Article ; Online: Modes of cell death induced by tetrahydroisoquinoline-based analogs in MDA-MB-231 breast and A549 lung cancer cell lines.
Drug design, development and therapy
2018 Volume 12, Page(s) 1881–1904
Abstract: Background: A and B rings of the steroidal microtubule disruptor, 2-methoxyestradiol, and its analogs can be mimicked with a tetrahydroisoquinoline (THIQ) core. THIQs are cytotoxic agents with potential anticancer activities. The aim of this in vitro ... ...
| Abstract | Background: A and B rings of the steroidal microtubule disruptor, 2-methoxyestradiol, and its analogs can be mimicked with a tetrahydroisoquinoline (THIQ) core. THIQs are cytotoxic agents with potential anticancer activities. The aim of this in vitro study was to investigate the modes of cell death induced by four nonsteroidal THIQ-based analogs, such as STX 2895, STX 3329, STX 3451 and STX 3450, on MDA-MB-231 metastatic breast and A549 epithelial lung carcinoma cells. Materials and methods: Cytotoxicity studies determined the half-maximal growth inhibitory concentration of the analogs to be at nanomolar concentrations without the induction of necrosis. Light and fluorescent microscopy determined that compounds caused microtubule depolymerization and displayed morphological hallmarks of apoptosis. Results: Flow cytometric analyses confirmed apoptosis induction as well as an increased G Conclusion: Thus, it can be concluded that these four THIQ-based analogs exert anti-proliferative and antimitotic effects, induce apoptosis and involve autophagic processes. Further investigation into the efficacy of these potential anticancer drugs will be conducted in vitro and in vivo. |
|---|---|
| MeSH term(s) | Apoptosis/drug effects ; Cell Cycle/drug effects ; Cell Line, Tumor ; Cytochromes c/metabolism ; Humans ; L-Lactate Dehydrogenase/analysis ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Membrane Potential, Mitochondrial/drug effects ; Microscopy, Polarization ; Tetrahydroisoquinolines/pharmacology |
| Chemical Substances | Tetrahydroisoquinolines ; Cytochromes c (9007-43-6) ; L-Lactate Dehydrogenase (EC 1.1.1.27) |
| Language | English |
| Publishing date | 2018-06-25 |
| Publishing country | New Zealand |
| Document type | Journal Article |
| ZDB-ID | 2451346-5 |
| ISSN | 1177-8881 ; 1177-8881 |
| ISSN (online) | 1177-8881 |
| ISSN | 1177-8881 |
| DOI | 10.2147/DDDT.S152718 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
More links
Kategorien
Order via subito
This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.