scholarly journals Novel Cell-Based Assay to Investigate Monoacylglycerol Acyltransferase 2 Inhibitory Activity Using HIEC-6 Cell Line

ACS Omega ◽  
2021 ◽  
Author(s):  
Yeshvanthi Singh ◽  
Akshay Datey ◽  
Dipshikha Chakravortty ◽  
Ajay W. Tumaney
Keyword(s):  
Cell Line ◽  
Inhibitory Activity ◽  
Monoacylglycerol Acyltransferase

scholarly journals A New CDK2 Inhibitor with 3-Hydrazonoindolin-2-One Scaffold Endowed with Anti-Breast Cancer Activity: Design, Synthesis, Biological Evaluation, and In Silico Insights

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 412
Author(s):  
Mohammad M. Al-Sanea ◽  
Ahmad J. Obaidullah ◽  
Mohamed E. Shaker ◽  
Garri Chilingaryan ◽  
Mohammed M. Alanazi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Flow Cytometric Analysis ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Intrinsic Activity ◽  
Binding Interaction ◽  
Mcf 7

Background: Cyclin-dependent kinases (CDKs) regulate mammalian cell cycle progression and RNA transcription. Based on the structural analysis of previously reported CDK2 inhibitors, a new compound with 3-hydrazonoindolin-2-one scaffold (HI 5) was well designed, synthesized, and biologically evaluated as a promising anti-breast cancer hit compound. Methods: The potential anti-cancerous effect of HI 5 was evaluated using cytotoxicity assay, flow cytometric analysis of apoptosis and cell cycle distribution, ELISA immunoassay, in vitro CDK2/cyclin A2 activity, and molecular operating environment (MOE) virtual docking studies. Results: The results revealed that HI 5 exhibits pronounced CDK2 inhibitory activity and cytotoxicity in human breast cancer MCF-7 cell line. The cytotoxicity of HI 5 was found to be intrinsically mediated apoptosis, which in turn, is associated with low Bcl-2 expression and high activation of caspase 3 and p53. Besides, HI 5 blocked the proliferation of the MCF-7 cell line and arrested the cell cycle at the G2/M phase. The docking studies did not confirm which one of geometric isomers (syn and anti) is responsible for binding affinity and intrinsic activity of HI 5. However, the molecular dynamic studies have confirmed that the syn-isomer has more favorable binding interaction and thus is responsible for CDK2 inhibitory activity. Discussion: These findings displayed a substantial basis of synthesizing further derivatives based on the 3-hydrazonoindolin-2-one scaffold for favorable targeting of breast cancer.

scholarly journals Bioactive Compounds and Antioxidative, Antileukemic and Anti-MMPs Activity of Eleutherococcus Species Cultivated in Poland

2012 ◽  
Vol 7 (11) ◽  
pp. 1934578X1200701
Author(s):  
Daniel Załuski ◽  
Helena D. Smolarz ◽  
Urszula Gawlik-Dziki
Keyword(s):  
Biological Activity ◽  
Cell Line ◽  
Bioactive Compounds ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Apoptotic Cells ◽  
Biological Studies ◽  
Dpph Activity ◽  
Leaves And Roots

The content of phenols (TPC), and the antioxidative, antileukemic and anti-MMPs properties of Eleutherococcus spp. cultivated in Poland are reported. The highest TPC was found in the spring leaves (20.3 – 37.2 mg/g). The spring leaves and roots of E. divaricatus had the strongest anti-DPPH activity (EC50 1.2 and 1.2 mg/mL), whereas the greatest ability of iron (II) chelating was shown by autumn leaves of E. setchuensis (EC50 0.3 mg/mL), and the ethanolic extract of E. gracilistylus roots showed the strongest lipid antiperoxidation activity (EC50 0.7 mg/mL). The highest number of apoptotic cells was observed in the Jurkat 45 cell line after treatment with the ethanolic extract of E. sessiliflorus roots (27%). Only the chloroform extracts of roots of E. gracilistylus and E. divaricatus showed the inhibitory activity against MMPs. Most of the studied species have a significant biological activity that is probably due to the presence of phenols. To the best of our knowledge, neither detailed phytochemical nor biological studies have been performed for most of the investigated species.

P-Glycoprotein Inhibitory Activity of Lipophilic Constituents of Echinacea pallida Roots in a Human Proximal Tubular Cell Line

Planta Medica ◽  
2008 ◽  
Vol 74 (3) ◽  
pp. 264-266 ◽  
Author(s):  
Nadia Romiti ◽  
Federica Pellati ◽  
Paola Nieri ◽  
Stefania Benvenuti ◽  
Barbara Adinolfi ◽  
...  
Keyword(s):  
Cell Line ◽  
Inhibitory Activity ◽  
Proximal Tubular Cell ◽  
Tubular Cell ◽  
P Glycoprotein ◽  
Echinacea Pallida ◽  
Proximal Tubular

scholarly journals E-Cadherin Suppresses Cellular Transformation by Inhibiting β-Catenin Signaling in an Adhesion-Independent Manner

2001 ◽  
Vol 153 (5) ◽  
pp. 1049-1060 ◽  
Author(s):  
Cara J. Gottardi ◽  
Ellen Wong ◽  
Barry M. Gumbiner
Keyword(s):  
Tumor Suppressor ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Growth Suppression ◽  
Binding Region ◽  
Suppressor Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Sw480 Cells ◽  
E Cadherin

E-cadherin is a tumor suppressor protein with a well-established role in cell–cell adhesion. Adhesion could contribute to tumor suppression either by physically joining cells or by facilitating other juxtacrine signaling events. Alternatively, E-cadherin tumor suppressor activity could result from binding and antagonizing the nuclear signaling function of β-catenin, a known proto-oncogene. To distinguish between an adhesion- versus a β-catenin signaling–dependent mechanism, chimeric cadherin constructs were expressed in the SW480 colorectal tumor cell line. Expression of wild-type E-cadherin significantly inhibits the growth of this cell line. Growth inhibitory activity is retained by all constructs that have the β-catenin binding region of the cytoplasmic domain but not by E-cadherin constructs that exhibit adhesive activity, but lack the β-catenin binding region. This growth suppression correlates with a reduction in β-catenin/T cell factor (TCF) reporter gene activity. Importantly, direct inhibition of β-catenin/TCF signaling inhibits the growth of SW480 cells, and the growth inhibitory activity of E-cadherin is rescued by constitutively activated forms of TCF. Thus, the growth suppressor activity of E-cadherin is adhesion independent and results from an inhibition of the β-catenin/TCF signaling pathway, suggesting that loss of E-cadherin expression can contribute to upregulation of this pathway in human cancers. E-cadherin–mediated growth suppression was not accompanied by overall depletion of β-catenin from the cytosol and nucleus. This appears to be due to the existence of a large pool of cytosolic β-catenin in SW480 cells that is refractory to both cadherin binding and TCF binding. Thus, a small pool of β-catenin that can bind TCF (i.e., the transcriptionally active pool) can be selectively depleted by E-cadherin expression. The existence of functionally distinct pools of cytosolic β-catenin suggests that there are mechanisms to regulate β-catenin signaling in addition to controlling its level of accumulation.

scholarly journals Extract of Solidago chilensis Meyen inflorescences: cytotoxicity and inhibitory activity on nitric oxide synthesis in activated macrophage cell line J774A.1

2020 ◽  
Vol 56 ◽  
Author(s):  
Thais Morais de Brito ◽  
Fabio Coelho Amendoeira ◽  
Temistocles Barroso de Oliveira ◽  
Valber da Silva Frutuoso ◽  
Fausto Klabund Ferraris ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Nitric Oxide Synthesis ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Activated Macrophage ◽  
Solidago Chilensis

Synthesis ofβ-Ketosulfone Derivatives As New Non-Cytotoxic Urease InhibitorsIn Vitro

2020 ◽  
Vol 16 (2) ◽  
pp. 244-255 ◽  
Author(s):  
Sarosh Iqbal ◽  
Ajmal Khan ◽  
Rashid Nazir ◽  
Shumaila Kiran ◽  
Shahnaz Perveen ◽  
...  
Keyword(s):  
Peptic Ulcer ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Medicinal Chemistry ◽  
Urease Inhibitors ◽  
Urease Inhibition ◽  
Chemistry Research ◽  
Ic50 Values ◽  
Urease Inhibitory

Background:Peptic ulcer and urolithiasis are largely due to infection caused by ureaseproducing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research.Objective:The main aim of the work was to identify novel urease inhibitors with no cytotoxicity.Method:During the current study, a series of β-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential.Results:Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 µM, in comparison to standard thiourea (IC50 = 21 ± 0.11 µM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line.Conclusion:This study has identified β-ketosulfones as novel and non-cytotoxic urease inhibitors.

A small molecular mass inhibitor of growth of 3T3 cells and porcine aortic smooth muscle cells released from the macrophage cell line P388D1

1993 ◽  
Vol 106 (4) ◽  
pp. 1301-1311 ◽  
Author(s):  
H.F. McMurray ◽  
D. Proudfoot ◽  
J.B. Davis ◽  
D.P. Parrott ◽  
D.E. Bowyer
Keyword(s):  
Smooth Muscle ◽  
Smooth Muscle Cells ◽  
Molecular Mass ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Transforming Growth Factor ◽  
Muscle Cells ◽  
Tgf Beta ◽  
Aortic Smooth Muscle Cells ◽  
Aortic Smooth Muscle

Murine peritoneal macrophages and the macrophage-like cell line, P388D1, were found to release both mitogenic and inhibitory modulators of growth of cells in culture. These growth factors were effective against both murine Swiss 3T3 fibroblasts and porcine aortic smooth muscle cells as assessed by [3H]thymidine incorporation into DNA and by measurement of cell number. Partial characterisation of the inhibitory activity demonstrated it to be lost on dialysis using a membrane with a 10 kDa cut-off, trypsin sensitive, heat stable, and slightly sensitive to freeze-thawing. The inhibitory activity not only affected cell growth but was found to change the morphology of porcine aortic smooth muscle cells. Gel permeation studies showed an estimated molecular mass in the range 2.5 to 6.5 kDa. The inhibitory activity could be partially purified using ion-exchange chromatography. Experiments with a neutralising antibody against transforming growth factor beta (TGF-beta) showed that TGF-beta is not responsible for the activity observed. Indomethacin had no effect on the production of inhibitor suggesting that it is not an inhibitory prostanoid. The inhibitory activity was not due to a non-specific toxic mechanism as confirmed by a [3H]adenine release assay. Incubation of P388D1 cells with cycloheximide prevented the release of inhibitory activity.

Isolation and structure of the unusual Indian Ocean Cephalodiscusgilchristi components, cephalostatins 5 and 6

1989 ◽  
Vol 67 (10) ◽  
pp. 1509-1513 ◽  
Author(s):  
George R. Pettit ◽  
Yoshiaki Kamano ◽  
Claude Dufresne ◽  
Masuo Inoue ◽  
Nigel Christie ◽  
...  
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Magnetic Resonance ◽  
Indian Ocean ◽  
Cell Line ◽  
South African ◽  
Inhibitory Activity ◽  
Lymphocytic Leukemia ◽  
Two Dimensional ◽  
P388 Cell ◽  
The Indian Ocean

The Indian Ocean (South African) marine worm Cephalodiscusgilchristi (Hemichordata phylum) has been found to contain a series of unusual disteroidal alkaloids, designated the cephalostatins, that possess exceptionally potent lymphocytic leukemia (murine P388) cell line inhibitory activity (to ED50 10−9 μg/mL). Two of the less prominent members with P388 ED50 10−3–10−2 μg/mL, cephalostatins 5 (2) and 6 (3), were isolated and assigned structures based on rigorous interpretation of two-dimensional 400-MHz 1H and 13C nuclear magnetic resonance. Keywords: cephalostatins 5 and 6, disteroidal alkaloids, lymphocytic leukemia, cytostatic, Cephalodiscusgilchristi.

Sign in / Sign up

Export Citation Format

Share Document