scholarly journals Antiproliferative Properties of Scandium Exopolysaccharide Complexes on Several Cancer Cell Lines

Marine Drugs ◽  
2021 ◽  
Vol 19 (3) ◽  
pp. 174
Author(s):  
Javier Muñoz-Garcia ◽  
Mattia Mazza ◽  
Cyrille Alliot ◽  
Corinne Sinquin ◽  
Sylvia Colliec-Jouault ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Protein Interactions ◽  
Transmembrane Protein ◽  
Biological Effects ◽  
Growth Factor Receptor ◽  
Predictive Biomarker ◽  
Biological Properties ◽  
Osteosarcoma Cell

Antimetastatic properties on both murine and human osteosarcoma cell lines (POS-1 and KHOS) have been evidenced using exopolysaccharide (EPS) derivatives, produced by Alteromonas infernus bacterium. These derivatives had no significant effect on the cell cycle neither a pro-apoptotic effect on osteosarcoma cells. Based on this observation, these EPSs could be employed as new drug delivery systems for therapeutic uses. A theranostic approach, i.e., combination of a predictive biomarker with a therapeutic agent, has been developed notably by combining with true pair of theranostic radionuclides, such as scandium 47Sc/44Sc. However, it is crucial to ensure that, once complexation is done, the biological properties of the vector remain intact, allowing the molecular tropism of the ligand to recognize its molecular target. It is important to assess if the biological properties of EPS evidenced on osteosarcoma cell lines remain when scandium is complexed to the polymers and can be extended to other cancer cell types. Scandium-EPS complexes were thus tested in vitro on human cell lines: MNNG/HOS osteosarcoma, A375 melanoma, A549 lung adenocarcinoma, U251 glioma, MDA231 breast cancer, and Caco2 colon cancer cells. An xCELLigence Real Cell Time Analysis (RTCA) technology assay was used to monitor for 160 h, the proliferation kinetics of the different cell lines. The tested complexes exhibited an anti-proliferative effect, this effect was more effective compared to EPS alone. This increase of the antiproliferative properties was explained by a change in conformation of EPS complexes due to their polyelectrolyte nature that was induced by complexation. Alterations of both growth factor-receptor signaling, and transmembrane protein interactions could be the principal cause of the antiproliferative effect. These results are very promising and reveal that EPS can be coupled to scandium for improving its biological effects and also suggesting that no major structural modification occurs on the ligand.

scholarly journals Epicatechins Purified from Green Tea (Camellia sinensis) Differentially Suppress Growth of Gender-Dependent Human Cancer Cell Lines

2006 ◽  
Vol 3 (2) ◽  
pp. 237-247 ◽  
Author(s):  
Mepur H. Ravindranath ◽  
Thiruverkadu S. Saravanan ◽  
Clarence C. Monteclaro ◽  
Naftali Presser ◽  
Xing Ye ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Ovarian Cancer ◽  
Epithelial Ovarian Cancer ◽  
Cell Lines ◽  
Green Tea ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines

The anticancer potential of catechins derived from green tea is not well understood, in part because catechin-related growth suppression and/or apoptosis appears to vary with the type and stage of malignancy as well as with the type of catechin. Thisin vitrostudy examined the biological effects of epicatechin (EC), epigallocatechin (EGC), EC 3-gallate (ECG) and EGC 3-gallate (EGCG) in cell lines from human gender-specific cancers. Cell lines developed from organ-confined (HH870) and metastatic (DU145) prostate cancer, and from moderately (HH450) and poorly differentiated (HH639) epithelial ovarian cancer were grown with or without EC, EGC, ECG or EGCG. When untreated cells reached confluency, viability and doubling time were measured for treated and untreated cells. Whereas EC treatment reduced proliferation of HH639 cells by 50%, EGCG suppressed proliferation of all cell lines by 50%. ECG was even more potent: it inhibited DU145, HH870, HH450 and HH639 cells at concentrations of 24, 27, 29 and 30 µM, whereas EGCG inhibited DU145, HH870, HH450 and HH639 cells at concentrations 89, 45, 62 and 42 µM. When compared with EGCG, ECG more effectively suppresses the growth of prostate cancer and epithelial ovarian cancer cell lines derived from tumors of patients with different stages of disease.

scholarly journals Genistein Derivatives Regioisomerically Substituted at 7-O- and 4′-O- Have Different Effect on the Cell Cycle

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
A. Byczek ◽  
J. Zawisza-Puchalka ◽  
A. Gruca ◽  
K. Papaj ◽  
G. Grynkiewicz ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Dna Lesions ◽  
Hydroxyl Group ◽  
Human Cancer Cell Lines

Our previous studies on antiproliferative properties of genistein derivatives substituted at C7 hydroxyl group of the ring A revealed some compounds with antimitotic properties. The aim of this work was to synthesize their analogues substituted at the 4′-position of the ring B in genistein and to define their antiproliferative mechanism of action in selected cancer cell linesin vitro. C4′-substituted glycoconjugates were obtained in a three-step procedure: (1) alkylation with anω-bromoester; (2) deacylation; (3) Ferrier-type rearrangement glycosylation with acylated glycals. Biological effects including antiproliferative effects of the compounds, cell cycle, DNA lesions (ATM activation, H2A.X phosphorylation, and micronuclei formation), and autophagy were studied in human cancer cell lines. Some of the tested derivatives potently inhibited cell proliferation. The presence of a substituent at the 4′-position of the ring B in genistein correlated to a p53-independent G1 cell-cycle arrest. The derivatives substituted at C4′ did not induce DNA lesions and appeared to be nongenotoxic. The tested compounds induced autophagy and caused remarkable decrease of cell volume.

scholarly journals mTOR/EGFR/iNOS/MAP2K1/FGFR/TGFB1 Are Druggable Candidates for N-(2,4-Difluorophenyl)-2′,4′-Difluoro-4-Hydroxybiphenyl-3-Carboxamide (NSC765598), With Consequent Anticancer Implications

2021 ◽  
Vol 11 ◽  
Author(s):  
Bashir Lawal ◽  
Ching-Yu Lee ◽  
Ntlotlang Mokgautsi ◽  
Maryam Rachmawati Sumitra ◽  
Harshita Khedkar ◽  
...  
Keyword(s):  
Growth Factor ◽  
Growth Inhibition ◽  
Cell Lines ◽  
Squamous Cell ◽  
Protein Interactions ◽  
Squamous Cell Cancer ◽  
Cell Cancer ◽  
Growth Factor Receptor ◽  
Anticancer Activities

BackgroundThe application of computational and multi-omics approaches has aided our understanding of carcinogenesis and the development of therapeutic strategies. NSC765598 is a novel small molecule derivative of salicylanilide. This study aims to investigate the ligand-protein interactions of NSC765598 with its potential targets and to evaluate its anticancer activities in vitro.MethodsWe used multi-computational tools and clinical databases, respectively, to identify the potential drug target for NSC765598 and analyze the genetic profile and prognostic relevance of the targets in multiple cancers. We evaluated the in vitro anticancer activities against the National Cancer Institute 60 (NCI60) human tumor cell lines and used molecular docking to study the ligand-protein interactions. Finally, we used the DTP-COMPARE algorithm to compare the NSC765598 anticancer fingerprints with NCI standard agents.ResultsWe identified mammalian target of rapamycin (mTOR)/epidermal growth factor receptor (EGFR)/inducible nitric oxide synthase (iNOS)/mitogen-activated protein 2 kinase 1 (MAP2K1)/fibroblast growth factor receptor (FGFR)/transforming growth factor-β1 (TGFB1) as potential targets for NSC765598. The targets were enriched in cancer-associated pathways, were overexpressed and were of prognostic relevance in multiple cancers. Among the identified targets, genetic alterations occurred most frequently in EGFR (7%), particularly in glioblastoma, esophageal squamous cell cancer, head and neck squamous cell cancer, and non–small-cell lung cancer, and were associated with poor prognoses and survival of patients, while other targets were less frequently altered. NSC765598 displayed selective antiproliferative and cytotoxic preferences for NSCLC (50% growth inhibition (GI50) = 1.12–3.95 µM; total growth inhibition (TGI) = 3.72–16.60 μM), leukemia (GI50 = 1.20–3.10 µM; TGI = 3.90–12.70 μM), melanoma (GI50 = 1.45–3.59 µM), and renal cancer (GI50 = 1.38–3.40 µM; TGI = 4.84–13.70 μM) cell lines, while panels of colon, breast, ovarian, prostate, and central nervous system (CNS) cancer cell lines were less sensitive to NSC765598. Interestingly, NSC765598 docked well into the binding cavity of the targets by conventional H-bonds, van der Waal forces, and a variety of π-interactions, with higher preferences for EGFR (ΔG = −11.0 kcal/mol), NOS2 (ΔG = −11.0 kcal/mol), and mTOR (ΔG = −8.8 kcal/mol). NSC765598 shares similar anti-cancer fingerprints with NCI standard agents displayed acceptable physicochemical values and met the criteria of drug-likeness.ConclusionNSC765598 displayed significant anticancer and potential multi-target properties, thus serve as a novel candidate worthy of further preclinical studies.

scholarly journals RID: Evaluation of the Possible Inhibiting Effect of the Proinflammatory Signaling Induced by TNF-α through NF-κβ and AP-1 in Two Cell Lines of Breast Cancer

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
F. A. Monsalve ◽  
A. Rojas ◽  
I. Gonzalez ◽  
R. Perez ◽  
C. Añasco ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Transmembrane Protein ◽  
Growth Factor Receptor ◽  
Cancer Cell Line ◽  
Receptor Internalization ◽  
Cell Surface Expression

Receptor internalization and degradation (RID), is a transmembrane protein coded within the E3 region expression cassette of adenoviruses. RID downregulates the cell surface expression of epidermal growth factor receptor (EGFR), tumor necrosis factor receptor (TNFR), and apoptosis antigen 1 (FAS), causing a reduction of the effects of their respective ligands. In addition, RID inhibits apoptosis by decreasing the secretion of TNF-related apoptosis-inducing ligand (TRAIL) by normal tissue cells. In this article, we report that RID inhibited chemokine expression in human breast cancer cell line MDA-MB-231 but showed no effect in cell line MCF7. These dissimilar results may be due to the different molecular and functional properties of both cell lines. Therefore, it is necessary to replicate this study in other breast cancer cell models.

scholarly journals Met-HER3 crosstalk supports proliferation via MPZL3 in MET-amplified cancer cells

2021 ◽  
Author(s):  
Yaakov Elisha Stern ◽  
Stephanie Duhamel ◽  
Abdulhameed Al-Ghabkari ◽  
Anie Monast ◽  
Benoit Fiset ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Tyrosine Kinases ◽  
Human Cancer ◽  
Transmembrane Protein ◽  
Cancer Cell Lines ◽  
Her Family

Receptor tyrosine kinases (RTKs) are recognized as targets of precision medicine in human cancer upon their gene amplification or constitutive activation, resulting in increased downstream signal complexity including heterotypic crosstalk with other RTKs. The Met RTK exhibits such reciprocal crosstalk with several members of the human EGFR (HER) family of RTKs when amplified in cancer cells. We show that Met signaling converges on HER3 tyrosine phosphorylation across a panel of seven MET-amplified cancer cell lines and that HER3 is required for cancer cell expansion and oncogenic capacity in-vitro and in-vivo. Gene expression analysis of HER3-depleted cells identified MPZL3, encoding a single-pass transmembrane protein, as a HER3-dependent effector in multiple MET-amplified cancer cell lines. MPZL3 interacts with HER3 and MPZL3 loss phenocopies HER3 loss in MET-amplified cells, while MPZL3 overexpression rescues proliferation upon HER3 depletion. Together, these data support an oncogenic role for a HER3-MPZL3 axis in MET-amplified cancers.

scholarly journals Redounding of Cuscuta chinensis Lam. on BxPC-3, HepG2, and U2OS Human Cancer Cell Lines

2020 ◽  
Vol 10 (03) ◽  
pp. 354-359
Author(s):  
Basma Talib Al-Sudani ◽  
Nadia H. Mohammed ◽  
Fadia H. Al-Sultany
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
U2os Cell ◽  
Time Interval ◽  
Osteosarcoma Cell ◽  
Human Cancer Cell Lines ◽  
Cuscuta Chinensis

Objective: The present study was designed to investigate in vitro cytotoxic effect of aqueous extract from whole Cuscuta chinensis on human hepatocellular carcinoma (HepG2), biopsy xenograft of pancreatic carcinoma line-3 (BxPC-3), and children human bone osteosarcoma cell line (U2OS). Materials and Methods: The anticancer effectiveness of the methanol-watery extract of C. chinensis Lam. was determined by using methyl tetrazolium bromide test (MTT) assay against cancer cells by using suspensions of BxPC-3, HepG2, and U2OS cell lines. The inhibitory concentration (IC50) was tested for each cancer cell line. BxPC-3, HepG2, and U2OS cell line death percent after incubation with extract for 24, 48, and 72-hours interval was compared with cisplatin death percent. Results: The results showed that the IC50 of Cuscuta extract for BxPC-3, HepG2, and U2OS cell lines was 13, 6.5, and 0.73 μg/mL, respectively. The HepG2 cell line death%, when treated with 50 μg/mL Cuscuta extract at 24, 48, and 72-hour time interval, was 90.41, 91.45, and 92.93%, while cells were treated with 15 μg/mL cisplatin, the death percent was 88.8, 93.7, and 96.61%, respectively. The BxPC-3 cell line death%, when treated with 50 μg/mL Cuscuta extract, was 51.46, 83.37, and 91.28%, respectively, and when treated with 15 μg/mL cisplatin was 81.64, 88.02, and 96.67%, respectively. The U2OS cell line death%, when treated with 50 μg/mL Cuscuta extract, was 69.43, 69.75, and 88.89%, and was 74.1, 84.61, and 93.39%, respectively, when treated with 15 μg/mL cisplatin. Conclusion: The methanol-watery extract of C. chinensis Lam. may have a potential role as an adjunct therapy for cancers in the future.

scholarly journals Genomic Characterization and Therapeutic Targeting of HPV Undetected Cervical Carcinomas

Cancers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 4551
Author(s):  
Fiona J. Ruiz ◽  
Aishwarya Sundaresan ◽  
Jin Zhang ◽  
Chandra S. Pedamallu ◽  
Mari K. Halle ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cell Cycle Progression ◽  
Clinical Decision Making ◽  
Predictive Biomarker ◽  
Clinical Decision ◽  
Cancer Cell Lines ◽  
Survival Outcomes ◽  
Alternative Treatment Strategy

Cervical cancer tumors with undetectable HPV (HPVU) have been underappreciated in clinical decision making. In this study, two independent CC datasets were used to characterize the largest cohort of HPVU tumors to date (HPVU = 35, HPV+ = 430). Genomic and transcriptome tumor profiles and patient survival outcomes were compared between HPV+ and HPVU tumors. In vitro analyses were done to determine efficacy of the selective CDK4/6 inhibitor palbociclib on HPVU cancer cell lines. Patients with HPVU CC tumors had worse progression-free and overall survival outcomes compared to HPV+ patients. TP53, ARID1A, PTEN, ARID5B, CTNNB1, CTCF, and CCND1 were identified as significantly mutated genes (SMGs) enriched in HPVU tumors, with converging functional roles in cell cycle progression. In vitro HPVU, but not HPV+, cancer cell lines with wild type RB1 were sensitive to palbociclib monotherapy. These results indicate that HPVU status can be translated into the clinic as a predictive biomarker of poor patient response to standard of care treatments. We suggest primary cervix tumors be routinely tested for HPV prior to treatment to identify patients who will benefit from more aggressive precision-driven therapy. Our results identify palbociclib as a lead candidate as an alternative treatment strategy for HPVU CC patients.

scholarly journals Evaluating the Targeting Efficiency of Anti-EGFR Functionalised Nanoparticles to Head and Neck Cancer Cells for Use in NIR-II Optical Window

2021 ◽  
Author(s):  
Teklu Egnuni ◽  
Nicola Ingram ◽  
P. Louise Coletta ◽  
James R. McLaughlan
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Near Infrared ◽  
Photoacoustic Imaging ◽  
Growth Factor Receptor ◽  
Optical Window ◽  
Targeting Efficiency ◽  
Optical Attenuation ◽  
Significant Difference

Gold nanoparticles have been indicated for use in a diagnostic and/or therapeutic role in several cancer types. The use of gold nanorods (AuNRs) with a surface plasmon resonance (SPR) in the second Near-Infrared II (NIR-II) optical window promises deeper anatomical penetration through increased maximum permissible exposure and lower optical attenuation. In this study, the targeting efficiency of anti-epidermal growth factor receptor (EGFR) antibody functionalised AuNRs with an SPR at 1064 nm was evaluated in vitro. Four cell lines, KYSE-30, CAL-27, Hep-G2 and MCF-7 that either over or under expressed EGFR were used. This expression was confirmed by flow cytometry and immunofluorescence. Cytotoxicity assays showed no AuNRs toxicity to both EGFR positive and EGFR negative cell lines up to a concentrations of 19 µg/ml. Optical microscopy demonstrated a significant difference (p<0.0001) between targeted AuNRs (tAuNRs) and untargeted AuNRs (uAuNRs) in all four cancer cell lines. This study demonstrates that anti-EGFR functionalisation significantly increased the number of tAuNRs associated with each EGFR positive cancer cell. This successful targeting highlights the use of tAuNRs for molecular photoacoustic imaging or tumour treatment through plasmonic photothermal therapy.

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