Cytotoxic and cytostatic effects of DIGITOXIGENIN (cas 143-62-4) monodigitoxoside (DGX) in human lung cancer cells and its link to Na,K-ATPase
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Add time:09/29/2019 Source:infona.pl
Cardiac glycosides (CGs) are natural compounds widely used to treat several cardiac conditions and more recently have been recognized as potential antitumor agents. They are known as Na,K-ATPases ligands, which is a promising drug target in cancer. In this study, the short and long-lasting cytotoxic effects of the natural cardenolide DIGITOXIGENIN (cas 143-62-4) monodigitoxoside (DGX) were evaluated against two non-small cell lung cancer lines (A549 and H460 cells). It was found that DGX induced cytotoxic effects in both cells and the apoptotic effects were more pronounced on H460 cells. In long-term analysis, using the clonogenic and the cumulative population doubling (CPD) assays, DGX showed a reduction of cell survival, after 15days without re-treatment. To better understand DGX effects in A549 cells, several assays were conducted. In cell cycle analysis, DGX caused an arrest in S and G2/M phases. This compound also increased the number of cells in subG1 phase in a concentration- and time-dependent manner. The presence of β-galactosidase positive cells, large nucleus and flattened cells indicated senescence. Additionally, DGX inhibited Na,K-ATPase activity in A549 cells, as well as in purified pig kidney and in human red blood cell membrane preparations, at nanomolar range. Moreover, results of molecular docking showed that DGX binds with high efficiency (−11.4Kcal/mol) to the Na,K-ATPase (PDB:4HYT). Taken together, our results highlight the potent effects of DGX both in A549 and H460 cells, and disclose its link with Na,K-ATPase inhibition.
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Next:Synthesis and biological evaluation of 2-Hydroxy derivatives of DIGITOXIGENIN (cas 143-62-4) and 3-EpiDIGITOXIGENIN (cas 143-62-4)1A preliminary account of this work has been presented at the First International Electronic Conference on Synthetic Organic Chemistry (ECSOC-1), A0012, 1–30 September 1997; http://www.mdpi.org/escoc-1.htm1) - 【Back】【Close 】【Print】【Add to favorite 】
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- Synthesis and biological evaluation of 2-Hydroxy derivatives of DIGITOXIGENIN (cas 143-62-4) and 3-EpiDIGITOXIGENIN (cas 143-62-4)1A preliminary account of this work has been presented at the First International Electronic Conference on Synthetic Organic Chemistry (ECSOC-1), A0012, 1–30 September 1997; http://www.mdpi.org/escoc-1.htm109/30/2019
- Effect of ouabain, digoxin and DIGITOXIGENIN (cas 143-62-4) on potassium uptake and histamine release from rat peritoneal mast cells09/28/2019