Hempseed (Cannabis sativa) Peptides WVSPLAGRT and IGFLIIWV Exert Anti-inflammatory Activity in the LPS-Stimulated Human Hepatic Cell Line

2022 ◽  
Author(s):  
Ivan Cruz-Chamorro ◽  
Guillermo Santos-Sánchez ◽  
Carlotta Bollati ◽  
Martina Bartolomei ◽  
Jianqiang Li ◽  
...  
Keyword(s):  
Cell Line ◽  
Cannabis Sativa ◽  
Hepatic Cell ◽  
Inflammatory Activity ◽  
Hepatic Cell Line ◽  
Anti Inflammatory

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.

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

Cadmium disorganises the scaffolding of gap and tight junction proteins in the hepatic cell line WIF B9

2013 ◽  
Vol 105 (12) ◽  
pp. 561-575 ◽  
Author(s):  
Sylviane Boucherie ◽  
Catherine Decaens ◽  
Jean-Marc Verbavatz ◽  
Brigitte Grosse ◽  
Marie Erard ◽  
...  
Keyword(s):  
Tight Junction ◽  
Cell Line ◽  
Hepatic Cell ◽  
Tight Junction Proteins ◽  
Hepatic Cell Line ◽  
Junction Proteins

scholarly journals A dual mixture of persistent organic pollutants modifies carbohydrate metabolism in the human hepatic cell line HepaRG

2019 ◽  
Vol 178 ◽  
pp. 108628 ◽  
Author(s):  
Alix F. Leblanc ◽  
Eléonore A. Attignon ◽  
Emilie Distel ◽  
Spyros P. Karakitsios ◽  
Dimosthenis A. Sarigiannis ◽  
...  
Keyword(s):  
Carbohydrate Metabolism ◽  
Cell Line ◽  
Organic Pollutants ◽  
Persistent Organic Pollutants ◽  
Hepatic Cell ◽  
Hepatic Cell Line

HPLC–MS/MS methods for the quantitative analysis of ophthalmic acid in rodent plasma and hepatic cell line culture medium

2011 ◽  
Vol 54 (5) ◽  
pp. 1128-1135 ◽  
Author(s):  
Suzanne Geenen ◽  
Filippos Michopoulos ◽  
J. Gerry Kenna ◽  
Kyle L. Kolaja ◽  
Hans. V. Westerhoff ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Cell Line ◽  
Culture Medium ◽  
Hepatic Cell ◽  
Hepatic Cell Line

Cu isotope fractionation response to oxidative stress in a hepatic cell line studied using multi-collector ICP-mass spectrometry

2018 ◽  
Vol 410 (9) ◽  
pp. 2385-2394 ◽  
Author(s):  
María R. Flórez ◽  
Marta Costas-Rodríguez ◽  
Charlotte Grootaert ◽  
John Van Camp ◽  
Frank Vanhaecke
Keyword(s):  
Oxidative Stress ◽  
Mass Spectrometry ◽  
Cell Line ◽  
Isotope Fractionation ◽  
Hepatic Cell ◽  
Hepatic Cell Line ◽  
Icp Mass Spectrometry ◽  
Cu Isotope

scholarly journals A New Bithiophene from the Root of Echinops grijsii

2015 ◽  
Vol 10 (12) ◽  
pp. 1934578X1501001 ◽  
Author(s):  
Fang-Pin Chang ◽  
Chien-Chih Chen ◽  
Hui-Chi Huang ◽  
Sheng-Yang Wang ◽  
Jih-Jung Chen ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Cell Line ◽  
Natural Source ◽  
Inflammatory Activity ◽  
Raw 264.7 ◽  
Raw 264.7 Cell ◽  
Anti Inflammatory ◽  
First Time ◽  
Raw 264.7 Cell Line

A new bithiophene, 5-(4-hydroxy-3-methoxy-1-butyny)-2,2′-bithiophene (1), and sixteen known thiophenes: 2-(3,4-dihydroxybut-1-ynyl)-5-(penta-1,3-diynyl)thiophene (2), α-terthienyl (3), 5-(3,4-dihydroxybut-1-ynyl)-2,2′-bithiophene (4), 5-acetyl-2,2′-bithiophene (5), 5-formyl-2,2′-bithiophene (6), methyl 2,2′-bithiophene-5-carboxylate (7), 5-(but-3-en-1-ynyl)-2,2′-bithiophene (8), 5-(4-isovaleroyloxybut-1-ynyl)-2,2′-bithiophene (9), cardopatine (10), isocardopatine (11), 5-(3-hydroxy-4-isovaleroyloxybut-1-ynyl)-2,2′-bithiophene (12), 5-(3-hydroxymethyl-3-isovaleroyloxyprop-1-ynyl)-2,2′-bithiophene (13), 5-(4-hydroxy-1-butynyl)-2,2′-bithiophene (14), 5-(4-acetoxy-1-butynl)-2,2′-bithiophene (15), 2,2′-bithiophene-5-carboxylic acid (16) and 2-(4-hydroxybut-1-ynyl)-5-(penta-1,3-diynyl)thiophene (17) were isolated from the roots of Echinops grijisii Hance. Among them, compounds 6, 7 and 16 were isolated from a natural source for the first time. Compounds 2, 4 and 14 exhibited significant anti-inflammatory activity against nitrite of LPS-stimulated production in the RAW 264.7 cell line.

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