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Yi-Xin Wu, Jia-Hua Yang, Hirotomo Saitsu
Bortezomib (BTZ), a proteasome inhibitor, is the first proteasome inhibitor to be used in clinical practice. Here we investigated the mechanisms underlying acquired bortezomib resistance in hepatocellular carcinoma (HCC) cells. Using stepwise selection, we established two acquired bortezomib-resistant HCC cell lines, a bortezomib-resistant HepG2 cell line (HepG2/BTZ) and bortezomib-resistant HuH7 cell line (HuH7/BTZ). The 50% inhibitory concentration values of HepG2/BTZ and HuH7/BTZ were respectively 15- and 39-fold higher than those of parental cell lines...
October 18, 2016: Oncotarget
Jian Huang, Lei Zhao, Ping Yang, Zhen Chen, Ni Tang, Xiong Z Ruan, Yaxi Chen
Hepatitis B virus (HBV) is a hepatocyte-specific DNA virus whose gene expression and replication are closely associated with hepatic metabolic processes. Thus, a potential anti-viral strategy is to target the host metabolic factors necessary for HBV gene expression and replication. Recent studies revealed that fatty acid translocase CD36 is involved in the replication, assembly, storage, and secretion of certain viruses, such as hepatitis C virus (HCV) and human immunodeficiency virus (HIV). However, the relationship between CD36 and the HBV life cycle remains unclear...
2016: PloS One
Areerat Kunanopparat, Ingorn Kimkong, Tanapat Palaga, Pisit Tangkijvanich, Boonchoo Sirichindakul, Nattiya Hirankarn
AIM: To investigate autophagy-related genes, particularly ATG12, in apoptosis and cell cycle in hepatitis B virus (HBV)-associated hepatocellular carcinoma (HCC) and non-HBV-HCC cell lines. METHODS: The expression of autophagy-related genes in HBV-associated hepatocellular carcinoma and non-HBV-HCC cell lines and human liver tissues was examined by quantitative real-time reverse transcriptase-polymerase chain reaction (qRT-PCR) and western blotting. The silencing of target genes was used to examine the function of various genes in apoptosis and cell cycle progression...
October 7, 2016: World Journal of Gastroenterology: WJG
Chengliang Zhu, Guosheng Gao, Hui Song, Fengxia Xu, Kailang Wu, Xinghui Liu
BACKGROUND: Hepatitis B virus (HBV) infection causes lipid metabolism disorders. Apolipoprotein A5 (ApoA5) is a new apolipoprotein family member that plays an important role in the regulation of lipid metabolism. The present study was to investigate the impact of HBV on ApoA5 expression and its regulatory mechanism. METHODS: Reverse transcription polymerase chain reaction (RT-PCR) and western blotting were used to measure ApoA5 mRNA and protein expression in HepG2 and HepG2...
October 10, 2016: Lipids in Health and Disease
Dong-Ping Xu, Jie Zheng, Yue Zhou, Ya Li, Sha Li, Hua-Bin Li
The Thelephora ganbajun mushroom has been found to be a potential rich source of natural antioxidants. In this study, an ultrasound-assisted extraction (UAE) technique together with GRAS (generally recognized as safe) solvents (ethanol and water) was used to maximize the extraction of antioxidants from Thelephora ganbajun. Five extraction parameters (ethanol concentration, solvent to solid ratio, extraction time, temperature and ultrasound power) were investigated by single-factor experiments, and then a central composite rotatable design was employed to study interaction of three key extraction parameters...
October 1, 2016: International Journal of Molecular Sciences
Shadi A Esfahani, Pedram Heidari, Sun A Kim, Shuji Ogino, Umar Mahmood
Purpose: To assess optical imaging of Mesenchymal-Epithelial Transition factor (MET) for delineation and characterization of intrahepatic models of human hepatocellular carcinoma (HCC) and metastatic colorectal cancer (CRC), and thereby demonstrate its potential use in precision oncology. Materials and Methods: MET expression in human CRC and HCC was assessed in tissue microarrays. We used GE-137, a modified cyanine 5-tagged peptide for MET targeting. HepG2 and Huh-7 (HCC) and HT-29 (CRC) cells with MET overexpression, and LNCaP cells (negative control) with minimal MET expression were incubated with the probe...
2016: Theranostics
Sardar Sindhu, Nadeem Akhter, Steve Shenouda, Ajit Wilson, Rasheed Ahmad
BACKGROUND: Fetuin-A/AHSH is a novel hepatokine that acts as a vascular calcification inhibitor and as an endogenous TLR-4 ligand. Fetuin-A may act as a positive or negative acute phase protein (APP) in disease conditions. The relationship between circulatory fetuin-A and inflammatory biomarkers in type-2 diabetes (T2D) remains controversial. Therefore, the purpose of this study was to determine the plasma fetuin-A levels in 53 T2D (BMI = 29.7 ± 4.5 kg/m(2)) and 72 non-diabetic individuals (BMI = 28...
September 26, 2016: BMC Immunology
Hongxia Fan, Ping Lv, Jing Lv, Xiaopei Zhao, Min Liu, Guangling Zhang, Hua Tang
Hepatitis B virus (HBV) infection is a major health problem worldwide. The roles of microRNAs in the regulation of HBV expression are being increasingly recognized. In this study, we found that overexpression of miR-370 suppressed HBV gene expression and replication in Huh7 cells, whereas antisense knockdown of endogenous miR-370 enhanced HBV gene expression and replication in Huh7 cells and HepG2.2.15 cells. Further, we identified the transcription factor nuclear factor IA (NFIA) as a new host target of miR-370...
September 24, 2016: Journal of Medical Virology
Dan-Qi Li, Di Wang, Le Zhou, Ling-Zhi Li, Qing-Bo Liu, Ying-Ying Wu, Jing-Yu Yang, Shao-Jiang Song, Chun-Fu Wu
In the search for biologically active compounds from the roots of Bupleurum chinense D C., phytochemical investigation of its ethanol extract led to the isolation and identification of a new 8-O-4' neolignan glucoside, saikolignanoside A (1), along with eight known lignans (2-9). Their structures were determined on the basis of IR, UV, HRESIMS, and NMR spectroscopic analyses. The antioxidant and cytotoxic effects of isolated compounds were evaluated in vitro. The isolated compounds (IC50 > 200 μM) did not display 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity...
September 21, 2016: Journal of Asian Natural Products Research
Kai Ren, Linyan Ma, Dianlong Chong, Zhirui Zhang, Can Zhou, Hao Liu, Surong Zhao
OBJECTIVE: To investigate the effects of LCL161, a Smac mimetic, on the proliferation and apoptosis in hepatocellular carcinoma cells and the underlying mechanisms. 
 METHODS: The effect of LCL161 on the cell viability of HepG2 and SMMC7721 cells was measured by MTT assay. The effect of LCL161 at lower concentrations on the proliferation in hepatocellular carcinoma (HCC) cells was detected by colony formation assay. Apoptosis was assessed by flow cytometry with PI staining...
September 28, 2016: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
Sobhi M Gomha, Mastoura M Edrees, Farag M A Altalbawy
A new series of 1,4-bis(1-(5-(aryldiazenyl)thiazol-2-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-3-yl)benzenes 3a-i were synthesized via reaction of 5,5'-(1,4-phenylene)bis(3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide) (1) with hydrazonoyl halides 2a-i. In addition, reaction of 1 with ethyl chloroacetate afforded bis-thiazolone derivative 8 as the end product. Reaction of compound 8 with methyl glyoxalate gave bis-thiazolone derivative 10. The structures of the newly synthesized compounds were established on the basis of spectroscopic evidences and their alternative syntheses...
2016: International Journal of Molecular Sciences
Kyo Bin Kang, Jung Wha Kim, Won Keun Oh, Jinwoong Kim, Sang Hyun Sung
Ziziphus jujuba, a plant in the family Rhamnaceae, is used in several Asian countries as a food and traditional medicine. Fifteen new ceanothane-type (1-15) and three new lupane-type triterpenoids (16-18) were isolated from the roots of Z. jujuba, as well as 12 previously known triterpenoids (19-30). Their structures were elucidated by 1D and 2D NMR spectroscopic and HR mass spectrometric data analysis. Compounds 12 and 13 were found to possess a rare E-ring γ-lactone structure, and 14 was assigned as the first 2,28-dinorlupane derivative isolated as a natural product...
September 23, 2016: Journal of Natural Products
Zhongnan Wu, Yubo Zhang, Li Yang, Nenghua Chen, Lin Jiang, Siqi Jiang, Guoqiang Li, Yaolan Li, Guocai Wang
Three new ent-kaurane diterpenes, 3α-angeloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (1), 3α-tigloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (2) and 3α-cinnamoyloxykaur-9(11),16-dien-19-oic acid (3), along with five known compounds (4-8), were isolated from the herbs of Wedelia prostrata (Asteraceae). The structures were determined by extensive analysis of their spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The isolated compounds were evaluated for their cytotoxic activity on human hepatocellular carcinoma HepG2 cells...
September 7, 2016: Journal of Natural Medicines
Jignesh Lunagariya, Shenghui Zhong, Jianwei Chen, Defa Bai, Poonam Bhadja, Weili Long, Xiaojian Liao, Xiaoli Tang, Shihai Xu
Herein, we report design and synthesis of novel 26 galaxamide analogues with N-methylated cyclo-pentapeptide, and their in vitro anti-tumor activity towards the panel of human tumor cell line, such as, A549, A549/DPP, HepG2 and SMMC-7721 using MTT assay. We have also investigated the effect of galaxamide and its representative analogues on growth, cell-cycle phases, and induction of apoptosis in SMMC-7721 cells in vitro. Reckon with the significance of conformational space and N-Me aminoacid (aa) comprising this compound template, we designed the analogues with modification in N-Me-aa position, change in aa configuration from l to d aa and substitute one Leu-aa to d/l Phe-aa residue with respective to the parent structure...
September 3, 2016: Marine Drugs
Dian Yin, Yilang Wang, Wenli Sai, Liang Zhang, Yajun Miao, Lili Cao, Xiaolu Zhai, Xiu Feng, Li Yang
Hepatitis B virus (HBV) X protein (HBx) plays a key role in the initiation and progression of HBV infection‑induced hepatocellular carcinoma (HCC). Oncogenic microRNA-21 (miR-21) can be modulated by HBx protein in HCC. However, critical regulator genes in the pathway of HBx-induced miR-21 in HCC remain unclear. This study aimed to investigate the role of HBx-induced miR-21 in the apoptosis of HCC cells. In the study, interleukin-12 (IL-12) was demonstrated as a direct target of miR-21 by dual‑luciferase report assay, and miR-21 was highly expressed in HCC cells (HepG2 and HepG2 2...
October 2016: Oncology Reports
Manikankana Bandopadhyay, Neelakshi Sarkar, Sibnarayan Datta, Dipanwita Das, Ananya Pal, Rajesh Panigrahi, Arup Banerjee, Chinmay K Panda, Chandrima Das, Shekhar Chakrabarti, Runu Chakravarty
BACKGROUND: Hepatitis B virus (HBV) X protein (HBx) reported to be associated with pathogenesis of hepatocellular carcinoma (HCC) and miR-122 expression is down regulated in HCC. Previous studies reported miR-122 targets cyclin G1 (CCNG1) expression and this in turn abolishes p53-mediated inhibition of HBV replication. Here we investigated the involvement of HBx protein in the modulation of miR-122 expression in hepatoblastoma cells. METHODS: Expression of miR-122 was measured in HepG2 cells transfected with HBx plasmid (HBx-HepG2), full length HBV genome (HBV-HepG2) and in constitutively HBV synthesizing HepG2...
2016: Infectious Agents and Cancer
Fabiana Roberta Segura, Emilene Arusievicz Nunes, Fernanda Pollo Paniz, Ana Carolina Cavalheiro Paulelli, Gabriela Braga Rodrigues, Gilberto Úbida Leite Braga, Walter Dos Reis Pedreira Filho, Fernando Barbosa, Giselle Cerchiaro, Fábio Ferreira Silva, Bruno Lemos Batista
On November 5th, 2015, Samarco's iron mine dam - called Fundão - spilled 50-60 million m(3) of mud into Gualaxo do Norte, a river that belongs to Rio Doce Basin. Approximately 15 km(2) were flooded along the rivers Gualaxo do Norte, Carmo and Doce, reaching the Atlantic Ocean on November 22nd, 2015. Six days after, our group collected mud, soil and water samples in Bento Rodrigues (Minas Gerais, Brazil), which was the first impacted area. Overall, the results, water samples - potable and surface water from river - presented chemical elements concentration according to Brazilian environmental legislations, except silver concentration in surface water that ranged from 1...
November 2016: Environmental Pollution
Z Q Lyu, X Xie, Y B Ke
OBJECTIVE: To explore the potential effects of long-term and low-dose Di- (2-ethylhexyl) phthalate (DEHP) exposure on whole genome DNA methylation status and cytotoxicity of HePG2 cells. METHODS: HePG2 cells were exposed to 1.5、15.0 and 150.0 μmol/L DEHP for 24 hours, after continuous exposure for 20 generations, mRNA and protein expression level of DNA (cytosine-5) -methyltransferase 1 (DNMT 1) , whole genome DNA methylation, cell apoptosis levels and cell cycle were determined in both DEHP exposed cells and control cells...
May 20, 2016: Chinese Journal of Industrial Hygiene and Occupational Diseases
Nadine Al Alam, Sawsan Ibrahim Kreydiyyeh
Sphingosine-1-phosphate (S1P) was found previously to inhibit Na(+)-K(+) ATPase in HepG2 cells. Whether fingolimod (FTY720), a S1P receptor (S1PR) agonist, similarly inhibits the ATPase is a question that needs to be addressed. The aim of this work was to study the effect of FTY720P, the active form of the drug, on the activity of Na(+)-K(+) ATPase in HepG2 cells and determine its mechanism of action. The activity of the ATPase was assayed by measuring the amount of inorganic phosphate liberated in the presence and the absence of ouabain...
August 2016: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
Ladan Pourabdi, Mehdi Khoobi, Hamid Nadri, Alireza Moradi, Farshad Homayouni Moghadam, Saeed Emami, Mohammad M Mojtahedi, Ismaeil Haririan, Hamid Forootanfar, Alieh Ameri, Alireza Foroumadi, Abbas Shafiee
A series of tacrine-based pyrazolo[4',3':5,6]pyrano[2,3-b]quinolines and related compounds were designed and synthesized for targeting AChE, BuChE and 15-LOX enzymes in the field of Alzheimer's disease therapy. Most of compounds showed potent activity against cholinesterases and mild potency toward 15-LOX enzyme. In particular, compounds 29, 32 and 40 displayed inhibition at nano-molar level against AChE and BuChE (IC50s = 0.005-0.08 μM), being more potent than reference drug tacrine. Moreover, compound 32 with IC50 value of 31 μM was the most potent compound against 15-LOX...
November 10, 2016: European Journal of Medicinal Chemistry
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