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Chinese Journal of chemistry 2024年第6期42卷 605-610页

作者： Xiuhe Zhao Mengxue Lv Xiaonan Xi Yaxin Lu Liang Wang Yue Chen The State Key Laboratory of Medicinal Chemical Biology College of PharmacyNankai UniversityTianjin300350 China college of chemistry Nankai UniversityTianjin300071 China

The total synthesis of majusculamide D(1)was achieved from commercially available materials.In addition,we synthesized eight analogues including three stereoisomers of majusculamide D that differ in the fatty acid chain.Six analogues including a simplified analogue 29 exhibited significant nanomolar-level IC50 values against Panc-1 cells in MTT assays.A preliminary SAR analysis indicated that the hydroxyl group at C10 and C2−C3 unsaturated double bond of majusculamide D were essential in maintaining the high activity against Panc-1 cells and the orientation of C40-Me and C42-Me groups was tolerable.

关键词： Majusculamide D Natural products SAR Anti-pancreatic cancer Lipopentapeptide

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 activities.Methods: 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 data.Results: 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 position.Conclusion: Compound 1 was a new tetracyclic triterpenoid isolated from the endophytic fungus F.sporotrichioides. 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

Progress in experimental models to investigate the in vivo and in vitro antidiabetic activity of drugs

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Animal Models and Experimental Medicine 2024年第3期7卷 297-309页

作者： Yasodha Krishna Janapati Sunil Junapudi School of pharmacy&Health Sciences United States International University-AFRICA(USIU-A)NairobiKenya Department of Pharmaceutical chemistry Geethanjali College of PharmacyKeesaraIndia

Diabetes mellitus is one of the world's most prevalent and complex metabolic disorders,and it is a rapidly growing global public health issue.It is characterized by hyperglycemia,a condition involving a high blood glucose level brought on by deficiencies in insulin secretion,decreased activity of insulin,or both.Prolonged effects of diabetes include cardiovascular problems,retinopathy,neuropathy,nephropathy,and vascular alterations in both macro-and micro-blood vessels.In vivo and in vitro models have always been important for investigating and characterizing disease pathogenesis,identifying targets,and reviewing novel treatment options and medications.Fully understanding these models is crucial for the researchers so this review summarizes the different experimental in vivo and in vitro model options used to study diabetes and its consequences.The most popular in vivo studies involves the small animal models,such as rodent models,chemically induced diabetogens like streptozotocin and alloxan,and the possibility of deleting or overexpressing a specific gene by knockout and transgenic technologies on these animals.Other models include virally induced models,diet/nutrition induced diabetic animals,surgically induced models or pancreatectomy models,and non-obese models.Large animals or non-rodent models like porcine(pig),canine(dog),nonhuman primate,and Zebrafish models are also outlined.The in vitro models discussed are murine and human beta-cell lines and pancreatic islets,human stem cells,and organoid cultures.The other enzymatic in vitro tests to assess diabetes include assay of amylase inhibition and inhibition ofα-glucosidase activity.

关键词： animal models diabetes mellitus typeⅠ diabetes mellitus typeⅡ in vitro and in vivo models

Multi-stimuli-responsive aggregation-induced emission copper iodide cluster

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Science China chemistry 2024年第4期67卷 1193-1197页

作者： Bo Li Yuan-Yuan Liu Peng Luo Ye-Ru Liu Ying-Jun Chen Kai Li Shuang-Quan Zang college of chemistry and pharmacy Engineering Nanyang Normal UniversityNanyang 473061China Green Catalysis Center and college of chemistry Zhengzhou UniversityZhengzhou 450001China

Stimuli-responsive luminescent materials have attracted significant attention in the development of smart photoactive materials for both fundamental research and technological applications.In this work,a new copper iodide cluster(1)with aggregationinduced emission(AIE)characteristic,was obtained combining Cu_(4)I_(4) core with rhodamine B derivative ligand.1 has reversible and distinct multi-stimuli-responsive luminescence for external temperature,volatile organic compound,and mechanical force.Significantly,1 exhibited unusual large blue shift(84 nm)after being ground,which originated from the change of intermolecular interactions.Moreover,1 exhibits high oxygen quenching efficiency for 82.2% at 1 bar.Mechanistic studies showed that the multi-stimuli-responsive luminescence properties of 1 can be attributed to the regulation of cluster-centered luminescence process,metal-to-ligand charge transfer process,halide-to-metal charge transfer luminescence process and aggregationinduced barrier to oxygen process.This work not only reports an AIE copper iodide cluster,but also provides a new strategy to develop multi-stimuli-responsive luminescence materials.

关键词： copper iodide cluster aggregation-induced emission multi-stimuli-response

A network pharmacology study of Sendeng-4,a Mongolian medicine

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Chinese Journal of Natural Medicines 2015年第2期13卷 108-118页

作者： ZI Tian YU Dong Department of Natural Medicinal chemistry College of Pharmacy Inner Mongolia Medical University

We collected the data on the Sendeng-4 chemical composition corresponding targets through the literature and from Drug Bank, SuperT arget, TTD(Therapeutic Targets Database) and other databases and the relevant signaling pathways from the KEGG(Kyoto Encyclopedia of Genes and Genomes) database and established models of the chemical composition-target network and chemical composition-target- disease network using Cytoscape software, the analysis indicated that the chemical composition had at least nine different types of targets that acted together to exert effects on the diseases, suggesting a "multi-component, multi-target" feature of the traditional Mongolian medicine. We also employed the rat model of rheumatoid arthritis induced by Collgen Type II to validate the key targets of the chemical components of Sendeng-4, and three of the key targets were validated through laboratory experiments, further confirming the anti-inflammatory effects of Sendeng-4. In all, this study predicted the active ingredients and targets of Sendeng-4, and explored its mechanism of action, which provided new strategies and methods for further research and development of Sendeng-4 and other traditional Mongolian medicines as well.

关键词： Network pharmacology Mongolian medicine Sendeng-4 Drug targeting Disease pathway networks Rheumatoid arthritis In vivo evaluation

Olfactory dysfunction and its related molecular mechanisms in Parkinson’s disease

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Neural Regeneration Research 2024年第3期19卷 583-590页

作者： Yingying Gu Jiaying Zhang Xinru Zhao Wenyuan Nie Xiaole Xu Mingxuan Liu Xiaoling Zhang college of pharmacy Nantong UniversityNantongJiangsu ProvinceChina

Changes in olfactory function are considered to be early biomarkers of Parkinson’s disease.Olfactory dysfunction is one of the earliest non-motor features of Parkinson’s disease,appearing in about 90%of patients with early-stage Parkinson’s disease,and can often predate the diagnosis by years.Therefore,olfactory dysfunction should be considered a reliable marker of the disease.However,the mechanisms responsible for olfactory dysfunction are currently unknown.In this article,we clearly explain the pathology and medical definition of olfactory function as a biomarker for early-stage Parkinson’s disease.On the basis of the findings of clinical olfactory function tests and animal model experiments as well as neurotransmitter expression levels,we further characterize the relationship between olfactory dysfunction and neurodegenerative diseases as well as the molecular mechanisms underlying olfactory dysfunction in the pathology of early-stage Parkinson’s disease.The findings highlighted in this review suggest that olfactory dysfunction is an important biomarker for preclinical-stage Parkinson’s disease.Therefore,therapeutic drugs targeting non-motor symptoms such as olfactory dysfunction in the early stage of Parkinson’s disease may prevent or delay dopaminergic neurodegeneration and reduce motor symptoms,highlighting the potential of identifying effective targets for treating Parkinson’s disease by inhibiting the deterioration of olfactory dysfunction.

关键词： biomarker early-stage olfactory disorders olfactory dysfunction Parkinson’s disease

Development of lithium-free P2-type high-sodium content cathode materials with enhanced cycle and air stability for sodium-ion batteries

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Rare Metals 2024年第1期43卷 113-123页

作者： Jin-Lv Tian Lin-Rong Wu Hai-Jun Zhao Shou-Dong Xu Liang Chen Ding Zhang Xiao-Chuan Duan college of Chemical Engineering and Technology Taiyuan University of TechnologyTaiyuan 030024China college of chemistry Taiyuan University of TechnologyTaiyuan 030024China School of Chemical Engineering and pharmacy Wuhan Institute of TechnologyWuhan 430205China

The effect of partial substitution of Mg for Ni on a high-sodium and lithium-free layered P2-type Na_(45/54)Mg_(6)/_(54)Ni_(12/54)Mn_(34/54)O_(2) cathode with high initial Coulombic efficiency and excellent cyclic stability has been investigated in this study.Based on the crystal structural analysis,the Mg doping can retain the P2 structure up to 4.3 V,thus restraining the detrimental phase transformation of P2-02during the Na-ion intercalation/deintercalation process.Therefore,the obtained Mg-doped P2-type cathode exhibits a reversible specific capacity of 109 mAh·g^(-1) at 0.1C between 2.0 and 4.3 V and a retention rate of 81.5% after 200cycles at 1C.In addition,the full cell consisting of Mg-doped P2-type cathode and hard carbon anode shows a capacity retention rate of 85.6% after 100 cycles.This study provides new insight into the development of durable cathode materials for sodium-ion batteries.

关键词： Sodium-ion batteries Cathode material High sodium content Air stability

FeNi Prussian blue analogues on highly graphitized carbon nanosheets as efficient glucose sensors

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Rare Metals 2024年第6期43卷 2730-2738页

作者： Jin-Hang Xue Qiu-Hong Sun Cheng Han Yuan-Dong Yang Shao-Jie Xu Qi-Peng Li Jin-Jie Qian college of Life and Environmental Science Wenzhou University college of chemistry and Materials Engineering Wenzhou University college of chemistry and Chemical Engineering Zhaotong University

Meeting the continuous glucose monitoring requirements of individuals necessitates the research and development of sensors with high sensitivity and stability.In this study,a straightforward strategy was proposed for synthesizing ultra-thin oxygen-rich graphitized carbon nanosheets（denoted as GCS-O）.These nanosheets are obtained by calcining a topologically two-dimensional indium-based coordination polymer.Subsequently,the growth of FeNi Prussian blue analogue（PBA） on GCS-O effectively introduces active sites and increases the nitrogen content within the carbonaceous matrix.The resulting FeNi-PBA/GCS-O composite exhibits excellent glucose sensing performance with a broad linear range of 1 to 1300μmol·L-1.Meanwhile,it also achieves a high sensitivity of 2496 μA·mmol-1·L·cm-2,a limit of detection of 100nmol·L-1（S/N=3）,and commendable long-term durability.The relatively simple synthesis process,exceptional sensitivity,and satisfactory electrochemical sensing performance of FeNi-PBA/GCS-O open up new directions for biosensor applications.

关键词： Coordination polymer Carbon nanosheet Prussian blue analogue Surface reconstruction Glucose oxidation

Enantioselective Synthesis of Benzimidazole Atropisomers Featuring a N-N Axis

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Chinese Journal of chemistry 2024年第7期42卷 711-718页

作者： Fang-Bei Ge Qi-Kun Yin Chuan-Jun Lu Xuan Xuan Jia Feng Ren-Rong Liu college of chemistry and Chemical Engineering Qingdao UniversityQingdaoShandong 266071China School of pharmacy Key Laboratory of Mlecular Pharmacoogy and Drug EvaluationMinistry of EducationYantai Universit YantaiShandong 264005China

Atroposelective synthesis of N-N atropisomers is an emerging area but remains underexplored;in particular,the synthesis of N-N benzimidazole atropisomers is still unprecedented.Herein,the first enantioselective synthesis of N-N benzimidazole atropisomers via the palladium-catalyzed de novo construction of benzimidazole skeleton is presented.With readily available palladium catalyst and biphosphine ligand,a broad range of nonbiaryl benzimidazole and indole-benzimidazole atropisomers were conveniently ac-cessed in high yields and with excellent enantioselectivities.Significantly,these N-N benzimidazole atropisomers showed great anti-tumor activity and selectivity to breast cancer MCF-7 cells.The simple catalytic system,broad substrate scope,high enantioselectivi-ty,and good bioactivity make this approach highly attractive.

关键词： Asymmetric synthesis Atropisomerism Palladium Benzimidazole Antitumor

Surface reconstruction and structural transformation of twodimensional Ni-Fe MOFs for oxygen evolution in seawater media

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Nano Research 2024年第4期17卷 2429-2437页

作者： Liyuan Xiao Xue Bai Jingyi Han Tianmi Tang Siyu Chen Hui Qi Changmin Hou Fuquan Bai Zhenlu Wang Jingqi Guan Institute of Physical chemistry College of ChemistryJilin UniversityChangchun 130021China The Second Hospital of Jilin University Changchun 130021China State Key Laboratory of Inorganic Synthesis and Preparative chemistry College of ChemistryJilin UniversityChangchun 130012China Laboratory of Theoretical and Computational chemistry Institute of Theoretical ChemistryCollege of ChemistryChangchun 130023China

As a four-electron transfer reaction,oxygen evolution reaction(OER)is limited by large overpotential and slow kinetics.Here,we in-situ synthesized two-dimensional(2D)Ni-Fe metal-organic framework nanosheets on nickel foam(NixFe-TPA/NF,TPA=terephthalic acid)for oxygen evolution in alkaline and alkaline seawater electrolytes.In 1 M KOH,Ni3Fe-TPA/NF shows a low overpotential(η10)of 189 mV at 10 mA·cm^(-2) and an ultra-low overpotential of only 260 mV at 500 mA·cm^(-2).In alkaline seawater,Ni3Fe-TPA/NF still provides impressive OER performance,with anη10 of 265 mV.In-situ Raman characterization results show that the phase transition occurs during the OER,and Ni3FeOOH with more oxygen vacancies is in-situ formed,reducing the OER energy barrier.Density functional theory(DFT)reveals that the synergy between Ni and Fe reduces the energy barrier and accelerates the rate-determining step.In addition,the ultra-thin 2D sheet structure and the close combination of Ni3FeOOH and highly conductive NF support ensure the high catalytic OER activity.Therefore,the surface reconstruction and structural modification strategy can be used to design and prepare high-performance OER electrocatalysts for energy-related applications.

关键词： density functional theory(DFT)calculation Ni3FeOOH oxygen evolution reaction seawater electrolysis surface reconstruction