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1.
Artigo em Inglês | MEDLINE | ID: mdl-38157154

RESUMO

Lung malignancy is a major worldwide issue that occurs due to the dysregulation of various growth factors. Lung cancer has no apparent signs in the early stages, which makes it harder to catch it in time and leads to a higher fatality rate. So, the goal of this work was to create and analyze a novel chemical molecule called 4-nitro acetophenone thiosemicarbazone (4-NAPTSc) against the lung cancer cell line A549 and human non-tumorigenic lung epithelial cell line BAES-2B. The ligand was synthesized by refluxing the reaction mixture of 4-nitro acetophenone and thiosemicarbazide and was further characterized by UV, FTIR, and 1H and 13C NMR and Differential Scanning Calorimetry (DSC) study. Cytotoxicity assay/MTT (3-(4,5-dimethylthiazol-2-yl))2,5-diphenyltetrazolium bromide) was used to evaluate the cytotoxicity of the compound. Epidermal growth factor receptors (EGFR), polo-like kinase-1 (PLK1), and vascular endothelial growth factor receptors (VEGFR) were chosen as the target proteins for molecular docking to find potential ligand binding sites and inhibit their function. A novel yellow-colored crystalline solid has been synthesized. 4-NAPTSc had an IC50 of 2.93 µg/mL against the A549 lung cancer cells. When the dosage is increased from 5 to 15 µg/mL along with time, the cell viability falls. Docking results showed that the compound binds with the targeted proteins' amino acid residues, and the likeness profile of the compound is also favorable. This study reveals that the compound has the potential for further investigation and can be used in multitargeted cancer therapies.

2.
Curr Pharm Biotechnol ; 23(7): 932-945, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34375184

RESUMO

Occupational exposure to pesticides has been associated with adverse health conditions, including genotoxicity and cancer. Nullity of GSTT1/GSTM1 increases the susceptibility of pesticide workers to these adverse health effects due to lack of efficient detoxification process created by the absence of these key xenobiotic metabolizing enzymes. However, this assertion does not seem to maintain its stance at all the time; some pesticide workers with the null genotypes do not present the susceptibility. This suggests the modulatory role of other confounding factors, genetic and environmental conditions. Pesticides, aggravated by the null GSTT1/GSTM1, cause genotoxicity and cancer through oxidative stress and miRNA dysregulation. Thus, the absence of these adverse health effects together with the presence of null GSTT1/GSTM1 genotypes demands further explanation. Also, understanding the mechanism behind the protection of cells - that are devoid of GSTT1/GSTM1 - from oxidative stress constitutes a great challenge and potential research area. Therefore, this review article highlights the recent advancements in the presence and absence of cancer risk in occupational pesticide workers with GSTT1 and GSTM1 null genotypes.


Assuntos
Neoplasias , Praguicidas , Dano ao DNA , Genótipo , Glutationa , Glutationa Transferase/genética , Humanos , Praguicidas/toxicidade , Risco , Fatores de Risco
3.
Mol Cell Biochem ; 440(1-2): 1-9, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28819931

RESUMO

In the present era, cellular phones have changed the life style of human beings completely and have become an essential part of their lives. The number of cell phones and cell towers are increasing in spite of their disadvantages. These cell towers transmit radiation continuously without any interruption, so people living within 100s of meters from the tower receive 10,000 to 10,000,000 times stronger signal than required for mobile communication. In the present study, we have examined superoxide dismutase (SOD) enzyme activity, catalase (CAT) enzyme activity, lipid peroxidation assay, and effect of functional polymorphism of SOD and CAT antioxidant genes against mobile tower-induced oxidative stress in human population. From our results, we have found a significantly lower mean value of manganese superoxide dismutase (MnSOD) enzyme activity, catalase (CAT) enzyme activity, and a high value of lipid peroxidation assay in exposed as compared to control subjects. Polymorphisms in antioxidant MnSOD and CAT genes significantly contributed to its phenotype. In the current study, a significant association of genetic polymorphism of antioxidant genes with genetic damage has been observed in human population exposed to radiations emitted from mobile towers.


Assuntos
Antioxidantes/metabolismo , Catalase/sangue , Telefone Celular , Peroxidação de Lipídeos , Ondas de Rádio/efeitos adversos , Superóxido Dismutase/sangue , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade
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