scholarly journals Regulation of Human Cytosolic Sulfotransferases 1C2 and 1C3 by Nuclear Signaling Pathways in LS180 Colorectal Adenocarcinoma Cells

2013 ◽  
Vol 42 (3) ◽  
pp. 361-368 ◽  
Author(s):  
Elizabeth A. Rondini ◽  
Hailin Fang ◽  
Melissa Runge-Morris ◽  
Thomas A. Kocarek
Keyword(s):  
Signaling Pathways ◽  
Colorectal Adenocarcinoma ◽  
Nuclear Signaling ◽  
Adenocarcinoma Cells

scholarly journals p,p′-Dichlorodiphenyltrichloroethane inhibits the apoptosis of colorectal adenocarcinoma DLD1 cells through PI3K/AKT and Hedgehog/Gli1 signaling pathways

2015 ◽  
Vol 4 (5) ◽  
pp. 1214-1224
Author(s):  
Li Song ◽  
Meirong Zhao ◽  
Jianxin Liu ◽  
Zhuoyu Li ◽  
Hong Xiao ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Signaling Pathways ◽  
Colorectal Adenocarcinoma ◽  
Cancer Development ◽  
Adenocarcinoma Cells

p,p′-Dichlorodiphenyltrichloroethane is able to inhibit the apoptosis of human colorectal adenocarcinoma cells, which may be an important mechanism to contribute to colorectal cancer development.

α-Tocopherol attenuates the cytotoxic effect of δ-tocotrienol in human colorectal adenocarcinoma cells

2010 ◽  
Vol 397 (2) ◽  
pp. 214-219 ◽  
Author(s):  
Akira Shibata ◽  
Kiyotaka Nakagawa ◽  
Phumon Sookwong ◽  
Tsuyoshi Tsuduki ◽  
Akira Asai ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Colorectal Adenocarcinoma ◽  
Adenocarcinoma Cells

scholarly journals Aqueous Fraction of Nephelium ramboutan-ake Rind Induces Mitochondrial-Mediated Apoptosis in HT-29 Human Colorectal Adenocarcinoma Cells

Molecules ◽  
2012 ◽  
Vol 17 (6) ◽  
pp. 6633-6657 ◽  
Author(s):  
Chim Kei Chan ◽  
Bey Hing Goh ◽  
Muhamad Noor Alfarizal Kamarudin ◽  
Habsah Abdul Kadir
Keyword(s):  
Colorectal Adenocarcinoma ◽  
Aqueous Fraction ◽  
Adenocarcinoma Cells ◽  
Ht 29

scholarly journals Modulating Properties of Piroxicam, Meloxicam and Oxicam Analogues against Macrophage-Associated Chemokines in Colorectal Cancer

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7375
Author(s):  
Paulina Lewandowska ◽  
Izabela Szczuka ◽  
Iwona Bednarz-Misa ◽  
Berenika M. Szczęśniak-Sięga ◽  
Katarzyna Neubauer ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Colorectal Adenocarcinoma ◽  
Normal Mucosa ◽  
Colorectal Tumors ◽  
Adjacent Tissue ◽  
Inflammatory Drug ◽  
Chemokine Expression ◽  
Adenocarcinoma Cells ◽  
Thiazine Ring ◽  
N Stage

The mechanisms underlying the antineoplastic effects of oxicams have not been fully elucidated. We aimed to assess the effect of classic and novel oxicams on the expression/secretion of macrophage-associated chemokines (RTqPCR/Luminex xMAP) in colorectal adenocarcinoma cells, and on the expression of upstream the non-steroidal anti-inflammatory drug (NSAID)-activated genes NAG1, NFKBIA, MYD88, and RELA, as well as at the chemokine profiling in colorectal tumors. Meloxicam downregulated CCL4 9.9-fold, but otherwise the classic oxicams had a negligible/non-significant effect. Novel analogues with a thiazine ring substituted with arylpiperazine and benzoyl moieties significantly modulated chemokine expression to varying degree, upregulated NAG1 and NFKBIA, and downregulated MYD88. They inhibited CCL3 and CCL4, and their effect on CCL2 and CXCL2 depended on the dose and exposure. The propylene linker between thiazine and piperazine nitrogens and one arylpiperazine fluorine substituent characterized the most effective analogue. Only CCL19 and CXCL2 were not upregulated in tumors, nor was CXCL2 in tumor-adjacent tissue compared to normal mucosa. Compared to adjacent tissue, CCL4 and CXCL2 were upregulated, while CCL2, CCL8, and CCL19 were downregulated in tumors. Tumor CCL2 and CCL7 increased along with advancing T and CCL3, and CCL4 along with the N stage. The introduction of arylpiperazine and benzoyl moieties into the oxicam scaffold yields effective modulators of chemokine expression, which act by upregulating NAG1 and interfering with NF-κB signaling.

scholarly journals Effect of Pectin on the Expression of Proteins Associated with Mitochondrial Biogenesis and Cell Senescence in HT29-Human Colorectal Adenocarcinoma Cells

2019 ◽  
Vol 24 (2) ◽  
pp. 187-196
Author(s):  
José Javier Zamorano-León ◽  
Sandra Ballesteros ◽  
Natalia de las Heras ◽  
Luis Alvarez-Sala ◽  
Mariano de la Serna-Soto ◽  
...  
Keyword(s):  
Mitochondrial Biogenesis ◽  
Colorectal Adenocarcinoma ◽  
Cell Senescence ◽  
Adenocarcinoma Cells

Molecular Docking and In Vitro Anticancer Screening of Synthesized Arylthiazole linked 2H-indol-2-one Derivatives as VEGFR-2 Kinase Inhibitors

2021 ◽  
Vol 21 ◽  
Author(s):  
Nishtha Shalmali ◽  
Sandhya Bawa ◽  
Md Rahmat Ali ◽  
Sourav Kalra ◽  
Raj Kumar ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Active Sites ◽  
Colorectal Adenocarcinoma ◽  
Kinase Inhibitors ◽  
Adenocarcinoma Cells ◽  
Ic50 Values

Background: Indoline-2,3-dione comprises a leading course group of heterocycles endowed with appealing biological actions, including anticancer activity. There are significant justifications for exploring the anticancer activity of Schiff base derivatives of isatin as a vast number of reports have documented remarkable antiproliferative action of isatin nucleus against various cancer cell lines. Aims and Objectives: A series of arylthiazole linked 2H-indol-2-one derivatives (5a-t) was designed and synthesized as potential VEGFR-2 kinase inhibitors keeping the essential pharmacophoric features of standard drugs, like sunitinib, sorafenib, nintedanib, etc. They were evaluated for their in vitro anticancer activity. The aim of this study was to investigate and assess the anticancer potential of isatin-containing compounds along with their kinase inhibition activity. Methods: The title compounds were synthesized by reacting substituted isatins with para-substituted arylthiazoles using appropriate reaction conditions. Selected synthesized derivatives went under preliminary screening against a panel of 60 cancer cell lines at NCI, the USA, for single-dose and five dose assays. Molecular docking was performed to explore the binding and interactions with the active sites of the VEGFR-2 receptor (PDB Id: 3VHE). Derivatives 5a, 5b, 5c, 5d, 5g, 5h, and 5m were assessed for in vitro inhibition potency against Human VEGFR-2 using ELISA (Enzyme-Linked Immunosorbent Assay) kit. All the target compounds were determined against human colon cancer cell line SW480 (colorectal adenocarcinoma cells). Cellular apoptosis/necrosis was determined by flow cytometry using annexin V-FITC. DNA content of the cells was analyzed by flow cytometry and the cycle distribution was quantified. Results: Compounds 5a and 5g exhibited noteworthy inhibition during a five-dose assay against a panel of 60 cell lines with MID GI50 values of 1.69 and 1.54 µM, respectively. Also, both the lead compounds 5a and 5g demonstrated promising VEGFR-2 inhibitory activity with IC50 values of 5.43±0.95 and 9.63±1.32 µM, respectively. The aforesaid potent compounds were found effective against SW480 (colorectal adenocarcinoma cells) with IC50 values of 31.44 µM and 106.91 µM, respectively. Compound 5a was found to arrest the cell cycle at the G2/M phase, increasing apoptotic cell death. The docking study also supported VEGFR-2 inhibitory activity as both compounds 5a and 5g displayed promising binding and interactions with the active sites of VEGFR-2 receptor (PDB: 3VHE) with docking scores -9.355 and -7.758, respectively. All the compounds obeyed Lipinski’s rule of five. Conclusion: Indoline-2,3-dione and thiazole have huge potential to be considered a steer combination approach for developing promising kinase inhibitors as cancer therapeutics.

Study on the Toxicity of Calix[4]- and [6]-Arenes and their Sulfated Derivatives in Two- and Three-Dimensional Cell Cultures of Colorectal Adenocarcinoma

2021 ◽  
Vol 37 (1) ◽  
pp. 87-94
Author(s):  
S.V. Nikulin ◽  
B.Ya. Alekseev ◽  
A.N Gorbunov ◽  
I.M. Vatsuro ◽  
V.V. Kovalev ◽  
...  
Keyword(s):  
Cell Culture ◽  
Colorectal Adenocarcinoma ◽  
Three Dimensional ◽  
3D Cell Culture ◽  
Russian Science ◽  
Adenocarcinoma Cells ◽  
Therapeutic Molecules ◽  
Derivatives Of ◽  
Ht 29 ◽  
Dimensional Cell

A comparative study of the toxicity of two unsubstituted calixarenes consisting of 4 and 6 phenolic fragments, as well as their p-sulfated derivatives, was carried out on the HT-29 colorectal adenocarcinoma cells cultured in two-dimensional (2D) and three-dimensional (3D) formats. It was shown that both unsubstituted calixarenes decrease the viability of tumor cells; calix[4]arene and calix[6]arene exhibited a cytostatic and a cytotoxic effect, respectively. Sulfated derivatives of calixarenes did not have a pronounced toxic effect on HT-29 cells. However, due to their high hydrophilicity and the ability to form adducts with various therapeutic molecules, they can be used for delivery of anticancer drugs. calixarenes, cytotoxicity, HT-29 cells, 2D cell culture, 3D cell culture The work was financially supported by the Russian Science Foundation (project no. 19-15-00397).

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