scholarly journals Simple Trans-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin

2020 ◽  
Vol 21 (6) ◽  
pp. 2116
Author(s):  
Małgorzata Fabijańska ◽  
Magdalena Orzechowska ◽  
Agnieszka J. Rybarczyk-Pirek ◽  
Justyna Dominikowska ◽  
Alicja Bieńkowska ◽  
...  
Keyword(s):  
Gene Expression ◽  
Ovarian Cancer ◽  
Anticancer Activity ◽  
Evaluation Method ◽  
Elevated Temperatures ◽  
Platinum Complex ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
Relationship Of

Following previous studies devoted to trans–Pt(3-af)2Cl2, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures are presented in the Cambridge Structural Database (CSD). Molecular Hirshfeld surface analysis and computational methods were used to examine a possible relationship between the structure and anticancer activity of trans–Pt(3-af)2Cl2. The purpose of the article was also to investigate the effect of hyperthermia on the anticancer activity of cisplatin, cytostatics used in the treatment of patients with ovarian cancer and a new analogue of cisplatin-trans–Pt(3-af)2Cl2. The study was conducted on two cell lines of ovarian cancer sensitive to Caov-3 cytostatics and the OVCAR-3 resistant cisplatin line. The study used the MTT (3-(4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide) cell viability assay, LDH (lactate dehydrogenase), and the quantitative evaluation method for measuring gene expression, i.e., qPCR with TagMan probes. Reduced survivability of OVCAR-3 and Caov-3 cells exposed to cytostatics at elevated temperatures (37 °C, 40 °C, 43 °C) was observed. Hyperthermia may increase the sensitivity of cells to platinum-based antineoplastic drugs and paclitaxel, which may be associated with the reduction of gene expression related to apoptotic processes.

scholarly journals Synthesis, Characterization, and Anticancer Activity of New Benzofuran Substituted Chalcones

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Demet Coşkun ◽  
Suat Tekin ◽  
Süleyman Sandal ◽  
Mehmet Fatih Coşkun
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Cell Viability Assay ◽  
Anticancer Properties ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
Antitumor Properties ◽  
Mcf 7

Benzofuran derivatives are of great interest in medicinal chemistry and have drawn considerable attention due to their diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures of numerous natural products belonging to the flavonoid class, feature strong anticancer properties. A novel series of chalcones, 3-aryl-1-(5-bromo-1-benzofuran-2-yl)-2-propanones propenones (3a–f), were designed, synthesized, and characterized.In vitroantitumor activities of the newly synthesized (3a–f) and previously synthesized (3g–j) chalcone compounds were determined by using human breast (MCF-7) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested chalcone compounds was performed and thelog⁡IC50values of the compounds were calculated after 24-hour treatment. Our results indicate that the tested chalcone compounds show antitumor activity against MCF-7 and PC-3 cell lines (p<0.05).

scholarly journals Synthesis of Novel FTY720 Analogs with Anticancer Activity through PP2A Activation

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2750 ◽  
Author(s):  
Jitendra Shrestha ◽  
Sung Ki ◽  
Sang Shin ◽  
Seon Kim ◽  
Joo-Youn Lee ◽  
...  
Keyword(s):  
Cell Viability ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Sphingosine Kinase ◽  
Basic Structure ◽  
Docking Study ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Anticancer Effects ◽  
Pp2a Activation

FTY720 inhibits various cancers through PP2A activation. The structure of FTY720 is also used as a basic structure for the design of sphingosine kinase (SK) inhibitors. We have synthesized derivatives using an amide chain in FTY720 with a phenyl backbone, and then compounds were screened by an MTT cell viability assay. The PP2A activity of compound 7 was examined. The phosphorylation levels of AKT and ERK, downstream targets of PP2A, in the presence of compound 7, were determined. Compound 7 may exhibit anticancer effects through PP2A activation rather than the mechanism by inhibition of SK1 in cancer cells. In the docking study of compound 7 and PP2A, the amide chain of compound 7 showed an interaction with Asn61 that was different from FTY720, which is expected to affect the activity of the compound.

Evaluation of Paclitaxel (Taxol), Cisplatin, and the Combination Paclitaxel-Cisplatin in Ovarian Cancer in Vitro with the ATP Cell Viability Assay

1994 ◽  
Vol 53 (1) ◽  
pp. 44-49 ◽  
Author(s):  
Michael Untch ◽  
Bernd-Uwe Sevin ◽  
James P. Perras ◽  
Roberto Angioli ◽  
Andrea Untch ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cell Viability ◽  
Cell Viability Assay ◽  
Viability Assay

scholarly journals Minispheroids as a Tool for Ligament Tissue Engineering: Do the Self-Assembly Techniques and Spheroid Dimensions Influence the Cruciate Ligamentocyte Phenotype?

2021 ◽  
Vol 22 (20) ◽  
pp. 11011
Author(s):  
Ingrid Zahn ◽  
Tobias Braun ◽  
Clemens Gögele ◽  
Gundula Schulze-Tanzil
Keyword(s):  
Gene Expression ◽  
Tissue Engineering ◽  
Self Assembly ◽  
Cruciate Ligament ◽  
Methyl Cellulose ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Extracellular Matrix Components ◽  
Collagen Type 1 ◽  
Ligament Tissue Engineering

Spheroid culture might stabilize the ligamentocyte phenotype. Therefore, the phenotype of lapine cruciate ligamentocyte (L-CLs) minispheroids prepared either by hanging drop (HD) method or by using a novel spheroid plate (SP) and the option of methyl cellulose (MC) for tuning spheroid formation was tested. A total of 250 and 1000 L-CLs per spheroid were seeded as HDs or on an SP before performing cell viability assay, morphometry, gene expression (qRT-PCR) and protein immunolocalization after 7 (HD/SP) and 14 (SP) days. Stable and viable spheroids of both sizes could be produced with both methods, but more rapidly with SP. MC accelerated the formation of round spheroids (HD). Their circular areas decreased significantly during culturing. After 7 days, the diameters of HD-derived spheroids were significantly larger compared to those harvested from the SP, with a tendency of lower circularity suggesting an ellipsoid shape. Gene expression of decorin increased significantly after 7 days (HD, similar trend in SP), tenascin C tended to increase after 7 (HD/SP) and 14 days (SP), whereas collagen type 1 decreased (HD/SP) compared to the monolayer control. The cruciate ligament extracellular matrix components could be localized in all mini-spheroids, confirming their conserved expression profile and their suitability for ligament tissue engineering.

scholarly journals Effect of Metalloprotease Arazyme on the Expression of MMP2 and MMP9 Genes in Metastasis of Colon and Ovarian Cancer Cell Lines

Thrita ◽  
2020 ◽  
Vol 8 (2) ◽  
Author(s):  
Ghazaleh Amjadi ◽  
Kazem Parivar ◽  
Seyed Fazlollah Mousavi ◽  
Abbas Ali Imani Fooladi
Keyword(s):  
Ovarian Cancer ◽  
Cell Lines ◽  
The United States ◽  
Culture Cell ◽  
Bacterial Strains ◽  
Antitumor Effects ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Common Cancer

Background: After cardiovascular diseases, cancer is the main cause of death in the United States, and its prevalence is continually increasing. Ovarian cancer is a fetal and common cancer among women and is the eighth common cancer in Iran. Colorectal cancer is known as the second and fourth common cancer in Iranian women and men, respectively. Arazyme is a metalloprotease with strong antitumor effects on tumor cells. Objectives: This study aimed at studying the effect of metalloprotease arazyme in vitro on the expression of MMP2 and MMP9 genes, causing metastasis in ovarian and colon cancer. Methods: Bacterial strains and cell lines, the construction of an expression vector, and preparation of recombinant protein were done. Then, they were evaluated by Western blot, cell culture, cell viability assay, and reverse transcriptase-polymerase chain reaction. Results: The effects of arazyme on ovarian and colon cell lines were assessed by the MTT assay showing that the viability of cancer cells treated with arazyme decreased significantly in comparison with control cells. Also, RT-PCR showed that the expression of MMP2 and MMP9 genes decreased after treatment with arazyme, which was significant when compared to the results of pre-treatment. Conclusions: In this study, the results showed that the use of arazyme protein as a bacterial anti-protease can play a significant role in reducing the expression of metastatic genes. According to numerous studies on the role of bacterial proteases in the process of metastasis in recent years, this method can be considered as a therapeutic approach in reducing the metastatic process.

scholarly journals Bacteriophages M13 and T4 Increase the Expression of Anchorage-Dependent Survival Pathway Genes and Down Regulate Androgen Receptor Expression in LNCaP Prostate Cell Line

Viruses ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1754
Author(s):  
Swapnil Ganesh Sanmukh ◽  
Nilton José dos Santos ◽  
Caroline Nascimento Barquilha ◽  
Maira Smaniotto Cucielo ◽  
Márcio de Carvalho ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cell Line ◽  
Receptor Expression ◽  
Epithelial Cell Line ◽  
Lncap Cells ◽  
Cell Viability Assay ◽  
Prostate Cell ◽  
Growth And Survival ◽  
Viability Assay ◽  
Bacteriophage M13

Wild-type or engineered bacteriophages have been reported as therapeutic agents in the treatment of several types of diseases, including cancer. They might be used either as naked phages or as carriers of antitumor molecules. Here, we evaluate the role of bacteriophages M13 and T4 in modulating the expression of genes related to cell adhesion, growth, and survival in the androgen-responsive LNCaP prostatic adenocarcinoma-derived epithelial cell line. LNCaP cells were exposed to either bacteriophage M13 or T4 at a concentration of 1 × 105 pfu/mL, 1 × 106 pfu/mL, and 1 × 107 pfu/mL for 24, 48, and 72 h. After exposure, cells were processed for general morphology, cell viability assay, and gene expression analyses. Neither M13 nor T4 exposure altered cellular morphology, but both decreased the MTT reduction capacity of LNCaP cells at different times of treatment. In addition, genes AKT, ITGA5, ITGB1, ITGB3, ITGB5, MAPK3, and PI3K were significantly up-regulated, whilst the genes AR, HSPB1, ITGAV, and PGC1A were down-regulated. Our results show that bacteriophage M13 and T4 interact with LNCaP cells and effectively promote gene expression changes related to anchorage-dependent survival and androgen signaling. In conclusion, phage therapy may increase the response of PCa treatment with PI3K/AKT pathway inhibitors.

scholarly journals Antihistamines and Ovarian Cancer Survival: Nationwide Cohort Study and in Vitro Cell Viability Assay

2019 ◽  
Vol 112 (9) ◽  
pp. 964-967 ◽  
Author(s):  
Freija Verdoodt ◽  
Christian Dehlendorff ◽  
Marja Jäättelä ◽  
Robert Strauss ◽  
Anton Pottegård ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cell Death ◽  
Cohort Study ◽  
Cell Viability ◽  
Cancer Patients ◽  
Cancer Mortality ◽  
Specific Cell ◽  
Cell Viability Assay ◽  
Viability Assay

Abstract Antihistamines with cationic amphiphilic drug (CAD) characteristics induce cancer-specific cell death in experimental studies. Epidemiologic evidence is, however, limited. In a Danish nationwide cohort of ovarian cancer patients diagnosed during 2000–2015 (n = 5075), we evaluated the association between filled antihistamine prescriptions and cancer mortality. We used Cox regression models to estimate hazard ratios (HRs) with 95% confidence intervals (CIs) for ovarian cancer mortality. In an in vitro cell viability assay, we evaluated cell death in three ovarian cancer cell lines after treatment with clinically relevant doses of eight antihistamines. In our cohort study, CAD antihistamine use (≥1 prescription; n = 133) was associated with a hazard ratio of 0.63 (95% CI = 0.40 to 0.99) compared to use of non-CAD antihistamines (n = 304), and we found a tendency toward a dose-response association. In our cell viability assay, we found consistent and dose-dependent cytotoxicity for all CAD but not non-CAD antihistamines. In this nationwide cohort study, use of antihistamines with CAD characteristics is associated with a prognostic benefit in ovarian cancer patients.

Glucocorticoid receptor expression is associated with inferior overall survival independent of BRCA mutation status in ovarian cancer

2019 ◽  
Vol 29 (2) ◽  
pp. 357-364 ◽  
Author(s):  
Jennifer Taylor Veneris ◽  
Lei Huang ◽  
Jane E Churpek ◽  
Suzanne D Conzen ◽  
Gini F Fleming
Keyword(s):  
Gene Expression ◽  
Ovarian Cancer ◽  
Overall Survival ◽  
Glucocorticoid Receptor ◽  
Cancer Patients ◽  
Brca Mutation ◽  
Receptor Expression ◽  
High Grade ◽  
Mutation Status ◽  
Relationship Of

ObjectiveHigh glucocorticoid receptor (GR) protein expression is associated with decreased progression-free survival in ovarian cancer patients and decreased sensitivity to chemotherapy in preclinical models. Prior studies suggest wild type BRCA1 promotes GR activation. The objective of this study was to characterize the relationship of tumor GR gene expression to outcome in ovarian cancer, and to evaluate the relationship of GR expression with BRCA status.MethodsWhole exome and whole genome sequencing, gene expression, and clinical data were obtained for high-grade serous ovarian cancers in The Cancer Genome Atlas. Cases with pathogenic somatic or germline BRCA1 or BRCA2 mutations were identified and classified as BRCA mutated. High or low glucocorticoid receptor expression was defined as expression above or below median of the GR/nuclear receptor subfamily 3 C1 (NR3C1) gene level. Overall survival was estimated by the Kaplan-Meier method and compared by Cox regression analysis.ResultsCombined germline DNA sequencing and tumor microarray expression data were available for 222 high-grade serous ovarian cancer cases. Among these, 47 had a deleterious germline and/or somatic mutation in BRCA1 or BRCA2. In multivariate analysis, high glucocorticoid receptor gene expression was associated with decreased overall survival among ovarian cancer patients, independently of BRCA mutation status. No correlation of GR/NR3C1 gene expression with BRCA mutation status or BRCA1 or BRCA2 mRNA level was observed.ConclusionsIncreased GR gene expression is associated with decreased overall survival in ovarian cancer patients, independently of BRCA mutation status. High-grade serous ovarian cancers with high GR expression and wild type BRCA have a particularly poor outcome.

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