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Journal of Drug Targeting Dec 2021Peptic ulcer disease (PUD) is a common condition that is induced by acid and pepsin causing lesions in the mucosa of the duodenum and stomach. The pathogenesis of PUD is... (Review)
Review
Peptic ulcer disease (PUD) is a common condition that is induced by acid and pepsin causing lesions in the mucosa of the duodenum and stomach. The pathogenesis of PUD is a many-sided scenario, which involves an imbalance between protective factors, such as prostaglandins, blood flow, and cell renewal, and aggressive ones, like alcohol abuse, smoking, colonisation, and the use of non-steroidal anti-inflammatory drugs. The standard oral treatment is well established; however, several problems can decrease the success of this therapy, such as drug degradation in the gastric environment, low oral bioavailability, and lack of vectorisation to the target site. In this way, the use of strategies to improve the effectiveness of these conventional drugs becomes interesting. Currently, the use of drug delivery systems is being explored as an option to improve the drug therapy limitations, such as antimicrobial resistance, low bioavailability, molecule degradation in an acid environment, and low concentration of the drug at the site of action. This article provides a review of oral drug delivery systems looking for improving the treatment of PUD.
Topics: Administration, Oral; Animals; Anti-Ulcer Agents; Biological Availability; Drug Delivery Systems; Gastric Mucosa; Humans; Peptic Ulcer; Protective Factors; Risk Factors
PubMed: 33729081
DOI: 10.1080/1061186X.2021.1904249 -
Pharmaceutical Biology Dec 2022(Blume & T. Nees) Torrend (Ganodermataceae) is an edible mushroom with medicinal properties. However, the effects of on gastric ulcer remain unclear.
CONTEXT
(Blume & T. Nees) Torrend (Ganodermataceae) is an edible mushroom with medicinal properties. However, the effects of on gastric ulcer remain unclear.
OBJECTIVE
To investigate the gastroprotective efficacy of water extract of (WEA) on gastric ulcer.
MATERIALS AND METHODS
Sprague-Dawley rats were randomly grouped as control, model, lansoprazole and 200, 100 and 50 mg/kg of WEA. After pre-treatment for seven days, ethanol- and indomethacin-induced gastric ulcer models were established. The gastric ulcer and histopathology were investigated. Enzyme-linked immunosorbent assay (ELISA), quantitative polymerase chain reaction (Q-PCR) and Western blot assays were conducted to explore the potential anti-inflammatory effect and mechanism of WEA. Additionally, the pyloric ligation model was used to explore the influence of WEA on gastric acid and mucus.
RESULTS
Pre-treatment with WEA (200, 100 and 50 mg/kg) effectively reduced ulcerous area in both ethanol-induced (71%, 88% and 71%) and indomethacin-induced (77%, 65% and 86%) gastric ulcer model. The gastric levels of tumour necrosis factor-alpha (TNF-α) (34% and 50 mg/kg), interleukin-6 (IL-6) (32% and 100 mg/kg) and interleukin-1β (IL-1β) (36%, 45% and 41%) were reduced significantly ( < 0.05) by WEA. Serum nitric oxide was decreased significantly ( < 0.05) at 200 and 50 mg/kg and PGE2 concentration was increased remarkably ( < 0.05) at 100 mg/kg. Gene expression of inflammasome , and the nuclear translocation of nuclear factor-κB (NF-κB) P65 were significantly decreased by WEA pre-treatment. However, the pH of gastric acid and secretion of mucus did not show any significant change.
CONCLUSIONS
The gastroprotective effect of WEA on gastric damage is attributed to anti-inflammation through the inhibition on NF-κB P65 nuclear migration and gene expression.
Topics: Animals; Anti-Inflammatory Agents; Anti-Ulcer Agents; Disease Models, Animal; Dose-Response Relationship, Drug; Gene Expression Regulation; Inflammation; Male; NLR Family, Pyrin Domain-Containing 3 Protein; Polyporaceae; Rats; Rats, Sprague-Dawley; Stomach Ulcer; Transcription Factor RelA; Water
PubMed: 35277113
DOI: 10.1080/13880209.2022.2047210 -
Biomolecules Feb 2020Peptic ulcer disease (PUD) is a multifactorial and complex disease caused by an imbalance of protective and aggressive factors (endogenous and exogenous). Despite... (Review)
Review
Peptic ulcer disease (PUD) is a multifactorial and complex disease caused by an imbalance of protective and aggressive factors (endogenous and exogenous). Despite advances in recent years, it is still responsible for substantial mortality and triggering clinical problems. Over the last decades, the understanding of PUD has changed a lot with the discovery of Helicobacter pylori infection. However, this disease continues to be a challenge due to side-effects, incidence of relapse from use of various anti-ulcer medicines, and the rapid appearance of antimicrobial resistance with current H. pylori therapies. Consequently, there is the need to identify more effective and safe anti-ulcer agents. The search for new therapies with natural products is a viable alternative and has been encouraged. The literature reports the importance of monoterpenes based on the extensive pharmacological action of this class, including wound healing and anti-ulcerogenic agents. In the present study, 20 monoterpenes with anti-ulcerogenic properties were evaluated by assessing recent in vitro and in vivo studies. Here, we review the anti-ulcer effects of monoterpenes against ulcerogenic factors such as ethanol, nonsteroidal anti-inflammatory drugs (NSAIDs), and Helicobacter pylori, highlighting challenges in the field.
Topics: Helicobacter Infections; Helicobacter pylori; Humans; Monoterpenes; Peptic Ulcer; Risk Factors
PubMed: 32050614
DOI: 10.3390/biom10020265 -
Journal of Gastroenterology Sep 2023
Topics: Humans; Proton Pump Inhibitors; Pneumonia; Anti-Ulcer Agents
PubMed: 37454300
DOI: 10.1007/s00535-023-02022-6 -
Drug Design, Development and Therapy 2024Ulcer disorders including the oral mucosa, large intestine, and stomach mucosa, cause significant global health burdens. Conventional treatments such as non-steroid... (Review)
Review
Ulcer disorders including the oral mucosa, large intestine, and stomach mucosa, cause significant global health burdens. Conventional treatments such as non-steroid anti-inflammatory drugs (NSAIDs), proton pump inhibitors (PPIs), histamine H receptor antagonists (HRAs), and cytoprotective agents have drawbacks like mucosal injury, diminish gastric acid secretion, and interact with concurrent medications. Therefore, alternative therapeutic approaches are needed to tackle this health concern. Plants are rich in active metabolites in the bark, roots, leaves, fruits, and seeds, and have been utilized for medicinal purposes since ancient times. The use of herbal therapy is crucial, and regulations are necessary to ensure the quality of products, particularly in randomized studies, to assess their efficacy and safety in treating ulcer disorders. This study aims to explore the anti-ulcer activity of medicinal plants in treating peptic ulcer disease, ulcerative colitis, and aphthous ulcers. Articles were searched in Scopus and PubMed, and filtered for publication from 2013 to 2023, resulting in a total of 460 from Scopus and 239 from PubMed. The articles were further screened by title and abstract and resulted in 55 articles. Natural products, rich in active metabolites, were described to manage ulcer disease by protecting the mucosa, reducing ulcer effects, inhibiting pro-inflammatory factors, and reducing bacterial load, thus improving patients' quality of life. Natural extracts have proven effective in managing other health problems, including ulcers by reducing pain and decreasing lesions. This review provides an overview of preclinical and clinical studies on medicinal plants, focusing on their effectiveness in treating conditions like peptic ulcers, ulcerative colitis, and aphthous ulcers.
Topics: Humans; Ulcer; Colitis, Ulcerative; Stomatitis, Aphthous; Quality of Life; Peptic Ulcer; Anti-Ulcer Agents; Histamine H2 Antagonists; Proton Pump Inhibitors; Anti-Inflammatory Agents, Non-Steroidal
PubMed: 38318501
DOI: 10.2147/DDDT.S446949 -
The Korean Journal of Gastroenterology... Nov 2020Nonsteroidal anti-inflammatory drugs (NSAID) are some of the most commonly prescribed medications in clinical practice. The long-term use of NSAIDs is one of the main... (Review)
Review
Nonsteroidal anti-inflammatory drugs (NSAID) are some of the most commonly prescribed medications in clinical practice. The long-term use of NSAIDs is one of the main causes of peptic ulcers and the increased risk of upper gastrointestinal tract complications, such as perforation and bleeding. Thus, the prevention of NSAID-induced peptic ulcers is an important clinical issue. Previous studies have evaluated various strategies for preventing ulcers in patients requiring prolonged NSAID use. The Korean clinical practice guidelines have been published recently based on the evidence of the currently available data. This review describes the strategies for the prevention of peptic ulcers due to NSAID. An assessment of the risk factors for peptic ulcers from NSAID is recommended to identify patients who should be considered for primary prophylaxis. The risk of NSAID-induced peptic ulcers can be reduced by the concomitant use of proton pump inhibitors (PPI), misoprostol, and histamine-2 receptor antagonists. Selective cyclooxygenase-2 inhibitors can be used with caution due to concerns regarding cardiovascular toxicity. Attempts should be made to use the lowest dose and shortest duration of the NSAID.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Anti-Ulcer Agents; Histamine H2 Antagonists; Humans; Peptic Ulcer; Pharmaceutical Preparations; Proton Pump Inhibitors; Risk Factors
PubMed: 33234769
DOI: 10.4166/kjg.2020.139 -
The British Journal of General Practice... Dec 2022Proton pump inhibitor (PPI) indications are limited to gastrointestinal disorders and ulcer prophylaxis. However, PPIs are among the most frequently prescribed drugs. (Observational Study)
Observational Study
BACKGROUND
Proton pump inhibitor (PPI) indications are limited to gastrointestinal disorders and ulcer prophylaxis. However, PPIs are among the most frequently prescribed drugs.
AIM
To evaluate the appropriateness of PPI prescriptions and identify predictive factors for inappropriate PPI use.
DESIGN AND SETTING
Observational study using a Dutch primary care database with all new PPI prescriptions between 2016 and 2018.
METHOD
Individual patient data and details on PPI use were collected. The appropriateness of initiation and continuation of PPI prescriptions was evaluated using the applicable guidelines.
RESULTS
In total, 148 926 patients (aged ≥18 years) from 27 general practices were evaluated. A total of 23 601 (16%) patients started PPI therapy (mean age 57 [SD 17] years, 59% female). Valid PPI indications at initiation were seen in 10 466 PPI users (44%). Predictors for inappropriately initiated PPI use were older age (odds ratio [OR] 1.03, 95% confidence interval [CI] = 1.03 to 1.03), and use of non-selective non-steroidal anti-inflammatory drugs (OR 5.15, 95% CI = 4.70 to 5.65), adenosine diphosphate receptor inhibitors (OR 5.07, 95% CI = 3.46 to 7.41), COX-2 inhibitors (also known as coxibs) (OR 3.93, 95% CI = 2.92 to 5.28), and low-dose aspirin (OR 3.83, 95% CI = 3.07 to 4.77). Despite an initial valid indication, PPI use was inaccurately continued in 32% of patients on short-course therapy for dyspepsia and in 11% of patients on ulcer prophylaxis.
CONCLUSION
More than half of PPI users in primary care were found to have an inappropriate indication, with unnecessary ulcer prophylaxis related to drug use being one of the leading causes. Future initiatives to reduce PPI use for unnecessary ulcer prophylaxis and timely deprescription if PPI is no longer indicated, are needed.
Topics: Humans; Female; Adolescent; Adult; Middle Aged; Male; Proton Pump Inhibitors; Ulcer; Anti-Inflammatory Agents, Non-Steroidal; Aspirin; Primary Health Care
PubMed: 36127156
DOI: 10.3399/BJGP.2022.0178 -
Natural Product Research Jun 2021The present study aimed to detect the bioactive metabolites from aerial parts which are responsible for the antiulcer activity of the total ethanol extract (TEE) as...
The present study aimed to detect the bioactive metabolites from aerial parts which are responsible for the antiulcer activity of the total ethanol extract (TEE) as well as different fractions (petroleum ether, dichloromethane, ethyl acetate and aqueous). Six flavonoids were isolated from the dichloromethane fraction which was the most potent; with an ulcer index value of 2.67 ± 2.18*** and % inhibition of ulcer of 97.7%; following a bioassay-guided fractionation. The isolated flavonoids were subjected to molecular docking analysis in an attempt to explain their significant antiulcer potential, and the results revealed that salvitin followed by sideritiflavone were the main active ones acting against M3 and H-2 receptors, respectively. Moreover, a molecular dynamics simulation illustrated the formation of two persistent H-bonds between salvitin and the two amino acids of the active site (Asn507 and Asp147) formed in 42 and 65% of the frames, respectively.
Topics: Acetates; Anti-Ulcer Agents; Catalytic Domain; Ethanol; Flavonoids; Molecular Docking Simulation; Molecular Dynamics Simulation; Ocimum; Phytochemicals; Plant Extracts; Solvents; Toxicity Tests, Acute; Ulcer
PubMed: 31359776
DOI: 10.1080/14786419.2019.1645662 -
Journal of Ethnopharmacology Mar 2021Malvaviscus arboreus is traditionally used in Mexico and Central America for culinary and medicinal purposes. Leaves and flowers of this species are commonly used for...
ETHNOPHARMACOLOGICAL RELEVANCE
Malvaviscus arboreus is traditionally used in Mexico and Central America for culinary and medicinal purposes. Leaves and flowers of this species are commonly used for preparation of salads, herbal teas and herbal dyes. Panamanian, Guatemalan and Mexican healers use this medicinal plant for the management of fever, respiratory complications, dysentery, liver and gallbladder problems, stomachache and gastritis between other health troubles.
AIM OF THE STUDY
Considering the traditional use of M. arboreous as well as its content in flavonoids and other polyphenols, the objective of this work was to evaluate the gastroprotective effect of an aqueous extract and identify the potential bio-active principles from flowers of this species.
MATERIAL AND METHODS
Fresh flowers of Malvaviscus arboreus were collected, dried, and macerated with water. The aqueous extract (ExAq) was partitioned using an immiscible mixture of water and ethyl acetate, giving an aqueous (MaAq) and organic (MaEA) fractions. The gastroprotective effect was carried out using an ethanol-induced gastric ulcer experimental test in male rats. While tween 20 was used as a negative control, famotidine (10 mg/kg) and L-arginine (300 mg/kg) were used as positive controls. Compounds 1 and 2 were isolated by several chromatographic techniques and the chemical characterization was carried out by means of the analysis of the NMR spectra in one and two dimensions.
RESULTS
The integrate extract (ExAq) to 250, 500 and 750 mg/kg showed gastroprotective effect with high levels of 97.8%, 79.5% and 91.1% respectively. The organic fraction (MaEA) displayed a protection of 91.2%, 96.0% and 99.4% when it was evaluated at 125, 250 and 500 mg/kg respectively. Comparison of these results with famotidine at 10 mg/kg (83% of gastroprotection) indicated that ethyl acetate fraction showed a better gastroprotection. The bio-guided separation of this organic mixture, allowed obtaining the most active fraction (C1F4, 60 mg/kg) which was finally purified to obtain two glycosylated flavonols: kaempferol 3-O-D-sophoroside (1) and kaempferol 3-O-D-sambubioside (2). This mixture of flavonoids (40 y 60 mg/kg) showed 93.7 and 92% of gastroprotective activity respectively.
CONCLUSION
This study allowed demonstrating that an aqueous extract and its organic fraction (MaEA) from M. arboreous contain glycosylated flavonoids (1 and 2) which are responsible of the gastroprotective properties of M. arboreous. These results will be used in the future development of a standardized treatment useful in the therapeutic management of gastric ulcers.
Topics: Animals; Anti-Ulcer Agents; Dose-Response Relationship, Drug; Ethanol; Gastrointestinal Agents; Glycosides; Kaempferols; Male; Malva; Plant Extracts; Random Allocation; Rats; Rats, Sprague-Dawley; Stomach Ulcer
PubMed: 33253829
DOI: 10.1016/j.jep.2020.113633 -
Clinical and Translational Science Jul 2020Ranitidine has been the topic of recent media reports. Current findings, confirmed by the US Food and Drug Administration, indicate that some ranitidine products contain...
Ranitidine has been the topic of recent media reports. Current findings, confirmed by the US Food and Drug Administration, indicate that some ranitidine products contain a substance that may be carcinogenic. Providers and patients require additional information on the risks of continuing therapy vs. the benefits of the medication. This article comments on what is currently known about the evolving situation of elevated N-nitrosodimethylamine levels in ranitidine and the limits of the existing information to assess best practices.
Topics: Carcinogenesis; Dimethylnitrosamine; Drug Contamination; Drug Recalls; Drug Stability; Gastroesophageal Reflux; Humans; Information Dissemination; Mass Media; Neoplasms; Ranitidine; United States; United States Food and Drug Administration
PubMed: 32107850
DOI: 10.1111/cts.12753