检索结果-南通市图书馆

Chinese Journal of Integrative Medicine 2009年第6期15卷 442-447页

作者：聂红孟兰贞周玖瑶樊晓峰罗勇张广文 College of Pharmacy Jinan University Guangzhou University of Chinese Medicine Research Center for Analytical Sciences of Northeastern University College of Science and Engineering Jinan University

Objective:To demonstrate the vasodilatation activity of the coumarin-containing Angelica dahurica *** and to further analyze active components in the herb ***:(1) The vasodilatation effects induced by different extracts(cyclohexane,ethyl acetate,acetone,methanol,95%ethanol and water) of Angelica dahurica *** on mouse thoracic aorta pre-contracted with phenylephrine were investigated. (2) The amount of imperatorin and isoimperatorin in each extract was measured by high-perfor...

关键词： Angelica dahurica var.formosana thoracic aorta vasodilatation imperatorin isoimperatorin high-performance liquid chromatography

Estrogenic activity of osthole and imperatorin in MCF-7 cells and their osteoblastic effects in Saos-2 cells

在线全文

学校读者我要写书评

暂无评论

Chinese Journal of Natural Medicines 2016年第6期14卷 413-420页

作者： JIA Min LI Yuan XIN Hai-Liang HOU Ting-Ting ZHANG Nai-Dai XU Hong-Tao ZHANG Qiao-Yan QIN Lu-Ping Department of Pharmacognosy School of Pharmacy Second Military Medical University

There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy(HRT). The present study was designed to investigate the in vitro effects of estrogen-like activities of two widespread coumarins, osthole and imperatorin, using the MCF-7 cell proliferation assay and their alkaline phosphatase(ALP) activities in osteoblasts Saos-2 cells. The two compounds were found to strongly stimulate the proliferation of MCF-7 cells. The estrogen receptor-regulated ERα, progesterone receptor(PR) and PS2 m RNA levels were increased by treatment with osthole and imperatorin. All these effects were significantly inhibited by the specific estrogen receptor antagonist ICI182, 780. Cell cycle analysis revealed that their proliferation stimulatory effect was associated with a marked increase in the number of MCF-7 cells in S phase, which was similar to that observed with estradiol. It was also observed that they significantly increased ALP activity, which was reversed by ICI182,780. These results suggested that osthole and imperatorin could stimulate osteoblastic activity by displaying estrogenic properties or through the ER pathway. In conclusion, osthole and imperatorin may represent new pharmacological tools for the treatment of osteoporosis.

关键词： Osthole imperatorin MCF-7 Estrogenic activity Estrogen receptors Osteoblasts Alkaline phosphatase

Identification of Herbal Compound imperatorin with Adverse Effects on ANO1 and CFTR Chloride Channels

在线全文

学校读者我要写书评

暂无评论

Chemical Research in Chinese Universities 2011年第3期27卷 461-463页

作者： HAO Feng YI Fei ZHANG Di N1NG Yan SU Wei-heng FENG Xue-chao YANG Hong MA Tong-hui Membrane Channel Research Laboratory Northeast Normal University Changchun 130024 P. R. China School of Life Sciences Liaoning Normal University Dalian 116029 P. R. China

Calcium-activated chloride channels（CaCCs） are the crucial regulators of transepithelial fluid secretion, smooth muscle contraction and sensory transduction. Recently, compelling evidence has indicated that TMEM16A（ANO1 or anoctamin-1） is a bona fide calcium-acvtivated chloride channel. A few small molecule CaCCs regulators are available for functional and therapeutic studies. We screened 126 natural compounds from Chinese herbs. Screening was performed with an iodide influx assay in Fischer rat thyroid epithelial cells to coexpress ANO1 and an iodide-sensitive fluorescent indicator（EYFP-H148Q/I152L）. imperatorin, a coumarin compound, was identified to inhibit ANO1-mediated chloride transport activated by multiple calcium-elevating agonists. The inhibitory effect is dose-dependent with IC50～14.63 μmol/L. Interestingly, imperatorin activated CFTR chloride channel with EC50～35.52 μmol/L. The adverse effects of imperatorin on CaCC and CFTR chloride channels will make it useful in pharmacological dissection of chloride transport in airway and intestinal epithelium. Further studies are required to evaluate the therapeutic effects of imperatorin on hypertension, asthma and certain tumors.

关键词： Calcium-acvtivated chloride channel(CaCC) ANO1 imperatorin Cystic fibrosis transmembrane conductance regulator(CFTR)

imperatorin alleviates Aβ-induced spatial learning memory impairment and neuroinflam⁃mation in model mice of Alzheimer disease

在线全文

学校读者我要写书评

暂无评论

中国药理学与毒理学杂志 2021年第9期35卷 642-643页

作者： WAN Hang-juan LUO Li LIU Xin HE Wei Department of Pharmacology Gannan Medical UniversityKey Laboratory of Cerebrovascular Pharmacology of Jiangxi ProvinceKey Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Diseases of Ministry of Edu-cationGanzhou 341000China

OBJECTIVE To investigate the effects of imperatorin on the spatial learning memory impairment and neuroinflammation in model mice of Alzheimer disease(AD)induced by intracerebroventricular injection of Aβ*** Mouse model of AD was established by injection of Aβ1-42 into the lateral ***⁃peratorin(2.5 and 5.0 mg·kg-1,daily)was inject⁃ed by intraperitoneally 1 h after intracerebroven⁃tricular injection for 13 *** effect of imperato⁃rin on the spatial learning and memory impair⁃ment was assessed by eight arm maze *** levels of cytokines TNF-α,IL-1β,IL-6,IL-18 and chemokines MCP-1 in mouse cortex and hip⁃pocampus were detected by *** protein expression of NF-κB P65,TLR4,MyD88,p-P38,p-ERK,and p-JNK were detected by Western *** As compared with the AD model group,imperatorin treatment significantly attenuated Aβ1-42-induced spatial learning and memory impairment assessed by eight arm maze *** addition,imperatorin significantly reduced the levels of cytokines TNF-α,IL-1β,IL-6,IL-18 and chemokines MCP-1 in the cerebral cortex and ***,Western blotting results showed that imperatorin treat⁃ment significantly down-regulated the protein expression of NF-κB P65,TLR4,MyD88,p-P38,p-ERK,and *** imperatorin has neuroprotective effects in the Aβ1-42 induced AD model mice and its mechanism may be partially associated with the inhibition of inflam⁃matory response in the cortex and hippocampus.

关键词： imperatorin Alzheimer disease Aβ1-42 learning and memory impairment inflam⁃matory response

Mechanisms of imperatorin on regulating Pglycoprotein in blood-brain barrier based on network pharmacology and in vitro experiment

在线全文

学校读者我要写书评

暂无评论

中国药理学与毒理学杂志 2023年第S1期37卷 17-18页

作者： SONG Yizhen YIN Wanxin MA Yicong AN Yufan HUANG Jiaqi YAN Zhongjie WU Xiuwen WANG Yuanyu School of Pharmaceutical Sciences Hebei Medical UniversityShijiazhuang 050017China Department of Neurosurgery the Second Hospital of Hebei Medical UniversityShijiazhuang 050000China

OBJECTIVE To explore mecha⁃nisms of imperatorin on regulating P-glycoprotein(P-gp)in blood-brain barrier(BBB)based on net⁃work pharmacology combined with in vitro experi⁃*** Drug targets were predicted using the Pharmapper and Swiss targets data⁃bases;disease targets were obtained through the Genecards database;intersections between drugs and disease targets were screened by Cytoscape software;the obtained core targets were used to construct protein-protein interaction(PPI)network,gene ontology(GO)functions,and Kyoto encyclopedia of genes and genomes(KEGG)pathway enrichment *** effects of imperatorin(20,50,100μmol·L^(-1))on P-gp activity were monitored in hCMEC/D3 in vitro BBB model,and the effects of imperatorin on the expression of target proteins were verified using Western blot *** 55 drug targets and 3102 disease targets were obtained from the network pharmacology screening,and 37 core targets were obtained after the *** analysis showed that core targets were closely related to chemical synaptic trans⁃mission regulation,neurotransmitter receptor activity,protein kinase regulation activity,G proteincoupled receptor signaling pathway,neural active ligand receptor interaction pathway,PI3K-Akt sig⁃naling pathway,VEGF signaling pathway,etc..In vitro experimental validation suggested that all tested concentration groups of imperatorin signifi⁃cantly reduced the activity and expression of P-gp,which were achieved by significantly downregu⁃lating the phosphorylation levels of PI3K and Akt,and repressing the expression of VEGFR2 pro⁃*** Network pharmacology was used to predict the core targets and signaling pathways of imperatorin on regulating P-gp in BBB and relevant validation was conducted through in vitro experiments,providing a refer⁃ence basis for further exploration of the mecha⁃nisms of imperatorin on regulating P-gp in BBB.

关键词： imperatorin blood-brain barrier P-glycoprotein network pharmacology in vitro experiment

imperatorin inhibits the expression of alpha-hemolysin in Staphylococcus aureus strain BAA-1717(USA300)

在线全文

学校读者我要写书评

暂无评论

Imperatorin inhibits the expression of alpha-hemolysin in St...

An LC-MS/MS Method for Determination of imperatorin and Isoimperatorin in Rat Plasma and Application to a Pharmacokinetic Study

第七届中国畜牧科技论坛

作者： Yin lizi Sun mao Ouyang ping Chen junjie Yin zhongqiong Lin juchun Shu gang He changliang Wang kaiyu College of Veterinary Medicine Sichuan Agriculture University

Both community-associated and hospital-acquired infections with methicillin-resistant Staphylococcus aureus(MRSA) have been increasingly reported around the world in the past 20 *** 2006,the Centers for Disease Control and Prevention(CDC) reported that 64%of MRSA isolates were of the USA300 clonal type in infected patients in *** aim of our study was to estimate the in vitro effect of imperatorin on MRSA strain BAA-1717(USA300).The effects of imperatorin on alpha-hemolysin(Hla) production,when strain BAA-1717 was co-cultured with sub-inhibitory concentrations of imperatorin,were analysed using susceptibility testing,hemolysis assays,western blotting and real-time ***/Dead analysis and cytotoxicity assays were employed to examine the protective effect of imperatorin against the strain BAA-1717-mediated injury of human alveolar epithelial cells(A549).The results showed that imperatorin has no *** activity at the tested concentrations in ***,imperatorin can observably inhibit the production of Hla in culture supernatants and reduce the transcriptional levels of hla(the gene encoding Hla) and arg(the accessory gene regulator).imperatorin prevented Hla-mediated A549 epithelial cell injury in a coculture *** conclusion,our results suggested that imperatorin has the potential to be developed as a new anti-virulence drug candidate for managing *** infection.

关键词： Methicillin-resistant Staphylococcus aureus USA300 alpha-hemolysin imperatorin virulence factor

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

Pharmacology & Pharmacy 2013年第5期4卷 417-424页

作者： Junbo Xing Hong Cao Yumin Chen Caihong Shui Tingting Shan Dan Hu Department of Traditional Chinese Medicine Institute for Drug and Instrument Control of Health Department GLD of PLA Beijing China.

A highly sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the de-termination of imperatorin and isoimperatorin in rat plasma using psoralen as internal standard. Analyses were performed on a Shimadzu HPLC system using a Shimadzu C18 column eluted with a mobile phase of methanol-water (25:75), containing 0.1% formic acid at a flow rate of 0.4 ml/min. The detection was performed by positive ion elec-trospray ionization in multiple reactions monitoring mode, monitoring the transitions m/z 203→147 and m/z 203→159 for imperatorin and isoimperatorin, respectively. The method was validated over the concentration range of 2.5 -1000.0 ng/mL for imperatorin and isoimperatorin. The limits of detection and quantification were 1.0 and 3.0 ng/mL, repectively for both analytes. The intra-day and inter-day accuracy and precision of the assay were less than 10.9%. This method has been applied successfully to a pharmacokinetic study involving the intragastric administration of extract of Angelicae Dahuricae Radix to rats.

关键词： imperatorin Isoimperatorin LC-MS/MS Pharmacokinetic

imperatorin suppresses proliferation and angiogenesis of human colon cancer cell by targeting HIF-1α via the m TOR/p70S6K/4EBP1 and MAPK pathways

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

Imperatorin suppresses proliferation and angiogenesis of hum...

Protective effects of imperatorin against cerebral ischemia/reperfusion-induced oxidative stress through Nrf2 signaling pathway in rats

中国化学会第十一届全国天然有机化学学术会议

作者： Chunliu Mi Juan Ma Ke Si Wang Xuejun Jin Key Laboratory of Natural Resources of Changbai Mountain ＆ Functional Molecules Ministry of education Molecular Medicine Research Center College of Pharmacy Yanbian University

imperatorin is an active natural furocoumarin component originating from the traditional Chinese medicine Angelica dahurica and has been shown to exhibit multiple bioeffector functions, including anti-cancer activity. However, the mechanism by which imperatorin inhibits tumor growth is not fully understood. We here demonstrated the effect of imperatorin on HIF-1 activation. imperatorin showed a potent inhibitory activity against HIF-1 activation induced by hypoxia in various human cancer cell lines. This compound markedly decreased the hypoxia-induced accumulation of HIF-1α protein dose-dependently, whereas it did not affect the expressions of HIF-1β and topoisomerase-I（Topo-I）. Further analysis revealed that imperatorin inhibited HIF-1α protein synthesis, without affecting the expression level of HIF-1α m RNA or degradation of HIF-1α protein. Moreover, the phosphorylation levels of mammalian target of rapamycin（m TOR）, ribosomal protein S6 kinase（p70S6K）, e IF4 E binding protein-1（4E-BP1）, eukaryotic initiation factor 4E（e IF4E）, extracellular signalregulated kinase-1/2（ERK1/2）, SAPK/JNK and p38 were significantly suppressed by imperatorin. Furthermore, imperatorin prevented hypoxia-induced expression of HIF-1 target genes and flow cytometric analysis indicated that imperatorin induced G1 phase arrest in human colon cancer cell（HCT116）. We found that imperatorin administration inhibits tumor growth and blocks tumor angiogenesis in a xenograft tumor model. Taken together, our results suggested that imperatorin is an effective inhibitor of HIF-1, thereby, providing new perspectives into the mechanism of its anticancer activity.

关键词： imperatorin HIF-1α translation antitumor

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

中国药理学与毒理学杂志 2017年第10期31卷 988-988页

作者： Wei HE Wei-wei CHEN Xian-hua HUANG Yu-mei ZHOU Fang LIAO Department of Pharmacology Gannan Medical UniversityKey Laboratory of Cerebrovascular Pharmacology of Jiangxi Province

OBJECTIVE To investigates the effects of imperatorin on the oxidative stress in the cerebral cortex and hippocampus after focal cerebral ischemia/reperfusion *** Transient focal cerebral ischemia/reperfusion model in male Sprague-Dawley rats was induced by 2 h middle cerebral artery occlusion followed by 24 h ***(1.25 and 2.5 mg·kg-1)or vehicle were administered intraperitoneally at 1,5 and 9 h after the onset of *** 24 h after reperfusion,the biomarkers of oxidative stress such as the levels of reactive oxygen species(ROS),lipid peroxidation products malondialdehyde(MDA),nitric oxide(NO)and total antioxidant capacity(T-AOC),the activities of inducible nitric oxide synthase(iN OS),superoxide dismutase(SOD)and catalase(CAT)in the cerebral cortex and hippocampus were *** also assessed the nuclear factor erythroid 2-related factor 2(Nrf2),heme oxygenase-1(HO-1),and the NAD(P)H-quinone oxidoreductase 1(NQO-1)protein expression by Western *** As compared to vehicle-treated animals,imperatorin treatment significantly reduced the ROS,MDA,NO levels and i NOS activity,increased T-AOC and the activities of SOD and ***,imperatorin treatment also significantly induced the nuclear translocation of Nrf2,enhanced the protein expression of HO-1 and NQO-1 in the cerebral cortex and *** Our findings indicate that imperatorin can protect the brain against the excessive oxidative stress induced by cerebral ischemia/reperfusion through activation of Nrf2 signaling pathway.

关键词： imperatorin cerebral ischemia/reperfusion reactive oxygen species nuclear factor erythroid 2-related factor 2

Expression of intercellular adhesion molecule-1 in U937 foam cells and the inhibitory effect of imperatorin

在线全文

学校读者我要写书评

暂无评论

Expression of intercellular adhesion molecule-1 in U937 foam...