scholarly journals Anti-human lung cancer activities and survey of gluthation reductase and gluthation S transferase inhibition properties with molecular modeling studies of 2′-Hydroxy-5′-methyl-3′-nitroacetophenone: A pre-clinical trial study

2021 ◽  
Author(s):  
Yawei Dou ◽  
shanshan Lv ◽  
Attalla F. El-kott ◽  
Ayman E. El-kenawy
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Human Lung ◽  
Antioxidant Properties ◽  
Human Lung Cancer ◽  
Lung Cancers ◽  
Anticancer Properties ◽  
Ic50 Values ◽  
Human Lung Carcinoma

IntroductionRecently, scientists have tried to increase organic chemistry productions for the treatment of many cancers such as lung cancers. In this regard, antioxidant molecules have a special place in the treatment of several cancers. The molecular docking method was found to calculate the biological activity of the 2′-Hydroxy-5′-methyl-3′-nitroacetophenone (2′-H-5′-M-3′-N) molecule against the enzymes studied.Material and methodsIn these calculations, the enzymes used are gluthation reductase (GR) enzyme and Glutathione S-Transferase (GT) enzyme, respectively. After the modeling calculations were completed, the ADME/T parameters were examined to calculate the future drug use properties of the 2′-H-5′-M-3′-N molecule. To survey the antioxidant properties of 2′-H-5′-M-3′-N, the DPPH test was used. Several human lung adenocarcinoma cell lines i.e., lung moderately differentiated adenocarcinoma (LC-2/ad), lung poorly differentiated adenocarcinoma (PC-14), and lung well-differentiated bronchogenic adenocarcinoma (HLC-1) cell lines were used to determine the anticancer properties of the recent molecule.ResultsCell viability of 2′-H-5′-M-3′-N was very low against PC-14, LC-2/ad, and HLC-1 cell lines without any cytotoxicity on the normal cell line. The IC50 values of 2′-H-5′-M-3′-N against LC-2/ad, PC-14, and HLC-1 cell lines were found 475, 250, and 691 µg/mL, respectively. The best anti-human lung cancer properties of 2′-H-5′-M-3′-N against the above cell lines was in the case of PC-14 cell line.ConclusionsAs mentioned, the 2′-H-5′-M-3′-N had significant antioxidant and anti-human lung cancer properties. It appears that the anti-human lung carcinoma effect of 2′-H-5′-M-3′-N is due to their antioxidant effects.

Antiproliferative Activity of Protopine Extract from Fumaria agraria Against Human Lung Cancer Cell Lines

2021 ◽  
Author(s):  
K. Bougoffa-Sadaoui ◽  
F. Maiza-Benabdesselam ◽  
H. Ouadid-Ahidouch
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Lung ◽  
Cancer Cell Lines ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Antitumor Effects ◽  
Fumaria Agraria

Little information is reported on the antitumor effects of isoquinoline alkaloids, particularly protopine, a major component of Fumaria agraria, on lung cancer. The purpose of our study is to determine the cytotoxic effect of protopine from an extraction by fractionation of the aerial part of Fumaria agraria on two lung cancer cell lines, NCI-H23 and NCI-H460. The basic fraction containing protopine (60.7%) has cytotoxicity to the two lung cancer cell lines studied here. The cell line NCI-H460 is more sensitive after 72 h of treatment by protopine with an IC50 of 08.5 ± 0.09 μMthan the cell line NCI-H23 (IC50 = 14.8 ± 0.03 μM).

scholarly journals Efficient culture of SARS-CoV-2 in human hepatoma cells enhances viability of the virus in human lung cancer cell lines permitting the screening of antiviral compounds

2020 ◽  
Author(s):  
Santseharay Ramirez ◽  
Carlota Fernandez-Antunez ◽  
Long V. Pham ◽  
Line A. Ryberg ◽  
Shan Feng ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cell ◽  
Human Lung ◽  
Human Cells ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Human Lung Cancer Cell

AbstractEfforts to mitigate COVID-19 include screening of existing antiviral molecules that could be re-purposed to treat SARS-CoV-2 infections. Although SARS-CoV-2 propagates efficiently in African green monkey kidney (Vero) cells, antivirals such as nucleos(t)ide analogs (nucs) often exhibit decreased activity in these cells due to inefficient metabolization. Limited SARS-CoV-2 replication and propagation occurs in human cells, which are the most relevant testing platforms. By performing serial passages of a SARS-CoV-2 isolate in the human hepatoma cell line clone Huh7.5, we selected viral populations with improved viability in human cells. Culture adaptation led to the emergence of a significant number of high frequency changes (>90% of the viral population) in the region coding for the spike glycoprotein, including a deletion of nine amino acids in the N-terminal domain and 3 amino acid changes (E484D, P812R, and Q954H). We demonstrated that the Huh7.5-adapted virus exhibited a >3-Log10 increase in infectivity titers (TCID50) in Huh7.5 cells, with titers of ~8 Log10TCID50/mL, and >2-Log10 increase in the human lung cancer cell line Calu-1, with titers of ~6 Log10TCID50/mL. Culture adaptation in Huh7.5 cells further permitted efficient infection of the otherwise SARS-CoV-2 refractory human lung cancer cell line A549, with titers of ~6 Log10TCID50/mL. The enhanced ability of the virus to replicate and propagate in human cells permitted screening of a panel of nine nucs, including broad-spectrum compounds. Remdesivir, EIDD-2801 and to a limited extent galidesivir showed antiviral effect across these human cell lines, whereas sofosbuvir, uprifosbuvir, valopicitabine, mericitabine, ribavirin, and favipiravir had no apparent activity.ImportanceThe cell culture adapted variant of the SARS-CoV-2 virus obtained in the present study, showed significantly enhanced replication and propagation in various human cell lines, including lung derived cells otherwise refractory for infection with the original virus. This SARS-CoV-2 variant will be a valuable tool permitting investigations across human cell types, and studies of identified mutations could contribute to our understanding of viral pathogenesis. In particular, the adapted virus can be a good model for investigations of viral entry and cell tropism for SARS-CoV-2, in which the spike glycoprotein plays a central role. Further, as shown here with the use of remdesivir and EIDD-2801, two nucs with significant inhibitory effect against SARS-CoV-2, large differences in the antiviral activity are observed depending on the cell line. Thus, it is essential to select the most relevant target cells for pre-clinical screenings of antiviral compounds, facilitated by using a virus with broader tropism.

scholarly journals A pre-clinical trial study on Afzelin: Anti-human lung cancer, anti-cholinesterase, and anti-glucosidase properties

2021 ◽  
Author(s):  
Ming Cao ◽  
Bo Fan ◽  
Tianchang Zhen ◽  
Junling Wang
Keyword(s):  
Lung Cancer ◽  
Human Lung ◽  
Human Lung Cancer ◽  
Cytotoxicity Test ◽  
Acetyl Cholinesterase ◽  
Ic50 Values ◽  
Human Lung Carcinoma ◽  
Plant Metabolite ◽  
Antibacterial And Antifungal

IntroductionAfzelin is a glycosyloxyflavone that is kaempferol attached to an alpha-L-rhamnosyl residue at position 3 via a glycosidic linkage. It has a role as a plant metabolite, an antimicrobial (Antibacterial and antifungal) agent and an anti-inflammatory agent. It is a glycosyloxyflavone, a trihydroxyflavone and a monosaccharide derivative. In this work, we determined the anticholinergic, antiepileptic, antidiabetic, and anti-human lung cancer capacities of afzelin.Material and methodsIC50 values were calculated for both acetylcholinesterase, and α-glycosidase as key enzymes effects of afzelin. The cytotoxicity and anticancer potential of human lung over the Afzelin using the common cytotoxicity test i.e., 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay in vitro condition.ResultsIC50 values obtained 365.11 nM for acetyl cholinesterase and 0.94 nM for α-glycosidase were calculated in this study. Indeed, for these enzymes, Ki values were found as 300.65±56.01 nM for acetyl cholinesterase and 1.65±0.11 nM for α-glucosidase. Cell viability of Afzelin was very low against lung poorly differentiated adenocarcinoma (PC-14), lung moderately differentiated adenocarcinoma (LC-2/ad), and lung well-differentiated bronchogenic adenocarcinoma (HLC-1) cell lines without any cytotoxicity on the normal cell line.ConclusionsAs mentioned, the Afzelin had significant antioxidant and anti-human lung cancer properties. It appears that the anti-human lung carcinoma effect of Afzelin is due to their antioxidant effects.

Toxic effect of TiO2 nanoparticles against human lung cancer cell line A549

2011 ◽  
Vol 31 (10) ◽  
pp. 1091-1095
Author(s):  
Xiao-lin LI ◽  
Yan-fang ZHANG ◽  
Kai TANG ◽  
Ying TANG ◽  
Ruo-bing JIN ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Toxic Effect ◽  
Cell Line ◽  
Cancer Cell ◽  
Human Lung ◽  
Cancer Cell Line ◽  
Lung Cancer Cell Line ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Human Lung Cancer Cell

scholarly journals Apoptosis Activation in Human Lung Cancer Cell Lines by a Novel Synthetic Peptide Derived from Conus californicus Venom

Toxins ◽  
2016 ◽  
Vol 8 (2) ◽  
pp. 38 ◽  
Author(s):  
Irasema Oroz-Parra ◽  
Mario Navarro ◽  
Karla Cervantes-Luevano ◽  
Carolina Álvarez-Delgado ◽  
Guy Salvesen ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Synthetic Peptide ◽  
Human Lung ◽  
Cancer Cell Lines ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Human Lung Cancer Cell
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