scholarly journals Anticancer Activities of the Quinone-Methide Triterpenes Maytenin and 22-β-hydroxymaytenin Obtained from Cultivated Maytenus ilicifolia Roots Associated with Down-Regulation of miRNA-27a and miR-20a/miR-17-5p

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 760
Author(s):  
Camila Hernandes ◽  
Lucyene Miguita ◽  
Romario Oliveira de Sales ◽  
Elisangela de Paula Silva ◽  
Pedro Omori Ribeiro de Mendonça ◽  
...  
Keyword(s):  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Biological Activities ◽  
Intraperitoneal Administration ◽  
Kidney Tissue ◽  
Quinone Methide ◽  
Wide Range ◽  
Maytenus Ilicifolia

Natural triterpenes exhibit a wide range of biological activities. Since this group of secondary metabolites is structurally diverse, effects may vary due to distinct biochemical interactions within biological systems. In this work, we investigated the anticancer-related activities of the quinone-methide triterpene maytenin and its derivative compound 22-β-hydroxymaytenin, obtained from Maytenus ilicifolia roots cultivated in vitro. Their antiproliferative and pro-apoptotic activities were evaluated in monolayer and three-dimensional cultures of immortalized cell lines. Additionally, we investigated the toxicity of maytenin in SCID mice harboring tumors derived from a squamous cell carcinoma cell line. Both isolated molecules presented pronounced pro-apoptotic activities in four cell lines derived from head and neck squamous cell carcinomas, including a metastasis-derived cell line. The molecules also induced reactive oxygen species (ROS) and down-regulated microRNA-27a and microRNA-20a/miR-17-5p, corroborating with the literature data for triterpenoids. Intraperitoneal administration of maytenin to tumor-bearing mice did not lead to pronounced histopathological changes in kidney tissue, suggesting low nephrotoxicity. The wide-ranging activity of maytenin and 22-β-hydroxymaytenin in head and neck cancer cells indicates that these molecules should be further explored in plant biochemistry and biotechnology for therapeutic applications.

scholarly journals Gene status of head and neck squamous cell carcinoma cell lines and cetuximab-mediated biological activities

2011 ◽  
Vol 102 (9) ◽  
pp. 1717-1723 ◽  
Author(s):  
Norio Kondo ◽  
Mamoru Tsukuda ◽  
Takahide Taguchi ◽  
Kouichi Nakazaki ◽  
Atsuko Sakakibara ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Lines ◽  
Squamous Cell ◽  
Carcinoma Cell ◽  
Biological Activities ◽  
Squamous Cell Carcinoma Cell ◽  
Carcinoma Cell Lines ◽  
Gene Status

scholarly journals Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures

2021 ◽  
Vol 14 (11) ◽  
pp. 1158
Author(s):  
Benas Balandis ◽  
Vytautas Mickevičius ◽  
Vilma Petrikaitė
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Triple Negative Breast Cancer ◽  
Heterocyclic Compounds ◽  
Triple Negative ◽  
Biological Activities ◽  
Human Malignant Melanoma ◽  
Imidazole Derivatives ◽  
Wide Range

Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In this work, we have synthesized a series of new imidazole derivatives incorporating a benzenesulfonamide moiety in their structure, which then were evaluated for their cytotoxicity against human triple-negative breast cancer MDA-MB-231 and human malignant melanoma IGR39 cell lines by MTT assay. Benzenesulfonamide-bearing imidazole derivatives containing 4-chloro and 3,4-dichlorosubstituents in benzene ring, and 2-ethylthio and 3-ethyl groups in imidazole ring have been determined as the most active compounds. Half-maximal effective concentration (EC50) of the most cytotoxic compound was 27.8 ± 2.8 µM against IGR39 cell line and 20.5 ± 3.6 µM against MDA-MB-231 cell line. Compounds reduced cell colony formation of both cell lines and inhibited the growth and viability of IGR39 cell spheroids more efficiently compared to triple-negative breast cancer spheroids.

scholarly journals Potentially Novel Candidate Biomarkers for Head and Neck Squamous Cell Carcinoma Identified Using an Integrated Cell Line-based Discovery Strategy

2012 ◽  
Vol 11 (11) ◽  
pp. 1404-1415 ◽  
Author(s):  
Lusia Sepiashvili ◽  
Angela Hui ◽  
Vladimir Ignatchenko ◽  
Willa Shi ◽  
Susie Su ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Western Blotting ◽  
Squamous Cell ◽  
Control Cell ◽  
Data Set ◽  
Qrt Pcr ◽  
Increased Risk

Head and neck squamous cell carcinomas (HNSCC) can arise from the oral cavity, oropharynx, larynx or hypopharynx, and is the sixth leading cancer by incidence worldwide. The 5-year survival rate of HNSCC patients remains static at 40–60%. Hence, biomarkers which can improve detection of HNSCC or early recurrences should improve clinical outcome. Mass spectrometry-based proteomics methods have emerged as promising approaches for biomarker discovery. As one approach, mass-spectrometric identification of proteins shed or secreted from cancer cells can contribute to the identification of potential biomarkers for HNSCC and our understanding of tumor behavior. In the current study, mass spectrometry-based proteomic profiling was performed on the conditioned media (i.e. secretome) of head and neck cancer (HNC) cell lines (FaDu, UTSCC8 and UTSCC42a) in addition to gene expression microarrays to identify over-expressed transcripts in the HNSCC cells in comparison to a normal control cell line. This integrated data set was systematically mined using publicly available resources (Human Protein Atlas and published proteomic/transcriptomic data) to prioritize putative candidates for validation. Subsequently, quantitative real-time PCR (qRT-PCR), Western blotting, immunohistochemistry (IHC), and ELISAs were performed to verify selected markers. Our integrated analyses identified 90 putative protein biomarkers that were secreted or shed to the extracellular space and over-expressed in HNSCC cell lines, relative to controls. Subsequently, the over-expression of five markers was verified in vitro at the transcriptional and translational levels using qRT-PCR and Western blotting, respectively. IHC-based validation conducted in two independent cohorts comprising of 40 and 39 HNSCC biopsies revealed that high tumor expression of PLAU, IGFBP7, MMP14 and THBS1 were associated with inferior disease-free survival, and increased risk of disease progression or relapse. Furthermore, as demonstrated using ELISAs, circulating levels of PLAU and IGFBP7 were significantly higher in the plasma of HNSCC patients compared with healthy individuals.

scholarly journals Remedial Effects and Molecular Docking Studies of Nevadensin: ‎Antiglucosidase, Anti-cholinesterase, and Anti-Human Oral Squamous ‎Cell Carcinoma Potentials

2021 ◽  
Author(s):  
Xu Lan ◽  
Li Liu ◽  
Guangyu Wu
Keyword(s):  
Squamous Cell Carcinoma ◽  
Molecular Docking ◽  
Oral Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging

IntroductionNevadensin has a variety of pharmacological effects, including effects of anti-mycobacterium ‎tuberculosis, antitussive, anti-hypertensive, anti-inflammatory, and free radical-scavenging ‎activities. In this study, we investigated for their anticholinergics, antidiabetic, and anti-‎human oral squamous cell carcinoma potentials for nevadensin. ‎Material and methodsThe antioxidant activities of nevadensin were elucidated by using various bioanalytical assays. ‎On the other hand, IC50 values were calculated for acetylcholine esterase, α-glucosidase ‎inhibition effects of nevadensin. For determining of anti-human oral squamous cell carcinoma ‎properties of nevadensin, MTT assay was used on HUVEC, HSC-3, HSC-4, and Ca9-22 cell ‎lines. The molecular docking method used to compare the biological activities of the ‎nevadensin molecule against enzymes was used. Afterwards, the ADME/T analysis was ‎performed to investigate the drug availability of the nevadensin molecule and the obtained ‎parameters from ADME/T analysis were examined.‎ResultsThe cell viability of nevadensin was very low against human oral squamous cell carcinoma cell ‎lines without any cytotoxicity on the human normal (HUVEC) cell line. The IC50 of the ‎nevadensin against HSC-3, HSC-4, and Ca9-22 were 316, 273, and 399 µg/mL, respectively. ‎Thereby, the best cytotoxicity results and anti-human oral squamous cell carcinoma potentials ‎of our nevadensin was observed in the case of the HSC-4 cell line. ‎ConclusionsMaybe the anti-human lung carcinoma properties of nevadensin are related to their antioxidant ‎effects. ‎

scholarly journals Cancer cell line microarray as a novel screening method for identification of radioresistance biomarkers in head and neck squamous cell carcinoma

BMC Cancer ◽  
2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Johannes Routila ◽  
Karri Suvila ◽  
Reidar Grénman ◽  
Ilmo Leivo ◽  
Jukka Westermarck ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Stem Cell ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Stem Cell Marker ◽  
Cell Marker ◽  
Hnscc Cell

Abstract Background Currently, no clinically useful biomarkers for radioresistance are available in head and neck squamous cell carcinoma (HNSCC). This study assesses the usefulness of Cell Line Microarray (CMA) method to enhance immunohistochemical screening of potential immunohistochemical biomarkers for radioresistance in HNSCC cell lines. Methods Twenty-nine HNSCC cell lines were cultured, cell pellets formalin-fixed, paraffin-embedded, and arrayed. Radioresistance features of the cell lines were combined to immunohistochemical stains for p53, NDFIP1, EGFR, stem cell marker Oct4, and PP2A inhibitor CIP2A. Results Expression of p53, EGFR or CIP2A did not indicate intrinsic radioresistance in vitro. Stem cell marker Oct4 nuclear positivity and NDFIP1 nuclear positivity was correlated with increased intrinsic radioresistance. Conclusion The usefulness of CMA in analysis of HNSCC cell lines and discovery of biomarkers is demonstrated. CMA is very well adapted to both testing of antibodies in a large panel of cell lines as well as correlating staining results with other cell line characteristics. In addition, CMA-based antibody screening proved an efficient and relatively simple method to identify potential radioresistance biomarkers in HNSCC.

scholarly journals Identification and Characterization of Cancer Stem Cells from Head and Neck Squamous Cell Carcinoma Cell Lines

2015 ◽  
Vol 36 (2) ◽  
pp. 784-798 ◽  
Author(s):  
Valentina Pozzi ◽  
Davide Sartini ◽  
Romina Rocchetti ◽  
Andrea Santarelli ◽  
Corrado Rubini ◽  
...  
Keyword(s):  
Stem Cells ◽  
Squamous Cell Carcinoma ◽  
Cancer Stem Cells ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell

Background/Aims: Head and neck squamous cell carcinoma (HNSCC) ranks sixth worldwide for tumor-related mortality. A subpopulation of tumor cells, termed cancer stem cells (CSCs), has the ability to support cancer growth. Therefore, profiling CSC-enriched populations could be a reliable tool to study cancer biology. Methods: We performed phenotypic characterization of 7 HNSCC cell lines and evaluated the presence of CSCs. CSCs from Hep-2 cell line and HNSCC primary cultures were enriched through sphere formation and sphere-forming cells have been characterized both in vitro and in vivo. In addition, we investigated the expression levels of Nicotinamide N-methyltransferase (NNMT), an enzyme overexpressed in several malignancies. Results: CSC markers were markedly expressed in Hep-2 cell line, which was found to be highly tumorigenic. CSC-enriched populations displayed increased expression of CSC markers and a strong capability to form tumors in vivo. We also found an overexpression of CSC markers in tumor formed by CSC-enriched populations. Interestingly, NNMT levels were significantly higher in CSC-enriched populations compared with parental cells. Conclusion: Our study provides an useful procedure for CSC identification and enrichment in HNSCC. Moreover, results obtained seem to suggest that CSCs may represent a promising target for an anticancer therapy.

scholarly journals PD-L1 and MRN synergy in platinum-based chemoresistance of head and neck squamous cell carcinoma

2019 ◽  
Vol 122 (5) ◽  
pp. 640-647 ◽  
Author(s):  
Bin Shen ◽  
Dongyan Huang ◽  
Andrew J. Ramsey ◽  
Kevin Ig-Izevbekhai ◽  
Kevin Zhang ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Molecular Mechanisms ◽  
Cisplatin Resistance ◽  
Neck Squamous Cell Carcinoma ◽  
Hnscc Cell

Abstract Background We have been investigating the molecular mechanisms of cisplatin-induced chemoresistance in head and neck squamous cell carcinoma (HNSCC). Based on our previous findings, the present study investigates how the Mre11, Rad50, and NBS1 (MRN) DNA repair complex interacts at the molecular level with the programmed cell death ligand 1 (PD-L1) in cisplatin-induced chemoresistance. Methods Human HNSCC cell lines were used to determine the role played by PD-L1 in cisplatin resistance. Initial experiments investigated PD-L1 expression levels in cells exposed to cisplatin and whether PD-L1 interacts directly with the MRN complex. Finally, in vitro studies and in vivo experiments on BALB/c nu/nu mice were performed to determine whether interference of PD-L1 or NBS1 synthesis modulated cisplatin resistance. Results Exposure to cisplatin resulted in PD-L1 being upregulated in the chemoresistant but not the chemosensitive cell line. Subsequent co-immunoprecipitation studies demonstrated that PD-L1 associates with NBS1. In addition, we found that the knockdown of either PD-L1 or NBS1 re-sensitised the chemoresistant cell line to cisplatin. Finally, but perhaps most importantly, synergy was observed when both PD-L1 and NBS1 were knocked down making the formerly chemoresistant strain highly cisplatin sensitive. Conclusions PD-L1 plays a pivotal role in cisplatin resistance in chemoresistant human HNSCC cell lines.

scholarly journals A Human Head and Neck Squamous Cell Carcinoma Cell Line with Acquiredcis-Diamminedichloroplatinum-Resistance Shows Remarkable Upregulation of BRCA1 and Hypersensitivity to Taxane

2011 ◽  
Vol 2011 ◽  
pp. 1-4 ◽  
Author(s):  
Yuriko Saiki ◽  
Takenori Ogawa ◽  
Kiyoto Shiga ◽  
Makoto Sunamura ◽  
Toshimitsu Kobayashi ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Resistant Cell ◽  
Neck Squamous Cell Carcinoma ◽  
Cross Resistance ◽  
Parental Cell Line

Recently, an inverse relationship between resistance to platinum-based chemotherapeutic agents and taxanes has been implicated in breast and ovarian cancers, and a possible pivotal role for BRCA1 has also been suggested. Becausecis-diamminedichloroplatinum (CDDP) and taxanes are the most active antitumor agents against head and neck squamous cell carcinoma (HNSCC), we analyzed the sensitivity of nine HNSCC cell lines and their previously established derived CDDP-resistant cell lines to two representative taxanes: docetaxel and paclitaxel. None of the nine original cell lines showed any cross resistance between CDDP and taxanes, but one of the CDDP-resistant cell lines, RPMI2650CR, demonstrated hypersensitivity to both taxanes when compared to the parental cell line, RPMI2650. Furthermore, RPMI2650CR exhibited increased expression of BRCA1. These data suggest that (i) taxanes are a good candidate for a second-line therapeutic drug for HNSCC patients with acquired CDDP resistance and (ii) BRCA1 can be a candidate marker for predicting an inverse CDDP/taxane sensitivity phenotype in HNSCC.

Specific Targeting of HER2-Positive Head and Neck Squamous Cell Carcinoma Line HN5 by Idarubicin-ZHER2 Affibody Conjugate

2018 ◽  
Vol 19 (1) ◽  
pp. 65-73 ◽  
Author(s):  
Marzieh Ghanemi ◽  
Aminollah Pourshohod ◽  
Mohammad Ali Ghaffari ◽  
Alireza kheirollah ◽  
Mansour Amin ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Head And Neck ◽  
Cell Line ◽  
Squamous Cell ◽  
Optimum Concentration ◽  
Her2 Positive ◽  
Affibody Molecules ◽  
Specific Targeting ◽  
Mcf 7

Background:Expression of human epidermal growth factor receptor type 2 (HER2) in head and neck squamous cell carcinoma (HNSCC) cell line HN5 can be employed with great opportunities of success for specific targeting of anti-cancer chemotherapeutic agents.Objective:In the current study, HER2-specific affibody molecule, ZHER2:342 (an engineered protein with great affinity for HER2 receptors) was selected for conjugation to idarubicin (an anti-neoplastic antibiotic).Method:ZHER2:342 affibody gene with one added cysteine code at the its 5′ end was synthesized de novo and then inserted into pET302 plasmid and transferred to E. Coli BL21 hosting system. After induction of protein expression, the recombinant ZHER2 affibody molecules were purified using Ni- NTA resin and purity was analyzed through SDS-PAGE. Affinity-purified affibody molecules were conjugated to idarubicin through a heterobifunctional crosslinker, sulfosuccinimidyl 4-(Nmaleimidomethyl) cyclohexane-1-carboxylate (Sulfo-SMCC). Specific toxicity of idarubicin-ZHER2 affibody conjugate against two HER2-positive cells, HN5 and MCF-7 was assessed through MTT assay after an exposure time of 48 hours with different concentrations of conjugate.Results:Idarubicin in the non-conjugated form showed potent toxic effects against both cell lines, while HN5 cells were significantly more sensitive compared to MCF-7 cells. Dimeric ZHER2 affibody showed a mild decreasing effect on growth of both HN5 and MCF-7 cells at optimum concentration. Idarubicin-ZHER2 affibody conjugate at an optimum concentration reduced viability of HN5 cell line more efficiently compared to MCF-7 cell line.In conclusion, idarubicin-ZHER2 affibody conjugate in optimum concentrations can be used for specific targeting and killing of HN5 cells.

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