scholarly journals Synthesis, Characterization, and In Vitro Insulin-Mimetic Activity Evaluation of Valine Schiff Base Coordination Compounds of Oxidovanadium(V)

Biomedicines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 562
Author(s):  
Mihaela Turtoi ◽  
Maria Anghelache ◽  
Andrei A. Patrascu ◽  
Catalin Maxim ◽  
Ileana Manduteanu ◽  
...  
Keyword(s):  
Schiff Base ◽  
Hepatoma Cell ◽  
Tyrosine Phosphatase ◽  
High Capacity ◽  
Hepatoma Cell Line ◽  
Human Hepatoma Cell ◽  
Biologically Relevant ◽  
Insulin Mimetic ◽  
Global Health Issue

Type 2 diabetes became an alarming global health issue since the existing drugs do not prevent its progression. Herein, we aimed to synthesize and characterize a family of oxidovanadium(V) complexes with Schiff base ligands derived from L-/D-valine (val) and salicylaldehyde (sal) or o-vanillin (van) as insulin-mimetic agents and to assess their potential anti-diabetic properties. Two new oxidovanadium(V) complexes, [{VVO(R-salval)(H2O)}(μ2-O){VVO(R-salval)}] and [{VVO(R-vanval)(CH3OH)}2(μ2-O)], and their S-enantiomers were synthesized and characterized. The compounds exhibit optical activity as shown by crystallographic and spectroscopic data. The stability, the capacity to bind bovine serum albumin (BSA), the cytotoxicity against human hepatoma cell line, as well as the potential anti-diabetic activity of the four compounds are investigated. The synthesized compounds are stable for up to three hours in physiological conditions and exhibit a high capacity of binding to BSA. Furthermore, the synthesized compounds display cytocompatibility at biologically relevant concentrations, exert anti-diabetic potential and insulin-mimetic activities by inhibiting the α-amylase and protein tyrosine phosphatase activity, and a long-term increase of insulin receptor phosphorylation compared to the insulin hormone. Thus, the in vitro anti-diabetic potential and insulin-mimetic properties of the newly synthesized oxidovanadium(V) compounds, correlated with their cytocompatibility, make them promising candidates for further investigation as anti-diabetic drugs.

scholarly journals Pyrrolizidine Alkaloids Induce Cell Death in Human HepaRG Cells in a Structure-Dependent Manner

2020 ◽  
Vol 22 (1) ◽  
pp. 202
Author(s):  
Josephin Glück ◽  
Julia Waizenegger ◽  
Albert Braeuning ◽  
Stefanie Hessel-Pras
Keyword(s):  
Cell Death ◽  
Cell Viability ◽  
Pyrrolizidine Alkaloids ◽  
Defense Mechanism ◽  
Hepatoma Cell ◽  
Hepatoma Cell Line ◽  
Dependent Manner ◽  
Human Hepatoma Cell

Pyrrolizidine alkaloids (PAs) are a group of secondary metabolites produced in various plant species as a defense mechanism against herbivores. PAs consist of a necine base, which is esterified with one or two necine acids. Humans are exposed to PAs by consumption of contaminated food. PA intoxication in humans causes acute and chronic hepatotoxicity. It is considered that enzymatic PA toxification in hepatocytes is structure-dependent. In this study, we aimed to elucidate the induction of PA-induced cell death associated with apoptosis activation. Therefore, 22 structurally different PAs were analyzed concerning the disturbance of cell viability in the metabolically competent human hepatoma cell line HepaRG. The chosen PAs represent the main necine base structures and the different esterification types. Open-chained and cyclic heliotridine- and retronecine-type diesters induced strong cytotoxic effects, while treatment of HepaRG with monoesters did not affect cell viability. For more detailed investigation of apoptosis induction, comprising caspase activation and gene expression analysis, 14 PA representatives were selected. The proapoptotic effects were in line with the potency observed in cell viability studies. In vitro data point towards a strong structure–activity relationship whose effectiveness needs to be investigated in vivo and can then be the basis for a structure-associated risk assessment.

scholarly journals In Vitro Cytotoxicity of Oleanolic/Ursolic Acids-Loaded in PLGA Nanoparticles in Different Cell Lines

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 362 ◽  
Author(s):  
Amélia M. Silva ◽  
Helen L. Alvarado ◽  
Guadalupe Abrego ◽  
Carlos Martins-Gomes ◽  
Maria L. Garduño-Ramirez ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cell Line ◽  
Cell Lines ◽  
Specific Activity ◽  
Polymeric Nanoparticles ◽  
Hepatoma Cell ◽  
Plga Nanoparticles ◽  
Hepatoma Cell Line ◽  
Human Hepatoma Cell

Oleanolic (OA) and ursolic (UA) acids are recognized triterpenoids with anti-cancer properties, showing cell-specific activity that can be enhanced when loaded into polymeric nanoparticles. The cytotoxic activity of OA and UA was assessed by Alamar Blue assay in three different cell lines, i.e., HepG2 (Human hepatoma cell line), Caco-2 (Human epithelial colorectal adenocarcinoma cell line) and Y-79 (Human retinoblastoma cell line). The natural and synthetic mixtures of these compounds were tested as free and loaded in polymeric nanoparticles in a concentration range from 2 to 32 µmol/L. The highest tested concentrations of the free triterpene mixtures produced statistically significant cell viability reduction in HepG2 and Caco-2 cells, compared to the control (untreated cells). When loaded in the developed PLGA nanoparticles, no differences were recorded for the tested concentrations in the same cell lines. However, in the Y-79 cell line, a decrease on cell viability was observed when testing the lowest concentration of both free triterpene mixtures, and after their loading into PLGA nanoparticles.

scholarly journals In vivo and in vitro regulation of erythropoietin mRNA: measurement by competitive polymerase chain reaction

Blood ◽  
1993 ◽  
Vol 81 (3) ◽  
pp. 617-623 ◽  
Author(s):  
J Fandrey ◽  
HF Bunn
Keyword(s):  
Polymerase Chain Reaction ◽  
Hepatoma Cell ◽  
Hepatoma Cell Line ◽  
Mrna Levels ◽  
Chain Reaction ◽  
Human Hepatoma Cell ◽  
Competitive Polymerase Chain Reaction ◽  
Polymerase Chain

Abstract The regulation of erythropoietin (Epo) production was investigated by competitive polymerase chain reaction, a highly sensitive and accurate means of measuring Epo mRNA levels. Co-amplification of the test sample with added mutant Epo cDNA template corrects for variability in the efficiency of amplification. Epo mRNA levels were determined in tissues of normal rats and in animals with varying degrees of anemia. Reduction of the hematocrit level from 0.40 to 0.15–0.20 resulted in a 300-fold increase in kidney Epo mRNA, which comprised 80% of the total Epo mRNA versus 20% from the liver. In contrast, very low levels detected in lung and spleen were not significantly increased by anemia. The human hepatoma cell line, Hep3B, secretes high levels of Epo in response to hypoxia. This regulation is, to a large extent, transcriptional. When Hep3B cells were incubated in the presence of decreasing O2 tension from 160 to 7 mm Hg, there was a monotonic increase in Epo mRNA to 50 to 100 times the normoxic level. Hyperoxia did not suppress basal expression. When cells were incubated at a PO2 of 7 mm Hg, induction of Epo mRNA was first noted at 30 minutes and was maximal at 5 to 6 hours. After Epo mRNA was boosted by a 4-hour hypoxic incubation, cells were then exposed to normoxia, which shut off further transcription of the Epo gene. The decay of Epo mRNA levels closely followed first order kinetics with a half-life of 2 hours, an effective measurement of message stability.

Comparative Evaluation of Different Membranes for the Construction of an Artificial Liver Support System

1997 ◽  
Vol 20 (2) ◽  
pp. 119-124 ◽  
Author(s):  
S. Qiang ◽  
Y. Yaoting ◽  
L. Hongyin ◽  
H. Klinkmann
Keyword(s):  
Hepatoma Cell ◽  
Hepatoma Cell Line ◽  
Artificial Liver ◽  
Human Hepatoma Cell ◽  
Liver Support ◽  
Artificial Liver Support ◽  
Liver Support System ◽  
Extracorporeal Liver Support ◽  
Hepatocyte Growth

During the past decades, many technological improvements have been made in the construction of extracorporeal liver support systems. Among these achievements, membranes of artificial capillary system, used as substrates of hepatocyte growth, aroused our interest in their application for the construction of bioreactors. The present paper studied the comparison of hepatocyte growth and function on six different membranes. Four of them are cellulose based membranes, Cuprophan, Hemophan, Cellulose acetate, and Bioflux; two are synthetic polymer SPAN and Polysulphone. Human hepatoma cell line SMMC-7721, with moderately differentiated hepatocyte-specific functions, was inoculated into the hollow fiber cartridges. These cells were allowed to attach and to grow over these membranes. It was found that there existed differences in hepatocyte immobilization and growth among these membranes. They influenced the growth and functions of hepatoma cells in vitro to some extent. These results show that membrane is an important factor in the construction of capillary membrane bioreactors for artificial liver support.

scholarly journals Cell Clones Selected from the Huh7 Human Hepatoma Cell Line Support Efficient Replication of a Subgenomic GB Virus B Replicon

2002 ◽  
Vol 76 (15) ◽  
pp. 7736-7746 ◽  
Author(s):  
Amedeo De Tomassi ◽  
Maura Pizzuti ◽  
Rita Graziani ◽  
Andrea Sbardellati ◽  
Sergio Altamura ◽  
...  
Keyword(s):  
Host Cell ◽  
Cell Line ◽  
Hepatoma Cell ◽  
Hepatoma Cell Line ◽  
Human Hepatoma ◽  
Human Hepatoma Cell ◽  
Subgenomic Rna ◽  
Human Hepatoma Cell Line ◽  
Huh7 Cells

ABSTRACT Tamarins (Saguinus species) infected by GB virus B (GBV-B) have recently been proposed as an acceptable surrogate model for hepatitis C virus (HCV) infection. The availability of infectious genomic molecular clones of both viruses will permit chimeric constructs to be tested for viability in animals. Studies in cells with parental and chimeric constructs would also be very useful for both basic research and drug discovery. For this purpose, a convenient host cell type supporting replication of in vitro-transcribed GBV-B RNA should be identified. We constructed a GBV-B subgenomic selectable replicon based on the sequence of a genomic molecular clone proved to sustain infection in tamarins. The corresponding in vitro-transcribed RNA was used to transfect the Huh7 human hepatoma cell line, and intracellular replication of transfected RNA was shown to occur, even though in a small percentage of transfected cells, giving rise to antibiotic-resistant clones. Sequence analysis of GBV-B RNA from some of those clones showed no adaptive mutations with respect to the input sequence, whereas the host cells sustained higher GBV-B RNA replication than the original Huh7 cells. The enhancement of replication depending on host cell was shown to be a feature common to the majority of clones selected. The replication of GBV-B subgenomic RNA was susceptible to inhibition by known inhibitors of HCV to a level similar to that of HCV subgenomic RNA.

scholarly journals Hepatitis C virus infection of human hepatoma cell line 7721 in vitro

2001 ◽  
Vol 7 (5) ◽  
pp. 685 ◽  
Author(s):  
Zhi-Qiang Song ◽  
Fei Hao ◽  
Feng Min ◽  
Qiao-Yu Ma ◽  
Guo-Dong Liu
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Virus Infection ◽  
Cell Line ◽  
Hepatoma Cell ◽  
Hepatoma Cell Line ◽  
Human Hepatoma ◽  
Hepatitis C Virus Infection ◽  
Human Hepatoma Cell

Two New Oxovanadium(IV) Compounds Containing Amino Acid Schiff Base and 1,10-Bathophenanthroline Ligands: Syntheses, Crystal Structures, and In Vitro Evaluation of the Anticancer Activities

2017 ◽  
Vol 70 (5) ◽  
pp. 608 ◽  
Author(s):  
Yaping Cao ◽  
Hongmei Liu ◽  
Zeli Yuan ◽  
Gang Wei
Keyword(s):  
Schiff Base ◽  
Anticancer Agents ◽  
High Resolution Mass Spectrometry ◽  
Hepatoma Cell ◽  
A549 Cells ◽  
Molar Conductance ◽  
Anticancer Activities ◽  
Human Hepatoma Cell ◽  
Ic50 Values

Two new oxovanadium(iv) compounds containing 1,10-bathophenanthroline (Bphen) and amino Schiff base derivatives [VO(hnd-napha)(Bphen)] (1) and [VO(o-van-met)(Bphen)] (2) were synthesised (where hnd-napha and o-van-met are N-Schiff bases derived from the reaction of 2-hydroxy-1-naphthaldehyde with 3-(1-naphthyl)-l-alanine and o-vanillin with l-methionine, respectively). These compounds were characterised by elemental analysis, infrared spectroscopy, high-resolution mass spectrometry, and single-crystal X-ray diffraction (XRD). Both compounds showed low molar conductance values, indicating that they are non-electrolytes. The XRD results showed that the VIV atoms in both compounds existed in the VO3N3 coordination geometry with Schiff base and Bphen ligands. The in vitro anticancer activities of compounds 1 and 2 were evaluated against A549 human lung carcinoma and HepG2 human hepatoma cell lines using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and the results revealed that both compounds were cytotoxic with half maximal inhibitory concentration (IC50) values in the range of 8.22 ± 1.0 to 94.89 ± 3.2 μmol L−1. Notably, compound 2 exhibited much better anticancer activity in vitro against A549 cells (8.22 ± 1 μmol L−1) than [VO(acac)2] (24 ± 6 μmol L−1) or any of our previously reported oxovanadium(iv) compounds, making it comparable in activity to cisplatin (3.1 ± 0.5 μmol L−1). These results therefore suggest that compound 2 could be used as a promising lead for the development of anticancer agents for the treatment of lung cancer.

Sign in / Sign up

Export Citation Format

Share Document