Phytochemical Estimation and Therapeutic Amelioration of Aesculus hippocastanum L. Seeds Ethanolic Extract in Gastric Ulcer in Rats Possibly by Inhibiting Prostaglandin Synthesis / 中国结合医学杂志

OBJECTIVE@#To quantify phytochemicals using liquid chromatography and mass spectroscopy (LCMS) analysis and explore the therapeutic effect of Aesculus hippocastanum L. (AH) seeds ethanolic extract against gastric ulcers in rats.@*METHODS@#Preliminary phytochemical testing and LCMS analysis were performed according to standard methods. For treatment, the animals were divided into 7 groups including normal control, ulcer control, self-healing, AH seeds low and high doses, ranitidine and per se groups. Rats were orally administered with 10 mg/kg of indomethacin, excluding the normal control group (which received 1% carboxy methyl cellulose) and the per se group (received 200 mg/kg AH seeds extract). The test group rats were then given 2 doses of AH seeds extract (100 and 200 mg/kg, respectively), while the standard group was given ranitidine (50 mg/kg). On the 11th day, rats in all groups were sacrificed, and their stomach was isolated to calculate the ulcer index, and other parameters such as blood prostaglandin (PGE2), tissue superoxide dismutase (SOD), catalase (CAT), malonyldialdehyde (MDA), and glutathione (GSH). All isolated stomach tissues were analyzed for histopathological findings.@*RESULTS@#The phytochemical examination shows that the AH seeds contain alkaloids, flavonoids, saponins, phenolic components, and glycosides. LCMS analysis confirms the presence of quercetin and rutin. The AH seeds extract showed significant improvement in gastric mucosa conditions after indomethacin-induced gastric lesions (P<0.01). Further marked improvement in blood PGE2 and antioxidant enzymes, SOD, CAT, MDA and GSH, were observed compared with self-healing and untreated ulcer-induced groups (P<0.01). Histopathology results confirmed that AH seeds extract improved the mucosal layer and gastric epithelial membrane in treated groups compared to untreated ulcer-induced groups.@*CONCLUSIONS@#LCMS report confirms the presence of quercetin and rutin in AH seeds ethanolic extract. The therapeutic effect of AH seeds extract against indomethacin-induced ulcer in rat model indicated the regenerated membrane integrity, with improved cellular functions and mucus thickness. Further, improved antioxidant enzyme level would help to reduce PGE2 biosynthesis.

Gastroprotective potential and mechanisms of action of Hedera nepalensis

Abstract Hedera nepalensis (H. nepalensis) , belonging to the family Araliaceae, is a medicinal plant traditionally used to treat stomach problems. The current study investigated the gastroprotective potential and the mechanism of action of H. nepalensis in diclofenac-and ethanol-induced ulcer models. Anti-oxidant and lipid peroxidation inhibitory prospects of H. nepalensis were checked out by free radical scavenging assay and UV spectrophotometer respectively. Effect of H. nepalensis on the pH, gastric total acidity of gastric juice and protective effects of H. nepalensis against ulcer models have been examined. Histopathological studies have been carried out. The aqueous methanol extract of H. nepalensis (100 µg/mL) showed anti-oxidant (83.55%) and lipid peroxidation inhibitory (70.88%) potential at 1000 µg/mL; the extract had no buffer potential. The extract (400 mg/kg) significantly (81.12% and 63.46%) showed gastroprotective effect in diclofenac and ethanol-induced rat ulcer models respectively. Histopathological studies confirmed the biochemical findings. FTIR analysis showed the presence of carboxylic acid, alkanes, conjugated alkanes, aldehydes and alkyl-aryl ethers. Gallic acid, M-coumaric acid and quercetin were found by HPLC analysis. H. nepalensis exhibited significant protection against diclofenac and ethanol induced gastric damage by anti-oxidant and lipid peroxidation suppression effects suggesting potential broad utility in treatment of diseases characterized with gastric damage.

Gastroprotective herbs for headache management in Persian medicine: A comprehensive review / 中西医结合学报

The gut-brain axis is a bidirectional communication system that exists between the brain and gut. Several studies claimed that some types of headaches are associated with various gastrointestinal (GI) disorders. In Persian medicine (PM), physicians believed that gastric disturbances could stimulate headache and introduced some herbs for boosting gastric function as a therapeutic remedy for headache. Here we review the current evidence for the gastroprotective and antiheadache effects of herbs used in PM. Herbs used for their gastrotonic effects in PM were identified from selected Persian medical and pharmaceutical textbooks. PubMed, Scopus and Google Scholar were used to search for contemporary scientific evidence relating to the gastric and neurologic effects of these plants. A total of 24 plants were recorded from the selected sources included in this review, most of which belonged to the Rosaceae family. Phyllanthus emblica, Zingiber officinale, Boswellias errata, Punica granatum and Hypericum perforatum had the most recent studies related to GI disorder and headache, while current research about quince, rose, apple, hawthorn and pear was limited. Reducing Helicobacter pylori growth, gastritis, erosion of the stomach lining, hemorrhage and perforation, improving gastric mucosal resistance, antisecretary, antiulcer, antipyretic, analgesic, sedative, anxiolytic, anti-inflammatory, anticonvulsant, neuroprotective and antioxidant effects as well as improvement in memory scores were some of the gastrotonic and neuroprotective mechanisms described in the current research. These results confirmed that medicinal plants prescribed in PM may improve headache in patients through the management of GI abnormalities. However, further studies are recommended to investigate the efficacy and safety of the mentioned medicinal plants.

Phytochemical profile and gastroprotective potential of Myrcianthes pungens fruits and leaves

BACKGROUND: The last decade has been marked by increasing data regarding gastroinstestinal diseases, specially gastritis and ulcer. In order to prevent or treat these diseases, many studies have demonstrated the potential of medicinal plants. The aim of this study was to evaluate the phytochemical profile and the gastroprotective activity of the methanolic extract of Myrcianthes pungens whole fruit, peel, pulp, seeds, and leaves. METHODS: The methanolic extracts were analyzed by thin layer chromatography (TLC) to detect the presence of phenolic compounds by direct comparison with an authentic sample. To evaluate the gastroprotective activity, two experimental models were used: acute ulcer model induced by ethanol/HCl and acute ulcer model induced by nonsteroidal anti-inflammatory drug (indomethacin). Animals were divided in different groups (n= 6) and pretreated orally with the methanolic extracts of M. pungens at doses of 50, 125, and 250 mg/kg, the positive control (cimetidine 100 mg/kg) and negative control (distilled water).RESULTS: The TLC analysis indicated the presence of the flavonoids quercetin and quercitrin in the leaves, quercetinin the peel, and catechin and epicatechin in the leaves and seeds of M. pungens. The extracts of leaves, peel, and pulp showed significant gastroprotective potential regarding the relative area of the lesion observed only in acute ulcer model induced by ethanol. The extracts of whole fruit, peel, pulp, seeds, and leaves showed significant gastroprotective potential observed in acute ulcer induced by indomethacin model. CONCLUSIONS: The gastroprotective activity can be related with the presence of some phenolic compounds identified in phytochemical analysis.

Himatanthus drasticus: a chemical and pharmacological review of this medicinal species, commonly found in the Brazilian Northeastern region

ABSTRACT In order to compile the empirical use, as well as the chemical, pharmacological and biological aspects of Himatanthus drasticus (Mart.) Plumel, Apocynaceae, a review was carried out by searching PubMed, Google Scholar, Scientific Electronic Online Library, Web of Science, Science Direct, Scopus and Cochrane. For that, works in English, Spanish and Portuguese, preclinical studies and revisions, addressing chemical, pharmacological, biological properties and popular uses, from 1994 to 2017, were used. The therapeutic potential of the "milk-of-janaguba" (a mixture of the latex with water) became widely known for the treatment of neoplasias, mainly lung and lymphatic cancer types, in the 1970s. The available literature presents works related to the anti-inflammatory, antinociceptive, antitumor and gastroprotective properties of the latex from bark and leaves of H. drasticus. In addition, this review presents some of our own results with the triterpene-rich fraction from H. drasticus, attempting to clarify its action mechanisms at the molecular level. The antinociceptive and anti-inflammatory activities of H. drasticus are probably associated with inhibitions of inflammatory mediators, as TNF-alpha, iNOS, COX-2 and NF-kB. Most importantly, a triterpene-rich fraction also inhibited HDAC activity, and compounds with this activity have been considered as therapeutic agents with antitumor activity. In conclusion, although the literature shows several works on species of the Himatanthus genus, including H. drasticus, dealing with some bioactive compounds as triterpenes, translational studies focusing upon the clinical uses of this medicinal species are still in great need.

Prescribing Pattern and Safety Analysis of Nonsteroidal Anti-inflammatory Drug and Gastro- Protective Agent following Reimbursement Guidelines Relaxation

OBJECTIVE: The prevalence rate of osteoarthritis in Koreans aged 50 years or older is 14.3%, and the total amount of medical costs is more than KRW 1 trillion. Recently, the reimbursement guidelines for osteoarthritis treatment have changed. METHODS: In this study, we sought to describe prescription patterns of nonsteroidal anti-inflammatory drugs (NSAIDs) and gastro-protective agent (GPA) and analyze the clinical and economic impacts of the new policy using the national health insurance claims data. The incidence of upper gastrointestinal adverse event by policy change was identified through the odds ratio, and changes in medicine and medical costs related to osteoarthritis through mean and median. RESULTS: There were 204,552 patients before the reimbursement guidelines relaxation and 239,710 after it, a 17.2% rise. The prescription ratio was 3.3% for the patients prescribed with COX-2 selective NSAIDs alone and 1.3% for those with both COX-2 selective NSAIDs and GPA combination before the reimbursement guidelines relaxation. The reimbursement guidelines relaxation significantly increased their ratios to 6.9% and 2.8%, respectively. Gastrointestinal adverse events significantly reduced by 1.21%p after reimbursement guidelines relaxation. The average medicine cost per person increased significantly to KRW 140,291 from KRW 137,323 after the reimbursement guidelines relaxation, while the average medical cost per person slightly decreased from KRW 311,605 to KRW 310,755 after the relaxation, showing no meaningful difference. CONCLUSION: The reimbursement guidelines relaxation may influence on decreasing the upper gastrointestinal adverse event, increasing the medicine costs and maintaining the medical costs for osteoarthritis.

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam. ) Pers

ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.

Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonian Eunicella singularis

Objective: To explore anti-inflammatory activities of organic extract and its semi-purified fractions (ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis. Methods: The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature. Results: The fraction F-EtOH showed an important anti-inflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols. Conclusions: These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonian Eunicella singularis

OBJECTIVE@#To explore anti-inflammatory activities of organic extract and its semi-purified fractions (ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis.@*METHODS@#The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature.@*RESULTS@#The fraction F-EtOH showed an important anti-inflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols.@*CONCLUSIONS@#These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonianEunicella singularis

Objective:To explore anti-inflammatory activities of organic extract and its semi-purified fractions (ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis.Methods:The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature.Results: The fraction F-EtOH showed an important anti-inflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols.Conclusions: These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

Gastroprotective effects of combination of hot water extracts of turmeric (Curcuma domestica L.), cardamom pods (Ammomum compactum S.) and sembung leaf (Blumea balsamifera DC.) against aspirin-induced gastric ulcer model in rats

<p><b>OBJECTIVE</b>To investigate the protective effect of the combination of turmeric (Curcuma domestica), cardamom pods (Amomum compactum) and sembung leaf (Blumea balsamifera) on gastric mucosa in aspirin-induced gastric ulcer model rats.</p><p><b>METHODS</b>Thirty male Wistar rats weighing 150-200 g were divided into 6 groups. Four groups were administered with the hot water extracts combination consisted of cardamom pods 36.6 mg/200 g body weight and sembung leaf 91.5 mg/200 g body weight (fixed doses). The herbal extracts combination were also consisted of turmeric in various doses i.e. 10 mg/200 g body weight in the second group, 30 mg/200 g body weight in the first and third groups, and 50 mg/200 g body weight in the fourth group. The fifth group rats received sucralfate 72 mg /200 g body weight. Ten minutes after receiving herbal extracts combinations or sucralfate, the rats were induced with aspirin 90 mg/200 g body weight except the first group. Another group (sixth group) only received aspirin without any protective agent. All treatments were adsministered orally for seven days. The number and area of the gastric ulcers were counted and measured macroscopically. Score of mucosal damage and the number of eosinophils as well as the number of mast cells were observed in paraffin sections stained with hematoxylin eosin and toluidine blue, respectively.</p><p><b>RESULTS</b>The groups receiving herbal infuse combination exhibited less number and smaller area of gastric ulcers as well as smaller score of mucosal damage in comparison to those of aspirin group (P<0.05). The number of mast cells and eosinophil of herbal groups were also smaller than that of aspirin group.</p><p><b>CONCLUSIONS</b>The herbal extracts combination of turmeric (Curcuma domestica), cardamom pods (Amomum compactum) and sembung leaf (Blumea balsamifera) has potential gastroprotective effects.</p>

Gastroprotective effects of combination of hot water extracts of turmeric (Curcuma domestica L.), cardamom pods (Ammomum compactum S.) and sembung leaf (Blumea balsamifera DC.) against aspirin-induced gastric ulcer model in rats

Objective: To investigate the protective effect of the combination of turmeric (Curcuma domestica), cardamom pods (Amomum compactum) and sembung leaf (Blumea balsamifera) on gastric mucosa in aspirin-induced gastric ulcer model rats.Methods:were administered with the hot water extracts combination consisted of cardamom pods 36.6 mg/200 g body weight and sembung leaf 91.5 mg/200 g body weight (fixed doses). The herbal extracts combination were also consisted of turmeric in various doses i.e. 10 mg/200 g body weight in the second group, 30 mg/200 g body weight in the first and third groups, and 50 mg/200 g body weight in the fourth group. The fifth group rats received sucralfate 72 mg /200 g body weight. Ten minutes after receiving herbal extracts combinations or sucralfate, the rats were induced with aspirin 90 mg/200 g body weight except the first group. Another group (sixth group) only received aspirin without any protective agent. All treatments were adsministered orally for seven days. The number and area of the gastric ulcers were counted and measured macroscopically. Score of mucosal damage and the number of eosinophils as well as the number of mast cells were observed in paraffin sections stained with hematoxylin eosin and toluidine blue, respectively.Results:Thirty male Wistar rats weighing 150-200 g were divided into 6 groups. Four groups of gastric ulcers as well as smaller score of mucosal damage in comparison to those of aspirin group (P<0.05). The number of mast cells and eosinophil of herbal groups were also smaller than that of aspirin group.Conclusions:The herbal extracts combination of turmeric (Curcuma domestica), cardamom pods The groups receiving herbal infuse combination exhibited less number and smaller area (Amomum compactum) and sembung leaf (Blumea balsamifera) has potential gastroprotective effects.

Consumo de antiinflamatorios no esteroideos en pacientes que concurren por primera vez a un servicio de reumatología / Consumption of nonsteroidal anti-inflammaroty drug in patients attending for the first time a rehumatologic Unit

Introducción: El uso de antiinflamatorios no esteroideos (AINES) conlleva una mayor probabilidad de enfermedad gastrointestinal y cardiovascular en pacientes con factores de riesgo. Por tal motivo, se desarrollaron diversas recomendaciones con el fin de prevenir dichas complicaciones. Objetivo: Evaluar la frecuencia del consumo de AINES al momento de consultar por primera vez a un Servicio de Reumatología de demanda espontánea; y analizar tanto la conducta del médico así como el correcto cumplimiento de las recomendaciones para la toma de estos fármacos al finalizar la consulta. Material y métodos: Estudio observacional de corte transversal. Resultados: Se incluyeron 304 pacientes, 59,5% consumían AINES. La mayoría de estos pacientes presentaban riesgo gastrointestinal moderado/alto, sólo 28,3% recibían adecuada protección. De aquellos pacientes que recibían AINES, se consideró que requerían dicho tratamiento el 50%. Al finalizar la consulta, se tomó una conducta correcta en el 89% de los casos en relación al riesgo gastrointestinal. Conclusión: Más de la mitad de los pacientes consumían AINES. Se observó un buen cumplimiento de las recomendaciones por los médicos tratantes al finalizar la primera consulta. Sin embargo, es importante mencionar que el uso indiscriminado de AINES tanto por parte de los pacientes como por parte de los médicos sigue siendo alto.

Introduction: The use of Non-Steroidal Anti-Inflammatory DrugsNSAID (NSAIDS) leads to a higher probability of gastrointestinaland cardiovascular disease in patients with risk factors. Therefore,a number of recommendations were developed to prevent thesecomplications. The aim of this study was to evaluate the intake frequencyof NSAID by patients who attend to a rheumatology departmentfor the first time; and to analyze the attending physicians´ prescriptionas well as the correct implementation of the recommendationsfor the use of these drugs once this first visit was ended.Methods: We perform a cross-sectional observational study.Results: Three hundred and four patients were included, 59.5%were taking NSAIDs. Most of these patients had moderate/high gastrointestinalrisk and only 28.3% received adequate protection. Ofpatients receiving NSAIDs, it was considered that only 50% requiredsuch treatment. At the end of the first visit, the attending physiciansmade the correct implementation of the recommendations in 89%of cases in regard to gastrointestinal risk.Conclusion: More than half of the patients were taking NSAIDS.A good compliance with the recommendations by the attendingphysicians at the end of the first visit was observed. However, it isnoteworthy that the indiscriminate use of NSAIDs, both by patientsand by physicians, remains high.

Gastroprotective Activity of Methanol Leaves Extract of Barleria prionitis Linn. on Ethanol and Indomethacin Induced Ulcer in Rats.

Aims: Barleria prionitis L. (Family Acanthaceae) is a medicinal plant found road side in India and whole plant or its various parts like leaves, root, bark, stem and flowers are used traditionally for various treatments like toothache, inflammation, boils, glandular swellings and ulcer. Leaf juice is useful in gastric ulcer. Here, we attempt to prove the use of this plant as gastroprotective agent. Study Design: This study was conducted to evaluate the antiulcer activity of methanol extract obtained from the leaves of Barleria prionitis Linn. Place and Duration of Study: The experiments were conducted at Pharmacology lab of Institute of Pharmaceutical Sciences, Kurukshetra University during the period of July 2012 to December 2012. Material and Methods: Antiulcer activity was performed using the protocols of ulcer induced by ethanol and indomethacin at two different doses (250 and 500mg/kg). Parameters like volume of gastric juice, pH, free acidity, total acidity, aspartate amino transferase (AST) and alanine amino transferase (ALT) were also determined in ethanol induced ulcer model. Results: The reduction in ulcer index in Barleria prionitis treated animals was found to be statistically significant (P=.05), when compared with control groups in both the models. Significant changes were observed in total acidity only at dose 500mg/kg only and changes were significant in AST, ALT levels at both the doses. Other parameters showed non-significant results. Conclusion: The results of the present study show that the methanolic extract of Barleria prionitis L. possess antiulcer activity. This work supports the traditional use of this plant in treating gastric ulcer.

Drug utilization study of co-administration of nonsteroidal anti-inflammatory drugs and gastroprotective agents in an orthopaedics outpatients department of a tertiary care hospital in West Bengal.

Background: Non steroidal anti-inflammatory drugs (NSAIDs) are the commonly prescribed analgesic in the orthopaedics department. NSAIDs are prescribed for a long period in both acute condition (like fracture of bones, muscle injury, postoperative procedures etc) or chronic conditions (osteoarthritis etc). However, they have many adverse effects, especially gastrointestinal toxicity when use regularly. For this reason NSAIDs are frequently co-prescribed with gastro protective agents. Common gastroprotective agents are proton pump inhibitors (PPI), H2 blockers, sucralfate, antacids and misoprostol (prostaglandin analogue). Methods: A cross-sectional, unicentric drug utilization study was conducted. Prescriptions were collected from patients attending the orthopaedic outpatients department. The prescription pattern of NSAIDs, gastroprotective agents or co-administration of NSAIDS and gastroprotective agents were analyzed. Results: A total of 977 prescriptions were studied; in which 928 prescriptions contained NSAIDs with gastroprotective agents (97.92%). The most common gastroprotective agents combined with NSAIDs was H2 receptor blockers (60.56%), followed by proton pump inhibitors (PPIs) (21.65%), while antacids are prescribed least (17.78%). Misoprostol or sucralfate were not used at all. Conclusions: NSAIDs are commonly co-prescribed with gastroprotective agents in high percentage.

Gastroprotective effect of Desmodium gangeticum roots on gastric ulcer mouse models

In the present study, the ethanolic root extract of Desmodium gangeticum (L.) DC., Fabaceae, (EDG), have been studied in various acute and chronic ulcer mouse models. Oral administration of root extract, significantly decrease the ulcer index and lesion number in a dose dependent manner against ethanol induced acute gastric ulcer in mice. In gastric ulcerated animal that received high dose of 150 mg/kg EDG, the mucosa showed no ulceration with slight focal congestion and the glands appeared normal. Pylorus ligated mice, pretreated with EDG showed significant decrease in ulcerous activity under chronic condition. The highest dose (150 mg/kg) of the extract provoked a marked increase in protein and glutathione levels, when compare to control. Furthermore, gastric juice, free acidity and total acid output were inhibited in a dose-dependent manner at p<0.05 level. Our results indicate that the EDG possess gastroprotective activity and increasing regeneration of damaged gastric mucosa and thus safe for human use.

Antiulcer effect of epoxy-carvone

Epoxy-carvone is a monoterpene present in essential oils of various plants. It is a derivative of carvone, which has an epoxy group instead of the α- and β-unsaturated ketone group present in carvone. As recent studies have shown that several alcohol terpenes and compounds containing α, β-unsaturated ketone groups present antiulcer effect, the main of the present study was to evaluate the antiulcer effect of epoxy-carvone. The models of ulcers induced by ethanol and indomethacin were used in this study. Epoxy-carvone at the dose of 1 mg/kg did not present antiulcer effect against ulcer induced by ethanol, but at the doses of 10, 30 and 50 mg/kg it presented gastroprotective effect in both ulcer models. Epoxy-carvone also did not affect the gastric secretion in the pylorus ligation test. Moreover, pretreatment with indomethacin or L-nitroarginine methyl ester did not reverse the gastroprotection produced by this monoterpene. This study showed that epoxy-carvone presents antiulcer effect and suggests that this effect does not involve either antisecretory activity or increase of the nitric oxide and prostaglandin synthesis.

Gastroprotective Effects of Ascaridole on Gastric Ulcer in Rats / 中草药·英文版

ObjectiveTo evaluate the gastroprotective activity of ascaridole.MethodsThe gastroprotective effect of ascaridole was evaluated on ulcer healing in rats with acetic acid-induced chronic gastric ulcer,pylorus ligation- and Aspirininduced gastric ulcer.Ascaridole was ig administered with the dosages of 10 and 20 mg/kg once daily for 7 d.Results Ascaridole showed the significant anti-ulcer effects.In acetic acid-induced gastric ulcer rats,the ulcer areas after 10 and 20 mg/kg of ascaridole treatment were (65.1 ± 20.0) and (50.6 ± 11.0) mm2,respectively,which were significant lower (P ＜ 0.01) than that of the control group [(116.7 ± 35.8) mm2].For pylorus ligation model,ascaridole showed a gastric ulcer healing effect in a dose-dependent manner.Ascaridole at the dose of 20 mg/kg showed 50％ ulcer protection and had a significant (P ＜ 0.05) gastroprotective activity since it decreased the total acidity and pepsin activity.Compared to the control group,the two dosages of ascaridole showed the significant reduction (P ＜ 0.05) in the ulcer index on Aspirin-induced ulcer.ConclusionThis study provides evidence that ascaridole shows potential efficacy on the healing of gastric ulcers induced by acetic acid,Aspirin,and pylorus ligation.

The Pattern of Use of Oral NSAIDs with or without Co-prescription of Gastroprotective Agent for Arthritic Knee by Korean Practitioners

PURPOSE: The aim of this study was to describe the patterns of use of non-steroidal anti-inflammatory drugs (NSAIDs) for arthritic knees in clinical practice, particularly focusing on the co-prescription of gastroprotective agents for patients with risk factors for adverse gastrointestinal (GI) events. MATERIALS AND METHODS: Each cross-sectional cohort was a group of outpatients visiting 111 physicians who had prescribed NSAIDs for the patients' arthritic knees for more than three consecutive months. A self-administered questionnaire was completed by each patient and physician. RESULTS: Nine hundred and forty five patients (48%) of the whole 1,960 patients belonged to the group with a high or very high risk for NSAID-induced gastropathy determined by northern California Health Maintenance Organization guidelines. Overall, only less than half of the patients were given co-prescription of gastroprotective agents, regardless of the presence or absence of GI symptoms and irrespective of the level of risk for NSAID-induced gastropathy. CONCLUSIONS: The physician prescribing NSAIDs for arthritic knees should monitor any GI symptoms and the patient monitor anylevel for NSAIDinduced gastropathy, and be willing to add gastroprotective agents as necessary in order to prevent serious adverse GI events.

Anti-inflammatory, antioedema and gastroprotective activities of aristotelia chilensis extracts, part 2

Context: “Chilean black-berry” Aristotelia chilensis is a wild fruit that grows in Southern Chile. This fruit possesses a strong antioxidant activity and is commonly used in foods and beverages in Chile. Objective: The gastroprotective and anti-inflammatory activities of the extracts, fractions and subfractions as carrageenan – induced paw oedema in rats are reported here for the first time. Materials and methods: Extracts, fractions, subfractions and several compounds werer used for measuring the effects in carrageenan-induced paw oedema inflammation of rat model and the gastroprotective activity was analyzed. Results: The results showed that extract B, fraction F-4, and ovatofolin, quercetin, myricetin, luteolin and diosmetin used as pattern compounds were the most active samples together with those subfractions rich in aglycone and phenolic compounds. Thus, SF11-SF15, SF16-SF20, and SF21-SF25 showed the best subfractions inhibitors in similar form to indomethacin, a known selective COX inhibitor. Results demonstrated that these samples strongly inhibited the carrageenan-induced inflammation in paw of the rat oedema model. Discussion and conclusion: These findings demonstrate that the fruits and their constituents of A. chilensis are anti-inflammatory and gastroprotective and thus have grat potential nutraceuticals.

Contexto: Chilean Black-berry Aristotelia chilensis es un fruto silvestre que crece en el sur de Chile. Este fruto posee uan fuerte actividad antioxidante y comúnmente es usado en alimentos y bebidas en Chile. Objetivo: Se investigó la actividad anti-inflamatoria y gastroprotectora de los extractos, fracciones y subfracciones de este fruto y son informados aquí por primera vez. Materiales y métodos: Los extractos, fracciones y subfracciones fueron analizados por su efecto sobre la inflamación en pata de rata a través de la inducción con carragenina en dosis sencillas. Además se investigó la actividad gastroprotectora sobre la mucosa del estómago de rata. Resultados: Los resultados muestran que el extracto B, la fracción F-3, F4 y ovatifolina, quercetina, myricetina, luteolina y diosmetina que se usaron como muestras patrones, fueron las más activas junto con aquellas subfracciones ricas en compuestos fenólicos. Así SF11-SF15, SF16-SF20, y SF21-SF25 mostraron ser las mejores subfracciones inhibitorias en una forma similar a indometacina en conocido inhibidor selectivo de COX. Los resultados demuestran que estas muestras inhiben fuertemente la inflamación inducida en el modelo del edema de pata de rata. Discusión y conclusión. Estos hallazgos demuestran que los frutos y sus constituyentes de A. chilensis poseen una excelente actividad anti-inflamatoria y gastroprotectora, y así tienen un gran potencial como una fuente de productos naturales saludables. Adicionalmente, estos hallazgos muestran que los flavonoides, ácidos fenólicos y antiocianinas presentes en este fruto podrían ser los responsables de la actividad nutracéutica.