Monteverdia ilicifolia: um protetor gástrico / Monteverdia ilicifolia: a gastric protector / Monteverdia ilicifolia: protector gástrico

Monteverdia ilicifolia, conhecida popularmente como espinheira-santa, é uma planta da família Celastraceae de relevante ação terapêutica devido às suas propriedades medicinais, principalmente a sua atividade gastroprotetora, possuindo efeitos comprovados sobre acidez e úlceras estomacais. Desta forma o objetivo deste trabalho foi encontrar na literatura evidências para o uso terapêutico da M. ilicifolia, como uma alternativa frente aos fármacos sintéticos disponíveis na indústria farmacêutica voltados para o tratamento de problemas estomacais. Foi utilizado no presente trabalho a base de dados Google acadêmico. Os distúrbios estomacais afetam milhares de pessoas, influenciando de forma negativa na qualidade de vida da população e gerando prejuízos ao sistema de saúde. Os fármacos com atividade sobre a secreção da acidez gástrica são as medicações mais prescritas para essas enfermidades, destacando-se os antagonistas do receptor H2 de histamina e os inibidores da bomba de prótons, amplamente utilizados para o tratamento de úlceras e gastrite. Com o tempo, esses medicamentos passaram a ser indiscriminadamente utilizados, prática que põem em risco a saúde íntegra dos pacientes, mediante aos diversos efeitos adversos que esses medicamentos podem causar. As plantas medicinais têm sido aplicadas na terapia de diversas doenças em toda a história da humanidade. Nesse contexto, a espinheira-santa surge como uma alternativa segura e eficaz para a prevenção e tratamento dessas patologias. Dentre os compostos bioativos que podem desempenhar a atividade gastroprotetora, destacam-se os taninos, triterpenos e flavonóides. Os estudos analisados demonstram que a M. ilicifolia possui relevante ação terapêutica, com potencial para substituir os fármacos usualmente empregados no tratamento de úlceras e gastrite.

The Monteverdia ilicifolia, popularly known as espinheira-santa, is a plant of the Celastraceae's family with relevant therapeutic action due to its medicinal properties, mainly its gastroprotective activity, and possesses proven effects on acidity and stomach ulcers. The aim of this work was to find in the literature evidence for the therapeutic use of M. ilicifolia, as an alternative to the synthetic drugs available in the pharmaceutical industry for the treatment of stomach problems. The academic Google database was used in this work. Stomach disorders affect thousands of people, negatively influencing the population's quality of life and causing damage to the health system. The drugs with activity on gastric acid secretion are the most prescribed medications for these diseases, especially histamine H2 receptor antagonists and proton pump inhibitors, widely used for the treatment of ulcers and gastritis. Over time, these drugs began to be used indiscriminately, a practice that jeopardizes the health of patients, due to the various adverse effects that these drugs can cause. Medicinal plants have been applied in the therapy of various diseases throughout human history. In this context, the espinheira-santa emerges as a safe and effective alternative for the prevention and treatment of these pathologies. Among the bioactive compounds that can perform a gastroprotective activity, tannins, triterpenes, and flavonoids stand out. The analyzed studies demonstrate that M. ilicifolia has relevant therapeutic action, with the potential to replace the drugs usually used in the treatment of ulcers and gastritis.

Monteverdia ilicifolia, conocida popularmente como espinheira-santa, es una planta de la familia Celastraceae de relevante acción terapéutica por sus propiedades medicinales, principalmente su actividad gastroprotectora, con efectos probados sobre la acidez y las úlceras estomacales. Así, el objetivo de este trabajo fue encontrar evidencia en la literatura para el uso terapéutico de M. ilicifolia, como alternativa a las drogas sintéticas disponibles en la industria farmacéutica destinadas al tratamiento de problemas estomacales. En este trabajo se utilizó la base de datos académica de Google. Los trastornos estomacales afectan a miles de personas, influyendo negativamente en la calidad de vida de la población y provocando daños en el sistema de salud. Los fármacos con actividad sobre la secreción ácida gástrica son los más prescritos para estas enfermedades, especialmente los antagonistas de los receptores H2 de histamina y los inhibidores de la bomba de protones, muy utilizados para el tratamiento de úlceras y gastritis. Con el tiempo, estos medicamentos comenzaron a utilizarse de forma indiscriminada, práctica que pone en riesgo la salud de los pacientes, debido a los diversos efectos adversos que estos fármacos pueden ocasionar. Las plantas medicinales se han aplicado en la terapia de diversas enfermedades a lo largo de la historia humana. En este contexto, la espinheira-santa surge como una alternativa segura y eficaz para la prevención y el tratamiento de estas patologías. Entre los compuestos bioactivos que pueden realizar actividad gastroprotectora destacan los taninos, los triterpenos y los flavonoides. Los estudios analizados demuestran que M. ilicifolia tiene una acción terapéutica relevante, con potencial para reemplazar los fármacos habitualmente utilizados en el tratamiento de úlceras y gastritis.

Effects of Coffee on the Gastro-Intestinal Tract: A Narrative Review and Literature Update.

The objective of the present research was to review the state of the art on the consequences of drinking coffee at the different levels of the gastrointestinal tract. At some steps of the digestive process, the effects of coffee consumption seem rather clear. This is the case for the stimulation of gastric acid secretion, the stimulation of biliary and pancreatic secretion, the reduction of gallstone risk, the stimulation of colic motility, and changes in the composition of gut microbiota. Other aspects are still controversial, such as the possibility for coffee to affect gastro-esophageal reflux, peptic ulcers, and intestinal inflammatory diseases. This review also includes a brief summary on the lack of association between coffee consumption and cancer of the different digestive organs, and points to the powerful protective effect of coffee against the risk of hepatocellular carcinoma. This review reports the available evidence on different topics and identifies the areas that would most benefit from additional studies.

Quality of life and gastric acid-suppression medication post-laparoscopic fundoplication: a ten years retrospective study.

Background: Although medical treatment is the best approach for treating gastroesophageal reflux disease (GERD), surgery has a significant role to play not only in cases of failure of medical treatment but also as in a long-term approach, specifically in young patient. On the other hand, alarming reports have been published concerning the outcomes and usefulness of antireflux surgery (ARS). The aim of this study was to evaluate medium and long-term functional outcomes following ARS performed in our institution over a 10 year period.Methods: This was a retrospective review of patients in our department who underwent primary or redo laparoscopic fundoplication between 2005 and 2015. Evaluation of the outcomes was made using a validated questionnaire specifically dedicated to GERD (the Gastroesophageal Reflux Disease - Health-Related Quality of Life (GERD-HRQL) questionnaire) and by investigation about the continued use of proton-pump inhibitors (PPIs). Exclusion criteria were patients treated for GERD with Roux-en-Y gastric bypass, emergency reduction of hiatal hernia, patients missing from follow-up and patients deceased from unrelated causes.Results: 296 patients out of 309 met the inclusion criteria. Primary procedures included 214 Nissen, 35 Toupet, and 23 Collis gastroplasty; there were additionally 62 redo operations. Neither postoperative mortality nor conversion was observed. The mean follow-up was 8 years post-surgery, and contact was made with 96% of the original group. 85% of the patients had stopped PPI use since their operation (86% after Nissen, 73% after Toupet, 94% after Collis and 82% after redos). 90% of the patients had good to excellent functional results as reported by their GERD-HRQL score, and independent of the type of previous procedure. 31 patients were dissatisfied due to dysphagia in 7 and GERD recurrence in 24. Again 75% were extremely satisfied and 15% satisfied. Our own incidence of redo procedures was 11% but the functional result and satisfaction index were comparable between redo and primary procedures. The addition of Collis gastroplasty in cases of real short oesophagus did not alter the final result.Conclusions: Laparoscopic ARS presents a superior alternative to lifetime medication use and can provide long-term control of GERD symptoms in the majority of patients if it is performed skillfully and in carefully evaluated patients. Based on the present study, we believed that significant improvement in GERD health-related quality of life can be attained following both primary and reoperative ARS.

Tablet of Spondias mombin L. Developed from Nebulized Extract Prevents Gastric Ulcers in Mice via Cytoprotective and Antisecretory Effects.

Spondias mombin L. (Anacardiaceae) has a worldwide distribution and is present in all regions of Brazil. Its leaves, flowers and bark are used as teas in folk medicine to treat diseases of the digestive system. This study aimed to evaluate the acute non-clinical toxicity, gastroprotective activity, and the related mechanisms of action of nebulized extract and tablets based on dried Spondias mombin (SmNE). SmNE screening showed the presence of flavonoids (0.65%), polyphenols (25.50%), where the major compound is gallic acid. In the acute oral toxicity assay, a dose of 2000 mg/kg of SmNE administered orally in Swiss mice did not induce any behavioral changes. SmNE (250 or 500 mg/kg p.o) significantly reduced the ulcerative lesion area when compared to the control group in ethanol and non-steroidal anti-inflammatory drug (NSAIDs) models. Results showed that treatment with SmNE (250 mg/kg) reduced acid secretion and gastric content, accompanied with an increase in pH. Previous administration of indomethacin and glibenclamide reversed the protection provided by SmNE, confirming the participation of prostaglandins (PGs) and ATP-sensitive potassium channels (KATP) in its gastroprotective effect. The SmNE tablets met the pharmacopeial quality requirements with gastroprotective activity and similar protection in comparison to the isolated extract administrated. In conclusion, SmNe has a gastroprotective activity related to cytoprotective mechanisms, such as the participation of endogenous prostaglandins and KATP channels, having an anti-secretory effect with systemic action. The formulation obtained presented gastroprotective effects similar to the administration of the extract, the tablets showed favorable compression characteristics by the direct route and met the pharmacopeial quality requirements.

The gastroprotective effect of red propolis extract from Northeastern Brazil and the role of its isolated compounds.

ETHNOPHARMACOLOGICAL RELEVANCE: Propolis has been used in folk medicine to treat gastric disorders for centuries. However, although studies have been conducted to validate the gastroprotective and anti-ulcer activity of some types of propolis, red propolis activity remains unknown. AIM OF THE STUDY: The present study aimed to evaluate the gastroprotective effect of the hydroalcoholic extract of red propolis (HERP), its mode of action, and the main compounds involved in its activity, therefore contributing to validate the chemical and pharmacological potential of this product. MATERIAL AND METHODS: The effect of HERP (30, 100 and 300 mg/kg p.o. and 30 mg/kg i.p.), and the isolated compounds vestitol (VS), neovestitol (NV), methylvestitol (MV), medicarpin (MD), and oblongifolin AB (OB) (10 mg/kg p.o.) were evaluated on gastric ulcers induced by 60% ethanol/0.3 M HCl (5 mL/kg, p.o.) in mice. Histological changes and mucin levels were assessed by HE and PAS, respectively. Moreover, oxidative stress parameters and myeloperoxidase activity were analyzed on ulcerated tissue. The effect of HERP on gastric acid secretion was evaluated by pyloric ligature model and the mechanisms involved in its gastroprotective effect were investigated by pretreating mice with L-NAME (a non-selective nitric oxide synthase inhibitor, 70 mg/kg, i.p.), NEM (a sulfhydryl group chelator, 10 mg/kg, i.p.), yohimbine (an alpha-adrenergic receptor antagonist, 2 mg/kg, i.p.) and indomethacin (a non-selective cyclooxygenase inhibitor, 10 mg/kg, i.p.). RESULTS: HERP (300 mg/kg p.o. or 30 mg/kg i.p.), MV, and MD (10 mg/kg p.o.) protected gastric mucosa against the damage induced by ethanol/HCl. Histological changes were attenuated by the HERP, MV, and MD. Moreover, HERP and MV increased mucin levels. Besides, oxidative stress and MPO activity were reduced by the three treatments. HERP did not display anti-secretory action, but its effect was abolished by indomethacin treatment. CONCLUSIONS: HERP displays gastroprotective property against ethanol/HCl-induced damage. Its effect is dependent on prostaglandins and mucin production. The compounds MV and MD may have an essential role in the activity of HERP. Our data contribute to validate the traditional use of propolis for gastric disorders.

An agent-based simulator for the gastrointestinal pathway of Listeria monocytogenes.

We developed an agent-based gastric simulator for a human host to illustrate the within host survival mechanisms of Listeria monocytogenes. The simulator incorporates the gastric physiology and digestion processes that are critical for pathogen survival in the stomach. Mathematical formulations for the pH dynamics, stomach emptying time, and survival probability in the presence of gastric acid are integrated in the simulator to evaluate the portion of ingested bacteria that survives in the stomach and reaches the small intestine. The parameters are estimated using in vitro data relevant to the human stomach and L. monocytogenes. The simulator predicts that 5%-29% of ingested bacteria can survive a human stomach and reach the small intestine. In the absence of extensive scientific experiments, which are not feasible on the grounds of ethical and safety concerns, this simulator may provide a supplementary tool to evaluate pathogen survival and subsequent infection, especially with regards to the ingestion of small doses.

Effects of Paeonol and Gastroretention Tablets of Paeonol on Experimental Gastric Ulcers and Intestinal Flora in Rats.

Paeonol, a major ingredient isolated from Moutan Cort, has various pharmacological effects. Our previous studies have shown that paeonol can exert antioxidant and anti-inflammatory therapeutic effects on ethanol-induced experimental gastric ulcer (GU). Therefore, in this study, we designed two GU models in rats induced by pyloric ligation (PL) and acetic acid and evaluated the protective effects of paeonol and gastroretention tablets of paeonol (GRT-Ps; 24, 48, and 96 mg/kg) on GU in rats and the effect of paeonol (48 mg/kg) on the intestinal flora. In vivo experiments showed that paeonol or GRT-Ps remarkably reduced gastric mucosal damage in a dose-dependent manner in the different types of models and improved the superoxide dismutase (SOD) activity and the malondialdehyde (MDA) content. And in fact, the sustained-release effect of GRT-Ps is more conducive to the improvement of GU compared with the rapid clearance of free drugs. In the PL-induced model, gastric secretion parameters, that is, pH and total acid, showed significant differences compared with the model group. In addition, paeonol treatment can improve the richness and diversity of the intestinal flora and increase the amount of beneficial bacteria, such as Lactobacillus. Paeonol and its stable sustained-release tablet GRT-Ps can promote ulcer healing by inhibiting oxidative stress and regulating the intestinal flora. This study can provide basis for the clinical treatment of GU with paeonol. Graphical Abstract.

Cytoprotective and antisecretory properties of methanolic extract of Distemonanthus benthamianus (Caesalpiniaceae) stem bark on acute gastric ulcer in rats.

OBJECTIVES: In African traditional medicine, Distemonanthus benthamianus (Caesalpiniaceae) is used to treat many diseases including gastric ulcers. We evaluated in this study, the cytoprotective and antisecretory properties of the methanolic extract of the stem bark of this plant using different technics of gastric lesion induction. METHODS: Cytoprotective and antisecretory activity of the methanolic extract of D. benthamianus stem bark was evolved through six methods of gastric lesion induction in experimental Wistar male rats (150-200 g): (1) gastric lesions induced by HCl/ethanol, (2) gastric lesions induced by Indomethacin- HCl/ethanol, (3) gastric lesion induced by Indomethacin, (4) gastric lesions induced by Pylorus ligation, (5) gastric lesions induced by histamine-Pylorus ligation, (6) gastric lesions induced by carbachol-Pylorus ligation. Mucus and gastric mucosal ulceration were evaluated. pH, gastric volume, and acidity were quantified in all pylorus ligation induction technics. Nitric oxide (NO) level was determined in indomethacin induced gastric ulcers. RESULTS: At different doses (125, 250 and 500 mg/kg), extract reduced significantly the ulcer index. In all models used, that is 100.00% with HCl/ethanol; 100.00% with HCl/ethanol/indomethacin; 95.70% with Indomethacin; 74.79% with pylorus ligation, 95.94% histamine-Pylorus ligation, 99.54% carbachol-Pylorus ligation at the highest dose of 500 mg/kg. The lesion formation reduces in all the methods used followed by a significant increase of mucus production. The pylorus ligation technic revealed that the extract has an antisecretory activity. CONCLUSIONS: The methanolic extract of D. benthamianus stem bark has both cytoprotective and antisecretory effects. This extract exerts its antisecretory effect trough cholinergic and histaminergic pathways.

Development and evaluation of a biorelevant medium simulating porcine gastrointestinal fluids.

Simulated human intestinal media, have proved to be a useful biopharmaceutics tool as a dissolution media for predicting in vivo dissolution and pharmacokinetic profile in humans. During drug product development preclinical animal models are also required to assess drug product performance, and there is a need to develop species specific intestinal media to similarly predict in vivo pharmacokinetic profiles in each preclinical model. Pigs, are increasingly being used in preclinical drug development, however to date there is a lack of quantitative information about the composition of porcine gastrointestinal (GI) fluids. As a result, a porcine biorelevant medium has not yet been developed, which is essential to improve interpretation and forecast of preclinical results using biorelevant in vitro dissolution studies. GI fluid samples, were collected from landrace pigs, and characterized. Fasted State Simulated Intestinal Fluid of pigs (FaSSIFp) was developed based on the physiological composition of the GI fluids in terms of pH, buffer capacity, osmolality, surface tension, as well as the bile salt, phospholipid and free fatty acid content. This study demonstrated that FaSSIFp was superior at predicting the solubility of the six model drugs in porcine intestinal fluids (PIF). A markedly high correlation (r2 0.98) was observed between the solubility obtained in PIF and FaSSIFp, whereas poor correlation (r2 0.12) was found for the solubility of the model drugs between human FaSSIF and PIF. This confirms that species specific biorelevant intestinal media are crucial to provide more accurate predictions of pharmacokinetic studies in preclinical models. Additionally, the availability of a species specific intestinal medium offers the potential to improve in vitro-in silico approaches to predict in vivo absorption and to reduce the overall number of animals needed in oral drug product development testing.

A novel natural GRAS-grade enteric coating for pharmaceutical and nutraceutical products.

In this study, enteric coatings based exclusively on naturally occurring ingredients were reported. Alginate (Alg) and pectin (Pec) blends with or without naturally occurring glyceride, glycerol monostearate (GMS), were initially used to produce solvent-casted films. Incorporating GMS in the natural polymeric films significantly enhanced the acid-resistance properties in gastric medium. Theophylline tablets coated with Alg-Pec blends without GMS disintegrated shortly after incubation in gastric medium (pH 1.2), leading to a premature and complete release of theophylline. Interestingly, tablets coated with Alg-Pec blends that contain the natural glyceride (GMS) resisted the gastric environment for 2 h with minimal drug release (<5%) and disintegrated rapidly following introduction to the intestinal medium, allowing a fast and complete drug release. Furthermore, the coating system proved to be stable for six months under accelerated conditions. These findings are particularly appealing to nutraceutical industry as they provide the foundation to produce naturally-occurring GRAS based enteric coatings.

Consumption of medicines used for gastric acid-related disorders in Australia and South Korea: a cross-country comparison.

PURPOSE: The study's aim was to compare the use of proton pump inhibitors (PPIs), histamine 2-receptor antagonists (H2RAs) and mucoprotective medicines (MPs) used for gastric acid-related disorders (GARD) in Australia and South Korea (Korea) from 2004 to 2017. METHODS: Prescription data for PPIs, H2RAs and MPs for Australian outpatients were extracted from the Australian Statistics on Medicines annual reports, with dose-specific and expenditure data obtained from Medicare. Similar data were obtained from Korean National Health Insurance Service claims data. We analysed the volume and expenditure of medicines use annually using the defined daily dose per 1,000 population per day. We calculated which medicines accounted for 90% of use and estimated the proportions of use for low- and high-dose PPIs. RESULTS: While total utilisation for GARD medicines increased over time in both countries, patterns of use differed. Overall, use was somewhat higher in Australia but increased more rapidly in Korea. PPIs were used more extensively in Australia, while more MPs and H2RAs were used in Korea. Expenditure and use of low-dose PPIs is escalating in Korea. CONCLUSION: There were substantial differences in the use of GARD medicines in Australia and Korea over 14 years. Both countries face similar challenges to promote rational medicines use and contain medical care costs. The discrepant prescribing patterns can be attributed to differences in healthcare systems, pharmaceutical policies and demographics. This study provides a baseline to influence more rational use of these medicines. It provides insight into medicines policies for other countries that face similar challenges.

Blocking of gastric acid induced histopathological alterations, enhancing of DNA content and proliferation of goblet cells in the acute lung injury mice models by nano-fenugreek oral administration.

This current study aimed at detecting the potential protective role of nano-fenugreek seed on acute lung injury (ALI) induced by instillation gastric acid in male Swiss albino mice using histological and histochemical studies. Forty animals were grouped as follows: control group, HCl-treated group, low nano-fenugreek + HCl treated group, and high nano-fenugreek + HCl treated group. Pretreatment with nano-fenugreek in animal model of ALI resulted in marked ameliorations of the lung histological lesions and injury induced by HCL instillation in a dose dependent manner. It also caused inhibition in the increase of the DNA content and prevented proliferation of goblet cells induced by HCl instillation alone. In conclusion, pretreatment with Nano-fenugreek prior induction ALI could be suppress the aggregations of inflammatory cells, enhancing of DNA content, and proliferation of goblet cells induced by gastric acid in a dose dependent manner. We suggest that Nano-fenugreek may be useful in combating lung injury.

Bioavailability of Sulforaphane Following Ingestion of Glucoraphanin-Rich Broccoli Sprout and Seed Extracts with Active Myrosinase: A Pilot Study of the Effects of Proton Pump Inhibitor Administration.

We examined whether gastric acidity would affect the activity of myrosinase, co-delivered with glucoraphanin (GR), to convert GR to sulforaphane (SF). A broccoli seed and sprout extract (BSE) rich in GR and active myrosinase was delivered before and after participants began taking the anti-acid omeprazole, a potent proton pump inhibitor. Gastric acidity appears to attenuate GR bioavailability, as evidenced by more SF and its metabolites being excreted after participants started taking omeprazole. Enteric coating enhanced conversion of GR to SF, perhaps by sparing myrosinase from the acidity of the stomach. There were negligible effects of age, sex, ethnicity, BMI, vegetable consumption, and bowel movement frequency and quality. Greater body mass correlated with reduced conversion efficiency. Changes in the expression of 20 genes in peripheral blood mononuclear cells were evaluated as possible pharmacodynamic indicators. When grouped by their primary functions based on a priori knowledge, expression of genes associated with inflammation decreased non-significantly, and those genes associated with cytoprotection, detoxification and antioxidant functions increased significantly with bioavailability. Using principal components analysis, component loadings of the changes in gene expression confirmed these groupings in a sensitivity analysis.

Absorption Characteristics of Novel Compound Calcium Carbonate Granules: Effects of Gastric Acid Deficiency and Exogenous Weak Acids.

Calcium carbonates are commonly administered as supplements for conditions of calcium deficiency. We report here pharmacokinetic characteristics of a novel formulation, calcium carbonate compound granules (CCCGs), forming complexes of calcium carbonate and calcium citrate in water. CCCGs were compared to a kind of commonly-used calcium carbonate D3 preparation (CC) in the market in 5-week-old mice that had been treated with omeprazole, to suppress gastric acid secretion, and in untreated control mice. The results showed that: (1) CCCGs had better water solubility than CC in vitro; (2) In control mice, calcium absorption rates after CCCGs administration were comparable to those after CC administration; (3) Inhibition of gastric acid secretion did not affect calcium absorption after CCCGs, but moderately decreased it after CC; (4) The presence of phytic acid or tannin did not affect calcium absorption rates after CCCGs but did for CC; and (5) In normal mice, CCCGs did not inhibit gastric emptying and intestinal propulsion, and did not alter the gastrointestinal hormones. The results suggest that CCCGs may be therapeutically advantageous over more commonly used calcium supplement formulations, particularly for adolescents, because of their stable calcium absorption characteristics and their relatively favorable adverse effect profile.

A Comprehensive Review on the Screening Models for the Pharmacological Assessment of Antiulcer Drugs.

BACKGROUND: Due to inappropriate diet, smoking, alcohol consumption, regular use of drugs like NSAIDs and sedentary lifestyle, one may feel upper abdominal pain which may be the predictor of the gastrointestinal disorder called Peptic Ulcer. When an imbalance occurs between the defensive factor and aggressive factor of the stomach, ulcer formation in the esophageal lining, stomach, or duodenum takes place. This leads to the formation of small sores that cause pain. Another condition that synergizes the abdominal pain is vomiting materials which look like coffee grounds, blood in the stool, black or tarry stools. This pain may increase after lunch or dinner. This problem persists, that often leads to the gastroenterologist's consultation. OBJECTIVE: There are many antiulcer screening models present for the determination of antiulcer activity of the drug molecule. The main objective of this study is to find which model is best for the determination of antiulcer activity. METHODS: A literature search was conducted on the databases namely Science direct and PubMed with the help of different keywords such as "Anti-ulcer", "In-vitro models" and "In-vivo models". The search was customized by applying the appropriate filters so as to get the most relevant articles to meet the objective of this review article. RESULT: There are different research and review papers based on the antiulcer screening models for the determination of antiulcer activity of new drug molecules. CONCLUSION: On the basis of our study, we found some useful models for the antiulcer activity of drugs and suggested that, if we use in-vitro and in-vivo methods together, then we may obtain the most relevant result in our research area.

Cellular antioxidant activity and in vitro inhibition of α-glucosidase, α-amylase and pancreatic lipase of oregano polyphenols under simulated gastrointestinal digestion.

Different oregano species have been traditionally used as infusions in folk medicine. Oregano medicinal properties, such as antioxidant and anti-inflammatory, have been partially attributed to its polyphenolic content. However, information regarding bioaccessibility of oregano polyphenols is limited. Cell-based antioxidant activity, and in vitro hypoglycemic, and hypolipidemic properties of polyphenolic extracts from three species of oregano species, namely, Hedeoma patens (HP), Lippia graveolens (LG) and Lippia palmeri (LP), subjected to simulated gastrointestinal digestion were evaluated. LC-TOF-MS analysis of HP, LG and LP allowed the identification of 9 flavonoids and 6 hydroxycinnamic acid derivatives with nutraceutical significance. Oregano polyphenolic extracts and digests from HP, LG, and LP exhibited cellular antioxidant capacity, hypoglycemic and hypolipidemic properties. Altogether, our results suggest that HP, LG and LP polyphenols exhibit potential for use as hypoglycemic, hypolipidemic, and antioxidant agents.

Nuclear magnetic resonance-based metabolomics approach to evaluate preventive and therapeutic effects of Gastrodia elata Blume on chronic atrophic gastritis.

Chronic atrophic gastritis (CAG) is one of the most common digestive system diseases worldwide which defined by WHO as initial step of cancer. Gastrodia elata Blume (GEB) is a traditional herbal with multiple pharmacological activities which was widely used in Asian countries. This study aims to explore the preventive and therapeutical effects of Gastrodia elata Blume on auto-immune induced CAG in rats. Tissues of stomachs were collected and submitted to 1H NMR-based metabolomics analysis and histopathological inspection. The biochemical indexes of MDA, SOD, GSH, NO and XOD were measured. Gastrodia elata Blume could apparently ameliorate the damaged gastric glands and the biochemical parameters, enhance gastric acid secretion, and significantly relieve the inflammation of the stomach. Orthogonal signal correction-partial least squares-discriminant analysis (OSC-PLS-DA) of NMR profiles and correlation network analysis revealed that Gastrodia elata Blume could effectively treat CAG via regulating energy and purine metabolisms, and by anti-oxidation and anti-inflammation effects.

Refractory GERD, beyond proton pump inhibitors.

Pharmacologic therapy, surgery, minimally invasive therapies, and alternative therapies are different options available for the management of refractory GERD. The choice may depend on the cause of refractoriness. Increased gastric acid suppression therapy might be useful in the rare patients with persistent elevated esophageal acid exposure on proton pump inhibitors (PPI). Potassium-competitive acid blockers (P-CAB) might induce a more important acid inhibition than PPI. Baclofen might act as a reflux inhibitor and demonstrates a significant efficacy in rumination syndrome. The role of topical antacid-alginate in refractory GERD might be limited. Surgery might be a valid option in case of persistent pathological acid esophageal exposure despite PPI. Further evaluation of minimally invasive procedures is necessary. Finally diet, diaphragmatic breathing and transcutaneous electrical acustimulation might be of interest in patients with esophageal hypersensivity or functional symptoms.

Pea Ferritin Stability under Gastric pH Conditions Determines the Mechanism of Iron Uptake in Caco-2 Cells.

Background: Iron deficiency is an enduring global health problem that requires new remedial approaches. Iron absorption from soybean-derived ferritin, an ∼550-kDa iron storage protein, is comparable to bioavailable ferrous sulfate (FeSO4). However, the absorption of ferritin is reported to involve an endocytic mechanism, independent of divalent metal ion transporter 1 (DMT-1), the transporter for nonheme iron. Objective: Our overall aim was to examine the potential of purified ferritin from peas (Pisum sativum) as a food supplement by measuring its stability under gastric pH treatment and the mechanisms of iron uptake into Caco-2 cells. Methods: Caco-2 cells were treated with native or gastric pH-treated pea ferritin in combination with dietary modulators of nonheme iron uptake, small interfering RNA targeting DMT-1, or chemical inhibitors of endocytosis. Cellular ferritin formation, a surrogate measure of iron uptake, and internalization of pea ferritin with the use of specific antibodies were measured. The production of reactive oxygen species (ROS) in response to equimolar concentrations of native pea ferritin and FeSO4 was also compared. Results: Pea ferritin exposed to gastric pH treatment was degraded, and the released iron was transported into Caco-2 cells by DMT-1. Inhibitors of DMT-1 and nonheme iron absorption reduced iron uptake by 26-40%. Conversely, in the absence of gastric pH treatment, the iron uptake of native pea ferritin was unaffected by inhibitors of nonheme iron absorption, and the protein was observed to be internalized in Caco-2 cells. Chlorpromazine (clathrin-mediated endocytosis inhibitor) reduced the native pea ferritin content within cells by ∼30%, which confirmed that the native pea ferritin was transported into cells via a clathrin-mediated endocytic pathway. In addition, 60% less ROS production resulted from native pea ferritin in comparison to FeSO4. Conclusion: With consideration that nonheme dietary inhibitors display no effect on iron uptake and the low oxidative potential relative to FeSO4, intact pea ferritin appears to be a promising iron supplement.

Acid suppression medications reduce risk of oesophageal adenocarcinoma in Barrett's oesophagus: a nested case-control study in US male veterans.

BACKGROUND: Proton pump inhibitors (PPIs) and histamine-2 receptor antagonists (H2RAs) may reduce the risk of oesophageal adenocarcinoma (OAC) in Barrett's oesophagus; however, current epidemiologic studies are inconclusive. AIM: To evaluate the independent effects of PPIs and H2RAs on risk of OAC in patients with Barrett's oesophagus. METHODS: We conducted a nested case-control study of male veterans diagnosed with Barrett's oesophagus. Cases with incident OAC were matched by incidence density sampling on birth year and Barrett's diagnosis date to controls with Barrett's oesophagus who did not develop OAC. We identified prescription medication usage 1 year prior to Barrett's oesophagus diagnosis to 3 months prior to the OAC diagnosis. Odds ratios (OR) and 95% CI were estimated using conditional logistic regression. RESULTS: Compared with 798 controls, the 300 cases were less likely to use PPIs (90.0% vs 94.5%, P = 0.01) and H2RAs (19.7% vs 25.7%, P = 0.04). In the multivariable model including the use of statins, H2RAs, aspirin and nonsteroidal anti-inflammatory drugs, PPI use was associated with 41% lower risk of OAC (OR 0.59, 95% CI 0.35-0.99). While risk reduction of OAC was stronger for high-dose PPIs (omeprazole daily dose >40 mg, adjusted OR 0.11, 95% 0.04-0.36), we did not find a dose-response relationship with PPI duration (P trend = 0.45). Likewise, H2RA use was independently associated with 30% lower risk of OAC (OR 0.70, 95% CI 0.50-0.99). CONCLUSION: Use of PPIs and H2RAs among patients with Barrett's oesophagus are associated with lower risk of OAC. Further clinical trials are needed to confirm this possible chemopreventive effect.