Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: The impact of DBI-2 and BAY-876 on cell signaling pathways in LS174T ( A ) and HCT116 ( B ) CRC cells. Combination of DBI-2 (3 μmol/L) and GLUT1 inhibitor BAY-876 (1 μmol/L) resulted in enhanced depletion of Axin2 and c-Myc, increase in p-AMPK and p-ACC, and depletion of p-P70S6K and p-S6. Data are presented as the means ± SEM. * p < 0.05, and ** p < 0.01, n = 3. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques:

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: DBI-2 and BAY-876 synergically inhibited CRC cells in vitro. ( A , B ) DBI-2 inhibited colorectal cancer cell LS174T ( A ) and HCT116 ( B ) proliferation. The IC 50 of DBI-2 to inhibit the proliferation of LS174T cells and HCT116 cells was 1.14 μmol/L and 0.53 μmol/L, respectively. ( C , D ) Combinatorial effects of DBI-2 and BAY-876 on CRC cell proliferation. The cells were exposed to DBI-2 or BAY-876 at specified concentrations for a duration of 5 days, and the number of viable cells was determined. Data are presented as the means ± SEM. ** p < 0.01, n = 3. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques: In Vitro

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: Synergistic effects of DBI-2 and BAY-876 on LS174T and HCT116 CRC cells. ( A , B ) DBI-2 and BAY-876 synergistically inhibited the proliferation of colorectal cancer cells. The cells were exposed to DBI-2 and BAY-876 at specified concentrations over a period of 5 days, and the number of viable cells was determined. Synergy scores were measured utilizing SynergyFinder, with Bliss serving as the benchmark model. The synergy scores for drug combinations of DBI-2 and BAY-876 were 25 for LS174T cells ( A ) and 15 for HCT116 cells ( B ).

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques:

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: Synergistic effects of DBI-2 and BAY-876 on inducing apoptosis in LS174T cells and HCT116 cells through flow cytometry analysis using Annexin-V-FITC and propidium iodide (PI) dual staining. ( A , E ) Cells were treated with DMSO. The apoptosis rate was 16% and 17%, respectively. ( B , F ) Cells were treated with DBI-2 at 3 μmol/L. The percentage of apoptotic cells was 26% and 22%, respectively. ( C , G ) Cells were treated with BAY-876 at 1 μmol/L. The apoptosis rate was 34% and 23%, respectively. ( D , H ) Cells were treated with the combination of DBI-2 (3 μmol/L) with BAY-876 (1 μmol/L). The apoptosis rate was 70% and 75%, respectively. ( I , J ) Percentage of normal, early apoptotic, and late apoptotic cells in LS174T cells and HCT116 cells. Data are presented as the means ± SEM. * p < 0.05, and ** p < 0.01 versus control group, ## p < 0.01 versus DBI-2 or BAY-876 group, n = 3. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques: Flow Cytometry, Staining

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: Synergistic effects of DBI-2 and BAY-876 on inducing autophagy and necrosis in LS174T cells and HCT116 cells. ( A ) Detection of autophagic vacuoles by MDC staining in LS174T cells treated with DBI-2 and BAY-876 alone and in combination for 8 h (a: DMSO; b: DBI-2; c: BAY-876; and d: DBI-2 and BAY-876). ( B ) Expression of LC3-Ⅰ and LC3-Ⅱ in LS174T cells and HCT116 cells after 8 h treatment. ( C ) The LDH activity in the culture medium of LS174T cells and HCT116 cells. Data are presented as the means ± SEM. * p < 0.05, and ** p < 0.01, n = 3. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques: Staining, Expressing, Activity Assay

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: The combination of DBI-2/KD and the GLUT1 inhibitor BAY-876 exhibited a synergistic inhibitory effect on colon cancer cell xenografts in vivo. ( A – C ) The combination of DBI-2 (40 mg/kg/day, IP) with BAY-876 (3 mg/kg/day, PO) or ketogenic diet feeding significantly inhibited tumor growth in RAG1 −/− γc − mice. Notably, this treatment regimen did not induce any noticeable adverse effects based on body weight. ( D ) Pictures of tumors after treatment for 12 days. ( E ) H&E staining of tumor sections (arrows). ( F ) IHC staining of Ki67, p-AMPK, and AMPK. Data are presented as the means ± SEM. * p < 0.05, and ** p < 0.01, n = 12. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques: In Vivo, Staining, Immunohistochemistry

Journal: Cancers

Article Title: Inhibition of Carbohydrate Metabolism Potentiated by the Therapeutic Effects of Oxidative Phosphorylation Inhibitors in Colon Cancer Cells

doi: 10.3390/cancers16071399

Figure Lengend Snippet: Combination of DBI-2 with BAY-876 reduced blood glucose, plasma triglycerides (TG), T-CHO, and LDL-C. ( A ) Blood glucose tested from RAG1 −/− γc − mice tails. ( B – E ) The plasma TG, T-CHO, LDL-C, and HDL-C tested in tumor-bearing animals. Blood obtained via retro orbital eye bleeds prior to sacrifice. Blood samples spun and plasma separated. Data are presented as the means ± SEM. * p < 0.05, and ** p < 0.01, n = 6. One-way ANOVA followed by Tukey’s multiple comparisons test were applied as the statistical method.

Article Snippet: BAY-876 (i.e., N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide) was acquired from Medkoo Bioscience (Durham, NC, USA) (Cat No. 530485).

Techniques:

Journal: Journal of Oral Pathology & Medicine

Article Title: Transcriptional regulation of glucose transporters in human oral squamous cell carcinoma cells

doi: 10.1111/jop.13342

Figure Lengend Snippet: Fold change difference between 50% and 100% confluence of GLUT mRNA expression in OKF6 and oral squamous cell carcinoma cells when treated with BAY876 or WZB117. Each data point was obtained from 3 biological replicates and error bars represent the SD. The control was baseline expression with no inhibitor present and the SD is an averaged SD from all groups.

Article Snippet: Cells were treated with 500 nM BAY876 (GLUT1 inhibitor; A17216; ADOOQ Bioscience) and 25 μM WZB117 (GLUT1, GLUT3 and GLUT4 inhibitor; 19900; Cayman Chemical Company) 24 h before they were expected to reach the chosen confluency.

Techniques: Expressing, Control