Please use this identifier to cite or link to this item:
https://hdl.handle.net/10216/120481
Author(s): | Lima R.T. Sousa D. Gomes A.S. Mendes N. Matthiesen R. Pedro M. Marques F. Pinto M.M. Sousa E. Helena Vasconcelos M. |
Title: | The antitumor activity of a lead thioxanthone is associated with alterations in cholesterol localization |
Publisher: | MDPI |
Issue Date: | 2018 |
Abstract: | The search for novel anticancer small molecules and strategies remains a challenge. Our previous studies have identified TXA1 (1-{[2-(diethylamino)ethyl]amino}-4-propoxy-9H-thioxanthen-9-one) as a hit compound, with in vitro antitumor potential by modulating autophagy and apoptosis in human tumor cell lines. In the present study, the mechanism of action and antitumor potential of the soluble salt of this molecule (TXA1.HCl) was further investigated using in vitro and mouse xenograft tumor models of NSCLC. Our results showed that TXA1.HCl affected steroid biosynthesis, increased RagD expression, and caused abnormal cellular cholesterol localization. In addition, TXA1.HCl treatment presented no toxicity to nude mice and significantly reduced the growth of human NSCLC cells xenografts in mice. Overall, this work provides new insights into the mechanism of action of TXA1, which may be relevant for the development of anticancer therapeutic strategies, which target cholesterol transport. © 2018 by the authors. |
URI: | https://hdl.handle.net/10216/120481 |
Source: | Molecules, vol. 23(12):3301 |
Related Information: | info:eu-repo/grantAgreement/FCT/5876/147268/PT |
Document Type: | Artigo em Revista Científica Internacional |
Rights: | openAccess |
Appears in Collections: | CIIMAR - Artigo em Revista Científica Internacional I3S - Artigo em Revista Científica Internacional |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
Lima RT_2018.pdf | 4.05 MB | Adobe PDF | View/Open |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.