Spatio-Temporal Cell Cycle Analysis Using 3D Level Set Segmentation of Unstained Nuclei in Line Scan Confocal Fluorescence Images

The article entitled “Improved Level Set Segmentation Algorithm Based on Kernel Fuzzy Particles Swarm Optimization (KFPSO) Clustering for MRI Images”, by G. Elaiyaraja, P. Epsiba, N. Kumaratharan and G. Suresh, has been retracted. Kindly see Bentham Science Policy on Article retraction at the link given below: (https://www.benthamscience.com/journals/current-medical-imaging/author-guidelines/). This article has been retracted on the request of the Editor. The authors have plagiarized a paper that had already been published in the journal Current Medical Imaging (CMIM) (Formerly: Current Medical Imaging Reviews) 14(3), Page: 389-400. http://www.eurekaselect.com/149444. It is a pre-requisite for authors to declare explicitly that their work is original and has not been published elsewhere. Authors are advised to properly cite the original source to avoid plagiarism and copyright violation. As such this article represents a severe abuse of the scientific publishing system. Bentham Science Publishers takes a very strong view on this matter and apologizes to the readers of the journal for any inconvenience this may cause.

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Identification and Expression Analysis of CD73 Inhibitors in Cervical Cancer

Medicinal Chemistry ◽

10.2174/1573406416666200925141703 ◽

2020 ◽

Vol 16 ◽

Author(s):

Jamshed Iqbal ◽

Ayesha Basharat ◽

Sehrish Bano ◽

Syed Mobasher Ali Abid ◽

Julie Pelletier ◽

...

Keyword(s):

Cell Cycle ◽

Cervical Cancer ◽

Western Blot ◽

Hela Cell ◽

Cell Line ◽

Cell Apoptosis ◽

Immunofluorescence Staining ◽

Cell Cycle Analysis ◽

Hela Cell Line ◽

Cell Line Hela

Aims: The present study was conducted to examine the inhibitory effects of synthesized sulfonylhydrazones on the expression of CD73 (ecto-5′-NT). Background: CD73 (ecto-5′-NT) represents the most significant class of ecto-nucleotidases which are mainly responsible for dephosphorylation of adenosine monophosphate to adenosine. Inhibition of CD73 played an important role in the treatment of cancer, autoimmune disorders, precancerous syndromes, and some other diseases associated with CD73 activity. Objective: Keeping in view the significance of CD73 inhibitor in the treatment of cervical cancer, a series of sulfonylhydrazones (3a-3i) derivatives synthesized from 3-formylchromones were evaluated. Methods: All sulfonylhydrazones (3a-3i) were evaluated for their inhibitory activity towards CD73 (ecto-5′-NT) by the malachite green assay and their cytotoxic effect was investigated on HeLa cell line using MTT assay. Secondly, most potent compound was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis. After that, CD73 mRNA and protein expression were analyzed by real-time PCR and Western blot. Results: Among all compounds, 3h, 3e, 3b, and 3c were found the most active against rat-ecto-5′-NT (CD73) enzyme with IC50 (µM) values of 0.70 ± 0.06 µM, 0.87 ± 0.05 µM, 0.39 ± 0.02 µM and 0.33 ± 0.03 µM, respectively. These derivatives were further evaluated for their cytotoxic potential against cancer cell line (HeLa). Compound 3h and 3c showed the cytotoxicity at IC50 value of 30.20 ± 3.11 µM and 86.02 ± 7.11 µM, respectively. Furthermore, compound 3h was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis which showed promising apoptotic effect in HeLa cells. Additionally, compound 3h was further investigated for its effect on expression of CD73 using qRT-PCR and western blot. Conclusion: Among all synthesized compounds (3a-3i), Compound 3h (E)-N'-((6-ethyl-4-oxo-4H-chromen-3-yl) methylene)-4-methylbenzenesulfonohydrazide was identified as most potent compound. Additional expression studies conducted on HeLa cell line proved that this compound successfully decreased the expression level of CD73 and thus inhibiting the growth and proliferation of cancer cells.

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Novel Anthraquinone Derivatives as Dual Inhibitors of Topoisomerase 2 and Casein Kinase 2: In Silico Studies, Synthesis and Biological Evaluation on Leukemic Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180423111309 ◽

2019 ◽

Vol 18 (11) ◽

pp. 1551-1562 ◽

Cited By ~ 4

Author(s):

Abbas Kabir ◽

Kalpana Tilekar ◽

Neha Upadhyay ◽

C.S. Ramaa

Keyword(s):

Cell Cycle ◽

Cell Line ◽

Cell Lines ◽

Biological Evaluation ◽

Casein Kinase ◽

Casein Kinase 2 ◽

Cell Cycle Analysis ◽

Protein Targets ◽

Topoisomerase 2 ◽

Dual Inhibitors

Background: Cancer being a complex disease, single targeting agents remain unsuccessful. This calls for “multiple targeting”, wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) helps in removing DNA tangles and super-coiling during cellular replication, Casein Kinase 2 (CK2) is involved in the phosphorylation of a multitude of protein targets. Thus, in the present work, we have tried to develop dual inhibitors of Top2 and CK2. Objective: With this view, in the present work, 2 human proteins, Top2 and CK2 have been targeted to achieve the anti-proliferative effects. Methods: Novel 1-acetylamidoanthraquinone (3a-3y) derivatives were designed, synthesized and their structures were elucidated by analytical and spectral characterization techniques (FTIR, 1H NMR, 13C NMR and Mass Spectroscopy). The synthesized compounds were then subjected to evaluation of cytotoxic potential by the Sulforhodamine B (SRB) protein assay, using HL60 and K562 cell lines. Ten compounds were analyzed for Top2, CK2 enzyme inhibitory potential. Further, top three compounds were subjected to cell cycle analysis. Results: The compounds 3a to 3c, 3e, 3f, 3i to 3p, 3t and 3x showed excellent cytotoxic activity to HL-60 cell line indicating their high anti-proliferative potential in AML. The compounds 3a to 3c, 3e, 3f, 3i to 3p and 3y have shown good to moderate activity on K-562 cell line. Compounds 3e, 3f, 3i, 3x and 3y were found more cytotoxic than standard doxorubicin. In cell cycle analysis, the cells (79-85%) were found to arrest in the G0/G1 phase. Conclusion: We have successfully designed, synthesized, purified and structurally characterized 1- acetylamidoanthraquinone derivatives. Even though our compounds need design optimization to further increase enzyme inhibition, their overall anti-proliferative effects were found to be encouraging.

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Enhanced Anticancer Activity and Apoptosis Effect of Bioactive Compound Quercetin Extracted from Ocimum sanctum Leaves

Current Nanomedicine ◽

10.2174/2468187310999201117155414 ◽

2020 ◽

Vol 10 ◽

Author(s):

Amutha Santhanam ◽

Naveen Kumar Chandrasekharan ◽

Rajangam Ilangovan

Keyword(s):

Cell Cycle ◽

Anticancer Activity ◽

Cancer Cells ◽

Leaf Extract ◽

Nickel Nanoparticles ◽

Bioactive Compound ◽

Cell Cycle Analysis ◽

Ocimum Sanctum ◽

Sem Images ◽

Ft Ir

Background: The occurrence of Cancer results in cellular changes that causes the uncontrolled growth and division of cells. Apoptosis removes cells during development and eliminates the potentially cancerous cells. The bioactive compounds present in the herbal plant shows cytotoxic activity that result in apoptosis. The traditional herbal plants are used world-wide both in allopathy and other traditional ways. Objective: The main objective of this study is to extract the bioactive compound Quercetin from the medicinally significant plant Ocimum sanctum and also to develop nanomedicine as Qu-PEG-NiGs. Materials and Methods: Leaf extract of the medicinally significant plant Ocimum sanctum (O. sanctum) has been used for the synthesis of nickel nanoparticles (NiGs) and extraction of quercetin (Qu). The ethanolic extract of Ocimum sanctum is added to 1 mM Nickel Nitrate (Ni(NO3)2) and stirred for 3 hrs at RT and dried at 60°C for 3hrs and calcinated at 400°C for 2hrs and characterized using Uv-Vis Spectrophotometer, FT-IR, SEM, DLS and Zeta potential. The Quercetin is isolated from Ocimum sanctum leaf extract using the reflux condenser method. The bio-polymer is being PEG-coated over NiGs and Quercetin is loaded into it. The apoptosis activity using MCF-7 cells is performed with Qu-PEG-NiGs. The purity of Quercetin is characterized using HPLC. In order to analyse apoptosis efficiency, MTT assay, Reactive Oxygen Species (ROS), Cell cycle analysis has been performed. Results: The NiGs absorption spectrum gives a peak at 408nm. The FT-IR confirms the presence of particular functional groups shifting from the compound NiGs and then coated with PEG-Qu-NiGs. The SEM images show the size of NiGs ranging from 27.3 nm to 40.4 nm with varied morphology such as hexagonal and other irregular shapes. The presence of Quercetin extracted from the leaf powder is approximately 1.5 mg/g. The ROS results show the Qu-PEG-NiGs induced efficiency of the apoptosis, while the increased concentrations promote ROS and lead to activation of the apoptosis. The cell cycle analysis has shown the cytotoxic effect. Conclusion: PEG-coated nickel nanoparticles can be used as a promising chemotherapeutic agent against MCF7 breast cancer cells. It is the evidence to further studies for evaluating Qu-PEG-NiGs anticancer activity on different types of cancer cells.

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