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4,5,6,7-Tetrahydro-[1,2,3]triazolo[1,5-a]pyrazine as a new scaffold for heat shock protein 90 inhibitors

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Chinese Chemical Letters 2016年第1期27卷 11-15页

作者： Meng-Yi Xu Ni-na xue Di Liu Yu-Mei Zhou Wei Li Yong-Qiang Li Xiao-Guang Chen Xiao-Ming Yu Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College

Heat shock protein 90（hsp90） is a promising anticancer drug target. A library of 2,4-dihydroxyphenyl（resorcinol） substituted 4,5,6,7-tetrahydro-[1,2,3]triazolo[1,5-a]pyrazine compounds that target this protein were designed and prepared based on our earlier study. The compounds were tested in five cancer cell lines and seven of them showed notable anticancer activity（IC_（50）2-10 mmol/L）. The active subset compounds were further subjected to a polarized fluorescent assay and exhibited high binding affinity toward purified hsp90（IC_（50）60-100 nmol/L）. These results indicated that the tetrahydrotriazolopyrazine motif of the molecules may represent a novel scaffold for the development of hsp90 inhibitors.

关键词： Hsp90 inhibitor Anticancer drug Resorcinol Tetrahydrotriazolopyrazine

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王笑民教授治疗乳腺癌处方用药规律探析

中国医药导报 2024年第24期21卷 146-150,164页

作者：薛娜李欣许炜茹于明薇程培育雷勇王笑民首都医科大学附属北京中医医院肿瘤科北京100010 北京中医药大学研究生院北京100029

目的统计和收录王笑民教授治疗乳腺癌的病案,分析王教授诊治乳腺癌的思路及处方用药经验。方法选择2023年3月至2024年3月就诊于首都医科大学附属北京中医医院肿瘤科门诊诊断明确的激素受体阳性乳腺癌术后患者,经筛选后采集数据录入中医... 详细信息

目的统计和收录王笑民教授治疗乳腺癌的病案,分析王教授诊治乳腺癌的思路及处方用药经验。方法选择2023年3月至2024年3月就诊于首都医科大学附属北京中医医院肿瘤科门诊诊断明确的激素受体阳性乳腺癌术后患者,经筛选后采集数据录入中医传承辅助平台(V 2.5),采用软件“统计报表”及“数据分析”功能进行数据挖掘,分析王教授治疗乳腺癌常用药物、性味归经、核心处方及用药规律。结果共收集313首有效处方,涉及145味中药,出现频次排前3位分别为半枝莲、白花蛇舌草和黄芩。药物四气分布以寒、温、平为主;五味分布以甘、苦、辛常见;归经分布以肝、脾经为最多。最终得出5个药物核心组合及5首新处方,其中有重要临床意义的新处方2首。结论王教授治疗乳腺癌术后患者主要从肝、脾入手,以疏肝健脾、清热解毒、软坚散结和引火归元治则为主。

关键词：乳腺癌王笑民数据挖掘用药经验组方规律

Online Adaptive Vibration Control and Fault Diagnosis based on Identification for Offshore Platforms

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Online Adaptive Vibration Control and Fault Diagnosis based ...

Effects of preoperative ketamine on the endocrine-metabolic and inflammatory response to laparoscopic surgery

第40届中国控制会议

作者： xue-na Jiang Hui Ma College of Information Science and Engineering Ocean University of China

This paper investigates the vibration suppression and fault diagnosis problem of jacket-type offshore platforms with uncertainties and time delay. Firstly, through a model transformation, the original continuous-time model is transformed into an identifiable differential form. Secondly, according to the model-based theory, the fault diagnosis problem can be regarded as a parameter estimation issue. The Self-adjusting forgetting factor system identification algorithm is adopted to estimate the timevarying system parameter. By computing the residuals of the parameters in the fault-free model and the estimated parameters,we can detect the faults. Thirdly, we propose an adaptive controller to overcome the parameter uncertainty by using system identification algorithm. The controller parameters can converge to a new value as the physical parameters of offshore platforms change. The simulation results demonstrate the feasibility and efficiency of the design presented in this paper for eliminating vibration and fault diagnosis.

关键词： offshore platform uncertainties adaptive control system identification fault diagnosis

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Chinese Medical Journal 2011年第22期124卷 3721-3725页

作者： DU Jin HUANG Yu-guang YU xue-rong ZHAO na Department of Anaesthesiology Subei People＇s Hospital Yangzhou University Yangzhou Jiangsu 225001 China

Background Ketamine is hypothesized to reduce perioperative endocrine-metabolic and inflammatory responses in cardiac surgery patients. This randomized, placebo-controlled, double-blind study was performed to determine whether perioperative endocrine-metabolic and inflammatory responses are attenuated by preoperative administration of ketamine to healthy females receiving elective laparoscopic surgery. Methods Forty female patients with American Society of Anesthesiologist classification Ⅰ or Ⅱwho elected to receive gynecological laparoscopic surgery were randomly assigned to the ketamine-treated （group K; n = 20） or control （group C n = 20） group. At 2 minutes prior to induction patients in group K received ketamine （0.25 mg/kg） whereas those in group C received normal saline. All patients received standardized general anesthesia. Serum glucose and cortisol values were measured before ketamine administration （TO）, 2 minutes after tracheal intubation （T1）, 30 minutes after skin incision （T2）, 2 minutes after tracheal extubation （T3） and 1 hour postoperatively （T4）. Serum interleukin-6 and tumor necrosis factor-α values were determined at TO and T4. Postoperative analgesic efficacy, side effects of administered drugs, and time to discharge were recorded. Results Compared with subjects in group C, those in group K had lower serum glucose values at T1, T2, T3 and T4 and lower serum cortisol values at T4 （P 〈0.05）. Postoperative interleukin-6 and tumor necrosis factor-α concentrations for group K were lower than those for group C （P 〈0.05）. Postoperative visual analog scale scores at rest, cumulative fentanyl consumption, and time to discharge were lower in group K as compared to group C （P 〈0.05）. No significant differences in drug side effects were observed postoperatively between the two groups. Conclusion Endocrine-metabolic and inflammatory responses to laparoscopic surgery are attenuated in part by Dre-incisienal administration of ketamine.

关键词： endocrine-metabolic response inflammatory response ketamine laparoscopic surgery preemptive analgesia

一个融合网络安全信息的安全事件分析与预测模型

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东北大学学报（自然科学版） 2005年第3期26卷 228-231页

作者：彭雪娜赵宏东北大学软件中心辽宁沈阳110004

提出了一种融合网络安全信息的安全事件分析与预测模型·该模型能够对来自以IDS为主的多种安全部件和关键主机日志系统的网络安全信息进行校验、聚集和关联,从而整体上降低安全部件的误报率,扩展对网络中复杂攻击识别能力;能够结合目标... 详细信息

提出了一种融合网络安全信息的安全事件分析与预测模型·该模型能够对来自以IDS为主的多种安全部件和关键主机日志系统的网络安全信息进行校验、聚集和关联,从而整体上降低安全部件的误报率,扩展对网络中复杂攻击识别能力;能够结合目标网络安全策略,对目标网络的安全状况进行准确评估,分析出网络真正威胁所在;还能够基于特定攻击场景,对未来可能发生的具体攻击行为做预测,从而尽早发现潜在威胁,为采取有效响应措施赢得宝贵时间·

关键词：入侵检测系统网络安全信息融合告警聚集事件关联安全状态评估安全事件预测

Exploring predictive markers for liver failure post-hepatectomy in hepatocellular carcinoma patients

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World Journal of Gastrointestinal Surgery 2024年第5期16卷 1482-1484页

作者： Shi-Yan Zhang Xiong-Jian Ma xue-Xia Zhu na Cai Department of Clinical Laboratory Fuding HospitalFujian University of Traditional Chinese MedicineFuding 355200Fujian ProvinceChina

This letter to the editor addresses the study titled“Predictive value of NLR,Fib4,and APRI in the occurrence of liver failure after hepatectomy in patients with hepatocellular carcinoma”by Kuang et al in the World Journal of Gastrointestinal *** study acknowledges the comprehensive patient data analysis while suggesting that there is a need for further discussion on the clinical applicability of these markers across diverse patient *** letter recommends prospective studies for validation and considers the influence of confounding *** finding underscores the significance of this study in improving hepatocellular carcinoma management.

关键词： Neutrophil-to-lymphocyte ratio Hepatocellular carcinoma Liver failure Hepatectomy Letter to the Editor Commentary

Study on Catalytic Behavior of Iron-based Catalyst with IITP as Electron Donor in the Polymerization of Butadiene

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Chinese Journal of Polymer Science 2024年第5期42卷 612-619,I0007页

作者： Shi-Liang Xu Ying-nan Zhao Yao Yu Qi Yang Li-Hua na Heng Liu Chun-Yu Zhang xue-Quan Zhang Key Laboratory of Advanced Rubber Material Ministry of EducationSchool of Polymer Science and EngineeringQingdao University of Science&TechnologyQingdao266042China Shandong Provincial College Laboratory of Rubber Material and Engineering School of Polymer Science and EngineeringQingdao University of Science&TechnologyQingdao266042China Key Lab of Rubber-Plastics Ministry of Education/Shandong Provincial Key Lab of Rubber-plasticsSchool of Polymer Science and EngineeringQingdao University of Science&TechnologyQingdao266042China

In this study,a novel iron-based catalyst system,Fe(acac)3/(isocyanoimino)triptenylphosphorane(IITP)/AlR3,was employed for the synthesis of syndiotactic 1,2-polybutadiene in *** catalyst system exhibits remarkably high catalytic activity,achieving a polymerization activity of 762 kgpolymer·molcatalyst^(-1)·h^(-1)at 50℃with a[BD]/[Fe]molar ratio of ***,living polymerization characteristic were observed during the investigation of the polymerization kinetics of 1,3-butadiene *** characteristics were well demonstrated by a narrow molecular weight distribution(PDI≈2.0)of the resulting polybutadiene and a linear relationship between-ln(1-c)and polymerization time as well as number average molecular weight and polymer *** resultant polymer showed a 1,2-selectivity of approximately 76%and stereoregularity ranging from 62%to 73%(rrrr).Additionally,through kinetic studies on polymerization reaction,an apparent activation energy Ea value of this catalytic system was calculated to be 84.98 kJ·mol^(-1),which suggests that high polymerization temperature favors efficient polymerization.

关键词： Iron catalyst Syndiotactic 1,2-polybutadiene Elastomers Donor Selectivity

CPI-17-mediated contraction of vascular smooth muscle is essential for the development of hypertension in obese mice

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Journal of Genetics and Genomics 2019年第3期46卷 109-118页

作者： Jie Sun Tao Tao Wei Zhao Lisha Wei Fan She Pei Wang Yeqiong Li Yanyan Zheng Xin Chen Wei Wang Yanning Qiao xue-na Zhang Min-Sheng Zhu Model Animal Research Center and MOE Key Laboratory of Model Animal and Disease Study Nanjing University Key Laboratory of MOE for Modern Teaching Technology Shaanxi Normal University

Several factors have been implicated in obesity-related hypertension, but the genesis of the hypertension is largely unknown. In this study, we found a significantly upregulated expression of CPI-17(C-kinasepotentiated protein phosphatase 1 inhibitor of 17 kDa) and protein kinase C(PKC) isoforms in the vascular smooth muscles of high-fat diet(HFD)-fed obese mice. The obese wild-type mice showed a significant elevation of blood pressure and enhanced calcium-sensitized contraction of vascular smooth muscles. However, the obese CPI-17-deficient mice showed a normotensive blood pressure, and the calcium-sensitized contraction was consistently reduced. In addition, the mutant muscle displayed an abolished responsive force to a PKC activator and a 30%-50% reduction in both the initial peak force and sustained force in response to various G protein-coupled receptor(GPCR) agonists. Our observations showed that CPI-17-mediated calcium sensitization is mediated through a GPCR/PKC/CPI-17/MLCP/RLC signaling pathway. We therefore propose that the upregulation of CPI-17-mediated calcium-sensitized vasocontraction by obesity contributes to the development of obesity-related hypertension.

关键词： CPI-17 Calcium sensitization Obesity-related hypertension

Comparison of C50 for Propofol-remifentanil Target-controlled Infusion and Bispectral Index at Loss of Consciousness and Response to Painful Stimulus in Elderly and Young Patients

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Chinese Medical Journal 2015年第15期128卷 1994-1999页

作者： Ning Yang Ming-Zhang Zuo Yun Yue Yun Wang Yu Shi xue-na Zhang Department of Anaesthesiology Beijing Chao-Yang Hospital Capital Medical University Beijing 100020 China Department of Anaesthesiology Beijing Hospital Beijing 100730 China

Background：In this prospective randomized study,we compared the predicted blood and effect-site C50 for propofol and remifentanil target-controlled infusion （TCI） and the bispectral index （BIS） values at loss of consciousness （LOC） and response to a standard noxious painful stimulus （LOS） in elderly and young patients,*** hypothesized that the elderly patients will require lower target concentration of both propofol and remifentanil at above two clinical ***：There were 80 American Society of Anesthesiologists （ASA） physical status Ⅰ Ⅱ unpremedicated patients enrolled in this study,they were divided into elderly group （age ≥65 years,n =40） and young group （aged 18-54 years,n =40）.Propofol was initially given to a predicted blood concentration of 1.2 μg/ml and thereafter increased by 0.3 μg/ml every 30 s until Observer＇s Assessment of Alertness and Sedation score was *** propofol level was kept constant,and remifentanil was given to provide a predict blood concentration of 2.0 ng/ml,and then increased by 0.3 ng/ml every 30 s until loss of response to a tetanic *** （version 3.22,BIS Quattro sensor） was also ***：In elderly group,the propofol effect-site C50 at LOC of was 1.5 （1.4-1.6） μg/ml,was significantly lower than that of young group,which was 2.2 （2.1-2.3） μg/ml,the remifentanil effect-site C50 at LOS was 3.5 （3.3-3.7） ng/ml in elderly patients,was similar with 3.7 （3.6-3.8） ng/ml in young *** percent of patients lost consciousness at a BIS value of 57.3 （56.4-58.1）,was similar with that of young group,which was 55.2 （54.0-56.3）.Conclusion：In elderly patients,the predicted blood and effect-site concentrations of propofol at LOC were lower than that of young *** same sedation status,predicted blood and effect-site concentrations of remifentanil required at LOS were similar in elderly and young *** were not affected by ***-propofol/high-opioid may be optional TCI strategy for elderly

关键词： Bispectral Index Painful Stimulus Propofol-remifentanil Target-controlled Infusion