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Design,synthesis and antimycobacterial activity of novel nitrobenzamide derivatives

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chinese Chemical Letters 2019年第2期30卷 413-416页

作者： Hongjian Wang Kai Lv Xiaoning Li Bo Wang Apeng Wang Zeyu Tao Yunhe Geng Bin Wang Menghao Huang Mingliang Liu Huiyuan Guo Yu Lu Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences Peking Union Medical College Beijing Key Laboratory of drug Resistance Tuberculosis Research Department of Pharmacology Beijing Tuberculosis and Thoracic Tumor Research InstituteBeijing Chest Hospital Capital Medical University division of Gastroenterology and Hepatology Department of Medicine Indiana University School of Medicine

We report herein the design and synthesis of a series of novel nitrobenzamide derivatives. Results reveal that many of them display considerable in vitro antitubercular activity. Four N-benzyl or N- (pyridine-2-yl)methyl 3,5-dinitrobenzamides A6, All, Cl and C4 have not only the same excellent MIC values ofdrug-sensitive MTB strain H37 Rv and two drug-resistant clinical isolates as PBTZ169 and the lead 1, but also acceptable safety indices (SI > 1500), opening a new direction for further development.

关键词： Nitrobenzamides Synthesis Antimycobacterial activity Tuberculosis

Nonlinear Dynamic Responses of Tension Leg Platform with Slack-Taut Tether

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China Ocean Engineering 2009年第1期23卷 37-48页

作者：曾晓辉李宣文刘洋吴应湘 division of Engineering Sciences Institute of MechanicsChinese Academy of Sciences

The slack-taut state of tether is a particular adverse circumstance, which may influence the normal operation state of tension leg platform （TLP）. The dynamic responses of TLP with slack-taut tether are studied with consideration of several nonlinear factors introduced by large amplitude motions. The time histories of stresses of tethers of a typical TLP in slack- taut state are given. In addition, the sensitivities of slack to stiffness and mass are investigated by varying the stiffness of tether and mass of TLP. It is found that slack is sensitive to the mass of TLP. The critical curved surfaces （ over which indicates the slack） for the increase of mass are obtained.

关键词： tension leg platform slack-taut large amplitude motions sensitivity analysis

An Approximate Method for Calculation of Fluid Force and Response of A Circular Cylinder at Lock-in

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China Ocean Engineering 2008年第3期22卷 371-384页

作者：王艺 division of Engineering Sciences Institute of MechanicsChinese Academy of Sciences

In this paper, equations calculating lift force of a rigid circular cylinder at lock-in in uniform flow are deduced in detail. Besides, equations calculating the lift force on a long flexible circular cylinder at lock-in are deduced based on mode analysis of a multi-degree freedom system. The simplified forms of these equations are also given. Furthemore, an approximate method to predict the forces and response of rigid circular cylinders and long flexible circular cylinders at lock-in is introduced in the case of low mass-damping ratio. A method to eliminate one deficiency of these equations is introduced. Comparison with experimental results shows the effectiveness of this approximate method.

关键词： vortex-induced vibraton circular cylinder lock-in phase lift amplitude

A potent PGK1 antagonist reveals PGK1 regulates the production of IL-1βand IL-6

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Acta Pharmaceutica Sinica B 2022年第11期12卷 4180-4192页

作者： Liping Liao Wenzhen Dang Tingting Lin Jinghua Yu Tonghai Liu Wen Li Senhao Xiao Lei Feng Jing Huang Rong Fu Jiacheng Li Liping Liu Mingchen Wang Hongru Tao Hualiang Jiang Kaixian Chen Xingxing Diao Bing Zhou Xiaoyan Shen Cheng Luo Deparment of pharmacology&the Key Laboratory of Smart drug Delivery Ministry of EeducaionSchool of PharmacyFudan UniversityShanghai 201203China State Key Laboratory of drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of chinese Academy of Sciences Bejing 10049China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUniversity of Chinese Academy of SciencesHangzhou 310024China School of Pharmaceutical Sciences Zhejiang Chinese Medical UniversityHangzhou 310053China

Glycolytic metabolism enzymes have been implicated in the immunometabolism field through changes in metabolic status. PGK1 is a catalytic enzyme in the glycolytic pathway. Here, we set up a high-throughput screen platform to identify PGK1 inhibitors. DC-PGKI is an ATPcompetitive inhibitor of PGK1 with an affinity of Kd= 99.08 nmol/L. DC-PGKI stabilizes PGK1in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. In addition,DC-PGKI unveils that PGK1 regulates production of IL-1β and IL-6 in LPS-stimulated ***, inhibition of PGK1 with DC-PGKI results in NRF2(nuclear factor-erythroid factor 2-related factor 2, NFE2L2) accumulation, then NRF2 translocates to the nucleus and binds to the proximity region of Il-1β and Il-6 genes, and inhibits LPS-induced expression of these genes. DC-PGKI ameliorates colitis in the dextran sulfate sodium(DSS)-induced colitis mouse model. These data support PGK1 as a regulator of macrophages and suggest potential utility of PGK1 inhibitors in the treatment of inflammatory bowel disease.

关键词： Glycolysis Phosphoglycerate kinasel Macrophages NRF2 Inflammation

Unbiased screening reveals that blocking exportin 1 overcomes resistance to PI3Kαinhibition in breast cancer

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Signal Transduction and Targeted Therapy 2019年第1期4卷 211-213页

作者： Xue-Ling Liu Bo-Bo Wang Yi Wang Yu-Xiang Wang Chun-hao Yang Cun Tan Xi Zhang Qiao-jun He Jian Ding Ling-Hua Meng division of Anti-Tumor pharmacology Shanghai Institute of Materia MedicaChinese Academy of Sciences501 Haike RoadShanghai201203China Zhejiang Province Key Laboratory for drug Evaluation and Clinical Research First Affiliated HospitalSchool of MedicineZhejiang University79 Qingchun RoadHangzhou310003China Zhejiang Province Key Laboratory of Anti-Cancer drug Research College of Pharmaceutical SciencesZhejiang University866 Yuhangtang RoadHangzhou310058China University of chinese Academy of Sciences No.19A Yuquan RoadBeijing100049China Department of Medicinal Chemistry Shanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203China division of Anti-Tumor pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203China

Dear Editor,Targeting PI3K is a promising approach for cancer therapy,and the PI3Kα-selective inhibitor alpelisib has been approved for breast cancer treatment.1,2,3 However,the development of acquired resistance poses a significant clinical *** of PTEN and activation of mTOR,CDK4/6,or PIM have been reported to mediate acquired resistance to alpelisib.4,5,6,7 The mechanisms leading to resistance to PI3Kαinhibitors appear to be different under different circumstances,and the aforementioned strategies may be beneficial for a particular group of *** strategies to overcome acquired resistance in a broad spectrum of patients need to be discovered.

关键词： PI3K breast cancer

MULTIVARIATE FOURIER SERIES OVER A CLASS OF NON TENSOR-PRODUCT PARTITION DOMAINS

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Journal of Computational Mathematics 2003年第1期21卷 53-62页

作者： Jiachang Sun(Parallel Computing division, Institute of Software, chinese Academy of Sciences, Beijing 100080, China) Parallel Computing division Institute of Software Chinese Academy of Sciences 北京 100080

This paper finds a way to extend the well-known Fourier methods, to so-called n+1 directions partition domains in n-dimension. In particular, in 2-D and 3-D cases, we study Fourier methods over 3-direction parallel hexagon partitions and 4-direction parallel parallelogram dodecahedron partitions, respectively. It has pointed that, the most concepts and results of Fourier methods on tensor-product case, such as periodicity,orthogonality of Fourier basis system, partial sum of Fourier series and its approximation behavior, can be moved on the new non tensor-product partition case.

关键词： Multivariate Fourier methods Non tensor-product partitions Multivariate Fourier series

Sensitivity analysis of dimensionless parameters for physical simulation of water-flooding reservoir

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Science China(Technological Sciences) 2005年第4期48卷 441-453页

作者： BAI Yuhu LI Jiachun ZHOU Jifu division of Engineering Sciences Institute of Mechanics Chinese Academy of Sciences Beijing 100080 China Division of Engineering Sciences Institute of Mechanics Chinese Academy of Sciences Beijing 100080 China Division of Engineering Sciences Institute of Mechanics Chinese Academy of Sciences Beijing 100080 China

A numerical approach to optimize dimensionless parameters of water-flooding porous media flows is proposed based on the analysis of the sensitivity factor defined as the variation ration of a target function with respect to the variation of dimensionless parameters. A complete set of scaling criteria for water-flooding reservoir of five-spot well pattern case is derived from the 3-D governing equations, involving the gravitational force, the capillary force and the compressibility of water, oil and rock. By using this approach, we have estimated the influences of each dimensionless parameter on experimental results, and thus sorting out the dominant ones with larger sensitivity factors ranging from 10?4 to 100.

关键词： sensitivity analysis, model scaling, numerical experiment, water-flooding, two-phase flow.

Mechanical,Microstructural and Tribological Properties of Reactive Magnetron Sputtered Cr-Mo-N Films

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Journal of Materials Science & Technology 2015年第1期31卷 55-64页

作者： Dongli Qi Hao Lei Tiegang Wang Zhiliang Pei Jun Gong Chao Sun Surface Engineering of Materials division Institute of Metal ResearchChinese Academy of Sciences

The Cr-Mo-N films were deposited on high speed steel（HSS） substrates by a DC reactive magnetron sputtering equipment coupled with two horizontal magnetron *** effects of substrate negative bias voltage（Vb）,substrate temperature（Ts） and gas flow ratio（R= N2/（N2+ Ar）） on the microstructure,morphology,as well as the mechanical and tribological properties of the Cr-Mo-N films were investigated by virtue of X-ray diffraction（XRD） analysis,X-ray photoelectron spectroscopy（XPS）,field emission scanning electron microscopy（FESEM）,atomic force microscopy（AFM）,nano-indentation test,ball-on-disk tribometer,and Rockwell indenter et *** increasing Vbto-100 V,the preferred orientation of the films changed from（111） to（200） and their mechanical and tribological properties were improved gradually,*** was also found that Tsgave a significant effect on mechanical property *** the Tsreached 300 ℃,the film obtained the highest hardness and effective elastic modulus of approximately 30.1 and 420.5 GPa,respectively and its critical load increased to about 54 *** increasing R,the phase transformation from body-centered-cubic（bcc） Cr and hexagonal CrMoNxmultiphase to single face-centered-cubic（fcc） solid solution phase was *** correlations between values of hardness（H）,effective elastic modulus（E*）,HIE*,H3/E*2,elastic recovery（1/14） and tribological properties of the films were also *** results showed that the elastic recovery played an important role in the tribological behavior.

关键词： Cr-Mo-N films DC magnetron sputtering Hardness Cri

Sinomenine ester derivative inhibits glioblastoma by inducing mitochondria-dependent apoptosis and autophagy by PI3K/AKT/mTOR and AMPK/mTOR pathway

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Acta Pharmaceutica Sinica B 2021年第11期11卷 3465-3480页

作者： Xiangjin Zheng Wan Li Huanli Xu Jinyi Liu Liwen Ren Yihui Yang Sha Li Jinhua Wang Tengfei Ji Guanhua Du The State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Science and Peking Union Medical CollegeBeijing 100050China Key Laboratory of drug Target Research and drug Screen Institute of Materia MedicaChinese Academy of Medical Science and Peking Union Medical CollegeBeijing 100050China Department of pharmacology Capital Medical UniversityBeijing 100069China

Glioblastoma multiforme(GBM)in the central nervous system is the most lethal advanced glioma and currently there is no effective treatment for *** of sinomenine,an alkaloid from the chinese medicinal plant,Sinomenium acutum,showed that it had inhibitory effects on several kinds of ***,we synthesized a sinomenine derivative,sino-wcj-33(SW33),tested it for antitumor activity on GBM and explored the underlying ***33 significantly inhibited proliferation and colony formation of GBM and reduced migration and invasion of U87 and U251 *** also arrested the cell cycle at G2/M phase and induced mitochondria-dependent *** gene enrichment analysis and pathway validation showed that SW33 exerted anti-GBM effects by regulating PI3 K/AKT and AMPK signaling pathways and significantly suppressed tumorigenicity with no obvious adverse effects on the ***33 also induced autophagy through the PI3 K/AKT/mTOR and AMPK/mTOR ***,SW33 appears to be a promising drug for treating GBM effectively and safely.

关键词： SW33 GBM G2/M phase Apoptosis Autophagy mTOR Anti-inflammation Safety