Abstract

Artemisia annua L. (AA) has shown for many centuries important therapeutic virtues associated with the presence of artemisinin (ART). The aim of this study was to identify and quantify ART and other secondary metabolites in ethanolic extracts of AA and evaluate the biological activity in the presence of an inflammatory stimulus. In this work, after the extraction of the aerial parts of AA with different concentrations of ethanol, ART was quantified by HPLC and HPLC-MS. In addition, anthocyanins, flavanols, flavanones, flavonols, lignans, low-molecular-weight phenolics, phenolic acids, stilbenes, and terpenes were identified and semi-quantitatively determined by UHPLC-QTOF-MS untargeted metabolomics. Finally, the viability of human neuroblastoma cells (SH-SY5Y) was evaluated in the presence of the different ethanolic extracts and in the presence of lipopolysaccharide (LPS). The results show that ART is more concentrated in AA samples extracted with 90% ethanol. Regarding the other metabolites, only the anthocyanins are more concentrated in the samples extracted with 90% ethanol. Finally, ART and all AA samples showed a protective action towards the pro-inflammatory stimulus of LPS. In particular, the anti-inflammatory effect of the leaf extract of AA with 90% ethanol was also confirmed at the molecular level since a reduction in TNF-α mRNA gene expression was observed in SH-SY5Y treated with LPS.

Highlights

  • Introduction published maps and institutional affilArtemisia annua L. (AA) (Figure 1) is an annual plant native to Asia, with a herbaceous habit, belonging to the Asteraceae [1,2]

  • Aerial parts of Artemisia annua L. (AA) were collected from ten plants growing in the greenhouses of “AMBROGIO Italia” located in Leno (45◦ 210 52.300 N 10◦ 110 53.900 E), a province of Brescia, Italy

  • The initial objective of this work was to produce a set of extracts from the aerial parts of AA having different phytochemical profiles and differing in ART content

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Summary

Introduction

Introduction published maps and institutional affilArtemisia annua L. (AA) (Figure 1) is an annual plant native to Asia, with a herbaceous habit, belonging to the Asteraceae [1,2]. (AA) (Figure 1) is an annual plant native to Asia, with a herbaceous habit, belonging to the Asteraceae [1,2]. From an organographic point of view, AA shows a single stem, which can reach 2 m in height, and has leaves that can vary from 1.5 to 6.5 cm in length [1]. Glandular trichomes can be found both in leaves and the stem of AA and be rich in biologically active secondary metabolites. More than 600 secondary metabolites have been identified in AA, including sesquiterpenes, monoterpenes, and phenolic compounds, such as coumarins and flavonoids [3]. More than thirty sesquiterpenes have been identified in AA, which are mainly located in the aerial part [3,4]

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