Antiulcer Agent Research Articles

Control of Constipation in Patients Receiving CHOP or CHOP-Like Chemotherapy Regimens for Non-Hodgkin's Lymphoma.

Management of constipation in patients receiving cyclophosphamide, doxorubicin, vincristine and prednisolone (CHOP) or CHOP-like chemotherapy regimens is important for prevention of paralytic ileus. We reported earlier that the laxative action of magnesium oxide is reversed by the concomitant use of antacids in cancer patients receiving opioid analgesics. Here, we assessed the prevalence of prophylactic laxative medication for the control of constipation in patients receiving CHOP or CHOP-like regimens for non-Hodgkin's lymphoma. Data obtained from 211 eligible patients were retrospectively analyzed. Almost all patients (99%) received anti-ulcer agents such as proton pump inhibitors and H2 receptor antagonists for the prophylaxis of gastric disorders associated with prednisolone. Prophylactic laxatives were prescribed in 86 patients (40.8%), in which magnesium oxide was used most predominantly (88.4%). However, magnesium oxide at doses of ≦2000 mg/d was not effective for prevention of constipation, although the compound totally inhibited the incidence of constipation at doses higher than 2000 mg/d. Therefore, it is important to avoid negative drug interaction between magnesium oxide and antacids in patients receiving CHOP chemotherapy.

The In vitro/vivo Evaluation of Prepared Gastric Floating Tablets of Berberine Hydrochloride.

Currently available antiulcer drugs suffered from serious side effects which limited their uses and prompted the need for a safe and efficient new antiulcer agent. The objective of this project work was to retain the drug in the stomach for better antiulcer activity and less side effects. Hence, the aim of our present work was to prepare a gastric floating tablet of Berberine hydrochloride (Ber) with suitable in vitro/vivo properties. In this study, different Ber gastric floating tablets were prepared by simple direct compression using various amounts of HPMCK15M and Carbopol 971PNF combined with other tablet excipients. The properties of the tablets including hardness, buoyancy, swelling ability, in vitro drug release, and in vivo pharmacokinetic study were evaluated. The obtained results disclosed that hardness, floating, swelling, and in vitro drug release of the Ber tablets depended mainly on the ratio of polymer combinations. Moreover, among six formulations, F3 exhibited desirable floating, swelling, and extended drug release. In addition, in vivo pharmacokinetic study suggested that prepared gastric floating tablets had significantly sustained-releasing effects compared with market tablets. Therefore, the developed gastric floating tablets of Ber could be an alternative dosage form for treatment of gastrointestinal disease.

Isolation, characterization, and in silico, in vitro and in vivo antiulcer studies of isoimperatorin crystallized from Ostericum koreanum

Context: Ostericum koreanum (Maxim.) Kitagawa (Apiaceae) roots are traditionally used as an analgesic and antiulcer agent. However, the antiulcer potential of isoimperatorin isolated from O. koreanum has not yet been explored.Aim: To evaluate the antiulcer activity of isoimperatorin isolated from the roots of O. koreanum.Materials and methods: Isoimperatorin was isolated as cubic crystals by repeated column chromatography of the ethyl acetate fraction and structure was verified with 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS-FAB). The crystals obtained were analyzed with the single crystal X-ray method. The MTT assay was used to determine its cytotoxicity against chondrocytes at different concentrations (0.0–737.74 μM, 24 h). The in vivo antiulcer activity of isoimperatorin (40 mg/kg) was determined against ethanol-, indomethacin- and pyloric ligation-induced ulcers in Sprague-Dawley rats. Furthermore, the effect of isoimperatorin (0.0–737.74 μM, 24 h) on the expression of type II collagen in chondrocytes was determined using western blot method. The in vitro urease inhibitory activity of isoimperatorin (0–80 μM) and molecular docking was also performed against urease.Results and discussion: Isoimperatorin demonstrated significant inhibitory activity (IC50 36.43 μM) against urease as compared to the standard drug thiourea (IC50 33.57 μM) without cytotoxic effects. It provided 70.9%, 67.65% and 54.25% protection in ulcer models induced by ethanol, indomethacin and pyloric ligation, respectively. Isoimperatorin showed the highest expression level of type II collagen at 368.87 μM. The docking results confirmed strong binding affinity with the target protein.Conclusion: Isoimperatorin may be used to develop antiulcer drugs with decreased side effects.

Evaluating pharmaceutical waste disposal in pediatric units.

To verify the disposal of pharmaceutical waste performed in pediatric units. A descriptive and observational study conducted in a university hospital. The convenience sample consisted of pharmaceuticals discarded during the study period. Handling and disposal during preparation and administration were observed. Data collection took place at pre-established times and was performed using a pre-validated instrument. 356 drugs disposals were identified (35.1% in the clinic, 31.8% in the intensive care unit, 23.8% in the surgical unit and 9.3% in the infectious diseases unit). The most discarded pharmacological classes were: 22.7% antimicrobials, 14.8% electrolytes, 14.6% analgesics/pain killers, 9.5% diuretics and 6.7% antiulcer agents. The most used means for disposal were: sharps' disposable box with a yellow bag (30.8%), sink drain (28.9%), sharps' box with orange bag (14.3%), and infectious waste/bin with a white bag (10.1%). No disposal was identified after drug administration. A discussion of measures that can contribute to reducing (healthcare) waste volume with the intention of engaging reflective team performance and proper disposal is necessary. Verificar o descarte dos resíduos de medicamentos realizado em unidades pediátricas. Estudo descritivo e observacional, realizado em um hospital universitário. A amostra de conveniência foi constituída pelos medicamentos descartados durante o período de estudo. Observaram-se a manipulação e o descarte durante o preparo e a administração. A coleta dos dados ocorreu em horários preestabelecidos e realizada por meio de instrumento pré-validado. Identificaram-se 356 descartes de medicamentos (35,1% na clínica, 31,8% na unidade de cuidados intensivos, 23,8% na cirúrgica e 9,3% na infectologia). As classes farmacológicas mais descartadas foram: 22,7% antimicrobianos, 14,8% eletrólitos, 14,6% analgésicos, 9,5% diuréticos e 6,7% antiulcerosos. Vias mais utilizadas: caixa descartável para perfurocortante com saco amarelo (30,8%), ralo da pia (28,9%), caixa de perfurocortante com saco laranja (14,3%) e lixeira infectante com saco branco (10,1%). Não foi identificado descarte após a administração dos fármacos. Faz-se necessária a discussão de medidas que contribuam para a redução do volume de resíduos, com o intuito de engajar a atuação reflexiva da equipe e o descarte adequado.

Multiple Aryne Insertions into Oxindoles: Synthesis of Bioactive 3,3-Diarylated Oxindoles and Dibenzo[b,e]azepin-6-ones.

An aryne insertion cascade reaction on oxindoles has been observed and constitutes a convenient "one pot" preparation of bioactive di- and triarylated oxindoles in good yields under mild conditions. A temperature controlled "reaction switch" enables ready access to dibenzo[b,e]azepin-6-one derivatives employing the same reaction regime. This tactic has been extended to a short synthesis of potent antiulcer agent darenzepine.

FORMULATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ANTIULCER DRUG

ABSTRACTGastroretentive floating drug delivery system is utilised to target drug release in the stomach or to the upper part of intestine. Lansoprazole is proton pump inhibitor intended for oral administration used as antiulcer agent. The present investigation involved formulation and evaluation of Gastroretentive floating tablets of Lansoprazole for prolongation of gastric residence time with a view to deliver the drug at sustained and controlled manner in gastrointestinal tract. The tablets of Lansoprazole were prepared by direct compression method using gas generating agent and different polymer combinations (HPMCK4M, HPMC K100M, Psyllium husk) . The prepared tablets of Lansoprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study. The varying concentration of gas generating agent and polymers were found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating Gastroretentive tablet of Lansoprazole shown that the formulation F2 was found to be the best formulation as it releases 97.9% Lansoprazole in a controlled manner for extended period of time (upto 12 hrs.)Keywords: Lansoprazole, Gastroretentive, floating tablet, total floating time.

Brain-gut Axis and Pentadecapeptide BPC 157: Theoretical and Practical Implications.

BackgroundBrain-gut interaction involves, among others, peptidergic growth factors which are native in GI tract and have strong antiulcer potency and thus could from periphery beneficially affect CNS-disorders. We focused on the stable gastric pentadecapeptide BPC 157, an antiulcer peptidergic agent, safe in inflammatory bowel disease trials and now in multiple sclerosis trial, native and stable in human gastric juice.MethodsReview of our research on BPC 157 in terms of brain-gut axis.ResultsBPC 157 may serve as a novel mediator of Robert’s cytoprotection, involved in maintaining of GI mucosa integrity, with no toxic effect. BPC 157 was successful in the therapy of GI tract, periodontitis, liver and pancreas lesions, and in the healing of various tissues and wounds. Stimulated Egr-1 gene, NAB2, FAK-paxillin and JAK-2 pathways are hitherto implicated. Initially corresponding beneficial central influence was seen when BPC 157 was given peripherally and a serotonin release in particular brain areas, mostly nigrostriatal, was changed. BPC 157 modulates serotonergic and dopaminergic systems, beneficially affects various behavioral disturbances that otherwise appeared due to specifically (over)stimulated/damaged neurotransmitters systems. Besides, BPC 157 has neuroprotective effects: protects somatosensory neurons; peripheral nerve regeneration appearent after transection; after traumatic brain injury counteracts the otherwise progressing course, in rat spinal cord compression with tail paralysis, axonal and neuronal necrosis, demyelination, cyst formation and rescues tail function in both short-terms and long-terms; after NSAIDs or insulin overdose or cuprizone encephalopathies were attenuated along with GI, liver and vascular injuries.ConclusionBPC 157, a gastric peptide, may serve as remedy in various CNS-disorders.

Inhibiting renin angiotensin system in rate limiting step by aliskiren as a new approach for preventing indomethacin induced gastric ulcers

PurposePreviously blocking the renin angiotensin system (RAAS) has been effective in the prevention of gastric damage. Therefore, the aim of this study was to investigate the effects of aliskiren, and thus, direct renin blockage, in indomethacin-induced gastric damage model. MethodsEffects of aliskiren were evaluated in indomethacin-induced gastric damage model on Albino Wistar rats. Effects of famotidine has been investigated as standard antiulcer agent. Stereological analyses for ulcer area determination, biochemical analyses for oxidative status determination and molecular analyses for tissue cytokine and cyclooxygenase determination were performed on stomach tissues. In addition, to clarify antiulcer effect mechanism of aliskiren pylorus ligation-induced gastric acid secretion model was applied on rats. ResultsAliskiren was able to inhibit indomethacin-induced ulcer formation. It also inhibited renin, and thus, decreased over-produced Angiotensin-II during ulcer formation. Aliskiren improved the oxidative status and cytokine profile of the stomach, which was most probably impaired by increased Angiotensin II concentration. Aliskiren also increased gastroprotective prostaglandin E2 concentration. Finally, aliskiren did not change the gastric acidity in pylorus ligation model. ConclusionAliskiren exerted its protective effects on stomach tissue by decreasing inflammatory cytokines and oxidative stress as a result of inhibiting the RAAS, at a rate-limiting step, as well as its end product, angiotensin II. Aliskiren also significantly increased protective factors such as PGE2, but not affect aggressive factors such as gastric acidity.

Synthesis and SAR studies of potent H+/K+-ATPase inhibitors of quinazolinone-Schiff’s base analogues

A series of quinazolinone derived Schiff base derivatives 7–36 were synthesized and characterized by analytical and spectroscopic techniques. The synthesized analogues were screened for their in vitro H+/K+-ATPase inhibition. Most of the compounds showed excellent activity, compared to that of omeprazole, a reference drug. In particular, hydroxy and methoxy derivatives 13–24 were the most active compounds possessing a significant increase for different substituents on the benzene ring thus, contributing positively to gastric H+/K+-ATPase inhibition. Preliminary structure-activity relationship revealed that the compounds 13–24 with electron donating moiety (OH, OCH3) were found to be excellent activity and compounds 9–12 and 25–36 with electron withdrawing moiety (Cl, F, NO2 and Br) were found to be least antiulcer agents.

Plant-Derived Urease Inhibitors as Alternative Chemotherapeutic Agents.

Inhibition of the metalloenzyme urease has important pharmacologic applications in the field of antiulcer and antigastric cancer agents. Urease is involved in many serious infections caused by Helicobacter pylori in the gastric tract as well as by Proteus and related species in the urinary tract. Although numerous studies have described several novel urease inhibitors (UIs) used for the treatment of gastric and urinary infections, all these compounds have exhibited severe side effects, toxicity, and instability. Therefore, to overcome such problems, it is necessary to search for new sources of UIs, such as natural products, that provide reduced side effects, low toxicity, greater stability, and bioavailability. As limited studies have been conducted on plant-derived UIs, this paper aims to highlight and summarize the most promising compounds isolated and identified from plants, such as terpenoids, phenolic compounds, alkaloids, and other substances with inhibitory activities against plant and bacterial ureases; these are in vitro and in vivo studies with an emphasis on structure-activity relationship studies and types of inhibition that show high and promising levels of anti-urease activity. This will aid medicinal chemists in the design and synthesis of novel and pharmacologically potent UIs useful for the development of antiulcer drugs.

Investigation of the Tiger Milk Medicinal Mushroom, Lignosus rhinocerotis (Agaricomycetes), as an Antiulcer Agent.

The aim of this study was to determine the antiulcer activity of Lignosus rhinocerotis in rats. A total of 48 Sprague-Dawley rats were used in ethanol-induced, aspirin-induced, and water immersion-restraint stress-induced ulcer models. Rats were equally divided into 4 groups for each model and orally administered 5 mL/kg distilled water, 20 mg/kg omeprazole, as well as 250 and 500 mg/kg of L. rhinocerotis powder. L. rhinocerotis powder at both 250 and 500 mg/kg doses demonstrated significant (P < 0.05) protection against gastric ulceration in all the induced ulcer models. Histological studies revealed severe damage and hemorrhage of gastric mucosa in the negative control group for all ulcer-induced models. The study suggests that L. rhinocerotis powder possesses dose-dependent antiulcer activity in the gastric mucosa, as ascertained grossly and histologically, compared with the negative control groups.

Phytochemical Investigation and Hypoglycaemic Effect ofAbelmoschus esculentus

From ancient times mankind by virtue of their experience and experiments used to prepare medicine from plants as natural source for the treatment of various diseases. Plant parts were used as panacea as it has been mentioned in charaka samhita (a part of Ayurvedic System of medicine developed in the era of 3000–2000 BC). Plants not only cure the diseases but also can increase the prevention power (immunity) of human body. Therapeutically active components in plant are present most of the time in very low quantity. In recent times, focused on plant research has increased all over the universe and a large number of evidences have been collected to show immense potential of plants used in various pharmaceutical application. Therefore plant sources have become a key target to explore new pharmacologically active compounds and pharmaceutical excipients. Abelmoschus esculentus is growing widely throughout the tropical and temperate region in the world. It is traditionally used in Ayurveda, and Siddha and Unani. Its medicinal usage has been described in several diseases in all medicinal systems. Chemical groups such as cyanidin-3-glucoside; cyaniding-4-glucoside; 5, 7, 3′, 4′-tetrahydroxy-4′′-Omethyl flavonol -3-O-β-D-glucopyranoside; quercetin are mainly believed to be responsible for its various therapeutic actions. It is used as hypoglycaemic, antimicrobial, hypolipidaemic, antioxidant, neuroprotective and antiulcer agents. It is also used as pharmaceutical agents such as suspending, binding agent and mucoadhesive agents. Immature fruits (pods) and seeds of the plant have been used for the formulation of microencapsulated drug delivery system and polysaccharide isolated from it. Therefore it is worthwhile to review its therapeutic properties to give an overview of its status to scientists both modern and ancient. This review also encompasses on the potential applications of the Abelmoschus esculentus (dharosh) plant in the pharmaceutical field due to its wide pharmaceutical activities.

Ulcer healing potential of ethanolic extract of Caralluma attenuata on experimental diabetic rats.

Introduction:Available data indicated that diabetes mellitus (DM) increases the vulnerability of the gastric ulcers and the need of the hour is to develop effective agents to treat ulcer with diabetes for better patient compliance and cost effectiveness. The ulcer-healing properties of ethanolic extract of Caralluma attenuata (CAEt) against both chemically- and physically induced gastric ulcers in experimental rats are recently studied.Aim:To assess the ulcer healing potential of Ethanolic Extract of Caralluma attenuata on Experimental Diabetic Rats.Material and Methods:The current study aimed to evaluate ulcer healing properties of CAEt on the aspirin induced gastric ulcer in rats with streptozotocin induced DM. The hypothesis is based on the fact that DM results in compromising the mucosal defensive factors associated with delay in gastric ulcer healing, and if these changes can be corrected by using agents known for their antidiabetic and antiulcer properties. Experimental albino rats were divided into six groups. Except for Group I, other groups contained streptozotocin-induced diabetic rats. Group I (normal control) and Group II (diabetic control) were administered vehicle, Groups III and IV (diabetic experimental) were administered CAEt in dose of 100 mg/kg and 250 mg/kg, respectively, and Groups V and VI (positive controls) were respectively administered oral standard drugs omeprazole, 20 mg/kg, and tolbutamide 10 mg/kg.Result:The results confirmed that the CAEt significantly decreases the ulcer index (P < 0.05) in the aspirin-induced gastric ulcers and also significantly exhibit antioxidant and glucose lowering activity in the diabetic ulcer rats. The study showed that C. attenuata has the potential to be used as an antiulcer agent in experimental diabetic rats.

The Protective Effect of a &amp;lt;i&amp;gt;Puerariae flos&amp;lt;/i&amp;gt; Extract (Thomsonide) against Ethanol-Induced Gastric Lesions in Rats

Objectives: Puerariae flos has popularly been used to treat alcoholic disorders. However, the effect of Puerariae flos on alcoholic disorders in the gastrointestinal system has not been identified. We investigated the protective effect of an extract of Puerariae flos against the murine gastric mucosa. Methods: Thomsonide, the extracts containing large amounts of isoflavonoid and triterpenoid saponin, was obtained fr om Puerriae flos via Diaion HP-20 column chromatography using water and 99.5% ethanol. It was investigated whether thomsonide, as well as geranylgeranylacetone (teprenone), a popular anti-ulcer agent developed in Japan, had a cytoprotective effect that might be related to endogenous prostaglandins, which played an important role in preventing gastric mucosal lesions. Results: Thomsonide and teprenone inhibited ethanol-induced gastric lesions. Furthermore, thomsonide increased the production of PGE2 and 6-ketoPGF1α, a stable metabolite of PGI2, in the gastric mucosa, and protective effects of thomsonide, as well as teprenone, against ethanol-induced gastric lesions were attenuated by pretreatment with indomethacin. Conclusions: These findings suggest that thomsonide, as well as teprenone, has the gastro protective effect which may be related to the cytoprotective activity of endogenous prostaglandins. The results of this study also suggest that the gastro protective effect of thomsonide may partially mitigate alcoholic disorders in the gastrointestinal tract, and support our pharmacological belief that Puerariae flos is useful for treatment of alcoholic disorders.

Effect of midazolam on gastric secretion and stress-induced gastric ulceration in male albino rats

The term ‘benzodiazepine’ refers to a distinct chemical structure. Benzodiazepines are now used for testing acute anxiety states, and also as a premedication before surgery. Although diazepam is the prototype of benzodiazepine, midazolam is more potent. As peptic ulcers are now being diagnosed more often in school children, and because preanaesthetic management is difficult for children, the use of preoperative sedatives may help to diminish anxiety, minimize psychological trauma and improve the quality of anaesthesia. Midazolam is often used as a preoperative sedative, and during procedures such as endoscopy, where anaesthesia is not required. There is no available data about the effect of various doses of midazolam on gastric secretion and on restraint-induced gastric ulcers in rats. Therefore, the aim of the present study was to study the effect of 0.5, 1 and 2.5 mg/kg of midazolam on gastric secretion and on immobilization-induced gastric stress ulcers in rats. This study was conducted on 48 rats, divided into two big categories, each consisting of 24 rats, which were further divided into four groups, each group consisting of six rats. Administration of midazolam in doses of 0.5 and 1 mg/kg intraperitoneal to pyloric-ligated rats led to a significant decrease in gastric juice volume, acid concentration and the total acid output compared with the control group, which received normal saline. Midazolam administration in a dose of 2.5 mg/kg led to a significant increase in the gastric juice volume, and a significant decrease in the acid concentration and the total acid output compared with the control group. Our results concluded that midazolam administration in a dose of 0.5 mg/kg to children as a prophylactic dose during preanaesthetic medication leads to prevention of aspiration pneumonia, morbidity and mortality of children during endoscopies and elective surgical operations. Restraint-induced stress ulcers approach the ideal technique for ulcer production and testing of antiulcer agents. Our results showed that intraperitoneal administration of midazolam in doses of 0.5, 1 and 2.5 mg/kg to rats in a dose-dependent manner leads to a prophylactic effect against stress-induced gastric ulcers with a protection index of 9.4, 23.8 and 32.2%, respectively. The mechanism of prophylaxis is due to its sedative, anxiolytic and antisecretory effect.

Formulation and Evaluation of Cinitapride Controlled Release Tablets

The present study aimed at Formulation Development and Evaluation of controlled release tablets of Cinitapride for the treatment of ulcer. Cinitapride is a gastroprokinetic agent and antiulcer agent of the benzamide class. It act as an agonist of the 5-HT1 and 5-HT4 receptors and an antagonist of the 5-HT2 receptors. It is used in the treatment of gastrointestinal disorders associated with motility disturbances such as gastro esophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying. The matrix tablets of Cinitapride were prepared using wet granulation. Physical characterization of tablet and powder blends used to form the matrix tablet was under taken using a range of experimental techniques. Granules were evaluated for Bulk density, Tapped density, Compressibility index and Hausner's ratio. Tablets were tested for weight variation, hardness, thickness and friability as per official procedure. The tablets were evaluated for in-vitro drug release profile. Dissolution studies of Cinitapride controlled release tablets in media with different dissolution media 0.1N HCl, Phosphate buffer pH (6.8) as per US Pharmacopoeia. The dissolution data revealed that the ratio of polymers is very important to achieve a optimum formulation. The formulation of Cinitapride CR tablets shown that formulation F23 with Methocel K100M (20%) shown good drug release profile. Formulation F23, shown similar dissolution profile when compared with the marketed product (Cintapro). Stability study of the formulation F23 indicated no significant difference in release profile after a period of 3 months.

Synthesis of novel substituted 4-phenyl-5-phenoxymethyl-3-mercapto-1,2,4-triazole (4 H) derivatives as potential anti-ulcer agents

In this work, the series of new 4-phenyl-5-4-(R)-phenoxymethyl-1,2,4-triazole-3-ylthio-1-(R1)-acetophenones have been synthesized by alkylation of correspondent 4-phenyl-5-phenoxymethyl-3-mercapto-1,2,4-triazoles (4H) with the α-chloroacetophenones. The structure of the synthesized substances has been proven by NMR spectra. High possibility of anti-ulcer and anti-helicobacter activity was determined by the PASS program. Molecular docking and anti-ulcer screening of new 1,2,4-triazole(4H) derivatives on the acute alcohol-prednisolone model NSAID-inducеd ulcers in rats has been performed.

Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms

Ethnopharmacological relevanceCopaifera malmei Harms (Fabaceae) is a plant that occurs in the central region of Brazil, where the plant's leaves infusion is popularly used to treat gastric ulcer and inflammatory diseases. This study was aimed to investigate the gastroprotective activity and mode of action of the plants' leaves infusion in order to establish the scientific basis for such usage, and to assess its potential as a source of an anti-ulcer agent. Materials and methodsLeaves infusion extract of the plant (SIECm) was prepared, freeze dried and lyophilised. Its qualitative and quantitative phytochemical constituents were investigated using TLC and HPLC techniques. The safety profile was evaluated on CHO-k1 epithelial cells viability using the Alamar blue assay, and by acute toxicity test in mice. The gastroprotection and anti-ulcer efficacy of the SIECm (25, 100 and 400mg/kg, p.o.) were tested using acute (acidified ethanol, piroxicam and water restrain stress), and chronic (acetic acid) experimental ulcer models. The plausible mode of action of the SIECm was assessed using gastric secretion, gastric barrier mucus, nitric oxide, and its antioxidant (myeloperoxidase and catalase) effects in mice and rats. The histopathological analyses of the ulcerated tissues as well as the extract’s activity on Helicobacter pylori were also investigated. ResultsPhytochemical tests indicated the presence of mainly phytosterols, phenolics and flavonoids. The SIECm exhibited no cytotoxic effects on the CHO-k1 cells, and no oral acute toxicity in mice. It prevented against the acute induced ulcerations by enhancing gastroprotection through gastric mucus production, NO modulation, antioxidant, reduced gastric secretion and enhanced chronic ulcers healing process, as shown by reduction/prevention of epithelial and vascular damage, in addition to reduction in leucocyte infiltration. The SIECm however did not exhibit activity against H. pylori. ConclusionThe SIECm is safe, contain useful phytochemicals and exhibited significant gastroprotective/anti-ulcer effects. The results justify its folkloric usage, and provided scientific evidence of its potential as a source of new phytodrug to treat gastric ulcers.

Biological Evaluations of some Synthesized Pyrimidothieno [2,3-b] Pyrimidine Candidates as Antiulcer Agents

Biological Evaluations of some Synthesized Pyrimidothieno [2,3-b] Pyrimidine Candidates as Antiulcer Agents

Antiulcer Activities of Securidaca longepedunculata Fres. (Polygalaceae) and Luffa cylindrica Linn. (Cucurbitaceae) in Wistar Rats

Securidaca longepedunculata (SL) and Luffa cylindrica (LC) are medicinal plants commonly used in combination with other recipes in the treatment of many ailments in traditional medicine among the Yoruba ethnic group in Nigeria. In our recent survey, the two plants were among the most frequently mentioned plants for the treatment of gastric ulcer in Ado Odo local government area of Ogun state, Nigeria. This study was designed to examine whether the leaf extracts (methanol, ethylacetate and hexane extracts) of SL and LC possess antiulcer effect in rats. The antiulcer effects of the extracts were assessed using ethanol-induced gastric ulcer model of ulceration in rats. The vehicle, test drug or plant extracts were administered 50 min prior to ulcerogenic procedure. Ulceration was induced in animals with 1 mL absolute ethanol one hour before being sacrificed. Ulcer index, protein content and lipid peroxidation activity of the gastric tissues were determined. The standard antiulcer drug, Cimetidine (50 mg/kg b.w), used as negative control, has percentage protection of 59.4% and the methanol (150 and 300 mg/kg b.w), ethylacetate (150 and 300 mg/kg b.w) and hexane (150 and 300 mg/kg b.w) extracts of SL showed (68.8% and 78.1%) , (93.8% and 87.5%) and (71.9% and 75.0%), protection, respectively. Similarly, the 150 mg/kg b.w ethyl acetate extract of LC gave 78.1% inhibition while the 300 mg/kg ethyl acetate extract revealed 87.5% protection. Further, investigation showed that the extracts increased the protein content in the gastric tissues which suggests an ability to stimulate tissue regeneration. Lipid peroxidation levels were significantly (p&lt;0.05) lowered in the pretreated groups. Taken together, the present study demonstrates that the leaf extracts of SL and LCare possible potent gastro protective and antiulcer agents against ethanol-induced gastric ulcer thus providing evidences that may justify their ethno medicinal uses as antiulcer agentsKeywords: Securidaca longepedunculata, Luffa cylindrica, Ethanol-induced, Ulceration, Gastro Protective