Ulcer Inhibition Research Articles

In vitro immunomodulatory activity and in vivo anti-inflammatory and analgesic potential with gastroprotective effect of the Mediterranean red alga Laurencia obtusa

Context: Red algae have been recognized as a rich natural source of compounds possessing interesting biological and pharmacological activities.Objective: This work investigates anti-inflammatory, analgesic and gastroprotective activities of MeOH/CH2Cl2 crude extract and its fractions F1 (50% MeOH) and F2 (80% MeOH) from the whole alga plant Laurencia obtusa Hudson (Rhodomelaceae).Materials and methods: Anti-inflammatory activity was evaluated in vitro using cytometric bead array (CBA) technology to follow up the secretion of tumour necrosis factor alpha (TNF-α) in lipopolysaccharide activated THP-1 monocytic cells at doses of 10–250 μg/mL and in vivo using carrageenan-induced paw oedema in Wistar rats at doses of 25, 50, 100 and 200 mg/kg. Crude extract and fractions were tested at the doses of 25, 50, 100 and 200 mg/kg for peripheral and central analgesic activity by acetic acid-induced writhing test and hot-plate method, respectively, in Swiss albino mice. Gastroprotective activity was evaluated using HCl/ethanol-induced gastric ulcer test in rats at doses of 25, 50, 100 and 200 mg/kg.Results: Crude extract, F1 and F2 showed an interesting inhibition of TNF-α secretion with IC50 values of 25, 52 and 24 μg/mL, respectively, and a significant anti-inflammatory activity in vivo (p < 0.01), 3 h after carrageenan injection, the oedema inhibition was 55.37%, 52.18% and 62.86%, respectively, at the dose of 100 mg/kg. Furthermore, they showed a significant peripheral analgesic activity with 53.79%, 55.92% and 57.37% (p < 0.01) of writhing inhibition, respectively. However, no significant activity was found in the hot-plate test. An interesting gastroprotective effect was observed with crude extract and its fractions F1 and F2 with a gastric ulcer inhibition of 65.48%, 77.42% and 81.29%, respectively, at the dose of 50 mg/kg.Discussion and conclusion: These results suggest that L. obtusa might be used as a potential source of natural anti-inflammatory and analgesic agents with gastroprotective effect.

Phytochemistry and gastrointestinal benefits of the medicinal spice, Capsicum annuum L. (Chilli): a review.

Dietary spices and their active constituents provide various beneficial effects on the gastrointestinal system by variety of mechanisms such as influence of gastric emptying, stimulation of gastrointestinal defense and absorption, stimulation of salivary, intestinal, hepatic, and pancreatic secretions. Capsicum annuum (Solanaceae), commonly known as chilli, is a medicinal spice used in various Indian traditional systems of medicine and it has been acknowledged to treat various health ailments. Therapeutic potential of chilli and capsaicin were well documented; however, they act as double-edged sword in many physiological circumstances. In traditional medicine chilli has been used against various gastrointestinal complains such as dyspepsia, loss of appetite, gastroesophageal reflux disease, gastric ulcer, and so on. In chilli, more than 200 constituents have been identified and some of its active constituents play numerous beneficial roles in various gastrointestinal disorders such as stimulation of digestion and gastromucosal defense, reduction of gastroesophageal reflux disease (GERD) symptoms, inhibition of gastrointestinal pathogens, ulceration and cancers, regulation of gastrointestinal secretions and absorptions. However, further studies are warranted to determine the dose ceiling limit of chilli and its active constituents for their utilization as gastroprotective agents. This review summarizes the phytochemistry and various gastrointestinal benefits of chilli and its various active constituents.

Synergy Effects of Three Plant Extracts on Protection of Gastric Mucosa

The gastric mucosa protection effect of three natural plant extracts, Hericium erinaceus (HE), Centella asiatica (CA) and Amomum villosum (AV), were evaluated using the indomethacin damage model. Compared with a single extract, a combination of HE/CA/AV, especially with the ratios of 80:10:10, 45:45:10 and 45:10:45, showed significant synergistic effects for protection of the gastric mucosa with gastric ulcer inhibition rates of 97.8 ± 0.7%, 86.5 ± 2.8% and 86.1 ± 3.6%, respectively. Microscopic appearances of the gastric mucosa were carried out to help confirm the results.

Solid lipid microparticles: An approach for improving oral bioavailability of aspirin

The objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and pharmacodynamic properties. Aspirin-loaded solid lipid microparticles (SLMs) were formulated by hot homogenization and analysed for their encapsulation efficiency (EE%), in vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Particle size ranged from 33.10 ± 5.85 to 43.50 ± 7.27 µm for batches A1 to A3 SLMs loaded with 1, 3 and 5% aspirin and containing Poloxamer 407, while batches B1, B2 and B3 formulated with Soluplus as surfactant had particle size range of 31.10 ± 1.46 to 45.60 ± 2.92 µm. Batches A1 and B1 containing 1% of aspirin had the highest EE of 70 and 72% respectively. Maximum in vitro release of 95.1 and 93.2% were obtained at 8 h from batches A1 and B1 respectively. SLMs exhibited about 77.8% oedema inhibition, while the reference had 66.7% and ulcer inhibition range of 25–75%. Aspirin-loaded SLMs exhibited good properties and could be used orally twice daily for the treatment of inflammation.

Gastroprotective and antioxidant potentials of ethanolic stem bark extract of Margaritaria discoidea (Euphorbiaceae) in rats

Ethnopharmacological relevanceDecoctions prepared from the bark of Margaritaria discoidea (Baill.) G. L. Webster (Euphorbiaceae) are used in Nigeria and other parts of West Africa in the treatment of wounds and ulcers. The study was conducted to investigate the gastric ulcer protective effect of ethanolic stem bark extract of M. discoidea in rats. Materials and methodsAntiulcer assays were performed using ethanol, indomethacin and pylorus ligation-induced ulcer models at the dose of 50, 100 and 150mg/kg, p.o. The antioxidant effect of the extract was evaluated in vitro and by studying its effect on antioxidant enzymes (superoxide dismutase, catalase, and reduced glutathione) and lipid peroxidation in the stomach tissue of rats in ethanol-induced model. Solvent fractions (hexane, dichloromethane, ethyl acetate, butanol and aqueous) from the crude extract were investigated for antiulcerogenic effects in ethanol-induced ulcer model at the dose of 150mg/kg. GC–MS analysis of the active hexane fraction was also carried out. ResultsThe extract significantly (P<0.05) reduced gastric lesion in ethanol and indomethacin-induced ulcer models. The extract had significant influence on in vivo antioxidant status in ethanol-induced model. In pylorus ligation-induced model, only the dose of 150mg/kg showed significant reduction (88.89%, P<0.05) of ulcer lesions. There was no significant reduction in the gastric juice volume and total acidity. The solvent fractions showed ulcer inhibition in varying degrees but significance (P<0.01) was only observed in the hexane fraction. Ethyl esters of palmitic and linoleic acids were found as the major compounds in the GC–MS analysis of the hexane fraction. ConclusionOur results suggest that M. discoidea possesses gastroprotective activity possibly mediated through antioxidant mechanism. The data obtained in this study provide some support to the traditional use of M. discoidea in the treatment of gastric ulcer.

Paclitaxel or 5-fluorouracil/esophageal stent combinations as a novel approach for the treatment of esophageal cancer

Currently, esophageal cancer is rarely curable, and herein, a paclitaxel or 5-fluorouracil/esophageal stent combination (PTX or 5-FU/stent) was used to provide a new approach to treat this cancer. The PTX or 5-FU/stent was prepared by covering a nitinol stent with a bilayered polymer film that consisted of a layer of 50% PTX or 5-FU and a layer of drug-free backing. These treatment modalities were evaluated in vivo after implantation into the porcine esophagus. The percentages of the drugs that permeated from the backing layer over a period of 95 days were very small (0.61% for 5-FU), and an overwhelming majority of the PTX and the 5-FU was released from the other side of the film. During the follow-up period (120 days), the drug/stent was always maintained in the porcine esophagus, and did not show any obvious systemic or local toxicities. In contrast, this treatment had an effect on the inhibition of tissue proliferation and ulceration. In addition, the drug concentrations were highest in the esophagus compared with in the heart, liver, spleen, lung, kidney and blood (81500.0 ± 9475.2 ng/g vs. 3.9 ± 0.3 ng/mL of PTX in the plasma at 13 days). The PTX/stent and the 5-FU/stent have a dual function as both a stent and a local drug delivery device, which provides a potential treatment modality with high efficacy and non systematic toxicity for esophageal cancer.

Anti-ulcerogenic activity of aqueous extract of Carica papaya seed on indomethacin-induced peptic ulcer in male albino rats

ObjectiveCarica papaya is an important fruit with its seeds used in the treatment of ulcer in Nigeria. This study investigated the anti-ulcerogenic and antioxidant activities of aqueous extract of Carica papaya seed against indomethacin-induced peptic ulcer in male rats. MethodsThirty male rats were separated into 6 groups (A–F) of five rats each. For 14 d before ulcer induction with indomethacin, groups received once daily oral doses of vehicle (distilled water), cimetidine 200 mg/kg body weight (BW), or aqueous extract of C. papaya seed at doses of 100, 150 or 200 mg/kg BW (groups A, B, C, D, E and F, respectively). Twenty-four hours after the last treatment, groups B, C, D, E and F were treated with 100 mg/kg BW of indomethacin to induce ulcer formation. ResultsCarica papaya seed extract significantly (P<0.05) increased gastric pH and percentage of ulcer inhibition relative to indomethacin-induced ulcer rats. The extract significantly (P<0.05) decreased gastric acidity, gastric acid output, gastric pepsin secretion, ulcer index and gastric secretion volume relative to group B. These results were similar to that achieved by pretreatment with cimetidine. Specific activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase and glucose-6-phosphate dehydrogenase in the extract-treated groups (D, E and F) were increased significantly over the group B (P<0.05). Pretreatment with the seed extract protected rats from the indomethacin-mediated decrease in enzyme function experienced by the group B. Similarly, indomethacin-mediated decrease in reduced glutathione level and indomethacin-mediated increase in malondialdehyde were reversed by Carica papaya extract. ConclusionIn this study, pretreatment with aqueous extract of Carica papaya seed exhibited anti-ulcerogenic and antioxidant effects, which may be due to the enhanced antioxidant enzymes.

Gastric acid anti-secretory effects of aqueous leaf extract of Nauclea latifolia (Rubiaceae) in rats

The aqueous leaf extract of Nauclea latifolia has been shown to have anti-ulcer effect. Objectives: The present study was undertaken to investigate the effects of aqueous leaf extract of N. latifolia on gastric acid secretion as the possible mechanism of its anti-ulcer actions in male albino rats. Materials and Methods: A total of sixty (60) male albino rats were divided into two experimental studies of thirty (30) rats each. Each of the experimental studies was further divided into groups according to study design. The extract was administered orally at the doses of 100, 200 and 400 mg/kg for the experimental groups while the control and reference groups received distilled water (2 ml/kg, p.o) and cimetidine (32 mg/kg, p.o) respectively, 60 minutes prior to oral administration of indomethacin (30 mg/kg) to induce gastric mucosal injury. In the second study, gastric acid output was measured by the continuous perfusion of rat’s stomach under anesthesia with normal saline at the rate of 1 ml/min. Results: Phytochemical analysis revealed the presence of saponins, tannins, flavonoids, alkaloids and cardiac glycosides. Acute toxicity studies showed there were no deaths within 24 h after the application of the extract up to 1600 mg/kg B.W (i.p). Rats pre-treated with N. latifolia exhibited significant (P&lt;0.05), and dose-dependent inhibition of indomethacin-induced gastric ulceration. A significant decrease in gastric acid secretion was produced by the extract at all doses studied. Conclusion: Findings of this study suggest that, aqueous extract of N. latifolia significantly reduced gastric acid secretion in indomethacin-induced gastric ulceration by inhibiting histamine-stimulated gastric acid secretion probably by occupying H2 - receptors in rats.

Enrichment of anti‐ulcer activity of monoammonium glycerrhizin and Aloe vera gel powder through a novel drug delivery system

Usual treatment for Helicobacter pylori‐induced peptic ulcer includes a 14‐day “triple therapy” of two antibiotics and a proton pump inhibitor. However, the current therapy has side‐effects like stomach upset, non‐compliance, incomplete absorption of drug and antibiotic resistance. To overcome these limitations, there is a need to suggest an alternative therapy. The best possible alternative is to deliver herbal constituents. The purpose of the present study was to optimize the efficacy of herbal constituents by applying the concept of a novel drug delivery system.The present investigation is designed to deliver and retain two herbal constituents in the stomach for better action against gastric ulcers. The objective was to develop a bilayer floating tablet of monoammonium glycerrhizin and Aloe vera gel powder through rational combination of excipients to give the lowest possible lag time with maximum drug release in 7 h. Formulation OF2 containing hydroxy propyl methyl cellulose E5, crospovidone and effervescent agents in the ratio 1:2 gave 98% drug release with desired floating properties. Pharmacodynamic studies in rats showed that the combination of monoammonium glycerrhizin and Aloe vera gave 99% ulcer inhibition in comparison with 51% ulcer inhibition in the group administered with monoammonium glycerrhizin alone. X‐ray studies in rabbits proved the gastroretention of the tablet for more than 6 h. This suggests relevance of NDDS in delivery of herbal constituents in the treatment of gastric ulcer. Key words: Aloe vera, floating tablet, gastric ulcer, monoammonium glycerrhizin, pharmacodynamic studies

Antiulcer activity of the ethanolic extract and ethyl acetate fraction of the leaves of Markhamia tomentosa in rats

Ethnopharmacological relevanceThe leaves of Markhamia tomentosa (Benth.) K. Schum. Ex Engl. (Bignoniaceae) are used traditionally in the treatment of skin afflictions, sores, ulcers and inflammation. The aim of the study was to investigate the antiulcer activity of the crude ethanolic extract from the leaves of Markhamia tomentosa, determine the active fraction(s) of the extract and identify the chemical constituents in the active fraction by LC–MS. Materials and methodsThe antiulcer activity of the crude extract (50, 100 and 150mg/kg, p.o.) was evaluated in ethanol and indomethacin-induced models while the solvent fractions (150mg/kg) were screened using ethanol-induced gastric lesions in rats. Furthermore, anti-ulcer activity of the active fraction (50, 100 and 150mg/kg, p.o.) was performed using indomethacin and pylorus ligation models. Parameters such as gastric volume, pH and acidity were determined in the pylorus ligation model. LC–ESI–MS analysis was used to identify the components in the active fraction. ResultsThe extract at the dose of 50, 100 and 150mg/kg caused a significant (p<0.05) dose-dependent inhibition of ulcer in the ethanol and indomethacin-induced ulcer models, respectively. The ethyl acetate (EtOAc) fraction showed the most potent antiulcer activity from all the fractions tested. This fraction produced 72% and 92% inhibition of indomethacin and pylorus-induced ulcer at a dose of 150mg/kg respectively. Acteoside, luteolin, luteolin-7-rutinoside, Luteolin-3′,7-di-O-glucoside, carnosol, dilapachone, tormentic acid, oxo-pomolic acid and ajugol were detected in the EtOAc fraction. ConclusionOur data provide a rational base for the folkloric use of Markhamia tormentosa in the treatment of ulcers.

Pharmacological evaluation of the semi-purified fractions from the soft coral Eunicella singularis and isolation of pure compounds.

BackgroundGorgonians of the genus Eunicella are known for possessing a wide range of pharmacological activities such as antiproliferative and antibacterial effect. The aim of this study was to evaluate the anti-inflammatory and gastroprotective effect of the organic extract and its semi-purified fractions from the white gorgonian Eunicella singularis and the isolation and identification of pure compound(s) from the more effective fraction.MethodsAnti-inflammatory activity was evaluated, using the carrageenan-induced rat paw edema test and in comparison to the reference drug Acetylsalicylate of Lysine. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification of compound(s) from the more effective fraction was done by two chromatographic methods (HPLC and MPLC). The structure elucidation was determined by extensive spectroscopic analysis (1H and 13C NMR, COSY, HMBC, HMQC and NOESY) and by comparison with data reported in the literature.ResultsThe evaluation of the anti-inflammatory activity of different fractions from Eunicella singularis showed in a dependent dose manner an important anti-inflammatory activity of the ethanol fraction, the percentage of inhibition of edema, 3 h after carrageenan injection was 66.12%, more effective than the reference drug (56.32%). In addition, this ethanolic fraction showed an interesting gastroprotective effect compared to the reference drugs, ranitidine and omeprazol. The percentage of inhibition of gastric ulcer induced by HCl/ethanol in rats was 70.27%. The percentage of the reference drugs (ranitidine and omeprazol) were 65 and 87.53%, respectively. The purification and structure elucidation of compound(s) from this ethanolic fraction were leading to the isolation of five sterols: cholesterol (5α-cholest-5-en-3β-ol) (1); ergosterol (ergosta-5,22-dien-3β-ol) (2); stigmasterol (24-ethylcholesta-5,22-dien-3b-ol) (3); 5α,8α-epidioxyergosta 6,22-dien-3β-ol (4) and 3β-hydroxy-5α,8α-epidioxyergosta-6-ene (5); and one diterpenoid: palmonine D (6).ConclusionBased on data presented here, we concluded that diterpenoids and sterols detected in the ethanolic fraction can be responsible for its pharmacological activity.Electronic supplementary materialThe online version of this article (doi:10.1186/s40199-014-0064-7) contains supplementary material, which is available to authorized users.

Alkaloids from Mahonia bealei posses anti-H+/K+-ATPase and anti-gastrin effects on pyloric ligation-induced gastric ulcer in rats

The purpose of this study was to investigate the underlying mechanism(s) of the total alkaloids (TA) from Mahonia bealei in treating pyloric ligation-induced gastric ulcers in rats. Animals were sacrificed after 19h of the ligation. Gastric acid, peptic activities, mucin levels, H+/K+-ATPase activities and the gastrin level were analyzed. To improve the accuracy of the observations, IPP 6.0 software was introduced to measure the area of ulcer. TA (18.56mg/kg/day, i.g.) showed an antiulcer effect by significantly decreasing the gastric ulcer areas (11.28mm2) compared with model group (26.36mm2). The TA ulcer inhibition ratio was 57.2%, compared with the effect of the positive control, omeprazole (62.96%). The results also showed that TA had a significant effect in inhibiting the release of H+/K+-ATPase, reducing the content of gastrin and decreasing gastric acidity on experimental animals. However, the TA had no significant effects on gastric mucus secretion and pepsin activity. Data indicated that TA had gastric ulcer protective effects by modulating the H+/K+-ATPase activity and gastrin level. TA has a potential to be developed as a pharmacological agent for the treatment of gastric ulcers.

Exploring the Potential of Gastro Retentive Dosage Form in Delivery of Ellagic Acid and Aloe vera Gel Powder for Treatment of Gastric Ulcers

Approach of novel drug delivery system (NDDS) overcomes the limitations of conventional dosage forms. However, this concept is still not practiced to a large extent in delivery of herbal drugs in Ayurveda. Thus, the potential of herbal drugs has not been explored to its fullest. Hence, there is a growing need to amalgamate the concept of NDDS in delivery of herbal constituents. The present investigation is designed to deliver and retain two herbal constituents in stomach for better action against Helicobacter pylori induced gastric ulcers. The objective was to develop a bilayer floating tablet of ellagic acid and Aloe vera gel powder through rational combination of excipients to give the lowest possible lag time with maximum drug release in the period of 4 h. Formulation F9 containing 100 mg of HPMC K15M, 27 mg of crospovidone, 80 mg of mannitol and effervescent agents in the ratio 1:2 gave 92% drug release and desired floating properties. In vivo studies showed that combination of ellagic acid and Aloe vera gave 75 % ulcer inhibition in comparison to 57% ulcer inhibition in the group which was administered with ellagic acid alone. This suggests the use of bilayer floating tablet in gastric ulcer treatment.

Evaluation of the gastroprotective activity of the extracts, fractions, and pure compounds obtained from aerial parts of Rubus imperialis in different experimental models

Previous phytochemical studies carried out with Rubus imperialis Chum. Schl. (Rosaceae) have demonstrated the presence of triterpenes (niga-ichigoside F1 and 2β,3β,19α-trihydroxyursolic acid) in this species. The literature indicates that triterpenes are closely related to some pharmacological activities, including antiulcer activity. Therefore, in view of the previous promising results with this species, this work extends the phytochemical studies, as well as investigates its gastroprotective action in different models using rodents. The hydroalcoholic extract was tested using the following protocols in mice: ethanol/HCl and nonsteroidal anti-inflammatory drug (NSAID)-induced ulcer, acetic acid-induced chronic ulcer, ligature pylorus model, and free mucus quantification in mucosa. Isolated triterpenes were investigated in the ethanol/HCl-induced ulcer model. The results of this study show that R. imperialis extract (100, 250, or 500mg) displays gastroprotective activity in the ethanol-induced ulcer model with a percentage of inhibition of gastric lesions of 70, 71, and 86%, respectively. The extract also significantly reduced the ulcerative lesions in the indomethacin-induced ulcer. In this model, the percentage of inhibition of ulcer was 41, 44, and 70%, respectively. Regarding the model of gastric secretion, a reduction of gastric juice volume and total acidity was observed, as well as an increase in gastric pH; however, gastric mucus production was not altered by treatment with the extract. It was also observed that the ethyl acetate fraction presented higher activity, leading to the isolation of niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid, which presented antiulcer activity comparable to that of omeprazole, with an inhibition percentage of 98 and 99%, respectively. These results demonstrate that R. imperialis extract and isolated compounds (niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid) produce gastroprotective effects, and this activity seems, at least in part, to be related to antisecretory effects.

Antisecretory Action of the Extract of the Aerial Parts ofEremomastax speciosa (Acanthaceae)Occurs through Antihistaminic and Anticholinergic Pathways

Objective. The objective of this study was to find out the possible antiulcer mechanism of action of Eremomastax speciosa. Method. Carbachol- and histamine-induced hypersecretion, associated with the pylorus ligation technique, were used in rats. Gastric mucosal ulceration, mucus production, pH, gastric volume, and acidity were measured. Results. Histamine and carbachol raised gastric acidity to 86.50 and 84.80 mEq/L, respectively, in the control rats, and the extracts (200 mg/kg) reduced gastric acidity to 34.60 and 39.00 mEq/L, respectively. Intraduodenal aqueous extract (400 mg/kg) in histamine- and carbachol-treated rats produced significant (P < 0.001) decreases in acid secretion to 28.50 and 28.80 mEq/L, respectively, and 100 percent inhibition of gastric ulceration. Augmented histamine-induced gastric acid secretion (90.20 mEq/L) was significantly reduced to 52.60 and 27.50 mEq/L by the 200 and 400 mg/kg doses of the aqueous extract, respectively. The extract significantly reduced (P < 0.001) the volume of gastric secretion and significantly increased mucus production. The ulcer inhibition potential of the extract significantly dropped to 25–44% (oral extract) and to 29–37% (duodenal extract) in carbachol/indomethacin-treated rats. Conclusion. The aqueous extract of E. speciosa has both cytoprotective and antisecretory effects. The antisecretory effect may involve a mechanism common to both cholinergic and histaminergic pathways.

Effect of ovarian sex hormones on non-steroidal anti-inflammatory drug-induced gastric lesions in female rats

Objective:The objective of the following study is to investigate the effect of ovarian sex hormones on gastric ulcer in female rats.Materials and Methods:Female rats were treated daily with estrogen (0.05 and 0.1 mg/kg), progesterone (2.0 and 5.0 mg/kg), combined estrogen (0.05 mg/kg) and progesterone (2.0 mg/kg), ranitidine (30 mg/kg) or vehicle for 7 days. Ulcers were induced with aspirin on 7th day. Four hours later, animals were sacrificed and stomach were removed for macroscopic and biochemical examination.Results:Estrogen in 0.05 and 0.1 doses showed 32% and 18% of ulcer inhibition, respectively, progesterone 09% and 14% inhibition in 2.0 and 5.0 mg/kg doses, respectively, whereas combined estrogen and progesterone showed 23% and ranitidine showed 60% inhibition. However, the inhibition attained and the stomach malondialdehyde and glutathione levels in sex hormone treated groups were not statistically significant when compared to control group.Conclusion:At the tested doses, these ovarian sex hormones neither worsen nor protect against aspirin-induced gastric lesions in female rats.

해동피 및 유사생약 추출물의 위 손상에 대한 효과

해동피는 약리학적으로 진통, 소염작용이 있어, 허리와 무릎의 통증 등을 치료하는데 효과가 있다고 알려져 있다. 본 연구에서는 해동피(Kalopanax pictus)의 국산 및 중국산과 그 유사생약으로 사용되는 절동피(znthoxylum ailanthoides)의 국산과 중국산, 목면피(bombax malabaricum)의 <TEX>$H_2O$</TEX> 및 70% EtOH 추출물의 항위염 효과와 항산화효과에 대해 알아보았다. 먼저 HCl EtOH로 유발한 흰쥐위염 모델을 통해 효과를 확인하였고, 위염 및 위궤양, 위암의 원인으로 잘 알려진 H. pylori에 대한 colony 억제작용과 대표적 공격인자인 과다한 산에 대한 억제작용을 확인 하고자 제산력 시험법을 실시하였다. 항위염 효과에 대한 항산화 기전으로는 DPPH 시험법, 환원력 시험법, <TEX>${\beta}$</TEX>-carotene/linoleic acid syetem을 이용한 지질과산화 억제활성 시험을 실시하였고, 실험에 사용한 추출물 중 가장 효과가 우수한 해동피 국산 추출물을 이용하여 superoxide radical 및 hydrogen peroxide 소거 작용을 확인하였다. Indomethacin으로 유발한 흰쥐 위궤양 모델에서는 해동피 국산 <TEX>$H_2O$</TEX> 및 70% EtOH 추출물에서 각각 73.1%, 53.5%로 손상을 억제시킴을 확인하였다. 흰쥐를 이용한 gastric secretion 실험으로는 해동피 국산 <TEX>$H_2O$</TEX> 및 70% EtOH 추출물이 위액의 분비를 줄이고, pH를 상승 시켰으며 총 산도를 감소시킴을 확인하였다. 그 결과, 해동피국산 및 중국산, 절동피국산 및 중국산, 목면피중국산 해동피의 항산화 효과가 가장 우수하였으며 해동피 국산은 위염 및 위궤양에서 우수한 효과를 확인하였고, 건강 기능성 식품 및 천연물 의약품으로서의 개발 가능성을 확인할 수 있었다. 또한, 이 결과를 토대로 오랜 세월 한약재로 사용되어 온 해동피의 기원이 다른 유사품 및 불량약재의 무분별한 유통, 정확한 기원의 약재에 대한 기준 설정, 높아지는 한약재 수입 의존도에 따른 위품, 저질품의 혼입 방지와 객관적, 신뢰성 있는 표준규격 설정에 기여할 것으로 예상된다. Kalopanax pictus has pharmacologically anti-inflammatory and analgesic effect and is known to respond to treatment of backache, knee pain and etc. In this study, we investigated the effects on gastric lesions of Kalopanax pictus both from Korea (KPK) and China (KPC) compared with their related origin, Znthoxylum ailanthoide both from Korea (ZAK) and China (ZAC), and Korean Bombax malabaricum (BMK). In preliminary screening, KPK and KPC shown effective inhibition of HCI EtOH-induced gastritis in rats. To elucidate their protective effects on gastric lesions, we assessed inhibition of H. pylori colonization, 2,2-diphenyl-1-picrylhydrazyl(DPPH) radical scavenging activities, reducing power test, and inhibition of lipid peroxidation. KPK was the most effective from antioxidant assays. KPK also shown the inhibition of indomethacin-induced gastric ulcer in rats. Gastric secretion in rats, KPK reduced the secretion of gastric juice and total acidity and raised pH. Therefore, it is possible that KPK can be developed as health functional food and natural medicine. In addition, it can contribute to the standardization with objectivity and reliability for KPK through the criteria establishment of the precise origin of medicine, the prevention of indiscriminate distribution of imitation, and the rising rate of dependence on imports of medicinal herbs, and mixing prevention of low-quality goods.

Preclinical evaluation of Vallaris solanacea (roth) kuntze stem for its antiulcer and antioxidant activity in wistar albino rats

In the present study we evaluated the antiulcer and antioxidant activity of methanolic extract from stem of the plant Vallaris solanacea (roth) Kuntze using various experimental models in Wister albino rats. The methanolic extract was prepared for evaluation of antiulcer activity with dose [3.2 milligram (mg)/kilogram (kg) and 6.4 mg/kg] by using models–pylorus ligation (PL) and ethanol induced gastric ulcer in rats. Antioxidant activity was evaluated by estimation of lipid peroxidation and catalase activity in the ethanol induced gastric ulcer model in rats. The results obtained from present study revealed that Vallaris solanacea methanolic extract (VSME) decreases the ulcer index significantly (p < 0.001) compared to the positive control group (Ranitidine 30 mg/kg) in both models at the both dose level. VSME also showed significant ulcer inhibition at both dose levels. In PL model of ulcer VSME decreased the volume of gastric juice, pH, total and free acidity. VSME also shown significant (p < 0.001) antioxidant activity by reduces the lipid peroxidation (LPO) and increases the catalase (CAT) activity. Present study shows that the VSME possess dose dependent antiulcer and antioxidant activity. However, further studies are required to focus on the molecular mechanism of responsible phytochemical constituents and establish exact mode of action involved in its antiulcer and antioxidant action.

ANTIULCER ACTIVITY OF PREMNA SERRATIFOLIA AGAINST ASPIRIN INDUCED GASTRIC ULCER MODEL

The present study was carried out to investigate antiulcer activity of methanolic bark extract of Premna serratifolia against aspirin induced gastric ulcer models of male wistar rats. In aspirin induced pylorus ligation model, various parameters were s tudied viz. volume and pH of gastric juice, total acidity, free acidity, ulcer score, ulcer index and percentage protection was determined. Ulcer score, ulcer index and percentage inhibition of ulceration was determined for ulcer model . Ranitidine (50 mg/kg p.o.) was used as the standard drug. Pretreatment with the extracts (200 & 400 mg/kg p.o.) showed significant protection against ulcer model . In aspirin induced pylorus liga ted model, the methanolic bark extract showed significant decrease in the volume of gastric juice, free and total acidity, ulcer score, ulcer index and increase in pH of gastric juice as compared to the toxicant control group. In conclusion, Premna serratifolia possess significant anti - ulcer and cytoprotective effect.

Evaluation of Antiulcer Activity of Picrasma Quassioides Bennett Aqueous Extract in Rodents

The present study was focused to evaluate the protective activity of the Picrasma quassioides (PQ) whole plant aqueous extract against aspirin-pylorus ligation, HCl-ethanol and water immersion stress induced ulcers. In the present study aspirin-pylorus ligation induced gastric ulcer was adopted to screen the antisecretory activity of plant extract. PQ extract produced 64.63% ulcer inhibition at 400mg/kg body weight, when compared to that of standard (ranitidine, 50mg/kg) which produced 68.52% ulcer inhibition. In HCl-ethanol induced ulcer model 400mg/kg body weight of PQ produced 72.24% ulcer inhibition when compared that of standard (sucralfate, 100mg/kg) which produced 75.01% ulcer inhibition. In water immersion-stress induced ulcer model 400mg/kg body weight of PQ, produced 84.11% ulcer inhibition when compared to that of standard (omeprazole, 20mg/kg) which produced 82.17% ulcer inhibition. PQ showed significant percentage of ulcer inhibition in the three models tested. The glycosides which are present in the aqueous extract could be responsible for their antiulcer properties.