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- ItemAcesso aberto (Open Access)Analgesic activity of a triterpene isolated from Scoparia dulcis L. (vassourinha)(Instituto Oswaldo Cruz, Ministério da Saúde, 1991-01-01) Freire, Sonia Maria de Farias; Torres, Luce Maria Brandão [UNIFESP]; Roque, Nidia Franca; Souccar, Caden [UNIFESP]; Lapa, Antonio José [UNIFESP]; UFMA Departamento de Fisiologia; UFMA Departamento de Química; Universidade de São Paulo (USP); Universidade Federal de São Paulo (UNIFESP)Analgesic and anti-inflammatory activities of water (WE) and ethanolic (EE) extracts of Scoparia dulcis L. were investigated in rats and mice, and compared to the effects induced by Glutinol, a triterpene isolated by purification of EE. Oral adminsitration (p.o.) of either WE or EE(up to 2 g/Kg) did not alter the normal spontaneous activity of mice and rats. The sleeping time induced by sodium pentobarbital (50 mg/Kg, i.p.) was prolonged by 2 fold in mice pretreated with 0.5 g/Kg EE, p.o. Neither extract altered the tail flick response of mice in immersion test, but previous administration of EE (0.5 g/Kg, p.o.) reduced writhings induced by 0.8% acetic acid (0.1 ml/10 g, i.p.) in mice by 47% EE (0.5 and 1 g/Kg, p.o.) inhibited the paw edema induced by carrageenan in rats by respectively 46% and 58% after 2 h, being ineffective on the paw edema induced by dextran. No significant analgesic or anti-edema effects were detected in animals pretreated with WE (1 g/Kg, p.o.). Administration of Glutinol (30 mg/Kg, p.o.) reduced writhing induced by acetic acid in mice by 40% and the carrageenan induced paw edema in rats by 73%. The results indicate that the analgesic activity of S dulcis L. may be explained by explained by an anti-inflammatory activity probably related to the triterpene Glutinol.
- ItemSomente MetadadadosAnalgesic and antiinflammatory activities of the aqueous extract of Plantago major L.(Swets Zeitlinger Publishers, 1997-04-01) Guillen Nunez, Maria Elena [UNIFESP]; Emim, Jose Artur da Silva [UNIFESP]; Souccar, Caden [UNIFESP]; Lapa, Antonio José [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)This study aimed to validate the pharmacological effects of Plantago major L., a medicinal plant used to decrease pain and inflammation. The aqueous extract (AE) was prepared from the dried ground leaves. Pretreatment with AE (1 g/kg, p.o.) decreased writhing induced by acetic acid in mice but it did not change the tail Pick responses to heat nociceptive stimuli. In rats, AE (1 g/kg, p.o.) reduced the paw edema and pleurisy induced by carrageenin, but it did not alter the paw edema induced by dextran. The effect of AE on the carrageenin inflammatory responses was more intense than that obtained on the ear edema induced by croton oil in mice. In addition, daily treatment with AE (1 g/kg/day during 8 days, p.o.) inhibited the exudative process induced by croton oil injected into the air pouch of rats. The results indicate that the aqueous extract of Plantago major is endowed with effective antiinflammatory and analgesic activities.
- ItemSomente MetadadadosAntidepressant-like effect of Cecropia glazioui Sneth and its constituents - in vivo and in vitro characterization of the underlying mechanism(Elsevier B.V., 2007-06-01) Rocha, F. F.; Lima-Landman, M. T. R.; Souccar, C.; Tanae, M. M.; De Lima, T. C. M.; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP); Universidade Federal de Santa Catarina (UFSC)The present study aimed to characterize the antidepressant-like effect of a standardized aqueous extract (AE) of Cecropia glazioui Sneth and its purified fractions on in vivo (forced swimming test), ex vivo (hippocampal monoamines levels) and in vitro (serotonin, noradrenaline and dopamine uptake) tests, searching for the active principles and the underlying mechanisms of action. Treatment with AE, or with its butanolic fraction (BuF), the latter rich in catechins, procyanidins and flavonoids, reduced the immobility of rats in the forced swimming test indicating an antidepressant-like effect. Biochemical analysis of the hippocampal neurotransmitters in BuF-treated rats showed significant increase in monoamines levels. BuF and six of its purified constituents inhibited the uptake of [H-3]-serotonin, [H-3]-dopamine and [H-3]-noradrenaline by synaptosomes of different brain regions. Catechin, catechin (4 alpha -> 8) ent-catechin (Procyanidin B3 isomer) and epicatechin (4 beta -> 8) epicatechin (Procyanidin B2) were the most active compounds. Comparatively, the uptake of [H-3]-noradrenaline was the most affected. These results show that the antidepressant-like effect promoted by C. glazioui extract is most likely due to the blockade of the monoamines uptake in the CNS. (C) 2007 Elsevier GmbH. All rights reserved.
- ItemAcesso aberto (Open Access)Effect of Potato virus X on total phenol and alkaloid contents in Datura stramonium leaves(Grupo Paulista de Fitopatologia, 2008-02-01) Duarte, Lígia Maria Lembo; Salatino, Maria Luiza Faria; Salatino, Antonio; Negri, Giuseppina [UNIFESP]; Barradas, Maria Mércia; Instituto Biológico Centro de Pesquisa e Desenvolvimento de Sanidade Vegetal; University of São Paulo Institute of Biosciences; Universidade Federal de São Paulo (UNIFESP)The present paper reports results of the effect of Potato virus X (PVX) on the contents of total phenols and alkaloids in leaves of Datura stramonium. A significant decrease in the contents of phenols and alkaloids was observed in leaves inoculated with PVX (X-I). However, there was an increase in the percentage of phenols in leaves rubbed with phosphate buffer (C1-I) and in leaves from the nodes immediately above, possibly induced by mechanical injury. Gas chromatography/mass spectroscopy revealed amounts of scopolamine in samples submitted to all treatments, except X-I, in which the amount of this alkaloid was low. High amounts of an unidentified compound (molecular ion m/z 302 and a prominent peak at m/z 129) were noted in extracts from leaves X-I, C1-I and leaves from the nodes immediately above the leaves inoculated with PVX. It is suggested that the synthesis and accumulation of the unidentified compound is a result of stress from mechanical injury and virus inoculation.
- ItemSomente MetadadadosEvaluation of the antiurolithiatic activity of the extract of Costus spiralis Roscoe in rats(Elsevier B.V., 1999-08-01) Viel, Tãnia Araujo [UNIFESP]; Domingos, Cristina Diogo [UNIFESP]; Monteiro, Ana Paula da Silva [UNIFESP]; Lima-Landman, Maria Teresa Riggio [UNIFESP]; Lapa, Antônio José [UNIFESP]; Souccar, Caden [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)The antiurolithiatic activity of the water extract of Costus spiralis Roscoe was tested on formation of calculi on implants of calcium oxalate crystals or zinc disc in the urinary bladder of rats. The plant is a species from the family Zingiberaceae used in Brazilian folk medicine in urinary affections and for expelling urinary stones. Implantation of the foreign body in the urinary bladder of adult rats induced formation of urinary stones and hypertrophy of the smooth musculature. Oral treatment with the extract of Costus spiralis Roscoe (0.25 and 0.5 g/kg per day) after 4 weeks surgery reduced the growth of calculi, but it did not prevent hypertrophy of the organ smooth musculature. The contractile responses of isolated urinary bladder preparations to the muscarinic agonist bethanecol, in the presence and absence of the extract (0.3-3 mg/ml) or atropine (0.3-3 nM) did not differ among the experimental groups. The results indicate that the extract of Costus spiralis Roscoe is endowed with antiurolithiatic activity confirming thus folk information. The effect, however, was unrelated to increased diuresis or to a change of the muscarinic receptor affinity of the bladder smooth musculature to cholinergic ligands, (C) 1999 Elsevier Science Ireland Ltd. All rights reserved.
- ItemSomente MetadadadosEvaluation of the anxiolytic-like effects of Cecropia glazioui Sneth in mice(Elsevier B.V., 2002-01-01) Rocha, F. F.; Lapa, A. J.; De Lima, TCM; Universidade Federal de Santa Catarina (UFSC); Universidade Federal de São Paulo (UNIFESP)Cecropia glazioui Sneth has been used in most Latin American countries as an antihypertensive, cardiotonic, and antiasthmatic folk medicine. in the cardiovascular studies to define its antihypertensive action it was noteworthy that animals treated with the aqueous extract (AE) of C. glazioui were much calmer than control animals. That observation prompted the present study, aimed at an investigation of the effects of AE and of two semipurified fractions on mouse behavior as evaluated in the elevated plus-maze test (EPM). Male adult Swiss mice were treated with AE (0.25-1 g/kg po) acutely (1 h) or repeatedly (24, 7, and 1.5 h before the test). After repeated administration of AE, the frequency of entries in the open arms of EPM was increased threefold. A similar profile of action was observed after treatment with the butanolic fraction (Fbut) but not with the aqueous fraction (Faq). These findings suggest that the AE of C. glazioui promotes an anxiolytic-like effect in mice. the active principles responsible for this action are present in the less polar fraction of the extract, the main constituents of which are flavonoids and terpenes, among other compounds. (C) 2002 Elsevier Science Inc. All rights reserved.
- ItemSomente MetadadadosImplementation of the Three Rs in the Human Hazard Assessment of Brazilian Medicinal Plants: An Evaluation of the Cytotoxic and Genotoxic Potentials of Dipteryx alata Vogel(Frame, 2011-05-01) Esteves-Pedro, Natalia M.; Rodas, Andrea C. D.; Dal Belo, Chariston A.; Oshima-Franco, Yoko; Santos, Marcio G. dos; Lopes, Patricia Santos [UNIFESP]; Univ Sorocaba; IPEN CNEN SP; Fed Univ Pampa; Fed Univ Tocantins; Universidade Federal de São Paulo (UNIFESP)In Brazil, medicinal plants are widely used by the indigenous people, which leads to a constant requirement for toxicity tests to be performed on the plant extracts. Although the current Brazilian Directive 90/2004 on the preclinical toxicity testing of phytotherapeutics recommends only in vivo tests, some Brazilian researchers would like to change this situation by implementing the Three Rs in the toxicological testing of medicinal plants. The present study evaluated the cytotoxic and genotoxic potentials of bark extracts from Diptetyx alata Vogel, a medicinal plant of the Brazilian cerrado, by using CHO-K1 (Chinese hamster ovary) cells. An IC50 value was obtained, which corresponded to 0.16mg/ml of plant extract, and from this the equivalent LD50 was determined as 705mg/kg. In order to determine the genotoxic potential of the sample, the frequency of micronucleus formation was assessed. CHO-K1 cells were exposed, during targeted mitosis, to different concentrations of plant extract and cytochalasin B, in the presence and absence of an appropriate metabolic activation system (an S9 mix). The results obtained indicated that it might be possible to implement the Three Rs in assessing the potential human hazard of medicinal plants. The publication of such data can increase awareness of the Three Rs by showing how to optimise the management of animal use, if in vivo toxicological experiments are required.
- 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
- ItemAcesso aberto (Open Access)Inhibition of gastric secretion by a water extract from Baccharis triptera, Mart(Instituto Oswaldo Cruz, Ministério da Saúde, 1991-01-01) Gamberini, Maria T. [UNIFESP]; Skorupa, Ladislau Araújo; Souccar, Caden [UNIFESP]; Lapa, Antonio José [UNIFESP]; Universidade Federal de São Paulo (UNIFESP); EMBRAPA CENARGEMBaccharus triptera Mart, is a widespread Compositae usedin Brazilian folk medicine to treat gastrointestinal disturbances, rheumatic disease, mild fever, diabetes and as an anti-helminthic. Water extract of small branches of the plant (WE) administered to mice and rats (0.1 to 2 g/Kg, p.o) did not alter spontaneous motor activity, sleeping time induced by barbiturates or the tailflick response in mice. The extract decreasedby 40 por cento the number of writhings induced by 0.8 por cento scetic acid, i.p., but did not influence paw edema induced by carrageenan or dextran in rats WE (2g/Kg, p.o.) decreased the intestinal transit of charcoal in mice by 20//. Gastric secretion in pylorus ligated rats was reduced after treatment with WE (1 and 2 g/Kg. i.p. or intraduodenal and the gastric pH was raised. The extract (1 g/Kg, p.o.) prevented gastric ulcers induced in rats by immobilization at 4ºC, but not those induced by indomethacin (10 mg/Kg, s.c.). The results indicate that WE may relieve gastrointestinal disorders by reducing acid secretion and gastrointestinal hiperactivity. Neither analgesic nor anti-inflammatory activities were detectable.
- ItemSomente MetadadadosInhibition of histamine-induced bronchospasm in guinea pigs treated with Cecropia glaziovi Sneth and correlation with the in vitro activity in tracheal muscles(Elsevier B.V., 2007-05-01) Delarcina, S.; Lima-Landman, M. T. R.; Souccar, C.; Cysneiros, Roberta Monterazzo [UNIFESP]; Tanae, M. M.; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP)A standardized aqueous extract (AE) and a purified fraction (BuF) of Cecropia glaziovi Sneth leaves were tested in unrestrained guinea pigs challenged with histamine. Changes of the respiratory pressure and rate were recorded in a whole body plethysmograph before and after treatment. the concentration of histamine necessary to produce bronchospasm was increased by five-fold following administration of AE (1.0 g/kg p.o.), and by two-fold after treatment with the semi-purified procyanidin/flavonoids enriched BuF (0.1 g/kg p.o.). Both effects were blocked by previous treatment with propranolol (10.0 mg/kg i.p.). in vitro incubation of BuF (0.1-1.0 mg/ml) decreased by 13-55% the maximal response of guinea pig tracheal muscle to histamine, without significant change of EC50. the results confirmed old reports on the useful pulmonary effects of Cecropia extracts. the bronchodilation observed in vivo seems to be related to beta-adrenergic activity observed in vitro only with high concentrations of the purified extract. (C) 2007 Elsevier GmbH. All rights reserved.
- ItemAcesso aberto (Open Access)Leaf and Root Extracts from Campomanesia adamantium (Myrtaceae) Promote Apoptotic Death of Leukemic Cells via Activation of Intracellular Calcium and Caspase-3(Frontiers Media Sa, 2017) Campos, Jaqueline F.; de Toledo Espindola, Priscilla P.; Torquato, Heron F. V. [UNIFESP]; Vital, Wagner D.; Justo, Giselle Z. [UNIFESP]; Silva, Denise B.; Carollo, Carlos A.; Souza, Kely de Picoli; Paredes-Gamero, Edgar J. [UNIFESP]; dos Santos, Edson L.Phytochemical studies are seeking new alternatives to prevent or treat cancer, including different types of leukemias. Campomanesia adamantium, commonly known as guavira or guabiroba, exhibits pharmacological properties including antioxidant, antimicrobial, and antiproliferative activities. Considering the anticancer potential of this plant species, the aim of this study was to evaluate the antileukemic activity and the chemical composition of aqueous extracts from the leaves (AECL) and roots (AECR) of C. adamantium and their possible mechanisms of action. The extracts were analyzed by LC-DAD-MS, and their constituents were identified based on the UV, MS, and MS/MS data. The AECL and AECR showed different chemical compositions, which were identified as main compounds glycosylated flavonols from AECL and ellagic acid and their derivatives from AECR. The cytotoxicity promoted by these extracts were evaluated using human peripheral blood mononuclear cells and Jurkat leukemic cell line. The cell death profile was evaluated using annexin-V-FITC and propidium iodide labeling. Changes in the mitochondrial membrane potential, the activity of caspases, and intracellular calcium levels were assessed. The cell cycle profile was evaluated using propidium iodide. Both extracts caused concentration-dependent cytotoxicity only in Jurkat cells via late apoptosis. This activity was associated with loss of the mitochondrial membrane potential, activation of caspases-9 and -3, changes in intracellular calcium levels, and cell cycle arrest in S-phase. Therefore, the antileukemic activity of the AECL and AECR is mediated by mitochondrial dysfunction and intracellular messengers, which activate the intrinsic apoptotic pathway. Hence, aqueous extracts of the leaves and roots of C. adamantium show therapeutic potential for use in the prevention and treatment of diseases associated the proliferation of tumor cell.
- ItemSomente MetadadadosPharmacological properties and identification of cardiotonic principles from the Indian snuff, Maquira sclerophylla, Ducke(Wiley-Blackwell, 1997-03-01) deCarvalho, J. E.; Souccar, C.; Tersariol, I. L.; Torres, L. B.; Lapa, A. J.; Universidade Federal de São Paulo (UNIFESP); Universidade Estadual de Campinas (UNICAMP); UNIV FED MARANHAOThe powdered bark obtained from Maquira sclerophylla Ducke is a snuff used by Amazonian natives. Pharmacological studies on rodents, guinea-pigs, rabbits and dogs revealed cardiovascular changes as the major effects produced by the polar phase of the bark ethanol extract, Oriented by this pharmacological activity a cardenolide fraction was chemically purified from the crude extract. Both crude extract and the purified fraction produced a positive inotropic effect in isolated heart preparations from guinea-pigs and rabbits, and inhibited the Na+, K+-ATPase activity of the enzyme isolated from bovine ventricles. the fraction yielded two major purified cardenolides identified as Maquiroside A (C30H46O8) and Cymarin (C30H44O9). Simultaneous intracellular recordings of the resting membrane potential (RMP) and miniature endplate potentials in rat diaphragm muscle fibres showed that the effect of the purified fraction predominated on the motor nerve terminals enhancing the spontaneous transmitter release, without major changes of RMP values. Comparatively, the effect of ouabain prevailed on the muscle fibre membrane. Considering that both effects depend on the Na+, K+-ATPase activity, the results indicated that the compounds derived from Maquira exert differential actions on this enzyme in the nerve and muscle membrane. These observations may explain the use of this toxic snuff in native festivities. (C) 1997 by John Wiley & Sons, Ltd.
- ItemSomente MetadadadosPharmacology of Piper marginatum Jacq a folk medicinal plant used as an analgesic, antiinflammatory and hemostatic(Gustav Fischer Verlag, 1997-03-01) D'Angelo, Luiz Carlos Abbech [UNIFESP]; Xavier, Haroudo Satiro; Torres, Luce Maria Brandão [UNIFESP]; Lapa, Antonio José [UNIFESP]; Souccar, Caden [UNIFESP]; Universidade Federal de São Paulo (UNIFESP); Universidade Federal de Pernambuco (UFPE); UNIV FED MARANHAOThe pharmacological activities of the water extract of Piper marginatum Jacq. (Piperaceae), a plant reputed in the Brazilian folk medicine for its analgesic/antiinflammatory, hemostatic and skin wound-healing properties, were assessed. Intraperitoneal injection (i.p.) of the extract (0.1 to 1 g/kg) in mice and rats caused piloerection, sialorrhea, lacrimation, muscle relaxation and dyspnea. At doses above 1 g/kg the extract caused respiratory arrest and death. Intravenous injection of the extract (0.1 to 0.5 mg/kg) into anesthetized rats caused a dose-related hypertension (by 27 to 48 %) that was blocked by prazosin (1 mg/kg) and yohimbine (2 mg/kg). Pithing, reserpine treatment and ganglionic blockade with hexamethonium (5 mg/kg) enhanced the effect. Oral treatment of unanesthetized rats and intragastric administration to anesthetized animals also produced hypertension. The sympathomimetic activity of the extract in isolated vas deferens, left atria and mesenteric arterial bed preparations paralleled that of noradrenaline, and was blocked to the same extent as noradrenaline by alpha-blockers. The plant extract (0.5 and 1 g/kg, p.o.) also reduced carrageenin-induced paw edema in rats by 80 to 90 % of the control, but it had less effect on the volume of exudate and leucocyte migration in carrageenin-induced pleurisy. Likewise, the extract had a small analgesic effect on the acetic acid-induced writhing test in mice.It is concluded that the antiedema effect of the plant extract is mainly related to its vasoconstrictor constituent(s). This sympathomimetic activity may explain the plant's reputed hemostatic properties when applied topically to bleeding skin wounds. The predominant vasoconstrictor component of P. marginatum detected in HPLC analysis was noradrenaline, whose activity is apparently preserved in the crude extract and produces vasoconstriction after oral administration.
- ItemSomente MetadadadosPurification, biochemical and functional characterization of miliin, a new thiol-dependent serine protease isolated from the latex of Euphorbia milii(Bentham Science Publ Ltd, 2008-07-01) Moro, L. P.; Murakami, M. T.; Cabral, H.; Vidotto, A.; Tajara, E. H.; Arni, R. K.; Juliano, L. [UNIFESP]; Bonilla-Rodriguez, G. O.; UNESP; Ctr Struct Mol Biol; Universidade de São Paulo (USP); Universidade Federal de São Paulo (UNIFESP)Miliin, a new thiol-dependent serine protease purified from the latex of Euphorbia milii possesses a molecular weight of 79 kDa, an isoelectric point of 4.3 and is optimally active at 60 degrees C in the pH range of and 7.5-11.0. Activity tests indicate that milliin is a thiol-dependent serine protease.
- 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.
- ItemAcesso aberto (Open Access)The water extract of Coleus barbatus Benth decreases gastric secretion in rats(Instituto Oswaldo Cruz, Ministério da Saúde, 1991-01-01) Fischman, Lygia Adriane [UNIFESP]; Skorupa, Ladislau Araújo; Souccar, Caden [UNIFESP]; Lapa, Antonio José [UNIFESP]; Universidade Federal de São Paulo (UNIFESP); EMBRAPA CENARGEMColeus barbatus (Labiatae) Benth is popularly used in Brazil for the healing of liver and stomach diseases. The water extract (WE 1 to 10 g/Kg, p.o.) of stem and leaves given to rats and mice did not induce signs of intoxication. Preveious treatment of mice with WE (1 g/kg, p.o.) shortened the sleeping time induced by pentobarbital (50 mg/Kg, i.p.) by 37 por cento, althoyugh the extract alone did not increase the spontaneous activity nor did it induce hyperexcitability. In mice WE (2 g/Kg, p.o.) increased the intestinal transit of charcoal by 30 por cento, while reduced gastric secretions ion rats treated with WE (2g/Kg intraduodenal) 3,9 ± 1.0 to 0.5 ± 0.2 ml/4h, respectively). The treatment also reduced the total acid secretion from 34.4 ± 11.0 to 2.7 ± 0.5 mEq/l and raisedgastric pH from 2.2 ± 0.3 to 6.5 ± 0.8. Treatment with WE (2g/Kg, p.o.) protected against gastric ulcers induced by stress (5.3 ± 1.6 and 1.5 ± 0.5 ulcers/cm²), but did nor protect against indonethacin induced ulcers. The results show that the water extract of C barbatus Benth produces mild stimulation of thecentral nervous system and increases intestinal movements. The extract also reduces gastric secretion indicating an antidyspeptic activity, and protects against gastric ulcers induced by stress.