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Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors

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Chinese Journal of Polymer Science 2019年第2期37卷 129-135页

作者： Fan-Fan Fu Ben-Qing Zhou Zhi-Jun Ouyang yi-Lun wu jing-yi Zhu Ming-wu Shen Jin-Dong Xia Xiang-Yang Shi Key Laboratory of Science & Technology of Eco-Textile Ministry of Education College of Chemistry Chemical Engineering and Biotechnology Donghua University Department of Radiology Shanghai Songjiang District Central Hospital

We present here the development of cholesterol(Chol)-modified dendrimer system for targeted chemotherapy of folate(FA)receptor-expressing cancer cells. In our study, poly(amidoamine)(PAMAM) dendrimers of generation 5(G5) were functionalized stepby-step with Chol, fluorescein isothiocyanate(FI), and FA via a poly(ethylene glycol)(PEG) spacer(PEG-FA), and then acetamide to shield their remaining surface amines. The synthesized ***-Chol-FI-PEG-FA(for short, G5-CFPF) dendrimers were utilized to encapsulate 10-hydroxycamptothecin(HCP), a hydrophobic anticancer drug. We find that each G5-CFPF dendrimer can encapsulate 13.8 HCP molecules. The complexes show a slower release profiles of HCP in a pH-dependent manner than the control complexes formed using the same dendrimers without Chol under the same conditions. Thanks to the targeting role played by FA, the complexes display a specific inhibition efficacy to FA receptor-expressing cervical cancer cells. The designed Chol-modified dendrimers may be adopted as a promising carrier for application in targeted cancer therapy.

关键词： PAMAM dendrimers Folate Cholesterol 10-Hydroxycamptothecin Targeted cancer therapy

Synthesis and Anticholinesterase Activity of （-）-Physostigmine Analogues with Modifications at C3a and C5

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Chemical Research in Chinese Universities 2013年第5期29卷 888-893页

作者： WANG Hui-jing ZHANG Dan WANG Fu-sheng wu yi SONG Hao Innovative Drug Research Center Chongqing University Chongqing 401331 P. R. China Key Laboratory of Drug Targeting and Novel Delivery System of the Ministry of Education West China School of Pharmacy Sichuan University Chengdu 610041 P. R. China

A new series of physostigmine analogues 3a--3j with modifications at the C3a and C5 positions was de- signed and synthesized. Bioassay of the synthetic analogues 3a--3j, along with the previous synthesized C3a-ethyl-C5-triazole physostigmine analogues laJlg and 2a--2j was performed, which indicates that the replace- ment of the carbamoyl moiety of C3a-ethyl-C5-triazole analogues 1 and 2 with a triazole moiety decreased acetyl- cholinesterase（AchE） inhibitory activity, whereas the introduction of heterocycles into the triazole ring increased both AChE and butyrylcholinesterase（BchE） inhibitory activities. Structure-activity relationship（SAR） studies of C3a-methyl-C5-triazole analogues 3 reveal the C3a-methyl substituent is important for AChE and BChE inhibition and the introduction of a second ionizable N center improved the binding of the synthetic analogues to both AChE and BChE.

关键词： C3a-ethyl-C5-triazole physostigmine analogue C3a-methyl-C5-triazole physostigmine analogue Anti-cholinesterase activity Alzheimer's disease

Phase constitution,microstructure and mechanical properties of a Ni-based superalloy specially designed for additive manufacturing

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China Foundry 2021年第4期18卷 397-408页

作者： Bin wu jing-jing Liang Yan-hong Yang Jin-guo Li yi-zhou Zhou Shi-changxu Innovation Center for Advanced Materials Institute of Metal ResearchChinese Academy of SciencesShenyang 110016China School of Materials Science and Engineering University of Science and Technology of ChinaShenyang 110016China Space Manufacturing Technology(CAS Key Lab) Beijing 100094China

In this study,a kind of Ni-based superalloy specially designed for additive manufacturing(AM)was ***-Calc simulation and differential scanning calorimetry(DSC)analysis were used to determine phases and their transformation *** specimens were prepared by laser metal deposition(LMD)and traditional casting ***,phase constitution and mechanical properties of the alloy were characterized by scanning electron microscopy(SEM),transmission scanning electron microscopy(TEM),X-ray diffraction(XRD)and tensile *** results show that this alloy contains two basic phases,γ/γ’,in addition to these phases,at least two secondary phases may be present,such as MC carbides and Laves ***,the as-deposited alloy has finer dendrite,its mean primary dendrite arm space(PDAS)is about 30-45μm,and the average size ofγ’particles is 100-150 ***,the dendrite size of the as-cast alloy is much larger and its PDAS is 300-500μm with secondary and even third dendrite ***,the alloy displays different tensile behavior with different processing methods,and the as-deposited specimen shows better ultimate tensile stress(1,085.7±51.7 MPa),yield stress(697±19.5 MPa)and elongation(25.8%±2.2%)than that of the as-cast *** differences in mechanical properties of the alloy are due to the different morphology and size of dendrites,γ’,and Laves phase,and the segregation of elements,*** important information would be helpful for alloy application as well as new alloy development.

关键词： additive manufacturing laser metal deposition Ni-based superalloy tensile behavior

Regioselective Synthesis of Functionalized Dihydroquinolines via Organocatalytic Allylic Alkylation

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Chemical Research in Chinese Universities 2016年第4期32卷 634-640页

作者： MA Xiaoyuan wu yi ZHANG Yanjing TENG Lesheng XIE jing LIAO Weiwei Department of Pharmacology School of Pharmaceutical Science Jilin University Changchun 130021 P. R. China Department of Organic Chemistry College of Chemistry Jilin University Changchun 130012 P. R. China College of Life Sciences Jilin University Changchun 130012 P. R. China

The regioselective allylic alkylation of 1,2-dihydroquinolines and Morita-Baylis-Hillman（MBH） adducts has been developed. By surveying various reaction parameters, we summarized the effects of temperatures, relative reactant doses, catalysts, solvents and N-protected groups on the regioselectivity of this transformation. This method provides a facile protocol for the preparation of allylic a-substituted dihydroquinolines.

关键词： 1,2-Dihydroquinoline Regioselectivity Allylic alkylation

Synthesis and Biological Evaluation of Amino Alcohol Containing 1,3,4-Oxadiazole

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Chemical Research in Chinese Universities 2016年第5期32卷 760-767页

作者： wu yi ZHAO Yanping GUO jing LV Haoze ZHENG Nan WANG Ensi College of Pharmacy Jilin University Changchun 130021 P. R. China School of Clinical Medicine Jilin University Changchun 130021 P. R. China

A series of amino alcohol derivatives containing 1,3,4-oxadiazole moieties was synthesized with 7-bromo-2-tetralone as starting materials, 2,2-dimethyl-1,3-oxazolidine as intermediates and Strecker reaction and cyclization with POCt3 as key steps. The structures of the key intermediate and target compounds were confirmed by IH NMR, 13C NMR and HRMS. Some compounds have resulted in the generation of highly potent sphingosine 1-phosphate receptor type 1（S1P1） agonists.

关键词： Amino alcohol 1,3,4-Oxadiazole Bioactivity Strecker reaction

Scale-free brain ensemble modulated by phase synchronization

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Journal of Zhejiang University-Science C(Computers and Electronics) 2014年第10期15卷 821-831页

作者： Dan wu Chao-yi LI Jie LIU jing LU De-zhong YAO Department of Biomedical Engineering School of Computer and Information TechnologyBeijing Jiaotong University NeuroInformation of Ministry of Education University of Electronic Science and Technology of China

To listen to brain activity as a piece of music, we proposed the scale-free brainwave music(SFBM) technology, which could translate the scalp electroencephalogram(EEG) into music notes according to the power law of both EEG and music. In the current study, this methodology was further extended to a musical ensemble of two channels. First, EEG data from two selected channels are translated into musical instrument digital interface(MIDI) sequences, where the EEG parameters modulate the pitch, duration, and volume of each musical note. The phase synchronization index of the two channels is computed by a Hilbert transform. Then the two MIDI sequences are integrated into a chorus according to the phase synchronization index. The EEG with a high synchronization index is represented by more consonant musical intervals, while the low index is expressed by inconsonant musical intervals. The brain ensemble derived from real EEG segments illustrates differences in harmony and pitch distribution during the eyes-closed and eyes-open states. Furthermore, the scale-free phenomena exist in the brainwave ensemble. Therefore, the scale-free brain ensemble modulated by phase synchronization is a new attempt to express the EEG through an auditory and musical way, and it can be used for EEG monitoring and bio-feedback.

关键词： Brainwave Ensemble Music Scale-free Synchronization

Dietary Daidzein Enhances Antiapoptotic Effect of 17β-Estradiol (E_2) on Breast Cancer MCF-7 Cells

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Chinese Journal of Cancer Research 2010年第1期22卷 10-16页

作者： Xiao-fei wu yi-jing Wang Guo-liang Xia Mei-jia Zhang State Key Laboratory for Agrobiotechnology College of Biological Sciences China Agricultural University Beijing 100193 China

Objective： To investigate whether dietary daidzein interact with endogenous 17β-Estradiol （E2） to give rise to additive or inhibitory effects on proliferation and apoptosis in breast cancer cells. Methods： Cell cycle distribution and apoptosis induction were analyzed by using flow cytometry when breast cancer cell lines MCF-7 were cotreated with daidzein （1, 5 μmol/L） and E2 （0.1-10 nmol/L） for 5 days. Whether daidzein could alter E2-modulated mRNA expression of estrogen receptor alpha （ERα）, estrogen receptor beta （ERI3） and ERβ-estrogen response element （ERE） dependent transcription was investigated by RT-PCR and luciferase induction assays. The effects of daidzein on E2-modulated expression of proapoptotic p53, bax and antiapoptotic bcl-2 at both mRNA and protein levels were also investigated by RT-PCR and Western blot. Results： Daidzein enhanced the antiapoptotic effect in an Ea dose-dependent manner, but had no effect on E2-induced proliferation. Daidzein antagonized E2-induced ERβ mRNA expression and ERβ-ERE dependent transcription. In addition, daidzein only antagonized E2-upregulated expression of p53 and bax, but had no effect on E2-upregulated expression of bcl-2. Conclusion： Daidzein enhances the antiapoptotic effect of E2 on breast cancer cells by inhibiting E2-mediated p53-bax proapoptotic pathway. These results suggest that dietary daidzein may enhance deleterious effect of endogenous E2 in hormone-dependent breast cancer.

关键词： Daidzein E2 Breast cancer MCF-7 cells Antiapoptotic effect Estrogen receptor (ER)

Multiple Vandermonde Decomposition Based Channel Estimation for Mm Wave MIMO High-Mobility Communication in 5G and Beyond

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China Communications 2023年第4期20卷 12-25页

作者： Zhao yi Xiaojun jing School of Electronics and Information Hunan First Normal UniversityChangsha 410205China Key Laboratory of Trustworthy Distributed Computing and Service Ministry of EducationBeijing University of Posts and TelecommunicationsBeijing 100876China School of Information and Communication Engineering Beijing University of Posts and TelecommunicationsBeijing 100876China

Millimeter wave(mmWave)massive massive multiple input multiple output(MIMO)technique has been regarded as the viable solution for vehicular communications in 5G and *** achieve the substantial increase in date rates,it is important to take an effective channel state information(CSI).However,existing channel estimation strategies are unavailable since the users *** solve above issues,in this paper,inspired by a specific antenna structure,we propose a novel approach for fast time-varying channel ***,by considering the vehicle scenario with high-mobility,a corresponding mathematical model is firstly ***,based on the special structural of the sparse array,the switch network is used to replace the convention phase shifter of mmWave hybrid system,which can effectively reduce the number of radio-frequency(RF)chains and ***,by solving the semidefinite programming(SDP)duality problem,the Doppler frequency and path parameters are effectively *** results are shown that the computational complexity and estimation accuracy of the proposed algorithm is superior than that of the traditional schemes.

关键词： MIMO mmWave channel estimation high-mobility time-variant

Association of CDH11 with Autism Spectrum Disorder Revealed by Matched-gene Co-expression Analysis and Mouse Behavioral Studies

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Neuroscience Bulletin 2022年第1期38卷 29-46页

作者： Nan wu Yue Wang jing-Yan Jia yi-Hsuan Pan Xiao-Bing Yuan Key Laboratory of Brain Functional Genomics of Shanghai and the Ministry of Education Institute of Brain Functional GenomicsSchool of Life Science and the Collaborative Innovation Center for Brain ScienceEast China Normal UniversityShanghai200062China Hussman Institute for Autism Baltimore21201USA Department of Anatomy and Neurobiology University of Maryland School of MedicineBaltimore21201USA

A large number of putative risk genes for autism spectrum disorder(ASD)have been *** functions of most of these susceptibility genes in developing brains remain unknown,and causal relationships between their variation and autism traits have not been *** aim of this study was to predict putative risk genes at the whole-genome level based on the analysis of gene co-expression with a group of high-confidence ASD risk genes(hcASDs).The results showed that three gene features–gene size,mRNA abundance,and guanine-cytosine content–affect the genome-wide co-expression profiles of *** circumvent the interference of these features in gene co-expression analysis,we developed a method to determine whether a gene is significantly co-expressed with hcASDs by statistically comparing the co-expression profile of this gene with hcASDs to that of this gene with permuted gene sets of feature-matched *** method is referred to as"matched-gene co-expression analysis"(MGCA).With MGCA,we demonstrated the convergence in developmental expression profiles of hcASDs and improved the efficacy of risk gene *** results of analysis of two recently-reported ASD candidate genes,CDH11 and CDH9,suggested the involvement of CDH11,but not CDH9,in *** with this prediction,behavioral studies showed that Cdh11-null mice,but not Cdh9-null mice,have multiple autism-like behavioral *** study highlights the power of MGCA in revealing ASD-associated genes and the potential role of CDH11 in ASD.

关键词： CDH11 Autism spectrum disorder Gene co-expression analysis Matched-gene co-expression analysis