GC-MS Analysis, Bioactivity-based Molecular Networking and Antiparasitic Potential of the Antarctic Alga Desmarestia antarctica

Author:

Colepicolo-Neto Pio1,Debonsi Hosana Maria2,dos Santos Gustavo Souza2ORCID,Rangel Karen Cristina3,Teixeira Thaiz Rodrigues2ORCID,Gaspar Lorena Rigo3,Abreu-Filho Péricles Gama4,Pereira Luíz Miguel4,Yatsuda Ana Patrícia4,Gallon Marília Elias2,Gobbo-Neto Leonardo2,da Costa Clementino Leandro5,Graminha Márcia Aparecida Silva6,Jordão Laís Garcia7,Pohlit Adrian Martin7

Affiliation:

1. Chemistry Institute, University of São Paulo, São Paulo, SP, Brazil

2. Department of Biomolecular Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil

3. Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil

4. Department of Clinical Analysis, Toxicology and Food Science, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil

5. Institute of Chemistry, State University Júlio de Mesquita Filho, Araraquara, SP, Brazil

6. Department of Clinical Analysis, School of Pharmaceutical Sciences of São Paulo State University Júlio de Mesquita Filho, Araraquara, SP, Brazil

7. Technology and Innovation Department, National Institute of Amazon Research, Manaus, AM, Brazil

Abstract

AbstractLeishmaniasis, 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.

Funder

Brazilian Antarctic Program

Brazilian Marine Force, National Institute of Science and Technology

São Paulo Research Foundation

Brazilian research funding agencies Coordination of Improvement of Higher-Level Personnel

National Council for Scientific and Technological Development

Biomolecular Sciences and the Núcleo de Pesquisas em Produtos Naturais e Sintéticos – NPPNS

Publisher

Georg Thieme Verlag KG

Subject

General Medicine

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