Pylorus ligation-induced hyperacidity: synergistic prophylactic effects of linagliptin and L-arginine via up-regulation of EP4 receptor subtype and improvement of vascular endothelial damage.

Gastric hyperacidity and ulceration are chronic diseases characterized by repeated healing followed by re-exacerbation. The study aims to protect against gastric hyperacidity without interfering with gastric acid secretion. Pylorus ligation-induced hyperacidity is commonly utilized in the induction of gastric ulcers.Forty-two rats were distributed into seven groups (n = 6). Group I comprised sham-operated group. Group II served as pylorus-ligation group. Groups III-VII were given oral Linagliptin (LN; 3 and 6 mg/kg), L-arginine (LA; 150 and 300 mg/kg) and their combination (LN 3 + LA 150 mg/kg), respectively for 7 days. On the 8th day, groups II-VII were subjected to pylorus-ligation.Treatment of pylorus-ligated rats with LN, LA and their combination improved the gastric hyperacidity as exhibited by a marked reduction in the gastric juice volume, total and free acidities and pepsin contents with a noticeable increase in pH. Pre-treatment with LN, LA and their combination showed a marked alleviation in the gastric inflammatory indicators evidenced by reduction in the gastric levels of MCP-1and Il-1ß as well as elevation of eNOS levels versus the sham-operated group. A marked up-regulation in the gastric gene expression of PGE, EP4 and VEGF accompanied by an improvement of the histopathologic pictures/scores, and TNF-α and caspase-3 immuno-staining were also recorded.By estimating the combination-index, it can be concluded that combining LN with LA exhibited prophylactic synergistic effects in ameliorating pylorus ligated-induced hyperacidity, mainly via up-regulation of EP4 receptor and improvement of vascular endothelial damage through VEGF expression in gastric mucosa.

Gastroprotective Activities of Aqueous and 80% Methanol Leaf Extracts of Stephania abyssinica (Quart.-Dill. and A. Rich.) Walp. (Menispermaceae) in Rats.

Background: An ethnobotanical study showed that the leaf of Stephania abyssinica (S. abyssinica) is used for the treatment of gastritis, but there is no scientific investigation. Objective: The aim of this study was to evaluate the gastroprotective activities of both aqueous and 80% methanol leaf extracts of S. abyssinica in experimental rats. Methods: Decoction and maceration techniques were used to prepare aqueous and 80% methanol leaf extracts, respectively. The extracts were evaluated against pyloric ligation, indomethacin, and ethanol-induced gastric ulcer models at doses of 100, 200, and 400 mg/kg. Negative control received 2% tween 80, while positive controls received 20 mg/kg of omeprazole and 100 µg/kg of misoprostol. Parameters, such as ulcer index, gastric mucin content, gastric juice volume, pH, and free and total acidity were measured. Results: In the pyloric ligation induced gastric ulcer model, all doses of both extracts significantly reduced the ulcer index and gastric juice volume, while doses of 200 and 400 mg/kg exhibited a significant increment in mucus content and gastric juice pH as well as decrease in free and total acidity as compared to negative control. In indomethacin and ethanol induced gastric ulcer models, pretreatment with both extracts significantly reduced the ulcer index and enhanced gastric mucin content in a dose-dependent manner. Phytochemical screening of both extracts showed the existence of flavonoids, phenols, tannins, saponins, alkaloids, and coumarins with high contents of phenols, flavonoids, and alkaloids in 80% methanol extract. Conclusion: This study revealed that aqueous and 80% methanol leaf extracts of S. abyssinica possessed remarkable gastroprotective activities against experimentally induced gastric ulcer models, and this possibly justify the traditional use of S. abyssinica leaves to treat gastritis.

Evaluation of anti-gastric ulcer activity of aqueous and 80% methanol leaf extracts of Urtica simensis in rats.

Background: Gastric ulcer is a major public health problem globally and associated with severe complications including hemorrhages, perforations, gastrointestinal obstruction, and malignancy. Urtica simensis is widely used for traditional management of gastric ulcer in different parts of Ethiopia. The present study was undertaken to evaluate the anti-gastric ulcer activity of aqueous and 80% methanol extracts of U.simensis in rats. Methods: The leaf extracts were prepared using decoction (aqueous) and maceration (80% methanol) techniques and in vivo anti-gastric ulcer effects of various doses of U. simensis extracts and the effect were determined using the pylorus ligation, indomethacin and ethanol induced gastric ulcer models. Results: In pylorus ligation induced gastric ulcer model, both aqueous and 80% methanol extracts at doses of 200 and 400 mg/kg were exhibited significant reduction in total acidity, volume of gastric secretion (p < 0.001) and substansial rise in pH (p˂0.05) of the gastric secretion. In indomethacin induced ulcer model, both aqueous and methanol extracts were exhibited dose dependent increment in gastric wall mucus compared to control (p < 0.001). In ethanol induced ulcer model, all doses of extract produced significant increment in gastric wall mucus from 46.66 ± 0.96 (AQ100) to 75.87 ± 1.52 (ME 400) µg alcian blue/g wet stomach. Five days pre-treatment with 200 mg/kg of both and aqueous and methanolic extracts exhibited significant (P < 0.001) ulcer inhibition in both indomethacin and ethanol-induced ulcer models. Conclusion: Both extracts of U.simensis exhibited a promising anti-gastric ulcer activity in all of the three models and this findings supports for traditional claimed use of the leaf of U. simensis.

Evaluation of mechanism(s) of action underlying the antioxidant and antiulcer activity of Sesamum indicum leaves extract in experimental rats.

OBJECTIVE: The current study aimed to estimate phytochemical screening, in vitro antioxidant activity, and gastroprotective activity of Sesamum indicum Linn ethanolic extract. MATERIALS AND METHODS: The current study was held out by ulceration induced by pylorus ligation and indomethacin-induced ulcer screening models in Wister albino rats. The screening of antiulcer activity of ethanolic extract of S. indicum leaves (EESIL) at the different amounts (100, 200, and 400 mg/kg; per orally for 7 days) was compared with omeprazole as a usual antiulcer drug. Additional parameters such as gastric content, pH, total acidity, pepsin activity ulcer score, free acidity, ulcer index (UI), % inhibition of ulcers, mean mucin, pepsin content, and total protein content were observed. RESULTS: In the pylorus ligation model, the pepsin activity free acidity, pepsin content, UI, total acidity, ulcer score, total protein content, and percentage ulcer inhibition were considerably decreased (P < 0.05 and P < 0.01), and mean mucin and gastric content pH extensively elevated (P < 0.05 and P < 0.01) in EESIL tested groups in the comparison of the control group. Doses (100, 200, and 400 mg/kg p.o.) of EESIL showed dose-reliant gastro protective outcomes, a considerable (P < 0.05 and P < 0.01) decrease in gastric parameters as UI and ulcer score and induction in gastric pH and percentage inhibition of ulcer compared with the control group. CONCLUSION: Antioxidant, anti-Ulcer, EESIL, and EESIL show antioxidant activity at different concentration. The fallout of the study indicated that the EESIL had improved antiulcer potential due to the decrease in offensive factors and increase in defensive factors.

Evaluation of the antiulcerogenic activity of hydromethanol extracts of Solanum incanum L. (Solanaceae) leaves and roots in mice; single and repeated dose study.

OBJECTIVE: The aim of this study was to evaluate the antiulcer activity of hydromethanol extracts of Solanum incanum L. (Solanaceae) leaves and roots in mice. METHODS: The antiulcerogenic activity of the plant extracts were evaluated using Pylorus ligation and ethanol induced gastric ulcers in fasted mice. Data were analyzed using one way ANOVA, and P-values <0.05 were considered statistically significant. RESULTPYLORUS LIGATION-INDUCED ULCER: Single dose and repeated daily dose administration of the leaf and root extracts for 10 days didn't significantly (P > 0.05) affect pH, total acidity and volume of gastric secretion. Single dose of both extracts significantly reduced ulcer score (P = 0.036) and ulcer index (leaf, P = 0.037; root, P = 0.041) at the dose of 400 mg/kg. Similarly, significant reduction in ulcer score was observed after repeated daily treatment with 200 mg/kg (P = 0.030) and 400 mg/kg (P = 0.005) of the leaf extract and 400 mg/kg (P = 0.005) of the root extract. In addition, repeated administration of 400 mg/kg of the leaf (P = 0.004) and root (P = 0.005) extracts significantly reduced ulcer index. ETHANOL-INDUCED ULCER: Single dose of both extracts significantly reduced ulcer score at the dose of 200 mg/kg (leaf, P = 0.017; root, P = 0.036) and 400 mg/kg (leaf, P = 0.001; root, P = 0.001). Similarly, 200 mg/kg (leaf, P = 0.002; root, P = 0.018) and 400 mg/kg (leaf, P = 0.001; root, P = 0.001) of the extracts significantly reduced ulcer index after single dose treatment. Repeated daily treatment with leaf and root extracts for ten days caused a significant (P = 0.037, 0.001 and 0.001 for 100, 200 and 400 mg/kg leaf extract; P = 0.026, 0.018 and 0.001 for 100, 200 and 400 mg/kg root extract, respectively) reduction in ulcer score. In addition, both extracts significantly (P = 0.041, 0.004 and 0.000 for 100, 200 and 400 mg/kg leaf extract; P = 0.038, 0.008 and 0.000 for 100, 200 and 400 mg/kg root extract, respectively) reduced ulcer index after 10 days of treatment. CONCLUSION: This study has revealed hydromethanol extracts of Solanum incanum leaves and roots have antiulcerogenic activity using in vivo models. The antiulcer activity of the plant is not related to acid anti-secretory action, suggesting the plant may have cytoprotective effect on the gastric mucosa.

Evaluation of the Anti-Ulcer Activity of Hydromethanolic Crude Extract and Solvent Fractions of the Root of Rumex nepalensis in Rats.

BACKGROUND: Rumex nepalensis(RN) Spreng has been used to treat ulcer disease in Ethiopian folk medicine. This study aimed to determine the anti-ulcer activity of hydroalcoholic root crude extract and solvent fractions of R. nepalensis in rats. METHODS: The effect of R. nepalensis crude hydromethanolic extract and solvent fractions at doses (100, 200, 400 mg/kg/day) and repeated dosing (200 mg/kg/day for 10 and 20 days) was examined on ulcers in rats in pyloric ligation-, cold restraint stress-, and acetic acid-induced ulcer models. Cimetidine (100 mg/kg/day) and/or Omeprazole (20 mg/kg/day) were used as standard drugs and served as a positive control. Data were analyzed by one-way ANOVA post hoc followed by a Tukey HSD test with SPSS software version 24.0, and P≤ 0.05 was considered as statistically significant. RESULTS: In the pylorus ligation-induced ulcer model, pretreatment with the crude extract significantly reduced the degree of gastric secretions, pH, total acidity, and ulcerations in a dose-dependent manner. Gastroprotection offered by the R. nepalensis 400 mg/kg test extract was comparable to that of the standard. Among fractions, the ethyl acetate fraction at 400 mg/kg had the highest protection of ulcer but the chloroform fraction was ineffective. In the cold restraint stress-induced ulcer model, R. nepalensis at 200 and 400 mg/kg reduced the lesion index significantly (P<0.01). With relevant chronic ulcer model treatment, a dose of R. nepalensis at 200 and 400 mg/kg healed ulcers significantly with a curative ratio of 53.22% and 54.59%, respectively. CONCLUSION: From this study, it is concluded that hydromethanolic crude extract and solvent fractions of R. nepalensis root showed promising anti-ulcer activity. This upholds its folkloric use. Thus, it is considered as a possible source to develop a new anti-ulcer agent.

Phytochemical and Antiulcer Activity Screening of Seed Extract of Cordia africana Lam (Boraginaceae) in Pyloric Ligated Rats.

INTRODUCTION: Peptic ulcer disease represents a worldwide health problem because of its high morbidity, mortality and economic loss. It is a very prevalent condition affecting around 10%-15% of the general population worldwide. Most of the available antiulcer drugs are costly and have an incidence of relapse, drug interactions and several side effects upon chronic usage. Hence, the use of herbal medicine may be safe, economical and effective in such cases when drugs are used for long periods. Ethnobotanical reports showed traditional claims on the use of Cordia africana seeds for the treatment of gastric ulcers. However, the safety and efficacy of these remedies are not well known. The aim of this study is, therefore, to evaluate the antiulcer activity and safety of a crude extract of C. africana seeds in animal models. METHODS: Shade-dried seeds of C. africana were extracted by 80% methanol and dried by the rotator evaporator and lyophilized. The crude extract was used to evaluate antiulcer activity in vivo with pylorus ligation method, on Wistar albino rats weighing 230-250g. Preliminary phytochemical screening was performed using a standard procedure. Acute toxicity study was carried out in Swiss albino mice before antiulcer activity tests. RESULTS: No sign of toxicity was observed upon the administration of 2000 mg/kg of the crude extract to mice. Single-dose administration of 400 and 600 mg/kg extract showed a significant reduction in the volume of secretion and acidity of the stomach (p <0.01). The doses 400 and 600 mg/kg have reduced the ulcer score by 83.58% and 88%. CONCLUSION: The result of this study showed that the hydromethanolic crude extract of C. africana has strong antisecretory and ulcer protective activities against ulcers produced by pylorus ligation.

Combined therapy of gabapentin with pantoprazole exhibited better protective action against forestomach and pylorus ligation-induced gastric esophageal reflux disease in albino Wistar rats.

The current study was undertaken to evaluate the effect of combined therapy of gabapentin and pantoprazole against forestomach and pylorus ligation-induced gastric esophageal reflux disease (GERD) in albino Wistar rats. Rats were randomly divided into five groups, each group consisting of six rats, fasted for 24 h, underwent forestomach and pylorus ligation, received normal saline (3 ml/kg, p.o.), normal control, toxic control, pantoprazole (30 mg/kg, p.o.), gabapentin (50 mg/kg, p.o.), or their combination. After 10 h, animals were killed by cervical dislocation and evaluated for pH of gastric content, volume of gastric juice, total acidity, and esophagitis index. Esophageal tissues were further analyzed for biochemical parameters such as superoxide dismutase, glutathione, catalase, thiobarbituric acid reactive substances, and protein carbonyl, and scanning electron microscopy (SEM) and histopathology were used for morphological evaluation. The results show the combination therapy of gabapentin and pantoprazole significantly inhibited the volume of gastric juice and total acidity esophagitis index and significantly increased the pH of gastric juice. Treatment with gabapentin and pantoprazole exhibited maximum antioxidant effect in comparison with monotherapy. Marked protection and restoration of normal morphology was observed through SEM and histopathology in the combination therapy as compared to monotherapy. Finally, it was concluded that combination therapy of pantoprazole and gabapentin has beneficial effect against GERD.

Data of in vivo screening of antiulcer activity for methanolic extract of Vernonia elaeagnifolia DC.

The data present in this article is related to evaluation of standardized methanolic extract of Vernonia elaeagnifolia aerial parts [MEVE], a species of Asteraceae family for antiulcer potential. Antiulcer activity of MEVE (200 and 400 mg/kg, b.w., p.o.) was evaluated with ethanol and aspirin induced ulcer models and pylorus ligation induced gastric ulcer model. The antioxidant potential of MEVE was evaluated with nitric oxide radicals, hydroxyl radical and H2O2 radical scavenging assay against standard ascorbic acid to correlate antioxidant and antiulcerogenic action. MEVE significantly protects the gastric mucosa against the ethanol and aspirin induced ulcer and pylorus ligation induced ulcer challenge. MEVE had shown significant [normal control: p < 0.0001, disease control: p < 0.0001, standard: p < 0.0001] decrease in the ulcer index produced by all three models in rats as compared to the standard drug omeprazole [20 mg/kg, b.w., p.o.]. The present data suggest that aerial parts of Vernonia elaeagnifolia possess significant antiulcer activity, which may attributed to its antioxidant mechanism of action.

Protective roles of Vigna subterranea (Bambara nut) in rats with aspirin-induced gastric mucosal injury.

OBJECTIVE: Vigna subterranea is widely consumed as a traditional staple food in Nigeria and some West African countries. The ethanolic seed extract of V. subterranea (EEVS) was investigated for its gastroprotective effects on aspirin plus pylorus ligation-induced gastric ulcerated rats using an in vivo assay. METHODS: Gastric mucosal ulceration was induced experimentally in Groups 2 to 5 using aspirin plus pylorus ligation. Rats in Group 1 were orally pretreated with 3% Tween 80 only as normal control. Groups 2 to 5 were pretreated with 3% Tween 80 (ulcer group), 20 mg/kg of omeprazole (positive group), and 200 and 400 mg/kg of EEVS (experimental groups), respectively, once daily for 21 days before ulcer induction. Parameters including those for gastric secretions, ulcerated areas and gastric wall histology were assessed. Levels of superoxide dismutase (SOD), glutathione peroxidase (GPX), and malondialdehyde (MDA) in the gastric tissue homogenate were also determined. RESULTS: Pretreatment with EEVS significantly (P < 0.05) reduced the ulcer index, gastric volume and total acidity in rats with aspirin plus pylorus ligation-induced ulcer. The pH and mucus of gastric content increased significantly (P < 0.05) while the levels of SOD and GPX were observed to be elevated with a reduced amount of MDA. Significant severe gastric mucosal injury was exhibited in the ulcer group and EEVS or omeprazole offered significant (P < 0.05) protection against mucosal ulceration. Histologically, the gastric submucosal layer showed remarkable decrease in edema and leucocytes infiltration compared with ulcer group. CONCLUSION: The study suggests that EEVS offered a protective action against aspirin plus pylorus ligation-induced gastric ulcers in Wistar rats. The protective effect might be mediated via antisecretory, cytoprotective and antioxidative mechanisms.

Evaluation of traditional medicinal plant, Cissus setosa Roxb. (Vitaceae) for antiulcer property.

Cissus setosa is an indigenous medicinal herb commonly used for the treatment of gastro ulcers. In the current investigation the aerial methanolic extract of C. setosa was investigated for their antiulcer activity using pylorus ligation and ethanol in experimental rats. The extract was administered at the doses of 200 and 400 mg/kg b.w. orally for 3 days. However, higher dose of the extract subsequently reduced gastric ulcer induced aberrations by pylorus ligation (70.05%) and ethanol (78.16%) as judged by their altered biochemical parameters such as free acidity, total acidity, total carbohydrate, total protein and pepsin activity. Furthermore, macroscopic examination of rat's stomach also showed that the pretreatment with methanolic extract notably lowered the pylorus ligation and ethanol induced ulcers. As perceived in the present study, evidently, our findings basically supports the potency of the methanol extracts of C. setosa to treat gastrointestinal related disorders, thus lends pharmacological credence to the suggested folklore use.

Acid-gastric antisecretory effect of the ethanolic extract from Arctium lappa L. root: role of H+, K+-ATPase, Ca2+ influx and the cholinergic pathway.

BACKGROUND: Arctium lappa L., popularly known as burdock, is a medicinal plant used worldwide. The antiulcer and gastric-acid antisecretory effects of ethanolic extract from roots of Arctium lappa (EET) were already demonstrated. However, the mechanism by which the extract reduces the gastric acid secretion remains unclear. Therefore, this study was designed to evaluate the antisecretory mode of action of EET. MATERIALS AND METHODS: The effects of EET on H+, K+-ATPase activity were verified in vitro, whereas the effects of the extract on cholinergic-, histaminergic- or gastrinergic-acid gastric stimulation were assessed in vivo on stimulated pylorus ligated rats. Moreover, ex vivo contractility studies on gastric muscle strips from rats were also employed. RESULTS: The incubation with EET (1000 µg/ml) partially inhibited H+, K+-ATPase activity, and the intraduodenal administration of EET (10 mg/kg) decreased the volume and acidity of gastric secretion stimulated by bethanechol, histamine, and pentagastrin. EET (100-1000 µg/ml) did not alter the gastric relaxation induced by histamine but decreased acetylcholine-induced contraction in gastric fundus strips. Interestingly, EET also reduced the increase in the gastric muscle tone induced by 40 mM KCl depolarizing solution, as well as the maximum contractile responses evoked by CaCl2 in Ca2+-free depolarizing solution, without impairing the effect of acetylcholine on fundus strips maintained in Ca2+ -free nutritive solution. CONCLUSION: Our results reinforce the gastric antisecretory properties of preparations obtained from Arctium lappa, and indicate that the mechanisms involved in EET antisecretory effects include a moderate reduction of the H+, K+-ATPase activity associated with inhibitory effects on calcium influx and of cholinergic pathways in the stomach muscle.

Protective roles of Vigna subterranea (Bambara nut) in rats with aspirin-induced gastric mucosal injury / 中西医结合学报

<p><b>OBJECTIVE</b>Vigna subterranea is widely consumed as a traditional staple food in Nigeria and some West African countries. The ethanolic seed extract of V. subterranea (EEVS) was investigated for its gastroprotective effects on aspirin plus pylorus ligation-induced gastric ulcerated rats using an in vivo assay.</p><p><b>METHODS</b>Gastric mucosal ulceration was induced experimentally in Groups 2 to 5 using aspirin plus pylorus ligation. Rats in Group 1 were orally pretreated with 3% Tween 80 only as normal control. Groups 2 to 5 were pretreated with 3% Tween 80 (ulcer group), 20 mg/kg of omeprazole (positive group), and 200 and 400 mg/kg of EEVS (experimental groups), respectively, once daily for 21 days before ulcer induction. Parameters including those for gastric secretions, ulcerated areas and gastric wall histology were assessed. Levels of superoxide dismutase (SOD), glutathione peroxidase (GP), and malondialdehyde (MDA) in the gastric tissue homogenate were also determined.</p><p><b>RESULTS</b>Pretreatment with EEVS significantly (P < 0.05) reduced the ulcer index, gastric volume and total acidity in rats with aspirin plus pylorus ligation-induced ulcer. The pH and mucus of gastric content increased significantly (P < 0.05) while the levels of SOD and GP were observed to be elevated with a reduced amount of MDA. Significant severe gastric mucosal injury was exhibited in the ulcer group and EEVS or omeprazole offered significant (P < 0.05) protection against mucosal ulceration. Histologically, the gastric submucosal layer showed remarkable decrease in edema and leucocytes infiltration compared with ulcer group.</p><p><b>CONCLUSION</b>The study suggests that EEVS offered a protective action against aspirin plus pylorus ligation-induced gastric ulcers in Wistar rats. The protective effect might be mediated via antisecretory, cytoprotective and antioxidative mechanisms.</p>

Evaluation of Antiulcer Activity of Peltophorum Pterocarpum.

INTRODUCTION: Peltophorum pterocarpum is a rich source for phenols and the wood, leaves, and flowers of the plant are used as medicinal agents in traditional medicine. Peptic ulcer is a major disease of gastrointestinal tract, affecting nearly 40 lac people each year worldwide and affects 10% of world population with different aetiologies. Peltophorum pterocarpum consists of phenols and flavonoids, tannins which have potential antioxidant and cytoprotective activity. AIM: To evaluate the antiulcer activity of methanolic extract of the leaves of Peltophorum pterocarpum (MEPP) on albino rats. MATERIALS AND METHODS: The rats were divided into four groups as control, standard, test 1 (extract: 100 mg/kg) and test 2 (extract: 200 mg/kg) with six rats in each group. Gastric lesions were induced by oral administration of indomethacin (20 mg/kg) followed by pylorus ligation. Standard group of animals were treated with misoprostol and test group of animals were treated with MEPP at doses of 100 and 200 mg/kg. To determine the antiulcer activity of extract, mean ulcer index, free acidity and total acidity were evaluated. RESULTS: Ulcer index was significantly decreased at p<0.01 in MEPP treated groups as compared to control group. Total and free acidity was significantly decreased at p<0.01 in MEPP treated groups as compared to control group. Histological analysis also supported the gastro protective effect of MEPP treated groups when compared with control groups. CONCLUSION: The study revealed that MEPP exhibited potential antiulcer activity and showed dose dependent antiulcer effect.

Evaluation of Antiulcer and Antioxidant Activity of Barleria gibsoniDalz. Leaves.

BACKGROUND: Peptic ulcer is a digestive disorder most commonly found in clinical practice. Given the many side effects of modern medicine, the initial acquisition of fewer side effects, and medication of indigenous drugs, it should be considered as a better alternative for the treatment of peptic ulcer. OBJECTIVE: To assess antiulcer and antioxidant activity of ethanol extract of Barleria gibsoni (EBG) Dalz. leaves in ulcer-induced rats and in vitro antioxidants method, respectively. MATERIALS AND METHODS: Ethanol EBG was screened for antiulcer activity in pylorus ligation-induced ulcer models in Wistar rats. In vitro antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) radical scavenging activity. Total phenol and flavonoid content in the extracts were determined spectrophotometrically. RESULTS: Oral administration of ethanol extract of leaves at doses of 250, 500 mg/kg p.o. reduced significant gastric lesions induced by pylorus ligation-induced ulcer as compared to standard omeprazole (20 mg/kg p.o.). The IC50 values were found to be 150 µg/mL in leaves extract. The ethanol extracts showed good antioxidant capacity in DPPH radical scavenging assay and NO radical scavenging activity when compared to standard. The total phenolic content using Folin-Ciocalteu reagent estimated in 1 mg of leaves extracts was 368 µg and 481 µg with gallic acid equivalent and also the total flavonoid content found to be 240 and 410 µg, respectively, with quercetin equivalence. CONCLUSION: These findings suggest that the leaves of B. gibsoni possessed antiulcer potential and antioxidant compared to standard. This is the first ever report of antiulcer and antioxidant activities in B. gibsoni (Acanthaceae). SUMMARY: In vivo antiulcer and in vitro antioxidant activity of Barleria gibsoni was evaluated.Soxhelt extraction was carried out and extracts were subjected to qualitative phytochemical analysis. Extract obtained by Soxhlation showed higher total phenolic and flavonoid contents.EBG showed DPPH and Nitric oxide scavenging activity indicating its strong antioxidant potential.On pylorus ligation-accumulated secretions and the related ulcers confirm gastric acid output to be the basic cause of gastric ulcers. Ethanol extract of leaves attenuated the gastric volume, free acidity, total acidity and ulcer index thus showing the anti-secretory mechanism.The results of the histopathological investigation of Barleria gibsoni leaves for antiulcer effects using pylorus ligation induced ulcer model in rats laid credence to traditional use of the plant leaves in ulcer treatment. The ethanol extract of leaves demonstrated increase in percentage preventive index compared to omeprazole respectively. From the present study results reveals the antiulcer activity of ethanol extract leaves which is comparable to that of Omeprazole. Abbreviations Used: EBG: Ethanol extract prepared from the leaves of B. gibsoni, ROS: Reactive Oxygen Species, DPPH: 2, 2-diphenyl-1-picrylhydrazyl, NO: Nitric Oxide, IC50: The half maximal inhibitory concentration, m: mg, DNA: deoxyribonucleic acid, GAE: Gallic acid equivalence, AlCl3: Aluminium chloride.

Antiulcer Activity of Ethanolic Extract of Salvadora indica (W.) Leaves on Albino Rats.

BACKGROUND: Ulcer can be developed inside the inner lining of the stomach (gastric ulcer) or the small intestine (duodenal ulcer). Both the ulcers are also cumulatively referred as peptic ulcers. It affects nearly 10% of world population. AIM: To investigate the antiulcer activity of ethanolic extract of Salvadora indica W. leaves (ESIL) on albino rats. MATERIALS AND METHODS: The present study was carried by pylorus ligation, ethanol and cysteamine induced ulcer models in albino rats. The antiulcer activity of ESIL (150, 300 and 600 mg/kg p.o. for 7 days) was compared with standard drugs (Ranitidine). In pyloric ligation induced ulcer model, the studied parameters were gastric volume, pH, total acidity, free acidity, and ulcer index whereas in ethanol and cysteamine induced ulcer model, the ulcer index was determined for severity of ulcers. The parameters studied were ulcer index, gastric juice volume, pH, free acidity and total acidity. RESULTS: In pyloric ligation model; the volume of gastric content, total/free acidity and pepsin activity was significantly decreased at p<0.05 and p<0.01 and pH of the gastric juice was significantly increased at p<0.05 and p<0.01 in ESIL treated groups as compared to control group. All the doses of ESIL showed dose dependent antiulcer effect as well as significant (p<0.05 and p<0.01) reduction in the ulcer index as compared to control group in all the experimental models. CONCLUSION: The results of the study indicate that the ESIL have better potential against ulcer which supports the traditional claims in folklore medicine.

Vanillin abrogates ethanol induced gastric injury in rats via modulation of gastric secretion, oxidative stress and inflammation.

Vanillin is commonly used as an additive in food, medicine and cosmetics, but its effect has not yet been studied in gastric injury. Therefore the effect of vanillin was studied in experimental gastric ulcer. Gastric secretion and acidity were studied in pylorus ligated rats. Ulcer index, levels of gastric mucus, malondialdehyde (MDA), myeloperoxidase activity (MPO), expression of nuclear factor kappa B (NF-κB) p65, and histopathological changes were determined in ethanol induced gastric ulcer. Pre treatment with vanillin significantly reduced gastric secretion (P < 0.001) and acidity (P < 0.0001) and gastric ulcer index scores (P < 0.001). and augmented the gastric mucosal defense. Vanillin significantly restored the depleted gastric wall mucus levels (P < 0.0001) induced by ethanol and also significantly attenuated ethanol induced inflammation and oxidative stress by the suppression of gastric MPO activity (P < 0.001), reducing the expression of NF-κB p65 and the increased MDA levels (P < 0.001). Vanillin was also effective in alleviating the damage to the histological architecture and the activation of mast cells induced by ethanol. Together the results of this study highlight the gastroprotective activity of vanillin in gastric ulcers of rats through multiple actions that include inhibition of gastric secretion and acidity, reduction of inflammation and oxidative stress, suppression of expression of NF-κB, and restoration of the histological architecture.

Combination treatment of lycopene and hesperidin protect experimentally induced ulcer in laboratory rats.

AIM: Lycopene, a carotenoid and hesperidin, a flavonoid are naturally occurring in vegetables and fruits. Synergistic effect of a combination of carotenoid and flavonoid has been reported due to its antioxidant activity. Therefore, the present study was aimed to evaluate the protective effect of this combination on pylorus ligation induced ulcers in rats. MATERIALS AND METHODS: Thirty Wistar albino rats were divided into five groups (n = 6). Rats were fasted for 24 h before pylorus ligation. After 24 h of fasting the rats were treated with hesperidin (100 mg/kg) and lycopene (2 mg/kg) and their combination 1h prior to surgery. After an hour under ether anesthesia pylorus ligation was performed, after 5 h the animals were sacrificed, stomach was dissected, and gastric contents were collected and measured. Total acidity and pH of gastric content was estimated. Ulcer index was calculated, and macroscopic examination of the stomach was carried out. RESULTS: The sham operated rats showed a significant increase in pH, volume of gastric content and total acidity and ulcer index. The rats pretreated with lycopene and hesperidin showed significant improvement in the ulcer conditions. However, rats treated with a combination of lycopene and hesperidin showed more significant restoration of gastric function as compared to sham operated rats. Moreover, a significant difference was also noted in rats treated with a combination as compared to lycopene and hesperidin treatment alone. CONCLUSION: Thus experimentally the combination was seen to treat ulcers by anti-secretory, neutralizing, cytoprotective and mainly due to its antioxidant property.

Gastroprotective effects of D-002 (beeswax alcohols) and Lyprinol® on experimentally-induced gastric ulceration in rats

Introduction: D-002, a mixture of beeswax alcohols, has been effective in osteoarthritis models and for reducing osteoarthritis symptoms. Unlike the classic anti-inflammatory drugs, D-002 elicits gastroprotective rather than gastrotoxic effects. Lyprinol, used for ameliorating inflammation and arthritic symptoms, improves gastrointestinal dysfunction symptoms in osteoarthritis subjects. Both D-002 and Lyprinol inhibit cyclooxygenase and 5?lipoxygenase activities, and have been similarly effective for reducing inflammation experimentally. Objective: to compare the effects of D-002 and Lyprinol on gastric mucosa of normal and experimentally-induced ulcer rats. Methods: ulcer indexes were measured in normal rats and in rats with ethanol or pylorus ligation-induced ulcers, in which gastric volume and mucus secretion were also measured. Normal rats were randomized into a vehicle control, one acetic salicylic acid (150 mg/kg), three D-002, three Lyprinol groups; rats with ethanol-ulcers into a vehicle control, three D-002 and three Lyprinol-treated groups; and the experiment on pylorus ligation included a negative control and eight pylorus-ligated groups: one vehicle control, three D-002, three Lyprinol, one omeprazole 10 mg/kg. In all cases, D-002 and Lyprinol (50, 200 and 400 mg/kg) were given orally. Results: unlike D-002 and Lyprinol (50-400 mg/kg), acetic salicylic acid increased ulcer indexes and the incidence of ulcers versus the vehicle control. Single oral doses of D-002 (50-400 mg/kg) or Lyprinol (200 and 400 mg/kg) decreased significantly (p<0.01) and in a similar way ulcer indexes versus the ethanol-positive control. D-002 and Lyprinol (50-400 mg/kg) lowered significantly (p<0.01) and comparably ulcer indexes in rats with pylorus ligation versus the positive controls. D-002 (200 and 400 mg/kg) decreased gastric volume and increased gastric mucus secretion versus the positive control whereas only Lyprinol 400 mg/kg increased the gastric mucus secretion but without modifying the gastric volume. Omeprazole significantly reduced ulcer index (p<0.05) and gastric volume (p< 0.01), with no change in mucus secretion. Conclusion: D-002 and Lyprinol did not show gastrotoxic effects and similar efficacy in protecting against ethanol and pylorus ligation-induced gastric ulceration in rats(AU)

Introducción: el D‒002, una mezcla de alcoholes de la cera de abejas, efectivo en modelos de osteoartritis y para reducir los síntomas de la misma. A diferencia de los medicamentos antiinflamatorios clásicos el D‒002 produce efectos gastroprotectores más que efectos gastrotóxicos. El Lyprinol, usado para disminuir la inflamación y los síntomas artríticos, mejora los síntomas de disfunción gastrointestinal en sujetos con dicha enfermedad. D‒002 y Lyprinol inhiben las actividades de cyclooxigenasa y 5‒lipooxigenasa, y son similarmente efectivos para reducir la inflamación en modelos experimentales. Objetivo: comparar los efectos del D‒002 y el Lyprinol sobre la mucosa gástrica de ratas normales y de ratas con úlcera gástrica inducida experimentalmente. Métodos: se determinó el índice de úlcera en ratas normales y en ratas con úlceras gástricas inducidas por etanol e inducidas por ligadura de píloro, en las cuales se midió el volumen gástrico y la secreción de mucus. Las ratas normales se distribuyeron en un grupo control (vehículo), uno con ácido acetil salicílico (150 mg/kg), tres con D‒002 y tres con Lyprinol; las ratas con úlcera inducida por etanol en un grupo control (vehículo), tres con D‒002 y tres con Lyprinol; y el experimento con ligadura de píloro en un grupo control (vehículo), tres D‒002, tres Lyprinol y uno con omeprazol (10 mg/kg). En todos los casos, el D‒002 y el Lyprinol (50, 200 y 400 mg/kg) se administraron por vía oral. Resultados: el ácido acetil salicílico, no el D‒002 ni el Lyprinol (50‒400 mg/kg), incrementó el índice de úlceras y la incidencia de úlceras comparadas con el grupo control. Dosis orales únicas de D‒002 (50‒400 mg/kg) o Lyprinol (200 y 400 mg/kg) redujeron significativa (p<0,01) y similarmente el índice de úlceras comparado con el grupo control positivo con úlceras por etanol. El D‒002 y el Lyprinol (50‒400 mg/kg) redujeron significativamente (p<0,01) y comparablemente el índice de úlceras en ratas con ligadura de píloro comparado con el grupo control positivo. El D‒002 (200 y 400 mg/kg) redujo el volumen gástrico e incrementó la secreción de mucus gástrico respecto al grupo control positivo; mientras solo el Lyprinol 400 mg/kg aumentó la secreción de mucus gástrico pero sin modificar el volumen gástrico. El omeprazol redujo significativamente el índice de úlcera (p<0,05) y el volumen gástrico (p<0,01), sin modificar la secreción de mucus. Conclusiones: el D‒002 y el Lyprinol no presentaron efectos gastrotóxicos, y protegieron con eficacia similar de las úlceras gástricas inducidas por etanol y por ligadura del píloro en ratas(AU)

Comparative antidiarrheal and antiulcer effect of the aqueous and ethanolic stem bark extracts of Tinospora cordifolia in rats.

Tinospora cordifolia is indigenous to the tropical areas of India, Myanmar and Sri Lanka. The use of plant as remedy for diarrhea and ulcer is well-documented in Ayurvedic system of medicine. However, pharmacological evidence does not exist to substantiate its therapeutic efficacy for the same. The aim was to investigate the antidiarrheal and antiulcer activity of ethanolic and aqueous extracts of T. cordifolia in rats. The antidiarrheal activity of T. cordifolia extracts was evaluated by castor oil and magnesium sulfate-induced diarrhea using parameters such as onset of diarrhea, number of wet stools, total number of stool and weight of total number of stools. The antiulcer activity of extracts was investigated using ethanol and pylorus ligation-induced ulcer. Furthermore, tissue antioxidant parameters such as reduced glutathione, catalase activity and lipid peroxidation level were also investigated. Tinospora cordifolia extracts were more efficacious in reducing number of total stools in both the models of diarrhea and showed a dose-dependent antidiarrheal effect. The antiulcer activity of the extracts was confirmed by a reduction in ulcer index along with the decrease in gastric volume, total acidity, and an increase in pH of gastric content in both the models. The obtained results have established a pharmacological evidence for the folkloric use of the T. cordifolia as antidiarrhoeal and antiulcer agent.