Abstract

Extracts of five halophytes from southern Portugal (Arthrocnemum macrostachyum, Mesembryanthemum edule, Juncus acutus, Plantago coronopus and Halimione portulacoides), were studied for antioxidant, anti-inflammatory and in vitro antitumor properties. The most active extracts towards the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical were the methanol extracts of M. edule (IC50 = 0.1 mg/mL) and J. acutus (IC50 = 0.4 mg/mL), and the ether extracts of J. acutus (IC50 = 0.2 mg/mL) and A. macrostachyum (IC50 = 0.3 mg/mL). The highest radical scavenging activity (RSA) against the 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical was obtained in the ether extract of J. acutus (IC50 = 0.4 mg/mL) and H. portulacoides (IC50 = 0.9 mg/mL). The maximum total phenolic content (TPC) was found in the methanol extract of M. edule (147 mg gallic acid equivalents (GAE)/g) and in the ether extract of J. acutus (94 mg GAE/g). Significant decreases in nitric oxide (NO) production were observed after incubation of macrophages with lipopolysaccharide (LPS) and the chloroform extract of H. portulacoides (IC50 = 109 µg/mL) and the hexane extract of P. coronopus (IC50 = 98.0 µg/mL). High in vitro cytotoxic activity and selectivity was obtained with the ether extract of J. acutus. Juncunol was identified as the active compound and for the first time was shown to display selective in vitro cytotoxicity towards various human cancer cells.

Highlights

  • Halophytes are highly salt tolerant plants that can be found in sand dunes or rocky coasts, saline depressions or inland deserts, and in marine environments such as coastal salt marshes [1,2]

  • The results obtained in this work are in accordance with previous in vitro studies showing that M. edule is endowed with strong antioxidant compounds, possibly of a polyphenolic nature [9,10,11,12]

  • Our results indicate that juncunol is a good candidate for further studies on its potential use as an anticancer drug or as a valuable lead compound for the semi-synthesis or total synthesis of effective novel drugs

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Summary

Introduction

Halophytes are highly salt tolerant plants that can be found in sand dunes or rocky coasts, saline depressions or inland deserts, and in marine environments such as coastal salt marshes [1,2]. Having in mind the high diversity of halophytes (i.e., more than 2500 species have been identified so far), and the relatively small number of bioactive compounds identified, it is easy to understand why halophytes are considered to be an almost unexploited reservoir of novel bioactive molecules, or as novel sources for known compounds In this context, and following our interest in bioactive compounds present in marine organisms and in plants living in habitats with a strong marine influence, the in vitro antioxidant, anti-inflammatory and antitumoral activities of five maritime halophyte species common in the southern parts of Portugal—A. macrostachyum, M. edule, J. acutus, P. coronopus and H. portulacoides—were evaluated. The bioactive compound present in the most active species (J. acutus) was isolated and identified and its cytotoxicity and selectivity is reported here for the first time

Results and Discussion
Anti-Inflammatory Activity
Cytotoxic Activity
Reagents
Plant Material and Preparation of the Extracts
Cell Culture
Quantification of NO
Cell Viability Assay
Bioguided Fractionation and Isolation of the Bioactive Compound
3.10. Spectral and Chromatographic Analysis
3.11. Statistical Analysis
Conclusions

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