Musa Arafa, Shady Nourhan Hisham, Ahmed Shaimaa R, Alnusaire Taghreed S, Sayed Ahmed M, Alowaiesh Bassam F, Sabouni Ibrahim, Al-Sanea Mohammad M, Mostafa Ehab M, Youssif Khayrya A, Abu-Baih Dalia H, Elrehany Mahmoud A, Abdelmohsen Usama Ramadan
Pharmacognosy Department, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, Saudi Arabia.
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo 11371, Egypt.
Antioxidants (Basel). 2021 Apr 22;10(5):644. doi: 10.3390/antiox10050644.
Gastric ulceration is among the most serious humanpublic health problems. 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 L. cv. Arbequina leaf extract. LC-HRMS-based metabolic profiling of the alcoholic extract of L. cv. Arbequina led to the dereplication of 18 putative compounds (-). In vivo indomethacin-induced gastric ulcer in a rat model was established and the extract was tested at a dose of 300 mg kg compared to cimetidine (100 mg kg). The assessment of gastric mucosal lesions and histopathology of gastric tissue was done. It has been proved that significantly decreased the ulcer index and protected the mucosa from lesions. The antioxidant potential of the extract was evaluated using three in vitro assays, HO 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 () and oleacein () 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) ( and , respectively) exhibited a significant in vitro 5-LOX inhibitory activity with IC values of 8.6 and 5.8 µg/mL, respectively. The present study suggested a possible implication of leaves as a potential candidate having gastroprotective, antioxidant, and 5-LOX inhibitory activity for the management of gastric ulcers.
胃溃疡是最严重的人类公共卫生问题之一。阿贝基纳油橄榄（L. cv. Arbequina）是众多几乎未被研究的油橄榄品种之一。油橄榄植物所报道的抗氧化和抗炎潜力使其成为预防胃溃疡的潜在天然产物。因此，本研究的主要目的是探究阿贝基纳油橄榄叶提取物的胃保护作用。基于液相色谱 - 高分辨质谱的阿贝基纳油橄榄酒精提取物代谢谱分析鉴定出18种假定化合物（-）。建立了大鼠吲哚美辛诱导的胃溃疡体内模型，并将提取物以300 mg/kg的剂量与西咪替丁（100 mg/kg）进行比较测试。对胃黏膜损伤和胃组织病理学进行了评估。结果证明该提取物显著降低了溃疡指数并保护黏膜免受损伤。使用三种体外试验评估了提取物的抗氧化潜力，即羟基自由基清除、黄嘌呤氧化酶抑制和超氧阴离子自由基清除活性，结果显示出良好的活性。此外，对假定鉴定出的化合物进行了基于计算机模拟的研究，结果突出表明3 - 羟基酪醇（）和橄榄苦苷（）可以靶向5 - 脂氧合酶（5 - LOX）作为预防溃疡发病机制的保护机制。经实验验证，两种化合物3 - 羟基酪醇（HT）和橄榄苦苷（OC）（分别为和）均表现出显著的体外5 - LOX抑制活性，IC值分别为8.6和5.8 μg/mL。本研究表明阿贝基纳油橄榄叶作为具有胃保护、抗氧化和5 - LOX抑制活性的潜在候选物，可能对胃溃疡的治疗有作用。
