Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds
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 (Fu...
| Main Authors: | , , , , , , , , , , , , , , |
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| Format: | Article |
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PeerJ Inc.
2016-02-01
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| Online Access: | https://peerj.com/articles/1704.pdf |
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| author | Catarina Vizetto-Duarte Luísa Custódio Gerardo Acosta João H.G. Lago Thiago R. Morais Carolina Bruno de Sousa Katkam N. Gangadhar Maria João Rodrigues Hugo Pereira Raquel T. Lima M. Helena Vasconcelos Luísa Barreira Amélia P. Rauter Fernando Albericio João Varela |
| author_facet | Catarina Vizetto-Duarte Luísa Custódio Gerardo Acosta João H.G. Lago Thiago R. Morais Carolina Bruno de Sousa Katkam N. Gangadhar Maria João Rodrigues Hugo Pereira Raquel T. Lima M. Helena Vasconcelos Luísa Barreira Amélia P. Rauter Fernando Albericio João Varela |
| author_sort | Catarina Vizetto-Duarte |
| collection | DOAJ |
| description | 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 µg/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 V/propidium iodide (PI) binding and dose-dependent morphological alterations in DAPI-stained cells. Moreover, it had a noticeable disaggregating effect on 3D multicellular tumor spheroids. Demethoxy 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. |
| first_indexed | 2024-03-09T06:36:44Z |
| format | Article |
| id | doaj.art-ed9a1175cfcd41ca966e3144c018afff |
| institution | Directory Open Access Journal |
| issn | 2167-8359 |
| language | English |
| last_indexed | 2024-03-09T06:36:44Z |
| publishDate | 2016-02-01 |
| publisher | PeerJ Inc. |
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| spelling | doaj.art-ed9a1175cfcd41ca966e3144c018afff2023-12-03T10:57:58ZengPeerJ Inc.PeerJ2167-83592016-02-014e170410.7717/peerj.1704Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compoundsCatarina Vizetto-Duarte0Luísa Custódio1Gerardo Acosta2João H.G. Lago3Thiago R. Morais4Carolina Bruno de Sousa5Katkam N. Gangadhar6Maria João Rodrigues7Hugo Pereira8Raquel T. Lima9M. Helena Vasconcelos10Luísa Barreira11Amélia P. Rauter12Fernando Albericio13João Varela14Centre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalInstitute for Research in Biomedicine of Barcelona, Chemistry and Molecular Pharmacology, Barcelona Science Park, Baldiri Reixac, Barcelona, SpainInstitute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of Sao Paulo, São Paulo, BrazilInstitute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of Sao Paulo, São Paulo, BrazilCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, Portugali3S—Instituto de Investigação e Inovação em Saúde da Universidade do Porto, Rua Alfredo Allen, Porto, Portugali3S—Instituto de Investigação e Inovação em Saúde da Universidade do Porto, Rua Alfredo Allen, Porto, PortugalCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalCenter of Chemistry and Biochemistry, Department of Chemistry and Biochemistry, Faculty of Sciences, University of Lisbon, Lisbon, PortugalInstitute for Research in Biomedicine of Barcelona, Chemistry and Molecular Pharmacology, Barcelona Science Park, Baldiri Reixac, Barcelona, SpainCentre of Marine Sciences, Faculty of Sciences and Technology, Campus of Gambelas, University of Algarve, Faro, PortugalMarine 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 µg/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 V/propidium iodide (PI) binding and dose-dependent morphological alterations in DAPI-stained cells. Moreover, it had a noticeable disaggregating effect on 3D multicellular tumor spheroids. Demethoxy 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.https://peerj.com/articles/1704.pdfMarine natural productsBrown algaeAntioxidantAnti-hepatocarcinomaCystoseira |
| spellingShingle | Catarina Vizetto-Duarte Luísa Custódio Gerardo Acosta João H.G. Lago Thiago R. Morais Carolina Bruno de Sousa Katkam N. Gangadhar Maria João Rodrigues Hugo Pereira Raquel T. Lima M. Helena Vasconcelos Luísa Barreira Amélia P. Rauter Fernando Albericio João Varela Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds PeerJ Marine natural products Brown algae Antioxidant Anti-hepatocarcinoma Cystoseira |
| title | Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds |
| title_full | Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds |
| title_fullStr | Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds |
| title_full_unstemmed | Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds |
| title_short | Can macroalgae provide promising anti-tumoral compounds? A closer look at Cystoseira tamariscifolia as a source for antioxidant and anti-hepatocarcinoma compounds |
| title_sort | can macroalgae provide promising anti tumoral compounds a closer look at cystoseira tamariscifolia as a source for antioxidant and anti hepatocarcinoma compounds |
| topic | Marine natural products Brown algae Antioxidant Anti-hepatocarcinoma Cystoseira |
| url | https://peerj.com/articles/1704.pdf |
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