Abstract:
:Epidermal growth factor receptor (EGFR) is considered as a valid target in the clinical trials of anticancer therapy and tyrosine kinase inhibitors (TKIs) of EGFR are approved for cancer treatments. In present work, cucurbitacin IIb (CuIIb) was confirmed to exhibit the proliferation inhibitory activity in A549 cells. CuIIb induced apoptosis via STAT3 pathway, which was mitochondria-mediated and caspase-dependent. CuIIb also suppressed the cell cycle and induced G2/M phase cell cycle arrest. CuIIb was capable of suppressing the signal transmitting of the EGFR/mitogen-activated protein kinase (MAPK) pathway which was responsible for the apoptosis and cell cycle arrest. Homogeneous time-resolved fluorescence (HTRF) analysis demonstrated that the kinase activity of EGFR was inhibited by CuIIb. Molecular docking suggested that the CuIIb-EGFR binding fundamentally depends on the contribution of both hydrophobic and hydrogen-bonding interactions. Hence CuIIb may serve as a potential EGFR TKI.
journal_name
Environ Toxicol Pharmacoljournal_title
Environmental toxicology and pharmacologyauthors
Liang Y,Zhang T,Ren L,Jing S,Li Z,Zuo P,Li T,Wang Y,Zhang J,Wei Zdoi
10.1016/j.etap.2020.103542subject
Has Abstractpub_date
2021-01-01 00:00:00pages
103542eissn
1382-6689issn
1872-7077pii
S1382-6689(20)30219-2journal_volume
81pub_type
杂志文章abstract::There are significant challenges in assessing the toxicity of nanoparticles in the environment in which effective methods for detection are crucial. An inexpensive method that uses superhydrophobic well with an evaporating droplet followed by a simple squeeze flow is described here and found to provide practical high ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2015.06.015
更新日期:2015-07-01 00:00:00
abstract::Genistein receives much attention because of its potential to prevent hormone-related cancer and cardiovascular diseases. Limited information is available on the pharmacokinetics of this compound like, for instance, their intestinal uptake by humans and systematic bioavailability. In this study, the fate of the absorp...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2004.03.008
更新日期:2004-06-01 00:00:00
abstract::In this study, the effects of acute and subacute formaldehyde (FA) exposures on spontaneous locomotor activity (SLMA), wet dog shake (WDS) behavior and pentylenetetrazole (PTZ) induced seizures were evaluated in Balb/C mice. SLMA was concentration dependently reduced after acute FA exposures at 1.8, 3.2, 4.5, 6.4, 9.7...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/s1382-6689(01)00109-0
更新日期:2002-03-01 00:00:00
abstract::4-tert-octylphenol (4t-OP) is a well-known xenoestrogen. Our objective was to explore the effects and molecular mechanisms of 4t-OP on human sperm. Sperm samples were exposed to 0, 0.1, or 0.3 mM 4t-OP for two hours. Results showed that both sperm viability and motility were significantly injured by 0.3 mM 4t-OP. We a...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2018.07.010
更新日期:2018-09-01 00:00:00
abstract::Both β-amyloid (Aβ) catabolism and epigenetic regulation play critical roles in the onset of neurodegeneration. The latter also contribute to Pb neurotoxicity. The present study explored the role of epigenetic modifiers and Aβ degradation enzymes in Pb-induced latent effects on Aβ overproduction in vitro. Our results ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2018.12.015
更新日期:2019-02-01 00:00:00
abstract::Endosulfan, a chlorinated cyclodiene insecticide, is known to cause a significant enhancement of altered hepatic foci in rats and to be a potent inhibitor of gap-junctional intercellular communication in vitro. Both of these features are common to many tumor promoters. However, long-term studies in rodents provide no ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/1382-6689(96)00018-X
更新日期:1996-07-15 00:00:00
abstract::Epidemiological and experimental studies have demonstrated that cigarette smoking intensifies gastric ulceration. Although nicotine can act as an anxiolytic and antidepressant, its withdrawal may also lead to increased anxiety and depression. In order to associate the toxic actions of nicotine on gastric mucosa with a...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2008.10.006
更新日期:2009-03-01 00:00:00
abstract::A thiamine deficiency disease termed M74 syndrome affects the yolk-sac fry of wild and feral Baltic salmon. However, very little is known about the pharmacokinetics of thiamine in salmon. This study examined the pharmacokinetics of thiamine hydrochloride injected intraperitoneally into feral and farmed Baltic salmon f...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2004.06.001
更新日期:2005-01-01 00:00:00
abstract::The effect of neonatal manganese (Mn) exposure in a 6-hydroxydopamine (6-OHDA) rat model of Parkinson's disease was investigated. Pregnant Wistar rats were given drinking water with 10,000 ppm of Manganese (MnCl₂.4H₂O) from the time of conception until weaning on the 21st day after delivery. Control rats consumed tap ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2013.11.003
更新日期:2014-01-01 00:00:00
abstract::Uzuncayir Dam Lake is one of the most important water bodies in Tunceli. It is polluted by domestic wastewaters together with natural contamination and pesticides, which have had cumulatively negative effects. This study analyzes the effects of pollution by using the fish species, Capoeta umbla as a sentinel species, ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2014.04.001
更新日期:2014-05-01 00:00:00
abstract::DNA damage caused by environmental agents often lead to many chronic diseases, including cancer. The present study aimed to understand the relative toxicity possessed by Bisphenol A (BPA) and Bisphenol S (BPS) on human bronchial epithelial cells (BEAS-2B). The cells were exposed to either BPA or BPS and evaluated for ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2018.04.009
更新日期:2018-06-01 00:00:00
abstract::Mitochondrial damage can trigger mitophagy and eventually suppress proliferation. However, the effect of mitophagy on proliferation remains unclear. In this study, HepG2 cells were used to assess mitophagy and proliferation arrest in response to As2O3 exposure. The stimulatory effect of As2O3 on mitophagy was investig...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2016.06.006
更新日期:2016-07-01 00:00:00
abstract::The pathogenesis of atopic dermatitis (AD) involves T helper 2 (Th2) cells, and effective therapies remain elusive due to the paucity of animal models. We aimed to develop a mouse model of an immune system aberration caused by allergen. Experiments were conducted in two phases. In experiment 1, BALB/c mice were sensit...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2017.12.025
更新日期:2018-03-01 00:00:00
abstract::One purpose in this research was to determine the toxic effects of Cd on antioxidant enzymes of Oxya chinensis (Orthoptera: Acridoidae). Changes in the activities of the antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), and guaiacol peroxidase (GPx) were measured in O. chinensis insects injected with Cd(...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2005.04.001
更新日期:2005-11-01 00:00:00
abstract::The present study examines the effects of PCN congeners (PCN50 and PCN66) on zebrafish embryos. The embryos were exposed to different concentrations (20, 30 and 50μg/l) of the respective congeners by dissolving 0.08% acetone. The following endpoints were investigated (mortality, hatching rate, abnormalities and heart ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2007.09.001
更新日期:2008-01-01 00:00:00
abstract::The sensitivity of human lymphocytes from different donors to CdCl2 using a complex of methods for determination of cytotoxicity and genotoxicity was studied. As endpoints for cytotoxicity the mitotic index (MI) and apoptosis were evaluated. To indicate genotoxicity chromosome aberrations test (CA) was used. The resul...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2013.03.021
更新日期:2013-07-01 00:00:00
abstract::We have shown previously that prenatal exposure of rats to 0.5 mg/kg/day of methylmercury (MeHg) produces gender-dependent changes in motor activity in adulthood. In the present study we have investigated whether changes in motor activity could also be found during early ontogeny of the offspring. Pregnant rats were t...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/s1382-6689(00)00060-0
更新日期:2001-01-01 00:00:00
abstract::Cadmium (Cd) is a metal that is toxic to renal tubules. If renal tubules are damaged by Cd, urinary excretion of N-acetyl-β-D-glucosaminidase (NAG) and beta 2-microglobulin (β2-MG) increases. The aim of this study was to describe the changing patterns of urinary Cd, NAG, and β2-MG levels over a 3-year period in indivi...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2014.10.016
更新日期:2015-01-01 00:00:00
abstract::In this study, Al2O3, CuO and TiO2 nanoparticles (NPs) were administered to mature female rats (Rattus norvegicus var. albinos) via oral gavage (0, 0.5, 5, 50mg/kg b.w./day) for 14days to investigate their effects on 14 serum biomarkers and 4 antioxidant enzyme (catalase, superoxide dismutase, glutathione peroxidase, ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2017.02.007
更新日期:2017-03-01 00:00:00
abstract::The impact of commonly used pesticides, endosulfan and deltamethrin, on the molecular stress level in black tiger shrimp Penaeus monodon, was assessed using classical oxidative stress biomarkers, protein carbonylation profiles, and levels of heat shock proteins. Results showed that 4 days exposure to 0.1 μg L(-1) delt...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2009.05.006
更新日期:2009-09-01 00:00:00
abstract::CO2, as the typical greenhouse gas causing the greenhouse effect, is a major global environmental problem and has attracted increasing attention from governments. Using algae to eliminate CO2, which has been proposed as an effective way to reduce the greenhouse effect in the past decades, can be disturbed by a growing...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2015.08.034
更新日期:2015-11-01 00:00:00
abstract::The features of organophosphate-induced brain injuries were investigated. Rats were poisoned intraperitoneally with 9 mg/kg (1.8 LD(50)) of diisopropylfluorophosphate. Pyridostigmine bromide (0.1 mg/kg) and atropine methylnitrate (20 mg/kg), which are centrally inactive, were pre-treated intramuscularly to reduce the ...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/s1382-6689(99)00006-x
更新日期:1999-04-01 00:00:00
abstract::Myelotoxicity of pesticides and algal toxins was detected in vitro by using the granulocyte-macrophage colony forming unit assay (CFU-GM), and the MTT test with SR-4987 cells, an established stromal cell line derived from a long term murine bone marrow culture, which may represent a suitable in vitro model for studyin...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/s1382-6689(98)00029-5
更新日期:1998-10-01 00:00:00
abstract::This symposium on susceptibility and risk was the third in a series designed to bring together experts from diverse disciplines to discuss contemporary issues in risk assessment. The topic in 1996 was especially challenging since susceptibility is influenced by a myriad of factors including environmental, genetic, soc...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/s1382-6689(97)10010-2
更新日期:1997-12-01 00:00:00
abstract::Triazine herbicide atrazine is considered to be moderately toxic to various aquatic animals. The aim of our study was to evaluate the acute embryotoxicity of atrazine and its two degradation products, desisopropylatrazine and desethylatrazine, and their mixture to the early life stages of zebrafish (Danio rerio) by me...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2020.103370
更新日期:2020-07-01 00:00:00
abstract::Sodium fluoride (NaF), used as pesticides and for industrial purposes are deposited in the water bodies and therefore affects its biota. Zebrafish exposed to NaF in laboratory condition showed hyperactivity and frequent surfacing activity, somersaulting and vertical swimming pattern as compared to the control group. R...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2015.07.003
更新日期:2015-09-01 00:00:00
abstract::This study was to investigate the combined toxicity of silica nanoparticles (SiNPs) and methylmercury (MeHg) on cardiovascular system in zebrafish (Danio rerio) embryos. Ultraviolet absorption analysis showed that the co-exposure system had high absorption and stability. The dosages used in this study were based on th...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2016.05.004
更新日期:2016-06-01 00:00:00
abstract::Inhibition of intercellular communication (IC) between hepa1c1c7 cells was used as a possible bioassay to predict tumor promoting potency of polyhalogenated aromatic hydrocarbons (PAHs). Relative potencies with regard to 2,3,7,8-TCDD to inhibit IC and to induce cytochrome P450IA1/2 (EROD) in these hepa1c1c7 cells were...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/1382-6689(95)00006-2
更新日期:1996-02-15 00:00:00
abstract::Single-chemical and mixture concentration-response curves generated using a frog embryo model were examined for value in assessing whether chemicals exert toxic effects at the same or at different molecular sites of action. Toxicity tests were conducted on a series of osteolathyrogens, i.e. chemicals that inhibit cros...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2003.08.002
更新日期:2004-03-01 00:00:00
abstract::Butyl benzyl phthalate (BBP) is commonly added during the manufacturing of plastics to increase flexibility and elasticity. However, BBP leaches off of plastic and environment presence has been detected in soil, groundwater and sediment potentially effecting organisms in the environment. Given the widespread uses of B...
journal_title:Environmental toxicology and pharmacology
pub_type: 杂志文章
doi:10.1016/j.etap.2017.09.009
更新日期:2017-12-01 00:00:00