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https://www.readbyqxmd.com/read/29781726/in-vitro-analysis-of-glucose-and-quercetin-effects-on-m-tor-and-nrf-2-expression-in-hepg2-cell-line-diabetes-and-cancer-connection
#1
Amir Yarahmadi, Fatemeh Khademi, Zohreh Mostafavi-Pour, Fatemeh Zal
Some types of cancers show a strong relationship with diabetes and play a central role in mortality in the patient population suffering from diabetes mellitus. In this study, HepG2 cells have been used to investigate the toxic effects of hyperglycemia and/or quercetin (Q) on mammalian target of rapamycin (m-TOR) and nuclear factor erythroid 2-related factor 2 (Nrf-2) expression as central molecules involved in cancer. HepG2 cells were cultured with different concentrations of glucose (5.5, 30, and 50 mM) and/or Q (25 µM) for 48 and 72 h...
May 21, 2018: Nutrition and Cancer
https://www.readbyqxmd.com/read/29778425/lncrna-hotair-contributes-to-the-malignancy-of-hepatocellular-carcinoma-by-enhancing-epithelial-mesenchymal-transition-via-sponging-mir-23b-3p-from-zeb1
#2
Tao Yang, Xiaojun He, An Chen, Kai Tan, Xilin Du
Hepatocellular carcinoma (HCC) is the fifth most common cancer around the world, along with high mortality and metastasis rate. Our present study aimed to explore the role of LncRNA HOTAIR in the progression of HCC. Our data showed that HOTAIR was overexpressed in HCC tissues and cell lines (Huh7, Hep3B, HepG2, MHCC97H). Overexpressed HOTAIR promoted invasion and migration of HCC cells (Huh7) by enhancing epithelial-mesenchymal transition (EMT). Besides that, miR-23b-3p was predicted to be a target of HOTAIR and decreased expression of miR-23b-3p was observed in HCC tissues and cell lines...
May 17, 2018: Gene
https://www.readbyqxmd.com/read/29778027/influence-of-gastrointestinal-tract-on-metabolism-of-bisphenol-a-as-determined-by-in-vitro-simulated-system
#3
Yonghua Wang, Min Rui, Yang Nie, Guanghua Lu
Oral exposure is a major route of human bisphenol A (BPA) exposure. However, influence of gastrointestinal tract on BPA metabolism is unavailable. In this study, in vitro simulator of the human intestinal microbial ecosystem (SHIME) was applied to investigate the changes in bioaccessibility and metabolism of BPA in different parts of gastrointestinal tract (stomach, small intestine and colon). Then the human hepatoma cell line HepG2 was employed to compare toxic effects of BPA itself and effluents of SHIME system on hepatic gene expression profiles...
May 7, 2018: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/29777702/microrna-608-inhibits-human-hepatocellular-carcinoma-cell-proliferation-via-targeting-the-bet-family-protein-brd4
#4
Ling He, Dijuan Meng, Shi-Hu Zhang, Yi Zhang, Zhengming Deng, Lian-Bao Kong
Over-expression of the bromodomain and extraterminal (BET) family protein BRD4 is associated with hepatocellular carcinoma (HCC) progression. In the present study, we indentified a novel putative anti-BRD4 microRNA: microRNA-608 ("miR-608"). In HepG2 cells and primary human HCC cells, over-expression of miR-608, using a lentiviral construct, induced BRD4 downregulation and proliferation inhibition. Conversely, transfection of the miR-608 inhibitor increased BRD4 expression to promote HepG2 cell proliferation...
May 16, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29775890/triterpenic-acids-enriched-fraction-from-cyclocarya-paliurus-attenuates-non-alcoholic-fatty-liver-disease-via-improving-oxidative-stress-and-mitochondrial-dysfunction
#5
Meng-Ge Zhao, Xue-Ping Sheng, Ya-Ping Huang, Yi-Ting Wang, Cui-Hua Jiang, Jian Zhang, Zhi-Qi Yin
The effects of triterpenic acids-enriched fraction from Cyclocarya paliurus (CPT) on nonalcoholic fatty liver disease (NAFLD) were investigated using in vivo and in vitro models. In high fat diet-induced Wister rats, CPT significantly increased superoxide dismutase (SOD) activity and glutathione/oxidized glutathione (GSH/GSSG) ratio, reduced malondialdehyde (MDA) and protein carbonyl (PCO) levels. Moreover, CPT restored mitochondrial membrane potential dysfunction, decreased cytochrome P450 enzyme 2E1 (CYP2E1) activity, improved nuclear factor erythroid 2-related factor 2 (Nrf2) and Nrf2-mediated antioxidant enzyme heme oxygenase1 (HO-1) expression...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775214/pressurized-hot-water-extraction-of-bioactive-compounds-from-artichoke-by-products
#6
Imma Pagano, Anna Lisa Piccinelli, Rita Celano, Luca Campone, Patrizia Gazzerro, Mariateresa Russo, Luca Rastrelli
Artichoke by-products are a suitable source of health-promoting ingredients for the production of dietary supplements and food additives. A pressurized hot water extraction (PHWE) was developed to recover caffeoylquinic acids (CQAs) and flavone glycosides (FLs) from agro-industrial artichoke by-products. The main factors influencing PHWE efficiency and CQA isomerization (temperature, numbers of cycles, modifier and extraction time) were carefully studied and optimized by response surface design. The proposed PHWE procedure provides an exhaustive extraction of CQAs and FLs (recoveries: 93-105 and 90-105%) from artichoke external bracts and leaves of different cultivars (p > 0...
May 18, 2018: Electrophoresis
https://www.readbyqxmd.com/read/29774579/integrative-epigenetic-analysis-reveals-therapeutic-targets-to-the-dna-methyltransferase-inhibitor-sgi-110-in-hepatocellular-carcinoma
#7
Minmin Liu, Lian Zhang, Hongtao Li, Toshinori Hinoue, Wanding Zhou, Hitoshi Ohtani, Anthony El-Khoueiry, John Daniels, Casey O'Connell, Tanya B Dorff, Qianjin Lu, Daniel J Weisenberger, Gangning Liang
There is an urgent need for developing more effective therapies for hepatocellular carcinoma (HCC) because of its aggressiveness. Guadecitabine (SGI-110) is a second-generation DNA methyltransferase inhibitor (DNMTi) currently in clinical trials for HCC and shows greater stability and performance over first generation DNMTis. In order to identify potential therapeutic targets of SGI-110 for clinical trials, HCC cell lines (SNU398, HepG2 and SNU475) were used to evaluate effects of transient SGI-110 treatment by an integrative analysis of DNA methylation, nucleosome accessibility, gene expression profiles and its clinical relevance by comparisons to TCGA HCC clinical data...
May 18, 2018: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/29774349/role-of-arsenic-3-oxidation-state-methyltransferase-in-arsenic-mediated-apl-treatment-an-in-vitro-investigation
#8
Yasen Maimaitiyiming, Chao Wang, Shi Xu, Khairul Islam, Ye Jia Chen, Chang Yang, Qian Qian Wang, Hua Naranmandura
Arsenic (+3 oxidation state) methyltransferase (AS3MT) is a key enzyme responsible for arsenic metabolism in humans, which facilitates conversion of arsenic trioxide (As2O3) to more reactive metabolites such as monomethylarsonous acid (MMAIII) and dimethylarsinous acid (DMAIII). However, it is unclear whether the biotransformation of arsenic by AS3MT contributes to the promotion of acute promyelocytic leukemia (APL) therapy. In order to understand the probable role of AS3MT in APL patients, we evaluated the effects of arsenite (iAsIII) and three mixed arsenicals (i...
May 18, 2018: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/29773008/antimicrobial-cytotoxic-anti-inflammatory-and-antioxidant-activity-of-culinary-processed-shiitake-medicinal-mushroom-lentinus-edodes-agaricomycetes-and-its-major-sulfur-sensory-active-compound-lenthionine
#9
Kristyna Kupcova, Iveta Stefanova, Zuzana Plavcova, Jan Hosek, Pavel Hrouzek, Roman Kubec
The antimicrobial, cytotoxic, anti-inflammatory, and antioxidant properties of aqueous extracts of raw and culinary processed shiitake mushrooms were evaluated and compared with those of lenthionine (1,2,3,5,6-penta-thiepane), the principal aroma-bearing substance of the shiitake medicinal mushroom (Lentinus edodes). Antimicrobial activity was tested using a panel of 4 strains of bacteria, 2 yeasts, and 2 fungi. Cytotoxic properties were evaluated against 3 cell lines (HepG2, HeLa, PaTu), whereas the anti-inflammatory activity of tested samples was assayed based on their ability to attenuate the secretion of the cytokine tumor necrosis factor-α...
2018: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/29772746/design-synthesis-and-biological-evaluation-of-benzimidazole-derived-biocompatible-copper-ii-and-zinc-ii-complexes-as-anticancer-chemotherapeutics
#10
Mohamed F AlAjmi, Afzal Hussain, Md Tabish Rehman, Azmat Ali Khan, Perwez Alam Shaikh, Rais Ahmad Khan
Herein, we have synthesized and characterized a new benzimidazole-derived "BnI" ligand and its copper(II) complex, [Cu(BnI)₂], 1 , and zinc(II) complex, [Zn(BnI)₂], 2 , using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2 , but complex 1 showed more avid binding to HSA and DNA...
May 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29772386/novel-anticancer-hybrids-from-diazen-1-ium-1-2-diolate-nitric-oxide-donor-and-ros-inducer-plumbagin-design-synthesis-and-biological-evaluations
#11
Na Bao, Jinfeng Ou, Na Li, Pian Zou, Jianbo Sun, Li Chen
High levels of both nitric oxide (NO) and reactive oxygen species (ROS) could act as pro-apoptotic signals in cancerous cells. In this study, we conjugated diazeniumdiolates (NONOates), an important class of NO donors, with a natural occurring plumbagin (PL) which is primarily an excellent ROS inducer. Herein, a total of 12 novel plumbagin/NONOate hybrids have been synthesized and evaluated for their inhibitory effects on a panel of human cancer cell lines (MDA-MB-231, A549, HepG2 and HCT-116 cells) and two normal human cells (HK-2 and WRL-68 cells)...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29772305/jatrophane-diterpenoids-from-euphorbia-helioscopia-and-their-lipid-lowering-activities
#12
Jun Li, Hui-Hui Li, Wen-Qiong Wang, Wei-Bin Song, Yi-Ping Wang, Li-Jiang Xuan
The phytochemical study of Euphorbia helioscopia led to the isolation of 33 jatrophane diterpenoids (1-33), of which six (1-6) were new. This small jatrophane library was established to screen for potential lipid modulators. LDL-Uptake screening assay demonstrated that most of them improved LDL-Uptake rate in HepG2 cells, with compounds 16, 21 and 26 exhibiting more outstanding effects. Further exploration found that these three compounds could increase LDLR protein level in HepG2 cells dose-dependently. SAR studies suggested that substituted patterns of C-9, steric hindrance between C-14 and C-15, and the long conjugated fragment from C-5 to the carbonyl (C-9) were essential for the activity...
May 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29772274/pharmacodynamic-and-pharmacokinetic-characteristics-of-ymr-65-a-tubulin-inhibitor-in-tumor-bearing-mice
#13
Ali Fan, Jiali Wei, Mengru Yang, Qing Zhang, Yaliang Zhang, Qingwang Liu, Ning Li, Di Zhao, Yang Lu, Junxiu Li, Jie Zhao, Shuhua Deng, Bingjie Zhang, Hailiang Zhu, Xijing Chen
YMR-65, 5-(5-bromo-1-methyl-1H-indol-3-yl)-3-(3-methoxyphenyl)-4, 5-dihydro-1H-pyrazole-1-carboxamide, is a potential tubulin inhibitor exhibiting good anticancer activity. In our study, we illustrated the biological activities in HepG2 cells and the pharmacodynamic and pharmacokinetic profiles were evaluated in murine H22 hepatoma-bearing mice. Molecular docking assay and colchicine competition assay indicated that YMR-65 could bind tightly to the colchicine binding site of tubulin. Further investigation demonstrated that YMR-65 arrested cells in the G2/M phase of cell cycle and induced apoptosis in HepG2 cells...
May 14, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29771984/dna-methylation-of-hepatic-iron-sensing-genes-and-the-regulation-of-hepcidin-expression
#14
Paul A Sharp, Rachel Clarkson, Ahmed Hussain, Robert J Weeks, Ian M Morison
Production of the iron regulatory peptide hepcidin is tightly controlled by a network of proteins in hepatocytes that sense levels of iron in the circulation (as diferric-transferrin) and in tissues (in ferritin). Human studies show high variability in the normal range of serum hepcidin levels. We have postulated that this may, in part, be related to inter-individual variability in the expression of genes in the iron sensing pathway, potentially governed by epigenetic factors. Here, we have investigated whether genes encoding hepatic iron sensing proteins and hepcidin are regulated by DNA methylation...
2018: PloS One
https://www.readbyqxmd.com/read/29771951/antitumor-antioxidant-and-anti-inflammatory-activities-of-kaempferol-and-its-corresponding-glycosides-and-the-enzymatic-preparation-of-kaempferol
#15
Jingqiu Wang, Xianying Fang, Lin Ge, Fuliang Cao, Linguo Zhao, Zhenzhong Wang, Wei Xiao
Kaempferol (kae) and its glycosides are widely distributed in nature and show multiple bioactivities, yet few reports have compared them. In this paper, we report the antitumor, antioxidant and anti-inflammatory activity differences of kae, kae-7-O-glucoside (kae-7-O-glu), kae-3-O-rhamnoside (kae-3-O-rha) and kae-3-O-rutinoside (kae-3-O-rut). Kae showed the highest antiproliferation effect on the human hepatoma cell line HepG2, mouse colon cancer cell line CT26 and mouse melanoma cell line B16F1. Kae also significantly inhibited AKT phosphorylation and cleaved caspase-9, caspase-7, caspase-3 and PARP in HepG2 cells...
2018: PloS One
https://www.readbyqxmd.com/read/29771500/rational-design-of-cancer-targeted-selenadiazole-derivative-as-efficient-radiosensitizer-for-precise-cancer-therapy
#16
Delong Zeng, Shulin Deng, Chengcheng Sang, Jianfu Zhao Zhao, Tianfeng Chen
Chemical drug design based on the biochemical characteristics of cancer cells has become an important strategy for discovery of targeted therapies for personalized cancer medicine. Herein, cancer targeting RGD peptide has been covalently conjugated to selenadiazole derivative (RGD-SeD) to improve its cancer selectivity. The RGD decoration significantly enhances the anticancer efficacy of RGD-SeD in αVβ3 integrin-overexpressing HepG2 liver cancer cells, but not in normal liver cells. Cellular uptake assay and fluorescent imaging confirmed the selectivity of RGD-SeD to integrin overexpressing cancer cells...
May 17, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29771149/preparation-and-evaluation-of-tumour-microenvironment-response-multistage-nanoparticles-for-epirubicin-delivery-and-deep-tumour-penetration
#17
Jialing Dai, Shangcong Han, Fang Ju, Mei Han, Lisa Xu, Ruoyu Zhang, Yong Sun
Poor tumour penetration became a major challenge for the use of nanoparticles in anticancer therapy. To further enhance the tumour penetration efficiency, we developed a tumour-microenvironment-responsive multistage drug delivery system which was formed layer by layer via electrostatic interaction with cationic drug-loaded nanoparticles, hyaluronidase (HAase) and iRGD-modified gelatin (G-iRGD). The drug-loaded nanoparticles were formed by self-assembling mPEG-PDPA-PG and encapsulation with epirubicin (EPI)...
May 17, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29768704/syntheses-and-immunological-evaluation-of-self-adjuvanting-clustered-n-acetyl-and-n-propionyl-sialyl-tn-combined-with-a-t-helper-cell-epitope-as-antitumor-vaccine-candidates
#18
Tsung-Che Chang, Yoshiyuki Manabe, Yukari Fujimoto, Shino Ohshima, Yoshie Kametani, Kazuya Kabayama, Yuka Nimura, Chun-Cheng Lin, Koichi Fukase
Sialyl-Tn (STn) is a tumor-associated carbohydrate antigen (TACA) rarely observed on healthy tissues. We synthesized two fully synthetic N-acetyl and N-propionyl STn trimer (triSTn) vaccines possessing a T-helper epitope and a TLR2 agonist, since the clustered STn antigens are highly expressed on many cancer cells. Immunization of both vaccines in mice induced the anti-triSTn IgG antibodies, which recognized triSTn-expressing cell lines PANC-1 and HepG2. The N-propionyl triSTn vaccine induced the triSTn-specific IgGs, while IgGs induced by the N-acetyl triSTn vaccine were less specific...
May 16, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29767236/fenretinide-inhibits-the-proliferation-and-migration-of-human-liver-cancer-hepg2-cells-by-downregulating-the-activation-of-myosin-light-chain-kinase-through-the-p38%C3%A2-mapk-signaling-pathway
#19
Ling Zhang, Daobin Huang, Decui Shao, Hui Liu, Qing Zhou, Shuyu Gui, Wei Wei, Yuan Wang
N-(4-hydroxyphenyl)retinamide (4-HPR or fenretinide), which is a synthetic analog of all‑trans retinoic acid (ATRA), effectively inhibits the growth of several types of tumor cells; however, its molecular mechanism remains unclear. We found that 4‑HPR altered the morphology of human liver cancer HepG2 cells and also inhibited their proliferation and suppressed the colony formation in a dose‑ and time‑dependent manner. A wound healing assay revealed that 4‑HPR significantly hindered HepG2 cell migration, and that this was accompanied by the phosphorylation of p38‑MAPK (mitogen‑activated protein kinase)...
May 16, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29766185/the-curcumin-derivative-wz35-activates-ros-dependent-jnk-to-suppress-hepatocellular-carcinoma-metastasis
#20
Lihua Wang, Lijie Han, Zheying Tao, Zheng Zhu, Lei Han, Zhenfei Yang, Hao Wang, Dandan Dai, Liang Wu, Zhengzhong Yuan, Tongke Chen
Tumor metastasis is the leading cause of cancer death; due to the progress made in the elucidation of the mechanism of cancer cell metastasis, there is hope for patients with severe stages of cancer. Curcumin, as a novel anti-cancer drug, has been applied in cancer therapy; however, the toxicity of curcumin hinders its application. Herein, we constructed a novel derivative, WZ35, and evaluated its metastatic inhibition properties in vitro and in vivo. CCK-8 assay was performed to evaluate the tumor suppressive activity of WZ35...
May 16, 2018: Food & Function
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