Rational redesign of inhibitors of furin/kexin processing proteases by electrostatic mutations.

abstract：AIM:To study in vitro release and in vivo effect of four different types of sustained-release naltrexone microspheres on morphine analgesia. METHODS:Release of naltrexone from four types of biodegradable microspheres was investigated by HPLC. Their antagonist effects on morphine analgesia were observed using mouse hot...

journal_title：Acta pharmacologica Sinica

authors： He GA,Hou HM,Liu XJ

更新日期：2001-06-01 00:00:00

abstract：AIM:To investigate the anticancer mechanism of a methoxyflavanone derivative, WJ9708012, highlighting its role on a crosstalk between endoplasmic reticulum (ER) and mitochondrial stress. METHODS:Cell proliferation was examined using sulforhodamine B assay. Cell-cycle progression, Ca(2+) mobilization and mitochondrial ...

journal_title：Acta pharmacologica Sinica

authors： Kuo TC,Huang WJ,Guh JH

更新日期：2011-01-01 00:00:00

abstract：AIM:HMGB1 (high-mobility group box-1) is a nuclear protein containing a consensus RB (retinoblastoma)-binding LXCXE motif. In this study, we studied the potential association of HMGB1 and RB and the in vitro and in vivo activities of HMGB1 in human breast cancer cells. METHODS:The protein-protein interaction was deter...

journal_title：Acta pharmacologica Sinica

authors： Jiao Y,Wang HC,Fan SJ

更新日期：2007-12-01 00:00:00

abstract：AIM:Ischemia/reperfusion is an initial triggering event that leads to gut-induced acute lung injury (ALI). In this study, we investigated whether hypoxia inducible factor-1α (HIF-1α) played a role in the pathogenesis of lung injury induced by trauma and hemorrhagic shock (T/HS). METHODS:Male Wistar rats underwent lapa...

journal_title：Acta pharmacologica Sinica

authors： Jiang H,Huang Y,Xu H,Hu R,Li QF

更新日期：2012-05-01 00:00:00

abstract：AIM:To investigate the antidepressant-like effects of a novel 5-HT3 receptor antagonist N-(benzo[d]thiazol-2-yl)-3-methoxyquinoxalin-2-carboxamide (6z) in acute and chronic murine models of depression. METHODS:5-HT3 receptor antagonism was examined in guinea pig ileum in vitro. A tail suspension test (TST) was used as...

journal_title：Acta pharmacologica Sinica

authors： Gupta D,Radhakrishnan M,Kurhe Y,Thangaraj D,Prabhakar V,Kanade P

更新日期：2014-12-01 00:00:00

abstract：AIM:To investigate whether autologous transplantation of adult stem cells could improve post-infarcted heart function. METHODS:Bone marrow mononuclear cells (MNCs) were isolated from adult rabbits' tibias after coronary ligation. These cells were exposed to 5-azacytidine 10 micromol/L for 24 h on the third day of cult...

journal_title：Acta pharmacologica Sinica

authors： Lin GS,Lü JJ,Jiang XJ,Li XY,Li GS

更新日期：2004-07-01 00:00:00

abstract：:Embryonic stem (ES) cells and their differentiated progeny offer tremendous potential for regenerative medicine, even in the field of drug discovery. There is an urgent need for clinically relevant assays that make use of ES cells because of their rich biological utility. Attention has been focused on small molecules ...

journal_title：Acta pharmacologica Sinica

authors： Lou YJ,Liang XG

更新日期：2011-02-01 00:00:00

abstract：AIM:To investigate whether sodium ferulate (SF) can protect cortical neurons from glutamate-induced neurotoxicity and the mechanisms responsible for this protection. METHODS:Cultured cortical neurons were incubated with 50 micromol/L glutamate for either 30 min or 24 h, with or without pre-incubation with SF (100, 200...

journal_title：Acta pharmacologica Sinica

authors： Jin Y,Yan EZ,Fan Y,Guo XL,Zhao YJ,Zong ZH,Liu Z

更新日期：2007-12-01 00:00:00

abstract：AIM:Targeting the VEGF/VEGF receptor (VEGFR) pathway has proved to be an effective antiangiogenic approach for cancer treatment. Here, we identified 6-((2-((3-acetamidophenyl)amino)pyrimidin-4-yl)oxy)-N-phenyl-1-naphthamide (designated herein as DW10075) as a novel and highly selective inhibitor of VEGFRs. METHODS:In ...

journal_title：Acta pharmacologica Sinica

authors： Li MY,Lv YC,Tong LJ,Peng T,Qu R,Zhang T,Sun YM,Chen Y,Wei LX,Geng MY,Duan WH,Xie H,Ding J

更新日期：2016-03-01 00:00:00

abstract：AIM:KCNQ1 and KCNE1 form a complex in human ventricular cardiomyocytes, which are important in maintaining a normal heart rhythm. In the present study we investigated the effects of a homologous series of 1-alkanols on KCNQ1/KCNE1 channels expressed in Xenopus oocytes. METHODS:ECG recording was made in rats injected w...

journal_title：Acta pharmacologica Sinica

authors： Xie C,Liu HW,Pan N,Ding JP,Yao J

更新日期：2016-01-01 00:00:00

abstract：AIM:To investigate the pharmacokinetic profile and tissue distribution of a novel phosphodiesterase type 5 inhibitor, 5-ethyl-2-{5-[4-(2-hydroxy-ethyl)-piperazine-1-sulfonyl]-2-propoxy-phenyl}-7-propyl-3,5-dihydro-pyrrolo(3,2-d)pyrimidin-4-one (SK-3530), in rats after administration of the (14)C-labeled compound. METH...

journal_title：Acta pharmacologica Sinica

authors： Yoo HH,Kim NS,Im GJ,Kim DH

更新日期：2007-08-01 00:00:00

abstract：:Antimony, a natural element that has been used as a drug for over more than 100 years, has remarkable therapeutic efficacy in patients with acute promyelocytic leukemia. This review focuses on recent advances in developing antimony anticancer agents with an emphasis on antimony coordination complexes, Sb (III) and Sb ...

journal_title：Acta pharmacologica Sinica

authors： Sharma P,Perez D,Cabrera A,Rosas N,Arias JL

更新日期：2008-08-01 00:00:00

abstract：AIM:To test the ability of huperzine B (HupB) to alleviate injury from oxygen-glucose deprivation (OGD) in the rat pheochromocytoma line PC12 cells. METHODS:After OGD for 3 h and reoxygenation for 24 h, neuronal morphology was observed by phase-contrast microscopy; cell survival was quantified by the reduction of MTT;...

journal_title：Acta pharmacologica Sinica

authors： Wang ZF,Zhou J,Tang XC

更新日期：2002-12-01 00:00:00

abstract：AIM:Based on the structural analysis to reveal the mechanism of ligand binding to beta-secretase and the specificity of each binding sub-site. METHODS:Molecular dynamics was used to simulate on the ligand free beta-secretase and ligand bound beta-secretase. The trajectories were analyzed using the essential dynamics, ...

journal_title：Acta pharmacologica Sinica

authors： Xiong B,Huang XQ,Shen LL,Shen JH,Luo XM,Shen X,Jiang HL,Chen KX

更新日期：2004-06-01 00:00:00

abstract：AIM:To determine the role of dietary low histamine on the seizure development of pentylenetetrazol (PTZ)-induced kindling in rats. METHODS:After 14 d of feeding on a low histamine diet (LH, containing 0.145 mumol/g of histamine), the rats were chemically kindled by repeated intraperitoneal injection of a subconvulsant...

journal_title：Acta pharmacologica Sinica

authors： Jin CL,Sakurai E,Kiso Y,Luo JH,Yanai K,Chen Z

更新日期：2005-04-01 00:00:00

abstract：AIM:To study the changes and mechanisms of protein-tyrosine kinase (PTK) and protein-tyrosine phosphatase (PTP) activities in the hippocamal synaptosome following cerebral ischemia/reperfusion (I/R) in gerbil. METHODS:Transient (15 min) global ischemia was produced by bilateral carotid artery occlusion. Total PTK and ...

journal_title：Acta pharmacologica Sinica

authors： Pei L,Li Y,Yan JZ,Zhang GY,Cui ZC,Zhu ZM

更新日期：2000-08-01 00:00:00

abstract：AIM:To explore the anticancer effects and the molecular mechanisms of gambogic acid (GA) on Jurkat cells. METHODS:Cell viability was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Annexin V-fluorescein-isothiocyanate/propidium iodide, DNA defragmentation, and comet assay were used to d...

journal_title：Acta pharmacologica Sinica

authors： Wang Y,Chen Y,Chen Z,Wu Q,Ke WJ,Wu QL

更新日期：2008-03-01 00:00:00

abstract：AIM:To examine the protective effect of propofol in renal ischemia/reperfusion (I/R) injury and the role of heme oxygenase-1 (HO-1) in this process. METHODS:Sprague-Dawley rats were randomly divided into 3 groups: (i) sham-operated group; (ii) I/R group; and (iii) propofol group. Bilateral renal warm ischemia for 45 m...

journal_title：Acta pharmacologica Sinica

authors： Wang HH,Zhou HY,Chen CC,Zhang XL,Cheng G

更新日期：2007-08-01 00:00:00

abstract：AIM:To investigate the influences of betulinic acid (BA), a triterpenoid isolated from birch bark, on neuroinflammatory mediators involved in the pathogenesis of multiple sclerosis and experimental autoimmune encephalomyelitis in vitro. METHODS:Encephalitogenic T cells were prepared from draining lymph nodes and spina...

journal_title：Acta pharmacologica Sinica

authors： Blaževski J,Petković F,Momčilović M,Paschke R,Kaluđerović GN,Mostarica Stojković M,Miljković D

更新日期：2013-03-01 00:00:00

abstract：AIM:Toxicity of retinol (vitamin A) has been previously associated with apoptosis and/or cell malignant transformation. Thus, we investigated the pathways involved in the induction of proliferation, deformation and proliferative focus formation by retinol in cultured Sertoli cells of rats. METHODS:Sertoli cells were i...

journal_title：Acta pharmacologica Sinica

authors： Gelain DP,Pasquali MA,Caregnato FF,Castro MA,Moreira JC

更新日期：2012-04-01 00:00:00

abstract：:The serum and glucocorticoid-regulated kinase (SGK) family has been implicated in the regulation of many cellular processes downstream of the PI3K pathway. It plays a crucial role in PI3K-mediated tumorigenesis, making it a potential therapeutic target for cancer. SGK family consists of three isoforms (SGK1, SGK2, and...

journal_title：Acta pharmacologica Sinica

authors： Gong GQ,Wang K,Dai XC,Zhou Y,Basnet R,Chen Y,Yang DH,Lee WJ,Buchanan CM,Flanagan JU,Shepherd PR,Chen Y,Wang MW

更新日期：2018-12-01 00:00:00

abstract：:AIDS is presently treatable, and patients can have a good prognosis due to the success of highly active antiretroviral therapy (HAART), but it is still not curable or preventable. High toxicity of HAART, and the emergence of drug resistance add to the imperative to continue research into new strategies and interventio...

journal_title：Acta pharmacologica Sinica

authors： Krambovitis E,Porichis F,Spandidos DA

更新日期：2005-10-01 00:00:00

abstract：:Wound healing impairment represents a particularly challenging clinical problem to which no efficacious treatment regimens currently exist. The factors ensuring appropriate intercellular communication during wound repair are not completely understood. Although protein-type mediators are well-established players in thi...

journal_title：Acta pharmacologica Sinica

authors： Luo JD,Chen AF

更新日期：2005-03-01 00:00:00

abstract：:Autophagy is a cell self-digestion process via lysosomes that clears "cellular waste", including aberrantly modified proteins or protein aggregates and damaged organelles. Therefore, autophagy is considered a protein and organelle quality control mechanism that maintains normal cellular homeostasis. Dysfunctional auto...

journal_title：Acta pharmacologica Sinica

authors： He LQ,Lu JH,Yue ZY

更新日期：2013-05-01 00:00:00

abstract：AIM:To investigate the effects of deferiprone on doxorubicin-induced cardiotoxicity and determine its protection on cardiac contractility in vivo at tissue level. METHODS:Spontaneously-beating isolated atria from rats were pretreated with deferiprone for 10 min at 1.2 mmol/L or 0.3 mmol/L, respectively before co-incub...

journal_title：Acta pharmacologica Sinica

authors： Xu LJ,Jin L,Pan H,Zhang AZ,Wei G,Li PP,Lu WY

更新日期：2006-10-01 00:00:00

abstract：AIM:To differentiate the electrophysiological characteristics of somatic action potentials (AP) from isolated Neo and Juv nodose sensory neurons (NSN) and those from slices of intact Juv and adult rat nodose ganglia. METHODS:For isolated cell recordings nodose ganglia from 3-8 d old Neo and 4 weeks old Juv rats were d...

journal_title：Acta pharmacologica Sinica

authors： Li BY,Schild JH

更新日期：2002-06-01 00:00:00

abstract：AIM:The responses of the intracellular calcium ([Ca2+]i) and the intracellular pH (pHi) to kappa-opioid receptor stimulation were determined in the single right ventricular myocytes isolated from the hearts of chronically hypoxic rats which exhibited right ventricular hypertrophy (RVH). METHODS:With the spectrofluorom...

journal_title：Acta pharmacologica Sinica

authors： Pei JM,Wang YM,Zhu YL,Chen M,Wong TM

更新日期：2001-10-01 00:00:00

abstract：AIM:To study the effects of nimodipine on delayed cerebral injury in mice from subacute carbon monoxide (CO) exposure. METHODS:Mice were exposed to CO (100 mL/kg, ip) once a day, continuously for 7 d. After 7-d CO-exposure, mortality in mice, changes in learning ability and memory using passive avoidance test, the pat...

journal_title：Acta pharmacologica Sinica

authors： Yang JQ,Zhou QX

更新日期：2001-05-01 00:00:00

abstract：AIM:To investigate the protective effects of hydrogen sulfide (H2S) against inflammation, oxidative stress and apoptosis in a rat model of resuscitated hemorrhagic shock. METHODS:Hemorrhagic shock was induced in adult male SD rats by drawing blood from the femoral artery for 10 min. The mean arterial pressure was main...

journal_title：Acta pharmacologica Sinica

authors： Xu DQ,Gao C,Niu W,Li Y,Wang YX,Gao CJ,Ding Q,Yao LN,Chai W,Li ZC

更新日期：2013-12-01 00:00:00

abstract：:Type capital I, Ukrainian natural killer T cells (NKT cells), a subset of CD1d-restricted T cells with invariant Valphabeta TCR, are characterized by prompt production of large amounts of Th1 and/or Th2 cytokines upon primary stimulation through the TCR complex. The rapid release of cytokines implies that type capital...

journal_title：Acta pharmacologica Sinica

authors： Tan JQ,Xiao W,Wang L,He YL

更新日期：2010-09-01 00:00:00