scholarly journals Cystathionine β-synthase-derived hydrogen sulfide regulates lipopolysaccharide-induced apoptosis of the BRL rat hepatic cell line in vitro

2012 ◽  
Vol 4 (5) ◽  
pp. 832-838 ◽  
Author(s):  
JUN YAN ◽  
FEIXIANG TENG ◽  
WEIWEI CHEN ◽  
YINGLEI JI ◽  
ZHENYONG GU
Keyword(s):  
Hydrogen Sulfide ◽  
Cell Line ◽  
Hepatic Cell ◽  
Hepatic Cell Line ◽  
Induced Apoptosis

Synthesis, Characterization and In vitro Evaluation of N-Substituted- Sulfomoyl-Phenyl-Amino Carboxylic Acid Derivatives as Squalene Synthase Inhibitors

2019 ◽  
Vol 15 (4) ◽  
pp. 415-426
Author(s):  
Avani B. Chokshi ◽  
Mahesh T. Chhabria ◽  
Pritesh R. Desai
Keyword(s):  
Carboxylic Acid ◽  
Cell Line ◽  
Hepatic Cell ◽  
Squalene Synthase ◽  
Lipid Lowering ◽  
Assay Method ◽  
Aromatic Substituent ◽  
Hepatic Cell Line ◽  
Amino Carboxylic Acid

Background:Squalene Synthase is one of the cholesterol biosynthetic pathway enzymes, inhibition of which produces potent lipid lowering action. A variety of chemical classes have been evaluated for its inhibition to provide alternate antihyperlipidemic agents to statins.Methods:A series of N-substituted-sulfomoyl-phenyl-amino carboxylic acid derivatives were designed through pharmacophore modelling as Squalene Synthase inhibitors. We report here the synthesis, characterization and in vitro pharmacological screening of the designed molecules as Squalene synthase inhibitors. The target molecules were synthesized by a simple procedure and each molecule was characterized by IR, Mass, 1HNMR and 13CNMR spectroscopic techniques. As a primary site of action for cholesterol biosynthesis is liver, each of the molecules were first screened for in vitro cytotoxicity over human hepatic cell line (HepG2) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. The enzyme inhibition assay was performed on cell lysates prepared from HepG2 cells by Human Squalene Synthase ELISA kit, where test compounds were added in the nontoxic concentrations only.Results:Compound 5f was found to be most potent with the IC50 value of 11.91 µM. The CTC50 value for 5f on human hepatic cell line was > 1000 µM so it was considered that the compound was relatively safe and might be free of hepatotoxicity.Conclusion:From the results of our studies, it was observed that compounds with poly nuclear aromatic or hetero aromatic substituent on a side chain were more potent enzyme inhibitors and a distance of 4-5 atoms is optimum between amide nitrogen and hydroxyl group of carboxylic acid.

HepaRG human hepatic cell line utility as a surrogate for primary human hepatocytes in drug metabolism assessment in vitro

2011 ◽  
Vol 63 (1) ◽  
pp. 59-68 ◽  
Author(s):  
Marc Lübberstedt ◽  
Ursula Müller-Vieira ◽  
Manuela Mayer ◽  
Klaus M. Biemel ◽  
Fanny Knöspel ◽  
...  
Keyword(s):  
Drug Metabolism ◽  
Cell Line ◽  
Hepatic Cell ◽  
Human Hepatocytes ◽  
Primary Human Hepatocytes ◽  
Hepatic Cell Line

scholarly journals Spontaneous germline potential of human hepatic cell line in vitro

2012 ◽  
Vol 19 (4) ◽  
pp. 216-226 ◽  
Author(s):  
Zhan Ma ◽  
Ruilai Liu ◽  
Xiaojin Wang ◽  
Mingying Huang ◽  
Quan Gao ◽  
...  
Keyword(s):  
Cell Line ◽  
Hepatic Cell ◽  
Hepatic Cell Line

scholarly journals Cyanamide Potentiates the Ethanol-Induced Impairment of Receptor-Mediated Endocytosis in a Recombinant Hepatic Cell Line Expressing Alcohol Dehydrogenase Activity

2012 ◽  
Vol 2012 ◽  
pp. 1-5
Author(s):  
Dahn L. Clemens ◽  
Dean J. Tuma ◽  
Carol A. Casey
Keyword(s):  
Alcohol Dehydrogenase ◽  
Cell Line ◽  
Aldehyde Dehydrogenase ◽  
Hepatic Cell ◽  
Asialoglycoprotein Receptor ◽  
Ethanol Metabolism ◽  
Ethanol Administration ◽  
Receptor Mediated Endocytosis ◽  
Hepatic Cell Line

Ethanol administration has been shown to alter receptor-mediated endocytosis in the liver. We have developed a recombinant hepatic cell line stably transfected with murine alcohol dehydrogenase cDNA to serve as anin vitromodel to investigate these ethanol-induced impairments. In the present study, transfected cells were maintained in the absence or presence of 25 mM ethanol for 7 days, and alterations in endocytosis by the asialoglycoprotein receptor were determined. The role of acetaldehyde in this dysfunction was also examined by inclusion of the aldehyde dehydrogenase inhibitor, cyanamide. Our results showed that ethanol metabolism impaired internalization of asialoorosomucoid, a ligand for the asialoglycoprotein receptor. The addition of cyanamide potentiated the ethanol-induced defect in internalization and also impaired degradation of the ligand in the presence of ethanol. These results indicate that the ethanol-induced impairment in endocytosis is exacerbated by the inhibition of aldehyde dehydrogenase, suggesting the involvement of acetaldehyde in this dysfunction.

Chemical and biological insights into uranium-induced apoptosis of rat hepatic cell line

2015 ◽  
Vol 54 (2) ◽  
pp. 207-216 ◽  
Author(s):  
Fang Liu ◽  
Ke-Jie Du ◽  
Zhen Fang ◽  
Yong You ◽  
Ge-Bo Wen ◽  
...  
Keyword(s):  
Cell Line ◽  
Hepatic Cell ◽  
Hepatic Cell Line ◽  
Induced Apoptosis

Phagocytic uptake and ROS-mediated cytotoxicity in human hepatic cell line of amphiphilic polyphosphazene nanoparticles

2012 ◽  
Vol 101A (1) ◽  
pp. 285-297 ◽  
Author(s):  
Liyan Qiu ◽  
Yue Chen ◽  
Menghua Gao ◽  
Cheng Zheng ◽  
Qinghe Zhao
Keyword(s):  
Cell Line ◽  
Hepatic Cell ◽  
Hepatic Cell Line ◽  
Phagocytic Uptake

Novel Peptides Inhibit Zika NS2B-NS3 Serine Protease and Virus Replication in Human Hepatic Cell Line

2019 ◽  
Vol 25 (4) ◽  
pp. 1659-1668 ◽  
Author(s):  
Ammar Yasir Abdulrahman ◽  
Ahmad S. Khazali ◽  
Teow Chong Teoh ◽  
Hussin A. Rothan ◽  
Rohana Yusof
Keyword(s):  
Cell Line ◽  
Serine Protease ◽  
Virus Replication ◽  
Hepatic Cell ◽  
Hepatic Cell Line
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