Gastroprotective effects of ursolic acid isolated from Ochrosia elliptica on ethanol-induced gastric ulcer in rats

Elshamy, Abdelsamed I.; Farrag, Ashraf; Mohamed, S.A.; Ali, Naglaa A.; Mohamed, Tarik A.; Menshawy, Medhat M.; Zaglool, Asmaa W.; Efferth, Thomas

doi:10.1007/s00044-019-02465-8

Cited by 14 publications

(20 citation statements)

References 41 publications

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“…Crystal structures of H+/K+ ATPase α (gastric proton pumps) downloaded from Swiss-Prot Database ( https://swissmodel.expasy.org ) (ID: P20648) ( Elshamy et al., 2020 ) ( Yan et al., 2004 ). Protein structures preparation for molecular docking accomplished by Discovery Studio 4.1 ( http://accerys.com ) ( Biovia, 2017 ), and Molecular Graphics Laboratory (MGL) Tools 1.5.6 ( http://mgltools.scripps.edu ) ( Bibi et al., 2019 ) used to add polar hydrogens and saved in (pdbqt) file format.…”

Section: Methodsmentioning

confidence: 99%

Gastroprotective activity of Hypericum perforatum extract in ethanol-induced gastric mucosal injury in Wistar rats: A possible involvement of H+/K+ ATPase α inhibition

Sofi

Nuraddin

Amin

et al. 2020

Heliyon

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Hypericum perforatum (HP) is a plant native to Asia and Europe. It has been documented to enclose medical effects against many disorders such as anxiety, depression and burns. This experiment was performed to evaluate the gastro-protective effect of Hypericum perforatum leaf extract in ethanol induced gastric ulcer in rats as compared to esomeprazole (the drug of choice for stomach ulcers). The mechanism of action was performed by Auto Dock Vina method.Ethanol ingestion up regulated the inflammatory reaction as demonstrated by rise of gastric proinflammatory TNF-α with a decline of IL-1β. On the other hand, the phytochemical screening of HP revealed the presence of alkaloids, flavonoids, tannins, phenols, steroids and saponins. The high dose of HP group shows mild injuries to the gastric mucosa which is comparable to the esomeprazole group, in contrast, severe damages are observed in the gastric mucosa of the ulcer control rats group. In silico results revealed that Amentoflavone and Quercitrin have highest affinity and very good interactions with Hþ/Kþ ATPase α active site. This study showed that HP is nearly as effective as esomeprazole to prevent ethanol induced gastric ulcer the plant extract and it has more binding affinity than esomeprazole to gastric proton pumps.

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Section: Methodsmentioning

confidence: 99%

Gastroprotective activity of Hypericum perforatum extract in ethanol-induced gastric mucosal injury in Wistar rats: A possible involvement of H+/K+ ATPase α inhibition

Sofi

Nuraddin

Amin

et al. 2020

Heliyon

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“…Rats were randomly divided into six groups of six animals per group as follows: Group I: control rats); Group II: ethanol ulcerated group according to Elshamy, et al [ 22 ]; Group III: ulcerated rats pre-treated with 30 mg/kg ranitidine as a reference drug; Group IV: ulcerated rats pre-treated with 25 mg/kg of the extract; Group V: ethanol ulcerated rats pretreated with 50 mg/kg of extract. Group VI: ulcerated rats pre-treated with 100 mg/kg of extract.…”

Section: Methodsmentioning

confidence: 99%

“…Considering the well-reported medicinal uses of Cyperus plants and continuing our search for bioactive products for the treatment of gastric disorders of natural origin [ 5 , 6 , 22 ], we described herein the first metabolites profile of C. conglomeratus alcohol extract via UPLC-qTOF-MS, and its potential gastroprotective activity as monitored using biochemical and histopathological examinations.…”

Section: Introductionmentioning

confidence: 99%

UPLC-qTOF-MS Phytochemical Profile and Antiulcer Potential of Cyperus conglomeratus Rottb. Alcoholic Extract

Elshamy¹,

Farrag

Ayoub

et al. 2020

Molecules

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Cyperus has been commonly used as a multi-use medicinal plant in folk medicine worldwide. The objectives of our study were to determine the different metabolites in the Cyperus conglomeratus Rottb. methanol extract, and to assess its in vivo gastroprotective effect in ethanol-induced gastric ulcer model in rats. Serum levels of galactin-3 and TNF-α were employed as biochemical markers. To pinpoint for active agents, comprehensive metabolites profiling of extract via UPLC-qTOF-MS/MS was employed. A total of 77 chromatographic peaks were detected, of which 70 were annotated. The detected metabolites were categorized into phenolic acids and their derivatives, flavonoids, stilbenes, aurones, quinones, terpenes, and steroids. Rats were divided into six groups; healthy control, ulcer control, standard drug group, and 25, 50, 100 mg/kg of C. conglomeratus treated rats. Pre-treatment with C. conglomeratus alcohol extract significantly reduced galactin-3, and TNF-α in ethanol-induced ulcer model at 25, 50, and 100 mg/kg. Further histopathological and histochemical studies revealed moderate erosion of superficial epithelium, few infiltrated inflammatory cells, and depletion of gastric tissue glycoprotein in the ulcer group. Treatment with the extract protected the gastric epithelial cells in a dose-dependent manner. It could be concluded that C. conglomeratus extract provides significant gastroprotective activity in ethanol-induced gastric ulcer and ought to be included in nutraceuticals in the future for ulcer treatment.

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“…This analysis was conducted by several studies [30][31][32]. For the ulceration induction, the fasted rats (n = 6) were orally administrated with 1 mL EtOH (99.9% purity) [33]. After 4 h, sacrificing of all rats occurred under anesthesia by diethyl ether.…”

Section: Experimental Animals Ethical Statement Ulcer Induction and Groupingmentioning

confidence: 99%

“…Anti-ulcer drugs have the ability to prevent gastric acidification as the main factor of ulcer formation via gastric H + /K + ATPase. Accordingly, we investigated the binding mode and affinity of ST-1 with H + /K + ATPase; ranitidine was used as a positive control [33]. ST-1 showed a higher affinity to the proton pump than ranitidine (−9.86 vs. −6.21 kcal/mol, respectively) and exhibited a higher estimated inhibition constant (pk i values 59.72 nM vs. 27.92 µM, respectively).…”

Section: In Silico Inhibitory Effect Of St-1 On H + /K + -Atpasementioning

confidence: 99%

Gastroprotection against Rat Ulcers by Nephthea Sterol Derivative

et al. 2021

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Different species belonging to the genus Nephthea (Acyonaceae) are a rich resource for bioactive secondary metabolites. The literature reveals that the gastroprotective effects of marine secondary metabolites have not been comprehensively studied in vivo. Hence, the present investigation aimed to examine and determine the anti-ulcer activity of 4α,24-dimethyl-5α-cholest-8β,18-dihydroxy,22E-en-3β-ol (ST-1) isolated from samples of a Nephthea species. This in vivo study was supported by in silico molecular docking and protein–protein interaction techniques. Oral administration of ST-1 reduced rat stomach ulcers with a concurrent increase in gastric mucosa. Molecular docking calculations against the H+/K+-ATPase transporter showed a higher binding affinity of ST-1, with a docking score value of −9.9 kcal/mol and a pKi value of 59.7 nM, compared to ranitidine (a commercial proton pump inhibitor, which gave values of −6.2 kcal/mol and 27.9 µM, respectively). The combined PEA-reactome analysis results revealed promising evidence of ST-1 potency as an anti-ulcer compound through significant modulation of the gene set controlling the PI3K signaling pathway, which subsequently plays a crucial role in signaling regarding epithelialization and tissue regeneration, tissue repairing and tissue remodeling. These results indicate a probable protective role for ST-1 against ethanol-induced gastric ulcers.

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Gastroprotective effects of ursolic acid isolated from Ochrosia elliptica on ethanol-induced gastric ulcer in rats

Cited by 14 publications

References 41 publications

Gastroprotective activity of Hypericum perforatum extract in ethanol-induced gastric mucosal injury in Wistar rats: A possible involvement of H+/K+ ATPase α inhibition

Gastroprotective activity of Hypericum perforatum extract in ethanol-induced gastric mucosal injury in Wistar rats: A possible involvement of H+/K+ ATPase α inhibition

UPLC-qTOF-MS Phytochemical Profile and Antiulcer Potential of Cyperus conglomeratus Rottb. Alcoholic Extract

Gastroprotection against Rat Ulcers by Nephthea Sterol Derivative

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