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Small molecule conjugates with selective estrogen receptor β agonism promote anti-aging benefits in metabolism and skin recovery

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Acta Pharmaceutica Sinica B 2024年第5期14卷 2137-2152页

作者： Tarik Zahr Vijay K.Boda Jian Ge Lexiang Yu zhongzhi wu Jianwen Que Wei Li Li Qiang Naomi Berrie Diabetes Center Columbia UniversityNew YorkNY 10032USA Department of Molecular Pharmacology and Therapeutics Columbia UniversityNew YorkNY 10032USA Department of Pharmaceutical Sciences College of PharmacyUniversity of Tennessee Health Science CenterMemphisTN 38163USA Drug Discovery Center College of PharmacyUniversity of Tennessee Health Science CenterMemphisTN 38163USA Division of Digestive and Liver Diseases Columbia UniversityNew YorkNY 10032USA Center for Human Development Columbia UniversityNew YorkNY 10027USA Department of Pathology and Cell Biology Columbia UniversityNew YorkNY 10032USA Department of Medicine Columbia UniversityNew YorkNY 10032USA

Estrogen is imperative to mammalian reproductivity,metabolism,and ***,the hormone activating estrogen receptor(ERs)αcan cause major safety concerns due to the enrichment of ERαin female tissues and certain *** contrast,ERβis more broadly expressed in metabolic tissues and the ***,it is desirable to generate selective ERβagonist conjugates for maximizing the therapeutic effects of ERs while minimizing the risks of ERα***,we report the design and production of small molecule conjugates containing selective non-steroid ERβagonists Gtx878 or *** of aged mice with our synthesized conjugates improved aging-associated declines in insulin sensitivity,visceral adipose integrity,skeletal muscle function,and skin health,with validation in *** further uncovered the benefits of ERβconjugates in the skin using two inducible skin injury mouse models,showing increased skin basal cell proliferation,epidermal thickness,and wound ***,our ERβ-selective agonist conjugates offer novel therapeutic potential to improve aging-associated conditions and aid in rejuvenating skin health.

关键词： Estrogen receptorβ Aging Metabolism Skin injury Muscle metabolism Small molecule conjugates Regeneration Adiposity

Design,synthesis and biological evaluation of selective survivin inhibitors

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The Journal of Biomedical Research 2019年第2期33卷 82-100页

作者： Min Xiao Yi Xue zhongzhi wu Zi-Ning Lei Jin Wang Zhe-Sheng Chen Wei Li Department of Pharmaceutical Sciences University of Tennessee Health Science Center Department of Pharmaceutical Sciences College of Pharmacy and Health Sciences St.John's University

The differential distribution between cancer cells and normal adult tissues makes survivin a very attractive cancer drug target. We have previously reported a series of novel selective survivin inhibitors with the most potent compound MX 106 reaching nanomolar activity in several cancer cell lines. Further optimization of the MX 106 scaffold leads to the discovery of more potent and more selective survivin inhibitors. Various structural modifications were synthesized and their anticancer activities were evaluated to determine the structure activity relationships for this MX 106 scaffold. In vitro anti-proliferative assays using two human melanoma cell lines showed that several new analogs have improved potency compared to MX 106. Very interestingly, these new analogs generally showed significantly higher potency against P-glycoprotein overexpressed cells compared with the corresponding parental cells, suggesting that these compounds may strongly sensitize tumors that have high expressions of the Pglycoprotein drug efflux pumps. Western blotting analysis confirmed that the new MX 106 analogs maintained their mechanism of actions by selectively suppressing survivin expression level among major inhibitors of apoptotic proteins and induced strong apoptosis in melanoma tumor cells.

关键词： selective survivin inhibitors structure activity relationships melanoma human epidermoid carcinoma colorectal cancer P-glycoprotein drug efflux pumps

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面向民用飞机需求验证的自动化测试技术研究

图学学报 2024年第2期45卷 308-316页

作者：汪澔武仲芝唐剑中国商用飞机有限责任公司北京民用飞机技术研究中心北京102211

在商用飞机全生命周期的研制过程中,需求与概念论证环节作为商用飞机研制的早期环节,将极大地影响整个商用飞机的全生命周期成本。其中功能定义作为需求与概念论证阶段的核心产物之一,以一种统一化、标准化的描述了目标产品一系列的预... 详细信息

在商用飞机全生命周期的研制过程中,需求与概念论证环节作为商用飞机研制的早期环节,将极大地影响整个商用飞机的全生命周期成本。其中功能定义作为需求与概念论证阶段的核心产物之一,以一种统一化、标准化的描述了目标产品一系列的预期行为表达。功能性需求作为功能定义的重点输出产物,决定了商用飞机的核心产品竞争力。基于功能仿真的需求验证作为一种常用的需求质量评价手段,通过建立飞机的测试模型,仿真模拟特定场景下飞机的运行行为,以结果为评判依据确认早期方案设计是否满足需求。然而,在实际面向需求的仿真测试过程中,碍于场景外部环境的多变性,往往会出现“组合爆炸式”的测试用例,极大地增加了测试的规模和成本。为解决上述问题,提出基于模型的测试(MBT)方法,通过基于系统建模语言(SysML)模型自动化生成测试用例,缩短验证过程的周期并保证需求验证的可追溯性。

关键词：需求验证测试用例基于模型的测试 SysML

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如何选用变频器

建筑电气 2009年第3期28卷 3-9页

作者：吴忠智北京中瑞电子系统工程设计院北京市100039

变频器在传动领域应用广泛。对如何正确选用变频器作了全面分析与介绍。包括了解变频器的逆变元件、拓扑电路,变频器对拖动电机的控制方式、负载转矩特性等。在应用变频器时,应考虑变频器的输入输出电流中含有谐波,要选用相应的抑制谐... 详细信息

变频器在传动领域应用广泛。对如何正确选用变频器作了全面分析与介绍。包括了解变频器的逆变元件、拓扑电路,变频器对拖动电机的控制方式、负载转矩特性等。在应用变频器时,应考虑变频器的输入输出电流中含有谐波,要选用相应的抑制谐波的配套设备。

关键词：变频器电力电子器件拓扑电路负载特性谐波

GRAIN BOUNDARY SEGREGATION OF TRACE Sn IN A HIGH INDUCTION ORIENTED SILICON STEEL

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Acta Metallurgica Sinica(English Letters) 1993年第1期6卷 30-35页

作者： ZHAO Yu HE zhongzhi WENG Yuqing wu Baorong Central Iron and Steel Research Institute,Ministry of Metallurgical Industry,Beijing,China Doctorate Student,Department No.2,Central Iron and Steel Research Institute,Ministry of Metallurgical Industry,Beijing 100081,China

When Sn segregated at grain boundaries of high induction oriented silicon steel,no remarka- ble interaction between Sn and other elements was *** the starting temperature of secondary recrystallization,950℃,a certain Sn still segregates at grain *** seems to act as a supplemental inhibitor through grain boundary *** to theoreti- cal analysis,an addition of Sn may decrease the secondary recrystallization temperature of high induction oriented silicon steel,and it is in agreement with the experimental result.

关键词： silicon steel Sn segregation Auger secondary recrystallization

电化学反应性捕集CO_(2)研究进展与挑战

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能源环境保护 2024年第3期38卷 1-12页

作者：武中志刘静怡王茹洁汪黎东华北电力大学环境科学与工程系河北省燃煤电站烟气多污染物协同控制重点实验室河北保定071003

CO_(2)捕集是控制温室气体排放的关键技术之一,电化学CO_(2)还原是关闭人工碳循环的有效途径,但CO_(2)捕集和电化学CO_(2)还原过程均为能源密集型过程。过去的研究将两者视为相互独立的技术和科学领域进行发展。通过直接电解捕集介质(... 详细信息

CO_(2)捕集是控制温室气体排放的关键技术之一,电化学CO_(2)还原是关闭人工碳循环的有效途径,但CO_(2)捕集和电化学CO_(2)还原过程均为能源密集型过程。过去的研究将两者视为相互独立的技术和科学领域进行发展。通过直接电解捕集介质(如胺基富液和碳酸氢盐),将上游的碳捕集和下游的电化学还原过程进行集成耦合,可以避免高能耗的捕获介质再生和CO_(2)释放环节,避免CO_(2)的运输和存储操作,降低整体工艺的运行成本,提升整个碳循环的能量效率和经济效益,为节约能源和经济高效地捕集利用CO_(2)提供了一个潜在的解决方案。总结了目前电化学反应性捕集CO_(2)的研究进展,论述了在电极和电解质方面取得的成果,讨论了影响集成电解效率的限制因素,并分析了各类因素的潜在影响机制和可能的反应路径。最后,强调了直接电化学还原捕集介质领域的主要挑战和机遇,并对未来耦合碳捕集与电化学利用过程的发展进行展望。

关键词： CO_(2)捕集电化学还原捕集介质电化学反应性捕集CO_(2) 电解效率 CO_(2)捕集与利用集成

柴油十六烷值改进剂QT-01的研制、添加效果及应用试验

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石油炼制 1989年第9期20卷 31-36页

作者：高鸿顺岳秀英张忠智吴继敏李守莉齐鲁石化公司研究院

本文介绍了“混酸法”合成柴油十六烷值改进剂——硝酸烷基酯的一般方法。就国内不同产地的柴油进行了添加试验,不同产地的柴油对十六烷值改进剂 QT—01的感受性不同。一般来说,添加0.1V%QT—01可使柴油十六烷值增加2—5个单位,添加0.2V... 详细信息

本文介绍了“混酸法”合成柴油十六烷值改进剂——硝酸烷基酯的一般方法。就国内不同产地的柴油进行了添加试验,不同产地的柴油对十六烷值改进剂 QT—01的感受性不同。一般来说,添加0.1V%QT—01可使柴油十六烷值增加2—5个单位,添加0.2V%可增加4—7个单位,添加0.3V%增加6—9个单位。同时,进行了台架及燃烧分析试验、油品储存试验和两万公里行车试验。试验表明:加剂(QT—01)0号柴油和标准0号柴油,在使用与储存性能上基本无差别。QT—01十六烷值改进剂的研制成功,为改善柴油质量开辟了一条新的途径。

关键词：柴油十六烷值改进剂 QT-01

DNA Binding Properties and Cytotoxic Activities of Two Trinuclear Ruthenium（Ⅱ） Polypyridyl Complexes

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Chemical Research in Chinese Universities 2014年第3期30卷 461-467页

作者： XU Li CHEN Yu WEI Hui wu Wenshan LI zhongzhi LIN Yiwei CHAO Hui JI Liangnian School of Chemistry and Chemical Engineering Guangdong Pharmaceutical University Zhongshan 528458 P R. China State Key Laboratory of Biocontrol Department of Biochemistry College of Life Sciences Sun Yat-sen University Guangzhou 510006 P. R. China School of Chemistry and Chemical Engineering Sun Yat-sen University Guangzhou 510275 P. R. China

The interactions between two trinuclear Ru（II） complexes and calf thymus DNA（CT DNA） were studied via absorption spectroscopy, reverse salt titrations, binding stoichiometry, DNA melting experiments, as well as viscosity measurement. The results indicate that complexes 1 and 2 bind to DNA via the interaction of the planar π-delocalized system of the complexes with intrinsic binding constants of 4.18 × 10^5 and 3.85 × 10^6 L/tool, respectively, and non-electrostatic binding free energy makes a predominant contribution to the binding free energy. The in vitro cytotoxic activity of complexes 1 and 2 was evaluated by the MTT[3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyl- 2H-tetrazolium bromide] method. Complex I shows higher anticancer potency than complex 2 against four tumor cell lines. Further mechanism study indicates that complexes 1 and 2 can cause cell cycle arrest in the G2/M phase.

关键词： Ruthenium(Ⅱ) complex DNA binding Cell cycle

Phase calibration for integrated optical phased arrays using artificial neural network with resolved phase ambiguity

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Photonics Research 2022年第2期10卷 347-356页

作者： Lemeng Leng Zhaobang Zeng Guihan wu zhongzhi Lin Xiang Ji Zhiyuan Shi Wei Jiang College of Engineering and Applied Sciences Nanjing UniversityNanjing 210093China Key Laboratory of Intelligent Optical Sensing and Manipulation Ministry of EducationNanjing UniversityNanjing 210093China Jiangsu Key Laboratory of Artificial Functional Materials Nanjing UniversityNanjing 210093China National Laboratory of Solid-State Microstructures Nanjing 210093China

Phase calibration for optical phased arrays(OPAs) is a key process to compensate for the phase deviation and retrieve the initial working state. Conventional calibration approaches based on iterative optimization algorithms are tedious and time-consuming. The essential difficulty of such a problem is to inversely solve for the phase error distribution among OPA elements from the far-field pattern of an OPA. Deep-learning-based technology might offer an alternative approach without explicitly knowing the inverse solution. However, we find that the phase ambiguities, including conjugate ambiguity and periodic ambiguity, severely deter the accuracy and efficacy of deep-learning-based calibration. Device-physics-based analysis reveals the causes of the phase ambiguities, which can be resolved by creating a tailored artificial neural network with phase-masked far-field patterns in a conjugate pair and constructing a periodic continuity-preserving loss function. Through the ambiguity-resolved neural network, we can extract phase error distribution in an OPA and calibrate the device in a rapid, noniterative manner from the measured far-field patterns. The proposed approach is experimentally verified. Pure main-beam profiles with >12 dB sidelobe suppression ratios are observed. This approach can help overcome a crucial bottleneck for the further advance of OPAs in a variety of applications such as lidar.

关键词： resolved conjugate inverse