الملخص الإنجليزي
Plants of the genus Echinop (Asteraceae) are traditional medicinal plants used to treat several
GIT ailments, owing to their diverse bioactive secondary metabolites, including sesquiterpenoids,
triterpenoids, phytosterols, phenolics, flavonoids, alkaloids, and essential oils. Echinops erinaceus
Kit Tan is a wild perennial herb of the genus Echinops which is endemic to Oman, Saudi Arabia,
and Yemen. Currently, there are no previous reports exploring its anti-ulcer and anti-inflammatory
effects. Additionally, few reports have described the chemical profile of E. erinaceus Kit Tan. In the
current study, the CHCl3
fraction of the aerial parts of the plant was subjected to chromatographic
isolation and spectroscopic identification via 1D and 2D NMR, and MS. The plant afforded two
new compounds, designated erinaceolic acid (E3) and erinaceoside (E5), in addition to five known
compounds, namely taraxasterol acetate (E1), taraxasterol (E2), apigenin (E4), stigmasterol-3-O-β D-glucoside (E6), and speranskoside (E7). The evaluation of the gastric ulcer protective activity
of the total extract and successive fractions of E. erinaceus, using the in vivo ethanol-induced ulcer
in rats model, revealed the significant effect of the tested extracts and fractions on the percentage
of gastric ulcer protection and ulcer index (500 mg/kg) compared to antodine (20 mg/kg). The
tested extracts and fractions also reduced the stomach contents of TNF-α and reduced IL-6 as
compared to the untreated group. Histopathological examination of the gastric mucosal tissues of
rats supportedprevious results. In addition, the main subfractions and their isolates were assessed for
their in vitro anti-inflammatory activity against COX-2 and 15-LOX enzymes. The new compounds
erinaceolic acid (E3) and speranskoside (E7) exhibited strong inhibition against COX-2 (3.41 and
2.62 µg/mL) and 15-LOX (10.05 and 5.51 µg/mL), respectively. A molecular docking study was
performed to reveal the binding interaction modes of the most active compounds against the binding
sites of COX-2 (PDB ID 3LN1) and 15-LOX (PDB ID 1LOX) proteins. Speranskoside (E7) showed a
dual binding affinity better than that of the cocrystallized references, celecoxib and (2E)-3-(2-oct-1-yn 1-ylphenyl)acrylic acid (RS7) against both enzymes. This study shed a light on the potential use of
E. erinaceus in the protection and treatment of gastric ulcers.
