Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds

Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds

Author Vizetto-Duarte, Catarina Google Scholar
Custodio, Luisa Google Scholar
Acosta, Gerardo Google Scholar
Autor UNIFESP Google Scholar
Morais, Thiago R. Autor UNIFESP Google Scholar
de Sousa, Carolina Bruno Google Scholar
Gangadhar, Katkam N. Google Scholar
Rodrigues, Maria Joao Google Scholar
Pereira, Hugo Google Scholar
Lima, Raquel T. Google Scholar
Helena Vasconcelos, M. Google Scholar
Barreiro, Luisa Google Scholar
Rauter, Amelia P. Google Scholar
Albericioi, Fernando Google Scholar
Varela, Joao Google Scholar
Abstract Marine organisms are a prolific source of drug leads in a variety of therapeutic areas. In the last few years, biomedical, pharmaceutical and nutraceutical industries have shown growing interest in novel compounds from marine organisms, including macroalgae. Cystoseira is a genus of Phaeophyceae (Fucales) macroalgae known to contain bioactive compounds. Organic extracts (hexane, diethyl ether, ethyl acetate and methanol extracts) from three Cystoseira species (C. humilis, C. tamariscifolia and C. usneoides) were evaluated for their total phenolic content, radical scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals, and antiproliferative activity against a human hepatocarcinoma cell line (HepG2 cells). C. tamariscifolia had the highest TPC and RSA. The hexane extract of C. tamariscifolia (CTH) had the highest cytotoxic activity (IC50 = 2.31 mu g/mL), and was further tested in four human tumor (cervical adenocarcinoma HeLa; gastric adenocarcinoma AGS; colorectal adenocarcinoma HCT-15; neuroblastoma SH-SY5Y), and two non-tumor (murine bone marrow stroma S17 and human umbilical vein endothelial HUVEC) cell lines in order to determine its selectivity. CTH strongly reduced viability of all tumor cell lines, especially of HepG2 cells. Cytotoxicity was particularly selective for the latter cells with a selectivity index = 12.6 as compared to non-tumor cells. Incubation with CTH led to a 2-fold decrease of HepG2 cell proliferation as shown by the bromodeoxyuridine (BrdU) incorporation assay. CTH-treated HepG2 cells presented also pro-apoptotic features, such as increased Annexin Wpropidium iodide (PI) binding and dose-dependent morphological alterations in DAPI-stained cells. Moreover, it had a noticeable disaggregating effect on 3D multicellular tumor spheroids. Deme boxy cystoketal chromane, a derivative of the meroditerpenoid cystoketal, was identified as the active compound in CTH and was shown to display selective in vitro cYtotoxicitY towards HepG2 cells.
Keywords Marine natural products
Brown algae
xmlui.dri2xhtml.METS-1.0.item-coverage London
Language English
Foundation for Science and Technology (FCT)
Portuguese National Budget
Grant number SEABIOMED: PTDC/MAR/103957/2008
XtremeBio: PTDC/MAR-EST/4346/2012
FCT: CCMAR/Multi/04326/2013
FCT :IF/00049/2012
Date 2016
Published in Peerj. London, v. 4, p. -, 2016.
ISSN 2167-8359 (Sherpa/Romeo, impact factor)
Publisher Peerj Inc
Extent -
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000370949200004

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