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Synthesis and antiviral activity of 4H-[1,2,5]oxadiazolo-[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides

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Chinese Chemical Letters 2009年第4期20卷 404-406页

作者： Jing Bo Shi Jing Gao ya ping wang Qi Zheng yao School of Pharmacy China Pharmaceutical University Nanjing 210009 China School of Pharmacy Anhui Medical University Hefei 230032 China School of Pharmaceutical Science Jiangsu University Zhenjiang 212013 China Zhaoke Pharmaceutical Company Limited Hefei 230088 China

A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compound... 详细信息

关键词： Oxadiazolo[3,4-d]pyrimidine nucleoside Antivirus Synthesis

SPOP negatively regulates Toll-like receptor-induced inflammation by disrupting MyD88 self-association

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Cellular & Molecular Immunology 2021年第7期18卷 1708-1717页

作者： Yun-Hong Hu yang wang Fei wang yan-Ming Dong Wan-Ling Jiang ya-ping wang Xing Zhong Li-Xin Ma State Key Laboratory of Biocatalysis and Enzyme Engineering School of Life SciencesHubei UniversityWuhan430062China School of Biological and Chemical Engineering College of ZhixingHubei UniversityWuhan430011China

Toll-like receptor(TLR)signaling pathways need to be tightly controlled to avoid excessive inflammation and unwanted damage to the *** differentiation primary response gene 88(MyD88)is a critical adaptor of TLR ***,we identified the speckle-type POZ protein(SPOP)as a MyD88-associated *** was recruited to MyD88 following TLR4 ***4 activation also caused the translocation of SPOP from the nucleus to the *** depletion promoted the aggregation of MyD88 and recruitment of the downstream signaling kinases IRAK4,IRAK1 and ***,overexpression of SPOP inhibited the TLR4-mediated activation of NF-κB and production of inflammatory cytokines,whereas SPOP depletion had the opposite ***,knockdown of SPOP increased MyD88 aggregation and inflammatory cytokine production upon TLR2,TLR7 and TLR9 *** findings reveal a mechanism by which MyD88 is regulated and highlight a role for SPOP in limiting inflammatory responses.

关键词： SPOP MyD88 TLR inflammation

Morinda officinalis oligosaccharides increase serotonin in the brain and ameliorate depression via promoting 5-hydroxytryptophan production in the gut microbiota

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Acta Pharmaceutica Sinica B 2022年第8期12卷 3298-3312页

作者： Zheng-Wei Zhang Chun-Sheng Gao Heng Zhang Jian yang ya-ping wang Li-Bin Pan Hang Yu Chi-Yu He Hai-Bin Luo Zhen-Xiong Zhao Xin-Bo Zhou Yu-Li wang Jie Fu Pei Han Yu-Hui Dong Gang wang Song Li yan wang Jian-Dong Jiang Wu Zhong State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences/Peking Union Medical CollegeBeijing 100050China Beijing Institute of Pharmacology and Toxicology Beijing 100000China Beijing Synchrotron Radiation Facility Institute of High Energy PhysicsChinese Academy of SciencesBeijing 100049China The National Clinical Research Center for Mental Disorders&Beijing Key Laboratory of Mental Disorders Beijing Anding HospitalCapital Medical UniversityBeijing 100088China Advanced Innovation Center for Human Brain Protection Capital Medical UniversityBeijing 100069China School of Pharmaceutical Sciences Hainan UniversityHainan 570228China National Engineering Research Center for the Emergence Drugs Beijing 100000China

Morinda officinalis oligosaccharides(MOO) are an oral drug approved in China for the treatment of depression in China. However, MOO is hardly absorbed so that their anti-depressant mechanism has not been elucidated. Here, we show that oral MOO acted on tryptophan → 5-hydroxytryptophan(5-HTP) → serotonin(5-HT) metabolic pathway in the gut microbiota. MOO could increase tryptophan hydroxylase levels in the gut microbiota which accelerated 5-HTP production from tryptophan;meanwhile, MOO inhibited 5-hydroxytryptophan decarboxylase activity, thus reduced 5-HT generation,and accumulated 5-HTP. The raised 5-HTP from the gut microbiota was absorbed to the blood, and then passed across the blood-brain barrier to improve 5-HT levels in the brain. Additionally, pentasaccharide,as one of the main components in MOO, exerted the significant anti-depressant effect through a mechanism identical to that of MOO. This study reveals for the first time that MOO can alleviate depression via increasing 5-HTP in the gut microbiota.

关键词： Depression Morinda oficinalis oligosaccharides Gut microbiota Tryptophan hydroxylase 5-Hydroxytryptophan decarboxylase 5-Hydroxytryptophan Serotonin Drug metabolism

Ultrasonographic Observation of the Breast in Early Postmenopausal Women during Therapy with Cimicifuga Foetida Extract and Sequential Therapy with Estrogen and Progestin

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Chinese Medical Journal 2015年第8期128卷 1000-1004页

作者： Sharen Gaowa Ai-Jun Sun Ying Jiang Fa-Wei He Ting-ping Zheng ya-ping wang Department of Health Management Peking Union Medical College Hospital Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100730 China Department of Obstetrics and Gynecology Peking Union Medical College Hospital Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100730 China Department of Diagnostic Ultrasound Peking Union Medical College Hospital Chinese Academy o1 Medical Sciences and Peking Union Medical College Beijing 100730. China

Background： It is now recognized that Cimicifuga foetida （C. foetida） extract is effective in alleviating menopausal symptoms. But the durations reported were usually short, The aim of this study was to investigate the effects of C. fl）etida extract therapy and different estrogen and progesterone sequential therapies, on the breasts of early postmenopausal women. Methods： This was a prospective randomized trial. Ninety-six early menopausal women were recruited and randomly assigned into three groups treated with different therapies for 2 years. Patients were given C. foetida extract in Group A, estradiol valerate and medroxyprogesterone acetate in Group B, and estradiol valerate and progesterone in Group C. Ultrasonography was used to monitor changes in breast during treatment. Results： In comparing breast glandular section thickness before and after 1 and 2 years of treatment, no significant difference was observed in Group A （11.97 ± 2.84 mm vs. 12.09 ± 2.58 mm and 12.61 ± 3.73 mm, P 〉 0.05）; in Group B glandular section thickness had increased significantly （10.98 ± 2.34 mm vs. 11.84± 2.72 mm and 11.90 ± 3.33 mm, P 〈 0.05） after treatment, the same as Group C （ 11.56 ± 3.03 mm vs. 12.5 ± 3.57 mm and 12.22 ± 4.39 mm P 〈 0.05）. In comparing breast duct width betbre and after 1 and 2 years of treatment, no significant difference was seen in Group A （1.07 ± 0.19 mm vs. 1.02 ±0.18 mm and 0.98 ± 0.21 mm, P 〉 0.05）; in Group B the duct width had a downward trend after treatment （0.99 ± 0.14 mm vs. 0.96 ± 0.22 mm and 0.90 ± 0.18 mm, P 〈 0.05）, the same as Group C （ 1.07 ± 0.20 mm vs. 1.02 ± 0.17 mm and 0.91 ± 0.19 mm, P 〈 0.05）. The nodules detected before treatment had disappeared after 1 -year of treatment or exhibited no distinct changes in the three groups. However, new breast nodules had appeared after 2 years of treatment： There was one case in Group A, two cases in Group B and four cases in Group C, with breast hyperplasia after the molybdenum target check. Conclu

关键词： Breast Cimicifuga Foetida Extract Hormone Replacement Therapy Ultrasound

A Planning Method for Operational Test of UAV Swarm Based on Mission Reliability

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Computer Modeling in Engineering & Sciences 2024年第8期140卷 1889-1918页

作者： Jingyu wang ping Jiang Jianjun Qi College of Systems Engineering National University of Defense TechnologyChangsha410073China Beijing Special Engineering Design Institution Beijing100028China

The unmanned aerial vehicle(UAV)swarm plays an increasingly important role in the modern battlefield,and the UAV swarm operational test is a vital means to validate the combat effectiveness of the UAV *** to the high cost and long duration of operational tests,it is essential to plan the test in *** solve the problem of planning UAV swarm operational test,this study considers the multi-stage feature of a UAV swarm mission,composed of launch,flight and combat stages,and proposes a method to find test plans that can maximize mission ***,a multi-stage mission reliability model for a UAV swarm is proposed to ensure successful implementation of the mission.A multi-objective integer optimization method that considers both mission reliability and cost is then formulated to obtain the optimal test *** study first constructs a mission reliability model for the UAV swarm in the combat ***,the launch stage and flight stage are integrated to develop a complete PMS(Phased Mission Systems)reliability ***,the Binary Decision Diagrams(BDD)and Multi Objective Quantum Particle Swarm Optimization(MOQPSO)methods are proposed to solve the *** optimal plans considering both reliability and cost are *** proposed model supports the planning of UAV swarm operational tests and represents a meaningful exploration of UAV swarm test planning.

关键词： UAV swarm PMS MOQPSO BDD mission reliability operational test planning

Identifying Brand Consistency by Product Differentiation Using CNN

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Computer Modeling in Engineering & Sciences 2024年第7期140卷 685-709页

作者： Hung-Hsiang wang Chih-ping Chen Department of Industrial Design National Taipei University of TechnologyTaipeiTaiwan Department of Product Design Ming Chuan UniversityTaoyuanTaiwan

This paper presents a new method of using a convolutional neural network(CNN)in machine learning to identify brand consistency by product appearance *** Experiment 1,we collected fifty mouse devices from the past thirty-five years from a renowned company to build a dataset consisting of product pictures with pre-defined design features of their appearance and *** show that it is a challenge to distinguish periods for the subtle evolution of themouse devices with such traditionalmethods as time series analysis and principal component analysis(PCA).In Experiment 2,we applied deep learning to predict the extent to which the product appearance variation ofmouse devices of various *** investigation collected 6,042 images ofmouse devices and divided theminto the Early Stage and the Late *** show the highest accuracy of 81.4%with the CNNmodel,and the evaluation score of brand style consistency is 0.36,implying that the brand consistency score converted by the CNN accuracy rate is not always perfect in the real *** relationship between product appearance variation,brand style consistency,and evaluation score is beneficial for predicting new product styles and future product style *** addition,the CNN heat maps highlight the critical areas of design features of different styles,providing alternative clues related to the blurred *** study provides insights into practical problems for designers,manufacturers,and marketers in product *** not only contributes to the scientific understanding of design development,but also provides industry professionals with practical tools and methods to improve the design process and maintain brand *** can use these techniques to find features that influence brand ***,capture these features as innovative design elements and maintain core brand values.

关键词： Machine learning product differentiation brand consistency principal component analysis convolutional neural network computer mouse

Multi-functional Hollow Structures for Intelligent Drug Delivery

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Chemical Research in Chinese Universities 2024年第3期40卷 394-412页

作者： HOU ping yaNG Nailiang wang Dan State Key Laboratory of Biochemical Engineering Institute of Process EngineeringChinese Academy of SciencesBeijing 100190P.R.China School of Chemical Engineering University of Chinese Academy of SciencesBeijing 100049P.R.China Key Laboratory of Biopharmaceutical Preparation and Delivery Chinese Academy of SciencesBeijing 100049P.R.China

Multi-fountional hollow structures have emerged as promising platforms for intelligent drug delivery due to their unique properties,such as high loading capacities and programmed drug *** particular,hollow multishell structures(HoMSs)with multilevel shell and space can regulate the molecular-level interaction between drugs and materials,so as to achieve the temporal-spatial order and sequential release of *** anisotropic hollow structures can control the drug diffusion process by inducing the macroscopic interface flow through autonomous movement,realizing the targeted drug transport and *** this paper,a key focus will be HoMSs with their temporal-ordered architectures and anisotropic hollow carriers with directional *** synthesis mechanisms,structure-property relationships,smartly programmed drug delivery and biomedical applications will be discussed,providing insights into designing next-generation intelligent drug carriers.

关键词： Hollow multishell structure Anisotropic hollow structure Intelligent drug carrier Temporal-spatial order Directional movement

A novel and efficient route for the preparation of atorvastatin

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Chinese Chemical Letters 2011年第10期22卷 1159-1162页

作者： Jian Gao yang Hui Guo ya ping wang Xiang Jing wang Wen Sheng Xiang Department of Biochemical Engineering Northeast Agricultural University Harbin 150030 China Zhejiang Hisun Pharmaceutical Co. Ltd. Taizhou 318000 China

A novel and efficient synthetic method of atorvastatin was *** key step of the synthesis was the construction of the olefin linkage between the chiral side chain and skeleton via a Horner-Wadsworth-Emmons reaction,resulting in the advanced intermediate of atorvastatin under hydrogenation of the olefin over Pd/*** novel method is more useful for the practical synthesis of atorvastatin than its document reported methods.

关键词： Atorvastatin Horner-Wadsworth-Emmons reaction Synthesis Intermediate

Excited State Intramolecular Proton Transfer of 1-Hydroxyanthraquinone

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Chinese Journal of Chemical Physics 2015年第5期28卷 -页

作者： Si-mei Sun Song Zhang Kai Liu ya-ping wang Miao-miao Zhou Bing Zhang State Key Laboratory of Magnetic Resonance and Atomic and Molecular Physics Wuhan Institute of Physics and Mathematics Chinese Academy of Sciences Wuhan 430071 China

The excited state intra-molecular proton transfer dynamics of 1-hydroxyanthraquinone in solution are investigated by femtosecond transient absorption spectroscopy and quantum chemistry calculations. Two characteristic bands of excited state absorption and stimulated emission are observed in transient absorption spectra with the excitation by the pump wavelength of 400 nm. From the delayed stimulated emission signal, the time scale of the intra-molecular proton transfer is determined to be about 32 fs. The quantum chemistry calculations show that the molecular orbits and the order of the S2 and S1 states are reversal and a conical intersection is demonstrated to exist along the proton transfer coordinate. After proton transfer, the second excited state of tautomer populated via the conical intersection undergoes the internal conversion with ∼200 fs and the following intermolecular energy relaxation with ∼16 ps. The longer component 300 ps can be explained in terms of the relaxation from excited-state tautomer to its ground state. From our observations, two proton transfer pathways via a conical intersection are proposed and the dominated one preserves the molecular orbits.

关键词： Proton transfer Conical intersection Transient absorption spectroscopy 1-Hydroxyanthraquinone