Searching for Molecules against Cancer in the Azores: Plants, Macroalgae, and Synthetic Compounds †
by
, and
Maria do Carmo Barreto
1,*
,
Vera Lúcia Gouveia
2,
Gonçalo Pereira Rosa
1 and
Ana Maria Loureiro Seca
1,3 1
cE3C-ABG/Faculty of Sciences and Technology-Azores University, 9501-801 Ponta Delgada, Portugal
2
Faculty of Sciences and Technology-Azores University, 9501-801 Ponta Delgada, Portugal
3
QOPNA & LAQV-REQUIMTE, University of Aveiro, 3810-193 Aveiro, Portugal
*
Author to whom correspondence should be addressed.
†
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 61; https://doi.org/10.3390/proceedings2019022061
Published: 12 August 2019
(This article belongs to the Proceedings of The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery)
Pursuing the goal of finding active molecules against cancer using various approaches, we focused on natural-based scaffolds in terrestrial plants and in marine macroalgae, taking advantage of the rich biodiversity of the Azores islands. We also focused on molecules obtained by synthesis. In the present work, we report examples of molecules which illustrate these investigations.
Concerning plants such as Juniperus brevifolia, an Azorean endemic conifer, we isolated dehydroabietinol, which was active against human tumor cell lines MCF7, A549 and especially against HeLa (IC50 = 15.7 μM, with a selectivity index SI = IC50Vero/IC50HeLa of 1.78) [1].
From seaweed Cystoseira abies-marina, two new meroditerpenes, cystoazorols A and B, were isolated. Cystoazorol A exhibited the highest growth inhibition against HeLa cells (21.6 and 5.9 μM in lag and log growth phases, respectively), with an SI higher than taxol, the positive control [2].
Finally, we report the antitumor activity of chalcones obtained by chemical synthesis. Among the different compounds synthesized, the best results against A549 cell line were IC50 values of 367.4 and 311.4 μM for a chalcone and a flavanone, respectively. Although the activity of these molecules is lower than that of the natural compounds referred above, it should be noted that this activity may be modulated by variating substituent groups.
Acknowledgments
Thanks are due to the University of Aveiro and FCT/MCT for financial support for QOPNA research Unit (FCT UID/QUI/00062/2019) through national funds and, where applicable, co-financed by FEDER, within the PT2020 Partnership Agreement, and to the Portuguese NMR Network and the cE3c centre (UID/BIA/00329/2013; UID/BIA/00329/2019) and to DRCT for funding Azorean Biodiversity Group).
References
- Moujir, L.M.; Seca, A.M.L.; Araujo, L.; Silva, A.M.S.; Barreto, M.C. A new natural spiro heterocyclic compound and the cytotoxic activity of the secondary metabolites from Juniperus brevifolia leaves. Fitoterapia 2011, 82, 225–229. [Google Scholar] [CrossRef] [PubMed]
- Gouveia, V.; Seca, A.M.L.; Barreto, M.C.; Neto, A.; Kijjoa, S.; Silva, A.M.S. Cytotoxic meroterpenoids from the macroalga Cystoseira abies-marina. Phytochem. Lett. 2013, 6, 593–597. [Google Scholar] [CrossRef]
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MDPI and ACS Style
Barreto, M.d.C.; Gouveia, V.L.; Rosa, G.P.; Seca, A.M.L. Searching for Molecules against Cancer in the Azores: Plants, Macroalgae, and Synthetic Compounds. Proceedings 2019, 22, 61. https://doi.org/10.3390/proceedings2019022061
AMA Style
Barreto MdC, Gouveia VL, Rosa GP, Seca AML. Searching for Molecules against Cancer in the Azores: Plants, Macroalgae, and Synthetic Compounds. Proceedings. 2019; 22(1):61. https://doi.org/10.3390/proceedings2019022061
Chicago/Turabian StyleBarreto, Maria do Carmo, Vera Lúcia Gouveia, Gonçalo Pereira Rosa, and Ana Maria Loureiro Seca. 2019. "Searching for Molecules against Cancer in the Azores: Plants, Macroalgae, and Synthetic Compounds" Proceedings 22, no. 1: 61. https://doi.org/10.3390/proceedings2019022061
