Journal: Bioorganic chemistry

Article Title: New quinoline/chalcone hybrids as anti-cancer agents: Design, synthesis, and evaluations of cytotoxicity and PI3K inhibitory activity

doi: 10.1016/j.bioorg.2018.10.064

Figure Lengend Snippet: GI 50 of compounds 9i and 9j against 59 cell lines in 9 different cancer panels tested using NCI’s in vitro five dose anticancer assay.

Article Snippet: The presence of such geometry might also be responsible for the absence of the 2-pyrazoline cyclization usually observed in hydrazide-chalcone reactions. fig ft0 fig mode=article f1 fig/graphic|fig/alternatives/graphic mode="anchored" m1 Open in a separate window Fig. 2. caption a7 Possible stacking interaction for compound 9i . fig ft0 fig mode=article f1 fig/graphic|fig/alternatives/graphic mode="anchored" m1 Open in a separate window Scheme 1. caption a7 Synthesis of ( E )- N’ -(( Z )-1-(4-aminophenyl)-3-phenylallylidene)-2-(phenyl)quinoline-4-carbohydrazide derivatives 9a-t . table ft1 table-wrap mode="anchored" t5 caption a7 Panel/cell line GI 50 Compound Panel/cell line GI 50 Compound 9i 9j 9i 9j Leukemia Melanoma CCRF-CEM 5.84 4.53 LOX IMVI 1.56 4.00 HL-60(TB) 2.54 3.49 MALME-3M > 100 > 100 K-562 1.05 3.09 M14 1.16 2.54 MOLT-4 3.30 3.23 MDA-MB-435 0.305 1.00 RPMI-8226 3.86 4.10 SK-MEL-2 2.03 3.81 SR 0.595 3.29 SK-MEL-28 3.78 6.23 Non-small cell lung cancer SK-MEL-5 0.701 2.50 A549/ATCC 2.33 4.79 UACC-257 > 100 33.7 EKVX 3.78 3.99 UACC-62 0.556 2.06 HOP-62 3.21 4.62 Ovarian cancer HOP-92 1.92 4.10 IGROV1 4.98 6.48 NCI-H226 7.54 6.47 OVCAR-3 0.462 2.98 NCI-H23 3.14 5.02 OVCAR-4 1.82 4.71 NCI-H322M 6.00 4.73 OVCAR-5 5.51 8.43 NCI-H460 1.89 3.51 OVCAR-8 4.16 5.25 NCI-H522 0.307 0.622 NCI/ADR-RES 0.519 2.54 Colon cancer SK-OV-3 3.32 4.94 COLO 205 1.99 2.80 Renal cancer HCC-2998 3.40 4.28 786–0 1.84 4.22 HCT-116 1.41 3.18 A498 0.375 1.64 HCT-15 1.03 3.33 ACHN 1.47 4.19 HT29 1.13 3.35 RXF 393 0.698 1.63 KM12 1.15 3.46 SN12C 4.27 6.84 SW-620 1.24 4.24 TK-10 52.30 8.51 CNS cancer UO-31 1.55 2.20 SF-268 2.19 4.09 SF-295 0.540 3.13 Breast cancer SF-539 1.41 2.43 MCF7 0.442 2.53 SNB-19 5.54 6.51 MDA-MB231/ATCC 3.28 3.94 SNB-75 0.371 1.41 HS 578T 1.05 4.68 U251 2.18 4.51 BT-549 2.04 3.92 Prostate cancer T-47D 2.70 2.73 PC-3 2.03 3.40 MDA-MB-468 2.95 4.91 DU-145 3.16 3.68 Open in a separate window GI 50 of compounds 9i and 9j against 59 cell lines in 9 different cancer panels tested using NCI’s in vitro five dose anticancer assay.

Techniques: In Vitro

Journal: Biomedicines

Article Title: Anti-Inflammatory and Cancer-Preventive Potential of Chamomile ( Matricaria chamomilla L.): A Comprehensive In Silico and In Vitro Study

doi: 10.3390/biomedicines12071484

Figure Lengend Snippet: Confocal immunofluorescence microscopy of the microtubule network in U2OS cells upon treatment with ( A ) quercetin and ( B ) lupeol at concentrations of 0.1 µM, 1 µM, and 10 µM for 24 h. Vincristine (1 µM) and paclitaxel (1 µM) served as positive controls and DMSO as the negative control. The cells were imaged using a Thunder Imager Live Cell microscope with a 63×/1.40 NA objective lens (HC PL APO CS2 63×/1.40 OIL UV). The microtubules were visualized using green fluorescence for GFP (green), and the images were merged with DAPI (blue) to highlight the nucleus.

Article Snippet: In this context, it was interesting that the cytotoxicity of both compounds in CCRF-CEM and U2OS cells was not caused by apoptosis as the most common mode of cell death but by necrosis.

Techniques: Immunofluorescence, Microscopy, Negative Control, Fluorescence

Journal: Biomedicines

Article Title: Anti-Inflammatory and Cancer-Preventive Potential of Chamomile ( Matricaria chamomilla L.): A Comprehensive In Silico and In Vitro Study

doi: 10.3390/biomedicines12071484

Figure Lengend Snippet: Cell cycle arrest of U2OS cells by quercetin and lupeol. ( A ) Debris was gated out (SSC-A vs. FSC-A) with the first gate. ( B ) With the second gate (FSC-H vs. FSC-A), only single cells of normal morphology were gated. Duplets were gated out. ( C , D ) Three-dimensional representation of DNA histograms of U2OS cells exposed to 1 × IC 50 and 4 × IC 50 quercetin and lupeol for 72 h. DMSO was used as the negative control, and 1 × IC 50 vincristine was used as the positive control. ( C ) Cells treated with lupeol and ( D ) cells treated with quercetin. The histograms were obtained through flow cytometry using an excitation of 488 nm and an emission wavelength of 530 nm. ( E , F ) Bar diagrams showing the distinct phases of cell cycle upon treatment with quercetin and lupeol for 72 h. ( E ) Cells treated with lupeol and ( F ) cells treated with quercetin. The bar diagrams were created through the calculation of the mean values ± SD of three independent experiments. *** p < 0.001, ** p < 0.01, and * p < 0.05 compared to the negative control using paired two-tailed t -test.

Article Snippet: In this context, it was interesting that the cytotoxicity of both compounds in CCRF-CEM and U2OS cells was not caused by apoptosis as the most common mode of cell death but by necrosis.

Techniques: Negative Control, Positive Control, Flow Cytometry, Two Tailed Test

Journal: Biomedicines

Article Title: Anti-Inflammatory and Cancer-Preventive Potential of Chamomile ( Matricaria chamomilla L.): A Comprehensive In Silico and In Vitro Study

doi: 10.3390/biomedicines12071484

Figure Lengend Snippet: Dose–response curves of quercetin and lupeol as determined through resazurin assay. The mean values and standard deviation values are from three independent experiments. The tumor cells were subjected to treatment with each compound at concentrations of 10 µM, 25 µM, 50 µM, and 100 µM for 72 h. ( A ) Sensitive CCRF-CEM and the drug-resistant P-glycoprotein overexpressing CEM/ADR5000 leukemia cells. ( B ) U87/ΔEGFR transfected with a deletion-activated cDNA of EGFR and its wild-type U87MG glioblastoma cells. ( C ) HCT116 p53 +/+ and knockout HCT116 p53 −/− colorectal cancer cells. ( D ) U2OS osteosarcoma cells.

Article Snippet: In this context, it was interesting that the cytotoxicity of both compounds in CCRF-CEM and U2OS cells was not caused by apoptosis as the most common mode of cell death but by necrosis.

Techniques: Resazurin Assay, Standard Deviation, Transfection, Knock-Out

Journal: Biomedicines

Article Title: Anti-Inflammatory and Cancer-Preventive Potential of Chamomile ( Matricaria chamomilla L.): A Comprehensive In Silico and In Vitro Study

doi: 10.3390/biomedicines12071484

Figure Lengend Snippet: Detection of cell death in U2OS cells using flow cytometry and annexin-V/PI staining using a flow cytometer. ( A , B ) Cells treated for 72 h with 0.5 × IC 50 , 1 × IC 50 , 2 × IC 50 , and 4 × IC 50 of lupeol and quercetin, respectively. ( C , D ) represent bar diagrams of the percentage of cells in quadrium treated with lupeol ( C ) and quercetin ( D ). For details, see . Treatment with both compounds at 4 × IC 50 showed a tendency for increased necrosis, which was, however, not statistically significant compared to the negative control.

Article Snippet: In this context, it was interesting that the cytotoxicity of both compounds in CCRF-CEM and U2OS cells was not caused by apoptosis as the most common mode of cell death but by necrosis.

Techniques: Flow Cytometry, Staining, Negative Control