Abstract
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.
Highlights
Receptor: Biophysical Studies.Colorectal cancer (CRC), known as bowel cancer, affects over 1.93 million people worldwide and has led to almost 935,000 deaths according to the report published by the World Health Organization (WHO) in March 2021
The major drawbacks in these therapies have led to extensive studies in the last three decades aimed at designing selective anticancer agents targeting only cancer cells such as those based on nanotechnology, surface modifications of polymer drugs, and the use of cancer biomarkers [7]
The compound mode of action is mediated by an apoptosis mechanism that is considered to be an important aspect in defeating cancer
Summary
Colorectal cancer (CRC), known as bowel cancer, affects over 1.93 million people worldwide and has led to almost 935,000 deaths according to the report published by the World Health Organization (WHO) in March 2021. Calixarenes have received particular attention in the pharmaceutical field as active anticancer, antidiabetic, anti-obesity [8], and antibacterial agents [9] Studies on their anticancer properties have been the subject of several research groups [10,11], where investigations in vitro against different types of cancer cell lines were conducted. The outcome of their research revealed that these cancer activity, especially in melanoma cells (skin cancer) and lymphoblastic leukaemia calix[4]arene derivatives have groups a potenthave anticancer especially in melanoma cells.
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