Aim: To validate 3-(6,7-dimethoxy-3,4-dihydroisoquinoline-2-carbonyl)-N-(2 methoxyphenyl)benzenesulphonamide (B1) as a potential BRAF V600E inhibitor via in vitro analyses.
Study Design: Tests were carried out on HT-29 human colon cancer
cell lines. Various studies such as clonogenic assay, apoptotic studies,
Reactive Oxygen Species (ROS) studies and Indirect ELISA tests were carried out
in both the control sample and B1-incorporated sample for determining the
efficacy of B1.
Place and Duration of Study: The study was conducted at Sahrdaya
College of Engineering and Technology, Kodakara and Centre for Research on
Molecular and Applied Sciences, Thiruvananthapuram, between October 2023 and
February 2024.
Methodology: In this study, many in vitro analyses were carried
out to verify the BRAF V600E inhibition ability of B1 to be used as a potential
drug candidate against the treatment of CRC. HT-29 human colon cancer cell
lines were grown. Following that, clonogenic assay was performed to measure the
cell growth, apoptotic studies to figure out the cell vitality, Reactive Oxygen
Species (ROS) studies to calculate the amount of ROSs present, and Indirect
ELISA tests to quantify the total protein concentration were performed in both
control sample and B1-incorporated sample.
Results: The molecule B1 significantly reduced the colony formation,
increased the cell mortality, and elevated ROSs levels. The concentration of
ERK (the downstream protein of BRAF) was likewise significantly reduced in the
B1 sample, implying that the substance B1 is an efficient inhibitor of BRAF.
All the results pointed to the fact that B1 can be used as an effective BRAF
V600E inhibitor.
Conclusion: This work established the effectiveness of the
molecule B1 as an effective inhibitor against BRAF for the treatment of CRC.
Author
(s) Details
Amrutha
Krishnan K
Department of Applied Science and Humanities, Sahrdaya College of
Engineering and Technology, Kodakara, Affiliated to APJ Abdul Kalam
Technological University, Thiruvananthapuram, India.
Sudha
George Valavi
Department of Applied Science and Humanities, Sahrdaya College of
Engineering and Technology,
Kodakara, Affiliated to APJ Abdul Kalam Technological University,
Thiruvananthapuram, India.
Amitha
Joy
Department of Biotechnology, Sahrdaya College of Engineering and
Technology, Kodakara, Affiliated to APJ Abdul Kalam Technological University,
Thiruvananthapuram, India.
Please see the book here:- https://doi.org/10.9734/bpi/mono/978-93-49238-47-3/CH26
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