Hypokinetic Activity of Menthofuran on the Gastrointestinal Tract in Rodents.

The acute toxicity and hypokinetic activity induced by menthofuran on the gastrointestinal tract of rodents were investigated in the present study. An absence of acute toxicity was observed. Menthofuran delayed gastric emptying at oral doses of 25, 50, and 100 mg/kg in the experimental model of phenol red, as well as it reduced the intestinal transit at oral doses of 50 and 100 mg/kg. Interestingly, a scopolamine-similar hypokinetic effect was observed for menthofuran. In the experimental model of castor oil-induced intestinal hypermotility, menthofuran (50 and 100 mg/kg) reduced the number of loose stools as observed for the normal group. Additionally, menthofuran induced a marked concentration-dependent relaxation in rat ileum segments precontracted with KCl (EC50 = 0.059 ± 0.008 µg/mL) or carbachol (EC50 = 0.068 ± 0.007 µg/mL). These results suggest the possible decrease of calcium influx underlying the effects of menthofuran on the gastrointestinal tract, which opens the door for further study regarding this potential application for the treatment of gastrointestinal disorders, noting possible limitations of its use due to adverse effects in children.

Antioxidant Mechanisms Underlying the Gastroprotective Effect of Menthofuran on Experimentally Induced Gastric Lesions in Rodents.

Menthofuran is a monoterpene present in various essential oils derived from species from Mentha genus, and in Brazil, those species are widely used in treating gastrointestinal and respiratory disorders. Considering the wide pharmacological potential of monoterpenes, including their antioxidant activity, this study aimed to evaluate menthofuran-gastroprotective activity, as well as the involvement of antioxidant mechanisms in this effect. The acute toxicity was evaluated according to the fixed dose method. The antiulcerogenic activity was investigated by using experimental models of gastric ulcers induced by ethanol, indomethacin, and ischemia/reperfusion in rats. The antisecretory gastric activity, the catalase activity, and the gastric wall mucus were determined in pylorus ligated rats. Gastric wall nonprotein sulfhydryl (NPSH) group content, myeloperoxidase (MPO) activity, and malondialdehyde (MDA) content were evaluated in ethanol-induced the gastric ulcer model. Menthofuran (2 g/kg) presented low acute toxicity and showed gastroprotective activity against ethanol-, indomethacin-, and ischemia/reperfusion-induced ulcers. Moreover, menthofuran presented antisecretory activity, reduced the total acidity, and increased pH of gastric secretion. On the other hand, a decrease in mucus content of gastric wall without alteration of gastric juice volume and catalase activity was observed. Interestingly, menthofuran increased NPSH levels and reduced MDA levels and MPO activity. Gastroprotective effects of menthofuran appear to be mediated, at least in part, by the NOS pathway, endogenous prostaglandins, reduced gastric juice acidity, increased concentration of the NPSH groups, and reduced lipidic peroxidation. These findings support the menthofuran as an effective gastroprotective agent, as well as the marked participation of antioxidant mechanisms in this response.

Effects of consumption of mauritia flexuosa fruits on renal and hepatic functions in growing rats

INTRODUCTION: Previous studies have reported that buriti (Mauritia flexuosa L. f.) is a typical fruit from the Brazilian cerrado ecosystem and an important food source for low-income populations. Its composition is rich in carotenoid polyphenols, monounsaturated fatty acids, and ascorbic acid. However, studies on the biological effects resulting from the consumption of this fruit are scarce. OBJECTIVE: To evaluate the effects of a diet supplemented with buriti (Mauritia flexuosa L. f.) on kidney and liver functions in growing rats. METHODS: Determination of centesimal composition, carotenoids, and fatty acids content for buriti pulp, standard chow, and butiti-supplemented chow were performed. Then, Wistar rats of both sexes were fed a standard diet or supplemented with buriti pulp. Blood samples were collected at the end of the experiment to determine biochemical parameters. The unpaired t-test was applied, and differences were considered significant when p<0.05. RESULTS: A diet enriched with buriti pulp did not interfere with kidney function and most markers of liver function in animals. Alkaline phosphatase showed significantly higher plasma concentration in female rats, and albumin and uric acid showed lower concentrations in male rats in both experimental groups. CONCLUSION: The changes observed in biochemical markers did not provide evidence of adverse effects of buriti pulp supplementation on liver function. Thus, the intake of buriti pulp can be encouraged as it is a low-cost food source for the general population.

Antiulcerogenic and healing activity of hecogenin acetate in rodents.

Peptic ulcers are lesions in the gastric and duodenal mucosa generated by an imbalance between protective factors (gastroduodenal mucus secretion, bicarbonate production, adequate blood flow) and harmful factors (excess pepsin or hydrochloric acid). Some drugs used in peptic ulcer therapy are associated with adverse effects. The aim of this study was to evaluate the antiulcerogenic and healing activity of hecogenin acetate (HA) in acute and chronic models of gastric lesions in rodents. The antiulcerogenic activity of HA was evaluated in models of gastric lesions induced by absolute ethanol and in acidified ethanol with HA (5, 10, and 20 mg/kg). For the model of gastric lesions induced by ischemia and reperfusion, rats were pre-treated with HA (5, 10, 20 mg/kg). After that, they were submitted to 30 min of ischemia, followed by 1 h of reperfusion. To evaluate the healing activity was induced gastric ulcer using acetic acid (80%) in rats. After 24 h, they were treated for 7 consecutive days with HA (10 and 20 mg/kg). They were evaluated the possible signs of toxicity, measurement of the lesions, collagen deposition, and histological analysis. HA significantly reduced the area of the lesion in models of gastric lesions induced by absolute and acidified ethanol, ischemia-induced gastric lesions and reperfusion, and regarding healing. In the collagen deposition, the presence and increase of collagen demonstrate the healing effect. The AH has antiulcerogenic and healing potential demonstrated by the decrease in gastric injury and presence of collagen fibers, respectively.

Effects of "Bacuri" Seed Butter (Platonia insignis Mart.) on Metabolic Parameters in Hamsters with Diet-Induced Hypercholesterolemia.

This study aimed to evaluate the effects of the treatment with bacuri seed butter (BB) on body weight, growth, body mass index, lipid profile, atherosclerotic indices, and liver function in dyslipidemic hamsters. Freshly weaned, male hamsters were divided into four groups: (1) normal group (NG)-maintained with standard chow (AIN-93G); (2) dyslipidemia group (DG)-maintained with hyperlipidemic chow (AIN-93G modified) throughout the follow-up period; (3) bacuri seed butter 25 mg/kg/day (BB-25); and (4) bacuri seed butter 50 mg/kg/day (BB-50). BB groups (25 and 50 mg/kg/day) were also maintained with hyperlipidemic chow throughout the follow-up period, and the treatment started after 21 days receiving a hyperlipidemic diet to induce hypercholesterolemia and maintained for 28 days. No significant differences in triglycerides and total cholesterol were observed for BB-25 and BB-50 groups when compared with NG and DG groups. On the contrary, BB-25 and BB-50 induced both increase of HDL-c (51.40 ± 1.69 and 51.00 ± 2.34, respectively) and decrease of LDL-c (103.80 ± 6.87 and 100.50 ± 3.95, respectively) when compared with DG (41.00 ± 2.94 and 132.70 ± 9.41, respectively). In addition, BB promoted a reduction in the risk of atherosclerotic disease by decreasing (p < 0.05) the atherogenic index, coronary artery risk index, and LDL/CT ratio (p < 0.05) and increasing HDL/CT ratio. On the contrary, no changes were observed in total cholesterol and triglyceride levels or in body weight, growth, body mass index, or liver function parameters. Thus, bacuri seed butter at doses of 25 and 50 mg/kg/day has positive repercussions on the lipid profile, more precisely on plasma HDL-c and LDL-c, and additionally promotes reduction in the risk of atherosclerosis in hamsters.

Phytochemical screening, phenolic and flavonoid contents, antioxidant and cytogenotoxicity activities of Combretum leprosum Mart. (Combretaceae).

Combretum leprosum Mart. (Combretaceae), a shrub popularly known as mofumbo, is used in folk medicine for treatment of uterine bleeding, pertussis, gastric pain, and as a sedative. The aim of this study was to (1) determine the phytochemical profile,(2) identify chemical constituents and (3) examine antioxidant and cytogenotoxic activity of ethanolic extracts and fractions of stem bark and leaves. The plant material (leaf and stem bark) was submitted to extraction with ethanol, followed by partition using hexane, chloroform, and ethyl acetate. It was possible to identify and quantify the epicatechin in the ethanolic stem bark extract (0.065 mg/g extract) and rutin in the leaf extract (3.33 mg/g extract). Based upon in vitro tests a significant relationship was noted between findings from antioxidant tests and levels of total phenolic and flavonoid. Comparing all samples (extracts and fractions), the ethyl acetate fractions of stem bark (411.40 ± 15.38 GAE/g) and leaves (225.49 ± 9.47 GAE/g) exhibited higher phenolic content, whereas hexanic fraction of stem bark (124.28 ± 56 mg/g sample) and ethyl acetate fraction of leaves (238.91 ± 1.73 mg/g sample) demonstrated a higher content of flavonoids. Among the antioxidant tests, the intermediate fraction of stem bark (28.5 ± 0.60 µg/ml) and ethyl acetate fraction of leaves (40 ± 0.56 µg/ml) displayed a higher % inhibition of free radical DPPH activity, whereas intermediate fraction of stem bark (27.5 ± 0.9 µg/ml) and hydromethanol fraction of leaves (81 ± 1.4 µg/ml) demonstrated inhibition of the free radical ABTS. In biological tests (Allium cepa and micronucleus in peripheral blood), data showed that none of the tested concentrations of ethanolic extracts of leaves and stem bark produced significant cytotoxicity, genotoxicity, and mutagenic activity.Abbreviations AA%: percentage of antioxidant activity; ABTS: 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid); CEUA: Ethics Committee in the Use of Animals; TLC: Thin Layer Chromatography; DNA: deoxyribonucleic acid; DPPH: 1,1-diphenyl-2-picrylhydrazyl; ROS: Reactive oxygen species; EEB: ethanol extract of the stem bark; HFB: Hexanic fraction of stem bark; IFB: Intermediate fraction of stem bark; CFB: Chloroform fraction of stem bark; EAFB: Ethyl acetate fraction of stem bark; HMFB: Hydromethanol fraction of the stem bark; EEL: Ethanol extract from leaves; HFL: Hexane fraction of leaves; CFL: Chloroform fraction of leaves; EAFL: Ethyl acetate fraction of leaves; HMFL: Hydromethanol fraction of leaves; GAE: Gallic Acid Equivalent; IC50: 50% inhibition concentration; HCOOH: Formic acid; HCl: hydrochloric acid; HPLC: High-performance liquid chromatography; MN: micronucleus; WHO: World Health Organization; UFLC: Ultra-Fast Liquid Chromatography; UESPI: State University of Piauí.

Lycopene-Rich Extract from Red Guava (Psidium guajava L.) Decreases Plasma Triglycerides and Improves Oxidative Stress Biomarkers on Experimentally-Induced Dyslipidemia in Hamsters.

This work assessed the effects of a 28-day treatment with lycopene-rich extract (LRE) from red guava fruit (Psidium guajava L.) on the lipid profile and oxidative stress in an experimental model of dyslipidemia. Male hamsters (116.5 ± 2.16 g) were fed with the AIN 93G diet containing casein (20%), coconut fat (13.5%) and cholesterol (0.1%). The animals were divided into four groups: normolipidemic control (standard feed; NC, n = 7); hypercholesterolemic control (HC, n = 7); LRE 25 mg/kg/day (LRE-25, n = 7) and LRE 50 mg/kg/day (LRE-50, n = 9). After treatment, plasma concentrations of triglycerides (TG), total cholesterol (TC), low-density lipoprotein (LDL) cholesterol (LDL-c), high-density lipoprotein (HDL) cholesterol (HDL-c), malondialdehyde (MDA-p) and myeloperoxidase (MPO), as well as erythrocytic superoxide dismutase (SOD-e) and the atherogenic index, were determined. Malondialdehyde (MDA-h), catalase (CAT), glutathione peroxidase (GPx) and superoxide dismutase (SOD-h) levels were assessed. Feed intake (FI) and weight gain (WG) were also determined. The LRE-25 group presented significantly lower TG levels and atherogenic index than did the HC group (p < 0.05). Both LRE-25 and LRE-50 groups presented lower levels of MDA-p and MPO than did the HC group (p < 0.05). LRE demonstrated a promising effect against dyslipidemia and oxidative stress.

In vitro and in vivo antioxidant activity of Buriti fruit (Mauritia flexuosa L. f) / La actividad antioxidante in vitro e in vivo de la fruta burití (Mauritia flexuosa L. f)

Introduction: studies have shown high concentration of monounsaturated fatty acids, carotenoids, polyphenols and ascorbic acid in Buriti fruit (Mauritia flexuosa L.f.). This study evaluated the in vitro and in vivo antioxidant activities of buriti fruit (Mauritia flexuosa L.f.). Methods: the chemical composition and total phenolic and carotenoid contents of the buriti pulp and the feed rations were determined, and the in vitro antioxidant activity was analyzed using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical assay. Wistar rats (21 days old) were randomly allocated (n=10) into a control groups and experimental groups (feed enriched with buriti pulp). After 60 days, the in vivo antioxidant activity was evaluated through the determination of the catalase activity and non-protein sulfhydryl (NPSH) groups in the liver and quantification of malondialdehyde (MDA) in the plasma and tissues. Results: high contents of oleic fatty acids (73.3%), phenolic compounds (192 ± 0.3 mg/100 g) and carotenoids (23.9 ± 0.5 mg/100 g) as well as elevated in vitro antioxidant activity were found in the buriti pulp. The enriched diet had higher contents of phenols and carotenoids as well as higher antioxidant activity compared with the standard feed (p < 0.05). There were no differences between the groups regarding catalase activity in the liver and MDA concentrations in the plasma, liver and kidneys. The male rats of the experimental group had higher liver concentrations of NPSH compounds (p < 0.05). Conclusion: these results may corroborate the claim that buriti fruit is an antioxidant functional food and support its utilization in a nutritionally balanced diet (AU)

Introducción: estudios previos han demostrado que la fruta Burití (Mauritia flexuosa L.f). posee una alta concentración de ácidos grasos monoinsaturados, carotenoides, polifenoles y ácido ascórbico. Este estudio evaluó la actividad antioxidante in vitro e in vivo del Burití. Métodos: fueron determinadas la composición química, el contenido de compuestos fenólicos y de carotenoides tanto de la pulpa del Burití como de las raciones de alimento. La actividad antioxidante in vitro fue analizada utilizando el ensayo del radical 2,2-difenil-1-picrilhidrazil (DPPH). Ratas Wistar (21 días de edad) fueron asignadas al azar (n = 10) en grupos controles y grupos experimentales (alimentación enriquecida con pulpa de Burití). Después de 60 días, la actividad antioxidante in vivo se evaluó mediante la actividad enzimática de la catalasa y grupos sulfhidrílo no proteico (NPSH) en el hígado, y se cuantificó el malondialdehído (MDA) en plasma y tejidos. Resultados: la pulpa del Burití presentó alto contenido de ácido graso oleico (73,3%), compuestos fenólicos (192 ± 0,3 mg/100 g) y carotenoides (23,9 ± 0,5 mg/100 g), así como una elevada actividad antioxidante in vitro. La dieta enriquecida tenía mayor contenido de fenoles y carotenoides, y una mayor actividad antioxidante en comparación con la alimentación estándar (p < 0,05). No se observaron diferencias entre los grupos con respecto a la actividad de la catalasa en el hígado y las concentraciones de MDA en plasma, hígado y riñones. Las ratas macho del grupo experimental tuvieron concentraciones hepáticas más altas de NPSH (p < 0,05). Conclusión: estos resultados pueden corroborar la hipótesis de que la fruta Burití es un alimento funcional antioxidante y su consumo es conveniente en una dieta nutricionalmente equilibrada (AU)

Antibacterial, antibiofilm and cytotoxic activities of Terminalia fagifolia Mart. extract and fractions.

BACKGROUND: The methicillin resistance of bacteria from the genus Staphylococcus and its ability to form biofilms are important factors in pathogenesis of these microorganisms. Thus, the search for new antimicrobials agents, especially from plants, has been intensified. In this context, Terminalia species have been the subject of research for many pharmacological activities. In this study we evaluated the antibacterial, antibiofilm and cytotoxic activities of the ethanol extract (EtE) from Terminalia fagifolia stem bark as well as that of three fractions of the extract (AqF, HaF and WSF). METHODS: We determined the minimum inhibitory concentration (MIC) by microdilution in 96-well plates, where the strains were exposed to serial dilutions of the ethanol extract and fractions, ranging from 12.5 to 400 µg/mL. We then determined the minimum bactericidal concentration (MBC), seeding the inoculum (10 µL) with concentrations equal to or greater than the MIC in Mueller-Hinton agar. To test the antibiofilm activity biofilm formation was induced in the presence of concentrations equivalent to 1/2, 1/4 and 1/8 of the MIC extract or fraction tested. In addition, the effect of the EtE and the fractions on cell viability was tested by the MTT assay on human MCF-7 breast cancer and mouse fibroblast NIH/3T3. To obtain high-resolution images of the effect of the aqueous fraction on the bacterial morphology, atomic force microscopy (AFM) imaging of treated S. aureus cells was performed. RESULTS: We observed antibacterial activity of EtE and fractions with MICs ranging from 25-200 µg/mL and MBCs ranging from 200-400 µg/mL. Regarding antibiofilm activity, both the EtE as the AqF, HaF and WSF fractions showed significant inhibition of the biofilm formation, with inhibition of biofilms formation of over 80% for some strains. The EtE and fractions showed a moderate cytotoxicity in cell line NIH/3T3 viability and potential antitumoral activity on human breast cancer cell line MCF-7. The microscopic images obtained revealed morphological changes to the S. aureus ATCC 29213 surface caused by AqF, as well as significant size alterations. CONCLUSIONS: The results show potential antibacterial, antibiofilm and antitumoral activities of the ethanol extract and fractions of T. fagifolia.