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Facile preparation and characterization of novel oleanane-type triterpene functionalized β-cyclodextrin conjugates

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Chinese Chemical Letters 2019年第3期30卷 690-693页

作者： Pingxuan jiao Shouxin Wang Shuobin Liang Man Li Qianqian Gao dezhong ji Yingying Chen Haiwei Li Fuxiang Ran Yongmin Zhang Lihe Zhang Demin Zhou Sulong Xiao State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University School of Pharmacy Jining Medical University Sorbonne Universite Institut Parisien de Chimie Moleculaire CNRS UMR 8232 State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of Botany Chinese Academy of Sciences

Oleanolic acid(OA) and echinocystic acid(EA), two naturally occurring pentacyclic oleanane triterpenes,are gaining increasing attention due to their promising pharmacological activities. Conjugation with amphiphilic α(β)-cyclodextrin(CD) via "click chemistry" can improve their solubility and anti-HCV entry potency. In the present work,four water-soluble β-CD-pentacyclic triterpene conjugates were designed and synthesized, in which OA and EA was coupled to one of the primary hydroxyl groups of β-CD via ester and amide bonds. The structures of the conjugates were unambiguously determined by ~1H NMR, ^(13)C NMR and HRMS or MALDI-TOF-MS. All the conjugates showed lower hydrophobicity(AlogP) than their parent compounds and no significant cytotoxicity was found to HL-60, A549, Hela and Bel-7402 cells at concentrations up to 10 μmol/L. Further anti-HCV entry activity and mechanism studies are under way in our laboratory.

关键词： β-Cyclodextrin DIBAL-H Oleanolic acid Echinocystic acid Synthesis

Metal-Free Selective Functionalization of 8-amidoquinolines on the C-5 Position

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Metal-Free Selective Functionalization of 8-amidoquinolines ...

Proximity-enabled covalent binding of IL-2 to IL-2Rα selectively activates regulatory T cells and suppresses autoimmunity

中国化学会第十三届全国有机合成化学学术研讨会

作者： dezhong ji Xin He Yizhu Xu Qihua Zhu Zhibin Wang Yungen Xu State Key Laboratory of Natural Medicines China Pharmaceutical University jiangsu Key Laboratory of Drug Design and Optimization Department of Medicinal ChemistryChina Pharmaceutical University

Quinoline is an important scaffold in various natural products and synthetic compounds with wide applications in medicinal and materials *** the recent decades,it has attracted much attention toward functionalizing quinoline scaffolds at the C2,C4,and C8 *** comparison,methodology for the C-5 selective formation of carbon-heteroatom still remains ***,several groups reported remote C-H functionalization of quinolines on the C5 ***,almost all of the reported methods used high temperature and metal catalysis which wasenvironment ***,we developeda synthetic method to construct C-N bonds at C-5 position of 8-amidoquinolines usinghypervalent iodine compounds as oxidant reagents and dibenzenesulfonimides as nitrogen source under room temperature without metal *** the same time,we also found an interesting conversion for the hypervalent iodine compounds mediated C-O formation at C-5 position using dibenzenesulfonhydrazines（thissection of work will be published in the next three months）.

关键词： 8-amidoquinolines hypervalentiodine compounds C-H functionalization metal-free

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Signal Transduction and Targeted Therapy 2023年第2期8卷 795-812页

作者： Bo Zhang jiaqi Sun Yeshuang Yuan dezhong ji Yeting Sun Yudong Liu Shengjie Li Xingxing Zhu Xunyao Wu jin Hu Qiu Xie Ling Wu Lulu Liu Boyang Cheng Yuanjie Zhang Lingjuan jiang Lidan Zhao Fei Yu Wei Song Min Wang Yue Xu Shiliang Ma Yunyun Fei Lihe Zhang Demin Zhou Xuan Zhang State Key Laboratory of Complex Severe and Rare Diseases Peking Union Medical College HospitalDepartment of RheumatologyBeijing HospitalNational Center of GerontologyInstitute of Geriatric MedicineChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100730China State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China Department of Rheumatology Beijing HospitalNational Center of GerontologyInstitute of Geriatric MedicineClinical Immunology CenterGraduate School of Peking Union Medical CollegeChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100730China Department of Rheumatology and Clinical Immunology Peking Union Medical College HospitalChinese Academy of Medical Sciences and Peking Union Medical CollegeThe Ministry of Education Key LaboratoryBeijing 100730China

Interleukin-2(IL-2)is a pleiotropic cytokine that orchestrates bidirectional immune responses via regulatory T cells(Tregs)and effector cells,leading to paradoxical ***,we report a strategy that exploited genetic code expansion-guided incorporation of the latent bioreactive artificial amino acid fluorosulfate-L-tyrosine(FSY)into IL-2 for proximity-enabled covalent binding to IL-2Rαto selectively promote Treg *** found that FSY-bearing IL-2 variants,such as L72-FSY,covalently bound to IL-2Rαvia sulfur-fluoride exchange when in proximity,resulting in persistent recycling of IL-2 and selectively promoting the expansion of Tregs but not effector *** assessment of L72-FSY-expanded Tregs demonstrated that L72-FSY maintained Tregs in a central memory phenotype without driving terminal differentiation,as demonstrated by simultaneously attenuated expression of lymphocyte activation gene-3(LAG-3)and enhanced expression of programmed cell death protein-1(PD-1).Subcutaneous administration of L72-FSY in murine models of pristane-induced lupus and graft-versus-host disease(GvHD)resulted in enhanced and sustained therapeutic efficacy compared with wild-type IL-2 *** efficacy of L72-FSY was further improved by N-terminal PEGylation,which increased its circulatory retention for preferential and sustained *** proximity-enabled covalent binding strategy may accelerate the development of pleiotropic cytokines as a new class of immunomodulatory therapies.

关键词： sustained proximity consequences

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高COD枣加工生产废水预处理实验

水处理技术 2018年第4期44卷 66-68页

作者：李德钟冀雅琬刘伟王娜刘俊良河北农业大学城乡建设学院保定市排水总公司鲁岗污水处理厂河北保定071000

针对枣加工生产废水具有COD高、pH低等特点,以聚合氯化铝(PAC)为混凝剂,聚丙烯酰胺(PAM)为助凝剂,通过单因素和正交实验预处理枣加工生产废水,结果表明,优化混凝条件为:混凝剂PAC投加量120mg/L,助凝剂PAM投加量15mg/L,pH为7,混凝时间为2... 详细信息

针对枣加工生产废水具有COD高、pH低等特点,以聚合氯化铝(PAC)为混凝剂,聚丙烯酰胺(PAM)为助凝剂,通过单因素和正交实验预处理枣加工生产废水,结果表明,优化混凝条件为:混凝剂PAC投加量120mg/L,助凝剂PAM投加量15mg/L,pH为7,混凝时间为20min。在此条件下,处理后废水的COD为46.22g/L,浊度28NTU,COD和浊度的去除率分别为54%和88%。可保证后续生物处理的顺利进行。

关键词：枣加工生产废水预处理聚合氯化铝正交实验

Evaluation of hollow fiber T-type zeolite membrane modules for ethanol dehydration

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Chinese Journal of Chemical Engineering 2017年第5期25卷 581-586页

作者： Xuerui Wang ji jiang dezhong Liu Youquan Xue Chun Zhang Xuehong Gu State Key Laboratory of Materials-Oriented Chemical Engineering College of Chemistry and Chemical EngineeringThe Synergetic Innovation Center for Advanced MaterialsNanjing Tech University

This work presents the design of hollow fiber T-type zeolite membrane modules with different geometric configurations. The module performances were evaluated by pervaporation dehydration of ethanol/water mixtures. Strong concentration polarization was found for the modules with big membrane bundles. The concentration polarization was enhanced at high temperature due to the higher water permeation flux. The increase of feed flow could improve water permeation flux for the membrane modules with small membrane *** fluid dynamics was used to visualize the flow field distribution inside of the modules with different configurations. The membrane module with seven bundles exhibited highest separation efficiency due to the uniform distribution of flow rate. The packing density could be 10 times higher than that of the tubular membrane module. The hollow fiber membrane module exhibited good stability for ethanol dehydration.

关键词： Hollow fiber Module Pervaporation T-type zeolite membrane

遗传算法动态修正核素大气扩散模型的适应度函数研究

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核技术 2014年第4期37卷 58-63页

作者：吉志龙马元巍王德忠上海交通大学核科学与工程学院上海200240

放射性核素大气扩散模型中,基于示踪实验获得的经验扩散参数依赖于具体的实验条件,在事故条件下,由于风场、大气湍流、地表状态等与实验条件存在差异,经验扩散参数难以准确反映实际扩散过程。为了弥补这一不足,可以以经验参数为先验值,... 详细信息

放射性核素大气扩散模型中,基于示踪实验获得的经验扩散参数依赖于具体的实验条件,在事故条件下,由于风场、大气湍流、地表状态等与实验条件存在差异,经验扩散参数难以准确反映实际扩散过程。为了弥补这一不足,可以以经验参数为先验值,使用实际观测数据对其进行实时动态修正。本文基于遗传算法,建立动态修正模型,通过数值模拟得到4种适应度函数对修正结果的影响。结果表明,根据观测误差设置不同权重的适应度函数修正效果更好。在此基础上,使用Kincaid实验数据集进行模型预测能力的验证,结果表明,使用遗传算法对拉格朗日扩散模型中的扩散参数进行修正,可明显提高扩散模型的预测能力。

关键词：大气扩散模型遗传算法适应度函数数值模拟核事故后果评价

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一种基于虚拟化平台的安全外包技术研究

信息网络安全 2018年第5期 82-88页

作者：李月姜玮季佳华段德忠上海出入境检验检疫局上海200135 北京信城通数码科技有限公司北京100070

当前,随着互联网技术的发展和信息安全建设的推进,政府选择服务外包已经成为大势所趋,而对服务外包的有效监督和管理将成为保障信息安全的重要手段。信息化合作开发运维面临技术手段防不住、管理制度难保护的困境和难题。文章提出了一... 详细信息

当前,随着互联网技术的发展和信息安全建设的推进,政府选择服务外包已经成为大势所趋,而对服务外包的有效监督和管理将成为保障信息安全的重要手段。信息化合作开发运维面临技术手段防不住、管理制度难保护的困境和难题。文章提出了一种创新的信息技术外包管理思路,通过将零客户终端与虚拟化平台技术结合,定制配套的运维桌面,研发配套的管理系统,实现技术及管理双管齐下。

关键词：信息安全外包管理虚拟化平台零客户端

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辊轮密封系统的综合改造

润滑与密封 2010年第5期35卷 103-105页

作者：季玉茹王德忠吉林化工学院吉林省吉林市132022

分析密封结构、工作介质腐蚀性、粉体静压力对辊轮组合密封的影响,讨论组合密封中迷宫密封与唇形密封的失效原因,给出迷宫密封结构和密封方向的改进方案、唇形密封装配的方法和环形压紧弹簧材料的改造措施及方法,并给出静轴的防腐措施... 详细信息

分析密封结构、工作介质腐蚀性、粉体静压力对辊轮组合密封的影响,讨论组合密封中迷宫密封与唇形密封的失效原因,给出迷宫密封结构和密封方向的改进方案、唇形密封装配的方法和环形压紧弹簧材料的改造措施及方法,并给出静轴的防腐措施及其加工要求。实践证明:采取这些方案和措施进行系统改造后生产运行成本降低,密封的使用寿命大大提高。

关键词：腐蚀性迷宫密封唇形密封

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造粒机辊轮密封失效原因的分析

润滑与密封 2009年第5期34卷 103-105页

作者：王德忠季玉茹吉林化工学院吉林吉林市132022

分析了密封结构、工作介质、粉体静压力对辊轮组合密封的影响,讨论了组合密封中迷宫密封与唇型密封的失效原因,给出了改进的措施及方法。静压力使得粉体物料进入阶梯型迷宫密封形成堆积,并堆积到唇型密封圈的"唇口"而形成内外压力差,当... 详细信息

分析了密封结构、工作介质、粉体静压力对辊轮组合密封的影响,讨论了组合密封中迷宫密封与唇型密封的失效原因,给出了改进的措施及方法。静压力使得粉体物料进入阶梯型迷宫密封形成堆积,并堆积到唇型密封圈的"唇口"而形成内外压力差,当压力差超过设计压力差时,唇型密封圈失效;工作介质的腐蚀性使密封面、静轴和环型螺旋弹簧严重锈蚀,导致辊轮的密封失效。通过改变阶梯型迷宫密封的结构,增大密封压力,提高密封面、静轴和环型螺旋弹簧的耐蚀性能以及改进布料器的设计等可延长辊轮组合密封的寿命。

关键词：失效迷宫密封唇型密封圈