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- ItemSomente MetadadadosEvaluation of Baccharis trimera and Davilla rugosa in tests for adaptogen activity(Wiley-Blackwell, 2007-06-01) Mendes, Fulvio Rieli; Tabach, Ricardo [UNIFESP]; Carlini, E. A.; Universidade Federal de São Paulo (UNIFESP)Baccharis trimera (Asteraceae) and Davilla rugosa (Dilleniaceae) are used popularly as tonics, aphrodisiacs and for stomach ailments, among other uses. Hydroallcohol extracts of the aerial parts of both plants were investigated with regard to their chemical constitution and their pharmacological activity in tests that evaluate adaptogen activity. Alkaloids, flavonoids, saponins, polyphenols/tannins and coumarins were identified in both extracts, while lignans were found only in the extract of Davilla rugosa. This extract presented also a marked antioxidant activity and exerted a moderate antiulcer effect in rats submitted to cold immobilization stress. It did not, however, inhibit the increase in the levels of ACTH and corticosterone induced by stress. Moreover, the Davilla rugosa did not improve the physical performance of mice submitted to forced exercise and the learning time of old rats in the T-maze, neither did it reduce the blood viscosity of the old animals. Conversely, the Baccharis trimera extract only presented a moderate antioxidant activity, without any positive effect on the other tests. These results point to the absence of an adaptogen activity of Baccharis trimera, with some effects that could be related to such an activity as regards the Davilla rugosa. Copyright (C) 2007 John Wiley & Sons, Ltd.
- 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 a standardized aqueous extract of Cecropia glaziovii Sneth and underlying mechanism(Elsevier B.V., 2008-06-01) Souccar, C. [UNIFESP]; Cysneiros, Roberta Monterazzo [UNIFESP]; Tanae, M. M. [UNIFESP]; Torres, L. M. B. [UNIFESP]; Lima-Landman, M. T. R. [UNIFESP]; Lapa, A. J. [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)Cecropia glazioui Sneth (Cecroplaceae) is used in folk medicine in tropical and subtropical Latin America as cardiotonic, diuretic, hypotensive, anti-inflammatory and anti-asthmatic. the hypotensive/antihypertensive activity of the plant aqueous extract (AE) and isolated butanolic fraction (BuF) has been confirmed and putatively related to calcium channels blockade in vascular smooth musculature [Lapa, AJ., Lima-Landman, M.T.R., Cysneiros, R.M, Borges, A.C.R., Souccar, C., Barreta, I.P., Lima, T.C.M., 1999. the Brazilian folk medicine program to validate medicinal plants - a topic in new ant1hypertensive drug research. In: Hostettman, K., Gupta, M.P., Marston, A. (Eds.), Proceedings Volume, IOCD/CYTED Symposium, PanamA City, PanamA, 23-26 February 1997. Chemistry, Biological and Pharmacological Properties of Medicinal Plants from the Americas. Harwood Academic Publishers, Amsterdam, pp. 185-196; Lima-Landman, M.T., Borges, A.C., Cysneiros, R.M., de Lima, T.C., Souccar, C., Lapa, A.J., 2007. Anti hypertensive effect of a standardized aqueous extract of Cecropia glaziovii Sneth in rats: an in vivo approach to the hypotensive mechanism. Phytomedicine 14, 314-320]. Bronchodilation and antidepressant-like activities of both AE and BuF have been also shown (Delarcina, S., Lima-Landman, M.T., Souccar, C., Cysneiros, R.M., Tanae, M.M., Lapa, AJ., 2007. Inhibition of histamine-induced bronchospasm in guinea pigs treated with Cecropia glaziovi Sneth and correlation with the in vitro activity in tracheal muscles. Phytomedicine 14, 328-332; Rocha, F.F., Lima-Landman, M.T., Souccar, C., Tanae, M.M., de Lima, T.C., Lapa, A.J., 2007. Antidepressant-like effect of Cecropia glazioui Sneth and its constituents - in vivo and in vitro characterization of the underlying mechanism. Phytomedicine 14, 396-402]. This study reports the antiulcer and antisecretory gastric acid activities of the plant AE, its BuF and isolated compounds with the possible mechanism involved. Both AE and BuF were assayed on gastric acid secretion of pylorus-ligated mice, on acute models of gastric mucosal lesions, and on rabbit gastric H(+), K(+) -ATPase preparations. Intraduodenal injection of AE or BuF (0.5-2.0g/kg, i.d) produced a dose-related decrease of the basal gastric acid secretion in 4-h pylorus-ligated mice. At 1.0 g/kg, BuF decreased the volume (28%) and total acidity (33%) of the basal acid secretion, and reversed the histamine (2.5 mg/kg, s.c.)- or bethanecol (1.0 mg/kg, s.c.)-induced acid secretion to basal values, indicating inhibition of the gastric proton pump. Pretreatment of mice with the BuF (0.05-0.5 g/kg, p.o.) protected against gastric mucosal lesions induced by 75% ethanol, indomethacin (30mg/kg, s.c.) or restraint at 4 degrees C. BuF also decreased the gastric H(+), K(+)-ATPase activity in vitro proportionately to the concentration (IC(50) = 58.8 mu g/ml). the compounds isolated from BuF, consisting mainly of cathechins, procyanidins and flavonoids [Tanae, M.M., Lima-Landman, M.T.R., de Lima, T.C.M., Souccar, C., Lapa, AJ., 2007. Chemical standardization of the aqueous extract of Cecropia glaziovii Sneth endowed with anti hypertensive, bronchodilator, antacid secretion
- 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 and Toxicological Study of Maytenus ilicifolia Leaf Extract. Part I - Preclinical Studies(Wiley, 2017) Tabach, Ricardo [UNIFESP]; Duarte-Almeida, Joaquim M. [UNIFESP]; Carlini, Elisaldo A. [UNIFESP]One of the Brazilians medicinal plants most cited in ethnopharmacological surveys for the treatment of ulcers and gastric diseases was evaluated for its efficacy and toxicity. Maytenus ilicifolia leaf extract (MIE) was acutely and chronically (180days) administered to rats, mice, and dogs. Acute tests were antiulcer effect and toxicological trials (observational pharmacological screening, LD50, motor coordination, sleeping time and motor activity). Chronic tests were the following: weight gain/loss and behavioral parameters in rats and mice
- 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.