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- ItemSomente MetadadadosIn vivo inhibition of gastric acid secretion by the aqueous extract of Scoparia dulcis L. in rodents(Elsevier B.V., 2007-05-04) Mesia-Vela, Sonia; Bielavsky, Monica; Brandao Torres, Luce Maria; Freire, Sonia Maria; Lima-Landman, Maria Teresa R.; Souccar, Caden; Lapa, Antonio Jose; Universidade Federal de São Paulo (UNIFESP)The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4 h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). the AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H+,K+-ATPase with an IC50 of 500 mu g/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED50 = 313 mg/kg, p.o.) and ethanol (ED50 = 490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances. (c) 2006 Elsevier Ireland Ltd. All rights reserved.
- ItemSomente MetadadadosInhibition of gastric acid secretion by the aqueous extract and purified extracts of Stachytarpheta cayennensis(Georg Thieme Verlag, 1997-02-01) Mesia-Vela, Sonia [UNIFESP]; Souccar, C.; LimaLandman, MTR; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP)Stachytarpheta cayennensis Schauer (Verbenaceae) is used in folk medicine to treat gastric and intestinal disturbances. the freeze-dried aqueous extract of the whole plant tested to rodents up to the dose of 2 g kg(-1), p.o., did not produce signs of toxicity. the extract (0.5-2 g kg(-1), p.o.) increased the intestinal motility and protected mice against ulcers induced by restraint-in-cold, ethanol or indomethacin. Injected into the duodenal lumen the extract inhibited the basal acid secretion as well as that induced by histamine and bethanecol in pylorus-ligated mice. Partition of the aqueous extract in organic solvents yielded semipurified fractions whose antiacid activity guided further chemical purification. All the fractions were chromatographically characterized, the main substances in the active extract being flavonoids and amines; some substances were revealed only under UV light. the most purified active fraction obtained presented a specific activity 5-10 times higher than that detected in the original extract. Data from pharmacological studies indicate that the antiulcer activity of S. cayennensis is related to a specific inhibition of gastric acid secretion. Cholinergic and histaminergic stimulation of acid secretion were similarly reduced by the extracts suggesting inhibition of common steps in both pathways, possibly at the level of histamine release/H-2 receptor interaction, or at the proton pump. Whatever the mechanisms involved, the present data confirm the plant effectiveness as antiacid/antiulcer and laxative.
- ItemSomente MetadadadosPharmacological study of Stachytarpheta cayennensis Vahl in rodents(Urban & Fischer Verlag, 2004-11-01) Mesia-Vela, S.; Souccar, C.; Lima-Landman, MTR; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP)Freeze-dried aqueous extracts (AEs, 0.1-1 g/kg body wt., p.o.) obtained from entire or selected parts of Stachytarpheta cayennensis were tested for their effects on gastric secretion, gastric motility, inflammation and pain in rodents, with the purpose of validating the plant's ethnomedical uses. the AE-Total, AE-Flowers and AE-Leaves but not AE-Stems inhibited the gastric acid secretion in pylorus-ligated rats with varying potency. Purification of AEs yielded the semipurifed fractions EtFs rich in iridoids. All the EtFs with exception of EtF-Stems inhibited gastric acid secretion of pylorus ligated mice. While AE-Total stimulated the intestinal transit of mice by 43%, AE-eaves delayed it by 38%. These effects on intestinal transit were not observed when the EtFs were tested. Only AE-Leaves and AE-Flowers altered the gastric emptying of semisolids, increasing it by 45% and 69%, respectively. These results indicate that the compounds related to inhibition of gastric acid secretion and gastrointestinal motility are different. the AE-Total reduced abdominal writhing induced by acetic acid potently (ED50 value = 700 mg/kg, p.o.) without altering the writhes induced by acetylcholine. Attempts to identify the mechanism of analgesia were unsuccessful since the AETotal did not show analgesic effects when tested in different models of pain such as formalin and capsaicin or the tailflick test. Pretreatment of animals with AE-Total did not show antiinflammatory activity in any of the acute (paw edema induced by carrageenin, dextran or histamine, pleurisy induced by carrageenin and capsaicin-induced mouse ear edema) or chronic (air pouch) models used. No toxic signs were observed after administration of the different extracts up to 2 g/kg body wt., p.o.Collectively, the results confirmed folk information indicating presence of analgesic, mild laxative and potent inhibition of gastric secretion activities in the aqueous extracts of S. cayennensis. the results do not, however confirm the folk use of the plant as an antiinflammatory medicine. (C) 2004 Elsevier GmbH. All rights reserved.
- ItemSomente MetadadadosSolanum paniculatum L. (Jurubeba): Potent inhibitor of gastric acid secretion in mice(Urban & Fischer Verlag, 2002-09-01) Mesia-Vela, S.; Santos, M. T.; Souccar, C.; Lima-Landman, MTR; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP)Solanum paniculatum L. is used commonly in Brazilian folk medicine for the treatment of liver and gastrointestinal disorders. the freeze-dried aqueous extracts (WEs) obtained from distinct parts of the plant (flowers, fruits, leaves, stems and roots) were tested to determine their antiulcer and antisecretory gastric acid activities using mice. the aqueous extracts of roots, stems and flowers inhibited gastric acid secretion in pylorus-ligated mice with ED50 values of 418, 777 and 820 mg/kg body wt. (i.d.), respectively. Extracts of leaves (0.5-2 g/kg body wt., Ld) did not affect gastric secretion, whereas fruit extracts (0.5-2 g/kg body wt., U) stimulated gastric acid secretion. the stimulatory effect of the fruit extract was inhibited by pretreatment with atropine (5 mg/kg body wt., i.m.) but not with ranitidine (80 mg/kg body wt., i.p.) suggesting that the fruit extract activates the muscarinic pathway of gastric acid secretion. in contrast, administration of the root extract into the duodenal lumen inhibited histamine- and bethanechol-induced gastric secretion in pylorus-ligated mice. in addition, the aqueous extract of roots (ED50 value, 1.2 g/kg body wt., p.o.) protected the animals against production of gastric lesions subsequent to the hypersecretion induced in mice by stress following cold restraint. This effect was not reproduced when the lesions were induced by blockade of prostaglandins synthesis via subcutaneous injection of indomethacin. Thus, antiulcer activity of the plant extracts appears to be related directly to a potent anti-secretory activity. No toxic signs were observed following administration of different extracts up to 2 g/kg body wt., p.o. Collectively, the results validate folk use of Solanum paniculatum L. plant to treat gastric disorders.