Antiulcer Potential of Olea europea L. cv. Arbequina Leaf Extract Supported by Metabolic Profiling and Molecular Docking

Abstract

Gastric ulceration is among the most serious humanpublic health problems. Olea europea L. cv. Arbequina is one of the numerous olive varieties which have scarcely been studied. The reported antioxidant and anti-inflammatory potential of the olive plant make it a potential prophylactic natural product against gastric ulcers. Consequently, the main goal of this study is to investigate the gastroprotective effect of Olea europea L. cv. Arbequina leaf extract. LC-HRMS-based metabolic profiling of the alcoholic extract of Olea europea L. cv. Arbequina led to the dereplication of 18 putative compounds (1–18). In vivo indomethacin-induced gastric ulcer in a rat model was established and the Olea europea extract was tested at a dose of 300 mg kg−1 compared to cimetidine (100 mg kg−1). The assessment of gastric mucosal lesions and histopathology of gastric tissue was done. It has been proved that Olea europea significantly decreased the ulcer index and protected the mucosa from lesions. The antioxidant potential of the extract was evaluated using three in vitro assays, H2O2 scavenging, xanthine oxidase inhibitory, and superoxide radical scavenging activities and showed promising activities. Moreover, an in silico based study was performed on the putatively dereplicated compounds, which highlighted that 3-hydroxy tyrosol (4) and oleacein (18) can target the 5-lipoxygenase enzyme (5-LOX) as a protective mechanism against the pathogenesis of ulceration. Upon experimental validation, both compounds 3-hydroxy tyrosol (HT) and oleacein (OC) (4 and 18, respectively) exhibited a significant in vitro 5-LOX inhibitory activity with IC50 values of 8.6 and 5.8 µg/mL, respectively. The present study suggested a possible implication of O. europea leaves as a potential candidate having gastroprotective, antioxidant, and 5-LOX inhibitory activity for the management of gastric ulcers.

The Chemical Profiling, Docking Study, and Antimicrobial and Antibiofilm Activities of the Endophytic fungi Aspergillus sp. AP5

“…AP5-derived extract to the neural networking and pharmacophore-based prediction software PASS. This platform has proven successful in its predictions, particularly for those with a probability higher than Pa = 0.5 [ 26 , 48 , 49 , 50 , 51 , 52 , 53 ].…”

Anti-Cancer and Anti-Inflammatory Potential of the Green Synthesized Silver Nanoparticles of the Red Sea Sponge Phyllospongia lamellosa Supported by Metabolomics Analysis and Docking Study

“…Accordingly, we subjected the metabolites (1-25) identified in the P. lamellosa-derived extracts (i.e., CE and EE) to the neural networking-based prediction software PASS. This software has shown very good success rate in its predictions, particularly for predictions higher than Pa = 0.5 [27][28][29][30][31][32][33].…”

“…Moreover, they showed a number of hydrophobic interactions with LEU-5, MET-21, HIS-46, TYR-50, and LYS-6 (Figure 6). sPLA2 has been reported to have a crucial role in the growth and development of different types of human cancers (e.g., breast, prostate, liver, and skin), and identified to be a promising target to control these types of tumors [24][25][26][27][28][29][30][31][32][33][34][35].…”

“…It is worth noting that the compounds 1-15 have also shown to be COX inhibitors according to PASS prediction; however, their scoring was poor (Pa < 0.5) (Figure 7). sPLA2 has been reported to have a crucial role in the growth and development of different types of human cancers (e.g., breast, prostate, liver, and skin), and identified to be a promising target to control these types of tumors [22,[24][25][26][27][28][29][30][31][32][33][34].…”

Antioxidant Capacity of Free Volatile Compounds from Olea europaea L. cv. Oblica Leaves Depending on the Vegetation Stage

“…It is also used in cosmetics as it protects against UVB rays, slows the aging process, and promotes wound healing and re-epithelialization [ 20 , 21 ]. Many phenolic compounds isolated from olive leaves can exert a pronounced antioxidant activity, which in turn can accelerate the healing process of ulcers [ 22 ]. Generally, the olive leaf has the highest antioxidant activity of all parts of the olive tree [ 11 , 23 ].…”