Joaquim Corsino da Silva Lima

Gastroprotective and ulcer-healing mechanisms of ellagic acid in experimental rats.

Ellagic acid (EA), a plant-derived polyphenol, exhibits antioxidant, anti-inflammatory, and gastroprotective effects. Its gastroprotective mechanisms have not been fully elucidated nor have its effects on chronic ulcer previously been described. Toward these ends, the antiulcer activities of EA were evaluated in acute (ethanol and indomethacin) and chronic (acetic acid) ulcer models in Wistar rats. In this study, oral administration of EA significantly prevented the gastric ulceration caused by ethanol, indomethacin, and acetic acid treatments. Its gastroprotective mechanism in ethanol-induced ulcer were partly due to intensification in the endogenous production of nitric oxide, an antioxidant effect by replenishing depletion of endogenous nonprotein sulfhydryls and attenuation of tumor necrosis factor-α increase, whereas in indomethacin ulcer, it is partly due to a reduction in the plasma level of leukotriene B(4). In acetic acid ulcer, promotion of ulcer-healing effects was partly due to attenuation of the elevated levels of the inflammatory cytokines TNF-α, interferon-γ, and interleukins-4 and -6. These findings suggest that ellagic acid exerts its antiulcer activity by strengthening the defensive factors and attenuating the offensive factors.

Levantamento etnobotânico de plantas popularmente utilizadas como antiúlceras e antiinflamatórias pela comunidade de Pirizal, Nossa Senhora do Livramento-MT, Brasil

An ethnobotanical survey was conduced to study the vegetal species from Pantanal, in the district of Pirizal-MT, popularly used as anti-inflammatory and anti-ulcer. Ethnobotanical data were collected through open interviews and ethnopharmacology questionnaire with 38 local informers, in the age group of 25 to 75 years old. The local name, the part normally used, the mode of preparation and the administration route were asked to them. A bibliographic review of the plants most cited in the study was carried out using the conventional databases. A total of 49 species were cited belonging to 47 genera and 32 families, with emphasizing the Fabaceae family. The plants most cited were Lafoensia pacari St. Hil (9.2%), Hyptis crenata Pohl (8.8%), Hyptis suaveolens (L.) Poit (6.7%), Stachytarpheta cayenensis (L.C.Rich) Vahl (5.8%), Waltheria indica L. (5%), Strychnos pseudoquina St.Hil (4.2%) and Vatairea macrocarpa (Benth.) Ducke (3.3%). The part of the plant most cited was the leaf (57.1%), the most used administration route in the treatment of ulcers was oral (100%), in the form of teas (75%), while in the inflammations, topical baths were preferentially used (60%). The literature review indicated the need for further chemical-pharmacological studies on Vatairea macrocarpa (Benth.) Ducke and Hyptis crenata Pohl.

Antimicrobial screening of some medicinal plants from Mato Grosso Cerrado

Hexane, dichloromethane, ethyl acetate and ethanol extracts from stem barks of Bowdichia virgilioides, Calophyllum brasiliense, Cariniana rubra, Lafoensia pacari, and Stryphnodendron obovatum and rhizome of Simaba ferruginea and Dragons blood red sap from Croton urucurana were screened against a panel of bacteria and fungi using the micro-broth dilution method. Dragons blood from Croton urucurana was the most effective antimicrobial plant material. Ethyl acetate and hexane extracts of Calophyllum brasiliense stem bark deserved distinction by their selective antibacterial activity. Lafoensia pacari stem bark polar extracts distinguished by their potent and selective anti-yeast activity and Bowdichia virgilioides polar and non-polar extracts by their antifungal activity towards hyalohypho-mycetes and dermatophytes. This is the first report showing antifungal activity for polar extracts of Cariniana rubra and Simaba ferruginea. This study has demonstrated antimicrobial activity of Mato Grosso Cerrado ethnomedicinal plants in in vitro assays and has indicated that they can be effective potential candidates for the development of new strategies to treat fungal and bacterial infections.

Levantamento etnobotânico de plantas utilizadas como anti-hiperlipidêmicas e anorexígenas pela população de Nova Xavantina-MT, Brasil

This study checked the use of medicinal plants found in the Cerrado mato-grossense for the treatment of hyperlipidemia and obesity. Interviews with 180 people over 50 years were held in Nova Xavantina-MT. The questionnaire addressed popular name, part used, type of preparation and use of the species mentioned, beyond general information about the use of plants. The ten plants most cited were collected, identified and studied through a literature review. Most respondents (95.6%) said using medicinal plants regularly, while 71.5% of them inherited the knowledge of plants of parents and grandparents and 94.20% reported the use to advise youngsters. Furthermore, 93.6% attested that the plants are more effective than the drugs from pharmacy and 57% considered the strong effect of the same, i.e., they always solved health problems. Regarding adverse effects, 95.9% said they have never felt them after the use of plants. Of the respondents, 56.7% knew or had used medicinal plants in the treatment of hyperlipidemias and obesity, being cited 54 medicinal species belonging to 53 different genera and 38 families, with emphasis on Fabaceae (13%). The ten most cited were: guatambu (Aspidosperma tomentosum Mart.), quina-do-cerrado (Strychnos pseudoquina St. Hil.), ipe-roxo [Tabebuia impetiginosa (Mart. Ex DC.) Standl], embauba (Cecropia pachystachya Trec.), calunga (Simaba sp.), pata-de-vaca [Bauhinia rufa (Bong.) Steud.], mangaba (Hancornia speciosa Gomez), batata-de-tiu [Jatropha elliptica (Pohl.) Muell. Arg.], folha-de-carne (Casearia sylvestris Sw.) and manaca (Spiranthera odoratissima A. St.-Hil.). The leaf was the most used (46%) and the preparation of the plants occurs mainly through the infusion cited by 36,5% of respondents. Despite the popular use of these plants for treatment of obesity and hyperlipidemia, further chemical and pharmacological studies are required to demonstrate these activities, in order to develop a phytotherapic product.

Evaluation of antiulcer activity and mechanism of action of methanol stem bark extract of Lafoensia pacari A. St.-Hil. (Lytraceae) in experimental animals

ETHNOPHARMACOLOGICAL RELEVANCE Lafoensia pacari St.-Hil. is a tree native to the Brazilian Cerrado. Its bark macerate is popularly used in Brazilian folk medicine for the treatment of peptic ulcer, wound healing and inflammation. AIM OF THE STUDY To evaluate the antiulcer activities of the methanol extract of Lafoensia pacari (MELP) and possible mechanisms of actions involved. MATERIALS AND METHODS The stem bark of Lafoensia pacari was macerated in methanol to obtain the crude methanol extract of Lafoensia pacari (MELP). The gastroprotective and ulcer healing of MELP were evaluated using ethanol, indomethacin, cold-restraint stress-induced (acute) and acetic acid (chronic) ulcer models. The probable mode of action of MELP was also evaluated by determining intestinal transit, involvement of non-protein sulfhyhydryls (NP-SH), gastric mucus secretion, gastric secretory parameters and pro-inflammatory cytokines, tumor necrosis factor-α (TNF-α) and interleukin-17 (IL-17). Phytochemical analysis was carried out using classical methods and ellagic acid, one of the most important pharmacological active compounds was confirmed by HPLC. RESULTS The results of the pharmacological studies on MELP demonstrated potent and effective gastroprotection against ethanol, indomethacin and cold stress-induced acute ulcers and ulcer healing in acetic acid induced chronic ulcer. MELP had no significant effect on the intestinal motility and it is also independent of mucus production but rather have a mucolytic effect. In pylorus-ligated rats the extract showed anti-secretory activity by decreasing total gastric juice volume and gastric acidity while increasing the gastric pH. The gastroprotection against ethanol is partially attributed to effective attenuation in the decrease in NP-SH levels, inhibition of the increases in the pro-inflammatory cytokines, TNF-α and IL-17. Phytochemical analysis of MELP revealed the presence of pyrrogalic tannins, saponins, steroids, triterpenoids and simple phenols, with ellagic acid being the major components. CONCLUSION The results of this study showed that MELP possesses preventive and curative effects against gastric ulcer in experimental animals. These effects are partly dependent on its anti-oxidant, anti-secretory properties and inhibition of pro-inflammatory cytokines and independent of gastric/intestinal motility and mucus secretion. Ellagic acid, a compound of proven antiulcer activity, was found in MELP as the major component. These results confirmed the traditional use of MELP in Brazilian popular medicine for the treatment of gastric ulcers and shed some light on some of its mechanisms of action.

Triagem da atividade antibacteriana in vitro do látex e extratos de Croton urucurana Baillon

We evaluated the antibacterial activity of the latex and extracts from different polarities and pharmacogens of Croton urucurana using antimicrobial assays. The pharmacogens were collected in Barao de Melgaco-MT. The extracts were obtained by cold maceration in hexane, dichloromethane, ethyl acetate, ethanol and chloroform. They were concentrated in rotatory evaporator and dried in stove. In the disk diffusion assay, the latex showed a potent action against all bacterial strains, excepting E. coli, not differing in the potency and antibacterial spectrum. The hexane, dichloromethane and ethanol extracts of leaves showed activity against S. pyogenes, K. pneumoniae, P. aeruginosa, S. typhimurium, S. aureus and S. epidermidis in the major doses. Extracts obtained of stem bark were actives against S. aureus, S. epidermidis, P. aeruginosa, E. faecalis, S. pyogenes, E. coli, K. pneumoniae and S. typhimurium. The latex showed higher potency and broad-spectrum of action than extracts from stem bark and leaves. Among the stem bark extracts, the chloroform was the most potent one, followed by the ethanol extract. This result suggests the presence of different active principles. In the broth-microdilution, the latex and all extracts showed activity, even though, the latex presented more potency. Our results indicate that C. urucurana presents antibacterial activity, in different parts of the plant and by different secondary metabolites.

Topical and systemic anti-inflammatory effects of Echinodorus macrophyllus (Kunth) Micheli (Alismataceae).

Echinodorus macrophyllus leaf has been used in Brazilian folk medicine to treat inflammatory conditions and kidney dysfunctions. The present study evaluated the effects of leaf ethanolic extract from E. macrophyllus (EEEm) in acute and subchronic models of inflammation. The EEEm was found to cause significant and potent inhibition of carrageenan- and dextran-induced paw edema in rats and marked decreases in the exudate volume and leukocyte migration in rats with carrageenan-induced pleurisy, the vascular permeability increase induced by intraperitoneal acetic acid, and the croton oil-induced topical ear edema in mice. On the other hand, the EEEm was not active in the test model of cotton pellet-induced granuloma in rats. Phytochemical analysis with E. macrophyllus leaves revealed the presence of triterpenoids, steroids, flavones, flavonols, and xanthones. Two flavonoids were isolated from the ethyl acetate fraction and identified as isovitexin and vitexin. Our results support the traditional use of E. macrophyllus leaves in the treatment of acute inflammatory conditions.

Phytochemical and antiulcerogenic properties of rhizomes from Simaba ferruginea St. Hill. (Simaroubaceae).

Abstract Simaba ferruginea (Simaroubaceae) is a Brazilian medicinal plant used in traditional medicine to treat several ailments, including gastric ulcers, fever, diarrhea, and dolorous and inflammatory processes. This study examines the chemical composition and antiulcerogenic effects of rhizomes from this plant. Bioassay-guided fractionation led to the isolation of two bioactive indole alkaloids called canthin-6-one (1) and 4-methoxycanthin-6-one (2). The alkaloid fraction and both alkaloids demonstrated potent antiulcerogenic effects when evaluated in gastric lesion-induced animals, as well as significant antinociceptive activity in mice. These results confirm and justify the popular use of S. ferruginea against gastric ulcers and dolorous processes.

Sphenodesme involucrata var. paniculata (C.B. Clarke) Munir.: Chemical characterization, anti-nociceptive and anti-inflammatory activities of methanol extract of leaves

ETHNOPHARMACOLOGICAL RELEVANCE Sphenodesme involucrata var. paniculata (C. B. Clarke) Munir is native as well as endemic to South India. Its leaves are used in folklore medicine to treat pain and rheumatism. OBJECTIVE This study was aimed to investigate the chemical characterization, anti-nociceptive and mode of action underlying the anti-inflammatory effects of methanol extract of S. involucrata leaves (MESi). METHODS Phytoconstituents of MESi was analyzed using colorimetric and liquid chromatography-mass spectrometry (LC-MS) methods, and the oral acute toxicity was evaluated in mice up to 2000 mg/kg. The anti-nociceptive effect was evaluated in hot plate and writhing tests; whereas the anti-inflammatory effect was investigated using carrageenan, cotton pellet and lipopolysaccharide (LPS)-induced peritonitis models at doses of 100, 200 and 400 mg/kg. Additionally nitric oxide (NO) and inflammatory cytokines levels were also evaluated. RESULTS MESi exhibited the high content of phenolics and flavonoids as well as compounds like austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin were detected in LC-MS. In the acute toxicity study, oral administration of MESi did not cause any toxic effect and mortality up to 2000 mg/kg body weight in mice. In the anti-nociceptive tests, MESi augmented the latency period at higher dose (400 mg/kg), on the other hand attenuated writhings at the dose of 400 mg/kg by 87.87% (p < 0.001). In the carrageenan induced paw oedema MESi significantly inhibited the oedema formation at dose 400 mg/kg by 32.1%; besides, anti-inflammatory effect was registered in the cotton pellets-induced inflammation model at doses 200 and 400 mg/kg by 27.09% (p < 0.001) and 35.47% (p < 0.001) respectively. On the other hand, MESi appreciably reduced leukocyte, neutrophils infiltration, nitric oxide, TNF-α and IL-1β levels and increased the IL-10 level in the (LPS)-induced peritonitis model. CONCLUSION The results conclude that MESi has no acute toxic effect and it demonstrated potent anti-nociceptive and anti-inflammatory activities. Its anti-nociceptive activities are probably mediated through peripheral and central mechanisms. The anti-inflammatory effect of MESi involved the inhibition of neutrophils migration and the modulation of Th1 and Th2 cytokines, besides the attenuation of production of PGE2 and NO. LC-MS analysis revealed the predominant presence of the austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin compounds, which are possibly involved in the anti-nociceptive and anti-inflammatory effects of MESi. The current study provided supportive evidence for the folklore use of S. involucrata in the treatment of pain and inflammatory conditions.