检索结果-南通市图书馆

Reverse effect of curcumin on CDDP-induced drug-resistance via Keap1/p62-Nrf2 signaling in A549/CDDP cell

Asian Pacific Journal of Tropical Medicine 2017年第12期10卷 1190-1196页

作者： Jie Shen Ya-Juan Chen Yuan-Wei Jia Wen-Ying Zhao Guang-Hai Chen Ding-Feng Liu Yun-Yu Chen Chao Zhang Xiao-Ping Liu anhui provincial center for drug clinical evaluation Yijishan HospitalWannan Medical CollegeWuhuAnhui 241001China Pharmacy School Wannan Medical CollegeWuhuAnhui 241002China Department of clinical Pharmacy Yijishan HospitalWannan Medical CollegeWuhuAnhui 241001China anhui provincial Engineering Research center for Polysaccharides drugs Wannan Medical CollegeWuhuAnhui 241001China oncology department yijishan hospital wannan medical college

Objective: To assess the effect of curcumin on CDDP-induced drug resistance and explore the underlying molecular mechanism through Nrf2 system and autophagy ***: A drug-resistant cell model was established by exposing A549/CDDP cell to2 μg/mL CDDP. A549/CDDP cell was treated with 20 μg/mL CDDP and 10 μM curcumin. The cell viability and apoptosis level, the signals of Keap1/P62-Nrf2 and autophagy pathway were ***: CDDP induction promoted drug-resistant phenotype in A549/CDDP cell and activated autophagy as well as Nrf2 signals in A549/CDDP cell. Meanwhile, curcumin combination attenuated autophagy and Nrf2 activation induced by CDDP, and reversed the drug-resistant phenotype. Notably, curcumin combination augmented Keap1 transcription. Furthermore, Keap1 ablation with short hairpin RNAs hampered the efficacy of curcumin, suggesting Keap1 played a crucial role on reversal effect of ***: The present findings demonstrate that CDDP promotes abnormal activation of Nrf2 pathway and autophagy, leading to drug resistance of A549/CDDP *** attenuates this process and combat drug-resistance through its potent activation on Keap1 transcription, which is essential for interplay between oxidative stress induced Nrf2 activation and autophagy/apoptosis switch.

关键词： Curcumin drug-resistance Keap1 Nrf2 Autophagy

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

UFLC-ESI-MS/MS method to investigate bioavailability,influence of dosage levels and multiple-doses on helicid pharmacokinetics behavior

UFLC-ESI-MS/MS method to investigate bioavailability,influen...

引用

2016“定量药理学与药物临床评价”国家级继续教育培训班

作者： Yuanwei Jia Haitang Xie Jie Shen Minhui Wang anhui provincial center for drug clinical evaluation Yijishan HospitalWannan Medical College

A rapid,simple,sensitive and reliable UFLC-ESI-MS/MS method was developed for quantifying helicid in rat *** lower limit of quantitation(LLOQ) of helicid was ***/mL while the run time was 2 *** method was validated for selectivity,linearity,accuracy and precision,extraction recoveries,matrix effects,carry-over,cross talk,dilution integrity,stability and incurred sample reanalysis(ISR).Using this validated method,bioavailability,and influences of different dosage levels or multiple-doses on pharmacokinetic behaviors of helicid were fully *** showed that after intragastric administration(i.g.) at three dose levels(25,50,100 mg/kg),helicid had a linear pharmacokinetic behavior and the bioavailabilities at three dose levels were 48.34%,48.17%and 60.34%.Meanwhile,besides T,multiple-dosing of helicid(50 mg/kg,tid) for 6 days seemed not greatly affect the PK profiles and cause no accumulation in rats.

关键词： helicid ultra fast liquid chromatography-electrospray ionization-tandem mass spectrometry(UFLC-ESI-MS/MS) bioavailability Pharmacokinetics

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

豆腐果苷WN7-6类衍生物抗抑郁活性筛选探索研究

引用

中国临床药理学与治疗学 2007年第10期12卷 1190-1191页

作者：童九翠谢海棠江思艳杨斌芮家亮 anhui provincial center for drug clinical evaluation Yijishan Hospital of Wannan Medical College

AIM: To search some compounds that have anti-depressive activity from Helicid WN7-6 and its derivatives, and to explore their structure-function relationship. METHODS: 21 compounds including WN7-6, the lead compound were screened for antidepressant effect by the behavioral despair models(tail suspension test and the forced swimming test). And to study their stimulative effect on central nerve system(CNS) by mice autonomic activity test. RESULTS: Results shown that 11 of these compounds could decrease immobile time in suspend tail test and 6 compounds had the similar effect in force swimming test, compared with that of control group, the immobile time was obviously reduced (P<0.05, P<0.01). The results of autonomic activity test indicated that only 7 compounds could inhibit the activities of CNS (P<0.05, P<0.01). CONCLUSION: 30%-50% of these derivatives have anti-depressive activities, and much attention should be paid to further researches.

关键词：豆腐果苷WN7-6类衍生物抗抑郁活性筛选药物

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

evaluation of repeated exposure systemic toxicity test of PVC with new plasticizer on rats via dual parenteral routes

引用

Regenerative Biomaterials 2018年第1期5卷 9-14页

作者： Li Hou Chunguang Fan Chenghu Liu Qiujin Qu ChunrenWang Yanping Shi Department of Biological evaluation Key Lab of Biological Evaluation of Medical DevicesShandong Provincial Inspection Center for Medical DevicesJinan 250101China Department of Biomaterials and Tissue Engineering National Institutes for Food and Drug Control of ChinaBeijing 100050China

Systemic toxicity caused by repeated exposure to both polar and nonpolar leachables of di(2-ethylhexyl)-1,2-cyclohexane plasticized polyvinyl chloride(PVC)was evaluated with dual routes of parenteral administration method on rats in the *** group and control group were designed by *** intravenous injection with 0.9%sodium chloride injection extracts and intraperitoneal injection with corn oil extracts were conducted to the experimental rats while tail intravenous injection with 0.9%sodium chloride Injection and intraperitoneal injection with corn oil were conducted to the control *** 14 days,blood specimens were collected for clinical pathology(hematology and clinical chemistry)*** organs were weighed and a histopathological examination was *** a result,compared with the control animals,there were no toxicity-related changes on the parameters *** results show that the rats do not show obvious systemic toxicity reaction caused by repeated exposure with dual routes of parenteral administration method on rats after administration with both polar and nonpolar exacts of di(2-ethylhexyl)-1,2-cyclohexane plasticized PVC simultaneously up for 14 days.

关键词： plasticized PVC repeated exposure systemic toxicity test dual routes of parenteral administration method

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

A novel marine-derived anti-acute kidney injury agent targeting peroxiredoxin 1 and its nanodelivery strategy based on ADME optimization

引用

Acta Pharmaceutica Sinica B 2024年第7期14卷 3232-3250页

作者： Ping Yu Tanwei Gu Yueyang Rao Weimin Liang Xi Zhang Huanguo Jiang Jindi Lu Jianglian She Jianmin Guo Wei Yang Yonghong Liu Yingfeng Tu Lan Tang Xuefeng Zhou Guangdong provincial Key Laboratory of New drug Screening Guangdong-Hong Kong-Macao Joint Laboratory for New Drug ScreeningSchool of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology Guangdong Key Laboratory of Marine Materia MedicaSouth China Sea Institute of OceanologyChinese Academy of SciencesGuangzhou 510301China NMPA Key Laboratory for Research and evaluation of drug Metabolism School of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China Guangdong Lewwin Pharmaceutical Research Institute Co. Ltd.Guangdong Provincial Key Laboratory of Drug Non-Clinical Evaluation and ResearchGuangdong Engineering Research Center for Innovative Drug Evaluation and ResearchGuangzhou 510990China

Insufficient therapeutic strategies for acute kidney injury(AKI)necessitate precision therapy targeting its *** study reveals the new mechanism of the marine-derived anti-AKI agent,piericidin glycoside S14,targeting peroxiredoxin 1(PRDX1).By binding to Cys83 of PRDX1 and augmenting its peroxidase activity,S14 alleviates kidney injury efficiently in Prdx1-overexpression(Prdx1-OE)***,S14 also increases PRDX1 nuclear translocation and directly activates the Nrf2/HO-1/NQO1 pathway to inhibit ROS *** to the limited druggability of S14 with low bioavailability(2.6%)and poor renal distribution,a pH-sensitive kidney-targeting dodecanaminechitosan nanoparticle system is constructed to load S14 for precise treatment of AKI.L-Serine conjugation to chitosan imparts specificity to kidney injury molecule-1(Kim-1)-overexpressed *** developed S14-nanodrug exhibits higher therapeutic efficiency by improving the in vivo behavior of S14 *** encapsulation with micelles,the AUC_(0-t),half-life time,and renal distribution of S14 increase 2.5-,1.8-,and 3.1-fold,*** main factors contributing to the improved druggability of S14 nanodrugs include the lower metabolic elimination rate and UDPglycosyltransferase(UGT)-mediated *** summary,this study identifies a new therapeutic target for the marine-derived anti-AKI agent while enhancing its ADME properties and druggability through nanotechnology,thereby driving advancements in marine drug development for AKI.

关键词： Acute kidney injury Piericidin glycoside Peroxiredoxin 1 Nanodrug Kim-1 targeted ADME Marine drug druggability

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Effects of total flavonoids of Rhododendra simsii on ameliorating brain injury via G protein-coupled SOCE pathway mediated by STIM and Orai in subacute phase of ischemia/reperfusion

引用

中国药理学与毒理学杂志 2021年第10期35卷 768-769页

作者： LU Jia-jun JIANG Chen-chen HE Yu-xiang SHI Lei YIN Xiu-yun CHEN Zhuo CAO Di HAN Jun Department of Pharmacology Drug Research and Development CenterSchool of pharmacyWannan Medical CollegeWuhu 241002China anhui provincial Engineering Laboratory for Screening and Re-evaluation of Active Compounds of Herbal Medicines in Southern anhui Wuhu 241002China anhui provincial Engineering Research center for Polysaccharide drugs Wuhu 241002China

OBJECTIVE To explore the effect of total flavonoids of Rhododendra simsii(TFR)on improving cerebral ischemia/reperfusion injury(CIRI)and its relationship with STIM/Orai-regulated operational Ca^(2+)influx(SOCE)*** Oxygen-glucose deprivation/reoxygenation(OGD/R)PC12 cells were used to simulate CIRI in vitro,and the intracellular Ca^(2+)concentration and apoptosis rate of PC12 cells were detected by laser confocal microscope and flow cytometry,*** regulation of STIM/Orai on SOCE was analyzed by STIM/Orai gene silencing and STIM/O rai gene *** CIRI model was established by MCAO in SD *** activities of inflammatory cytokines IL^(-1),IL-6 and TNF-αin serum were detected by *** pathological changes of ischemic brain tissue and the infarction of rat brain tissue were detected by HE staining and TTC *** protein and mRNA expression levels of STIM1,STIM2,Orai1,caspase-3 and PKB in brain tissue were detected by Western blotting and RT-qPCR,*** The results of in vitro experiment showed that the fluorescence intensity of Ca^(2+)and apoptosis rate in PC12 cells treated with TFR were significantly lower than those in OGD/R group,and this trend was enhanced by SOCE antagonist ***1/STIM2/Orai1 gene silencing significantly reduced apoptosis and Ca^(2+)overload in OGD/R model,while TFR combined with overexpression of STIM1/STIM2/Orai1 aggravated apoptosis and Ca2+*** the in vivo experiment,TFR significantly reduced the brain histopathological damage,infarction of brain tissue,the contents of IL^(-1),IL-6 and TNF-αin the serum in MCAO rats and down-regulated the expression of STIM1,STIM2,Orai1 and caspase-3 protein and mRNA in the brain tissue,and up-regulated the expression of *** above effects were enhanced by the addition of *** The above results indicate that TFR may reduce the contents of inflammatory factors and apoptosis,decrease Ca2+overload and ameliorate brain injury b

关键词： total flavonoids of Rhododendra simsii cerebral ischemia/reperfusion injury STIM/Orai store-operated calcium entry 2-APB

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Schisandra lignans ameliorate nonalcoholic steatohepatitis by regulating aberrant metabolism of phosphatidylethanolamines

引用

Acta Pharmaceutica Sinica B 2023年第8期13卷 3545-3560页

作者： Lijuan Xue Keanqi Liu Caixia Yan Junling Dun Yexin Xu Linlin Wu Huizhu Yang Huafang Liu Lin Xie Guangji Wang Yan Liang Key Lab of drug Metabolism&Pharmacokinetics State Key Laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjing 210009China Zhejiang provincial Key Laboratory for drug evaluation and clinical Research Department of Clinical Pharmacythe First Affiliated HospitalZhejiang University School of MedicineHangzhou 310003China Analytical Applications center Shimadzu(China)Co.Ltd.Shanghai 200233China

Nonalcoholic steatohepatitis(NASH)is a spectrum of chronic liver disease characterized by hepatic lipid metabolism *** reports emphasized the contribution of triglyceride and diglyceride accumulation to NASH,while the other lipids associated with the NASH pathogenesis remained *** specific purpose of our study was to explore a novel pathogenesis and treatment strategy of NASH via profiling the metabolic characteristics of ***,multi-omics techniques based on LC—Q-TOF/MS,LC—MS/MS and MS imaging were developed and used to screen the action targets related to NASH progress and treatment.A methionine and choline deficient(MCD)diet-induced mouse model of NASH was then constructed,and Schisandra lignans extract(SLE)was applied to alleviate hepatic damage by regulating the lipid metabolism-related enzymes CES2A and *** lipidomics indicated that MCD-diet led to aberrant accumulation of phosphatidylethanolamines(PEs),and SLE could significantly reduce the accumulation of intrahepatic ***,exogenous PE(18:0/18:1)was proved to significantly aggravate the mitochondrial damage and hepatocyte *** PE(18:0/18:1)also deteriorated the NASH progress by up regulating intrahepatic proinflammatory and fibrotic factors,while PE synthase inhibitor exerted a prominent hepatoprotective *** current work provides new insights into the relationship between PE metabolism and the pathogenesis of NASH.

关键词： Nonalcoholic steatohepatitis Multi-omics Schisandra lignans extract Phosphatidyle thanolamine PE(18:0/18:1)

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Quantum entangled connectivity and functional connectivity of human brain

引用

International Journal of Biomathematics 2023年第8期16卷 109-120页

作者： You Zhai Linjie Qiu Chenxiang He Lina Wang Jian Zhai Research center for clinical Pharmacy Zhejiang provincial Key Laboratory for drug evaluation and clinical Research The First Affiliated Hospital Zhejiang University School of Medicine Hangzhou310003China School of Mathematical Sciences Zhejiang University Hangzhou 310027China The Second Affiliated Hospital Zhejiang University School of Medicine Hangzhou 310003 China

Quantum process may conduce to brain ***,it was proposed that the Posner molecules,Cag(PO4)6,can serve as neural qubits,which can maintain quantum entanglement between phosphorus nuclei for quite a long *** study the process from entangled Posner molecules to the synchronized activities of brain.A diffusion model of Posner molecules with appropriate boundary conditions and the mean first arriving time of Posner molecules from one area of brain to another are *** establish linkages between the quantum entangled connectivity of brain and the remaining time of entangled Posner molecules before *** on these results,we find direct correlations between entangled Posner molecules and the functional connectivity of human ***,we discover that the quantum entangled connectivity depends on age.

关键词： Posner molecule diffusion model quantum entangled connectivity functional connectivity

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Exploration of 5-cyano-6-phenylpyrimidin derivatives containing an 1,2,3-triazole moiety as potent FAD-based LSD1 inhibitors

引用

Acta Pharmaceutica Sinica B 2020年第9期10卷 1658-1668页

作者： Liying May Haojie Wangy Yinghua You Chaoya Ma Yuejiao Liu Feifei Yang Yichao Zheng Hongmin Liu Collaborative Innovation center of New drug Research and Safety evaluation Henan ProvinceKey Laboratory of Technology of Drug Preparation(Zhengzhou University)Ministry of Education of ChinaKey Laboratory of Henan Province for Drug Quality and EvaluationSchool of Pharmaceutical SciencesZhengzhou UniversityZhengzhou 450001China

Histone lysine specific demethylase 1(LSD1)has become a potential therapeutic target for the treatment of *** and develop novel and potent LSD1 inhibitors is a challenge,although several of them have already entered into clinical ***,for the first time,we reported the discovery of a series of 5-cyano-6-phenylpyrimidine derivatives as LSD1 inhibitors using flavin adenine dinucleotide(FAD)similarity-based designing strategy,of which compound 14 q was finally identified to repress LSD1 with IC50=183 nmol/*** analysis suggested that compound 14 q fitted well into the FAD-binding *** mechanism studies showed that compound 14 q may inhibit LSD1 activity competitively by occupying the FAD binding sites of LSD1 and inhibit cell migration and invasion by reversing epithelial to mesenchymal transition(EMT).Overall,these findings showed that compound14 q is a suitable candidate for further development of novel FAD similarity-based LSD1 inhibitors.

关键词： LSD1 inhibitors Pyrimidine Anticancer Flavin adenine dinucleotide(FAD) Gastric cancer

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Protective effects of timosaponin BⅡ and sarsasapogenin on timosaponin AⅢ-induced hepatotoxicity in rats

Protective effects of timosaponin BⅡ and sarsasapogenin on ...

引用

2016“定量药理学与药物临床评价”国家级继续教育培训班

作者： Cuifeng Zhang Yuanwei Jia Hua Hu Chenggang Huang Guoyu Pan Haitang Xie Department of clinical Pharmacy Yijishan Hospital of Wannan Medical CollegeAnhui Provincial Center for Clinical Drug Evaluation Shanghai Institute of Materia Medica Chinese Academy of Sciences

Timosaponin BⅡ(TB Ⅱ) is a natural bioactive steroid glycoside isolated from Anemarrhena asphodeloides Bge(***),which is metabolized to Timosaponin AⅢ(TAⅢ) and then to sarsasapogenin(SGA) by intestinal *** previous study reported that TAⅢ caused liver injury by inducing oxidative stress and down-regulating bile acid ***,no liver injury was observed after TB Ⅱ administration in *** hypothesized that TB Ⅱ and SGA may protect the liver against TAⅢ-induced *** influences of TB Ⅱ and SGA on the level of reactive oxygen species(ROS) and cell viability and mitochondrial function(ATP) in primary rat hepatocytes were *** addition,in vitro enterobacteria metabolism and the pharmacokinetics of the three compounds were ***,an integrated multiple compartment PK-TD model was constructed,which illustrated the distribution of the three compounds in the liver and plasma,and indicated whether there were hepatotoxicity after TB Ⅱ *** in *** results showed that 1) the liver concentration of TAⅢwas about 10-fold higher than TBⅡ and SGA after TBⅡ *** in rats,and TBⅡcould be directly metabolized to SGA.2) Compared with administration of TAⅢ alone,the TAⅢ+TBⅡ and TAⅢ+SGA groups exhibited significantly decreased ROS generation by TAⅢand increased cell viability and ATP levels.3) The model simulation indicated that there were no hepatotoxicity after TB Ⅱ i.g administration in *** summary,these results indicated that TB IT and SGA can protect TAⅢ-induced hepatotoxicity after TB IT *** in rats.

关键词：

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：