Journal: Nature Communications

Article Title: Late-stage (radio)fluorination of alkyl phosphonates via electrophilic activation

doi: 10.1038/s41467-024-54208-y

Figure Lengend Snippet: a Late-stage radiofluorination of PET tracers and 18 F-synthons. RCC TLC determined by radio-TLC ( n = 3); RCY = isolated 18 F-product activity amount/starting amount of radioactivity (decay corrected). cLog P values were predicted using ALOGPS 2.1 ( http://www.vcclab.org/lab/alogps ). Blue arrows pointing upward indicate an increase in cLog P /Log D 7.4 compared to the parent compound, while downward arrows indicate a decrease. The small pink ball after cLog P /Log D 7.4 represents the target of the parent compound. b Preparation α v β 3 integrin receptor developer [ 18 F]BFPA-E[c(RGDyK)] 2 . c MicroPET images of [ 18 F]BFPA-E[c(RGDyK)] 2 in U87MG xenograft mice at 30 min after tail vein injection. 200 μg of E[c(RGDyK)] 2 was used to block the tumor uptake of [ 18 F]BFPA-E[c(RGDyK)] 2 . The white circle is the tumor area. d Preparation of PET tracer [ 18 F]BFPA-Flurpiridaz targeting MC I. e MicroPET/CT images of healthy mice [ 18 F]BFPA-Flurpiridaz 60 min after caudal vein injection. f Molecular Docking. Flurpiridaz and BFPA-Flurpiridaz to MC I (PDB: 7ZM8). Cyan: residues composing the substrate-binding cavity; yellow: residues forming hydrogen bonds; yellow dashed lines: locations of hydrogen bond.

Article Snippet: The glioma cell line U87MG was obtained from the China Center for Type Culture Collection of the Chinese Academy of Sciences.

Techniques: Isolation, Activity Assay, Radioactivity, Injection, Blocking Assay, Binding Assay

Journal: Biomedicines

Article Title: The Sesquiterpene Lactone Cynaropicrin Manifests Strong Cytotoxicity in Glioblastoma Cells U-87 MG by Induction of Oxidative Stress

doi: 10.3390/biomedicines10071583

Figure Lengend Snippet: Cytotoxic effects of Cyn on human glioblastoma U-87 MG cells. ( A ) Molecular structure of SL Cynaropicrin (IUPAC name: ([(3 a R,4S,6 a R,8S,9 a R,9 b R)-8-hydroxy-3,6,9-trimethylidene-2-oxo-3 a ,4,5,6 a ,7,8,9 a ,9 b -octahydroazuleno[4,5- b ]furan-4-yl] 2-(hydroxymethyl)prop-2-enoate). ( B ) Determination of IC50 values on U-87 MG cells using GraphPad Prism 7 software after 24, 48 and 72 h of incubation with Cyn 0.01, 0.1, 1, 10, 25, 50 and 100 µM and DMSO 0.1% as the vehicle control. ( C ) Dose and time-dependent reduction of the U-87 MG cell number under daily exposure to Cyn 4, 8 and 10 µM for 24, 48 and 72 h. ( D ) Morphological change of 4, 8 and 10 µM Cyn-treated U-87 MG cells for 24, 48 and 72 h. White arrows indicate round-shaped cells with a loss of filaments and the presence of cell shrinkage. ( E ) Cytotoxic effects of daily exposure to Cyn 4, 8 and 10 µM for 24, 48 and 72 h on the U-87 MG cell metabolism. ( F ) Effect of Cyn 4 µM on the U-87 MG clonogenic potential. For all the experiments, values are the mean ± SEM of 3 individual determinations. One-way ANOVA test, p -value < 0.05. According to GraphPad Prism 7 software, **** p -value < 0.0001 (extremely significant).

Article Snippet: Human continuous glioblastoma cell line U-87 MG was purchased from the Sigma Aldrich Collection (LGC Promochem, Teddington, UK).

Techniques: Software, Incubation, Control

Journal: Biomedicines

Article Title: The Sesquiterpene Lactone Cynaropicrin Manifests Strong Cytotoxicity in Glioblastoma Cells U-87 MG by Induction of Oxidative Stress

doi: 10.3390/biomedicines10071583

Figure Lengend Snippet: Cyn-induced oxidative stress in human glioblastoma U-87 MG cells. ( A ) Pretreatment of U-87 MG cells with NAC 3 mM for 4 h, followed by incubation for 24 h with Cyn 0.01, 0.1, 1, 10, 25, 50 and 100 μM. DMSO 0.1% was used as the vehicle control. ( B ) Preincubation with NAC 3 mM for 4 h preserved U-87 MG from Cyn-induced morphological change, since the cells maintained their protrusions rather than appeared round-shaped (white arrows). ( C ) Quantitative analysis of ROS generation in U-87 MG cells under 2 and 6 h of treatment with Cyn 8 and 25 μM. DMSO 0.1% was used as the vehicle control. ( D ) Qualitative analysis of ROS production after 2 h of exposure to Cyn 8 and 25 μM. ( E ) Immunofluorescence staining of NRF2 in U-87 MG treated for 24 h with Cyn 25 µM, which showed a nuclear localization with respect to the control cells treated with 0.1% DMSO (white arrows). Magnification 20×. Data were analyzed by a Student’s t -test, p -value < 0.05. According to GraphPad Prism 7 software, * p -values from 0.01 to 0.05 (significant) and ** p -values from 0.001 to 0.01 (very significant).

Article Snippet: Human continuous glioblastoma cell line U-87 MG was purchased from the Sigma Aldrich Collection (LGC Promochem, Teddington, UK).

Techniques: Incubation, Control, Immunofluorescence, Staining, Software

Journal: Biomedicines

Article Title: The Sesquiterpene Lactone Cynaropicrin Manifests Strong Cytotoxicity in Glioblastoma Cells U-87 MG by Induction of Oxidative Stress

doi: 10.3390/biomedicines10071583

Figure Lengend Snippet: Cytotoxic effects of Cyn on patient-derived glioblastoma cell lines NULU and ZAR. ( A ) Cytotoxic effects of daily exposure to Cyn 4, 8 and 10 µM for 24, 48 and 72 h on NULU ( A ) and ZAR ( B ) cell metabolism. DMSO 0.1% was used as the vehicle control. ( C ) Morphological changes for the 4, 8 and 10 µM Cyn-treated NULU and ZAR cell lines for 24, 48 and 72 h. Data were analyzed by the Student’s t -test, p -value < 0.05. According to GraphPad Prism 7 software, * p -value 0.01–0.05 was considered statistically significant, ** p -value 0.001–0.01 very significant, *** p -value 0.0001–0.001 extremely significant and while **** p -values < 0.0001 were extremely significant. Taking together, these results clearly indicate the potentialities of Cyn as adjuvant therapy to conventional chemotherapy TMZ in IDH-mutant and wild-type glioblastoma.

Article Snippet: Human continuous glioblastoma cell line U-87 MG was purchased from the Sigma Aldrich Collection (LGC Promochem, Teddington, UK).

Techniques: Derivative Assay, Control, Software, Adjuvant, Mutagenesis

Journal: Frontiers in Molecular Biosciences

Article Title: Proteomic Analysis on Anti-Proliferative and Apoptosis Effects of Curcumin Analog, 1,5-bis(4-Hydroxy-3-Methyoxyphenyl)-1,4-Pentadiene-3-One-Treated Human Glioblastoma and Neuroblastoma Cells

doi: 10.3389/fmolb.2021.645856

Figure Lengend Snippet: The cell viability in percentage (%) of (A) U-87 MG glioblastoma and (B) SH-SY5Y neuroblastoma cells upon treatment with MS13 and curcumin. The concentration (ranged from 0 to 100 μM) of MS13 or curcumin was log10 transformed. The cell viability of both cells decreased as the concentration of MS13 or curcumin increased. Results are expressed as the average of percentage of cell viability. Error bars represent mean ± standard error mean. The experiments were performed in triplicates and results were compared between three biological replicates. Statistical analysis was performed using analysis of variance (ANOVA), comparing cell viability of each concentration with the untreated sample. Asterisks indicate the difference in the statistical significance of the mean values between treated and untreated cells. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: Human glioblastoma (U-87 MG) cell line was purchased from ElabScience ® (Wuhan, China), whereas human neuroblastoma (SH-SY5Y) cell line and normal human epithelial hepatocytes, WRL-68 were obtained from the American Type Culture Collection (ATCC, Rockville, MD, United States).

Techniques: Concentration Assay, Transformation Assay

Journal: Frontiers in Molecular Biosciences

Article Title: Proteomic Analysis on Anti-Proliferative and Apoptosis Effects of Curcumin Analog, 1,5-bis(4-Hydroxy-3-Methyoxyphenyl)-1,4-Pentadiene-3-One-Treated Human Glioblastoma and Neuroblastoma Cells

doi: 10.3389/fmolb.2021.645856

Figure Lengend Snippet: The anti-proliferative effect of MS13 and curcumin on (A) U-87 MG glioblastoma and (B) SH-SY5Y neuroblastoma cells at 24, 48, and 72 h. Results are expressed as the average of cell viability in percentage (%) against concentration (μM). Error bars represent mean ± standard error mean. All experiments were performed in triplicates and results were compared between three biological replicates. Statistical analysis was performed using ANOVA, comparing cell viability of each concentration with the untreated sample. Asterisks indicate the difference in the statistical significance of the mean values between treated and untreated cells. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: Human glioblastoma (U-87 MG) cell line was purchased from ElabScience ® (Wuhan, China), whereas human neuroblastoma (SH-SY5Y) cell line and normal human epithelial hepatocytes, WRL-68 were obtained from the American Type Culture Collection (ATCC, Rockville, MD, United States).

Techniques: Concentration Assay