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Design and synthesis of chitin synthase inhibitors as potent fungicides

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Chinese Chemical Letters 2017年第6期28卷 1232-1237页

作者： Qi chen Ji-Wei Zhang lu-lu chen Jun Yang Xin-Ling Yang Yun Ling Qing Yang State Key Laboratory of Fine Chemical Engineering and School of Life Science and Biotechnology Dalian University of Technology Dalian 116024 China Key Laboratory of Pesticide Chemistry and Application Ministry of Agriculture Department of Applied Chemistry College of Science China Agricultural University Beijing 100193 China Central Research Institute of China Chemical Science & Technology Beijing 100083 China

Chitin is a structural component of fungal cell walls but is absent in vertebrates,mammals,and *** synthase is thus an attractive molecular target for developing *** on the structure of its donor substrate,UDP-N-acetyl-glucosamine,as well as the modelled structure of the bacterial chitin synthase NodC,we designed a novel scaffold which was then further optimized into a series of chitin synthase *** most potent inhibitor,compound 13,exhibited high chitin synthase inhibitory activity with an IC（50） value of 64.5 μmol/L All of the inhibitors exhibited antifungal activities against the growth of agriculturally-destructive fungi,Fusarium graminearum,Botrytis *** Colletotrichum *** work presents a new scaffold which can be used for the development of novel fungicides.

关键词： Chitin synthase Inhibitor Fungicide UDP-N-acetyl-D-glucosamine

Multiple neurofibromas plus fibrosarcoma with familial NF1 pathogenicity:A case report

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World Journal of Clinical Cases 2020年第7期8卷 1306-1310页

作者： Yang Wang Xiao-Fan lu lu-lu chen Ying-Wei Zhang Bing Zhang Department of Radiology The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical SchoolNanjing 210008Jiangsu ProvinceChina Research Center of Biostatistics and Computational Pharmacy China Pharmaceutical UniversityNanjing 210009Jiangsu ProvinceChina Department of Respiration The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical SchoolNanjing 210008Jiangsu ProvinceChina

BACKGROUND Neurofibromatosis(NF)is a genetic disease consisting of seven types,of which types 1 to 4 are caused by a dominant autosomal gene mutation;such disease sometimes arises in patients with NF type ***,it remains unclear whether the origin of neurofibrosarcoma is directly linked to the incidence of NF type 1,as no reports have been published on this ***,we report a case of NF1-positive multiple neurofibromas with malignant fibrosarcomatous transformation in the pleural *** SUMMARY A 51-year-old male was admitted to our hospital due to fever accompanied by coughing,chest tightness and asthma for more than one *** preliminary diagnosis was NF type 1,which was pathologically confirmed by a subsequent thoracoabdominal subcutaneous *** definitive diagnosis was neurofibrosarcoma with a pathogenic NF1 *** patient refused surgery and chemoradiotherapy,and died two months *** is a genetic disease consisting of seven types,of which types 1 to 4 are caused by a dominant autosomal gene *** case reported belongs to the class of NF1-positive dominant *** is a malignant tumor derived from cells surrounding the peripheral ***,due to the lack of previous reports,it remains unclear whether the origin of neurofibrosarcoma is directly linked to the incidence of NF type *** We report the first case of NF1-positive multiple neurofibromas with malignant fibrosarcomatous transformation in the pleural cavity.

关键词： Multiple neurofibromas Fibrosarcoma Neurofibromatosis type 1 pathogenicity Pseudochylothorax Pleural cavity Case report

Comparison of OCT and OCTA manifestations among untreated PCV, neovascular AMD, and CSC in Chinese population

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International Journal of Ophthalmology(English edition) 2020年第1期13卷 93-103页

作者： Ming-Zhen Yuan lu-lu chen Jing-Yuan Yang Ming-Yue luo You-Xin chen Department of Ophthalmology Peking Union Medical College Hospital Chinese Academy of Medical Sciences and Peking Union Medical College

AIM: To compare the qualitative and quantitative features among untreated polypoidal choroidal vasculopathy(PCV), neovascular age-related macular degeneration(nv-AMD) and central serous chorioretinopathy(CSC) using optical coherence tomography(OCT) and OCT angiography(OCTA).METHODS: This retrospective study included 16 eyes with thin-choroid PCV, 18 eyes with thick-choroid PCV, 16 eyes with nv-AMD and 17 eyes with CSC, respectively. The indicators were obtained by OCT and ***: Sub-foveal choroidal thickness(SFCT) in CSC was thicker compared to other groups(all P<0.05). SFCT in nv-AMD was thicker compared to thin-choroid PCV, but thinner compared with thick-choroid PCV(both P<0.05). As the ratio of thickness of Haller's layer to thickness of SFCT, which of thin-choroid PCV was significantly higher than CSC(P<0.001). Likewise, thick-choroid PCV had significantly higher ratio than nv-AMD(P=0.016) or CSC(P<0.001). There were differences among them in pigment epithelium detachment(PED). The whole-superficial retinal vessel density(RVD), deep RVD and choroidal capillary vessel density(CCVD) in CSC were significantly higher compared to other three groups, respectively(all P<0.05). The whole CCVD in nv-AMD was higher compared to thick-choroid PCV(P=0.032). Cross-sectional local angiographic form was 87.50%, 83.33%, 0 and 35.29% in thin-choroid PCV, thickchoroid PCV, nv-AMD and CSC, respectively. Cross-sectional diffuse angiographic form was 12.50%, 16.67%, 100% and 5.88% in thin-choroid PCV, thick-choroid PCV, nv-AMD and CSC, ***: Combination of OCT and OCTA can effectively observe the significant alterations existed in PCV, CSC and nv-AMD, and there are distinctive differences among them. The pathogenesis is not exactly the same between PCV and nv-AMD, or PCV and CSC.

关键词： polypoidal choroidal vasculopathy neovascular age-related macular degeneration central serous chorioretinopathy Haller's layer vascular density pigment epithelium detachment

Synthesis and anti-inflammatory-analgesic activity of 2',4'-difluoro-3-(carbamoyl)biphenyl-4-yl benzoates

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Chinese Chemical Letters 2008年第12期19卷 1419-1422页

作者： Guang Xiang Zhong lu lu chen Jian Li Wei Xiao Hu Min You Qi College of Pharmaceutical Science Zhejiang University of Technology Hangzhou 310032 PR China

Eighteen 2′,4′-difluoro-3-（carbamoyl）biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.

关键词： 2′,4′-Difluoro-3-(carbamoyl)biphenyl-4-yl benzoate Anti-inflammatory activity Analgesic activity Diflunisal

Effect of intradermal needle therapy at combined acupoints on patients’ gastrointestinal function following surgery for gastrointestinal tumors

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World Journal of Clinical Cases 2022年第31期10卷 11427-11441页

作者： Min Guo Man Wang lu-lu chen Fu-Juan Wei Jin-E Li Qing-Xiu lu Li Zhang Hai-Xia Yang School of Nursing Xi'an Jiaotong University Health Science CenterXi'an 710061Shaanxi ProvinceChina School of Medicine Zhejiang UniversityHangzhou 310016Zhejiang ProvinceChina Department of Geriatric Gastrosurgery The Second Affiliated Hospital of Xi'an Jiaotong UniversityXi'an 710046Shaanxi ProvinceChina Department of General Surgery The Second Affiliated Hospital of Xi'an Jiaotong UniversityXi'an 710046Shaanxi ProvinceChina Department of Traditional Chinese Medicine The Second Affiliated Hospital of Xi'an Jiaotong UniversityXi'an 710046Shaanxi ProvinceChina

BACKGROUND Postoperative gastrointestinal function recovery is critical for rapid rehabilitation of patients with gastrointestinal *** Chinese medicine offers considerable advantages for gastrointestinal disease ***,no study has reported the clinical efficacy of intradermal needle therapy(INT)at the Yuan-source,luo-connecting,and He-sea points of the corresponding meridian for gastrointestinal function in patients following surgery for gastrointestinal *** To investigate the effect of INT at combined acupoints on patients’gastrointestinal function following surgery for gastrointestinal *** This randomized controlled trial was conducted at the Second Affiliated Hospital of Xi’an Jiaotong University on patients with diagnosed gastrointestinal cancer,no distant metastases or organ failure,and hospitalized for elective radical tumor resection,who did not receive preoperative radiotherapy or *** were randomly allocated to either the intervention(n=32)or the control(n=32)*** in the control group received enhanced recovery care,while those in the intervention group received enhanced recovery care combined with INT at the Yuan-source,luo-connecting,and He-sea *** surgery,INT was performed immediately upon the patient's return to the ward,and continued for seven consecutive *** independent samples t-test,chi-square test,and generalized estimating equations were used for data *** The participants’ages ranged from 40 to 80 years(average 63±10.1 years).Most participants underwent surgery for either gastric(43.8%)or colon cancer(39.1%)and had adenocarcinoma(87.5%).Significant differences were noted in time to first postoperative flatus passage(66±27 h vs 103±41 h,Pluding abdomin

关键词： Acupuncture Acupuncture points Gastric tumors Traditional Chinese medicine Postoperative care

Automatic Botnet Attack Identification Based on Machine Learning

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Computers, Materials & Continua 2022年第11期73卷 3847-3860页

作者： Peng Hui Li Jie Xu Zhong Yi Xu Su chen Bo Wei Niu Jie Yin Xiao Feng Sun Hao Liang Lan lu lu chen Jiangsu Police Institute Nanjing210000China Public Security Department of Jiangsu Province Nanjing210000China The University of Adelaide Adelaide5005SAAustralia

At present,the severe network security situation has put forward high requirements for network security defense *** order to automate botnet threat warning,this paper researches the types and characteristics of *** has special characteristics in attributes such as packets,attack time interval,and packet *** this paper,the attack data is annotated by means of string recognition and expert *** attack features are extracted from the labeled attack data,and then use K-means for cluster *** clustering results show that the same attack data has its unique characteristics,and the automatic identification of network attacks is realized based on these *** the same time,based on the collection and attribute extraction of Botnet attack data,this paper uses RF,GBM,XGBOOST and other machine learning models to test the warning results,and automatically analyzes the attack by importing attack *** the early warning analysis results,the accuracy rates of different models are *** the descriptive values of the three accuracy rates of Accuracy,Precision,and F1_Score,the early warning effect of each model can be comprehensively *** the five algorithms used in this paper,three have an accuracy rate of over 90%.The three models with the highest accuracy are used in the early warning *** research shows that cyberattacks can be accurately *** this technology is applied to the protection system,accurate early warning can be given before a network attack is launched.

关键词： Honeypot log network attack machine learning

FLEXIBILITY OF ENZYME ACTIVE SITES

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Chinese Science Bulletin 1989年第10期34卷 793-799页

作者：邹承鲁 Laboratory of Biomacromolecules Institute of Biophysics Academia Sinica Beijing

The effects of structural changes on the activity of enzymes have been extensively studied. However, previous authors concentrated largely on the modification of the primary structures of the enzymes. On the other han... 详细信息

关键词： conformational enzymes concentrated reversible residues folding integrity largely monomer buried

Research progress of artesunate in diabetes and its complications

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Traditional Medicine Research 2023年第5期8卷 44-51页

作者： Yuan-Hui Guo lu-lu chen Ying LI Jia-Jia Duan Chuan-Xin Liu Hong-Wei Jiang Endocrine and Metabolic Disease Center First Affiliated HospitalCollege of Clinical Medicine of Henan University of Science and TechnologyMedical Key Laboratory of Hereditary Rare Diseases of HenanLuoyang Sub-center of National Clinical Research Center for Metabolic DiseasesLuoyang 471003China College of Clinical Medicine of Henan University of Science and Technology Department of Pharmacy First Affiliated Hospital of Henan University of Science and TechnologyLuoyang 471003China College of Clinical Medicine of Henan University of Science and Technology Laboratory Department of the First Affiliated Hospital of Henan University of Science and TechnologyLuoyang 471003China

Diabetes is a metabolic disease characterized by abnormally elevated blood glucose *** hyperglycemia leads to diabetic nephropathy,diabetic retinopathy,diabetes with periodontal disease and other diabetic *** diseases have become the main causes of disability and death in diabetic *** is well known as an antimalarial drug for controlling malaria *** studies have shown that artesunate improves diabetes and its complications by protecting islet cells,improving glucose and lipid metabolism,anti-inflammatory and immune *** on the research status in recent years,this paper focuses on the mechanism of artesunate in diabetes and its complications,to provide a theoretical basis for future diabetes research.

关键词： Artesunate diabetes diabetic complications islet cells glycolipid metabolism anti-inflammatory immunoregulation

Monitoring Neovascularization of Malignant Solid Tumors with Horseradish Peroxidase-Functionalized Near-Infrared-II PbS Quantum Dots

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Chemical & Biomedical Imaging 2023年第1期1卷 81-90页

作者： lu-lu chen Zhi-Gang Wang Hao Zhang Li-Ming chen Liang Zhao Zhen-Ya Liu Wei Zhao Lin-Han Jiang Ai-Xin Ma Xiaohui Yang Shu-Lin Liu Shiwu Zhang Dai-Wen Pang State Key Laboratory of Medicinal Chemical Biology Frontiers Science Centre for New Organic MatterTianjin Key Laboratory of Biosensing and Molecular RecognitionResearch Centre for Analytical SciencesCollege of ChemistrySchool of Medicine and Frontiers Science Center for Cell ResponsesNankai UniversityHaihe Laboratory of Sustainable Chemical TransformationsTianjin 300071P.R.China Tianjin Union Medical Center Nankai UniversityTianjin 300121P.R.China

The growth and metastasis of malignant solid tumors depend closely on newblood vessels. Vasculogenic mimicry provides a special pathway of blood supply during theearly growth of malignant tumors, and real-time monitoring of its occurrence anddevelopment in vivo is important to clinical applications. However, there are few labelswith sufffcient brightness and stability in vivo to achieve high spatiotemporal resolutionimaging of deep tissue for noninvasive optical detection of vasculogenic mimicry in tumortissues. In this study, we constructed a high-brightness ffuorescent label with ffuorescence inthe near-infrared-II region, which can be used not only for in vivo tumor imaging but also fortissue section imaging. Real-time high-resolution imaging of tumor vessels has been achievedwith PbS quantum dots (QDs) surface-coupled with horseradish peroxidase (HRP) (HRPQDs) by taking advantage of the low background autoffuorescence of tissue at the nearinfrared-II wavelength for in vivo and tissue section imaging. Qualitative and quantitativeanalysis of early blood supply patterns of tumor growth enables monitoring neovascularizationto accurate noninvasive identiffcation of benign and malignant solid tumors.

关键词： In vivo imaging Quantum dot Near-infrared Tumor Vasculogenic mimicry