Abstract
The olive tree is a venerable Mediterranean plant and often used in traditional medicine. The main aim of the present study was to evaluate the effect of Olea europaea L. cv. Arbosana leaf extract (OLE) and its encapsulation within a spanlastic dosage form on the improvement of its pro-oxidant and antiproliferative activity against HepG-2, MCF-7, and Caco-2 human cancer cell lines. The LC-HRESIMS-assisted metabolomic profile of OLE putatively annotated 20 major metabolites and showed considerable in vitro antiproliferative activity against HepG-2, MCF-7, and Caco-2 cell lines with IC50 values of 9.2 ± 0.8, 7.1 ± 0.9, and 6.5 ± 0.7 µg/mL, respectively. The encapsulation of OLE within a (spanlastic) nanocarrier system, using a spraying method and Span 40 and Tween 80 (4:1 molar ratio), was successfully carried out (size 41 ± 2.4 nm, zeta potential 13.6 ± 2.5, and EE 61.43 ± 2.03%). OLE showed enhanced thermal stability, and an improved in vitro antiproliferative effect against HepG-2, MCF-7, and Caco-2 (IC50 3.6 ± 0.2, 2.3 ± 0.1, and 1.8 ± 0.1 µg/mL, respectively) in comparison to the unprocessed extract. Both preparations were found to exhibit pro-oxidant potential inside the cancer cells, through the potential inhibitory activity of OLE against glutathione reductase and superoxide dismutase (IC50 1.18 ± 0.12 and 2.33 ± 0.19 µg/mL, respectively). These inhibitory activities were proposed via a comprehensive in silico study to be linked to the presence of certain compounds in OLE. Consequently, we assume that formulating such a herbal extract within a suitable nanocarrier would be a promising improvement of its therapeutic potential.
Highlights
Olea europaea is a venerable cultural plant habitat in the Mediterranean [1]
The results showed that OLE and its derived spanlastics were able to inhibit the activity of the Glutathione reductase (GR) enzyme significantly with IC50 values of
The results showed that OLE and its derived spanlastics were able to inhibit the activity of the superoxide dismutase (SOD)
Summary
Olea europaea is a venerable cultural plant habitat in the Mediterranean [1]. The cultivation of this tree extends back many thousands of years and perhaps took place in the Eastern Mediterranean [1]. More than 300 original olive varieties have been developed worldwide to produce olive products [1] These outputs represent a significant branch of industry in the Mediterranean regions, especially Spain, Italy, and Greece [1]. Olive fruits and leaves are well-known for their therapeutic potential in many diseases [2]. Volatile compounds from O. europaea fruits and leaves and their functions in aroma improvement have been an intense field of modern research [9]
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