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Chinese Journal of Chemistry 2016年第4期34卷 403-411页

作者： Yilin Fang Mengwu Xiao Aixi Hu Jiao Ye wenwen lian Ailin Liu College of Chemistry and Chemical Engineering Hunan University Changsha Hunan 410082 China Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beifing 100050 China

A series of novel 3-（（4-（t-buty-）-2-（2-benzylidenehydrazinyl）thiazol-5-yl）methyl）quinolin-2（1H）-ones （7a--7z） were designed, synthesized and evaluated for their ability of inhibiting neuraminidase （NA） of influenza H1N1 virus. Some compounds displayed moderate influenza NA inhibitory activity. Compound 71 with the scaffold of 2-（2-（2-methoxybenzylidene）hydrazinyl）thiazole was the best one, exhibiting moderate NA inhibitory activity with ICs0 of 44.66 ~tmol/L. Structure-activity relationship showed that compounds with methoxy or hydroxy groups at the ortho position, fluorine and nitro groups at the meta position and chlorine and bromine groups at the para posi- tion of phenyl ring were more active. Docking study indicated that compound 71 has important interactions with some key residues （including Asp151, Glu119, Arg292, Tyr406, and Asn347） and binds to 430-cavity adjacent to NA active site.

关键词： neuraminidase inhibitor 3-((4-(t-butyl)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones 2-(2-hydrazinyl)thiazole scaffold synthesis docking

Astragaloside IV Alleviates Acute Liver Failure Induced by D-GalN/LPS by Upregulating Autophagy and Reducing Inflammation

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Infectious Microbes & Diseases 2024年第1期6卷 20-28页

作者： Meng Hong wenwen lian Ying Yang Zhi Chen State Key Laboratory for Diagnosis and Treatment of Infectious Diseases National Clinical Research Center for Infectious DiseasesNational Medical Center for Infectious DiseasesCollaborative Innovation Center for Diagnosis and Treatment of Infectious DiseasesThe First Affiliated HospitalZhejiang University School of MedicineHangzhouChina

Acute liver failure(ALF)is a life-threatening condition that manifests in an extremely serious manner and progresses *** following study investigated the protective effect of astragaloside IV(AS-IV),a traditional Chinese drug,on ALF,and its underlying mechanisms,focusing on autophagy and inflammation *** were randomly divided into a saline group,a D-galactosamine and lipopolysac-charide(D-GalN/LPS)group and an AS-IV *** analysis,immunohistochemistry,cytometric bead array,high-throughput quantitative PCR,flow cytometry and Western analysis were used to assess inflammation and liver damage 5 hours after D-GalN/LPS *** IV treatment reduced mortality by alleviating D-GalN/LPS–induced hepatic damage and decreasing inflammation(decreasing Ly6c+monocyte levels,reducing inflammatory cytokines and increasing anti-inflammatory factors)as well as upregulating ***,PCR array was used to detect expression of autophagy-related genes,which demonstrated a Log2 fold change in gene expression between the AS-IV and D-GalN/LPS groups ranging from 1.19 to-3.53,with Tnfsf10 showing the largest alteration be-tween the two *** data suggest that AS-IV may alleviate ALF by upregulating autophagy and reducing inflammation,and it may therefore be an interesting drug for alleviating ALF.

关键词： astragaloside IV acute liver failure inflammation autophagy

Synthesis of Chaicone Derivatives Containing Furan or/and Pyran Ring as Neuraminidase Inhibitors

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Chemical Research in Chinese Universities 2019年第3期35卷 395-402页

作者： CHEN Aiyu lianG Yongdong YE Jiao HU Aixi lian wenwen LIU Ailin DU Guanhua College of Chemistry and Chemical Engineering Hunan UniversityChangsha 410082P.R.China Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050P.R.China

Twenty-seven novel chaicone derivatives were designed and synthesized as neuraniinidase(NA) inhibitors. A concise suitable synthetic strategy was employed in the target compounds? synthesis with relatively high yields. The synthesized compounds were evaluated for their inhibitory activities against the NA of influenza A virus in vitro. The results show that compound 9b possesses the most potent NA inhibitory activity. Structure-activity relationship studies indicate that the chaicone system and hydrogen bond donor substituent are significant for the NA inhibitory activity. And the chaicone derivatives containing pyran ring have better NA inhibitory activity than those without the pyran ring. In addition, molecular docking studies reveal that compounds 9b and 9u are in the good binding mode with Zanamivir binding sites. This study indicates that compound 9b could be selected as a potent compoxind for further structural optimization and development of novel NA inhibitors.

关键词： Chaicone derivative Neuraminidase inhibitor Molecular docking

Pharmacokinetic study of gallocatechin-7-gallate from Pithecellobium clypearia Benth. in rats

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Acta Pharmaceutica Sinica B 2016年第1期6卷 64-70页

作者： Chao Li Xiaowei Song Junke Song Xiaocong Pang Zhe Wang Ying Zhao wenwen lian Ailin Liu Guanhua Du Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing Key Laboratory of Drug Target and Screening Research State Key Laboratory of Bioactive Substance and Function of Natural Medicines

The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was used to calculate the pharmacokinetic parameters. For different i.v. doses of J10688, the mean peak plasma concentration (C-0) values ranged from 11.26 to 50.82 mg/L, and mean area under the concentration -time curve (ALC(0-i)) values ranged from 1.75 to 11.80 (mg ' h/L). J10688 lacked dose dependent pharmacokinetic properties within doses between 1 and 10 mg/kg, based on the power model. The method developed in this study was sensitive, precise, and stable. The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values. These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

关键词： Galloeatechin-7-gallata LC-MS Pharmacokinetics Dose proportionality Non-compartment mode

FXYD3 enhances IL-17A signaling to promote psoriasis by competitively binding TRAF3 in keratinocytes

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Cellular & Molecular Immunology 2023年第3期20卷 292-304页

作者： Wenjuan Yang Rukun He Hao Qu wenwen lian Yue Xue Tao Wang Wenlong Lin Peishuo Zhu Meng Xia Lihua Lai Qingqing Wang Institute of Immunology Zhejiang University School of Medicine310058 HangzhouChina liangzhu Laboratory Zhejiang University Medical Center1369 West Wenyi Road311121 HangzhouChina Department of Orthopedic Surgery The Second Affiliated HospitalZhejiang University School of Medicine310009 HangzhouChina Department of Pharmacology Zhejiang University School of Medicine310058 HangzhouChina

Psoriasis is a common chronic inflammatory skin disease characterized by inflammatory cell infiltration and epidermal ***,the regulatory complexity of cytokine and cellular networks still needs to be ***,we show that the expression of FXYD3,a member of the FXYD domain-containing regulators of Na+/K+ATPases family,is significantly increased in the lesional skin of psoriasis patients and mice with imiquimod(IMQ)-induced ***-17A,a cytokine important for the development of psoriatic lesions,contributes to FXYD3 expression in human primary ***3 deletion in keratinocytes attenuated the psoriasis-like phenotype and inflammation in an IMQ-induced psoriasis ***,FXYD3 promotes the formation of the IL-17R-ACT1 complex by competing with IL-17R for binding to TRAF3 and then enhances IL-17A signaling in *** promotes the activation of the NF-κB and MAPK signaling pathways and leads to the expression of proinflammatory *** results clarify the mechanism by which FXYD3 serves as a mediator of IL-17A signaling in keratinocytes to form a positive regulatory loop to promote psoriasis *** FXYD3 may serve as a potential therapeutic approach in the treatment of psoriasis.

关键词： FXYD3 TRAF3 IL-17signaling Keratinocytes Psoriasis

Astragaloside IV Ameliorates Inflammatory Damage in Mice with Acute Liver Failure

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Chinese Medicine 2023年第4期14卷 221-241页

作者： Ying Yang Meng Hong wenwen lian Zhi Chen State Key Laboratory for Diagnosis and Treatment of Infectious Diseases The First Affiliated Hospital Zhejiang University School of Medicine Hangzhou China National Clinical Research Center for Infectious Diseases The First Affiliated Hospital Zhejiang University School of Medicine Hangzhou China National Medical Center for Infectious Diseases The First Affiliated Hospital Zhejiang University School of Medicine Hangzhou China Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases The First Affiliated Hospital Zhejiang University School of Medicine Hangzhou China

Acute liver failure is a life-threatening clinical syndrome with a high mortality rate. Currently, the research on Astragaloside IV in liver diseases primarily focuses on liver cancer, and there is limited understanding of its mechanism in acute liver failure’s innate immunity. Therefore, this study aims to investigate the potential protective effect of Astragaloside IV on acute liver failure and its impact on innate immune cells. The study employed D-GalN/LPS-induced acute liver failure mouse models and employed various techniques such as a range of molecular and analytical techniques. The experimental results demonstrated that treatment with Astragaloside IV significantly reduced the inflammatory response, alleviated liver injury, and improved the survival rate of mice with acute liver failure induced by D-GalN/LPS. Further investigations revealed that AS-IV played a beneficial role by regulating the proportion of CD11b+Ly6Chi monocytes and the secretion of inflammatory cytokines and anti-inflammatory metabolites. These findings suggest that the pharmacological mechanism of AS-IV may involve targeted regulation of CD11b+Ly6Chi monocytes in both peripheral blood and liver. The implications of this study’s results are twofold. Firstly, they provide a basis for the clinical application of AS-IV in treating liver failure, offering potential therapeutic benefits. Secondly, they serve as a reference for further development of safer and more effective modified compounds.

关键词： Astragaloside IV Acute Liver Failure Inflammation Monocyte Autophagy

Deficiency of FXYD3 in IECs accelerates DSS-induced colitis through STAT3 signaling

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Deficiency of FXYD3 in IECs accelerates DSS-induced colitis ...

全媒体环境下北京农学院大学生记者团文化素养提升途径探索——以北京农学院大学生记者团为例

第十三届全国免疫学学术大会

作者： Yue Xue Wenjuan Yang Jiaqi Zhi wenwen lian Lihua Lai Qingqing Wang Institute of Immunology Zhejiang University School of Medicine

Background: FXYD3 belongs to a family of Na, K-ATPase regulators which have a domain of ***3, mainly expresses in breast, colon, stomach and prostate, is able to interact with Na, K-ATPase and sequentially modifies the transport properties of Na, *** study aims to investigate the function of FXYD3 in regulating intestine ***: Firstly, we detected the distribution of FXYD3 in colon tissues with immunofluorescence(IF) *** used DSS-induced colitis model in FXYD3(WT) and P-villin-cre FXYD3(cKO) mice to investigate the role of FXYD3 in intestinal epithelial cells(IEC).Then we measured the permeability of colon with FITC-dextran in mice during ***67 staining and western blot assays were used to detect the cell proliferation and signaling activation in *** used flow cytometry assay to investigate the changes of colitis-related inflammatory cells in WT and cKO *** was used to detect the growth rate of human goblet cell line LS174T with knocking down FXYD3 by ***: The results of IF in mice colon revealed that FXYD3 co-localized with goblet cell marker *** colitis was found in cKO mice with lower body weight and more tissue damage in colon *** were a higher FITC-dextran concentration in cKO mice and more colitis-related inflammatory *** down FXYD3 in LS174T cells decreased the growth rate and STAT3 signaling ***: FXYD3 is selectively expressed in colon goblet cells, which is dispensable for goblet cells proliferation through activating STAT3 ***3 deficiency in IECs accelerates DSS-induced colitis.

关键词： FXYD3 Goblet cell Colitis STAT3

来源： cnki会议 cnki会议评论

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文化创新比较研究 2021年第10期5卷 92-95页

作者：廉文文北京农学院北京102206

全媒体的迅猛发展提升了新闻传播的效率和影响力,也大大提升了高校新闻传播的宣传力度和覆盖面,已经成为高校宣传的发展必然趋势。全媒体的迅猛发展对高校大学生记者团的素质提升提出了新的更高的要求。该文一方面分析了全媒体时代的高... 详细信息

全媒体的迅猛发展提升了新闻传播的效率和影响力,也大大提升了高校新闻传播的宣传力度和覆盖面,已经成为高校宣传的发展必然趋势。全媒体的迅猛发展对高校大学生记者团的素质提升提出了新的更高的要求。该文一方面分析了全媒体时代的高校宣传特点,以及大背景下北京农学院大学生记者团的实际情况和面临的困境,通过北京农学院大学生记者团的实际建设,探索了提升大学生记者文化素养的路径。

关键词：全媒体大学生记者团文化素养

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妊娠期糖尿病流行病学特征及危险因素分析

中国公共卫生管理 2024年第3期40卷 416-418,425页

作者：张蕾连文文宁波市鄞州第二医院浙江宁波315100

目的调查分析妊娠期糖尿病(gestational diabetes mellitus,GDM)流行病学特征及危险因素,为制定GDM预防方案提供依据。方法选取2020—2022年在鄞州第二医院建档的3204名孕妇作为调查对象,应用χ^(2)检验、二分类logistic回归分析评估GD... 详细信息

目的调查分析妊娠期糖尿病(gestational diabetes mellitus,GDM)流行病学特征及危险因素,为制定GDM预防方案提供依据。方法选取2020—2022年在鄞州第二医院建档的3204名孕妇作为调查对象,应用χ^(2)检验、二分类logistic回归分析评估GDM患病的影响因素。结果GDM患病率为11.11%,且2020—2022年患病率逐年增长(χ^(2)=5.624,P=0.037)。年龄、产次、糖尿病家族史、孕前BMI、多囊卵巢综合征(OR=3.047、2.423、3.904、3.323、3.010)是GDM的独立危险因素。结论鄞州第二医院2020—2022年GDM患病率逐年增长,且与年龄、产次、糖尿病家族史、孕前BMI、多囊卵巢综合征等因素相关。因此,应加强高危人群的早期筛查,同时做好针对性措施,从而降低GDM发生风险。

关键词：妊娠期糖尿病流行病学特征孕前 BMI

疼痛门诊慢性非癌性疼痛病人阿片类药物使用情况分析及评价

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中国疼痛医学杂志 2023年第10期29卷 748-753页

作者：安龙牟致平孔旭东樊碧发连雯雯覃旺军中日友好医院药学部北京100029 北京中医药大学东直门医院药学部北京101121 中日友好医院疼痛科北京100029

目的:分析疼痛专科门诊慢性非癌性疼痛病人阿片类药物的使用情况,为慢性非癌性疼痛病人合理用药提供参考。方法:回顾性分析2022年3月至2022年8月中日友好医院疼痛科门诊中慢性非癌性疼痛病人使用阿片类药物的处方,整理病人基本信息、疾... 详细信息

目的:分析疼痛专科门诊慢性非癌性疼痛病人阿片类药物的使用情况,为慢性非癌性疼痛病人合理用药提供参考。方法:回顾性分析2022年3月至2022年8月中日友好医院疼痛科门诊中慢性非癌性疼痛病人使用阿片类药物的处方,整理病人基本信息、疾病病种、药物用量等信息,结合指南进行处方的合理性评价。结果:纳入符合标准的处方1102张,涉及1070例次病人。使用最多的品种为盐酸曲马多缓释片,为691例次(占比54.41%)。阿片类药物日剂量在50~90吗啡毫克当量(morphine milligram equivalents,MME)范围内的病人最多,为604例次(占比56.45%)。老年(年龄≥65岁)病人的阿片类药物平均日剂量为80 MME,显著高于非老年(0.05)。依据指南,我院阿片类药物处方共含21类/种慢性非癌性疼痛适应证。1833疾病例次(占比96.37%)含18类/种适应证,在指南中被推荐可选用阿片类药物治疗;18疾病例次(占比0.95%)含2类/种适应证,在不同指南中对是否可以使用阿片类药物治疗的推荐存在争议。结论:门诊慢性非癌性疼痛病人的阿片类药物使用合理性高,老年病人使用日剂量相对较大,需要给予更多药学监护。

关键词：慢性非癌性疼痛阿片类药物吗啡毫克当量