scholarly journals In Vitro Activity of Monofunctional Pt-II Complex Based on 8-Aminoquinoline against Human Glioblastoma

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2101
Author(s):  
Valentina Coccè ◽  
Isabella Rimoldi ◽  
Giorgio Facchetti ◽  
Emilio Ciusani ◽  
Giulio Alessandri ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Significant Activity ◽  
Glioblastoma Cell ◽  
Main Target ◽  
Human Carcinomas ◽  
A Minor ◽  
Glioblastoma Cell Lines ◽  
Minor Activity

A new cationic Pt(II) complex bearing 8-aminoquinoline as chelating ligand (called Pt-8AQ) was evaluated against two human carcinomas, one mesothelioma, and three glioblastoma cell lines. The in vitro comparison to the clinically approved CisPt showed a minor activity of Pt-8AQ against carcinoma and mesothelioma, whereas a significant activity of Pt-8AQ was observed on the proliferation of the three glioblastoma cell lines (U87-MG IC50 = 3.68 ± 0.69 µM; U373-MG IC50 = 11.53 ± 0.16 µM; U138-MG IC50 = 8.05 ± 0.23 µM) that was higher than that observed with the clinically approved CisPt (U87-MG IC50 = 7.27 + 1.80 µM; U373-MG IC50 = 22.69 ± 0.05 µM; U138-MG IC50 = 32.1 ± 4.44 µM). Cell cycle analysis proved that Pt-8AQ significantly affected the cell cycle pattern by increasing the apoptotic cells represented by the sub G0/G1 region related with a downregulation of p53 and Bcl-2. Moreover, an NMR investigation of Pt-8AQ interaction with 9-EtG, GSH, and Mets7 excluded DNA as the main target, suggesting a novel mechanism of action. Our study demonstrated the high stability of Pt-8AQ after incubation at 37 °C and a significant antineoplastic activity on glioblastomas. These features also make Pt-8AQ a good candidate for developing a new selective advanced cell chemotherapy approach in combination with MSCs.

In vitro and in vivo characterization of a novel hedgehog signaling antagonist in human glioblastoma cell lines

2012 ◽  
Vol 131 (2) ◽  
pp. E33-E44 ◽  
Author(s):  
Pietro Ferruzzi ◽  
Federica Mennillo ◽  
Antonella De Rosa ◽  
Cinzia Giordano ◽  
Marco Rossi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Hedgehog Signaling ◽  
Glioblastoma Cell ◽  
Human Glioblastoma ◽  
Human Glioblastoma Cell ◽  
In Vivo Characterization ◽  
Glioblastoma Cell Lines

Brefeldin A Induces Apoptosis and Cell Cycle Blockade in Glioblastoma Cell Lines

Oncology ◽  
2003 ◽  
Vol 64 (4) ◽  
pp. 459-467 ◽  
Author(s):  
Isabelle Pommepuy ◽  
Faraj Terro ◽  
Barbara Petit ◽  
Frank Trimoreau ◽  
Virginie Bellet ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Brefeldin A ◽  
Glioblastoma Cell ◽  
Glioblastoma Cell Lines

In vitro and in vivo evaluations of the tyrosine kinase inhibitor NSC�680410 against human leukemia and glioblastoma cell lines

2002 ◽  
Vol 50 (6) ◽  
pp. 479-489 ◽  
Author(s):  
Ioannis A. Avramis ◽  
Garyfallia Christodoulopoulos ◽  
Atsushi Suzuki ◽  
Walter E. Laug ◽  
Ignacio Gonzalez-Gomez ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitor ◽  
Cell Lines ◽  
Kinase Inhibitor ◽  
Human Leukemia ◽  
Glioblastoma Cell ◽  
Glioblastoma Cell Lines

scholarly journals Neutralization of Adrenomedullin Inhibits the Growth of Human Glioblastoma Cell Lines in Vitro and Suppresses Tumor Xenograft Growth in Vivo

2002 ◽  
Vol 160 (4) ◽  
pp. 1279-1292 ◽  
Author(s):  
L'Houcine Ouafik ◽  
Samantha Sauze ◽  
Françoise Boudouresque ◽  
Olivier Chinot ◽  
Christine Delfino ◽  
...  
Keyword(s):  
Cell Lines ◽  
Tumor Xenograft ◽  
Glioblastoma Cell ◽  
Human Glioblastoma ◽  
Human Glioblastoma Cell ◽  
Xenograft Growth ◽  
Tumor Xenograft Growth ◽  
Glioblastoma Cell Lines

Establishment and Characterization of Human Glioblastoma Cell Lines in vitro and their Xenografts in Nude Mice

1989 ◽  
Vol 12 (4) ◽  
pp. 169-174 ◽  
Author(s):  
H. Fischer ◽  
W.J. Zeller ◽  
K. Schwechheimer ◽  
K.-J. Hutter ◽  
B. Wowra ◽  
...  
Keyword(s):  
Cell Lines ◽  
Nude Mice ◽  
Glioblastoma Cell ◽  
Human Glioblastoma ◽  
Human Glioblastoma Cell ◽  
Glioblastoma Cell Lines

Targeting of CD317 by the immunotoxin HM1.24-ETA’ to allow immunotherapy in glioblastoma patients.

2019 ◽  
Vol 37 (15_suppl) ◽  
pp. e13560-e13560
Author(s):  
Dorothee Gramatzki ◽  
Emese Szabo ◽  
Martin Gramatzki ◽  
Matthias Peipp ◽  
Michael Weller
Keyword(s):  
Mrna Expression ◽  
Cell Lines ◽  
Dependent Manner ◽  
Glioblastoma Cell ◽  
Single Chain ◽  
Human Glioblastoma ◽  
Human Glioblastoma Cell ◽  
Protein Levels ◽  
Glioblastoma Cell Lines

e13560 Background: Glioblastoma is the most common primary malignant brain tumor with a poor prognosis. CD317 (HM1.24) is a transmembrane protein and may exist in differently spliced variants. It is highly expressed on plasma cells in multiple myeloma, as well as in certain solid tumor types. While several antibody drug conjugates are already in clinical practice, small immunotoxins with a different intracellular mode of action are only established in hairy cell leukemia. The immunotoxin HM1.24-ETA’ protein is a CD317 single chain Fv (scFv) antibody fused to a truncated version of Pseudomonas aeruginosa exotoxin A (ETA’). Methods: In vivo CD317 mRNA expression in human glioma of different grades and survival probabilities of glioblastoma patients based on CD317 mRNA expression were analyzed using the database of the Cancer Genome Atlas network (TCGA). CD317 protein expression was analyzed by immunohistochemistry in a human tissue microarray (TMA). In vitro CD317 mRNA expression was assessed by RT-PCR and CD317 protein levels by flow cytometry in several human glioblastoma cell lines. A cytotoxicity assay after treatment with HM1.24-ETA’ immunotoxin was performed in human glioblastoma cell lines. Results: Data on mRNA expression from the TCGA database demonstrated, that CD317 was upregulated in human glioblastomas compared to lower grade gliomas. In the group of glioblastoma patients increased CD317 mRNA expression was associated with decreased probability of survival ( p< 0.001). CD317 protein levels correlated directly with the tumor grade of astrocytic gliomas in the TMA. CD317 was expressed heterogeneously on mRNA and protein levels in the tested cell-lines in vitro. HM1.24-ETA’ induced cytotoxicity in CD317-positive glioblastoma cells in a concentration-dependent manner. Animal experiments currently performed suggest activity in glioblastoma xenografted mice. Conclusions: These data highlight CD317 as an interesting target antigen and HM1.24-ETA’ immunotoxin as a strategy for immunotherapy of glioblastoma patients.

Sign in / Sign up

Export Citation Format

Share Document