scholarly journals Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines

2016 ◽  
Vol 11 (6) ◽  
pp. 3917-3924 ◽  
Author(s):  
XIAO-MENG CHEN ◽  
MENG ZHANG ◽  
PENG-LI FAN ◽  
YU-HUA QIN ◽  
HONG-WEI ZHAO
Keyword(s):  
Cell Lines ◽  
Renal Cancer ◽  
Hek 293 ◽  
Chelerythrine Chloride

New Spirocyclic Hydroxamic Acids as Effective Antiproliferative Agents

2020 ◽  
Vol 20 ◽  
Author(s):  
Margarita E. Neganova ◽  
Sergey G. Klochkov ◽  
Yulia R. Aleksandrova ◽  
Vladimir N. Osipov ◽  
Dmitry V. Avdeev ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Histone Deacetylase ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antioxidant Activities ◽  
Hydroxamic Acids ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Hek 293 ◽  
Underlying Mechanisms

Aims: The main goal of this work where is to synthesize new original spirocyclic hydroxamic acids, investigate their cytotoxicity against to the panel of tumor cell lines and possible mechanism of action of these active compounds. Background: Hydroxamic acids are one of the promising classes of chemical compounds with proven has anticancer potential properties. This is manifested in the presence of metal chelating and antioxidant activities, the ability to inhibit histone deacetylase enzymes and a chemosensitizing effect against well known cytostatics. Objective: Original spirocyclic hydroxamic acids were synthesized and spectrums of their antiproliferative activities were investigated. Methods: The cytotoxic activities on different tumor lines (SH-SY5Y, HeLa and healthy cells HEK-293) were investigated and determined possible underlying mechanisms of their activity. Result: New original spirocyclic hydroxamic acids were synthesized. These compounds exhibit antiproliferative properties against of the various tumor cultures cells and also exhibits antioxidant activity, a depolarizing effect on the mitochondrial membrane, inhibit the activity of the histone deacetylase enzyme, and also decrease of basal glycolysis and glycolytic capacity reserve of HeLa and SH-SY5Y tumor cell lines. Conclusion: The most promising are compounds 5j-l containing two chlorine atoms as substituents in the quinazoline part of the molecule and hydroxamate function. Therefore, these compounds can be considered as hit compounds for the development on their basis multi-target anticancer agents.

scholarly journals Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening

2019 ◽  
Vol 25 (1) ◽  
pp. 9-20 ◽  
Author(s):  
Olivia W. Lee ◽  
Shelley Austin ◽  
Madison Gamma ◽  
Dorian M. Cheff ◽  
Tobie D. Lee ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
High Throughput ◽  
High Throughput Screening ◽  
Drug Targets ◽  
Large Scale ◽  
Early Stage ◽  
Cancer Cell Line ◽  
Hek 293 ◽  
Cytotoxic Compounds

Cell-based phenotypic screening is a commonly used approach to discover biological pathways, novel drug targets, chemical probes, and high-quality hit-to-lead molecules. Many hits identified from high-throughput screening campaigns are ruled out through a series of follow-up potency, selectivity/specificity, and cytotoxicity assays. Prioritization of molecules with little or no cytotoxicity for downstream evaluation can influence the future direction of projects, so cytotoxicity profiling of screening libraries at an early stage is essential for increasing the likelihood of candidate success. In this study, we assessed the cell-based cytotoxicity of nearly 10,000 compounds in the National Institutes of Health, National Center for Advancing Translational Sciences annotated libraries and more than 100,000 compounds in a diversity library against four normal cell lines (HEK 293, NIH 3T3, CRL-7250, and HaCat) and one cancer cell line (KB 3-1, a HeLa subline). This large-scale library profiling was analyzed for overall screening outcomes, hit rates, pan-activity, and selectivity. For the annotated library, we also examined the primary targets and mechanistic pathways regularly associated with cell death. To our knowledge, this is the first study to use high-throughput screening to profile a large screening collection (>100,000 compounds) for cytotoxicity in both normal and cancer cell lines. The results generated here constitute a valuable resource for the scientific community and provide insight into the extent of cytotoxic compounds in screening libraries, allowing for the identification and avoidance of compounds with cytotoxicity during high-throughput screening campaigns.

Sulforaphane as an adjunctive to everolimus counteracts everolimus resistance in renal cancer cell lines

Phytomedicine ◽  
2017 ◽  
Vol 27 ◽  
pp. 1-7 ◽  
Author(s):  
Eva Juengel ◽  
Stephanie Euler ◽  
Sebastian Maxeiner ◽  
Jochen Rutz ◽  
Saira Justin ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Renal Cancer ◽  
Cancer Cell Lines ◽  
Renal Cancer Cell

scholarly journals Evaluation of cytotoxic profile of hydroalcoholic extract of fruit rinds of Garcinia pedunculata on human embryonic kidney and breast carcinoma cells

2020 ◽  
Vol 9 (2) ◽  
pp. 259
Author(s):  
Sukrant Sharma ◽  
Ravi Mundugaru ◽  
Pradeepa H. Dakappa ◽  
Pundalik R. Naik
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
Metastatic Breast ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Alcoholic Extract ◽  
Human Embryonic Kidney ◽  
Hek 293

Background: The fruit rinds of Garcinia pedunculata has potential medicinal properties and used in many chronic ailments. It has been demonstrated that cytoprotective effects in various experimental research works. But its cytotoxic effect has not been evaluated. The present study was aimed to screen its relative cytotoxic effect on normal and cancer cell lines.Methods: In the present study, the cytotoxic effect of hydro alcoholic extract of Garcinia pedunculata was evaluated on normal human embryonic kidney (HEK-293) and M.D. Anderson metastatic breast cancer cell lines (MDA-MB 231) using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay.Results: Higher dose level of hydro alcoholic extract of Garcinia pedunculata (HAGP) (500 μg/ml) has shown considerable increase (112.503) in the percentage viability of HEK-29 whereas; there is a remarkable decrease in the viable cell population (77.490) in MDA-MB 231.Conclusions: Based on the observed results we could conclude that HAGP has potential cytotoxic effect on the cancer cell line without altering the normal cell growth and proliferation. Thus it has potential to develop as a safer chemotherapeutic agent. Further detailed exploration is required to confirm its therapeutic efficacy in different cancer cell lines.

scholarly journals Antioxidant and cytotoxic studies of Acacia nilotica twig extract and their green synthesized silver nanoparticles

2020 ◽  
Vol 9 (2) ◽  
pp. 975-980 ◽  
Keyword(s):  
Antioxidant Activity ◽  
Silver Nanoparticles ◽  
Cell Lines ◽  
Antioxidant Activities ◽  
Reducing Power ◽  
Acacia Nilotica ◽  
Total Phenolic ◽  
Hek 293 ◽  
Selected Area Electron Diffraction ◽  
Wide Range

Acacia nilotica (L.) Delile is well known as “Desi Kikar”or Babul in India that possesses a wide range of pharmacological activities. In the present study, Acacia nilotica twig extract and its synthesized silver nanoparticles (AgNPs) were evaluated for total phenolic content (TPC), antioxidant activity and cytotoxic effects. Characterization of AgNPs was done by UV-Visible spectroscopy, Fourier-transform infrared spectroscopy (FTIR), Transmission electron microscopy (TEM) and Selected area electron diffraction (SAED) techniques. Antioxidant potential was determined using different assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), reducing power and β-carotene linoleic acid. Cytotoxicity was tested by 3-(4,5-dimethyl-2-yl)-2,5-diphynyl tetrazolium bromide (MTT) assay on Human embryonic kidney (HEK)-293 cell lines. The results indicated that AgNPs exhibited higher antioxidant activity (81.11 %) and TPC (57.35 mg of GAE/mL of extract) as compare to plant extract. A positive correlation was observed between the TPC and antioxidant activities. The inhibitory concentration (IC50) of A. nilotica extract and AgNPs was 52.08µg/mL and 56.82µg/mL respectively. Cytotoxicity against HEK-293 cell lines was dose dependent. Accordingly, it is summarized that A. nilotica based AgNPs could serve as a potential antioxidant for therapeutic purposes.

scholarly journals Expression of 9-O- and 7,9-O-Acetyl Modified Sialic Acid in Cells and Their Effects on Influenza Viruses

mBio ◽  
2019 ◽  
Vol 10 (6) ◽  
Author(s):  
Karen N. Barnard ◽  
Brian R. Wasik ◽  
Justin R. LaClair ◽  
David W. Buchholz ◽  
Wendy S. Weichert ◽  
...  
Keyword(s):  
Cell Lines ◽  
Influenza A ◽  
A549 Cells ◽  
Sialic Acids ◽  
Influenza Viruses ◽  
Obvious Effect ◽  
Hek 293 ◽  
Chemically Modified ◽  
Modified Forms ◽  
In Cells

ABSTRACT Sialic acids (Sia) are widely displayed on the surfaces of cells and tissues. Sia come in a variety of chemically modified forms, including those with acetyl modifications at the C-7, C-8, and C-9 positions. Here, we analyzed the distribution and amounts of these acetyl modifications in different human and canine cells. Since Sia or their variant forms are receptors for influenza A, B, C, and D viruses, we examined the effects of these modifications on virus infections. We confirmed that 9-O-acetyl and 7,9-O-acetyl modified Sia are widely but variably expressed across cell lines from both humans and canines. Although they were expressed on the cell surfaces of canine MDCK cell lines, they were located primarily within the Golgi compartment of human HEK-293 and A549 cells. The O-acetyl modified Sia were expressed at low levels of 1 to 2% of total Sia in these cell lines. We knocked out and overexpressed the sialate O-acetyltransferase gene (CasD1) and knocked out the sialate O-acetylesterase gene (SIAE) using CRISPR/Cas9 editing. Knocking out CasD1 removed 7,9-O- and 9-O-acetyl Sia expression, confirming previous reports. However, overexpression of CasD1 and knockout of SIAE gave only modest increases in 9-O-acetyl levels in cells and no change in 7,9-O-acetyl levels, indicating that there are complex regulations of these modifications. These modifications were essential for influenza C and D infection but had no obvious effect on influenza A and B infection. IMPORTANCE Sialic acids are key glycans that are involved in many different normal cellular functions, as well as being receptors for many pathogens. However, Sia come in diverse chemically modified forms. Here, we examined and manipulated the expression of 7,9-O- and 9-O-acetyl modified Sia on cells commonly used in influenza virus and other research by engineering the enzymes that produce or remove the acetyl groups.

scholarly journals Antiproliferative Oleanane Saponins from Polyscias Guilfoylei

2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Giuseppina Cioffi ◽  
Antonio Vassallo ◽  
Laura Lepore ◽  
Fabio Venturella ◽  
Fabrizio Dal Piaz ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
2D Nmr ◽  
Human Cancer Cell ◽  
Hek 293 ◽  
Human Cancer Cell Lines ◽  
Echinocystic Acid ◽  
Aerial Parts

Three new oleanane saponins (1–3), together with four known ones (4–7), were isolated from the aerial parts of Polyscias guilfoylei. Their structures were elucidated by 1D and 2D NMR experiments, including 1D TOCSY, DQF-COSY, ROESY, HSQC, and HMBC spectroscopy, as well as ESIMS analysis. The antiproliferative activity of all compounds was evaluated using three murine and human cancer cell lines; J774.A1, HEK-293, and WEHI-164. All the compounds were inactive except for 3β- O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl]-echinocystic acid 28-[ O-β-D-glucopyranosyl-(1→6) O-β-D-glucopyranosyl] ester (3), which was active against all the cell lines.

Differential induction of mafF, mafG and mafK expression by electrophile-response-element activators

2002 ◽  
Vol 361 (2) ◽  
pp. 371-377 ◽  
Author(s):  
Julie A. MORAN ◽  
Erica L. DAHL ◽  
R. Timothy MULCAHY
Keyword(s):  
Stress Response ◽  
Cell Lines ◽  
Expression Patterns ◽  
Constitutive Expression ◽  
Response Element ◽  
Hek 293 ◽  
Physiological Processes ◽  
Absolute Requirement ◽  
Differential Induction ◽  
Phenylethyl Isothiocyanate

The three small Maf proteins, MafF, MafG and MafK, have been implicated in a number of physiological processes, including development, differentiation, haematopoiesis and stress response. Here we report the constitutive expression of mafF, mafG and mafK in six human cell lines derived from various tissues (HepG2, IMR-32, K-562, HEK-293, RD and A549). The expression patterns of mafF, mafG and mafK varied widely among cell lines. Because small Maf proteins have been implicated in electrophile response element (EpRE)-mediated stress response, the ability of three EpRE activators [pyrrolidinedithiocarbamate (PDTC), phenylethyl isothiocyanate (PEITC) and t-butylhydroquinone (tBHQ)] to induce small Maf expression was examined in detail in HepG2 cells. Both PDTC and PEITC induced mafF, mafG and mafK expression, whereas tBHQ failed to markedly induce any of the three small Mafs. Where a response was observed, mafF was induced to the greatest extent compared with mafG and mafK, and this response was transcriptionally mediated. PDTC also induced small Maf expression in the other cell lines examined, with patterns of induction varying among cell lines. The differences in expression among the cell lines examined, coupled with the induction patterns observed, indicate that the three small maf genes are stress-responsive, but may be regulated via differing mechanisms. Furthermore, the fact that tBHQ, PDTC and PEITC induce EpRE activity, but that tBHQ fails to markedly induce any of the small Mafs, suggests that up-regulation of small Mafs is not an absolute requirement for EpRE-mediated gene expression.

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