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.

scholarly journals Antimelanoma and Antityrosinase fromAlpinia galangalConstituents

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Chih-Yu Lo ◽  
Po-Len Liu ◽  
Li-Ching Lin ◽  
Yen-Ting Chen ◽  
You-Cheng Hseu ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cell Line ◽  
Food Industry ◽  
Human Melanoma ◽  
Therapeutic Application ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Anticancer Effects ◽  
Spectroscopic Analyses ◽  
Melanin Contents

Two compounds, 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (BHPHTO) and bisdemethoxycurcumin (BDMC) they have been isolated from the rhizomes ofAlpinia galangal, and the structures of both pure constituents were determined using spectroscopic analyses. The study examined the bioeffectivenesses of the two compounds on the human melanoma A2058 and showed that significantly inhibited the proliferation of melanoma cells in the cell viability assay. This research was also taken on the tests to B16-F10 cell line and showed minor inhibitory consequences of cellular tyrosinase activities and melanin contents. Our results revealed the anticancer effects ofA. galangalcompounds, and therefore, the target compounds could be potentially applied in the therapeutic application and the food industry.

scholarly journals Bryostatin I inhibits growth of breast cancer cells through the inhibition of synuclein-A expression

2016 ◽  
Vol 11 (3) ◽  
pp. 615 ◽  
Author(s):  
Jun-Xia Sun ◽  
Yan Yan ◽  
Jian-Hong Xia ◽  
Li-Qing Zhou
Keyword(s):  
Breast Cancer ◽  
Cell Viability ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Video Clip ◽  
Inhibitory Effect ◽  
Oncostatin M ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Induced Apoptosis

<p class="Abstract">The present study was aimed to investigate the effect of bryostatin I on the expression of synuclein-A in breast cancer cells. Western blot analysis showed a significant (p&lt;0.005) reduction in the expression of synuclein-A from a concentration of 20 µM in H3922 cells. The inhibitory effect of bryostatin I on synuclein-A expression was further confirmed by the treatment of H3922 cells with known synuclein-A inhibitor, cytokine oncostatin M. Bryostatin I treatment of H3922 cells also significantly increased their sensitivity to the taxol. Incubation of the cells with 25 µM concentration of bryostatin I followed by treatment with 0.5 μM concentration of taxol induced apoptosis in 89% cells compared to 9% cells in the taxol alone treated cultures. Treatment of the H3922 cells with bryostatin I at 25 µM concentration led to a significant increase in the activation of histone H1 protein. The results from MTT assay showed a significant decrease in the cell viability from 10 µM concentration of bryostatin I. Thus, bryostatin I inhibits the growth of breast cancer cells through inhibition of synuclein-A expression and can be used for breast cancer treatment.</p><p><strong>Video Clip</strong></p><p><a href="https://youtube.com/v/VzeWcEMjrJA">Cell viability assay:</a> 5 min 14 sec </p>

scholarly journals Preparation, Characterization, and Anticancer Effects of Capsaicin-Loaded Nanoliposomes

Nutrients ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 3995
Author(s):  
Ali Al-Samydai ◽  
Walhan Alshaer ◽  
Emad A. S. Al-Dujaili ◽  
Hanan Azzam ◽  
Talal Aburjai
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Therapeutic Potential ◽  
Drug Loading ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Anticancer Effects ◽  
Pharmacokinetic Properties ◽  
Quantitative Analyses

Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.

scholarly journals Triptolide Enhances Chemotherapeutic Accumulation Through P-Gp Inhibition in Cisplatin-Resistant HNE1/DDP Nasopharyngeal Cancer Cells

2021 ◽  
Author(s):  
Xiu Wang ◽  
Yu-shuai Wang ◽  
Jing-jing Zhang ◽  
Jian-chun Li
Keyword(s):  
Cell Viability ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Nasopharyngeal Cancer ◽  
Underlying Mechanism ◽  
Drug Resistant ◽  
Cell Viability Assay ◽  
Atp Level ◽  
Viability Assay ◽  
And Function

Abstract Background: We have previously shown that triptolide (TPL) could synergize with cisplatin (DDP) in drug-resistant nasopharyngeal cancer cells (NPC). However, the underlying mechanism remains elusive. Therefore, we hypothesized that TPL could inhibit P-glycoprotein (P-gp) expression, reduce the chemotherapeutic agent efflux from tumor cells and increase their drug content, then by increasing drug efficiency against the tumor cells. So the study was performanced to elucidate the mechanism of triptolide (TPL) sensitization with chemotherapeutics in drug-resistant nasopharyngeal cancer cells. Methods and Results:Cell viability was analyzed by MTT. The apoptosis and intracellular concentration of doxorubicin/rhodanmine123 were determined by flow cytometry. The expression of P-gp, MRP1, Caspse-3, CAP1, and CAP2 were measured by western blot. The ATP level was examined by Cell Titer-Glo Luminescent Cell Viability Assay kit. The results showed that TPL inhibited cell viability, increased apoptosis, and intracellular doxorubicin accumulation. Furthermore, TPL inhibited the rhodanmine123 efflux, reduced the ATP level and the expression of P-gp, MRP1, and CAP1, while it increased the expression of CAP2 and Caspase-3. Conclusions:The results of this study confirm the role of TPL in restoring the sensitivity of cancer cells to chemotherapeutics by down regulating P-gp expression and function in drug-resistant nasopharyngeal cancer cells.

scholarly journals Noninvasive and Safe Cell Viability Assay for Breast Cancer MCF-7 Cells Using Natural Food Pigment

Biology ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 227
Author(s):  
Kyohei Yamashita ◽  
Ryoma Tagawa ◽  
Yoshikazu Higami ◽  
Eiji Tokunaga
Keyword(s):  
Breast Cancer ◽  
Cell Viability ◽  
Cancer Cells ◽  
Living Cells ◽  
Natural Food ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
A Cell ◽  
Reduced Nicotinamide Adenine Dinucleotide ◽  
Mcf 7

A dye exclusion test (DET) was performed to determine the viability of human breast cancer cells MCF-7, using natural food pigments as compared with trypan blue (TB), a typical synthetic dye for DET known to exhibit teratogenicity and cytotoxicity. We demonstrated that Monascus pigment (MP) is noninvasive to living cells and can effectively stain only dead cells. This study is the first verification of the applicability of MP to cancer cells. The appropriate MP concentration was 0.4% (0.02% as the concentration of pure MP) and all the dead cells were stained within 10 min. We found that the cell proliferation or the reduced nicotinamide adenine dinucleotide (NADH) activity of living cells was maintained over 48 h. Although 0.1% TB did not show an increase in dead cells, a marked decrease in NADH activity was confirmed. In addition, even when MP coexisted with cisplatin, staining of dead cells was maintained for 47 h, indicating stability to drugs (reagents). The cost of MP is estimated to be about 1/10 of TB. The fact that MP can be used as a cell viability determination reagent for Euglena and Paramecium, as shown in preceding papers, and also for MCF-7, as shown in this paper, indicates the possibility of application in more cells of different species.

Three Pt-Pt Complexes with Donor-acceptor Feature: Anticancer Activity, DNA Binding Studies and Molecular Docking Simulation

2019 ◽  
Vol 19 (14) ◽  
pp. 1762-1774 ◽  
Author(s):  
Pezhman Ashoo ◽  
Reza Yousefi ◽  
Syed M. Nabavizadeh ◽  
Marzieh D. Aseman ◽  
Sareh Paziresh ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Dna Binding ◽  
Cell Viability ◽  
Anticancer Activity ◽  
Docking Simulation ◽  
Platinum Complexes ◽  
Binding Studies ◽  
Cell Viability Assay ◽  
Molecular Docking Simulation ◽  
Viability Assay

Background: Due to their unique properties and potential applications in variety of areas, recently, a special attention is given to the binuclear platinum (II) complexes. They reveal a highly tunable features upon the modification of their cyclometallating and bridging ligands. Objective: The aim of this study was to evaluate the anticancer activity and DNA binding affinity of three binuclear platinum (II) complexes, including ht-[(p-FC6H4)Pt(µ-PN)(µ-NP)PtMe2](CF3CO2)(1), ht-[(p- MeC6H4)Pt(µ-PN)(μ-NP)Pt(p MeC6H4) Me] (CF3CO2)(2) and ht-[Pt2Me3(µ-PN)2](CF3CO2) (3). Methods: MTT assay was performed to study the cell viability of Jurkat and MCF-7 lines against synthesized complexes, followed by apoptosis detection experiments. Several spectroscopic methods with molecular docking simulation were also used to investigate the detail of interaction of these platinum complexes with DNA. Results: Cell viability assay demonstrated a notable level of cytotoxicity for the synthetic platinum complexes. Further studies proved that a pathway of cell signaling initiating the apoptosis might be activated by these complexes, particularly in the case of complexes 1 and 2. The results of both UV-visible and CD measurements showed the significant ability of these complexes to interact with DNA. While fluorescence data revealed that these complexes cannot enter DNA structure by intercalation, molecular docking assessment proved their DNA groove binding ability. Conclusion: The remarkable apoptosis inducing activity of the binuclear platinum complexes 1 and 2 and their considerable interaction with DNA suggest them as the potential antitumor medicines.

Do We have a Satisfactory Cell Viability Assay? Review of the Currently Commercially-Available Assays

2020 ◽  
Vol 17 (1) ◽  
pp. 2-22 ◽  
Author(s):  
Abdel-Baset Halim
Keyword(s):  
Cell Viability ◽  
Data Interpretation ◽  
Positive Control ◽  
Live Cells ◽  
Proof Of Concept ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Current Cell ◽  
Dying Cells ◽  
Differential Permeability

:Cell-based assays are an important part of the drug discovery process and clinical research. One of the main hurdles is to design sufficiently robust assays with adequate signal to noise parameters while maintaining the inherent physiology of the cells and not interfering with the pharmacology of target being investigated.:A plethora of assays that assess cell viability (or cell heath in general) are commercially available and can be classified under different categories according to their concepts and principle of reactions. The assays are valuable tools, however, suffer from a large number of limitations. Some of these limitations can be procedural or operational, but others can be critical as those related to a poor concept or the lack of proof of concept of an assay, e.g. those relying on differential permeability of dyes in-and-out of viable versus compromised cell membranes. While the assays can differentiate between dead and live cells, most, if not all, of them can just assess the relative performance of cells rather than providing a clear distinction between healthy and dying cells. The possible impact of relatively high molecular weight dyes, used in most of the assay, on cell viability has not been addressed. More innovative assays are needed, and until better alternatives are developed, setup of current cell-based studies and data interpretation should be made with the limitations in mind. Negative and positive control should be considered whenever feasible. Also, researchers should use more than one orthogonal method for better assessment of cell health.

scholarly journals Promising biocompatible hydrogels of crosslinked polyelectrolytes for biomedical applications

2017 ◽  
Vol 3 (2) ◽  
pp. 695-698
Author(s):  
Andreas Brietzke ◽  
Christian von der Ehe ◽  
Sabine Illner ◽  
Claudia Matschegewski ◽  
Niels Grabow ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Ionic Liquids ◽  
Cell Viability ◽  
Biomedical Applications ◽  
High Potential ◽  
Cell Viability Assay ◽  
Mouse Fibroblasts ◽  
Viability Assay ◽  
Intelligent Implant ◽  
L929 Mouse

AbstractFor the development of intelligent implant systems hydrogels (HG) from crosslinked ionic liquids feature a high potential to be utilised as a drug depot. Biocompatibility of the HGs is one key prerequisite for biomedical applications. HGs were polymerised from a variety of different ionic monomers based on methacrylate, methacrylamide, styrene or vinyl imidazolium derivatives in aqueous solution. N,N'-methylenebisacrylamide was used as crosslinker. CellQuanti-Blue™ Cell Viability Assay Kit was implemented to proof viability of L929 mouse fibroblasts. The predominant part of the HG eluates generated only a marginal reduction of less than 15% cell viability at 100% eluate concentration. This underlines the excellent suitability of these HGs for biomedical applications and revealed some promising candidates for the development of drug depots for implants.

scholarly journals Sensitive cell viability assay for use in drug screens and for studying the mechanism of action of drugs inDictyostelium discoideum

BioTechniques ◽  
2006 ◽  
Vol 41 (5) ◽  
pp. 591-595 ◽  
Author(s):  
Junxia Min ◽  
Priya Sridevi ◽  
Stephen Alexander ◽  
Hannah Alexander
Keyword(s):  
Cell Viability ◽  
Mechanism Of Action ◽  
Sensitive Cell ◽  
Cell Viability Assay ◽  
Viability Assay
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