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Abstract: Ethnopharmacological relevance: Brassica oleracea L. var. acephala D.C. has been extensively used in Brazilian traditional medicine to treat gastric ulcer. Aim of the study: This study was conducted to evaluate the in vivo genotoxic and/or antigenotoxic potential of a Brassica oleraceae hydroalcoholic extract obtained from the leaves, in different cells of mice. Materials and methods: Analyses were performed using the comet assay, on leukocytes (collected 4 and 24h after treatment), liver, brain, bone marrow and testicular cells (collected 24h after treatment), and using the micronucleus test (MN) in bone marrow cells. Eight groups of albino Swiss mice were treated (N=6): control (C), positive control (doxorubicin 80mg/kg (DXR)), and six experimental groups, which received 500, 1000 and 2000mg/kg of Brassica oleraceae extract alone by gavage, while a further three groups received the same doses plus DXR (80mg/kg). We calculated the damage scores, and their averages were compared by ANOVA followed by the Tukey test for multiple comparisons. Results: The results demonstrated that none of the tested doses of Brassica oleraceae extract showed genotoxic effects by the comet assay, or clastogenic effects by the MN test. On the other hand, for all cells evaluated, the three tested doses of the Brassica extract promoted inhibition of DNA damage induced by DXR. Conclusions: Under our experimental conditions, Brassica oleraceae leaf extract showed no genotoxic or clastogenic effects in different cells of mice. However, it did show a significant decrease in DNA damage induced by doxorubicin. It is suggested that the antigenotoxic properties of this extract may be of great pharmacological importance, and may be beneficial for cancer prevention. [Copyright &y& Elsevier]

Abstract: Relevance: Simaba ferruginea A. St-Hil. (Simaroubaceae) is a subshrub typical of the Brazilian Cerrado, whose rhizomes are popularly used as infusion or decoction for the treatment of gastric ulcers, diarrhea and fever. Aim of the study: To evaluate the pharmacological mechanism(s) of action of the antiulcer effects of the methanol extract of Simaba ferruginea and its alkaloid canthin-6-one. Materials and methods: Rhizome of Simaba ferruginea was macerated with methanol to obtain the methanol extract (MESf) from which was obtained, the chloroform fraction. Canthin-6-one alkaloid (Cant) was purified and then isolated from the chloroform fraction (CFSf). The isolated Cant was identified by HPLC. Anti-ulcer assays were determined using ethanol and indomethacin-induced ulcer models in mice and rats respectively. In order to determine the probable mechanisms of actions of MESf and Cant animals were pretreated with l-NAME prior to anti-ulcer agent treatments and ulcer induction and nitric oxide (NO) level determined in order to assess NO involvement in the gastroprotective effects. Assays of malondialdehyde (MDA), myeloperoxidase (MPO), pro-inflammatory cytokines: interleukin 8 (IL-8) and tumor necrosis factor-alpha (TNF-α) and prostaglandin E2 (PGE2) were also carried out according to previously described methods. Results: The results indicate that the antiulcerogenic effects of MESf and Cant in ethanol-induced ulcer is mediated in part through increase in the production of protective endogenous NO as the antiulcerogenic activity of MESf and Cant was reduced in animals pre-treated with l-NAME. In indomethacin-induced ulcer pre-treatment with MESf and Cant showed reduction in the levels of MPO and MDA in the gastric tissue, thus indicating the participation of the antioxidant mechanisms on the gastroprotective effects. The plasma levels of IL-8 in ulcerated rats with indomethacin were also reduced by Cant, but not by MESf, indicating that inhibition of this cytokine contributes to the gastroprotective effect of Cant. However MESf and Cant had no effect on the mucosal membrane levels of PGE2, indicating that the gastroprotective effects of these agents is independent of PGE2 modulation. Conclusion: The results obtained in this study with MESf and Cant added insights into the pharmacological mechanisms involved in their mode of antiulcer action. The results indicate that Cant is one of the compounds responsible for these effects. Such findings are of extreme importance in the strive for future development of potent, safer and effective antiulcer agent. The efficacy of MESf and Cant in gastroprotection shows that Simaba ferruginea might be a promising antiulcer herbal medicine, in addition to confirming the popular use of this plant against gastric ulcer models utilised in this study. [Copyright &y& Elsevier]

Abstract Ethnopharmacological relevance Popular medicine use stems of Philodendron bipinnatifidum (Araceae) in inflammation cases, such as in erysipelas, as well as orchitis and rheumatism treatment. The present study, conducted for the first time in literature, investigate the antinociceptive and anti-inflammatory activities of P. bipinnatifidum stems ethyl acetate extract (EPB). Materials and methods GC/MS and HPLC analysis were performed for EPB extract. We used EPB at 250, 375 and 500 mg/kg (oral route, p.o.) in male Swiss mice. The antinociceptive activity of the plant extract assessed by acetic acid induced writhing and formalin tests. To investigate the possible participation of opioid system in EPB-mediated effects, we previously administered naloxone to the mice. Anti-inflammatory activity was evaluated using carrageenan-induced paw oedema. The open-field test aimed to investigate the possible EPB effects on the locomotor and exploratory activities. To assess the protective role of EPB on carrageenan-induced oxidative stress, the levels of NPSH, TBARS, as well as SOD and CAT activities were evaluated in blood and paw tissue. The acute toxicity of the EPB was investigated using OECD 423 guideline. Results The EPB chemical analysis by GC/MS and HPLC revealed the presence of flavonoids (luteolin and quercetin) and phytosterols (β-sitosterol and stigmasterol). The oral treatment with the EPB inhibited mice abdominal writhings (P < 0.01) at 375 and 500 mg/kg, and reduced the formalin effect at the first-phase (500 mg/kg, P < 0.05) and also at the second-phase (500 mg/kg, P < 0.001) of the test. E P B (375 and 500 mg/kg) did not alter spontaneous locomotion in open field test, however the number of fecal bolus was significantly lower for the EPB group at 500 mg/kg when compared to the vehicle group (P < 0.05). The pretreatment with naloxone caused significant inhibition of antinociceptive activity induced by EPB in the formalin test, revealing the possible involvement of opioid receptors. EPB extract administered at 500 mg/kg (p.o.) prevented carrageenan-induced paw oedema (P < 0.05 and 0.01) until 6 h after carragenan injection. Evaluation of TBARS and NPSH levels, SOD and CAT activities in the blood and paw tissue of animals submitted to the carrageenan assay suggested that the anti-inflammatory effect of EPB may be linked to oxidative stress inhibition. The acute administration of the EPB (2000 mg/kg, p.o.) caused no mortality, demonstrating low toxicity. Conclusions The extract of P. bipinnatifidum displays antinociceptive and anti-inflammatory activities, causing no toxicological effects. The pharmacological activity of this vegetal species may be related to the presence of flavonoids and phytosterols. Our results support the ethnomedical use of this vegetal species as analgesic and anti-inflammatory agent. Graphical abstract fx1 [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The leaves from Vernonia condensata Baker are broadly used in folk medicine for the treatment of gastric ulcers and dyspepsia. The Brazilian Public Health System (SUS) describes this species as having the potential to serve as a new herbal product with therapeutic benefits. Aim of the study The purpose of the study was to evaluate the gastroprotective activity and gastric healing properties of a crude ethanolic extract from leaves of V. condensata (CEEV) in different animal models. Materials and methods In order to assess the gastroprotective potential of CEEV, ulcer models were established using ethanol and indomethacin. The gastric healing effect was then evaluated in the acetic acid-induced ulcer model, where the tissue was used to assess oxidative levels (reduced glutathione and lipid hydroperoxide levels, as well as superoxide dismutase and catalase activity), inflammatory [myeloperoxidase (MPO)] parameters, and mucin content. Furthermore, the ligature pylorus model, with and without secretagogue stimuli, was employed to investigate the mechanism of action of CEEV. In addition, H + K + -ATPase activity, MPO activity, and antioxidant activity through the DPPH assay were examined through in vitro trials. Phytochemical analyses were also performed. The ethanol/HCl-induced gastric ulcer method was employed to verify the gastroprotective effect of the main compound in CEEV. Results CEEV (30 and 300 mg/kg, p.o) exhibited gastroprotective activity and prevented both gastric lesions induced by ethanol or indomethacin in rats. The gastric healing effect of CEEV (300 mg/kg, p.o. taken twice a day for a duration of seven days) was confirmed by examining the macroscopic and microscopic appearance of chronic gastric ulcers induced by acetic acid in rats. The restorative effect of CEEV was accompanied by a significant increase in mucin content (PAS staining) and by a reduction in oxidative stress and inflammatory parameters at the site of the ulcer. Moreover, CEEV (300 mg/kg), administered via an intraduodenal route, significantly reduced the volume, pH, total acidity and pepsin activity of gastric content in the pylorus ligature model in rats. The gastric acid antisecretory effect of CEEV was maintained even in the presence of cholinergic and gastrinergic, but not histaminergic, stimuli. In vitro , CEEV (1–10 µg/ml) was able to scavenge free radical DPPH, but did not promote inhibitory effects on MPO or H + ,K + -ATPAse activity. Phytochemical analysis of CEEV indicated that luteolin is the main compound present in the extract. However, luteolin (1, 3 and 10 mg/kg, p.o or 1 mg/kg, i.p.) did not promote gastroprotection against ethanol/HCl in mice. It is also important to mention that oral administration of CEEV did not produce any sign of acute toxicity in animals. Conclusions V. condensata extract demonstrates gastroprotective effects through the inhibition of gastric secretion via cholinergic and gastrinergic pathways. Furthermore, it exhibits cytoprotective effects, involving antioxidant activity, an increase in mucin content and inhibition of neutrophil migration. Thus, this medicinal plant may be a suitable natural source for the prevention and treatment of gastric lesions. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Maytenus robusta Reissek (Celastraceae) is traditionally used in Brazilian folk medicine to treat gastric ulcer, as a substitute for M. ilicifolia , which is almost extinct. The gastroprotective properties of M. robusta were demonstrated previously using only preventive approaches, such as acute gastric ulcer models. However, the healing effect of M. robusta in gastric ulcers remains unclear. Aim of the study The current study was carried out to investigate the healing effectiveness of M. robusta hydroalcoholic extract (HEMR) from aerial parts in the acetic acid-induced chronic ulcer model and to determine its effect on cell proliferation, scavenging free radicals, and inflammatory and oxidative damage. Material and methods To evaluate the healing properties of HEMR in vivo, chronic gastric ulcer was induced in rats by 80% acid acetic. Next, different groups of animals ( n =6) were treated orally with vehicle (water plus 1% tween, 1 ml/kg), omeprazole (20 mg/kg), or HEMR (1–10 mg/kg), twice daily for 7 days. At the end of the treatment, the total ulcer area (mm 2 ) was measured and a sample of gastric tissue was taken for histological and histochemical analysis. Evaluation of GSH and LOOH levels, GST, SOD, CAT and MPO activity was also performed at the site of the lesion. In parallel, radical scavenging activity, cytoprotective effect, and cell proliferation activity in fibroblasts (L929 cells) were determined by in vitro trials. The antisecretory properties were evaluated using the pylorus ligature model in rats, and the anti- Helicobacter pylori activity was determined in vitro. Acute toxicity was evaluated by relative organ weight and biochemical parameters in serum. The prokinetic properties were also evaluated in mice. Results Oral administration of HEMR (10 mg/kg) reduced the gastric ulcer area by 53%, compared to the vehicle group (120.0±8.3 mm 2 ), the regeneration of gastric mucosa was evidenced in histological analysis. Moreover, HEMR treatment increased gastric mucin content and reduced oxidative stress and inflammatory parameters at the site of the ulcer. In vitro, HEMR (1–1000 µg/ml) was able to scavenge free radical DPPH and promote cytoprotection against H 2 O 2 in fibroblasts at 0.1–100 µg/ml. Moreover, HEMR healing properties also were confirmed by enhancement of proliferation and coverage of scratched wounds in fibroblast monolayer. However, HEMR (10 mg/kg) by the intraduodenal route did not promote changes in volume, pH, total acidity or pepsin activity in the pylorus ligature model, and HEMR up to 2000 µg/ml also did not present considerable activity against H. pylori . In relation to gastrointestinal motility, HEMR (10 mg/kg, p.o) did not provoke alterations. It is also important to mention that oral administration of HEMR did not produce any sign of acute toxicity in animals. Conclusions The data here obtained show that M. robusta has evident ulcer healing potential, mainly through the strengthening of protective factors of gastric mucosa, such as mucus layer, antioxidant defenses and cell proliferation. Taking into account the advantages of cultivation and harvesting of M. robusta compared to M. ilicifolia , and the evidence presented here, it is plausible to conclude that hydroalcoholic extract obtained from aerial parts of M. robusta is an interesting source for the development of a phytotherapeutic formulation to treat gastric ulcer. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Brassica oleracea var. acephala DC has been extensively used in Brazilian traditional medicine to treat gastric ulcer. Aim of the study: This study was conducted to evaluate the antiulcerogenic property of hydroalcoholic extract obtained from the leaves of Brassica oleracea. Materials and methods: Antiulcer assays were performed using the protocol of ulcer induced by ethanol/HCl, and non-steroidal anti-inflammatory drugs (NSAIDs). Parameters of gastric secretion (volume, pH and [H+]) were determined by the pylorus ligation model and mucus in gastric contents. Results: In the ethanol-induced ulcer model, we observed a significant reduction in all the parameters analyzed, obtaining curative ratios of 58.8±11.5, 86.2±12.2 and 42.8±6.6% for the groups treated with 50 and 100mg/kg of extract and omeprazole (30mg/kg), respectively. The dose of 25mg/kg of hydroalcoholic extract of Brassica oleracea showed no significant results. In the indomethacin-induced ulcer, the percentages of ulcer inhibition were 64.3±9.9, 66.4±12.3 and 81.2±7.5% for the groups treated with 50 and 100mg/kg extract and positive control (cimetidine, 100mg/kg), respectively. The results showed a significant increase in pH and mucus production in the groups treated with Brassica oleracea when compared with the control group. No sign of toxicity was observed in the acute toxicity study. Conclusions: The results of the present study show that hydroalcoholic extract of Brassica oleracea displays antiulcer activity, as demonstrated by the significant inhibition of ulcer formation induced using different models. The data suggest that the effectiveness of the extract is based on its ability to stimulate the synthesis of mucus, increase pH and decrease H+ ions in the stomach. This work corroborates the ethnopharmacology use of Brassica oleracea preparations, contributing to its pharmacological validation by suggesting that preparations obtained from Brassica oleracea could be used for the development of new phytopharmaceuticals for the treatment of gastric ulcer. [Copyright &y& Elsevier]

Ethnopharmacological relevance: Achyrocline satureoides is a medium-sized South American indigenous herb, commonly known as “Marcela” or “Macela”. The infusion obtained from inflorescences of this plant is widely used in Brazilian folk medicine as an antispasmodic, anti-inflammatory, hypoglycemic, and hypocholesterolemic, mainly to treat gastrointestinal disorders such as gastric ulcers and dyspepsia. However, the antiulcer properties of this species have not yet been fully studied. Aim of the study: This study was conducted to evaluate and contribute to validating the antiulcer activity of hydroalcoholic extract of inflorescences of Achyrocline satureoides. Materials and methods: The antiulcer assays were performed using the ethanol-induced ulcer, and nonsteroidal anti-inflammatory drug (NSAID)-induced ulcer protocols. Gastric secretion parameters were also evaluated (volume, pH and total acidity) by the pylorus ligated model, and the mucus in the gastric content was determined. Results: In the ethanol-induced ulcer model, it was observed that the treatment with Achyrocline satureoides extract significantly reduced the lesion index by 75.1±8.6, 85.0±9.2, 86.6±7.4 and 75.5±5.3 for the groups treated with 100, 250 and 500mg/kg of extract of inflorescences of Achyrocline satureoides and the positive control (omeprazole 30mg/kg), respectively. Significant inhibition was also observed in the lesion index in the indomethacin-induced ulcer model, with decreases of 62.5±7.1, 62.5±6.1, 63.6±5.5 and 96.2±3.6 for the groups treated with 100, 250 and 500mg/kg of extract and the positive control (cimetidine 100mg/kg), respectively. The parameters of gastric secretion (pH, volume, [H+]) showed no alteration in the different doses of the treatment. On the other hand the treatment with the hydroalcoholic extract of Achyrocline satureoides (100, 250 and 500mg/kg), significantly increased mucus production (p <0.01), when compared with the groups treated with indomethacin (100mg/kg), cimetidine (100mg/kg) and negative control (vehicle). No signs of toxicity was observed in the acute toxicity study. Conclusions: The results of the present study show that hydroalcoholic extract of Achyrocline satureoides displays antiulcer activity, as demonstrated by the significant inhibition of the formation of ulcers induced using different models. However, this activity appears not be related to the antisecretor mechanisms. Moreover, this work suggests that preparations obtained from Achyrocline satureoides could be used for the development of new phytotherapic drugs for the treatment of gastric ulcer. [Copyright &y& Elsevier]