Search Results (9)

Background/Objectives: Gastro-oesophageal reflux disease (GERD) refers to a disease in which stomach acid rises into the oesophagus. Currently, proton pump inhibitors (PPIs) are the most commonly used medications to treat GERD. However, long-term use of PPIs is not free from side effects, and new treatment strategies are needed. The present study was conducted to evaluate the gastroprotective potential of four different formulations containing both antiacids and medicinal plants considered useful for the treatment of GERD. Methods: The protective effects of the formulations on gastric ulcers in pyloric ligation-induced gastric mucosal lesions in mice were evaluated by measuring gastric emptying, the ulcer index, gastric content, total acidity, and the pH of the gastric fluid. Gastric damage was also assessed by measuring myeloperoxidase (MPO) activity. Results: Formulations containing Glycyrrhiza glabra L. or Glycyrrhiza glabra L. plus Opuntia ficus-indica Mill. and Olea europaea L. (formulations 3 and 4, respectively) increased gastric emptying. All formulations decreased gastro-oesophageal damage (ulceration and MPO activity) and gastric contents and had no effects on total acidity or gastric fluid pH in the pyloric ligation ulcer model. Conclusions: Our results show that all formulations are able to exert cytoprotective and anti-ulcerative effects. However, among the formulations, formulation 4 seems to be the most promising because of its better effects on gastric injury and gastric emptying. These results support the hypothesis of the possible use of medicinal plants in combination with antacid agents in the treatment of GERD. Full article

Background and Objectives: Acute gastric injury is a prevalent gastrointestinal disorder characterized by inflammation and damage to the stomach lining. In this study, we investigated the therapeutic potential effects of broccoli stem extract (BSE) against acute gastritis in a rat model. Materials and Methods: The antioxidant properties of BSE were evaluated through DPPH and ABTS radical scavenging activity assays and total polyphenol content analysis. Acute gastric injury was induced using 150 mM HCl/60% EtOH, and male SD rats (6-weeks old, n = 6/group) were administered BSE by oral gavage at concentrations of 50, 125, and 250 mg/kg. Results: The BSE 250 mg/kg group exhibited significant relief of clinical signs compared to the negative control group. In addition, the BSE 250 mg/kg group showed significant improvements in gastric tissue, including macroscopic reductions in ulcer size and improved overall gastric morphology as assessed through gross examination, as well as microscopic improvements such as reduced inflammation and the restoration of mucosal integrity observed in histopathological analysis. BSE modulated NF-κB signaling, decreased inflammatory cytokines (TNF-α, IL-1β, and IL-6), and increased PGE₂ levels. Pyloric ligation experiments demonstrated reduced pepsin and gastric acid secretion. Improvements in gastric emptying and gastrointestinal motility were also observed in the BSE-treated group. Conclusions: These findings highlight the potential of BSE as an effective therapeutic agent for acute gastritis in rats, offering significant improvements in gastric damage, inflammation, and motility. Full article

The presence of ammonium ions in urine, along with basic pH in the presence of urease-producing bacteria, promotes the production of struvite stones. This causes renal malfunction, which is manifested by symptoms such as fever, nausea, vomiting, and blood in the urine. The involvement of urease in stone formation makes it a good target for finding urease enzyme inhibitors, which have the potential to be developed as lead drugs against kidney stones in the future. The documented ethnopharmacology of coumarin 2-one against bacterial, fungal and viral strains encouraged us to synthesize new derivatives of coumarins by reacting aromatic aldehydes with 4-aminocoumarin. The synthesized compounds (2a to 11a) were evaluated for their antimicrobial, in vitro, and in silico properties against the urease enzyme. The study also covers in vivo determination of the synthesized compounds with respect to different types of induced ulcers. The molecular docking study along with extended MD simulations (100 ns each) and MMPBSA study confirmed the potential inhibitory candidates as evident from computed ∆G_bind (3a = −11.62 and 5a = −12.08 Kcal/mol) against the urease enzyme. The in silico analyses were augmented by an enzymatic assay, which revealed that compounds 3a and 5a had strong inhibitory action, with IC₅₀ of 0.412 µM (64.0% inhibition) and 0.322 µM (77.7% inhibition), respectively, compared to standard (Thiourea) with 82% inhibition at 0.14 µM. Moreover, the most active compound, 5a, was further tested in vivo for antiulcer activity by different types of induced ulcers, including pyloric ligation-, ethanol-, aspirin-, and histamine-induced ulcers. Compound 5a effectively reduced gastric acidity, lipid peroxidation, and ulceration in a rat model while also inhibiting gastric ATPase activity, which makes it a promising candidate for ulcer treatment. As a result of the current research, 3a and 5a may be used as new molecules for developing potent urease inhibitors. Additionally, the compound 3a showed antibacterial activity against Staphylococcus aureus and Salmonella typhimurium, with zones of inhibition of 41 ± 0.9 mm and 35 ± 0.9 mm, respectively. Compound 7a showed antibacterial activity against Staphylococcus aureus and Salmonella typhimurium, with zones of inhibition of 30 ± 0.8 mm and 42 ± 0.8 mm, respectively. These results prove that the synthesized compounds also possess good antibacterial potential against Gram-positive and Gram-negative bacterial strains. Full article

Tongkat ali (Eurycoma longifolia Jack) (ELJ) is a plant in the Simaroubaceae family. Its roots are used in traditional Thai medicine to treat inflammation, pain, and fever; however, the antiulcer abilities of its ethanolic extract have not been studied. This study examined the anti-inflammatory, antinociceptive, antipyretic, and gastroprotective effects of ethanolic ELJ extract in animal models and found that ELJ effectively reduced EPP-induced ear edema in a dose-dependent manner and that a high dose of ELJ inhibited carrageenan-induced hind paw edema formation. In cotton-pellet-induced granuloma formation, a high dose of ELJ suppressed the increases in wet granuloma weight but not dry or transudative weight. In the formalin-induced nociception study, ELJ had a significant dose-dependent inhibitory impact. Additionally, the study found that yeast-induced hyperthermia could be significantly reduced by antipyretic action at the highest dose of ELJ. In all the gastric ulcer models induced by chemical substances or physical activity, ELJ extracts at 150, 300, and 600 mg/kg also effectively prevented gastric ulcer formation. In the pyloric ligation model, however, the effects of ELJ extract on gastric volume, gastric pH, and total acidity were statistically insignificant. These findings support the current widespread use of Eurycoma longifolia Jack in traditional medicine, suggest the plant’s medicinal potential for development of phytomedicines with anti-inflammatory, antinociceptive, and antipyretic properties, and support its use in the treatment of gastric ulcers due to its gastroprotective properties. Full article

Foxtail millet has been traditionally considered to possess gastroprotective effects, but studies evaluating its use as a treatment for gastric ulcers are lacking. Here, we assessed the antiulcer effects of foxtail millet protein hydrolysate (FPH) and explored its mechanism by using blocking agents. In a mouse model of ethanol-induced gastric ulcers, pretreatment with FPH reduced the ulcerative lesion index, downregulated the expression of inflammatory cytokines in the gastric tissue, increased the activity of antioxidant enzymes, and improved the oxidative status. FPH increased constitutive the activity of nitric oxide synthase (cNOS), NO levels, and mucin expression in gastric mucosa, and inhibited the activation of the ET-1/PI3K/Akt pathway. In a mouse model of pyloric ligation-induced gastric ulcers, FPH inhibited gastric acid secretion and decreased the activity of gastric protease. Pretreatment of mice with the sulfhydryl blocker NEM and the NO synthesis inhibitor L-NAME abolished the gastroprotective effect of FPH, but not the KATP channel blocker glibenclamide and the PGE2 synthesis blocker indomethacin. Among the peptides identified in FPH, 10 peptides were predicted to have regulatory effects on the gastric mucosa, and the key sequences were GP and PG. The results confirmed the gastroprotective effect of FPH and revealed that its mechanism was through the regulation of gastric mucosal mucus and NO synthesis. This study supports the health effects of a millet-enriched diet and provides a basis for millet protein as a functional food to improve gastric ulcers and its related oxidative stress. Full article

Gastritis and gastric ulcers caused by stressors such as drinking are common. The ability of functional foods to protect the stomach more effectively and reduce the risk of side effects is of interest. The fermentation process can increase the preservation and bioactive compound content of kiwi fruits. This study produced fermented kiwi powder using two lactic acids separated from gold kiwi fruits. Gold kiwi puree (Actinidia chinensis L.) was fermented using beneficial bacteria. Fermentation increased the content of bioactive compounds such as organic acids, flavonoids, and carotenoids. We investigated whether fermented gold kiwi (FGK) extract had antioxidant and gastric protective effects in an HCl/EtOH-induced gastritis animal model and pyloric ligation animal model. FGK increased radical scavenging activity in a dose-dependent manner. In the gastritis model, FGK inhibited inflammation-related factors such as iNOS, COX-2, IL-6, and TNF-α, while increasing the expression of the protective molecule PGE2. Furthermore, FGK administration improved gastric lesion site appearance, clinical symptoms, and mucosal thickness in rats. FGK also reduced gastric fluid volume, free acidity, total acidity, and pepsin activity in the pyloric ligation model. These results suggest that FGK can decrease the inflammatory response and protect the gastric mucosa. FGK therefore has the potential to prevent and treat gastritis and gastric ulcers. Full article

This study was designed to determine whether α-humulene, a major constituent in many plants used in fragrances, has a protective role against gastric injury in vivo and in vitro. A rat model of hydrochloric acid (HCl)/ethanol-induced gastritis and human mast cells (HMC-1) were used to investigate the mucosal protective effect of α-humulene. α-Humulene significantly inhibited gastric lesions in HCl/ethanol-induced acute gastritis and decreased gastric acid secretion pyloric ligation-induced gastric ulcers in vivo. In addition, α-humulene reduced the amount of reactive oxygen species and malondialdehyde through upregulation of prostaglandin E2 (PGE2) and superoxide dismutase (SOD). In HMC-1 cells, α-humulene decreased intracellular calcium and increased intracellular cyclic adenosine monophosphate (cAMP) levels, resulting in low histamine levels. α-Humulene also reduced the expression levels of cytokine genes such as interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF) by downregulating nuclear factor-κB (NF-κB) nuclear translocation. Finally, α-humulene upregulated the expression levels of mucin 5AC (Muc5ac), Muc6, trefoil factor 1 (Tff1), trefoil factor 2 (Tff2), and polymeric immunoglobulin receptor (pigr). α-Humulene may attenuate HCl/ethanol-induced gastritis by inhibiting histamine release and NF-κB activation and stimulating antioxidants and mucosal protective factors, particularly Muc5ac and Muc6. Therefore, these data suggest that α-humulene is a potential drug candidate for the treatment of stress-induced or alcoholic gastritis. Full article

Polygonum cuspidatum is widely used as food and medicine in Korea, China, and Japan. Its major bioactive components, resveratrol and emodin, reportedly protect against gastric lesions. We therefore aimed to investigate: (1) the gastroprotective effects of P. cuspidatum roots in hydrochloric acid/ethanol (HCl/EtOH)- and indomethacin-induced acute gastric ulcer rat models; (2) the healing effects in an acetic acid-induced ulcer model; and (3) potential mechanisms by measuring gastric acid secretion-related parameters in a pyloric ligation-induced ulcer model, and by measuring antioxidant enzyme and prostaglandin E₂ levels in the gastric tissue of HCl/EtOH-treated rats. Oral administration of P. cuspidatum extract (PCE) at doses of 100 and 300 mg/kg significantly decreased HCl/EtOH- and indomethacin-induced gastric lesions. PCE at 300 mg/kg significantly reduced gastric lesions in acetic acid-induced ulcers. PCE increased superoxide dismutase (SOD) activity and glutathione (GSH) and prostaglandin E₂ levels in gastric tissue, whereas it did not alter gastric acid secretion-related parameters. Our findings indicate that PCE has gastroprotective effects against HCl/EtOH and non-steroidal anti-inflammatory drugs (NSAIDs) and promotes healing of acetic acid-induced ulcers. These gastric mucosal protection and ulcer healing effects are associated with antioxidant effects and the augmentation of prostaglandin E₂ and suggest that P. cuspidatum might be a promising preventive and therapeutic agent for treating gastric ulcers. Full article

Recently, an alternative disease treatment approach is the research of medicaments from traditional medicine. Plants with anti-oxidant capabilities are used as herbal treatments for ulcer diseases. Medicinal/herbal extracts containing phytoconstituents have significant anti-ulcer activities in in vivo experiments on animal models, compared to reference drugs. The current study aims to inspect gastro-protective as well as in vitro and in vivo anti-oxidant potential of Althaea officinalis and Solanum nigrum extracts on pyloric-ligation/indomethacin-induced gastric-ulceration in rats. Rats were divided into six groups: normal control, gastric ulcer control, two standard pretreatment groups receiving omeprazole and misoprostol, and two test pretreatment groups receiving Althaea officinalis and Solanum nigrum. Pretreatments were administrated orally for 14 days. On the 15th day, animals, excluding the normal control group, were exposed to pyloric-ligation followed by indomethacin injection. After four hours, the rat’s stomachs were removed and gastric juice and blood samples were collected. Pyloric-ligation/indomethacin administration caused considerable elevation in ulcer number, ulcer index, acid and pepsin productivity, aggressive factors, and gastric mucosal lipid-peroxide contents. Moreover, reduction in titratable acidity, gastric mucosal nitric-oxide, anti-oxidant contents, and protective factors accompanied gastric-ulceration. Additionally, elevation in pro-inflammatory cytokines content and reduction in cystathionine-β-synthase and heme-oxygenase-1 expression was witnessed. Omeprazole, misoprostol, Althaea officinalis, and Solanum nigrum pretreatments fixed blood and tissue biomarkers, thereby protecting them from pyloric-ligation/indomethacin-induced gastric-ulceration in rats, which is hopeful for clinical examinations. Full article