scholarly journals Targeting Colorectal Cancer Cells with a Functionalised Calix[4]arene Receptor: Biophysical Studies

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 510
Author(s):  
Angela F Danil de Namor ◽  
Nawal Al Hakawati ◽  
Sami Y Farhat

Colorectal cancer (CRC) is a disease which is causing a high degree of mortality around the world. The present study reports the antiproliferative impact of the thioacetamide calix[4]arene, CAII receptor on a highly differentiated Caco-2 cell line. This statement is corroborated by the MTT assay results which revealed a reduction in the cell viability with an IC50 value of 19.02 ± 0.04 µM. Microscopic results indicated that at the starting amount of 10 µM of CAII, a decrease in cells confluency can already be observed in addition to changes in cells morphology. Cell metabolic pathway changes were also investigated. 1H NMR findings showed downregulation in lactate, pyruvate, phosphocholine, lipids, and hydroxybutyrate with the upregulation of succinate, indicating a decline in the cells proliferation. Some biochemical alterations in the cells as a result of the CAII treatment were found by Raman spectroscopy.

The Analyst ◽  
2020 ◽  
Vol 145 (17) ◽  
pp. 5878-5888
Author(s):  
Julia Gala de Pablo ◽  
David R. Chisholm ◽  
Carrie A. Ambler ◽  
Sally A. Peyman ◽  
Andrew Whiting ◽  
...  

Tracking of the accumulation, activation, degradation of a photosensitiser and cell response in live colorectal cancer single-cells using Raman spectroscopy.


2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Ardalan Montazeri ◽  
Mina Ramezani ◽  
Azadeh Mohammadgholi

Background: Bromelain (BL) is an enzyme extracted from Ananas comosus, which has been known for its therapeutic properties. Objectives: The anticarcinogenic activity of BL was examined with and without the presence of magnetic carbon nanotubes (MCNTs) against HT-29 colorectal cancer cells. Methods: The operational factors affecting BL adsorption, such as contact time (30, 60, 90, 120, and 180 min), adsorbent dosage (1 g/L and 5 g/L), initial bromelain concentration (50, 150, and 300 mg/L), and temperature (35 and 50°C) were studied in details. Then, cancer cells were exposed to various BL concentrations (0.1, 1, 10, and 100 μg/mL), and the cell viability was determined by methylthiazol tetrazolium (MTT) assay after 24, 48, and 72 h. Results: The highest adsorption of BL on nanotubes was at 41.62 mg/L and achieved at 35°C and 90 min at the initial concentration of 50 mg/L and 1 g/L of MCNTs. The adsorption followed the Freundlich model and second-order kinetics. The results indicated that MCNTs could be a potential effective adsorbent for the removal of BL. Conclusions: MTT assay indicated that BL at a concentration of 100 μg/mL alone and in combination with MCNTs efficiently inhibited the HT-29 cancerous cells. However, encapsulated BL had a considerable advantage of slow delivery, which is favorable for cancer treatment.


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1741
Author(s):  
Anna Clua ◽  
Carme Fàbrega ◽  
Jesús García-Chica ◽  
Santiago Grijalvo ◽  
Ramon Eritja

Fluoropyrimidines, such as 5-fluorouracil (5-FU) and related prodrugs have been considered first-line chemotherapy agents for the treatment of colorectal cancer. However, poor specificity and tumor cell resistance remain major limiting bottlenecks. G-quadruplexes, have been suggested as preferred nanostructures for enhancing cellular uptake mediated by G-quadruplex binding proteins which are abundant at the membranes of some tumor cells. In the current study, we propose a new strategy to deliver 5-fluoro-2′-deoxyuridine (5-FdU) monophosphate, the main active drug from 5-FU derivatives that may circumvent the cellular mechanisms of FU-resistant cancer cells. Two G-quadruplexes delivery systems containing four and six G-tetrads ((TG4T) and (TG6T)) linked to a FdU oligonucleotide were synthesized. Biophysical studies show that the G-quadruplex parallel structures are not affected by the incorporation of the 5 units of FdU at the 5’-end. Internalization studies confirmed the ability of such G-quadruplex nanostructures to facilitate the transport of the FdU pentamer and increase its cytotoxic effect relative to conventional FU drug in FU-resistant colorectal cancer cells. These results suggest that FdU oligomers linked to G-quadruplex parallel sequences may be a promising strategy to deliver fluoropyrimidines to cancer cells.


The Analyst ◽  
2019 ◽  
Vol 144 (20) ◽  
pp. 6098-6107 ◽  
Author(s):  
Abdullah S. Mondol ◽  
Samir F. El-Mashtoly ◽  
Tatjana Frick ◽  
Klaus Gerwert ◽  
Jürgen Popp ◽  
...  

Label-free screening for cancer cells exposed to monoclonal antibody-based drugs using HCS-RS.


2021 ◽  
Vol 30 ◽  
pp. 096368972110532
Author(s):  
Xiao-Yu Chen ◽  
Sheng-Yong Yang ◽  
Xiao-Jie Ruan ◽  
Hong-Yue Ding ◽  
Ning-Xi Wang ◽  
...  

Methionine sulfoxide reductase B1 (MsrB1) can catalyze both free and protein-bound R-methionine sulfoxides (R-MetO) to methionine (Met). It has been reported that MsrB1 plays an important role in the development of HCC and human bone osteosarcoma. However, little is known about the functions of MsrB1 in human colorectal cancer (CRC). Herein, we detected MsrB1 expression level in CRC tissue and cell lines, and investigated the effect of MsrB1 knockdown on CRC phenotypes and possible mechanisms involved in. The results showed that MsrB1 was highly expressed in both CRC tissues and cell lines, and that cell proliferation, migration and invasion were significantly inhibited, but apoptosis was increased after MsrB1 knockdown in colorectal cancer HCT116 and RKO cell lines, compared to control siRNA group. In addition, E-cadherin protein level was increased, vimentin and Snail protein were greatly decreased after knockdown of MsrB1 in cells. Furthermore, pGSK-3β (Ser9) and β-catenin protein levels were reduced, the promoter activity of TCF/LEF construction was inhibited after MsrB1 knockdown in cells, suggesting that GSK-3β/β-catenin signaling axis was involved in the tumorigenesis of CRC. In conclusion, the oncogenic role and related mechanisms of MsrB1 in CRC discovered in our work determined the potential role of MsrB1 as a biomarker and may provide a new target for clinical therapy of CRC.


2021 ◽  
Author(s):  
Nakul Nautam Patel ◽  
Lucy Ghali ◽  
Ivan Roitt ◽  
Leonardo Pantoja Munoz ◽  
Richard Bayford

Colorectal cancer (CRC) is the fourth most common cancer in the world. Due to its asymptomatic nature, CRC is diagnosed at an advanced stage where the survival rate is <5%....


2003 ◽  
Vol 2 (1) ◽  
pp. 33-50
Author(s):  
Göran Gunner

Authors from the Christian Right in the USA situate the September 11 attack on New York and Washington within God's intentions to bring America into the divine schedule for the end of the world. This is true of Pat Robertson and Jerry Falwell, and other leading figures in the ‘Christian Coalition’. This article analyses how Christian fundamentalists assess the roles of the USA, the State of Israel, Islam, Iraq, the European Union and Russia within what they perceive to be the divine plan for the future of the world, especially against the background of ‘9/11’. It argues that the ideas of the Christian Right and of President George W. Bush coalesce to a high degree. Whereas before 9/11 many American mega-church preachers had aspirations to direct political life, after the events of that day the President assumes some of the roles of a mega-religious leader.


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