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Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids

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Chinese Chemical Letters 2011年第7期22卷 757-760页

作者： Hong shan Liu Hu Ling Zheng Mei Ge Peng Xia ying chen Department of Medicinal Chemistry School of Pharmacy Fudan University Shanghai 201203 China Laiyi Biological Drug Research and Development Center Co. Ltd. Shanghai 201203 China

Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with ECs0 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.

关键词： Pyrazo-annulated steroid 2-Methoxyestradiol (2-ME) VEGF inhibitory activity

Biodegradable Polypeptide-based Vesicles with Intrinsic Blue Fluorescence for Antibacterial Visualization

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Chinese Journal of Polymer Science 2021年第11期39卷 1412-1420页

作者： Yu-ying Yang Ling-shan chen Min Sun Cong-Yu Wang Zhen Fan Jian-Zhong Du Department of Orthopedics Shanghai Tenth People's HospitalTongji UniversityShanghai 200072China Department of Polymeric Materials School of Materials Science and EngineeringTongji UniversityShanghai 201804China Institute for Advanced Study Tongji UniversityShanghai 200092China

Fluorescence imaging has been an indispensable tool to provide dynamic information about the localization and quantity of ***,due to the intrinsic hollow structure and modularized biofunctionalities,polymer vesicles have been widely applied in biomedical ***,most polymer vesicles are embedded with organic fluorophores for fluorescence imaging,which have certain drawbacks such as leakage and possible ***,we present a biodegradable polypeptide-based vesicle with intrinsic blue fluorescence without introducing any fluorophore for real-time visualization of antibacterial *** modular design to integrate multiple functional fragments,poly(ε-caprolactone)-block-poly(tryptophan)-block-poly(lysine-stat-phenylalanine)[PCL25-b-PTrp2-b-P(Lys13-statPhe4)]was synthesized,where PCL chains form the hydrophobic membrane,P(Lys-stat-Phe)and PTrp provide intrinsic fluorescence and broadspectrum antibacterial *** is noteworthy that the fluorescence emission was shifted from invisible ultraviolet range of amino acids to visible range(emission maximum at 436 nm),which makes it possible to visualize the antibacterial *** addition,through utilizing the intrinsic fluorescence of vesicles,confocal fluorescent imaging of vesicles with bacteria validated the specific adhesion of vesicle towards bacteria,and the bacterial death through membrane ***,we provided a novel approach to developing biodegradable fluorescent polypeptide-based vesicles for real-time visualization of antibacterial process.

关键词： Polypeptide-based vesicles Intrinsic fluorescence Antibacterial visualization

Engineering a high-barrier d-f single-molecule magnet centered with hexagonal bipyramidal Dy(Ⅲ)unit

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Science China Chemistry 2024年第10期67卷 3291-3298页

作者： Wei Deng Chan-ying Yao Yan-Cong chen ying-Qian Zhou shan-Nan Du Jun-Liang Liu Ming-Liang Tong Key Laboratory of Bioinorganic and Synthetic Chemistry of Ministry of Education School of ChemistryInstitute of Green Chemistry and Molecular EngineeringGuangdong Basic Research Center of Excellence for Functional Molecular EngineeringSun Yat-sen UniversityGuangzhou 510006China

In the pursuit of high-performance single-molecule magnets(SMMs),incorporating intramolecular magnetic coupling emerges as a pivotal *** these,d-f SMMs have garnered significant attention due to their remarkable versatility,which lies in their ability to tune coordination environments and facilely substitute metal ***,achieving performance-centric d-f SMMs through the synergistic interplay between highly anisotropic f ions and d-f magnetic interactions remains a formidable *** mononuclear hexagonal bipyramidal(D_(6h))Dy^(Ⅲ)SMMs have been successfully isolated,the exploration of d-f SMMs featuring D_(6h)-lanthanide metal centers remains uncharted *** this study,we employed planar bipodal ligands in conjunction with“staple-like”axial phenoxide ligands to synthesize the first hexagonal bipyramidal d-f ***,this compound exhibits alternating-current magnetic susceptibilities peaking up to 68 K with an energy barrier surpassing 1,200 K,thus establishing a new benchmark within the heterometallic d-f SMM landscape inclusive of complexes with diamagnetic d metals and paramagnetic f ***,the ferromagnetic interaction at the d-f sites engenders oscillating relaxation times contingent on the magnetic field—a characteristic distinct from mononuclear *** findings shed light on a deliberate design approach for d-f SMMs,emphasizing the cooperative utilization of high-barrier lanthanide modules alongside d ions through magnetic *** synergy significantly enhances and diversifies the magnetic dynamics of these intriguing molecular systems.

关键词： single-molecule magnets magnetic coupling crystal engineering hexagonal bipyramid energy barrier

Strong earthquake activity all over the world and strong-moderate earthquake activity within and near China (December, 2000 ~ January, 2001)

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Acta Seismologica Sinica(English Edition) 2001年第2期14卷 356-357页

作者： chen Pei-shan Institute of Geophysics China Seismological Bureau Beijing China

IllustrationAll the data in this catalog are chosen from the 2Preliminary Seismological Report of Chine-se Seismic Stations2 (Its abbreviation is 2Monthly Report2). The catalog includes the events of M34.7 in and near China and M36 all over the world. The 2Monthly Report2 is monthly compiled by the Ninth Section of Institute of Geophysics, CSB.The origin times of earthquakes in the catalog adopt coordinated universal time (UTC) in accordance with international convention. The location of every epicenter is expressed by its latitude and longitude, at the same time by the corresponding geographical region proposed by Flinn and Engdahl. The regional names are only for references and do not imply any political significance. The number of stations used and standard deviation are also given in order to illus-trate the precision of location.The surface wave magnitude MS is measured from the records of intermediate period broad band SK seismographs and adopting the surface wave magnitude formula of Beijing Station of 1965: MS= lg(AH/T)+1.66lgD +3.5 (1°

关键词： the world standard deviation in order

The coninvolutory decomposition and its computation for a complex matrix

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Applied Mathematics(A Journal of Chinese Universities) 2013年第3期28卷 303-310页

作者： chen Xiao-shan School of Mathematics South China Normal University

A complex, square matrix E is called coninvolutory if EE = I, where E denotes complex conjugate of the matrix E and I is an identity matrix. In this paper we introduce the coninvolutory decomposition of a complex matrix and investigate a Newton iteration for computing the coninvolutory factor. A simple numerical example illustrates our results.

关键词： coninvolutory decomposition Newton iteration spectral norm.

Pharmacological targeting cGAS/STING/NF-κB axis by tryptanthrin induces microglia polarization toward M2 phenotype and promotes functional recovery in a mouse model of spinal cord injury

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Neural Regeneration Research 2025年第11期20卷 3287-3301页

作者： Ziwei Fan Mengxian Jia Jian Zhou Zhoule Zhu Yumin Wu Xiaowu Lin Yiming Qian Jiashu Lian Xin Hua Jianhong Dong Zheyu Fang Yuqing Liu Sibing chen Xiumin Xue Juanqing Yue Minyu Zhu ying Wang Zhihui Huang Honglin Teng Department of Orthopedics(Spine Surgery) the First Affiliated Hospital of Wenzhou Medical UniversityWenzhouZhejiang ProvinceChina School of Pharmacy Hangzhou Normal UniversityHangzhouZhejiang ProvinceChina Department of Neurology The First Affiliated Hospital of Wenzhou Medical UniversityWenzhouZhejiang ProvinceChina Department of Pathology Affiliated Hangzhou First People’s HospitalSchool of MedicineWestlake UniversityHangzhouZhejiang ProvinceChina Department of Clinical Research Center Affiliated Hangzhou First People’s HospitalSchool of MedicineWestlake UniversityHangzhouZhejiang ProvinceChina

The M1/M2 phenotypic shift of microglia after spinal cord injury plays an important role in the regulation of neuroinflammation during the secondary injury phase of spinal cord *** of shifting microglia polarization from M1(neurotoxic and proinflammatory type)to M2(neuroprotective and anti-inflammatory type)after spinal cord injury appears to be *** possesses an anti-inflammatory biological ***,its roles and the underlying molecular mechanisms in spinal cord injury remain *** this study,we found that tryptanthrin inhibited microglia-derived inflammation by promoting polarization to the M2 phenotype in *** promoted M2 polarization through inactivating the cGAS/STING/NF-κB ***,we found that targeting the cGAS/STING/NF-κB pathway with tryptanthrin shifted microglia from the M1 to M2 phenotype after spinal cord injury,inhibited neuronal loss,and promoted tissue repair and functional recovery in a mouse model of spinal cord ***,using a conditional co-culture system,we found that microglia treated with tryptanthrin suppressed endoplasmic reticulum stress-related neuronal *** together,these results suggest that by targeting the cGAS/STING/NF-κB axis,tryptanthrin attenuates microglia-derived neuroinflammation and promotes functional recovery after spinal cord injury through shifting microglia polarization to the M2 phenotype.

关键词： cGAS/STING functional recovery microglia neuroinflammation neuroprotection nuclear factor-κB polarization spinal cord injury tryptanthrin

Novel approach for determining the optimal axial preload of a simulating rotary table spindle system

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Journal of Zhejiang University-Science A(Applied Physics & Engineering) 2007年第5期8卷 812-817页

作者： shan Xiao-biao XIE Tao chen Wei-shan School of Mechatronics Engineering Harbin Institute of Technology Harbin 15001 China

This paper presents a new theoretical model to determine the optimal axial preload of a spindle system, for challenging the traditional method which relies heavily on experience of engineers. The axial preloading stiffness was treated as the sum of the spindle modal stiffness and the framework elastic stiffness, based on a novel concept that magnitude of preloads can be controlled by measuring the resonant frequency of a spindle system. By employing an example of a certain type of aircraft simulating rotary table, the modal stiffness was measured on the Agilent 35670A Dynamic Signal Analyzer by experimental modal analysis. The equivalent elastic stiffness was simulated by both finite element analysis in ANSYS? and a curve fitting in MATLAB?. Results showed that the static preloading stiffness of the spindle was 7.2125×107 N/m, and that the optimal preloading force was 120.0848 N. Practical application proved the feasibility of our method.

关键词： Three-axis simulating rotary table Axial position preload Stiffness Experimental modal analysis Finite elementanalysis

MaMADS1-MaNAC083 transcriptional regulatory cascade regulates ethylene biosynthesis during banana fruit ripening

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Horticulture Research 2023年第10期10卷 101-111页

作者： Wei Wei ying-ying Yang Chao-jie Wu Jian-fei Kuang Jian-ye chen Wang-jin Lu Wei shan Guangdong Provincial Key Laboratory of Postharvest Science of Fruits and Vegetables/Engineering Research Center of Southern Horticultural Products Preservation Ministry of EducationCollege of HorticultureSouth China Agricultural UniversityGuangzhou 510642China

The hormone ethylene is crucial in the regulation of ripening in climacteric fruit,such as *** transcriptional regulation of ethylene biosynthesis throughout banana fruit ripening has received much study,but the cascaded transcriptional machinery of upstream transcriptional regulators implicated in the ethylene biosynthesis pathway is still poorly *** we report that ethylene biosynthesis genes,including MaACS1,MaACO1,MaACO4,MaACO5,and MaACO8,were upregulated in ripening ***(NAM,ATAF,CUC)transcription factor,MaNAC083,a ripening and ethylene-inhibited gene,was discovered as a potential binding protein to the MaACS1 promoter by yeast one-hybrid *** in vitro and in vivo experiments indicated that MaNAC083 bound directly to promoters of the five ethylene biosynthesis genes,thereby transcriptionally repressing their expression,which was further verified by transient overexpression experiments,where ethylene production was inhibited through MaNAC083-modulated transcriptional repression of ethylene biosynthesis genes in banana ***,MaMADS1,a ripening-induced MADS(MCM1,AGAMOUS,DEFICIENS,SRF4)transcription factor,was found to directly repress the expression of MaNAC083,inhibiting trans-repression of MaNAC083 to ethylene biosynthesis genes,thereby attenuating MaNAC083-repressed ethylene production in *** findings collectively illustrated the mechanistic basis of a MaMADS1-MaNAC083-MaACS1/MaACOs regulatory cascade controlling ethylene biosynthesis during banana fruit *** findings increase our knowledge of the transcriptional regulatory mechanisms of ethylene biosynthesis at the transcriptional level and are expected to help develop molecular approaches to control ripening and improve fruit storability.

关键词： thereby collective verified

Clique-Transversal Sets in 4-Regular Claw-Free Graphs

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Acta Mathematica Sinica,English Series 2011年第5期27卷 883-890页

作者： Er Fang shan Li ying KANG Department of Mathematics Shanghai University Shanghai 200444 P. R. China

A clique-transversal set D of a graph C is a set of vertices of G such that D meets all cliques of G. The clique-transversal number, denoted by To（G）, is the minimum cardinality of a clique- transversal set in G. In this paper we give the exact value of the clique-transversal number for the line graph of a complete graph. Also, we give a lower bound on the clique-transversal number for 4-regular claw-free graphs and characterize the extremal graphs achieving the lower bound.

关键词： Clique-transversal set claw-free graph line graph regular graph