Efecto gastroprotector y antisecretor de un fitofármaco de hojas de matico (Piper aduncum) / Gastroprotective and antisecretory effect of a phytochemical made from matico leaves (Piper aduncum)

Objetivos. Determinar el efecto gastroprotector y antisecretor del extracto etanólico de las hojas de matico (Piper aduncum) en modelos animales. Materiales y métodos. Para la evaluación del efecto gastroprotector se utilizó 220 ratones de la cepa Balb C57, los cuales fueron aleatorizados en 22 grupos de diez animales, a los cuales se les indujo la formación de úlceras gástricas con indometacina, la gastroprotección se determinó a través de tres aspectos: inflamación, número de bandas hemorrágicas y número de úlceras. Para evaluar el efecto antisecretor se utilizó 64 ratas albinas machos Holtzman, los cuales fueron aleatorizados en ocho grupos de ocho animales, un control y siete grupos de tratamiento con un nivel de dosis de los extractos y dos niveles de dosis en los fitofármacos; la antisecreción se realizó con el ensayo de ligazón pilórica. Resultados. Para la gastroprotección, los extractos de diclorometano, cloroformo, hexano y metanol, lograron una disminución de la inflamación de más del 66% (p<0,05); el extracto etanólico presenta una actividad de 100% para disminuir el número de bandas hemorrágicas (p<0,05); el extracto clorofórmico presenta una actividad antiulcerosa de 75% (p<0,05). Respecto a la antisecreción, el fitofármaco en cápsulas conteniendo el extracto etanólico logró un 72% de reducción del volumen de la secreción gástrica (p<0,01) y un incremento del pH en 104,3% (p<0,01). Conclusiones. En condiciones experimentales los extractos etanólico, sus fracciones y su fitofármaco son gastroprotectores en ratones y antisecretores en ratas.

Objectives. To determine the gastroprotective and antisecretory effect of ethanol extract from matico leaves (Piper aduncum) in animal models. Materials and methods. To evaluate the gastroprotective effect, 220 mice of the Balb C57 strain were used. They were randomized in 22 groups of ten animals each, in which the formation of gastric ulcers was induced with indomethacin. Gastroprotection was determined by evaluating three aspects: inflammation, number of hemorrhagic shocks and number of ulcers. To evaluate the antisecretory effect, 64 white male Holtzman rats were used, which were randomized in eight groups of eight animals, one control and seven groups of treatment with one extract dose level and two phytochemical dose levels. Antisecretion was obtained through the pylorus ligation. Results. Regarding gastroprotection, dichloromethane, chloroform, hexane and methanol extracts decreased inflammation to over 66% (p<0,05). The ethanolic extract shows 100% activity in reducing the number of hemorrhagic bands (p<0,05). The chloroform extract shows antiulcer activity at 75% (p<0,05). In terms of antisecretion, the phytochemical in capsules containing the ethanolic extract achieved 72% reduction of the gastric secretion volume (p<0,01) and 104,3% (p<0,01) PH increase. Conclusions. In experimental conditions, ethanolic extracts, their fractions and phytochemicals have a gastroprotective effect in mice and antisecretory effect in rats.

Anti-ulcer & antioxidant activities of Hedranthera barteri {(Hook F.) Pichon} with possible involvement of H+, K+ ATPase inhibitory activity.

Background & objective: Hedranthera barteri (HB) is used in folk medicine as a vermifuge, laxative and an anti-inflammatory agent. The aim of this study was to evaluate the anti-ulcer and antioxidant properties of the dichloromethane fraction of HB root (DMHBR). Methods: Anti-ulcerogenic activity was assessed in cold-restraint (CRU), aspirin (ASP), alcohol (AL), pyloric ligation (PL) induced gastric ulcer models in rats and histamine-induced duodenal ulcer (HST) in guinea pigs. The effect of DMHBR (100 mg/kg) on gastric juice for free and total acidity, peptic activity and mucin secretion, using the pylorus ligated model, were evaluated. The H+, K+-ATPase activity was assayed in gastric microsomes, spectrophotometrically. The in vitro anti-oxidant assays were explored through DPPH, nitric oxide, hydroxyl radical, superoxide anion scavenging assays. Results: DMHBR reduced the incidence of ulcers in CRU (63.3%), PL (58.5%), ASP (52.7%), HST (75.0%) and AL (53.87%). Also, reductions were observed in the free acidity (49.4%), total acidity (45.8%) and peptic activity (32.9%) with increase in the mucin secretion by 81.6 per cent. DMHBR (60-100 μg/ml) inhibited the H+,K+-ATPase activity with IC50 of 89.64 μg/ml compared with omeprazole (10-50 μg/ml ) with IC50 of 32.26 μg/ml. DMHBR showed antioxidant activity with IC50 values of DPPH (397.69 μg/ml), nitric oxide (475.88 μg/ml), hydroxyl radical (244.22 μg/ml) and superoxide anion radical (285.20 μg/ml). Interpretation & conclusion: DMHBR showed anti-ulcer activity against experimentally-induced peptic ulcer models and exhibited both cytoprotective and anti-secretory property. It exhibited a proton pump inhibition activity and its anti-ulcer properties may be partly ascribed to its antioxidant activities.

[ effect of omeprazol and ranitidine on gastric acidity in ICU patients]

ICU patients especially those under mechanical ventilation or with a history of coagulation disorders are at the risk of stress ulcer development and related GI bleeding. Typically H2 blockers administration showed prophylactic role to control gastric acidity. Preliminary studies have shown that administration of intravenous omeperazol is effective. The object of this study was to compare the effect of oral rout administration of omerprazol with intravenous ranitidine on gastric pH. In this experimental study 40 ICU patients under mechanical ventilation allocated into same conditions and matched ranitidine and omeprazol groups [20 subjects in each group]. First group received 50 mg intravenous ranitidine twice per day and the second group received 40 mg oral omeperazol once a day. The gastric acidity was monitored using Chroning method. Gastric pH was determined before administration and three times per day after drugs administration then followed for three consequent days. Data was analyzed using T-test and SPSS software. The mean gastric pH in the Ranitidine group was 2.07 +/- 0.79 before and 2.80 +/- 0.85 after drug administration. In the Omperazol group gastric pH was 2.01 +/- 1.52 before and 3.90 +/- 1.52 after drug administration. The oral Omeperazol administration was significantly effective than intravenous Ranitidine administration [p<0.005]. Our data suggest that in critically ill patients oral rout administration of Omeparazol is more effective than intravenous H2 blocker [Ranitidine] to decrease gastric acidity and may prevent from stress ulcer

Effect of the tetracyclic antidepressant maprotiline ongastric secretion and ethanol induced ulcer in rats

The effect of maprotiline [a tetracyclic antidepressant] in a dose of 5 mg/kg, orally for 21 days on gastric secretions and ethanol induced gastric ulcer was tested in rats. Maprotiline decreased the volume, free and total HCI acid concentration and peptic activity. While it produced an increase in mucin content as compared with the control group. Moreover, Maprotiline pretreatment [5 mg/kg, daily for 21 days orally] decreased the ulcer index of ethanol induced ulcer by 59.2%. The data suggest that Maprotiline in the tested dose had acid-pepsin antisecretory effect and ulcer protective activity against ethanol induced ulcer. These effects may be mediated through anticholinergic, antihistaminergic and the possible antidopaminergic effects of Maprotiline

Comparison of the effects of oral ranitidine, famotidine and omeprazole on gastric volume and pH

This study compared the efficacy of ranitidine, famotidine and omeprazole at reducing gastric secretion in elective surgical patients. Seventy patients ASA 1 and 2 scheduled to undergo elective surgery under general anesthesia were randomly allocated to receive one of two regimens for orally administered chemoprophylaxis against acid aspiration: famotidine 40 mg, ranitidine 150 mg or omeprazole 40 mg orally the night before the operation or supplemented by the same dose 2 hours before the operation. Intragastric pH and volume were measured immediately after induction of anesthesia. Three drugs caused significant decreases in volume and acidity of gastric contents when compared to placebo [p <0.05]. Patients receiving omeprazole had a higher pH and a lower volume than those receiving either famotidine or ranitidine. The double dose regimen proved to be superior to the single dose regimen. It was concluded that orally administered omeprazole in a dose of 40 mg the night before surgery supplemented by another 40 mg dose 2 hours before surgery appears to be superior to both ranitidine and famotidine in providing some protection from aspiration pneumonia

Effect of a mucolytic agent on gastric secretory functions

To explore the effects of carbocysteine drug, a mucolytic one, on the secretory functions of stomach, this study was carried out on 20 adult persons of both sexes aged between 25-50 years. All persons were subjected to the determination of free and total acidity, mucin content and peptic activity in their fasting gastric juice samples taken before and after two weeks of carbocysteine administration. The results revealed that there is a significant decrease of total gastric acidity, while the free acidity was nonsignificantly decreased. However, the mucin content and the peptic activity were nonsignificantly increased. Also, there was a significant inverse correlation between the mucin content and both of free and total acidity. It was concluded that carbocysteine does not affect the gastric secretory functions and may have a beneficial effect on the gastric mucosa as it helps tissue repair

Effect of calcium on basal and stimulated gastric secretion

The role of extracellular calcium in the control of basal and stimulated gastric secretion was studied by using the Ca[++] channel blocker, verapamil. The volume of gastric secretion [in ml], free and total acidity [as unit%] and peptic activity [as unit/ml] were the parameters used to assess gastric function. All the drugs were given intraperitoneally every day for four successive days. The results demonstrated a stimulatory effect of prednisolone [25 mg/kg] and histamine [1 mg/kg] on gastric secretion. Verapamil [7 mg/kg] resulted in significant decrease in basal gastric secretion. Still, verapamil inhibited the stimulatory effect of prednisolone and histamine on basal gastric secretion. This inhibition was significantly more on prednisolone than histamine simulated gastric secretion, an interesting finding that needs further clarification. The mechanism of the inhibitory effect of verapamil could be through inhibiting the action of H[+] - K[+] ATPase enzyme or due to inhibiting transmembrane flux of Ca[++] ion which is necessary for the process of gastric secretion

Effect of pretreatment with labetalol on gastric secretions altered by ethanol administration

The present work was carried out on 80 pylorus ligated rats to study the effects of oral 50% ethanol [1 ml/150 g rat] for a period of 3 hours on gastric secretion and the effect of pre-treatment with graded doses of labetalol administered by intraperitoneal [IP] route before oral ethanol on the same parameters. The collected gastric juice was analyzed for volume [ml], titratable acidity [Meq/l], total acid output [Meq/h], pepsin concentration [mg/ml] and glycoprotein content [mg hexose/ml]

Antiulcerogenic and anti-inflammatory effects of emodin, isolated from Rhamnus triquerta wall.

Emodin, an anthraquinone derivative, isolated from the whole plant of R. triquerta, in 15 mg/kg dose (ip) exhibited anti-inflammatory activity against carrageenin-induced pedal inflammation in rats. In the same dosage it also showed antiulcer activity against 4 hr pylorus-ligated, aspirin and immobilization stress-induced gastric ulcers in rats. It decreased acid and pepsin output and augmented mucus secretion in terms of total carbohydrate: protein ratio in the gastric juice of aspirin treated pylorus-ligated rats, indicating that the antiulcerogenic effect of emodin may be due to its effect on gastric secretion.

Effect of nabumetone [reliflex], indomethacin and naproxen on the gastric secretion and on the incidence of gastric ulceration in experimental animals

In the present work, nabumetone [Relifex]; a new non steroidal antiinflammatory drug is compared with the well established NSAIDS drugs; indomethacin and naproxen on gastric secretion and the incidence of gastric ulceration. Indomethacin and naproxen caused gastric ulcer in 100% of two groups of rats receiving the drugs. The mean ulcer score and index was 3.5 +/- 0.27 and 350 for the group receiving indomethacin while it was 2.5 +/- 0.27 and 250 for the naproxen group. On the other hand, rats receiving nabumetone showed only 33% incidence of ulceration, 0.33 +/- 0.26 for mean ulcer score and 10.89 was the ulcer index. In addition, there is an increase in the mean acid output and the mean acid concentration in the stomach of rats receiving indomethacin and naproxen compared to the control group. Rats treated with nabumetone showed decreased mean acid concentration and output. These results may be attributed to a less effect of nabumetone on the gastric prostaglandin synthetase inhibitory enzyme, in addition to a lack of its effect on bleeding time and platelet function

Effects of metoclopramide and ranitidine on gastric fluid volume and its acidity.

The effects of metoclopramide 10 mg and ranitidine 150 mg on gastric fluid volume and its pH are studied when given orally either alone or in combination, 3 hours before induction of anaesthesia in adult surgical patients. The study shows that metoclopramide causes reduction of gastric fluid volume but does not elevate its pH. Ranitidine elevates the pH of gastric fluid satisfactorily in all cases, but reduces the gastric volume below the critical level only in 50% cases. A combination of the said two drugs offered most satisfactory protection against acid aspiration syndrome almost in all cases. This regime seems to be superior to either ranitidine or metoclopramide alone in order to reduce the risk factors for aspiration of gastric contents.

Efectos del aloe barbadensis sobre las lesiones y la secreción gástricas producidas por etanol y estrés en ratas / Effect of aloe barbadensis on lesions and gastric secretion produced by ethanol and stress in rats

Se estudia el efecto de extractos de Aloe barbadensis sobre las lesiones gástricas producidas por 2 modelos de úlcera gástrica experimental en ratas. Se usaron 2 extractos, uno preparado en dosis de 10 y 20 mg y otro preparado en dosis de 12,5 y 25 mg sobre las lesiones gástricas producidas por los modelos de etanol y de estrés por inmovilización más frio. También se estudió la secreción gástrica. Las dosis de 20 mg produjo frente al efecto dañino del etanol una discreta disminuciòn del número de lesiones así como una disminuciòn significativa del índice de lesión. La administración de las dosis de 25 mg provocó frente al daño del etanol una disminucion significativa, tanto del número como de la severidad de las lesiones. La dosis de 12,5 mg no protegió a la mucosa de la acción del etanol. La administración por vía intraperitoneal de este extracto no protegió la mucosa gástrica del daño producido por el estrés por inmovilización más frio y produjo una disminuciòn de la acidez total y un aumento del pH del jugo gástrico significativos, mientras que la administraciòn por vía oral produjo una disminuciòn significativa tanto del número de lesiones como del índice de lesión y no ocasionó modificaciones en la secreción gástrica

Immunopharmacological studies on Picrorhiza kurroa Royle ex Benth. Part VI: Effect on anaphylactic activation events in rat peritoneal mast cells.

Mechanism of inhibition of mast cell anaphylaxis by P. kurroa-extract (PK) treatment in rats was investigated. Mast cell-IgE binding, assessed from induction of passive sensitization, was not affected. Calcium-independent early activation events in mast cell anaphylaxis indicated on inhibitory influence of PK-treatment. Inhibition of membrane-protease release by PK-treatment was suggested by study of gastric secretion and exhibition of saturable synergism with Di-isopropyl fluoro phosphate on inhibition of anaphylactic degranulation. pH-independence of mast cell stabilizing effect negates any PK-influence on phospholipid transmethylation. The results complement findings of earlier studies on indirect effects of PK through alteration of membrane structure/function.

Citoprotección gástrica por cromoglicato disódico y RS-7540 / Gastric cytoprotection by disodium chromoglycate and RS-7540

Se estudió el efecto de la droga RS-7540 sobre la secreción gástrica en ratas sometidas a ligadura del piloro por una hora. Se comparó, con la utilización de dosis equimolares (2,0. 10 mol/kg) la acción del CGDS con li de la droga RS-7540 en el modelo de inducción de lesiones por etanol al 96% Se encontró que la droga RS-7540 no inhibió significativamente el volumen ni la acidez de la secreción gástrica y protegió la mucosa gástrica de las lesiones inducidas por etanol al 96%, por lo que tiene un efecto citoprotector. No existen diferencias significativas sobre el efecto citoprotector de la droga RS-7540 y del cromoglicato disódico. La administración simultánea de ambas drogas no aumenta la protección de la mucosa gástrica