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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.
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

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