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Chinese Chemical Letters 2024年第5期35卷 290-295页

作者： Jiajia Lv Jie Gao Hongyu Li Zeli Yuan Nan Dong school of Chemistry and Chemical Engineering Guizhou UniversityGuiyang 550025China school of pharmacy Zunyi Medical UniversityZunyi 563003China Guizhou International Scientific and Technological Cooperation Base for Medical Photo-Theranostics Technology and Innovative Drug Development Zunyi 563003China

As key biomarkers,amyloid-β(Aβ)plaques are frequently used to diagnose Alzheimer’s disease(AD).Although fluorescence imaging has proven to be effective in detecting these plaques,the gold standard probe thioflavin T(ThT),used for Aβaggregates,cannot be applied in vivo owing to its invasive ***,the development of novel fluorescent probes capable of identifying Aβplaques in situ is *** on the ThT structure,twoπ-conjugated heterocyclic D-π-A probes were designed bearing the hydroxytricyanopyrrole acceptor and N,N-dimethylaminophenyl *** probes exhibited red to near-infrared fluorescence emission(λ_(max)=732 nm),large Stokes shifts(>100 nm),exceptional signal-to-noise ratio,rapid response(<30 s),and high binding affinity(NT-HTCP=33.32 nmol/L;NF-HTCP=53.35 nmol/L)for Aβ*** the best candidate,NT-HTCP was used for in situ imaging of Aβplaques in AD mouse ***,in vivo research demonstrated that NT-HTCP could cross the blood-brain barrier and continue imaging the Aβplaques with a good signal-to-noise ***,the outcomes of the docking computations helped guide the development of the Aβ*** study expands the family of N,N-dimethylaminophenyl-based Aβ-sensitive fluorophores,with NTHTCP emerging as a highly promising imaging agent.

关键词： Amyloid-β Fluorescent probe Hydroxytricyanopyrrole Fluorescence imaging Alzheimer’s disease

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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 *** 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 ***,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 *** 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 *** 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

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Reversing artemisinin resistance by leveraging thermo-responsive nanoplatform to downregulating GSH

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Chinese Chemical Letters 2024年第6期35卷 392-397页

作者： Yong-Dan Zhao Yidan Wang Rongrong Wang Lina Chen Hengtong Zuo Xi Wang Jihong Qiang Geng Wang Qingxia Li Canqi Ping Shuqiu Zhang Hao Wang school of pharmacy Shanxi Medical UniversityTaiyuan 030001China National Center for Nanoscience and Technology Beijing 100190China Artemisinin Research Center Institute of Chinese Materia MedicaBeijing 100700China

Artemisinin(ART)resistance has been an emerging clinical problem,severely compromising antimalarial efficacy and threatening the global malaria elimination *** intensive studies about the molecular mechanism for ART resistance are under way,no effective therapeutic targets for reversing resistance have been ***,we explore glutathione(GSH)as a therapeutic target to develop a thermo-responsive nanoplatform to specifically co-deliver ART and GSH synthesis inhibitor(L-buthionine sulfoximine,BSO)in a sustained manner,effectively reversing ART resistance in *** combining with BSO,ART exerts increased antimalarial activity with reduced half-maximal inhibitory concentration(IC50)by 7.43-fold in ART-resistant *** work reveals that the GSH in ART-resistant parasites can be a promising therapeutic target for reversing ART resistance,paving the way for developing drug candidates and intelligent nanomedicines in malaria therapy.

关键词： Nanomedicines Drug delivery Artemisinins resistance Malaria Glutathione

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GIPC1 promotes tumor growth and migration in gastric cancer via activating PDGFR/PI3K/AKT signaling

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Oncology Research 2024年第2期32卷 361-371页

作者： TINGTING LI WEI ZHONG LIU YANG ZHIYU ZHAO LI WANG CONG LIU WANYUN LI HAIYAN LV SHENGYU WANG JIANGHUA YAN TING WU GANG SONG FANGHONG LUO Cancer Research Center School of MedicineXiamen UniversityXiamen361000China Department of pharmacy Xiamen Mental Health CenterXiamen Xianyue HospitalXiamen361000China

The high mortality rate associated with gastric cancer(GC)has resulted in an urgent need to identify novel therapeutic targets for *** study aimed to investigate whether GAIP interacting protein,C terminus 1(GIPC1)represents a therapeutic target and its regulating mechanism in ***1 expression was elevated in GC tissues,liver metastasis tissues,and lymph node ***1 knockdown or GIPC1 blocking peptide blocked the platelet-derived growth factor receptor(PDGFR)/PI3K/AKT signaling pathway,and inhibited the proliferation and migration of GC ***,GIPC1 overexpression markedly activated the PDGFR/PI3K/AKT signaling pathway,and promoted GC cell proliferation and ***,platelet-derived growth factor subunit BB(PDGF-BB)cytokines and the AKT inhibitor attenuated the effect of differential GIPC1 ***,GIPC1 silencing decreased tumor growth and migration in BALB/c nude mice,while GIPC1 overexpression had contrasting *** together,our findings suggest that GIPC1 functions as an oncogene in GC and plays a central role in regulating cell proliferation and migration via the PDGFR/PI3K/AKT signaling pathway.

关键词： GIPC1 PDGFR Gastric cancer Proliferation Migration

LA-D-B1,a novel Abemaciclib derivative,exerts anti-breast cancer effects through CDK4/6

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BIOCELL 2024年第5期48卷 847-860页

作者： LING MA ZIRUI JIANG XIAO HOU YUTING XU ZIYUN CHEN SIYI ZHANG HANXUE LI SHAOJIE MA GENG ZHANG XIUJUN WANG JING JI Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening College of PharmacyJiangsu Ocean UniversityLianyungang222000China school of Medicine Xiamen UniversityXiamen361102China

Background:Regulatory proteins involved in human cellular division and proliferation,cyclin-dependent kinases 4 and 6(CDK4/6)are overexpressed in numerous cancers,including triple-negative breast cancer(TNBC).TNBC is a common pathological subtype of breast cancer that is prone to recurrence and metastasis,and has a single treatment *** one of the CDK4/6 inhibitors,abemaciclib can effectively inhibit the growth of breast *** this study,we synthesized LA-D-B1,a derivative of Abemaciclib,and investigated its anti-tumor effects in breast ***:Cellular viability was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)*** cloning and migration abilities were determined by colony formation assay and wound healing *** invasion abilities and adhesion were determined by cell invasion assay and cell adhesion *** impact of compound LA-D-B1 on cell proliferation and the cell cycle was analyzed through Western blotting,which quantified the levels of proteins associated with the cyclin-dependent kinase(CDK)4/6-cyclin D-Rb-E2F *** in vivo anti-tumor activity of compound LA-D-B1 was investigated using a chick chorioallantoic membrane(CAM)***:The study demonstrated that LA-D-B1 effectively suppressed breast cancer cell proliferation,induced apoptosis,and caused cell cycle ***,LA-D-B1 reduced the expression of key proteins in the CDK4/6-cyclin D-Rb-E2F pathway,including CDK4,CDK6 and *** results also indicated significant antitumor activity of LA-D-B1 in a transplanted tumor ***:In this study,LA-D-B1 demonstrated a potent anti-tumor effect by effectively suppressing cell proliferation and inhibiting cell cycle progression in breast *** findings highlight the potential of LA-D-B1 as a valuable compound for enhancing therapeutic outcomes and controlling the progression of breast cancer.

关键词： CDK4/6 inhibitor Breast cancer Antitumor activity Cell cycle

Vitamin D,selenium,and antidiabetic drugs in the treatment of type 2 diabetes mellitus with Hashimoto's thyroiditis

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World Journal of Diabetes 2024年第2期15卷 209-219页

作者： Fen Feng Bin Zhou Ci-La Zhou Ping Huang Gang Wang Kuang Yao school of pharmacy Shaoyang UniversityShaoyang 422099Hunan ProvinceChina Department of Endocrinology The Central Hospital of ShaoyangShaoyang 422099Hunan ProvinceChina

BACKGROUND Diabetes and thyroiditis are closely *** occur in combination and cause significant damage to the *** is no clear treatment for type-2 diabetes mellitus(T2DM)with Hashimoto's thyroiditis(HT).While single symptomatic drug treatment of the two diseases is less effective,combined drug treatment may improve *** To investigate the effect of a combination of vitamin D,selenium,and hypoglycemic agents in T2DM with *** This retrospective study included 150 patients with T2DM and HT treated at The Central Hospital of Shaoyang from March 2020 to February *** patients were assigned to the control group,test group A,and test group B according to different treatment *** control group received low-iodine diet guidance and hypoglycemic drug *** group A received the control treatment plus vitamin D *** group B received the group A treatment plus *** levels of markers of thyroid function[free T3(FT3),thyroid stimulating hormone(TSH),free T4(FT4)],autoantibodies[thyroid peroxidase antibody(TPOAB)and thyroid globulin antibody(TGAB)],blood lipid index[low-density lipoprotein cholesterol(LDL-C),total cholesterol(TC),triacylglycerol(TG)],blood glucose index[fasting blood glucose(FBG),and hemoglobin A1c(HbA1c)]were measured pre-treatment and 3 and 6 months after *** relationships between serum 25-hydroxyvitamin D3[25(OH)D3]level and each of these indices were *** The levels of 25(OH)D3,FT3,FT4,and LDL-C increased in the order of the control group,test group A,and test group B(all P

关键词： Type-2 diabetes mellitus Hashimoto's thyroiditis Vitamin D Selenium agent Hypoglycemic drugs Curative effect

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 Molecular Pharmacology and Drug EvaluationMinistry of EducationYantai UniversityYantaiShandong 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 ***,the first enantioselective synthesis of N-N benzimidazole atropisomers via the palladium-catalyzed de novo construction of benzimidazole skeleton is *** 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 ***,these N-N benzimidazole atropisomers showed great anti-tumor activity and selectivity to breast cancer MCF-7 *** 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

Spin chiral anisotropy of diamagnetic chiral mesostructured In_(2)O_(3)films

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Nano Research 2024年第8期17卷 7756-7761页

作者： Ting Ji Quanzheng Deng Hao Chen Lu Han Zhibei Qu Shunai Che Yingying Duan Frontiers Science Center for Transformative Molecules State Key Laboratory of Metal Matrix CompositesShanghai Key Laboratory for Molecular Engineering of Chiral DrugsSchool of Chemistry and Chemical EngineeringShanghai Jiao Tong UniversityShanghai 200240China school of Chemical Science and Engineering Tongji UniversityShanghai 200092China Department of Medicinal Chemistry School of PharmacyFudan UniversityShanghai 201203China

Spin chiral anisotropy(SChA)refers to the occurrence of different spin polarization in antipodal chiral ***,we report the SChA in diamagnetic chiral mesostructured In2O3 films(CMIFs)with manifestation of chirality-dependent magnetic circular dichroism(MCD)*** were grown on fluorine-doped tin dioxide conductive glass(FTO)substrates,which were synthesized via a hydrothermal route,with malic acid used as the symmetry-breaking *** levels of chirality have been identified in CMIFs:primary nanoflakes with atomically twisted crystal lattices and secondary helical stacking of the *** exhibit chirality-dependent asymmetric MCD signals due to the different interactions of chirality-induced effective magnetic field and external magnetic field,which distinguish from the commonly observed external magnetic fielddependent symmetric MCD *** findings provide insights into spin manipulation of spin-paired diamagnets.

关键词： chiral inorganics mesostructure diamagnet spin chiral anisotropy(SChA) magnetic circular dichroism(MCD)

Combining network pharmacology， molecular docking， and experimental verification to investigate the anti-rheumatoid arthritis effect and mechanism of Baeckea frutescens leaves

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Food Science and Human Wellness 2024年

作者： Xueyang Guo Mengyao Zhang Haixia Cai Xinyue Jiang Siyuan Zhou Wen Gong Zijiao Wei Weili Qiao Beixi Jia Department of Pharmacognosy school of Pharmaceutical Science Zhengzhou University Department of pharmacy Henan Provincial People's Hospital

The aromatic Baeckea frutescens leaves (BFL) known as “Gang-Song-Cha” is a popular drink (Tea) in South China. To explore the healthcare value， a systematic and in-depth study on BFL alleviating rheumatoid arthritis (RA) was carried out by integrating network pharmacology， molecular docking， and experimental verification. The efficacy was first evaluated， and the BFL extract could ameliorate RA by inhibiting articular swelling， lowering immune organ index， improving the ankle pathologies， and regulating serum levels of TNF-α， IL-6， and IL-10 in CIA rats. Then the anti-RA mechanism of BFL was investigated by leveraging the high-content and active component 5-hydroxy-7-methoxy-2-isopropylchromone (Chro.)， and the potential signaling pathway and related target proteins for Chro. acting on RA were analyzed by KEGG enrichment and docking simulation. Finally， the experimental validations were conducted on RA-FLS cells， and compound Chro. could inhibit cell invasion and migration， block cell cycle at G2/M phase and induce apoptosis， and reduce the secretion of inflammatory cytokines by suppressing the PI3K-Akt pathway. These results provided pharmacological basis for the folk usage of “Gang-Song-Cha (Tea)” for intervening RA.

关键词：

Discrimination of polysorbate 20 by high-performance liquid chromatography-charged aerosol detection and characterization for components by expanding compound database and library

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Journal of Pharmaceutical Analysis 2024年第5期14卷 722-732页

作者： Shi-Qi Wang Xun Zhao Li-Jun Zhang Yue-Mei Zhao Lei Chen Jin-Lin Zhang Bao-Cheng Wang Sheng Tang Tom Yuan Yaozuo Yuan Mei Zhang Hian Kee Lee Hai-Wei Shi Jiangsu Institute for Food and Drug Control Nanjing210019China school of pharmacy China Pharmaceutical UniversityNanjing211112China school of pharmacy Nanjing University of Chinese MedicineNanjing210046China Chinese Pharmacopoeia Commission Beijing100061China Nanjing Well Pharmaceutical Group Co. Ltd.Nanjing210018China school of Environmental and Chemical Engineering Jiangsu University of Science and TechnologyZhenjiangJiangsu212003China University of Massachusetts Amherst Amherst01003USA Department of Chemistry National University of SingaporeSingapore117543Singapore

Analyzing polysorbate 20(PS20)composition and the impact of each component on stability and safety is crucial due to formulation variations and individual *** similar structures and polarities of PS20 components make accurate separation,identification,and quantification *** this work,a high-resolution quantitative method was developed using single-dimensional high-performance liquid chromatography(HPLC)with charged aerosol detection(CAD)to separate 18 key components with multiple *** separated components were characterized by ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UHPLC-Q-TOF-MS)with an identical gradient as the HPLC-CAD *** polysorbate compound database and library were expanded over 7-time compared to the commercial *** method investigated differences in PS20 samples from various origins and grades for different dosage forms to evaluate the composition-process ***-Q-TOF-MS identified 1329 to 1511 compounds in 4 batches of PS20 from different *** method observed the impact of 4 degradation conditions on peak components,identifying stable components and their tendencies to ***-CAD and UHPLC-Q-TOF-MS results provided insights into fingerprint differences,distinguishing quasi products.

关键词： Polysorbate 20 Component Database Discrimination Degradation