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作者： GUO, Liangqin ZHANG, Hongjun CheN, Ping CLAUSEN, Dane FRADERA, Xavier HAN, Yongxin he, shuwen HUANG, Xianhai PASTERNAK, Alexander PU, Qinglin XIAO, Li

标准号: EP3781142(A1)

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

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广州市谷河黑臭评价及其与裸藻丰度和生物量相关性分析

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环境科学学报 2019年第3期39卷 696-705页

作者：何淑雯于菲刘玉杨翔翡梁仁思蔡逸莉中山大学环境科学与工程学院广州510275 广东省环境污染控制与修复技术重点实验室广州510275

藻类密度增加是黑臭现象发生的重要原因之一.目前的黑臭评价标准缺少藻类等水生生物指标,而黑臭河流中浮游微藻时空特征研究也极少.于2017年秋和2018年冬和春在谷河布设6个样点,采用污染指数法(I_1)和黑臭多因子加权指数法(I_2)评价谷... 详细信息

藻类密度增加是黑臭现象发生的重要原因之一.目前的黑臭评价标准缺少藻类等水生生物指标,而黑臭河流中浮游微藻时空特征研究也极少.于2017年秋和2018年冬和春在谷河布设6个样点,采用污染指数法(I_1)和黑臭多因子加权指数法(I_2)评价谷河黑臭情况,同时调查浮游微藻的丰度和生物量等,并对黑臭评价结果和微藻进行Pearson相关分析.结果表明,I_2指数法更适合评价谷河的黑臭情况;裸藻门丰度与I_2的相关系数较高(r=0.784,p<0.01);裸藻门丰度比例和生物量比例与I_2的相关系数分别为0.750和0.776(p<0.01);裸藻门的种数和裸藻门污染指示种个数与I_2的相关系数均为0.623(p<0.01).裸藻门可能适合于作为评价谷河黑臭的水生生物指标.天然水体中微藻或裸藻与致臭物质的产生等有待深入研究.

关键词：黑臭河流浮游微藻丰度生物量裸藻门谷河

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Total saponins from Panax japonicus mediate the paracrine interaction between adipocytes and macrophages to promote lipolysis in the adipose tissue during aging via the NLRP3 inflammasome/GDF3/ATGL axis

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PHYTOMEDICINE 2025年 136卷 156304页

作者： Xia, Fangqi Hu, Yaqi Wang, Yaqi Xue, Mengzhen Zhu, Leiqi Li, Yuanyang Zhang, Yifan Wang, shuwen Wang, Rui Yuan, Qi he, Yumin Yuan, Ding Zhang, Jihong Yuan, Chengfu China Three Gorges Univ Grade Pharmacol Lab Tradit Chinese Med 3 State Adm Tradit Chinese Med Yichang 443002 Peoples R China China Three Gorges Univ Coll Basic Med Sci Yichang 443002 Peoples R China China Three Gorges Univ Coll Med & Hlth Sci Yichang 443002 Peoples R China China Three Gorges Univ Hubei Clin Res Ctr Funct Digest Dis Tradit Chinese Yichang 443002 Peoples R China China Three Gorges Univ Tradit Chinese Med Hosp Yichang 443002 Peoples R China

Adipocytic lipolysis is strongly related to the increase of visceral fat, decrease of exercise capacity, and various other metabolic syndromes during aging. It is significantly influenced by the paracrine relationship between adipocytes and the adipose tissue macrophages (ATMs), and the cytokines secreted by ATMs have endocrine effects on adjacent tissues. We previously reported that the total saponins from Panax japonicus (TSPJs) can enhance lipid metabolism. In this work, we for the first time proved that TSPJs promoted adipocytic lipolysis by preventing NLRP3 activation in ATMs to inhibit the expression of GDF3. The decrease of GDF3 by TSPJs restored the expression of the adipose triglyceride lipase (ATGL) and phosphorylated hormone-sensitive lipase (p-HSL), both of which are known to decrease with aging. Thus, the NLRP3 inflammasome/GDF3/ATGL axis may be a worthy target in developing future clinical solutions for aging-related obesity.

关键词： Aging Total saponins from Panax japonicus NLRP3 inflammasome Lipolysis

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Novel Acyl Thiourea-Based Hydrophobic Tagging Degraders Exert Potent Anti-Influenza Activity through Two Distinct Endonuclease Polymerase Acidic-Targeted Degradation Pathways

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JOURNAL OF MEDICINAL CheMISTRY 2024年第11期67卷 8791-8816页

作者： Ma, Xiaoyu Wang, Xueyun Chen, Feifei Zou, Wenting Ren, Junrui Xin, Lilan he, Pei Liang, Jinsen Xu, Zhichao Dong, Chune Lan, Ke Wu, shuwen Zhou, Hai-Bing Wuhan Univ Zhongnan Hosp Sch Pharmaceut Sci Dept Hematol Wuhan 430071 Peoples R China Wuhan Univ Coll Life Sci State Key Lab Virol Wuhan 430072 Peoples R China Wuhan Univ Frontier Sci Ctr Immunol & Metab Technol Res Ctr Fluorinated Pharmaceut State Key Lab VirolProv Key Lab Dev Originated Di Wuhan 430071 Peoples R China Wuhan Univ Hubei Prov Engn & Technol Res Ctr Fluorinated Phar Wuhan 430071 Peoples R China

The spread of the influenza virus has caused devastating pandemics and huge economic losses worldwide. Antiviral drugs with diverse action modes are urgently required to overcome the challenges of viral mutation and drug resistance, and targeted protein degradation strategies constitute excellent candidates for this purpose. herein, the first degradation of the influenza virus polymerase acidic (PA) protein using small-molecule degraders developed by hydrophobic tagging (HyT) technology to effectively combat the influenza virus was reported. The SAR results revealed that compound 19b with Boc(2)-(L)-Lys demonstrated excellent inhibitory activity against A/WSN/33/H1N1 (EC50 = 0.015 mu M) and amantadine-resistant strain (A/PR/8/H1N1), low cytotoxicity, high selectivity, substantial degradation ability, and good drug-like properties. Mechanistic studies demonstrated that the proteasome system and autophagic lysosome pathway were the potential drivers of these HyT degraders. Thus, this study provides a powerful tool for investigating the targeted degradation of influenza virus proteins and for antiviral drug development.

关键词： Antimicrobial agents Degradation Hydrophobicity Peptides and proteins Viruses

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Controllable power transfer in a double-channel magneto-optical photonic crystal waveguide 10

Controllable power transfer in a double-channel magneto-opti...

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10th International Symposium on Advanced Optical Manufacturing and Testing Technologies - Novel Optoelectronic Functional Materials and Devices

作者： he, Peide Xie, shuwen Liu, Jiawei Liang, Wenyao South China Univ Technol Guangzhou 510641 Peoples R China

ISBN: (数字)9781510650244

ISBN: (纸本)9781510650244;9781510650237

We have studied the coupling effect of topological photonic states in a double- channel magneto-optical photonic crystal waveguide by introducing a two-layer ordinary alumina (Al2O3) photonic crystal as the coupling layer. Interestingly, for the structure with the same widths of the two channels, the electromagnetic wave propagates one-way to the right side and exhibits wave- like path within the waveguide due to the coupling effect of topological photonic states. This unique property provides an effective way to achieve desired power ratio between two right outputs by terminating the structure at different length of waveguide. Moreover, the power ratio can be tuned by the external magnetic field conveniently. As for an asymmetric waveguide with different channel widths, there exist two asymmetric one-way topological photonic states (i.e., the odd- like and even-like modes) in the bandgap. The eigenfield analyses show that the electric field of oddlike mode is stronger in the lower channel, while that of even-like mode is contrary. As the old- like mode propagates rightwards, electromagnetic waves in the two channels couple with each other via the coupling layer, then the power in the upper channel gradually transfers to the lower channel, and finally reach almost 100% transmittance in the lower output. However, the case for the even-like mode is totally contrary. These results hold great promise for many application fields such as signal transmission, optical modulation, and the design of topological devices.

关键词： topological photonic states magneto-optical photonic crystal coupling layer power ratio

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Cardioprotective effects of sinomenine in myocardial ischemia/ reperfusion injury in a rat model

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SAUDI PHARMACEUTICAL JOURNAL 2022年第6期30卷 669-678页

作者： Lu, Changhong Guo, Xiao he, Xianghui Chang, Yu Zheng, Fa Xu, Chenji Zhang, shuwen Zhou, Yaqun Li, Junfang Qingdao Fuwai Cardiovasc Hosp Heart Ctr 201 Nanjing Rd Qingdao 266034 Shandong Peoples R China Qingdao Fuwai Cardiovasc Hosp Dept Emergency 201 Nanjing Rd Qingdao 266034 Shandong Peoples R China Qingdao Univ Dept Cardiac Ultrasound Affiliated Hosp 16 Jiangsu Rd Qingdao 266000 Shandong Peoples R China QIngdao Univ Orthoped Dept Dept Cardiac Ultrasound Affiliated Hosp 16 Jiangsu Rd Qingdao 266000 Shandong Peoples R China

Background: Ischemia reperfusion (I/R) play an imperative role in the expansion of cardiovascular dis-ease. Sinomenine (SM) has been exhibited to possess antioxidant, anticancer, anti-inflammatory, antiviral and anticarcinogenic properties. The aim of the study was scrutinized the cardioprotective effect of SM against I/R injury in rat. Methods: Rat were randomly divided into normal control (NC), I/R control and I/R + SM (5, 10 and 20 mg/ kg), respectively. Ventricular arrhythmias, body weight and heart weight were estimated. Antioxidant, inflammatory cytokines, inflammatory mediators and plasmin system indicator were accessed. Results: Pre-treated SM group rats exhibited the reduction in the duration and incidence of ventricular fibrillation, ventricular ectopic beat (VEB) and ventricular tachycardia along with suppression of arrhyth-mia score during the ischemia (30 and 120 min). SM treated rats significantly (P < 0.001) altered the level of antioxidant parameters. SM treatment significantly (P < 0.001) repressed the level of creatine kinase MB (CK-MB), creatine kinase (CK) and troponin I (Tnl). SM treated rats significantly (P < 0.001) repressed the tissue factor (TF), thromboxane B2 (TXB2), plasminogen activator inhibitor 1 (PAI-1) and plasma fib-rinogen (Fbg) and inflammatory cytokines and inflammatory mediators. Conclusion: Our result clearly indicated that SM plays anti-arrhythmia effect in I/R injury in the rats via alteration of oxidative stress and inflammatory reaction. (c) 2022 The Author(s). Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY license (http://***/licenses/by/4.0/).

关键词： Sinomenine Ischemia reperfusion Arrhythmias Antioxidant Plasmin system

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Construction and evaluation of pedotransfer functions for saturated hydraulic conductivity in the granite red soil regions of southern China

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JOURNAL OF HYDROLOGY-REGIONAL STUDIES 2023年 50卷

作者： he, Ling Duan, Xiaoqian Ding, shuwen Cai, Chongfa Deng, Yusong Guangxi Univ Coll Forestry Guangxi Key Lab Forest Ecol & Conservat Nanning 530004 Peoples R China Guangxi Univ Coll Agr Guangxi Key Lab Agr Environm & Agr Prod Safety Nanning 530004 Peoples R China Huazhong Agr Univ Coll Resources & Environm Wuhan 430070 Peoples R China

Study region: Six typical regions of granite red soil in southern *** focus: Regional large-scale Ks analysis of granite red soil in South China is still limited to a large number of repetitive and expensive workloads. It is necessary to construct Ks PTFs suitable for the granite red soil region of South China. In this study, six different regions granite red soil in South China were used to validate the prediction of classical PTFs for Ks, the best combination of predictors was screened and PTFs developed based on stepwise regression methods and machine learning algorithms. New hydrologic insights for the region: (1) The coefficient of variation for Ks is 69.87% in the granite red soil region of South China, with a large spatial variability. (2) The six typical PTFs of Ks were poor predictors of Ks for soils in southern China, R-2 < 0.4. (3) "Clay+Silt+Sand+BD+SOM+NCP" is the best combination of predictors of soil Ks in the granite red soil region of South China, which can be used in different machine learning algorithms. (4) The constructed MLR model "Ks= 1.501 + 0.043 xNCP-0.995 xBD+ 0.034 xSOM-0.013 xClay" with KNN, ANN and BRT machine algorithm models have a prediction accuracy R-2 greater than 0.8. This study provides different prediction models for soil Ks in the granitic regions of southern China and lays a theoretical basis for hydrological research in the these regions.

关键词： Soil saturated hydraulic conductivity (Ks) Granite red soils Pedotransfer functions (PTFs)

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Rhodium(III)-Catalyzed Three-Component Cascade Annulation for Modular Assembly of N-Alkoxylated Isoindolin-1-Ones with Quaternary Carbon Center

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ADVANCED SYNTheSIS & CATALYSIS 2022年第15期364卷 2589-2595页

作者： Hu, Wenbo Yan, Liqin Zuo, Youpeng Kong, shuwen Pu, Yue Tang, Qiang Wang, Xinyu he, Xinwei Shang, Yongjia Anhui Normal Univ Coll Chem & Mat Sci State Key Lab Cultivat Base Key Lab Funct Mol SolidsMinist EducAnhui Lab Mo Wuhu 241000 Peoples R China Hunan Normal Univ Key Lab Assembly & Applicat Organ Funct Mol Hunan Changsha 410081 Peoples R China

A cascade C-H activation, annulation, and etherification of N-hydroxybenzamides with propargylamines provides a flexible route to N-alkoxylated 3-arylisoindolin-1-ones. Three new bonds (C-C, C-N, and C-O) are generated to afford a series of isoindolin-1-ones bearing a tetrasubstituted carbon in 49-82% yield. The utility of this method was showcased by gram-scale synthesis and synthetic transformations of the product to access structurally diverse isoindolinones.

关键词： Annulation Isoindolin-1-ones Multicomponent reaction N-Hydroxybenzamides Propargylamines

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Global surveillance of circulating microRNA for diagnostic and prognostic assessment of acute myocardial infarction based on the plasma small RNA sequencing

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BIOMARKER RESEARCH 2024年第1期12卷 143页

作者： Wang, Xiaomin Lu, Yaojun Zhao, Ruiping Zhu, Bing Liu, Jian Yue, Qiang Wu, Rina Han, shuwen Gao, Yuanyuan Chen, Juan Gong, Jie he, Danna Xu, Teng Ying, Jianchao Baotou Cent Hosp Chest Pain Ctr Dept Cardiol Baotou Peoples R China Baotou Cent Hosp Inst Translat Med Baotou Peoples R China Dian Diagnost Grp Co Ltd Hangzhou Peoples R China Wenzhou Med Univ Affiliated Hosp 1 Wenzhou Key Lab Emergency Crit care & Disaster Med Cent Lab Wenzhou Peoples R China

BackgroundCirculating microRNAs (miRNAs) are recently a rapidly increasing of interest as non-invasive biomarkers for diagnosis and prognosis of acute myocardial infarction (AMI). Previous studies revealed that several miRNAs exhibited the capacity for diagnosis and prognosis of AMI, the reasons why these circulating miRNAs are concerned as targets for investigation are quite cryptogenic, presumably due to the lack of clues provided by global surveillance at the transcriptome level, and the current data for some miRNAs are controversial and inconsistent among independent *** comprehensively profiling the potential miRNAs for diagnosis and prognosis of AMI, we reported transcriptomes of circulating miRNAs in the plasma of 27 healthy controls, 64 AMI patients (37 STEMI and 27 NSTEMI) and 20 AMI patients who were subjected to reperfusion therapy. Meanwhile, the cTnI of AMI patients was parallel determined. Differentially-circulated miRNAs were analyzed between each group. All detected circulating miRNAs were examined by ROC analysis and then LASSO dimension reduction to obtain an optimal panel for diagnosis of AMI. A five-year period follow-up towards the AMI and reperfusion patients was performed, and the prognostic value of circulating miRNAs in these patients was estimated by using the Cox regression model, ROC and Kaplan-Meier *** global differences of miRNAs transcriptome among AMI, reperfusion patients and healthy controls were identified. A total of 40 miRNAs, called high diagnostic performance miRNAs, including several previous well-studied miRNAs with AUC greater than 0.85 were shown to discriminate AMI with healthy controls. In addition, 29 miRNAs were analyzed to be strongly correlated with the plasma cTnI level, of which 20 overlapped with high diagnostic performance miRNAs. These overlapped miRNAs are over-represented in the pathways which actually reflect the pathological cause of myocardial infarction, as well as the

关键词： Acute myocardial infarction Circulating microRNA Diagnostic biomarker

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Aptamers from random sequence space: Accomplishments, gaps and future considerations

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ANALYTICA CHIMICA ACTA 2022年 1196卷 339511-339511页

作者： Qian, shuwen Chang, Dingran he, Sisi Li, Yingfu McMaster Univ Michael G DeGroote Inst Infect Dis Res Dept Biochem & Biomed Sci 1280 Main St West Hamilton ON L8S 4K1 Canada McMaster Univ Dept Chem & Chem Biol 1280 Main St West Hamilton ON L8S 4K1 Canada Harbin Inst Technol Shenzhen Sch Sci Shenzhen 518055 Guangdong Peoples R China

Aptamers are molecular recognition elements made of nucleic acids. Diverse synthetic aptamers have been discovered in a large number of SELEX experiments since 1990. This review begins with the analysis of these SELEX experiments by examining the range of targets as well as the affinity and specificity for these targets by DNA, RNA or modified nucleic acid aptamers generated from these experiments. This is followed by comparisons of synthetic aptamers with natural RNA aptamers from riboswitches and with some of the best naturally occurring protein based recognition elements for proteins and small molecules. These comparisons reveal the gaps between man-made aptamers and natural recognition elements. We then put forward a series of ideas for consideration by the aptamer community towards developing better aptamers to solve real world problems. These include performing aptamer selections with libraries containing larger random sequence domains to derive larger aptamers with more intricate structures, conducting more reselection experiments using mutagenized DNA libraries based on initially selected aptamer sequences to search for better members of an aptamer family, selecting aptamers that are programmed to recognize two or more different epitopes of the same target in order to build multivalent aptamers for increased affinity, expanding the effort of selecting aptamers using modified nucleic acids with enhanced chemical functionalities, innovating SELEX methods to drive for the selection of aptamers with truly outstanding affinity and specificity, and having terminal applications in mind when creating new aptamers so that they are highly functional in the environment where the applications are planned. (c) 2022 Elsevier B.V. All rights reserved.

关键词： Aptamers SELEX In vitro selection DNA RNA Modified nucleic acids

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