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DOI: 10.1055/a-1219-2207
GC-MS Analysis, Bioactivity-based Molecular Networking and Antiparasitic Potential of the Antarctic Alga Desmarestia antarctica
Funding: This study had financial and logistic support from the Brazilian Antarctic Program (PROANTAR/MCT/CNPq N°64/2013), Brazilian Marine Force, National Institute of Science and Technology (INCT: BioNat), Grant # 465637/2014–0, and the State of São Paulo Research Foundation (FAPESP), Grant # 2014/50926–0 and Grant # 2017/03552–5. The authors are thankful to the University of São Paulo for providing access to necessary resources, the financial and fellowship support from the Brazilian research funding agencies Coordination of Improvement of Higher-Level Personnel (CAPES), and the National Council for Scientific and Technological Development (CNPq) for the scholarship provided, Grant #1408011/2018–4. The department of Biomolecular Sciences and the Núcleo de Pesquisas em Produtos Naturais e Sintéticos – NPPNS are acknowledged.![](https://www.thieme-connect.de/media/10.1055-s-00032099/202003/lookinside/thumbnails/2020-05-0032_10-1055-a-1219-2207-1.jpg)
Abstract
Leishmaniasis, malaria, and neosporosis are parasitic diseases that affect humans and animals, causing public health problems and billions in economic losses. Despite the advances in the development of new drugs, the severe side effects of available leishmaniasis treatments, the Plasmodium spp. resistance to antimalarial drugs, and the lack of a specific treatment against neosporosis lead us to the search for new anti-protozoan molecules from underexplored sources such as the Antarctic marine environment. Herein, we describe for the first time the chemical profile of Desmarestia antarctica crude extract and fractions using GC-MS and LC-MS/MS (molecular networking) approaches, and evaluate their antiparasitic activity against Leishmania amazonensis, Neospora caninum, and multi-drug-resistant Plasmodium falciparum. Furthermore, the cytotoxicity in 3T3 BALB/c fibroblasts and Vero cells was evaluated. D. antarctica fraction E ( IC50 of 53.8±4.4 μg mL− 1 and selectivity index of 3.3) exhibited anti-promastigote activity and was fourfold more selective to L. amazonensis rather than to the host cells. D. antarctica fraction D (IC50 of 1.6±1.3 μg mL− 1 and selectivity index of 27.8), D. antarctica fraction F (IC50 of 3.1±2.1 μg mL− 1 and selectivity index of 23.1), and D. antarctica fraction H (IC50 of 3.1±2.0 μg mL− 1 and selectivity index of 12.9) presented the highest antiparasitic effects against N. caninum with no cytotoxic effects. Also, D. antarctica fraction D presented a significant antiplasmodial inhibitory effect (IC50 of 19.1±3.9 μg mL− 1 and selectivity index of 6.0). GC-MS analysis indicated palmitic acid, myristic acid, fucosterol, phthalic acid, di(2-methylbutyl) ester, loliolide, and neophytadiene as the main components in the active fractions. In addition, this is the first report of a biological screening of macroalgae secondary metabolites against N. caninum parasites.
Key words
desmarestiaceae - desmarestia antarctica - leishmania amazonensis - neospora caninum - plasmodium falciparum - antiparasitic - molecular targets and activities - marine macroalgaePublikationsverlauf
Eingereicht: 06. Mai 2020
Eingereicht: 20. Juni 2020
Angenommen: 13. Juli 2020
Artikel online veröffentlicht:
21. August 2020
© 2020. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution-NonDerivative-NonCommercial-License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes, or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by-nc-nd/4.0/).
© Georg Thieme Verlag KG
Stuttgart · New York
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