scholarly journals Synthesis and tumour cell uptake studies of gadolinium(III)–phosphonium complexes

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Andrew J. Hall ◽  
Amy G. Robertson ◽  
Leila R. Hill ◽  
Louis M. Rendina
Keyword(s):  
Glioblastoma Multiforme ◽  
Tumour Cell ◽  
In Vitro Cytotoxicity ◽  
Cell Uptake ◽  
Solution Stability ◽  
T98g Cell ◽  
Human Glioblastoma Multiforme ◽  
Theranostic Agents ◽  
Uptake Studies

AbstractThe synthesis of a new series of Gd(III)-arylphosphonium complexes is described and the solution stability of selected compounds is reported. Their lipophilicity and uptake in human glial (SVG p12) and human glioblastoma multiforme (T98G) cell lines are presented. The in vitro cytotoxicity of all complexes was determined to be low at therapeutically-relevant concentrations. Selected Gd(III) complexes are potential candidates for further investigation as theranostic agents.

scholarly journals Lomeguatrib Increases the Radiosensitivity of MGMT Unmethylated Human Glioblastoma Multiforme Cell Lines

2021 ◽  
Vol 22 (13) ◽  
pp. 6781
Author(s):  
Anna Kirstein ◽  
Daniela Schilling ◽  
Stephanie E. Combs ◽  
Thomas E. Schmid
Keyword(s):  
Glioblastoma Multiforme ◽  
Cell Lines ◽  
Dna Methyltransferase ◽  
Treatment Options ◽  
Treatment Resistance ◽  
Cell Cycle Distribution ◽  
Human Glioblastoma ◽  
Human Glioblastoma Multiforme ◽  
Mgmt Protein

Background: Treatment resistance of glioblastoma multiforme to chemo- and radiotherapy remains a challenge yet to overcome. In particular, the O6-methylguanine-DNA-methyltransferase (MGMT) promoter unmethylated patients have only little benefit from chemotherapy treatment using temozolomide since MGMT counteracts its therapeutic efficacy. Therefore, new treatment options in radiotherapy need to be developed to inhibit MGMT and increase radiotherapy response. Methods: Lomeguatrib, a highly specific MGMT inhibitor, was used to inactivate MGMT protein in vitro. Radiosensitivity of established human glioblastoma multiforme cell lines in combination with lomeguatrib was investigated using the clonogenic survival assay. Inhibition of MGMT was analyzed using Western Blot. Cell cycle distribution and apoptosis were investigated to determine the effects of lomeguatrib alone as well as in combination with ionizing radiation. Results: Lomeguatrib significantly decreased MGMT protein and reduced radiation-induced G2/M arrest. A radiosensitizing effect of lomeguatrib was observed when administered at 1 µM and increased radioresistance at 20 µM. Conclusion: Low concentrations of lomeguatrib elicit radiosensitization, while high concentrations mediate a radioprotective effect.

scholarly journals Kinetic Studies of Sodium and Metforminium Decavanadates Decomposition and In Vitro Cytotoxicity and Insulin- Like Activity

Inorganics ◽  
2020 ◽  
Vol 8 (12) ◽  
pp. 67
Author(s):  
Aniela M. Silva-Nolasco ◽  
Luz Camacho ◽  
Rafael Omar Saavedra-Díaz ◽  
Oswaldo Hernández-Abreu ◽  
Ignacio E. León ◽  
...  
Keyword(s):  
Insulin Release ◽  
Hepg2 Cells ◽  
Kinetic Studies ◽  
Decomposition Reaction ◽  
Dose Dependence ◽  
In Vitro Cytotoxicity ◽  
Cell Uptake ◽  
Phosphorylated Akt ◽  
Hepg2 Cell Lines

The kinetics of the decomposition of 0.5 and 1.0 mM sodium decavanadate (NaDeca) and metforminium decavanadate (MetfDeca) solutions were studied by 51V NMR in Dulbecco’s modified Eagle’s medium (DMEM) medium (pH 7.4) at 25 °C. The results showed that decomposition products are orthovanadate [H2VO4]− (V1) and metavanadate species like [H2V2O7]2− (V2), [V4O12]4− (V4) and [V5O15]5− (V5) for both compounds. The calculated half-life times of the decomposition reaction were 9 and 11 h for NaDeca and MetfDeca, respectively, at 1 mM concentration. The hydrolysis products that presented the highest rate constants were V1 and V4 for both compounds. Cytotoxic activity studies using non-tumorigenic HEK293 cell line and human liver cancer HEPG2 cells showed that decavanadates compounds exhibit selectivity action toward HEPG2 cells after 24 h. The effect of vanadium compounds (8–30 μM concentration) on the protein expression of AKT and AMPK were investigated in HEPG2 cell lines, showing that NaDeca and MetfDeca compounds exhibit a dose-dependence increase in phosphorylated AKT. Additionally, NaDeca at 30 µM concentration stimulated the glucose cell uptake moderately (62%) in 3T3-L1 adipocytes. Finally, an insulin release assay in βTC-6 cells (30 µM concentration) showed that sodium orthovanadate (MetV) and MetfDeca enhanced insulin release by 0.7 and 1-fold, respectively.

scholarly journals Novel O-methyl goniofufurone and 7-epi-goniofufurone derivatives: synthesis, in vitro cytotoxicity and SAR analysis

MedChemComm ◽  
2018 ◽  
Vol 9 (12) ◽  
pp. 2017-2027
Author(s):  
Jovana Francuz ◽  
Mirjana Popsavin ◽  
Sanja Djokić ◽  
Vesna Kojić ◽  
Tatjana Srdić-Rajić ◽  
...  
Keyword(s):  
Cell Lines ◽  
Tumour Cell ◽  
Methoxy Group ◽  
Antitumour Activity ◽  
In Vitro Cytotoxicity ◽  
Human Tumour ◽  
Tumour Cell Lines ◽  
Sar Analysis ◽  
Human Tumour Cell Lines

Novel goniofufurone (1) and 7-epi-goniofufurone (2) derivatives bearing a methoxy group at the C-5 and/or C-7 positions were prepared and their in vitro antitumour activity against some human tumour cell lines was evaluated.

scholarly journals The suppression of manganese superoxide dismutase decreased the survival of human glioblastoma multiforme T98G cells

2017 ◽  
Vol 26 (1) ◽  
pp. 19-25 ◽  
Author(s):  
Novi S. Hardiany ◽  
Mohamad Sadikin ◽  
Nurjati Siregar ◽  
Septelia I. Wanandi
Keyword(s):  
Hydrogen Peroxide ◽  
Superoxide Dismutase ◽  
Glioblastoma Multiforme ◽  
Manganese Superoxide Dismutase ◽  
Superoxide Radical ◽  
Specific Activity ◽  
Human Glioblastoma Multiforme ◽  
Manganese Superoxide ◽  
In Vitro Transfection

Background: Glioblastoma multiforme (GBM) is a primary malignant brain tumor which has poor prognosis. High incidence of oxidative stress-based therapy resistance could be related to the high antioxidant status of GBM cells. Our previous study has reported that manganese superoxide dismutase (MnSOD) antioxidant expression was significantly higher in high grade glioma than in low grade. The aim of this study was to analyze the impact of MnSOD suppression toward GBM cell survival.Methods: This study is an experimental study using human glioblastoma multiforme T98G cell line. Suppression of MnSOD expression was performed using in vitro transfection MnSOD-siRNA. The MnSOD expression was analyzed by measuring the mRNA using real time RT-PCR, protein using ELISA technique, and specific activity of enzyme using inhibition of xantine oxidase. Concentration of reactive oxygen species (ROS) intracellular was determined by measuring superoxide radical and hydrogen peroxide. Cell survival was analyzed by measuring viability, proliferation, and cell apoptosis.Results: In vitro transfection of MnSOD-siRNA suppressed the mRNA, protein, and specific activity of MnSOD. This treatment significantly increased the concentration of superoxide radical; however, it did not influence the concentration of hydrogen peroxide. Moreover, viability MnSOD-suppressing cell significantly decreased, accompanied by increase of cell apoptosis without affecting cell proliferation.Conclusion: The suppression of MnSOD expression leads to decrease glioblastoma multiforme cell survival, which was associated to the increase of cell apoptotic.

Tumour cell uptake of the metastasis inhibitor ruthenium complex NAMI-A and its in vitro effects on KB cells

2002 ◽  
Vol 50 (5) ◽  
pp. 405-411 ◽  
Author(s):  
Fabiana Frausin ◽  
Moreno Cocchietto ◽  
Alberta Bergamo ◽  
Vito Scarcia ◽  
Ariella Furlani ◽  
...  
Keyword(s):  
Tumour Cell ◽  
Ruthenium Complex ◽  
Cell Uptake ◽  
Kb Cells ◽  
In Vitro Effects ◽  
Metastasis Inhibitor

scholarly journals In-vitro cytotoxicity and cellular uptake studies of luminescent functionalized core-shell nanospheres

2017 ◽  
Vol 24 (6) ◽  
pp. 1392-1403 ◽  
Author(s):  
Anees A. Ansari ◽  
T.N. Hasan ◽  
N.A. Syed ◽  
J.P. Labis ◽  
Ali A. Alshatwi
Keyword(s):  
Cellular Uptake ◽  
In Vitro Cytotoxicity ◽  
Core Shell ◽  
Uptake Studies
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