Background: Lung cancer is the deadliest type of cancer in the world and the search for compounds that can treat this disease is highly important. Lawsone (2-hydroxy-1,4-naphtoquinone) is a naphthoquinone found in plants from the Lawsone genus that show a high cytotoxic effect in cancer cell lines and its derivatives show an even higher cytotoxic effect.
Methods: Sulforhodamine B was used to evaluate the cytotoxic activity of compounds on tumor cells. Clonogenic assay was used to analyze the reduction of colonies and wound healing assay to the migratory capacity of A549 cells. Apoptosis and necrosis were analyzed by flow cytometer and Giemsa staining. Hemolysis assay to determine toxicity in human erythrocytes.
Results: Lawsone derivatives were evaluated and compound 1 (O-propargyllawsone) was the one with the highest cytotoxic effect, with IC below 2.5 µM in A549 cells. The compound was able to reduce colony formation and inhibit cell migration. Morphological changes and cytometry analysis show that the compound induces apoptosis and necrosis in A549 cells.
Conclusions: These results show that O-propargyllawsone show a cytotoxic effect and may induce apoptosis in A549 cells.
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http://dx.doi.org/10.1186/s12906-023-04156-9 | DOI Listing |
Sci Rep
January 2025
Department of Biology, Biotechnical Faculty, University of Ljubljana, Ljubljana, Slovenia.
Aureobasidium melanogenum is a black yeast-like fungus that occurs frequently both in nature and in domestic environments. It is becoming increasingly important as an opportunistic pathogen. Nevertheless, its effect on human cells has not yet been studied.
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Clinical Medical College, Changchun University of Chinese Medicine, Changchun, China.
In addressing the formidable challenge posed by methicillin-resistant Staphylococcus aureus (MRSA), this investigation elucidates a novel therapeutic paradigm by specifically targeting the virulence factor sortase A (SrtA) utilizing Tubuloside A (TnA). SrtA plays a critical role in the pathogenicity of MRSA, primarily by anchoring surface proteins to the bacterial cell wall, which is crucial for the bacterium's ability to colonize and infect host tissues. By inhibiting SrtA, TnA offers a novel and distinct strategy compared to traditional antibiotics.
View Article and Find Full Text PDFPLoS One
January 2025
Department of Oncology, Peking University First Hospital, Taiyuan Hospital, Taiyuan, Shanxi, China.
This work established the cytotoxic, antioxidant and anticancer effects of copper nanoparticles (CuNPs) manufactured with fennel extract, especially on non-small cell lung cancer (NSCLC) as well. CuNPs caused cytotoxicity in a dose-dependent manner for two NSCLC cell lines, A549 and H1650. At 100 μg/ml, CuNPs reduced cell viability to 70% in A549 cells and 65% in H1650 cells.
View Article and Find Full Text PDFFree Radic Res
January 2025
College of Pharmacy and Integrated Research Institute for Drug Development, Dongguk University, 32 Dongguk-ro, Goyang, Gyeonggi-do 10326, Korea.
Cancer genome sequencing studies have identified somatic mutations in the KEAP1/NRF2 pathway. In an effort to identify novel NRF2 small molecule inhibitor(s), we have screened a natural compound library comprising 1,330 chemicals in A549-ARE-GFP-luciferase cells and identified that narciclasine significantly inhibits NRF2-dependent luciferase activity. Narciclasine suppressed the expression of NRF2 and NRF2 target genes, caused significant oxidative stress, and sensitized cisplatin-mediated apoptosis in A549 cells.
View Article and Find Full Text PDFBiomed Rep
March 2025
Department of Biology, Xavier University of Louisiana, New Orleans, LA 70125, USA.
As a putative lung specific oncogene, the transducin-like enhancer of split 1 (TLE1) corepressor drives an anti-apoptotic and pro-epithelial-mesenchymal transition (EMT) gene transcriptional programs in human lung adenocarcinoma (LUAD) cells, thereby promoting anoikis resistance and tumor aggressiveness. Through its survival- and EMT-promoting gene regulatory programs, TLE1 may impact drug sensitivity and resistance in lung cancer cells. In the present study, a novel function of TLE1 was uncovered as an inhibitor of the antitumor effects of the epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) gefitinib in the human LUAD cell line A549, which exhibits moderate sensitivity to EGFR-TKI.
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