scholarly journals Enhancement of Docetaxel Anticancer Activity by a Novel Diindolylmethane Compound in Human Non-Small Cell Lung Cancer

2009 ◽  
Vol 15 (2) ◽  
pp. 543-552 ◽  
Author(s):  
N. Ichite ◽  
M. B. Chougule ◽  
T. Jackson ◽  
S. V. Fulzele ◽  
S. Safe ◽  
...  
Cells ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1632
Author(s):  
Alexis Rugamba ◽  
Dong Young Kang ◽  
Nipin Sp ◽  
Eun Seong Jo ◽  
Jin-Moo Lee ◽  
...  

Recently, natural compounds have been used globally for cancer treatment studies. Silibinin is a natural compound extracted from Silybum marianum (milk thistle), which has been suggested as an anticancer drug through various studies. Studies on its activity in various cancers are undergoing. This study demonstrated the molecular signaling behind the anticancer activity of silibinin in non-small cell lung cancer (NSCLC). Quantitative real-time polymerase chain reaction and Western blotting analysis were performed for molecular signaling analysis. Wound healing assay, invasion assay, and in vitro angiogenesis were performed for the anticancer activity of silibinin. The results indicated that silibinin inhibited A549, H292, and H460 cell proliferation in a concentration-dependent manner, as confirmed by the induction of G0/G1 cell cycle arrest and apoptosis and the inhibition of tumor angiogenesis, migration, and invasion. This study also assessed the role of silibinin in suppressing tumorsphere formation using the tumorsphere formation assay. By binding to the epidermal growth factor receptor (EGFR), silibinin downregulated phosphorylated EGFR expression, which then inhibited its downstream targets, the JAK2/STAT5 and PI3K/AKT pathways, and thereby reduced matrix metalloproteinase, PD-L1, and vascular endothelial growth factor expression. Binding analysis demonstrated that STAT5 binds to the PD-L1 promoter region in the nucleus and silibinin inhibited the STAT5/PD-L1 complex. Altogether, silibinin could be considered as a candidate for tumor immunotherapy and cancer stem cell-targeted therapy.


Author(s):  
Kelvin F. Pratama ◽  
Muhammad Fauzi ◽  
Aliya Nur Hasanah

The biggest case of death in 2018 is caused by lung cancer. Non-small cell lung cancer (NSCLC) is most common. One of the cause lung cancer is the over expression of EGFR. Erlotinib is the first line of anticancer for NSCLC with EGFR mutations. However, erlotinib can cause side effects such as liver damage therefore new safe anticancer is needed. Trigonelline is an alkaloid compound from coffee beans that had anticancer activity in pancreatic cancer cells by inhibiting Nrf2 in vitro and in vivo at concentrations of 0.1-1 µM. Development of cancer cells by Nrf2 is regulated by EGFR. In this study screening and modification of trigonelline structure was carried out to obtain compounds that have anticancer activity on NSCLC against EGFR computationally. The research procedures carried out are modification of ten trigonelline derived structures, the molecular docking and prediction of physicochemical profiles from trigonelline and its modification also their ADMET. Based on results, KF9 has the lowest free energy of binding which was -8,88 kcal/mol and binds to Met769 which has biological activity with receptor. KF9 has good physiochemical profile and absorption, distribution, also toxicity parameters. KF9 has potential to become a new anticancer drug for NSCLC.Keywords: Coffee, Drug discovery and Drug development, Molecular structure modification, Nonsmall cell lung cancer, Trigonelline


2013 ◽  
Vol 30 (2) ◽  
pp. 863-869 ◽  
Author(s):  
HYUNSEUNG LEE ◽  
SOO JUNG KIM ◽  
KYUNG HEE JUNG ◽  
MI KWON SON ◽  
HONG HUA YAN ◽  
...  

2018 ◽  
Vol 156 ◽  
pp. 190-205 ◽  
Author(s):  
Huan Tang ◽  
Yongguang Zhang ◽  
Dan Li ◽  
Suhong Fu ◽  
Minghai Tang ◽  
...  

2019 ◽  
Vol 18 ◽  
pp. 153303381989226 ◽  
Author(s):  
Jian-Hua Ge ◽  
Jing-Wei Zhu ◽  
Hai-Yan Fu ◽  
Wen-Bo Shi ◽  
Chun-Lai Zhang

Non-small cell lung cancer is the most common malignant tumor in the world. Currently, chemotherapy is still the major method for non-small cell lung cancer treatment, but the problem of cancer drug resistance still exists, so we designed 5 different phosphorothioate oligonucleotides to silence key genes in tumor cell development, which could help avoid inducing cancer cell drug resistance. MicroRNAs have been shown to play a crucial role in the pathogenesis and progression of many malignancies, such as breast, colon, lung, and pancreatic cancer. According to the data from the Gene Expression Omnibus database, miR-21 has been reported to be one of the top 20 differentially expressed microRNAs screened using the Morpheus online tool, and miR-21 has been revealed to regulate a series of biological behaviors in cancer cells, including cell proliferation, migration, invasion, metastasis, and apoptosis. In recent years, gene therapy has emerged as a new therapeutic strategy for cancer treatment. Antisense oligonucleotides have recently been suggested as a novel approach for targeting microRNAs by antisense-based gene silencing. Five phosphorothioate oligonucleotides were designed, synthesized, and screened for anticancer activity. Reverse transcription-polymerase chain reaction was used to detect the relative expression of miR21. Among these 5 sequences, only phosphorothioate oligonucleotide 4 inhibited the proliferation of H1650 cells, and this effect was due to the induction of cancer cell apoptosis by activating the caspase-8 apoptotic pathway. In conclusion, this research confirmed the anticancer activity of phosphorothioate oligonucleotide 4 and revealed the underlying mechanism, which has the potential to be a novel anticancer strategy.


Sign in / Sign up

Export Citation Format

Share Document