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Molecules 2016, 21(1), 81; doi:10.3390/molecules21010081

Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis

1
CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, IUCS—Instituto Universitário de Ciências da Saúde, Rua Central de Gandra 1317, Gandra 4585-116, Portugal
2
i3S—Instituto de Investigação e Inovação em Saúde da Universidade do Porto, Rua Alfredo Allen 208, Porto 4200-135, Portugal
3
Cancer Drug Resistance Group, IPATIMUP—Institute of Molecular Pathology and Immunology of the University of Porto, Porto 4200-135, Portugal
4
Department of Pathology and Oncology, FMUP—Faculty of Medicine of the University of Porto, Alameda Prof. Hernâni Monteiro, Porto 4200-319, Portugal
5
Laboratory of Microbiology, Department of Biological Sciences, FFUP—Faculty of Pharmacy of the University of Porto, Rua de Jorge Viterbo Ferreira 228, Porto 4050-313, Portugal
6
Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, FFUP—Faculty of Pharmacy of the University of Porto, Rua de Jorge Viterbo Ferreira 228, Porto 4050-313, Portugal
7
UCIBIO/REQUIMTE, Laboratório de Microbiologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, Porto 4050-313, Portugal
8
Faculty of Medicinal Technology, Rangsit University, 52/347 Muang Ake, Phaholyothin Road, Lakhok, Pathumthani 10210, Thailand
9
Applied Radiation and Isotopes Department, Faculty of Science, Kasetsart University, Jatujak, Bangkok 10930, Thailand
10
CIIMAR/CIMAR—Centro Interdisciplinar de Investigação Marinha e Ambiental, Universidade do Porto, Rua dos Bragas 289, Porto 4050-123, Portugal
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 23 November 2015 / Revised: 27 December 2015 / Accepted: 7 January 2016 / Published: 13 January 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [8700 KB, uploaded 13 January 2016]   |  

Abstract

Our previous work has described a library of thioxanthones designed to have dual activity as P-glycoprotein modulators and antitumor agents. Some of these compounds had shown a significant cell growth inhibitory activity towards leukemia cell lines, without affecting the growth of non-tumor human fibroblasts. However, their effect in cell lines derived from solid tumors has not been previously studied. The present work aimed at: (i) screening this small series of compounds from an in-house library, for their in vitro cell growth inhibitory activity in human tumor cell lines derived from solid tumors; and (ii) initiate a study of the effect of the most potent compound on apoptosis. The tumor cell growth inhibitory effect of 27 compounds was first analysed in different human tumor cell lines, allowing the identification of a hit compound, TXA1. Its hydrochloride salt TXA1·HCl was then synthesized, to improve solubility and bioavailability. Both TXA1 and TXA1·HCl inhibited the growth of MCF-7, NCI-H460, A375-C5, HeLa, 786-O, Caki-2 and AGS cell lines. The effect of TXA1·HCl in MCF-7 cells was found to be irreversible and was associated, at least in part, with an increase in cellular apoptosis. View Full-Text
Keywords: antitumor activity screening; thioxanthones; in vitro cell growth assays; apoptosis antitumor activity screening; thioxanthones; in vitro cell growth assays; apoptosis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Barbosa, J.; Lima, R.T.; Sousa, D.; Gomes, A.S.; Palmeira, A.; Seca, H.; Choosang, K.; Pakkong, P.; Bousbaa, H.; Pinto, M.M.; Sousa, E.; Vasconcelos, M.H.; Pedro, M. Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis. Molecules 2016, 21, 81.

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