1.Design, synthesis and antiplatelet activity evaluation of novel quinoxaline antagonists of protease activated receptor 4 (PAR4)
Rou-jie XIE ; Shang-de LIU ; Duo YUAN ; Shan-shan LI ; Xiong ZHU
Acta Pharmaceutica Sinica 2022;57(3):731-740
Twenty-five compounds of novel quinoxaline-based scaffold with antiplatelet activity were designed and synthesized on the basis of previous quinoxaline analogues, and the structures were confirmed by 1H NMR, 13C NMR, and MS. The antiplatelet activity was evaluated, structure-activity relationship (SAR) study was summarized and the selectivity of PAR4 was confirmed by calcium mobilization assays. It was indicated that compound
2.Analysis and synthesis of the related substances of palbociclib
Duo YUAN ; Xiong ZHU ; Shijin ZHANG ; Duo WANG ; Zhiyu LI ; Liping SUN
Journal of China Pharmaceutical University 2015;46(6):696-699
To strengthen the quality control of palbociclib, three related substances were separated from the bulk drug. These substances were identified as 8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido [2, 3-d] pyrimidin-7(8H)-one(A), 8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridine-2-yl)amino)-6-vinylpyrido [2, 3-d] pyrimidin-7(8H)-one(B), tert-butyl4-(6-((6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7, 8-dihydropyrido [2, 3-d] pyrimidin-2-yl)amino)pyridin-3-yl)piperazi-ne-1-carboxylate(C). Based on the structures of the impurities, the possible routes to them were discussed, and their structures were elucidated by 1H NMR and MS.
4.Preliminary analysis on respiratory syncytial virus identified in children with acute respiratory infections in Tibet Autonomous Region, China.
Jie DENG ; Ru-Nan ZHU ; Yuan QIAN ; Yu SUN ; Lin-Qing ZHAO ; Fang WANG ; Hong WU ; Min-Na SHAN ; Mei-Duo DEJI
Chinese Journal of Virology 2012;28(2):97-102
To understand the role of respiratory syncytial virus (RSV) in children with acute respiratory infections (ARI) in Tibet Autonomous Region and the contribution of two major groups of RSV, nasopharyngeal aspirates (NPA) were collected from hospitalized children with ARI in Department of Pediatrics, Tibet People's Hospital in Lasa, Tibet from April to July in 2011 and tested for seven common respiratory viruses and human metapneumovirus (hMPV) by direct immunofluorescence assay (DFA). Total RNAs were extracted from RSV positive samples by DFA and reverse transcripted to cDNA. Nested-PCR was employed to determine the genogroups of RSV, which were confirmed by real time-PCR and sequence analysis for G protein encoding gene. The Characteristics and variations of G genes from RSV in this project were identified by sequence comparison with those G genes in GenBank. Out of 167 samples, 65 were positive for respiratory viruses with a total positive rate of 38.9%, including 45 (69.2%, 45/65)positive samples for RSV. Among 42 samples that were positive for RSV and genotyped, 40 were identified as group A and 2 as group B. Sequence analysis of full-length G genes for 7 RSV of group A indicated that all of these belonged to subgroup GA2. The nucleotide identities between RSVs from Tibet and prototype A2 strain were 90.7%-91.8%, with 86.5%-87.2% identities of amino acid. The mutations of amino acids were mainly located in both ends of a highly conserved region in the ectodomain of the G proteins. The data indicated that RSV was the most important viral etiologic agent of ARI in spring of 2011 in Tibet and group A of RSV was predominant during the study period. High divergence existed in the ectodomain of G proteins of RSVs from Tibet.
Acute Disease
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Amino Acid Sequence
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Female
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Humans
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Infant
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Male
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Molecular Sequence Data
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Phylogeny
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Respiratory Syncytial Virus Infections
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virology
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Respiratory Syncytial Viruses
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chemistry
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classification
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genetics
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isolation & purification
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Respiratory Tract Infections
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virology
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Sequence Alignment
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Tibet
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Viral Proteins
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chemistry
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genetics
5.Viruses and clinical features associated with hospitalized children with acute respiratory infections in Lhasa, Tibet.
Hong WU ; Jie DENG ; Yuan QIAN ; Ru-nan ZHU ; Yu SUN ; Lin-qing ZHAO ; Fang WANG ; Min-na SHAN ; Mei-duo DEJI
Chinese Journal of Pediatrics 2012;50(10):740-742
OBJECTIVETo investigate the viral etiology and clinical features of hospitalized children with acute respiratory tract infections in Tibet.
METHODNasopharyngeal aspirate samples were collected from children with acute respiratory tract infection hospitalized at the department of Pediatrics, Tibet Autonomous Region People's Hospital from April to July, 2011. The specimens of nasopharyngeal aspirate were screened for antigens of 7 common respiratory viruses by direct immunofluorescence (DIF) [respiratory syncytial virus (RSV), adenovirus (ADV), parainfluenza viruses type I-III, influenza virus A and B] and human metapneumovirus. Clinical data of the children were analyzed by statistical software SPSS16.
RESULTA total of 167 children with acute respiratory tract infections hospitalized from April to July 2011 were enrolled in this investigation. Sixty-five out of 167 specimens were positive for viral antigens. The virus positive rate for specimens was 38.9% (65/167). Two of 65 positive specimens were positive for 2 virus antigens (RSV + influenza B) and (hMPV + parainfluenza virus type III), respectively. RSV was detected in 45 cases (67.2%, 45/67) which was the most predominant, followed by parainfluenza virus type III detected in 7 cases (10.4%, 7/67), ADV in 6 cases (9.0%, 6/67), parainfluenza virus type I in 4 cases (6.0%, 4/67), influenza virus type B in 3 cases (4.5%, 3/67), and hMPV in 2 cases (3.0%, 2/67). In addition to clinical manifestations of pneumonia, such as cough and shortness of breath, only 3 virus positive cases (6.67%) presented with wheezing, but the signs of severe cyanosis, fine rales in lung were common. Most of the children in this study recovered soon, only a few younger children with underlying diseases or complications had severe illness.
CONCLUSIONVirus is an important pathogen for acute respiratory infections for hospitalized children in Tibet. RSV was the most predominant etiological agent, especially for those younger than 3 years old.
Acute Disease ; Adolescent ; Age Distribution ; Child ; Child, Hospitalized ; Child, Preschool ; Female ; Fluorescent Antibody Technique, Direct ; Humans ; Infant ; Male ; Nasopharynx ; virology ; Respiratory Syncytial Virus Infections ; epidemiology ; pathology ; virology ; Respiratory Syncytial Virus, Human ; isolation & purification ; Respiratory Tract Infections ; epidemiology ; pathology ; virology ; Tibet ; epidemiology ; Virus Diseases ; epidemiology ; etiology ; pathology ; virology ; Viruses ; classification ; isolation & purification
6.Molecular subtyping of Vibrio cholerae isolates from outbreaks of cholera by pulsed-field gel electrophoresis in Hainan in 2008.
Jie WU ; Bao-Wei DIAO ; Hai-Jian ZHOU ; Jian-Hua ZHU ; Duo-Chun WANG ; Bo PANG ; Rui-Bai WANG ; Biao KAN ; Shao-Ling WANG ; Xin-Yuan SU ; Yan MA
Chinese Journal of Preventive Medicine 2010;44(12):1083-1086
OBJECTIVETo analyze the molecular characteristics and genetic correlations of Vibrio cholerae isolates in Hainan in 2008, so as to provide pathogenic proof to diagnose the plague.
METHODSSeventy six cholera strains were isolated from this cholera epidemic.69 strains were obtained from patients, 7 were isolated from external environment, among which, one was from patient's toilet, one from water sample, three were isolated from fish pond near patient's home, one came from swab of the patient vomit on the ground of health center and one from swab of kitchen knife from Hainan University canteen respectively. With conventional aetiological methods, pulse-field gel electrophoresis was conducted and the patterns of the 76 isolates were analyzed. The PFGE image was analyzed using BioNumerics (Version4.0, Applied Maths BVBA, Belium). Image bands were identified and similarity coefficient was automatically generated.
RESULTSSeventy six strains were isolated from Vibrio cholerae outbreaks in Hainan in 2008.5 PFGE patterns of patient's isolates in June were the same, sharing a similarity coefficient of 100%. 70 PFGE patterns of patients and water in October and November were completely same, the similarity coefficient being 100%. But they were not same as that of June. 1 PFGE pattern of isolate from the sample in Hainan University was different, only sharing a similarity coefficient of 79.7%, which showed no correlation with the outbreak.
CONCLUSIONDifferent outbreaks of Vibrio cholera occurred in Hainan in 2008. The epidemic in October and November at different counties was one outbreak. The pollution of water in environment was an important factor for outbreak.
Bacterial Typing Techniques ; methods ; China ; epidemiology ; Cholera ; epidemiology ; microbiology ; DNA, Bacterial ; Disease Outbreaks ; Electrophoresis, Gel, Pulsed-Field ; methods ; Humans ; Vibrio cholerae ; classification ; isolation & purification
7.Miniature Non-invasive Blood Pressure Measurement and Verification System.
Hang-Duo NIU ; Si-Nian YUAN ; Zi-Fu ZHU ; Ji-Lun YE ; Xu ZHANG ; Hui YU
Chinese Journal of Medical Instrumentation 2022;46(3):278-282
Mercury sphygmomanometer based on traditional auscultation method is widely used in primary medical institutions in China, but a large amount of blood pressure data can not be directly recorded and applied in scientific research analysis, meanwhile auscultation data is the clinical standard to verify the accuracy of non-invasive electronic sphygmomanometer. Focusing on this, we designed a miniature non-invasive blood pressure measurement and verification system, which can assist doctors to record blood pressure data automatically during the process of auscultation. Through the data playback function,the software of this system can evaluate and verify the blood pressure algorithm of oscillographic method, and then continuously modify the algorithm to improve the measurement accuracy. This study introduces the hardware selection and software design process in detail. The test results show that the system meets the requirements of relevant standards and has a good application prospect.
Auscultation
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Blood Pressure/physiology*
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Blood Pressure Determination
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Oscillometry
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Sphygmomanometers
8.An Adaptive Method for Detecting and Removing EEG Noise.
Si-Nian YUAN ; Ruo-Wei LI ; Zi-Fu ZHU ; Sheng-Cai MA ; Hang-Duo NIU ; Ji-Lun YE ; Xu ZHANG
Chinese Journal of Medical Instrumentation 2022;46(3):248-253
To solve the problem of real-time detection and removal of EEG signal noise in anesthesia depth monitoring, we proposed an adaptive EEG signal noise detection and removal method. This method uses discrete wavelet transform to extract the low-frequency energy and high-frequency energy of a segment of EEG signals, and sets two sets of thresholds for the low-frequency band and high-frequency band of the EEG signal. These two sets of thresholds can be updated adaptively according to the energy situation of the most recent EEG signal. Finally, we judge the level of signal interference according to the range of low-frequency energy and high-frequency energy, and perform corresponding denoising processing. The results show that the method can more accurately detect and remove the noise interference in the EEG signal, and improve the stability of the calculated characteristic parameters.
Algorithms
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Electroencephalography
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Signal Processing, Computer-Assisted
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Signal-To-Noise Ratio
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Wavelet Analysis
9.Association between urinary arsenic level and serum testosterone in Chinese men aged 18 to 79 years.
Ya Wei LI ; Zheng LI ; Hao Can SONG ; Liang DING ; Sai Sai JI ; Miao ZHANG ; Ying Li QU ; Qi SUN ; Yuan Duo ZHU ; Hui FU ; Jia Yi CAI ; Chen Feng LI ; Ying Ying HAN ; Wen Li ZHANG ; Feng ZHAO ; Yue Bin LYU ; Xiao Ming SHI
Chinese Journal of Preventive Medicine 2023;57(5):686-692
Objective: To investigate the association between the urinary arsenic level and serum total testosterone in Chinese men aged 18 to 79 years. Methods: A total of 5 048 male participants aged 18 to 79 years were recruited from the China National Human Biomonitoring (CNHBM) from 2017 to 2018. Questionnaires and physical examinations were used to collect information on demographic characteristics, lifestyle, food intake frequency and health status. Venous blood and urine samples were collected to detect the level of serum total testosterone, urinary arsenic and urinary creatinine. Participants were divided into three groups (low, middle, and high) based on the tertiles of creatinine-adjusted urinary arsenic concentration. Weighted multiple linear regression was fitted to analyze the association of urinary arsenic with serum total testosterone. Results: The weighted average age of 5 048 Chinese men was (46.72±0.40) years. Geometric mean concentration (95%CI) of urinary arsenic, creatinine-adjusted urinary arsenic and serum testosterone was 22.46 (20.08, 25.12) μg/L, 19.36 (16.92, 22.15) μg/g·Cr and 18.13 (17.42, 18.85) nmol/L, respectively. After controlling for covariates, compared with the low-level urinary arsenic group, the testosterone level of the participants in the middle-level group and the high-level group decreased gradually. The percentile ratio (95%CI) was -5.17% (-13.14%, 3.54%) and -10.33% (-15.68%, -4.63). The subgroup analysis showed that the association between the urinary arsenic level and testosterone level was more obvious in the group with BMI<24 kg/m2 group (Pinteraction=0.023). Conclusion: There is a negative association between the urinary arsenic level and serum total testosterone in Chinese men aged 18 to 79 years.
Humans
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Male
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Arsenic/urine*
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Creatinine
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East Asian People
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Testosterone/blood*
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Urinalysis
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Adolescent
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Young Adult
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Adult
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Middle Aged
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Aged