BACKGROUND: Peptic ulcer is a condition characterized by open sores resulting from excessive acid production in the stomach or digestive tract, causing damage to the mucosal lining. Tamarix gallica (TG), is traditionally known for its anti-inflammatory, antioxidant, antibacterial activity, etc. Objective: The scientific evidences based on its efficacy specifically for anti-ulcers activity are limited, hence, the study aimed to evaluate protective effect of TG against aspirin-induced peptic ulcers.
METHODS: Phytochemical screening was performed followed by assessment of protective effect of TG against aspirin induced toxicity in rats. Network biology and polypharmacology studies were performed to determine the possible molecular targets involved in pathophysiology of ulcers.
RESULTS: The study revealed that the TG extract at high dose (500 mg/kg b.w.) significantly exhibits protective effect against aspirin induced ulcers via regulation of free acidity pepsin production, overall acidity via regulating antioxidant status (SOD, GSH, CAT, etc). Morphological studies revealed less damage with less disruption of the gastric mucosa layer having normal mucosal structure, no swelling or oedema was found in drug treated groups.
CONCLUSIONS: Moreover, network biology and polypharmacology outcomes revealed that SOD2, CAT, EPO, IL10, EGF, TGFB1 etc. play a significant role in functional gastrointestinal-associated disease or peptic ulcer. Hence, the study concludes that TG polyphenols including phenols and flavonoids play an important role in alleviation of peptic ulcer or associated complication and thus demonstrating TG as a natural therapeutic regimen against ulcers in glance of nature.

The objective of this study was to characterize the bioactive ingredients and antiulcer effects of Lactuca sativa leaves. Several bioactive chemicals were found in the cold methanolic extract of Lactuca sativa leaves after gas chromatography-mass spectrometry (GC-MS) research: 9,12-octadecadienoic acid (Z,Z)-, cyclononasiloxane, octadecamethyl-, n-hexadecanoic acid, Hexadecanoic acid, 2-hydroxy-1-(hydroxymethyl)ethyl, octadecanoic acid, 2-hydroxy-1-(hydroxymethyl)ethyl ester, 9-octadecenamide, (Z)-, hexadecanoic acid, stigmasterol, benzothiazole, ethyl iso-allocholate, and octacosane. Distinct fingerprint regions in GCMS indicated the existence of bioactive compounds. The leaf powder of Lactuca sativa (LPL) demonstrated substantial antiulcer properties at 400 mg/kg, which was almost equivalent to the standard drug at 20 mg/kg. The cytokine network was efficiently regulated by reducing the production of proinflammatory cytokines such as IL-1β, IL-6, and TNF-α. The levels of caspase-3 and caspase-9 were also considerably lowered at p < 0.05 significant level.

Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken as independent variables and their effects were evaluated on vesicle size (nm), entrapment efficiency (%, EE) and drug release (%, DR). Furthermore, optimized EZL-PNs (EZL-PNs-opt) formulation was evaluated for ex vivo permeation, pharmacokinetic and ulcer protection activity. Result: The EZL-PNs-opt formulation showed 616 ± 13.21 nm of vesicle size, and 81.21 ± 2.35% of EE. EZL-PNs-opt exhibited negative zeta potential and spherical confirmed scanning electron microscopy. EZL-PNs-opt showed sustained release of EZL (95.07 ± 2.10% in 12 h) than pure EZL dispersion. The ex-vivo gut permeation result exhibited a significantly (p < 0.05) enhanced flux than pure EZL. The in vivo results revealed 4.02-fold enhancement in bioavailability and 61.65% protection in ulcer than pure EZL dispersion (43.82%). Conclusion: Our findings revealed that EZL-PNs formulation could be an alternative delivery system of EZL to enhance oral bioavailability and antiulcer activity.

Peptic ulcer disease affects many people globally. With the increasing resistance to some orthodox antibiotics such as Clarithromycin and Metronidazole, it is important that new acceptable, safer and effective therapies are developed to manage this disease. Various herbal medicines have been used traditionally for the remedy of peptic ulcer disease (PUD), however scientific information with regards to their anti-peptic ulcer both in-vivo and in-vitro as well as clinical studies supporting their use is still inadequate. The Centre for Plant Medicine Research, (CPMR) Mampong-Akuapem, Ghana manufactures three herbal Products namely Enterica, Dyspepsia and NPK 500 capsules which are currently used for the remedy of PUD as a triple therapy at its out-patient clinic with promising effects. The aim of this review is to gather information from literature on the anti-ulcer properties, pharmacological, phytochemical constituents and related activities of herbal plants used at the CPMR for formulation of the triple herbal therapy. This review may, provide some scientific bases for the use of Enterica, Dyspepsia and NPK 500 capsules in the management of Peptic ulcer at the CPMR out-patient clinic.
METHODS: Organization for the review involved the on and/or offline search for information from available literature using electronic data and scientific research information resources such as PubMed, Science Direct and Google scholar.
RESULTS: In this review, fifteen ethno-medicinal plants used for the formulation of Enterica, Dyspepsia and NPK capsules have been discussed, presenting the description of the plants, composition and pharmacological activity.
CONCLUSIONS: Tables with the summary of reviewed medicinal plants with their anti-ulcer models and inference on possible mechanisms of action were drawn up. The mechanism(s) of action of individual plants and products (Enterica, Dyspepsia and NPK 500 capsules) must be further investigated and established experimentally in-vitro in addition to in-vivo pharmacological and clinical activity studies to confirm their use in the remedy of PUD.

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.

Stress is a typical body\'s natural defense to a generic physical or psychic change. A specific linking mechanism between ulcer onset and psycho-physical stress prolonged exposure has been reported. We decided to investigate the possible effects of Borago officinalis L. (Borago) in preventing physical (stress)-induced gastric ulcers in a rat model. Eighty male Sprague-Dawley rats were randomly divided into 16 groups, pretreated with a control solution, omeprazole (20 mg/kg), Borago methanolic extract (25, 50, 100, 250, and 500 mg/kg), Borago organic extract (50, 100, 250, and 500 mg/kg), Borago aqueous extract (5, 10, 20, 30, and 40 mg/kg), and D(-)-2-Amino-5-phosphonovaleric acid (AP5) (25 mg/kg) and kept in stressful conditions such as water immersion and restraint-induced stress ulcers. The animals were sacrificed and their stomach scored for the severity and the number of gastric ulcers. Methanolic extract (500 mg/kg) significantly reduced both ulcer parameters (*** p < 0.001 and ** p < 0.01, respectively). Aqueous and organic extract significantly decreased severity score at 5 and 10 mg/kg (** p < 0.01 and *** p < 0.001, respectively), and at 250 and 500 mg/kg (*** p < 0.001), respectively, while gastric ulcers\' resulted number significantly reduced only at 10 mg/kg (* p < 0.05) and at 500 mg/kg (** p < 0.01), respectively. On the other hand, aqueous extract significantly increased the mucosal gastric content of cAMP (* p < 0.05) and NR2A and NR2B subunits (* p < 0.05 and ** p < 0.01, respectively) at 5 mg/kg. Organic extract showed also a significant cytotoxic effect at 500 and 1,000 mg/kg with a 3T3 cell viability reduction of 43.6% (** p < 0.01) and 92.1% (*** p < 0.001), respectively. Borago aqueous extract at 10 mg/kg could be considered as a potential protective agent against stress-induced ulcers, and it is reasonable to possibly ascribe such protective activity to a modulation of the NR2A and NR2B subunit expression.

This study aims to evaluate the anti-inflammatory and anti-ulcer activities of Cucumis melo L. cv. Ismailawi fruits, as well as the investigation of the phenolic content and lipoidal matter composition via high performance liquid chromatography and gas chromatography coupled to mass spectrometry respectively. Both the petroleum ether and defatted methanol extracts of the fruit pulp showed 63.13% and 54.97% decrease in oedema volume respectively after 4 h in comparison to indomethacin standard drug. Both the petroleum ether extract and ethyl acetate fractions at a dose (200 mg/kg) showed significant anti-ulcer activity decreasing both ulcer number and severity in comparison to ranitidine as standard drug. Histopathological investigation further confirmed these results. Moreover; this is the first report for the investigation of the phenolic content and the lipoidal matter of Cucumis melo L. cv. Ismailawi fruits where methyl palmatate, gallic acid and rutin represented the major detected components.

UNASSIGNED: Diosmin showed poor water solubility and low bioavailability. Poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles were successfully used to improve the drugs solubility and bioavailability. Coating of PLGA nanoparticles with chitosan can ameliorate their gastric retention and cellular uptake.
UNASSIGNED: PLGA nanoparticles of diosmin were prepared using different drug and polymer amounts. Nanoparticles were selected based on entrapment efficiency% (EE%) and particle size measurements to be coated with chitosan. The selected nanoparticles either uncoated or coated were evaluated regarding morphology, ζ-potential, solid-state characterization, in vitro release, storage stability, and mucoadhesion. The anti-ulcer activity (AA) against ethanol-induced ulcer in rats was assessed through macroscopical evaluation, histopathological examination, immunohistochemical localization of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and transmission electron microscopic examination of gastric tissues compared to free diosmin (100 mg/kg) and positive control.
UNASSIGNED: Based on EE% and particle size measurements, the selected nanoparticles, either uncoated or coated with 0.1% w/v chitosan, were based on 1:15 drug-PLGA weight ratio and 20 mg diosmin employing methylene chloride as an organic phase. Examination by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed nanoscopic spherical particles. Drug encapsulation within the selected nanoparticles was suggested by Fourier transform-infrared, differential scanning calorimetry (DSC) and X-ray diffractometry results. Chitosan-coated nanoparticles were more stable against size enlargement probably due to the higher ζ-potential. Only coated nanoparticles showed gastric retention as revealed by SEM examination of stomach and duodenum. The superior AA of coated nanoparticles was confirmed by significant reduction in average mucosal damage, the majority of histopathological changes and NF-κB expression in gastric tissue when compared to positive control, diosmin and uncoated nanoparticles as well as insignificant difference relative to normal control. Coated nanoparticles preserved the normal ultrastructure of the gastric mucosa as revealed by TEM examination.
UNASSIGNED: The optimized chitosan-coated PLGA nanoparticles can be represented as a potential oral drug delivery system of diosmin.

Selenium (Se) is a dietary essential trace element with important biological roles. It is a nutrient related to the complex metabolic and enzymatic functions. Organoselenium compounds have been reported to have anti-ulcer activity and used as drug for the treatment of gastrointestinal disorders. The antiulcer activity of binapthyl diselenide (NapSe)2 was investigated in ethanol-induced gastric lesions in rats. A number of markers of oxidative stress were examined in rats stomach including thiobarbituric acid reactive species (TBARS), catalase (CAT), superoxide dismutase (SOD), non-protein thiol groups (NPSH) and ascorbic acid. (NapSe)2 was found to be significantly restoring the deficits in the antioxidant defense mechanisms (CAT, SOD, NPSH and ascorbic acid), and suppressed lipid peroxidation in rat stomach resulting from EtOH administration. It is experimentally concluded that ethanol exposure causes alterations in the antioxidant defense system and induces oxidative stress in rat stomach. These studies establish a promising foundation for investigating and understanding the beneficial effects of organoselenium compounds on human health. Moreover, (NaPSe)2 deserves further investigation as a therapeutic and preventive agent against gastric ulcer in humans.

Osyris quadripartita (OQ) Salzm. ex Decne. has been used to treat peptic ulcer disease in Ethiopian folk medicine, but its efficacy has not been validated. The present study was therefore carried out to evaluate the anti-ulcer activity of 80% methanol leaf extract of OQ in rats. The effect of OQ extract on gastric ulcer in rats in pylorus ligation-induced and ethanol-induced models was studied using single dosing (100, 200, 400 mg/kg) and repeated dosing (200 mg/kg for 10 and 20 days) approaches. Ranitidine (50 mg/kg) and sucralfate (100 mg/kg) were used as the standard drugs. Depending on the model, outcome measures were volume and pH of gastric fluid, total acidity, ulcer score, percent inhibition of ulcer score, ulcer index as well as percent inhibition of ulcer index. Data were analyzed using one-way analysis of variance followed by Tukey\'s post hoc test, and P<0.05 was considered as statistically significant. OQ significantly (P<0.001) reduced gastric ulcer index by 55.82% and 62.11%, respectively, in pylorus ligation-induced and ethanol-induced ulcer models at the 400 mg/kg dose, which is comparable to the standard drugs. Ten and 20 days pre-treatment with OQ200 exhibited significant (P<0.001) ulcer inhibition by 66.48% and 68.36% (pylorus ligation-induced model) as well as 71.48% and 85.35% (ethanol-induced model), respectively. OQ possesses both dose-dependent and time-dependent anti-ulcer effect in the two models. The oral median lethal dose (LD50) is estimated to be higher than 2000 mg/kg for the crude hydroalcoholic extract, and secondary metabolites such as flavonoids, tannins, and saponins were present. The findings of this study confirmed that OQ has anti-ulcer pharmacologic activity due to one or more of the secondary metabolites present in it. Therefore, this study validates its anti-ulcer use in Ethiopian folk medicine. Further investigations on isolation of specific phytochemicals and elucidating mechanisms of action are needed.