The Identification of a Novel Unsymmetrical Azine as an Apoptosis Inducer in Colorectal Cancer

2020 ◽  
Vol 20 ◽  
Author(s):  
Fahad M. Almutairi ◽  
Ayat G. Ali ◽  
Abdou O. Abdelhamid ◽  
Adel I. Alalawy ◽  
Mai K. Bishr ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Colorectal Carcinoma ◽  
Cell Line ◽  
Binding Affinity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Carcinoma Cell ◽  
Apoptosis Induction ◽  
Colorectal Carcinoma Cell Line ◽  
Hct 116

Background: Defects in the physiological mechanisms of apoptosis are one of the pivotal factors implicated in carcinogenesis. Thus, the development of novel compounds that target various apoptotic pathways has provided promising anticancer therapeutic opportunities. Objective: This study explores the cytotoxic effects of a novel unsymmetrical azine against specific cancer cell lines and investigates the mechanism of cytotoxicity. Methods: Molecular modeling was used to test the binding affinity of four new unsymmetrical azines to a model of an apoptosis inhibitor protein (XIAP). The compound with the highest binding affinity, C4, was further tested on different cell lines. Real-time polymerase chain reaction (PCR) and transmission electron microscope (TEM) were used to study apoptosis induction biochemically and morphologically. Results: In comparison to cisplatin as a control, the compound C4 exhibited notable cytotoxicity against all tested cancer cell lines, especially the human colorectal carcinoma cell line (HCT-116). Furthermore, C4-treated cells demonstrated marked overexpression of the pro-apoptotic proteins Bax and caspase-3 as well as the tumor suppressor p53. On the other hand, the expression of the anti-apoptotic protein Bcl-2 was inhibited. On TEM examination, C4-treated HCT-116 cells showed classical structural signs of apoptosis. Conclusion: This study identifies a novel azine (C4) which induces remarkable cytotoxicity against colorectal carcinoma cell line, mediated through apoptosis induction. These novel insights suggest C4 as a promising therapeutic agent in colorectal cancer.

scholarly journals Synthesis of New Pt(II) Complex Bearing Organoselenium Ligands and Evaluation of Cytotoxic Activity of Some Structurally Related Pd(II) Complexes

2020 ◽  
Vol 39 (1) ◽  
pp. 59
Author(s):  
Ninko Radenković ◽  
Marina Kostić ◽  
Nataša Đorđević ◽  
Zana Doličanin ◽  
Tanja Soldatović ◽  
...  
Keyword(s):  
Colorectal Carcinoma ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Mtt Assay ◽  
Carcinoma Cell ◽  
In Vitro Study ◽  
Colorectal Carcinoma Cell Line ◽  
Hct 116 ◽  
Healthy Lung

Herein we report the synthesis of new trans-bis(2-phenylselenylmethyl)oxolane)dichloroplatinum(II) complex Pt1. Newly synthetized complex, together with two, structurally related trans-Pd(II) complexes (trans-bis(2-(phenylselenylmethyl)oxolane)dichloropalladium(II) Pd1 and trans-bis(2-(phenylselenylmethyl)oxane)dichloropalladium(II)) Pd2, were screened for cytotoxic activity through in vitro study on the HCT-116 colorectal carcinoma cell line and on the MRC-5 healthy lung pleura cell line. Activity of complexes was assessed by comparing it to the cisplatin. The cells viability and proliferation were determined using MTT assay.

Characterization of Alternatively Spliced Isoforms of MUC4 and ADAM12 Genes in a Metastatic Colorectal Cancer Cell Line Model

2021 ◽  
Author(s):  
Saleh Althenayyan ◽  
Mohammed H AlMuhanna ◽  
Abdulkareem Al Abdulrahman ◽  
Bandar Alghanem ◽  
Suliman A. Alsagaby ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Metastatic Colorectal Cancer ◽  
Cell Line ◽  
Differential Expression ◽  
Cell Lines ◽  
Cancer Cell ◽  
Colorectal Cancer Cell ◽  
Line Model ◽  
Cell Line Model ◽  
Alternatively Spliced

Colorectal cancer prognosis get worse with advancement of disease into metastatic stage. There is a pertinent need to develop prognostic biomarkers that can be used for personalized and precision medicine. Alternative splicing provides an insight into understanding of changes at isoform expression level which may not be evident at gene level. In this direction, we utilized our prior knowledge about significant alternatively spliced genes and chose ADAM12 and MUC4 for further characterization in a metastatic cell line model. These genes were found to be good prognostic indicators in The Cancer Genome Atlas database. We studied the gene organization and designed primers to specifically amplify a group of isoforms. Differential expression of these group of isoforms was observed in normal, primary and metastatic colorectal cancer cell lines. We further validated the results using sanger sequencing. Isoform expression was found to respond to the 5-fluorouracil treatment. RNAseq analysis of the cell lines further validated the differential expression of gene isoforms. Successful detection of ADAM12 and MUC4 in cell lysates varied according to the antibody used which may reflect differential expression of isoforms. This comprehensive study underscores the importance of studying alternatively spliced isoforms and their probable used as prognostic or predictive biomarkers.

scholarly journals Promising Anticancer Activity of [Bis(1,8-quinolato)palladium (II)] Alone and in Combination

2020 ◽  
Author(s):  
Md. Nur Alam ◽  
Mohammad Moni ◽  
Jun Yu ◽  
Philip Beale ◽  
Peter Turner ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Epigallocatechin Gallate ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
Colorectal Cancer Cell Line

Abstract Due to similar coordination chemistry of palladium and platinum, a large number of palladium compounds too have been investigated for their anticancer activity. In the present study we describe synthesis, characterization and anticancer activity of palladium complex [Bis(1,8-quinolato)palladium (II)], coded as NH3 against seven different cancer cell lines. NH3 is found to have higher antitumour activity than cisplatin against both parent ovarian A2780 cell line and cisplatin-resistant cell lines. Also, NH3 has the lowest IC50 value against HT-29 colorectal cancer cell line. The higher antitumour activity of NH3 is due to the presence of bulky 8-hydroxy-quinoline ligand thus reducing its reactivity. Proteomic study has identified significantly expressed proteins which have been validated through bioinformatics. NH3 has been found to be less toxic than cisplatin at 2.5 mg/kg and 5 mg/kg dosages on mice models. Binary combinations of NH3 with curcumin and epigallocatechin gallate (EGCG) have demonstrated dose and sequence dependent synergism in ovarian and colorectal cancer models. All of the preclinical studies indicate promising therapeutic potentiality of NH3 [Bis(1,8-quinolato)palladium (II) ] as an anticancer drug.

scholarly journals Anti-migration Effect of Aaptos suberitoides Fraction in HCT-116 Colorectal Cancer Cell Line

2021 ◽  
Vol 8 (1) ◽  
Author(s):  
Dany Muhammad Daffa ◽  
Muhammad Hasan Bashari ◽  
Eko Fuji Ariyanto ◽  
Tenny Putri ◽  
Nurul Qomarilla
Keyword(s):  
Colorectal Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cellular Migration ◽  
Colorectal Cancer Cell Line ◽  
Migration Inhibition ◽  
Migration Activity ◽  
Migration Effect ◽  
Hct 116

Background: Colorectal cancer is the second leading cause of mortality and the most prevalent cancer worldwide. Most patients, who come with late-stage, have ineffective treatments and some side effects in chemotherapy. Aaptos suberitoides has potential anti-cancer effects due to its bioactive compounds such as aptamine. This study aimed to evaluate the migration inhibition effect of Aaptos suberitoides fraction in HCT-116 cell line.Methods: This study was an experimental study. Aaptos suberitoides specimen was taken in Tinjil Island and fractionated with ethyl acetate. HCT-116 cell line was added with Aaptos suberitoides fraction and cellular migration activity was observed in 48 hours of which the scratch assay was performed. The gap closure area was determined with ImageJ software.Results: The data showed that a low concentration of Aaptos suberitoides fraction inhibited migration activity in HCT-116 cell line as follow; 1 and 5 mg/L Aaptos suberitoides fraction inhibit 3-4 % cancer cell migration in 24 hours, and 10-11% inhibition in 48 hours, respectively. However, 10 mg/L fraction concentration only inhibited 7-14% of the migration effect.Conclusion: Aaptos suberitoides fraction suggests insignificant migration inhibition in colorectal cancer cells and only inhibits less than 15 % HCT-116 cell line.

Gamma-Tocopherol Enhances Apoptotic Effects of Lovastatin in Human Colorectal Carcinoma Cell Line (HT29)

2014 ◽  
Vol 66 (8) ◽  
pp. 1386-1393 ◽  
Author(s):  
Mohsen Rezaei ◽  
Leila Zeidooni ◽  
Mahmoud Hashemitabar ◽  
Sareh Razzazzadeh ◽  
Masoud Mahdavinia ◽  
...  
Keyword(s):  
Colorectal Carcinoma ◽  
Cell Line ◽  
Carcinoma Cell ◽  
Carcinoma Cell Line ◽  
Gamma Tocopherol ◽  
Colorectal Carcinoma Cell Line ◽  
Human Colorectal Carcinoma Cell ◽  
Human Colorectal Carcinoma ◽  
Apoptotic Effects
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