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Chemico-biological Interactions

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https://www.readbyqxmd.com/read/28818685/ethyl-carbamate-induces-cell-death-through-its-effects-on-multiple-metabolic-pathways
#1
Huichang Liu, Bo Cui, Yi Xu, Chaoyang Hu, Ying Liu, Guorun Qu, Dawei Li, Yongning Wu, Dabing Zhang, Sheng Quan, Jianxin Shi
Ethyl carbamate (EC), a multisite carcinogenic chemical causing tumors in various animal species, is probably carcinogenic to humans. However, information about the possible carcinogenic and toxicological effects of EC in humans is quite limited. Because EC is found in many dietary foods (such as fermented foods) and tobacco and its products, and exposure of humans to EC often occurs inevitably, its toxicological effects in humans need to be studied. This study was conducted to understand the metabolomic and transcriptomic changes in human hepatocellular carcinoma cells (HepG2) exposed to 100 mM EC for short term (4 h) and long term (12 h) period, respectively...
August 14, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28811126/flavonoids-from-psersimmon-diospyros-kaki-l-leaves-inhibit-proliferation-and-induce-apoptosis-in-pc-3%C3%A2-cells-by-activation-of-oxidative-stress-and-mitochondrial-apoptosis
#2
Yan Ding, Kai Ren, Huanhuan Dong, Fei Song, Jing Chen, Youtian Guo, Yanshan Liu, Weijie Tao, Yali Zhang
Persimmon (Diospyros kaki L.) leaves are extensively used in Chinese medicine and are also excellent source of dietary polyphenols. Here we investigated the antiproliferative and pro-apoptotic activity of the total flavonoids extracted from persimmon leaves (FPL) in PC-3 cells. After treating cells with different concentration of FPL, Quercetin or Rutin for 24 h, MTT and flow cytometry were used to measure the cytotoxicity, apoptotic rate and cell cycle arrest. Compared with Quercetin and Rutin, FPL showed higher cytotoxicity at 12...
August 12, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28811125/pharmacokinetics-and-pharmacodynamics-of-thiopurines-in-an-in-vitro-model-of-human-hepatocytes-insights-from-an-innovative-mass-spectrometry-assay
#3
Marco Pelin, Elena Genova, Laura Fusco, Monzer Marisat, Ute Hofmann, Diego Favretto, Marianna Lucafò, Andrea Taddio, Stefano Martelossi, Alessandro Ventura, Gabriele Stocco, Matthias Schwab, Giuliana Decorti
AIM: To apply an innovative LC-MS/MS method to quantify thiopurine metabolites in human hepatocytes and to associate them to cytotoxicity. METHODS: Immortalized human hepatocytes (IHH cells) were treated for 48 and 96 h, with 1.4 × 10(-4) M azathioprine and 1.1 × 10(-3) M mercaptopurine, concentrations corresponding to the IC50 values calculated after 96 h exposure in previous cytotoxicity analysis. After treatments, cells were collected for LC-MS/MS analysis to quantify 11 thiopurine metabolites with different level of phosphorylation and viable cells were counted by Trypan blue exclusion assay to determine thiopurines in vitro effect on cell growth and survival...
August 12, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28807745/acute-toxicity-of-functionalized-single-wall-carbon-nanotubes-a-biochemical-histopathologic-and-proteomics-approach
#4
Homa Ahmadi, Mohammad Ramezani, Rezvan Yazdian Robati, Behzad Behnam, Kamal Razavi Azarkhiavi, Azadeh Hashem Nia, Ahad Mokhtarzadeh, Maryam Matbou Riahi, Bibi Marjan Razavi, Khalil Abnous
Recently carbon nanotubes (CNTs) showed promising potentials in different biomedical applications but their safe use in humans and probable toxicities are still challenging. The aim of this study was to determine the acute toxicity of functionalized single walled carbon nanotubes (SWCNTs). In this project, PEGylated and Tween functionalized SWCNTs were prepared. BALB/c mice were randomly divided into nine groups, including PEGylated SWCNTs (75,150μg/mouse) and PEG, Tween80 suspended SWCNTs, Tween 80 and a control group (intact mice)...
August 11, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28803762/apigenin-protects-against-alcohol-induced-liver-injury-in-mice-by-regulating-hepatic-cyp2e1-mediated-oxidative-stress-and-ppar%C3%AE-mediated-lipogenic-gene-expression
#5
Feng Wang, Jin-Cheng Liu, Rui-Jun Zhou, Xi Zhao, Mei Liu, Hua Ye, Mei-Lin Xie
Alcohol is a major cause of liver injury, and there are currently no ideal pharmacological reagents that can prevent or reverse this disease. Apigenin is one of the most common flavonoids present in numerous plants and has many beneficial effects. But whether or not apigenin may protect against alcohol-induced liver injury remains unknown. Our aim was to examine the effect and potential mechanisms. The experimental mice were given 56% erguotou wine or simultaneously given apigenin 150-300 mg/kg by gavage for 30 days...
August 10, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28803117/phenolics-from-rubus-fairholmianus-induces-cytotoxicity-and-apoptosis-in-human-breast-adenocarcinoma-cells
#6
Blassan P George, Heidi Abrahamse, Nanjundaswamy M Hemmaragala
Herbal medicine is an important part of health care system in most of the countries. Rubus fairholmianus is an unexplored berry in folkloric medicine. In this study, we aimed to understand the importance of R. fairholmianus in pharmaceutical industry for the development of cost-effective cancer therapeutic drugs using in vivo and in vitro analysis. Chemical characterisation, antioxidant, antiproliferative and apoptosis inducing properties of R. fairholmianus root methanolic column subfraction (RFM) were investigated...
August 9, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28784314/clusterin-and-neuropilin-2-as-potential-biomarkers-of-tumor-progression-in-benzo-a-pyrene-transformed-16hbe-cells-xenografted-nude-mouse-model
#7
Yu Wang, Yongrui Jia, Lailai Yan, Juanling Fu, Mingmei Hao, Wen Chen, Biyun Yao, Peng Zhao, Zongcan Zhou
Benzo[a]pyrene (BaP) is a ubiquitous environment contaminant and its exposure could increase incidence of human lung cancer. In order to confirm and compare potential biomarkers of BaP-induce carcinogenesis and tumor progression, time-dependent changes of clusterin (CLU) and neuropilin-2 (NRP2) levels were evaluated in sera of BaP-transformed 16HBE cell line T-16HBE-C1 cells xenografted nude mice. Performance of CLU and NRP2 on tissue classification and tumor progression forecast was also calculated. Levels of CLU and NRP2 were significant elevated in both culture supernatant of T-16HBE-C1 cells and sera of T-16HBE-C1 cells xenografted nude mice compared with control...
August 4, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28782499/antitumor-activity-of-%C3%AE-2-himachalen-6-ol-in-colon-cancer-is-mediated-through-its-inhibition-of-the-pi3k-and-mapk-pathways
#8
Hamid E Daaboul, Costantine F Daher, Kikki Bodman-Smith, Robin I Taleb, Wassim N Shebaby, Joelle Boulos, Carole Dagher, Mohamad A Mroueh, Mirvat El-Sibai
Previous studies in our laboratory showed that Daucus carota oil extract (DCOE) possesses in vitro and in vivo anticancer activities. Chemical analysis of DCOE led to the isolation of β-2-himachalen-6-ol (HC) which exhibited potent anticancer activity against colon, breast, brain and skin cancer cells. The present study investigates the anticancer activity of HC against SW1116 colon cancer cell lines, and evaluates its effect in a 1,2-dimethylhydrazine (DMH) colon carcinogenesis black6 mice model. The SW1116 colon cancer cell line was treated with HC (1, 5, 10 and 25 μg/ml) and cell viability was evaluated with WST 1 assay kit...
August 3, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28780322/reduction-of-oxidative-damages-induced-by-titanium-dioxide-nanoparticles-correlates-with-induction-of-the-nrf2-pathway-by-gspe-supplementation-in-mice
#9
Linpeng Niu, Mengjiao Shao, Yuan Liu, Jinfeng Hu, Ruofan Li, Heran Xie, Lixiao Zhou, Lei Shi, Rong Zhang, Yujie Niu
Titanium dioxide nanoparticles (TiO2 NPs) are widely used to additives in cosmetics, pharmaceuticals, paints and foods. Recent studies have demonstrated that TiO2 NPs increased the risk of cancer and the mechanism might relate with oxidative stress. Grape seed procyanidin extract (GSPE) is a natural compound which has been demonstrated to possess a wide array of pharmacological and biochemical actions, including anti-inflammatory, anti-carcinogenic, and antioxidant properties. Our data show that GSPE prevents the changes of histopathology and biomarkers in heart, liver and kidney that occur in mice exposed to TiO2 NPs...
August 2, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28780321/activation-versus-inhibition-of-microsomal-glutathione-s-transferase-activity-by-acrolein-dependence-on-the-concentration-and-time-of-acrolein-exposure
#10
Mireille M J P E Sthijns, Gertjan J M den Hartog, Caterina Scasso, Jan P Haenen, Aalt Bast, Guido R M M Haenen
The toxicity of acrolein, an α,β-unsaturated aldehyde, is due to its soft electrophilic nature and primarily involves the adduction of protein thiols. The thiol glutathione (GSH) forms the first line of defense against acrolein. The present study confirms that acrolein added to isolated rat liver microsomes can increase microsomal GSH transferase (MGST) activity 2-3 fold, which can be seen as a direct adaptive increase in the protection against acrolein. At a relatively high exposure level, acrolein appeared to inhibit MGST...
August 2, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28757137/in%C3%A2-vitro-and-in%C3%A2-vivo-pharmacokinetics-and-toxicity-evaluation-of-curcumin-incorporated-titanium-dioxide-nanoparticles-for-biomedical-applications
#11
Sainulabdeen Sherin, Sathyabhama Sheeja, Rukhmini Sudha Devi, Sreedharan Balachandran, Rema Sreenivasan Soumya, Annie Abraham
The present study deals with the preparation of stable Curcumin incorporated Titaniumdioxide Nanoparticles (CTNPs) by coprecipitation method for improving the bioavailability of curcumin and site specific drug delivery. The prepared nanoparticles were characterized by UV visible spectroscopy, FTIR, XRD, DLS, SEM and EDX. The characterization studies showed the interaction of curcumin to titanium dioxide nanoparticles. The average size of the prepared CTNPs was found to be ∼29 nm with zetapotential of-53...
July 28, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28757134/effects-of-combined-inositol-hexakisphosphate-and-inositol-supplement-on-antioxidant-activity-and-metabolic-enzymes-in-the-liver-of-streptozotocin-induced-type-2-diabetic-rats
#12
Shadae R Foster, Lowell L Dilworth, Rory K Thompson, Ruby L Alexander-Lindo, Felix O Omoruyi
Diabetes mellitus is associated with elevated reactive oxygen species, lipid abnormalities, reduced antioxidant activity and organ damage. This study examines the effects of combined inositol hexakisphosphate (IP6) and inositol supplement on antioxidant levels and other biochemical parameters in the liver of type 2 diabetic rats. Five groups of Sprague-Dawley rats were studied. Six rats were fed normal diet (non-diabetic control), while 24 rats were fed high-fat diet (HFD) for 4 weeks. Diabetes was induced in 18 of the rats fed HFD by intraperitoneal administration of streptozotocin...
July 28, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28757136/iminoenamine-based-novel-androgen-receptor-antagonist-exhibited-anti-prostate-cancer-activity-in-androgen-independent-prostate-cancer-cells-through-inhibition-of-akt-pathway
#13
S Divakar, K Saravanan, P Karthikeyan, R Elancheran, S Kabilan, K K Balasubramanian, Rajlakshmi Devi, J Kotoky, M Ramanathan
Treatment by androgen receptor (AR) antagonists is one of the regimens for prostate cancer. The prolonged treatment with AR antagonist leads to the expression of point mutation in the ligand binding domain of the AR. This point mutation causes resistance to AR antagonist by converting them into an agonist. The T887A mutated AR was frequently expressed in androgen independent prostate cancer (AIPC) patients. Through literature survey and molecular modelling, we have identified a novel AR antagonist having a bulky β-iminoenamine BF2 complex scaffold...
July 27, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28757135/synergism-between-thioredoxin-reductase-inhibitor-ethaselen-and-sodium-selenite-in-inhibiting-proliferation-and-inducing-death-of-human-non-small-cell-lung-cancer-cells
#14
Xiaoqing Zheng, Wei Xu, Ruoxuan Sun, Hanwei Yin, Chaoran Dong, Huihui Zeng
New effective treatment for human non-small cell lung cancer (NSCLC) is needed. The thioredoxin (Trx) system composes of thioredoxin reductase (TrxR), Trx and NADPH. In this study, we combined an organic selenium compound--TrxR inhibitor ethaselen (BBSKE) with low dosage sodium selenite to inhibit proliferation and induce death of NSCLC cells, and identified underlying mechanisms. Synergistic anti-proliferation effect of BBSKE and selenite was found in human NSCLC cell lines, A549, NCI-H1299 and NCI-1266. A significant increase of apoptosis, necrosis and autophagy were observed in the group of BBSKE plus selenite in A549 cells...
July 27, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28756151/polyionic-complexes-of-butyrylcholinesterase-and-poly-l-lysine-g-poly-ethylene-glycol-comparative-kinetics-of-catalysis-and-inhibition-and-in%C3%A2-vitro-inactivation-by-proteases-and-heat
#15
Kirstin Hester, Jing Liu, Nicholas Flynn, Lester G Sultatos, Liyi Geng, Stephen Brimijoin, Joshua D Ramsey, Steven Hartson, Ashish Ranjan, Carey Pope
We previously reported that recombinant human butyrylcholinesterase (rhBChE) complexed with a series of copolymers of poly-l-lysine (PLL) with grafted (polyethylene) glycol (PEG) (i.e., PLL-g-PEG) showed reduced catalytic activity but relatively similar concentration-dependent inactivation of the organophosphorus inhibitor paraoxon. Herein, we compared the kinetics of catalysis (using butyrylthiocholine as the substrate) and inhibition (using four different inhibitors) of free and copolymer-complexed rhBChE...
July 27, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28756150/a-marine-sponge-alkaloid-derivative-4-chloro-fascaplysin-inhibits-tumor-growth-and-vegf-mediated-angiogenesis-by-disrupting-pi3k-akt-mtor-signaling-cascade
#16
Sonia Sharma, Santosh Kumar Guru, Sudhakar Manda, Ashok Kumar, Mubashir J Mintoo, Venna Deva Prasad, Parduman R Sharma, Dilip M Mondhe, Sandip B Bharate, Shashi Bhushan
Tumor angiogenesis and PI3K/Akt/mTOR pathway are two major molecular objectives for the treatment and management of breast cancer. Here we first time report the molecular mechanism of a marine sponge alkaloid derivative 4-chloro fascapysin (4-CF) for its anticancer and antiangiogenesis potential. It simultaneously targets multiple cancer and angiogenesis dynamics, such as proliferation, chemotaxis cell migration, and invasion, growth factors signaling cascade, autophagy and apoptosis in HUVEC and MDAMB-231 breast cancer cells...
July 26, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28756149/anticancer-potential-of-amaryllidaceae-alkaloids-evaluated-by-screening-with-a-panel-of-human-cells-real-time-cellular-analysis-and-ehrlich-tumor-bearing-mice
#17
Radim Havelek, Darina Muthna, Pavel Tomsik, Karel Kralovec, Martina Seifrtova, Lucie Cahlikova, Anna Hostalkova, Marcela Safratova, Maria Perwein, Eva Cermakova, Martina Rezacova
In this study, twenty-two Amaryllidaceae alkaloids were screened for their anticancer potential. All isolates were evaluated for antiproliferative activities on a panel of 17 human cell types of different tissue origin using WST-1 assay. In addition, we determined the antiproliferative effect with a real-time cell analysis xCELLigence system. Thereafter, to evaluate the barely known in vivo anticancer potential of the most potent molecule haemanthamine, a preliminary study was performed using an Ehrlich tumor-bearing mice model...
July 26, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28756148/ginsenoside-rg2-protects-pc12%C3%A2-cells-against-%C3%AE-amyloid25-35-induced-apoptosis-via-the-phosphoinositide-3-kinase-akt-pathway
#18
Jing Cui, Jiao Wang, Meizhu Zheng, Dongxia Gou, Chunming Liu, Yifa Zhou
Alzheimer's disease (AD) is one of the most debilitating neurodegenerative diseases in an aging population. Excessive accumulation of β-amyloid (Aβ) has been proposed as a pivotal event in the pathogenesis of AD. Ginsenoside Rg2 has been reported to exert neuroprotective effects. However, the underlying mechanism for its neuroprotection is not well-understood. In this study, we investigated the protective effects of ginsenoside Rg2 on Aβ25-35-induced neurotoxicity in PC12 cells and identified a potential molecular signaling pathway involved...
July 26, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28751004/polyphenols-activate-energy-sensing-network-in-insulin-resistant-models
#19
Radika Mutlur Krishnamoorthy, Anuradha Carani Venkatraman
Unhealthy diet deficient in fruits and vegetables but rich in calories is considered to be one factor responsible for the increased prevalence of insulin resistance and type 2 diabetes (T2D). The consumption of fast foods and soft drinks increases fructose consumption per se and this is of major concern since prolonged fructose intake induces insulin resistance and thereby T2D. The energy homeostasis is regulated by a network consisting of "fuel gauze" called AMP-activated protein kinase (AMPK), the NAD(+) dependent type III deacetylase (SIRT1) and peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) which is disrupted in T2D...
July 24, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28735861/protective-role-of-benzoselenophene-derivatives-of-resveratrol-on-the-induced-oxidative-stress-in-intestinal-myofibroblasts-and-osteocytes
#20
Vladana Domazetovic, Filippo Fontani, Damiano Tanini, Veronica D'Esopo, Caterina Viglianisi, Gemma Marcucci, Lucia Panzella, Alessandra Napolitano, Maria Luisa Brandi, Antonella Capperucci, Stefano Menichetti, Maria Teresa Vincenzini, Teresa Iantomasi
Resveratrol (RE), a polyphenolic compound present in some food and plants, is characterized by anti-inflammatory and antioxidant properties. However, it is quickly metabolized with consequent loss of its efficacy. In this study, the antioxidant effect of 2-phenyl-benzoselenophene derivatives (VD0, VD1 and VD2) was detected in intestinal myofibroblast and osteocyte cell lines in which the oxidative stress was induced by GSH depletion or starvation, respectively. In fact, the oxidative stress is involved in pathogenesis of inflammatory bowel diseases (IBD) and in increased osteoclastogenesis in osteoporosis...
July 21, 2017: Chemico-biological Interactions
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