scale production of protein nanoparticles must be comprehensively investigated before clinical application.

关键词： Polycytosine RNA-binding protein 1 Protein nanoparticle Osteoblast Ferroptosis Diabetes

Cobalamin-dependent radical S-adenosyl-L-methionine protein functions with a partner to successively methylate tricyclic indole alkaloid for chuangxinmycin maturation and derivatization

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Science China Chemistry 2025年第1期68卷 308-316页

作者： Sili Wang Jiancheng Huang Yanan Du Wei Huang Yufeng Xue Xiaokun Xu Guannan Zhong Yuanyuan Shi Bin Hong Xiaoying Bian Wen Liu state key laboratory of Chemical Biology Shanghai Institute of Organic ChemistryUniversity of Chinese Academy of SciencesChinese Academy of SciencesShanghai 200032China state key laboratory of Microbial Technology Shandong UniversityQingdao 266237China National Health Commission(NHC)key laboratory of Biotechnology for Microbial drugs Institute of Medicinal BiotechnologyChinese Academy of Medical Science&Peking Union Medical CollegeBeijing 100050China

Cobalamin(Cbl)-dependent radical S-adenosyl-L-methionine(SAM)proteins constitute the largest collection of the radical SAM superfamily that has hundreds of thousands of individual *** of these proteins are involved in the biosynthesis of pharmaceutically important natural products to catalyze chemically demanding *** the biosynthetic pathway of chuangxinmycin(CXM),a unique indole alkaloid antibiotic with potent anti-infective activity,functionalization of the characteristic thiopyrano[4,3,2-cd]indole scaffold by regio-and stereoselective C3-methylation is believed to rely on a Cbl-dependent radical process,which,however,remained to be reconstituted *** here report the dissection of this enzymatic process,which requires the incorporation of Cxm8,a Cbl-dependent radical SAM protein,with Cxm9,a DUF5825family protein that shares no homology to any proteins of known ***8 and Cxm9 function together by forming an unexpected heterodimeric complex that selectively catalyzes C3-methylation of the tricyclic indole-S-hetero ring system in a successive manner,achieving CXM and a recently identified,C3-dimethylated *** biochemical characterization,isotope labeling,structural simulation and bioinformatics analysis rationalized the catalysis of the Cxm8/Cxm9 complex and particularly the necessity of the DUF5825 protein for C3-methylase *** is the first example that a Cbl-dependent protein acts with a partner to exhibit radical SAM activity.

关键词： cbl-dependent radical SAM protein biosynthesis chuangxinmycin stereoselective methylation

I_(2)-DMSO mediated tetra-functionalization of enaminones for the construction of novel furo[2,3:4,5]pyrimido[1,2-b]indazole skeletons via in situ capture of ketenimine cations

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Chinese Chemical Letters 2025年第1期36卷 277-282页

作者： You Zhou Li-Sheng Wang Shuang-Gui Lei Bo-Cheng Tang Zhi-Cheng Yu Xing Li Yan-Dong Wu Kai-Lu Zheng An-Xin Wu National key laboratory of Green Pesticide International Joint Research Center for Intelligent Biosensor Technology and HealthCollege of ChemistryCentral China Normal UniversityWuhan 430079China Guangdong Provincial key laboratory of Research and Development of natural drugs The First Dongguan Affiliated HospitalSchool of PharmacyGuangdong Medical UniversityDongguan 523808China state key laboratory of Chemical Biology and Drug Discovery Department of Applied Biology and Chemical TechnologyThe Hong Kong Polytechnic UniversityHong Kong SAR 999077China

The first-ever synthesis of the unknown furo[2,3:4,5]pyrimido[1,2-b]indazole skeleton was demonstrated based on the undiscovered tetra-functionalization of enaminones,with simple substrates and reaction *** key to realizing this process lies in the multiple trapping of the in situ generated ketenimine cation by the 3-aminoindazole,which results in the formation of four new chemical bonds and two new rings in one ***,the products of this new reaction were found to exhibit aggregationinduced emission(AIE)without modification.

关键词： Unknown skeleton Tetra-functionalization Ketenimine cations Aggregation-induced emission

Single-cell multi-omics analysis revealing immune features of inactivated COVID-19 vaccination in systemic lupus erythematosus patients

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Science Bulletin 2025年第1期70卷 42-46页

作者： Yuxuan Zheng Siyuan Wang Xingyu Zhou Shitong Qiao Xin Zhao Yuan Chen Zijun Li Zhanguo Li Xiaolin Sun Shuguang Tan Jing He George Fu Gao CAS key laboratory of Pathogen Microbiology and Immunology Institute of MicrobiologyChinese Academy of Sciences(CAS)Beijing 100101China Department of Rheumatology and Immunology Peking University People’s HospitalBeijing Key Laboratory for Rheumatism and Immune Diagnosis(BZ0135)Beijing 100044China Medical School University of Chinese Academy of SciencesBeijing 100049China state key laboratory of natural and biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100871China

Studies have focused on neutralizing antibody titers and T-cell activation induced by vaccination against different SARS-CoV-2strains[1,2].Advanced single-cell technology has allowed for a comprehensive evaluation of immune responses to diverse vaccines,revealing potential antiviral mechanisms[3-5].Patients with rheumatic diseases(RDs)experience dysregulated cellular and humoral immune responses that affect their disease susceptibility,including COVID-19[6].

关键词： vaccination revealing titer