Abstract:
AIM:The interaction of anthracycline anticancer drugs with chromatin, nucleosomes and histone H1 has been extensively studied. In the present study, for the first time, we have investigated the binding of anthracycline antibiotic, daunomycin, to free and cross-linked thymus core histones (CL-core) in solution and in the absence of DNA. METHODS:Fluorescence, UV/Vis spectroscopy and equilibrium dialysis techniques were used. RESULTS:The UV spectroscopy results show that daunomycin induces hypochromicity in the absorption spectra of the core histones. Fluorescence emission intensity is decreased upon daunomycin binding and the process is concentration dependent. The equilibrium dialysis shows that the binding is positive cooperative with the binding sites as Scatchard plot and Hill Coefficient confirm it. CONCLUSION:The results suggest that daunomycin shows much higher affinity to core histones free in solution than to CL-core, implying that the binding is most likely due to the accessibility of these proteins to the environment. It is suggested that daunomycin binds strongly to open state of histones, such as in tumor cells, rather than to their compact structure seen in normal chromatin.
journal_name
Acta Pharmacol Sinjournal_title
Acta pharmacologica Sinicaauthors
Rabbani A,Abdosamadi S,Sari-Saraf Ndoi
10.1111/j.1745-7254.2007.00542.xsubject
Has Abstractpub_date
2007-05-01 00:00:00pages
731-7issue
5eissn
1671-4083issn
1745-7254journal_volume
28pub_type
杂志文章abstract:AIM:To study the changes of phospholipase D (PLD) activity of actively sensitized rat peritoneal mast cells (RPMC) in degranulation. METHODS:Degranulation of RPMC was determined by measurement of beta-hexosaminidase release. PLD activity assay was carried out by measurement of PLD product, choline, with chemiluminesce...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2004-01-01 00:00:00
abstract:AIM:Recent evidence shows that cultured mycelium Cordyceps sinensis (CMCS) effectively protects against liver fibrosis in mice. Here, we investigated whether the anti-fibrotic action of CMCS was related to its regulation of the activity of hepatic natural killer (NK) cells in CCl4-treated mice. METHODS:C57BL/6 mice we...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2015.129
更新日期:2016-02-01 00:00:00
abstract:AIM:To investigate the effect of melittin (Mel) on papillary muscles of guinea pigs. METHODS:Contraction of papillary muscles were examined by conventional method and action potentials (AP) were recorded by standard glass microelectrode technique. RESULTS:Mel (0.5, 3 micromol/L) significantly increased the contractil...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2001-08-01 00:00:00
abstract::Human ether-a-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, r...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章,评审
doi:10.1038/aps.2011.70
更新日期:2011-06-01 00:00:00
abstract:AIM:To study and establish a proteome reference map and regulation network of neonatal rat cardiomyocyte. METHODS:Cultured cardiomyocytes of neonatal rats were used. All proteins expressed in the cardiomyocytes were separated and identified by two-dimensional polyacrylamide gel electrophoresis (2-DE) and matrix-assist...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2011.86
更新日期:2011-09-01 00:00:00
abstract::Binding of a neurotransmitter to its ionotropic receptor opens a distantly located ion channel, a process termed allosteric activation. Here we review recent advances in the molecular mechanism by which the cys-loop receptors are activated with emphasis on the best studied nicotinic acetylcholine receptors (nAChRs). W...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章,评审
doi:10.1038/aps.2009.51
更新日期:2009-06-01 00:00:00
abstract:AIM:To develop and validate a novel precolumn derivatization method for the quantitative determination and pharmacokinetic application of acetylshikonin in macaque monkeys by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). METHODS:2-Mercaptoethanol was added to the blood sample a...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2008.00898.x
更新日期:2008-12-01 00:00:00
abstract:AIM:To ascertain the effects of erlotinib on CYP3A, to investigate the amplitude and kinetics of erlotinib-mediated inhibition of seven major CYP isoforms in human liver microsomes (HLMs) for evaluating the magnitude of erlotinib in drug-drug interaction in vivo. METHODS:The activities of 7 major CYP isoforms (CYP1A2,...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2010.218
更新日期:2011-03-01 00:00:00
abstract:AIM:To investigate the anti-neuroinflammatory activity of a novel synthetic compound, 7-methylchroman-2-carboxylic acid N-(2-trifluoromethyl) phenylamide (MCAP) against LPS-induced microglial activation in vitro. METHODS:Primary mouse microglia and BV2 microglia cells were exposed to LPS (50 or 100 ng/mL). The express...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2015.138
更新日期:2016-03-01 00:00:00
abstract::Recent evidence shows that raddeanin A (RA), an oleanane-type triterpenoid saponin extracted from Anemone raddeana Regel, exerts remarkable cytotoxicity against cancer cells in vitro and in vivo. In addition, RA has also been found to activate autophagy in human gastric cancer cells. In this study, we investigated the...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2017.139
更新日期:2018-04-01 00:00:00
abstract:AIM:To investigate the molecular mechanism and signaling pathway by which fenoterol, a beta(2)-adrenergic receptor (beta(2)-AR) agonist, produces anti-inflammatory effects. METHODS:THP-1, a monocytic cell line, was used to explore the mechanism of beta(2)-AR stimulation in LPS-induced secretion of inflammatory cytokin...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2009.153
更新日期:2009-11-01 00:00:00
abstract::Hepatic fibrosis is a disease characterized by excessive deposition of extracellular matrix (ECM) in the liver. Activation of hepatic stellate cells (HSCs) is responsible for most of ECM production. Oxidative stress and reactive oxygen species (ROS) may be important factors leading to liver fibrosis. NADPH oxidase 4 (...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/s41401-020-00545-9
更新日期:2020-10-28 00:00:00
abstract::Aberrant activity of enhancer of zeste homolog 2 (EZH2) is associated with a wide range of human cancers. The interaction of EZH2 with embryonic ectoderm development (EED) is required for EZH2's catalytic activity. Inhibition of the EZH2-EED complex thus represents a novel strategy for interfering with the oncogenic p...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2017.59
更新日期:2018-02-01 00:00:00
abstract::The signal transducer and activator of transcription 3 (STAT3) plays a critical role in platelet functions. This study sought to understand the effects of the STAT3 inhibitor SC99 on platelet activation and aggregation. Immunoblotting assays were applied to measure the effects of SC99 on the STAT3 signaling pathway. A...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2016.155
更新日期:2017-05-01 00:00:00
abstract:AIM:The role of caveolin-1 (Cav-1) in angiogenesis remains poorly understood. The endothelial nitric oxide (NO) synthase (eNOS), a caveolin-interacting protein, was demonstrated to play a predominant role in vascular endothelial growth factor (VEGF) -induced angiogenesis. The purpose of our study was to examine the rol...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2006.00462.x
更新日期:2006-12-01 00:00:00
abstract:AIM:Benzothiophene compounds are selective estrogen receptor modulators (SERMs), which are recently found to activate antioxidant signaling. In this study the molecular mechanisms of antioxidant signaling activation by benzothiophene compound BC-1 were investigated. METHODS:HepG2 cells were stably transfected with ant...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2012.168
更新日期:2013-03-01 00:00:00
abstract:AIM:Apolipoprotein E (ApoE) plays an important role in the transport and metabolism of lipids. Recent studies show that bone mass is increased in young apoE(-/-) mice. In this study we investigated the bone phenotype and metabolism in aged apoE(-/-) mice. METHODS:Femurs and tibias were collected from 18- and 72-week-o...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2015.95
更新日期:2015-12-01 00:00:00
abstract:AIM:To develop a high-throughput real-time assay based on molecular beacons to monitor the integrase 3'-processing reaction in vitro and apply it to inhibitor screening. METHODS:The recombinant human immunodeficiency virus (HIV)-1 integrase (IN) is incubated with a 38 mer oligonucleotide substrate, a sequence identica...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2007.00561.x
更新日期:2007-06-01 00:00:00
abstract:AIM:To investigate the effect of aluminum (Al) on high voltage-dependent calcium current (I(HVA)) and its modulation by ginkgolide B (Gin B). METHODS:The whole-cell, patch-clamp technique was used to record IHVA from acutely isolated hippocampal CA1 pyramydal neurons in rats. RESULTS:Al 0.1 mmol/L (low concentration)...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2005.00073.x
更新日期:2005-05-01 00:00:00
abstract:AIM:To observe the polymorphism of angiotensin-converting enzyme (ACE) gene in Northern Hans, Dahurs, and Ewenkis of China. METHODS:The polymerase chain reaction was used to type the insertion/deletion polymorphism at intron 16 of ACE gene among 90 Northern Hans, 84 Dahurs, and 64 Ewenkis individuals. The experiment d...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2001-08-01 00:00:00
abstract:AIM:To investigate whether or not brain histamine was involved in memory deficits induced by lesions of nucleus basalis magnocellularis (NBM) in rats. METHODS:Passive avoidance response was used to measure memory process in rats, and NBM was bilaterally lesioned by injection of ibotenic acid (6 microg/site). RESULTS:...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2002-01-01 00:00:00
abstract:AIM:To study the effects of cimetidine (Cim) on the production of interferon gamma (IFN gamma) and tumor necrosis factor alpha (TNF alpha) by splenocytes in immune-derived aplastic anemic (AA) mice. METHODS:Aplastic anemic mice model was constructed first, and then the splenocytes were induced to secrete IFN gamma and...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2001-03-01 00:00:00
abstract:AIM:alpha2 nAChR subunit mRNA expression in mice is most intense in the olfactory bulbs and interpeduncular nucleus. We aimed to investigate the properties of alpha2* nAChRs in these mouse brain regions. METHODS:alpha2 nAChR subunit-null mutant mice were engineered. Pharmacological and immunoprecipitation studies were...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2009.68
更新日期:2009-06-01 00:00:00
abstract:AIM:To investigate the ultrastructural localization of atrial natriuretic peptide (ANP)-synthesizing cells and the relationship between ANP-synthesizing cells and microvessels in rat gastric mucosa. METHODS:Immunohistochemistry techniques and postembedding immunoelectron microscopy techniques were used to validate the...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2006.00226.x
更新日期:2006-02-01 00:00:00
abstract::Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were ana...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2017.199
更新日期:2018-06-01 00:00:00
abstract:AIM:To explore the possible association of different polymorphic forms of human alpha-estrogen receptor (ER-alpha) and aryl hydrocarbon receptor gene (Ahr) with the risk to senile dementia in farmers in Shanghai suburb. METHODS:Senile dementia patients (n=52) were examined for ER-alpha and Ahr gene polymorphism genoty...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2003-07-01 00:00:00
abstract:AIM:To investigate whether low dose theophylline has an anti-inflammatory effect in asthma. METHODS:Nineteen asthmatic subjects were given 200 mg sustained-release theophylline preparation twice daily for 4 weeks. The mean serum concentration of theophylline was 7.9 mg/L. The percentage of eosinophils, EG2+ eosinophil...
journal_title:Acta pharmacologica Sinica
pub_type: 临床试验,杂志文章
doi:
更新日期:2001-05-01 00:00:00
abstract::Sepsis-induced multiple organ dysfunction and inflammatory response are life-threatening symptoms without effective treatment. Fisetin, a dietary flavonoid extracted from berries and family Fabaceae, has displayed neuroprotective and anti-oxidant activities. In this study we investigated whether fisetin exerted a prot...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/s41401-020-0462-y
更新日期:2020-10-01 00:00:00
abstract::Over half of patients with BRCA1-deficient cancers do not respond to treatment with poly(ADP-ribose) polymerase (PARP) inhibitors. In this study, we report that a combination of 53BP1 and BRCA1 may serve as a biomarker of PARP inhibitor sensitivity. Based on the mRNA levels of four homologous recombination repair (HR)...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2017.8
更新日期:2017-07-01 00:00:00
abstract:AIM:The current therapeutic approaches have a limited effect on the dysregulated pulmonary vascular remodeling, which is characteristic of pulmonary arterial hypertension (PAH). In this study we examined whether salvianolic acid A (SAA) extracted from the traditional Chinese medicine 'Dan Shen' attenuated vascular remo...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2016.22
更新日期:2016-06-01 00:00:00