当前位置： SCI文献检索 > TOXICOLOGY AND APPLIED PHARMACOLOGY期刊下所有文献 > RPF101, a new capsaicin-like analogue, disrupts the microtubule network accompanied by arrest in the G2/M phase, inducing apoptosis and mitotic catastrophe in the MCF-7 breast cancer cells.

RPF101, a new capsaicin-like analogue, disrupts the microtubule network accompanied by arrest in the G2/M phase, inducing apoptosis and mitotic catastrophe in the MCF-7 breast cancer cells.

Abstract：

:Breast cancer is the world's leading cause of death among women. This situation imposes an urgent development of more selective and less toxic agents. The use of natural molecular fingerprints as sources for new bioactive chemical entities has proven to be a quite promising and efficient method. Capsaicin, which is the primary pungent compound in red peppers, was reported to selectively inhibit the growth of a variety tumor cell lines. Here, we report for the first time a novel synthetic capsaicin-like analogue, RPF101, which presents a high antitumor activity on MCF-7 cell line, inducing arrest of the cell cycle at the G2/M phase through a disruption of the microtubule network. Furthermore, it causes cellular morphologic changes characteristic of apoptosis and a decrease of Δψm. Molecular modeling studies corroborated the biological findings and suggested that RPF101, besides being a more reactive molecule towards its target, may also present a better pharmacokinetic profile than capsaicin. All these findings support the fact that RPF101 is a promising anticancer agent.

journal_name

Toxicol Appl Pharmacol

journal_title

Toxicology and applied pharmacology

authors

de-Sá-Júnior PL,Pasqualoto KF,Ferreira AK,Tavares MT,Damião MC,de Azevedo RA,Câmara DA,Pereira A,de Souza DM,Parise Filho R

doi

10.1016/j.taap.2012.11.029

subject

Has Abstract

pub_date

2013-02-01 00:00:00

pages

385-98

issue

3

eissn

0041-008X

issn

1096-0333

pii

S0041-008X(12)00518-2

journal_volume

266

pub_type

杂志文章

相关文献

TOXICOLOGY AND APPLIED PHARMACOLOGY文献大全
  • The role of cholinergic and noncholinergic mechanisms in the cardiorespiratory failure produced by N-methylcarbamate cholinesterase inhibitors in rabbits.

    abstract：:We investigated the relative contribution of several cardiorespiratory components to acute lethality produced by N-methylcarbamate cholinesterase (ChE) inhibitors physostigmine, 2-sec-butylphenyl methylcarbamate (BPMC), and 2-isopropoxyphenyl methylcarbamate (PHC) in halothane-anesthetized rabbits. Intravenous injecti...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.2000.8924

    authors： Futagawa H,Kakinuma Y,Takahashi H

    更新日期：2000-05-15 00:00:00

  • Initial analyses of the relationship between "Thresholds" of toxicity for individual chemicals and "Interaction Thresholds" for chemical mixtures.

    abstract：:The inter-relationship of "Thresholds" between chemical mixtures and their respective component single chemicals was studied using three sets of data and two types of analyses. Two in vitro data sets involve cytotoxicity in human keratinocytes from treatment of metals and a metal mixture [Bae, D.S., Gennings, C., Cart...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.taap.2006.11.016

    authors： Yang RS,Dennison JE

    更新日期：2007-09-01 00:00:00

  • Comparative study of genotoxicity and tissue distribution of nano and micron sized iron oxide in rats after acute oral treatment.

    abstract：:Though nanomaterials (NMs) are being utilized worldwide, increasing use of NMs have raised concerns over their safety to human health and environment. Iron oxide (Fe(2)O(3)) NMs have important applications. The aim of this study was to assess the genotoxicity of Fe(2)O(3)-30nm and Fe(2)O(3)-bulk in female Wistar rats....

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2012.10.016

    authors： Singh SP,Rahman MF,Murty US,Mahboob M,Grover P

    更新日期：2013-01-01 00:00:00

  • Benzo[a]pyrene affects Jurkat T cells in the activated state via the antioxidant response element dependent Nrf2 pathway leading to decreased IL-2 secretion and redirecting glutamine metabolism.

    abstract：:There is a clear evidence that environmental pollutants, such as benzo[a]pyrene (B[a]P), can have detrimental effects on the immune system, whereas the underlying mechanisms still remain elusive. Jurkat T cells share many properties with native T lymphocytes and therefore are an appropriate model to analyze the effect...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2013.03.032

    authors： Murugaiyan J,Rockstroh M,Wagner J,Baumann S,Schorsch K,Trump S,Lehmann I,Bergen Mv,Tomm JM

    更新日期：2013-06-15 00:00:00

  • Antioxidant role of glutathione S-transferases: 4-Hydroxynonenal, a key molecule in stress-mediated signaling.

    abstract：:4-Hydroxy-2-trans-nonenal (4HNE), one of the major end products of lipid peroxidation (LPO), has been shown to induce apoptosis in a variety of cell lines. It appears to modulate signaling processes in more than one way because it has been suggested to have a role in signaling for differentiation and proliferation. It...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.taap.2015.10.006

    authors： Singhal SS,Singh SP,Singhal P,Horne D,Singhal J,Awasthi S

    更新日期：2015-12-15 00:00:00

  • Lower susceptibility of female mice to acetaminophen hepatotoxicity: Role of mitochondrial glutathione, oxidant stress and c-jun N-terminal kinase.

    abstract：UNLABELLED:Acetaminophen (APAP) overdose causes severe hepatotoxicity in animals and humans. However, the mechanisms underlying the gender differences in susceptibility to APAP overdose in mice have not been clarified. In our study, APAP (300mg/kg) caused severe liver injury in male mice but 69-77% lower injury in fema...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2014.09.002

    authors： Du K,Williams CD,McGill MR,Jaeschke H

    更新日期：2014-11-15 00:00:00

  • The effect of interferon-α on the expression of cytochrome P450 3A4 in human hepatoma cells.

    abstract：:Interferon α (IFNα) is used to treat malignancies and chronic viral infections. It has been found to decrease the rate of drug metabolism by acting on cytochrome P450 enzymes, but no studies have investigated the consequences of IFNα treatment on the CYP3A4 isoform, responsible for the metabolism of a majority of drug...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2011.03.019

    authors： Flaman AS,Gravel C,Hashem AM,Tocchi M,Li X

    更新日期：2011-06-01 00:00:00

  • Carcinogenicity of formaldehyde and hydrogen chloride in rats.

    abstract：:Previous studies in this laboratory have shown that the combined exposure of hydrogen chloride (HCI) and formaldehyde vapors (HCHO) elicited a significant incidence of nasal cancer in rats. In studies performed elsewhere, it has been demonstrated that exposure to formaldehyde alone induced a high nasal cancer response...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(85)90411-9

    authors： Sellakumar AR,Snyder CA,Solomon JJ,Albert RE

    更新日期：1985-12-01 00:00:00

  • Counteracting tabun inhibition by reactivation by pyridinium aldoximes that interact with active center gorge mutants of acetylcholinesterase.

    abstract：:Tabun represents the phosphoramidate class of organophosphates that are covalent inhibitors of acetylcholinesterase (AChE), an essential enzyme in neurotransmission. Currently used therapy in counteracting excessive cholinergic stimulation consists of a muscarinic antagonist (atropine) and an oxime reactivator of inhi...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2019.04.007

    authors： Kovarik Z,Maček Hrvat N,Kalisiak J,Katalinić M,Sit RK,Zorbaz T,Radić Z,Fokin VV,Sharpless KB,Taylor P

    更新日期：2019-06-01 00:00:00

  • Toxicometabolomics approach to urinary biomarkers for mercuric chloride (HgCl₂)-induced nephrotoxicity using proton nuclear magnetic resonance (¹H NMR) in rats.

    abstract：:The primary objective of this study was to determine and characterize surrogate biomarkers that can predict nephrotoxicity induced by mercuric chloride (HgCl₂) using urinary proton nuclear magnetic resonance (¹H NMR) spectral data. A procedure for (1)H NMR urinalysis using pattern recognition was proposed to evaluate ...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2010.08.017

    authors： Kim KB,Um SY,Chung MW,Jung SC,Oh JS,Kim SH,Na HS,Lee BM,Choi KH

    更新日期：2010-12-01 00:00:00

  • Ascorbic acid chronic alcohol consumption in the guinea pig.

    abstract：:Protection against the toxic effects of chronic alcohol consumption was observed in male guinea pigs maintained on a high-ascorbic-acid diet (vitamin C-deficient chow plus 2.0 mg ascorbic acid/ml drinking water) as compared to animals on a low-ascorbic-acid diet (vitamin C-deficient chow and from 0.025 to 0.050 mg asc...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(86)90141-9

    authors： Susick RL Jr,Abrams GD,Zurawski CA,Zannoni VG

    更新日期：1986-06-30 00:00:00

  • Induction of cytokine mRNAs in mice after oral exposure to the trichothecene vomitoxin (deoxynivalenol): relationship to toxin distribution and protein synthesis inhibition.

    abstract：:The effects of oral exposure to 0, 5, and 25 mg/kg body wt vomitoxin (VT) on cytokine mRNA levels in spleen, Peyer's patches (PP), liver, kidney, and small intestine were evaluated in B6C3F1 mice at 2 and 4 hr postexposure using RT-PCR in conjunction with Southern hybridization analysis. The abundance of mRNAs for sev...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.1995.1132

    authors： Azcona-Olivera JI,Ouyang Y,Murtha J,Chu FS,Pestka JJ

    更新日期：1995-07-01 00:00:00

  • Increased neutrophil adherence to endothelial cells exposed to asbestos.

    abstract：:Inhalation of asbestos may activate the pulmonary endothelium to promote an inflammatory cell phenotype that participates in the development of pulmonary fibrosis. However, little is known about the effects of asbestos on endothelial cell function. Therefore, endothelial cells were exposed to chrysotile and crocidolit...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.1996.0143

    authors： Treadwell MD,Mossman BT,Barchowsky A

    更新日期：1996-07-01 00:00:00

  • Mechanism of apoptosis induced by a polysaccharide, from the loach Misgurnus anguillicaudatus (MAP) in human hepatocellular carcinoma cells.

    abstract：:The biological activities of the polysaccharide have attracted more and more attention in the biochemical and medical areas due to their anti-cancer effects. To estimate the anti-tumor mechanism of MAP, a novel polysaccharide from the loach, Misgurnus anguillicaudatus, the apoptosis effects of the polysaccharide on th...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2005.04.019

    authors： Zhang CX,Huang KX

    更新日期：2006-02-01 00:00:00

  • Goniothalamin prevents the development of chemically induced and spontaneous colitis in rodents and induces apoptosis in the HT-29 human colon tumor cell line.

    abstract：:Colon cancer is the third most incident type of cancer worldwide. One of the most important risk factors for colon cancer development are inflammatory bowel diseases (IBD), thus therapies focusing on IBD treatment have great potential to be used in cancer prevention. Nature has been a source of new therapeutic and pre...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2016.03.009

    authors： Vendramini-Costa DB,Alcaide A,Pelizzaro-Rocha KJ,Talero E,Ávila-Román J,Garcia-Mauriño S,Pilli RA,de Carvalho JE,Motilva V

    更新日期：2016-06-01 00:00:00

  • Effects of methylmercuric chloride, cycloheximide, and colchicine on the reaggregation of dissociated mouse cerebellar cells.

    abstract：:High fetal and neonatal brain levels of methyl mercury (MeHg) have been associated with the abnormal migration of neurons within the cerebellar and cerebral cortices. How MeHg interferes with cellular proliferation, migration, and differentiation is poorly understood. In this study, a cell recognition/cohesion assay b...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(86)90363-7

    authors： Jacobs AJ,Maniscalco WM,Finkelstein JN

    更新日期：1986-12-01 00:00:00

  • Constitutive expression of metallothionein genes in mouse brain.

    abstract：:Metallothioneins (MTs) are ubiquitous low-molecular-weight proteins that are induced by a variety of inducers, including metals, lipopolysaccharides (LPS), cytokines, oxidative stress, etc., and are thought to play a protective role against various toxic insults. The constitutive level of metallothionein is an importa...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.1995.1056

    authors： Choudhuri S,Kramer KK,Berman NE,Dalton TP,Andrews GK,Klaassen CD

    更新日期：1995-03-01 00:00:00

  • Enhanced hepatic expression of P450IIE1 following inhalation exposure to pyridine.

    abstract：:Previous research has shown that intraperitoneal injection of the solvent pyridine results in a dose- and time-dependent induction of hepatic P450IIE1 in rats, with a twofold increase observed at 6 hr post-treatment. However, inhalation is the primary route of exposure expected for humans exposed to pyridine in labora...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.1993.1014

    authors： Hotchkiss JA,Kim SG,Novak RF,Dahl AR

    更新日期：1993-01-01 00:00:00

  • Synergistic interaction of ozone and respirable aerosols on rat lungs. II. Synergy between ammonium sulfate aerosol and various concentrations of ozone.

    abstract：:Pulmonary responses after continuous exposure of rats to concentrations of ozone (O3) ranging from 0.12 to 0.64 ppm were quantified by measuring tissue collagen synthesis rate, tissue protein and DNA content, and various constituents of bronchoalveolar lavage fluid. After 7 days of exposure to 0.64 ppm of O3, lung col...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(86)90252-8

    authors： Warren DL,Guth DJ,Last JA

    更新日期：1986-07-01 00:00:00

  • Effects of lead on the secretion and disappearance of renin in rabbits.

    abstract：:The disappearance rate of renin from plasma was evaluated in both acutely and chronically lead-exposed rabbits. In addition, the effects of lead (Pb) on in vitro renin secretion were determined with rabbit renal cortical slices. Rabbits acutely exposed to Pb (0.3 to 2.0 mg/kg, iv) demonstrated no increase in plasma re...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(83)90127-8

    authors： Keiser JA,Vander AJ,Germain CL

    更新日期：1983-06-15 00:00:00

  • Comparative effects of phenobarbital, DDT, and lindane on mouse hepatocyte gap junctional intercellular communication.

    abstract：:Gap junctional intercellular communication appears to be important in the regulation of cellular homeostasis, differentiated cell functions, and growth control in adult tissues. Interruption of intercellular communication by chemical compounds has been shown to be a sublethal response to a number of tumor promoters. T...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(90)90050-5

    authors： Klaunig JE,Ruch RJ,Weghorst CM

    更新日期：1990-03-01 00:00:00

  • Toxicity and toxicokinetics of metformin in rats.

    abstract：:Metformin is a first-line drug for the treatment of type 2 diabetes (T2D) and is often prescribed in combination with other drugs to control a patient's blood glucose level and achieve their HbA1c goal. New treatment options for T2D will likely include fixed dose combinations with metformin, which may require preclini...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2009.11.026

    authors： Quaile MP,Melich DH,Jordan HL,Nold JB,Chism JP,Polli JW,Smith GA,Rhodes MC

    更新日期：2010-03-15 00:00:00

  • Effect of chlorpromazine on cyanide intoxication.

    abstract：:Previous reports from our laboratory indicated that prophylactic protection against cyanide intoxication in mice can be enhanced by administration of chlorpromazine when it is given with sodium thiosulfate. The mechanism of potentiation of sodium thiosulfate by chlorpromazine was studied alone and in combination with ...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(83)90028-5

    authors： Kong A,Shen A,Burrows G,Sylvester D,Isom GE,Way JL

    更新日期：1983-12-01 00:00:00

  • Cardiac hypertrophy in aryl hydrocarbon receptor null mice is correlated with elevated angiotensin II, endothelin-1, and mean arterial blood pressure.

    abstract：:The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that mediates toxicity of xenobiotics, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin. Genetic deletion of the AhR leads to cardiac hypertrophy, suggesting a role for the AhR in cardiovascular physiology and disease; however, the pathways invo...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2003.08.008

    authors： Lund AK,Goens MB,Kanagy NL,Walker MK

    更新日期：2003-12-01 00:00:00

  • Toluene exposure increases aminophylline-induced seizure susceptibility in mice.

    abstract：:The effects of toluene on the sensitivity to seizures induced by aminophylline were investigated. Mice were pretreated with an ip injection of corn oil or toluene (100-500 mg/kg) followed by a timed intravenous infusion of aminophylline at various time intervals to assess the seizure thresholds and lethal doses. Tolue...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2003.08.002

    authors： Chan MH,Chen HH

    更新日期：2003-12-01 00:00:00

  • Autophagy blockade sensitizes the anticancer activity of CA-4 via JNK-Bcl-2 pathway.

    abstract：:Combretastatin A-4 (CA-4) has already entered clinical trials of solid tumors over ten years. However, the limited anticancer activity and dose-dependent toxicity restrict its clinical application. Here, we offered convincing evidence that CA-4 induced autophagy in various cancer cells, which was demonstrated by acrid...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2013.11.018

    authors： Li Y,Luo P,Wang J,Dai J,Yang X,Wu H,Yang B,He Q

    更新日期：2014-01-15 00:00:00

  • Ultrafine carbon particles promote rotenone-induced dopamine neuronal loss through activating microglial NADPH oxidase.

    abstract：BACKGROUND:Atmospheric ultrafine particles (UFPs) and pesticide rotenone were considered as potential environmental risk factors for Parkinson's disease (PD). However, whether and how UFPs alone and in combination with rotenone affect the pathogenesis of PD remains largely unknown. METHODS:Ultrafine carbon black (ufCB...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2017.03.005

    authors： Wang Y,Liu D,Zhang H,Wang Y,Wei L,Liu Y,Liao J,Gao HM,Zhou H

    更新日期：2017-05-01 00:00:00

  • Phorate-induced oxidative stress, DNA damage and transcriptional activation of p53 and caspase genes in male Wistar rats.

    abstract：:Male Wistar rats exposed to a systemic organophosphorus insecticide, phorate [O,O-diethyl S-[(ethylthio) methyl] phosphorothioate] at varying oral doses of 0.046, 0.092 or 0.184mg phorate/kg bw for 14days, exhibited substantial oxidative stress, cellular DNA damage and activation of apoptosis-related p53, caspase 3 an...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.taap.2011.12.006

    authors： Saquib Q,Attia SM,Siddiqui MA,Aboul-Soud MA,Al-Khedhairy AA,Giesy JP,Musarrat J

    更新日期：2012-02-15 00:00:00

  • Reaction between metabolically activated acetaminophen and phosphorothioate oligonucleotides.

    abstract：:Assessment of toxic or mutagenic risks associated with phosphorothioate oligonucleotides (PTO) is important. In vitro and in vivo data have shown that PTOs are nontoxic and nonmutagenic. However, these studies do not address interactions between PTOs and other compounds. The sulfur on PTOs may provide a novel reactive...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1006/taap.1995.1126

    authors： Copple BL,Gmeiner WM,Iversen PL

    更新日期：1995-07-01 00:00:00

  • Abnormal neurulation induced by 7-hydroxy-2-acetylaminofluorene and acetaminophen: evidence for catechol metabolites as proximate dysmorphogens.

    abstract：:Direct additions to culture media of either acetaminophen (APAP) or 7-hydroxy-2-acetylaminofluorene (7-OH-AAF) resulted in abnormal closure of the anterior neuropores of cultured rat embryos in the absence of an exogenous bioactivation system. Concentrations required to produce a 50% incidence of the defect were appro...

    journal_title：Toxicology and applied pharmacology

    pub_type： 杂志文章

    doi：10.1016/0041-008x(89)90192-0

    authors： Harris C,Stark KL,Luchtel DL,Juchau MR

    更新日期：1989-12-01 00:00:00