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Colletia paradoxa (Spreng.) Esc. (Rhamnaceae, Colletieae) is a medicinal plant, threatened with extinction in Brazil, presenting great morphological variability. Our objective is to investigate the phytochemical components, antioxidant capacity and antimycobacterial activity of different morphotypes of C. paradoxa in different environments. For this, the crude extract of the leaves and branches of the individuals sampled was used. The elimination capacity of the free radicals was determined by the DPPH method, the antimycobacterial activity by the broth microdilution method and the phenolic content by the spectrophotometric method using the Folin-Ciocalteu reagent and by HPLC. The extracts of C. paradoxa and its morphotypes showed significant amounts of phenolic compounds, including quercetin, quercitrin and rutin, besides considerable antioxidant and antimycobacterial activity No connection was detected between the phytochemical composition and different morphotypes of C. paradoxa .

Zanthoxylum alatum Roxb. (Rutaceae) is a medicinal plant, which abundantly grows in the hilly areas of Pakistan. In the present study, the hepatoprotective activity of the Z. alatum whole fruit was evaluated. The hepatoprotective effect of the aqueous extracts was studied on mice liver damage using a single dose of paracetamol (640 mg/kg) orally by monitoring biochemical parameters. Pre-treatment of mice with Z. alatum (100 mg/kg) aqueous extract orally for four days prevented the paracetamol induced rise in serum transaminases (ALT and AST), restored the altered levels of antioxidant enzyme (catalase), thiobarbituric acid reactive substances (TBARS), non-protein thiol and ascorbic acid to near normal levels. The major phenolic acids, some flavonoid aglycone and glycosides were identified in fruit by high performance liquid chromatography. Ellagic acid (24.57±0.01mg/g), chlorogenic acid (10.65±0.01mg/g), gallic acid (9.15±0.02mg/g), chrysin (16.81±0.03), quercetin (16.81±0.03mg/g) and epicatechin (10.93±0.01) were prédominant in infusion of Z. alatum. The result substianted the hepatoprotective activity of Z. alatum which may be associated with its potential use in liver disease.

Psidium guajava is a Myrtaceae plant whose medicinal properties are recognized in several locations. The use of teas and tinctures prepared from their leaves has been used to combat infections caused by fungi of the genus Candida . In this study, aqueous extracts of leaves and hydroethanolic were tested to verify the antifungal potential and its chemical composition has been investigated. The microbiological assays were performed by broth microdilution to determine the minimum inhibitory concentration (MIC) and from these the minimum fungicidal concentration was performed (MFC) by subculturing on solid media. A cell viability curve was obtained for demonstration of inhibition of fungal growth of strains of Candida albicans and Candida tropicalis . Tests to check morphological changes by the action of the extracts were performed in microcultive cameras depleted environment at concentrations of MIC/2, MIC and MIC × 2. Extracts analyzed by high performance liquid chromatography demonstrated flavonoids and phenolic acids. The extracts showed fungistatic effect and no fungicide with MIC >8192 μg/mL, MFC above 8192 μg/mL. The IC 50 was calculated ranging from 1803.02 to 5623.41 μg/mL. It has been found that the extracts affect the morphological transition capability, preventing the formation of pseudohyphae and hyphae. Teas and tinctures, therefore, have the potential antifungal, by direct contact, causing inhibition of fungal multiplication and its virulence factor, the cell dimorphism, preventing tissue invasion. Further studies are needed to elucidate the biochemical pathways and genes assets involved in these processes.

Traditionally, Ilex paraguariensis leaves are consumed in tea form or as typical drinks like mate and terere, while the fruits are discarded processing and has no commercial value. The aim of this work to evaluate phytochemical properties, total phenolic compounds, antioxidant and antimicrobial activity of extracts of Ilex paraguariensis fruits obtained from supercritical CO 2 and compressed propane extraction. The extraction with compressed propane yielded 2.72 wt%, whereas with supercritical CO 2 1.51 wt% was obtained. The compound extracted in larger amount by the two extraction solvents was caffeine, 163.28 and 54.17 mg/g by supercritical CO 2 and pressurized propane, respectively. The antioxidant activity was more pronounced for the supercritical CO 2 extract, with no difference found in terms of minimum inhibitory concentration for Staphylococcus aureus for the two extracts and better results observed for Escherichia coli when using supercritical CO 2 .

The purpose of this study was to evaluate the antiproliferative and antigenotoxic activity of Sambucus australis Cham. & Schltdl. aqueous extracts on the cell cycle of Allium cepa L. as well as determine the phenolic compounds in such extracts. S. australis inflorescences and leaves of two accessions were used for aqueous extract preparation at concentrations: 0.003 g/ml and 0.012 g/ml. A. cepa bulbs were rooted in distilled water and, subsequently, placed in treatments for 24 hours. Rootlets were collected and fixed in modified Carnoy's solution for 24 hours and kept. The squash technique was performed for slide preparation. Root tips were smashed and stained with 2% acetic orcein, and a total of 4000 cells per treatment were analyzed. The phenolic compounds were determined using high-performance liquid chromatography and data was analyzed using the Scott-Knott test. The results show that S. australis aqueous extracts have antiproliferative potential. Besides, the extracts prepared from S. australis leaves of both accessions at a concentration of 0.012 g/ml have shown antigenotoxic activity. The phytochemical analysis allowed us to determine the presence of flavonoids and phenolic acids, of which kaempferol and chrologenic acid were the most predominant compounds in the extracts from the inflorescences and leaves, respectively.

Ethnopharmacological Relevance: Tabernaemontana catharinensis (Apocynaceae) is a medicinal plant used for the treatment of painful and inflammatory disorders. Here, we investigated the antinociceptive potential of the ethyl acetate fraction (Eta) from T. catharinensis leaves and assessed its toxic effects in mice to validate its popular use., Materials and Methods: Adult male Swiss mice (30-35g) were used. The Eta antinociceptive effect (200-800mg/kg, oral route (p.o.)) was evaluated in the acetic acid, formalin, capsaicin and tail-immersion tests. Adverse effects were analyzed using rotarod and open-field tests, body temperature, biochemical analysis and gastric lesions assessment. To evaluate the acute (OECD 423) or sub-acute (OECD 407) toxicity of the Eta, it was administered orally at a single (2000mg/kg) or repeated doses (100-400mg/kg/day for 28 days), respectively. Mortality, behavioral changes, biochemical and hematological parameters were evaluated. The Eta effect on cellular viability also was evaluated., Results: Eta (200-800mg/kg) inhibited the nociception caused by acetic acid (93.9±1.5%), formalin (86.2±10.8%) or capsaicin (75.4±3.3%) without inducing gastric lesions. Moreover, Eta neither altered the body temperature, biochemical parameters, nor forced or spontaneous locomotor activity of mice. The acute administration of the Eta (2000mg/kg) promoted a decrease in blood glucose levels and alanine aminotransferase activity. In the sub-acute toxicity study, Eta increased the aspartate aminotransferase activity (400mg/kg) and platelet distribution width (200mg/kg). Furthermore, Eta did not alter the cellular viability in cortical slices., Conclusions: Eta presents antinociceptive effects and mild toxicity in mice. These results support its traditional use as a potential analgesic., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

Background: Scutia buxifolia (Rhamnaceae) has been extensively studied for its phenolics groups, which are able to capture free radicals; being therefore, considered promising as an antioxidant in preventing diseases resulting from oxidative stress., Hypothesis: Scutia buxifolia extract (SBE) presents antinociceptive and anti-inflammatory effect in mice., Study Design: SBE (400-800mg/kg) was tested in different pain models to investigate its antinociceptive and anti-inflammatory action., Methods: It was carried out the abdominal writhing test, capsaicin test, thermal hyperalgesia and incisional pain. The inflamed tissue by carrageenan was used for the analysis of interleukins (IL), interferon-γ (IFN-γ), tumor necrosis factor-α (TNF-α), c-reactive protein (CRP), nitrite and nitrate (NOx) determination and myeloperoxidase (MPO) activity. Furthermore, we evaluate the possible action mechanism of SBE using naloxone in capsaicin test., Results: SBE prevented the nociception caused by acetic acid, formalin and capsaicin test. However, neither the SBE prevented the thermal hyperalgesia in hot-plate test, nor the naloxone reversed the SBE antinociceptive effect in capsaicin test. Furthermore, the administration of SBE prevented significantly the increase of MPO activity, the NOx content, and the levels of IL-1, IL-6, TNF-α, INF-γ and CRP and was able to increase the IL-10 levels after the inflammation induced by carrageenan in mice. In addition, SBE prevented mechanical hyperalgesia in a postoperative pain model., Conclusion: The SBE presents great antinociceptive and anti-inflammatory activity in mice but this effect not seem to have its action mechanism like opioids. It is possible that its antinociceptive effects are associated with levels decrease of inflammatory mediators., (Copyright © 2016. Published by Elsevier GmbH.)

Medicinal plants are often the only therapeutic resource for many communities and ethnic groups. Cordia verbenacea DC., "Erva-baleeira," is one of the species of plants currently used to produce a phytotherapeutic product extracted from its leaves. The present study aimed to establish its chemical profile, antibacterial activity and resistance-modulating potential. The C. verbenacea extracts were prepared from fresh leaves using solvents as methanol and hexane. Ethyl Acetate was used for the preparation of the fraction. Phytochemical screening was carried out using HPLC-DAD for determination and quantification of the secondary metabolites present in the fractions. Antibacterial and resistance-modulation assays were performed to determine minimum inhibitory concentration (MIC) using a microdilution assay. The data were subjected to statistical analysis with two-way ANOVA and Bonferroni posttests. Results of phytochemical prospecting and HPLC analysis of the fractions were in agreement with the literature. The natural products presented moderate antibacterial activity when considering the clinical relevance of a MIC of 256 μg/mL against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa, and 512 μg/mL against P. aeruginosa. However, when the fractions were combined with antibiotics we observed a synergic effect, as natural products enhanced the antibacterial effect of aminoglycosides, significantly decreasing the MIC of antibiotics at 12.5%-98.4%. We believe that the data obtained from phytochemical analysis and from antibacterial and resistance modulation assays of C. verbenacea extracts new can open perspectives in the search for new alternatives for the treatment of bacterial infections and stimulate the renewed use of antibiotics with reduced effectiveness due to resistance., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Adansonia digitata ( A .  digitata ) leaves serve as food and has several medicinal uses in many parts of the world. This study evaluated the influence of blanching on the phenolics composition, antioxidant activity, and inhibitory effect of methanol extract of A .  digitata leaves on the activities of some key enzymes ( α -amylase, α -glucosidase, and aldose reductase) implicated in type 2 diabetes (T2D) in vitro. Reverse-phase HPLC analysis revealed that the leaves had appreciable levels of flavonoids and phenolic acids, including catechin, epicatechin, rutin, quercitrin, quercetin, kaempferol, and luteolin (flavonoids); gallic, chlorogenic, caffeic, and ellagic acids (phenolic acids). Blanching caused significant ( P  < 0.05) decrease in the flavonoids and phenolic acids contents; DPPH* (2,2 diphenyl-1-picrylhydrazyl radical) and ABTS* + [2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) radical cation] scavenging ability; reducing power; and Fe 2+ -induced lipid peroxidation inhibitory capacity of the extract. Similarly, the inhibitory effect of the extract on the activities of α -amylase, α -glucosidase, and aldose reductase was significantly ( P  < 0.05) reduced due to blanching. Thus, A .  digitata leaves extract could be effective for the management of T2D due to its flavonoids and phenolic acids content, antioxidant properties, and inhibitory potency on the activities of α -amylase, α -glucosidase, and aldose reductase. However, blanching militated against the levels of these functional attributes of the leaves and, therefore, may not be recommended for their optimal retention.

This work describes the antiparasitic and cytotoxic activities of three plant species from the Cerrado biome, Northeastern Brazil. Significant antiparasitic inhibition was observed against Trypanosoma cruzi (63.86%), Leishmania brasiliensis (92.20%) and Leishmania infantum (95.23%) when using ethanol extract from leaves of Guazuma ulmifolia Lam. (Malvaceae), at a concentration of 500 μg/mL. However, low levels of inhibition were observed when assessing leishmanicidal and trypanocidal (Clone CL-B5) activities of crude ethanol extracts from leaves and bast tissue of Luehea paniculata (Malvaceae) and leaves and bark of Prockia crucis (Salicaceae) at a concentration of 500 μg/mL. The extracts revealed the presence of phenolic acids such as gallic acid, chlorogenic acid, caffeic acid and rosmarinic acid, as well as flavonoids such as rutin, luteolin, apigenin and quercetin - the latter detected only in G. ulmifolia. G. ulmifolia extract displayed higher leishmanicidal activity probably due to the presence of quercetin, a potent known leishmanicidal compound. A cytotoxicity test indicated values over 50% at the highest concentration (1000 μg/mL) for all natural products, which were considered cytotoxic. This points out the need for further tests to enable future in vivo trials, including antineoplastic activity on human tumor cells.

Inflammation exerts a crucial pathogenic role in the development of hypertension. Hence, the aim of the present study was to investigate the effects of ginger (Zingiber officinale) and turmeric (Curcuma longa) on enzyme activities of purinergic and cholinergic systems as well as inflammatory cytokine levels in Nω-nitro-L-arginine methyl ester hydrochloride-induced hypertensive rats. The rats were divided into seven groups (n = 10); groups 1-3 included normotensive control rats, hypertensive (Nω-nitro-L-arginine methyl ester hydrochloride) rats, and hypertensive control rats treated with atenolol (an antihypertensive drug), while groups 4 and 5 included normotensive and hypertensive (Nω-nitro-L-arginine methyl ester hydrochloride) rats treated with 4 % supplementation of turmeric, respectively, and groups 6 and 7 included normotensive and hypertensive rats treated with 4 % supplementation of ginger, respectively. The animals were induced with hypertension by oral administration of Nω-nitro-L-arginine methyl ester hydrochloride, 40 mg/kg body weight. The results revealed a significant increase in ATP and ADP hydrolysis, adenosine deaminase, and acetylcholinesterase activities in lymphocytes from Nω-nitro-L-arginine methyl ester hydrochloride hypertensive rats when compared with the control rats. In addition, an increase in serum butyrylcholinesterase activity and proinflammatory cytokines (interleukin-1 and - 6, interferon-γ, and tumor necrosis factor-α) with a concomitant decrease in anti-inflammatory cytokines (interleukin-10) was observed in Nω-nitro-L-arginine methyl ester hydrochloride hypertensive rats. However, dietary supplementation of both rhizomes was efficient in preventing these alterations in hypertensive rats by decreasing ATP hydrolysis, acetylcholinesterase, and butyrylcholinesterase activities and proinflammatory cytokines in hypertensive rats. Thus, these activities could suggest a possible insight about the protective mechanisms of the rhizomes against hypertension-related inflammation., (Georg Thieme Verlag KG Stuttgart · New York.)

Recently, ginger has been used in traditional Chinese medicine as an herbal therapy for treating several cardiovascular diseases, however, information on its mechanism of action is limited. The present study assessed the effect of two ginger varieties (Zingiber officinale and Curcuma longa) on the arginase activity, atherogenic index, levels of liver thiobarbituric acid reactive substances (TBARSs), and plasma lipids in rats fed with a high-cholesterol (2%) diet for 14 days. Following the treatment period, it was found that feeding a high-cholesterol diet to rats caused significant (p < 0.05) increases in arginase activity, atherogenic index, levels of TBARS, total cholesterol (TC), triglycerides (TGs), and low-density lipoprotein cholesterol (LDL-C) with a concomitant decrease in high-density lipoprotein cholesterol (HDL-C). However, both ginger and turmeric (2% and 4%) caused significant (p < 0.05) decreases in arginase activity and the atherogenic index, and prevented hypercholesterolemia by decreasing the TC, TGs, and LDL-C while increasing the HDL-C when compared with the controls. In conclusion, dietary supplementation with both types of rhizomes (ginger and turmeric) inhibited arginase activity and prevented hypercholesterolemia in rats that received a high-cholesterol diet. Therefore, these activities of ginger and turmeric represent possible mechanisms underlying its use in herbal medicine to treat several cardiovascular diseases., (Copyright © 2015. Published by Elsevier B.V.)

Background/aim: Elevated uric acid level, an index of gout resulting from the over-activity of xanthine oxidase (XO), increases the risk of developing hypertension. However, research has shown that plant-derived inhibitors of XO and angiotensin 1-converting enzyme (ACE), two enzymes implicated in gout and hypertension, respectively, can prevent or ameliorate both diseases, without noticeable side effects. Hence, this study characterized the polyphenolics composition of guava leaves extract and evaluated its inhibitory effect on XO and ACE in vitro., Materials and Methods: The polyphenolics (flavonoids and phenolic acids) were characterized using high-performance liquid chromatography (HPLC) coupled with diode array detection (DAD). The XO, ACE, and Fe(2+)-induced lipid peroxidation inhibitory activities, and free radicals (2,2-diphenylpicrylhydrazyl [DPPH]* and 2,2´-azino-bis-3-ethylbenzthiazoline-6-sulphonic [ABTS]*(+)) scavenging activities of the extract were determined using spectrophotometric methods., Results: Flavonoids were present in the extract in the order of quercetin > kaempferol > catechin > quercitrin > rutin > luteolin > epicatechin; while phenolic acids were in the order of caffeic acid > chlorogenic acid > gallic acids. The extract effectively inhibited XO, ACE and Fe(2+)-induced lipid peroxidation in a dose-dependent manner; having half-maximal inhibitory concentrations (IC50) of 38.24 ± 2.32 μg/mL, 21.06 ± 2.04 μg/mL and 27.52 ± 1.72 μg/mL against XO, ACE and Fe(2+)-induced lipid peroxidation, respectively. The extract also strongly scavenged DPPH* and ABTS*(+)., Conclusion: Guava leaves extract could serve as functional food for managing gout and hypertension and attenuating the oxidative stress associated with both diseases.

Euphorbia tirucalli (L.), commonly known as aveloz, has been indiscriminately used in popular medicine to treat various illnesses. However, some components can have devastating consequences. Injury to a cell's genetic material can cause mutations, cancer, and cell death. Our main goal in this work was to evaluate the genotoxic and cytotoxic effects of E. tirucalli extract on human leukocytes. For this purpose, we performed a phytochemical analysis to evaluate the plant's components. In the second step, we treated cultured human leukocytes with different concentrations of the dry extract of the plant and then evaluated the oxidative and genotoxic profiles of these leukocytes. We found that at 1% and 10% concentrations, the aveloz extract acted as a genotoxic agent that could damage DNA and increase oxidative damage. We conclude that despite its popular use, aveloz can act as a genotoxic agent, especially when it contains phorbol ester. Aveloz's indiscriminate use might actually promote tumors and therefore carry a considerable genetic risk for its users.

Ethnopharmacological Relevance: Scutia buxifolia is a tree native to South America and is used as a cardiotonic agent; however, this property has not been associated with a clear mechanism or a specific compound., Aim of the Study: Given the importance of Na(+),K(+)-ATPase as a drug target in the treatment of heart failure, this study aimed to investigate the possible inhibitory effect of S. buxifolia crude extract and fractions (dichloromethane, ethyl acetate, and butanolic fractions), and identified compounds with effects on the activity of Na(+),K(+)-ATPase in vitro., Materials and Methods: First, we characterized the crude extract and fractions by high-performance liquid chromatography, and then monitored their effects on the activity of Na(+),K(+)-ATPase obtained from heart muscle and brain membranes of adult male Wistar rats., Results: We identified gallic acid, chlorogenic acid, caffeic acid, rutin, quercitrin, quercetin, and ursolic acid in S. buxifolia stem bark and leaves; quercitrin and ursolic acid were the main compounds in the ethyl acetate and dichloromethane fractions from leaves and stem bark. The crude extract (3 and 30mg/ml), and the ethyl acetate and dichloromethane fractions (0.1 and 1mg/ml) of both the stem bark and leaves inhibited Na(+),K(+)-ATPase activity in heart and brain samples. We found that, of the identified compounds, only ursolic acid (0.1mg/ml) was able to diminish Na(+), K(+)-ATPase activity in heart and brain samples., Conclusions: These data indicated that the cardiotonic effects of S. buxifolia may be due to the inhibition of Na(+),K(+)-ATPase activity in heart muscle, supporting the popular use of this plant as a treatment for heart failure., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

The infusion of Baccharis trimera (Less) DC, popularly known as "carqueja" (broom), is popularly used in the treatment of hepatic and digestive problems. In this study, we evaluated the acute and sub-chronic oral toxicities of B. trimera tincture on male and female Wistar rats according to Organization for Economic Cooperation and Development (OECD, guidelines 423 e 407, respectively). The B. trimera tincture was administered by oral gavage in a single dose (2000 mg/kg) in doses of 100, 200 and 400 mg/kg daily for 28 days. Blood was collected to analyze hematological and biochemical parameters. Kidneys and liver were homogenized to determine lipid peroxidation and δ-aminolevulinate dehydratase (δ-ALA-D) and catalase (CAT) enzyme activities. In acute treatment, tincture did not induce any signs of toxicity or mortality. Daily oral administration produced no significant changes in the hematological and biochemical parameters, except for the hepatic enzymes alanine aminotransferase (ALAT) and aspartate aminotransferase (ASAT) that showed a reduction in both sexes. Moreover, the B. trimera tincture did not increase lipid peroxidation or affected ALA-D and CAT activities. In conclusion, the tincture of B. trimera may be considered relatively safe in this protocol., (Copyright © 2015 Elsevier Inc. All rights reserved.)

Unlabelled: Background. Duguetia furfuracea is popular plant used in popular medicine. Hypothesis/Purpose. This claim evaluated the phytochemical composition of the hydroethanolic extract (HEDF), fractions of Duguetia furfuracea, and antioxidant and antifungal activity. Methods. The chemical profile was carried out by HPLC-DAD. The total phenolic contents and flavonoid components were determined by Folin-Ciocalteu and aluminium chloride reaction. The antioxidant activity was measured by scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical and ferric reducing ability of plasma (FRAP) methods. The antifungal activity was determined by microdilution assay., Results: HPLC analysis revealed caffeic acid and rutin as major compounds (HEDF), caffeic acid and quercitrin (Mt-OH fraction), and quercitrin and isoquercitrin (Ac-OEt fraction). The highest levels of phenols and total flavonoids were found for Ac-OEt fraction, and the crude extract showed higher in vitro antioxidant potential. The antifungal activity showed synergic effect with fluconazole and EHDF against C. krusei, fluconazole and Mt-OH against C. krusei and C. tropicalis, and Ac-OE and fluconazole against C. albicans. Conclusion. The highest levels of phenols and total flavonoids were marked with antioxidant effect. This is the first report of bioactivity of the synergic effect of HEDF and fractions. More studies would be required to better clarify its mechanism of synergic action.

Context: Syzygium cumini (Myrtaceae) presents antioxidant, anti-inflammatory, hypoglycemic and antibacterial effects; however, the cellular and molecular mechanisms of action in the immune system are not yet completely elucidated., Objective: This study evaluates the in vitro effect of gallic acid and aqueous S. cumini leaf extract (ASc) on adenosine deaminase (ADA) and dipeptidyl peptidase IV (DPP-IV) activities, cell viability and oxidative stress parameters in lymphocytes exposed to 2, 2'-azobis-2-amidinopropane dihydrochloride (AAPH)., Materials and Methods: Lymphocytes were incubated with ASc (100 and 500 µg/ml) and gallic acid (50 and 200 µM) at 37 °C for 30 min followed by incubation with AAPH (1 mM) at 37 °C for 2 h. After the incubation time, the lymphocytes were used for determinations of ADA, DPP-IV and lactate dehydrogenase (LDH) activities, lipid peroxidation, protein thiol (P-SH) group levels and cellular viability by colorimetric methods., Results: (i) HPLC fingerprinting of ASc revealed the presence of catechin, epicatechin, rutin, quercitrin, isoquercitrin, quercetin, kaempferol and chlorogenic, caffeic, gallic and ellagic acids; (ii) for the first time, ASc reduced the AAPH-induced increase in ADA activity, but no effect was observed on DPP-IV activity; (iii) ASc increased P-SH groups and cellular viability and decreased LDH activity, but was not able to reduce the AAPH-induced lipid peroxidation; (iv) gallic acid showed less protective effects than ASc., Discussion and Conclusion: ASc affects the purinergic system and may modulate adenosine levels, indicating that the extract of this plant exhibits immunomodulatory properties. ASc also may potentially prevent the cellular injury induced by oxidative stress, highlighting its cytoprotective effects.

The study investigated the hypoglycemic and anticholinesterase activities of some fermented legumes (bambara groundnut and locust bean) in Streptozotocin (STZ)-induced diabetic rats. The rats were made diabetic by intraperitoneal administration of STZ (35mg/kg b.w.) and were fed diets containing fermented legumes (10% inclusion) for 14 days. The effect of the diets on blood glucose, pancreatic glutathione peroxidase (GPx) activity, reduced glutathione (GSH) and malondialdehyde (MDA) contents, α-amylase, intestinal α-glucosidase and acetylcholinesterase activities were studied. Significant (P<0.05) increase in blood glucose, pancreatic MDA, α-amylase, intestinal α-glucosidase and acetylcholinesterase activities with concomitant decrease in pancreatic GPx and GSH contents were observed in diabetic rats. However, this trend was reversed in rats fed fermented legumes supplemented diets for 14 days. The HPLC-DAD finger printing revealed the presence of gallic acid, catechin, caffeic acid, epicatechin, rutin, isoquercitrin, quercitrin, quercetin and kaempferol as the dominant phenolic compounds of the fermented legumes. However, possible contributing role of some bioactive peptides could not be ruled out. Hence, the hypoglycemic and antiacetylcholinesterase activities of the fermented legume condiments could be attributed to their constituent phytochemicals., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

The aim of this study was to evaluate the chemical profile and antioxidant, antimicrobial and antiparasitic activities of the hydroalcoholic extract of the leaves of Ziziphus joazeiro Mart. (HELZJ). The antioxidant DPPH and FRAP assays and chemical profile were determined by colorimetric methods and HPLC/DAD. The antiparasitic, antibiotic and antibiotic-modifying activity were evaluated by microdilution assays. The HPLC-DAD assay showed the presence of mostly tannins and flavonoids, such as caffeic acid and quercetin. The levels of polyphenols and flavonoids were 183.136 mg/g extract and 7.37 mg/g extract, respectively. DPPH and FRAP showed low antioxidant activity for the extract. The antibacterial and antifungal activities were not of clinical relevance, showing MIC>1024 μg/mL. However, synergism was observed between HELZJ and the antibiotics amikacin and gentamicin, which resulted in decreased bacterial drug resistance. EHFZJ showed low toxicity in fibroblasts in vitro, while antiparasitic results against Trypnosoma cruzi, Leishmania braziliensis and Leishmania infantum were not clinically relevant. Thus, our results indicate that Z. joazeiro Mart. (HELZJ) could be a source of plant-derived natural products that could lead to the development of promising new antibiotic compounds for infectious diseases., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Recent interest in flavonoids has increased greatly due to their biological and pharmacological activities. Flavonoids consist of a large group of low molecular weight polyphenolic substances, naturally occurring in fruits, vegetables and tea, and are an integral part of the human diet. Quercetin and rutin are bioactive markers of Scutia buxifolia and no analytical methods reported so far, associated with quality control of polyherbal formulations containing this species. Therefore, there is a need to develop a sensitive, simple, rapid and reliable method that can simultaneously determine these markers in their combinations. A high-performance liquid chromatography method has been developed and validated as per ICH guidelines. The chromatographic analysis was performed using a C18 column, the mobile phase system consisted of acetonitrile-water (70 : 30, v/v) containing 0.5% (v/v) phosphoric acid and quercetin and rutin were quantificadoa to 356 nm. The proposed method for the quantification of quercetin and rutin in the S. buxifolia fraction (EaSb) and gel was linear, sensitive, precise, specific, accurate and robust. This validated method can be used to control the quality of the EaSb and the gel., (© The Author 2015. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.)

Psidium guajava (Myrtaceae), a common plant in Cariri region, Ceara, Brazil, as well as in various parts of the world, contains high concentrations of bioactive compounds and in many communities its parts are used for therapeutic purposes. Studies describe antioxidant, antimicrobial and anti-diarrheal actions from extracts obtained from leaves, but information about the activities of the fruits and comparison of these at different maturity stages (immature, partially mature and mature) are scarce. This study aims to evaluate the antioxidant properties by quantifying the levels of phenolic and flavonoid compounds, carotenoids and vitamin C of P. guajava fruits at different stages of maturation. The content of phenolic compounds for the immature fruit, partially mature and mature were: 22.41; 34.61 and 32.92 mg of AG/g fraction. The flavonoid content for immature fruits, intermediate and mature were: 2.83; 5.10 and 5.65 mg RUT/g fraction, respectively. Following the same standards of maturation stages, the ascorbic acid content was determined with values of 0.48; 0.38 and 0.21 mg AA/g fraction, respectively. HPLC analysis identified and quantified the presence of gallic acid, catechin, chlorogenic acid, caffeic acid, epicatechin, rutin, quercitrin, isoquercitrin, quercetin, kaempferol, glycosylated campeferol, tocopherol, β-carotene and lycopene. The antioxidant activity carried out by DPPH method showed the mature fruits bearing the best results, whereas chelation of Fe2+ ions showed higher percentage for the immature fruit. The results obtained by lipidic peroxidation were not satisfactory.

Background: Citrus peels are consumed in the form of infusions, candy or wine, based on their well-documented nutritional and medicinal properties. This study sought to investigate the effect of some citrus peels' [grapefruit (Citrus paradisii), orange (Citrus sinensis) and shaddock (Citrus maxima)] extracts on matrix metalloproteinase (MMP) and proteasome activities in primary human colonic tumor (Caco-2) and the metastatic cell lines (LoVo and LoVo/ADR) in a bid to explain the possible mechanism by which the peels could manage/prevent colon cancer., Methods: The inhibition of MMP and proteasome activities in the cells by the peel extracts, as well as the identification of phenolic compounds using high-performance liquid chromatography with diode-array detection (HPLC-DAD), was determined., Results: Orange peel extracts had the strongest inhibition of MMP in Caco-2 and LoVo cells, while shaddock had the least. Shaddock peel extracts also had the least MMP inhibition in LoVo/ADR lysates. Grapefruit had the least proteasome inhibition in Caco-2 and LoVo lysates, while there was no significant (p>0.05) difference in the proteasome inhibition of the peel extracts in LoVo/ADR lysates. The extracts inhibited proteasome activity in extract-treated cells, and HPLC fingerprinting of the extracts revealed the presence of some phenolic compounds such as quercetin, caffeic acid, kaempferol, catechin and naringin., Conclusions: The inhibition of MMP and proteasome activities in colon cancer cell lines suggests the potential use of citrus peels as functional food in the management and/or prevention of colon cancer.

Background: The effects of the aqueous seed extract of Syzygium cumini (ASc) in a short-term model of diabetes in rats are little explored. The present study was designed to evaluate the effect of the ASc on adenosine deaminase (ADA) activity and on biochemical and histopathological parameters in diabetic rats., Methods: ASc (100 mg/kg) was administered for 21 days in control and streptozotocin (STZ)-induced (60 mg/kg) diabetic rats. ADA activity, lipoperoxidation (cerebral cortex, kidney, liver and pancreas) and biochemical (serum) and histopathological (pancreas) parameters were evaluated., Results: The main findings in this short-term model of Diabetes mellitus (DM) were that the ASc (i) significantly reverted the increase of ADA activity in serum and kidney; (ii) ameliorated the lipoperoxidation in the cerebral cortex and pancreas of the diabetic group; (iii) demonstrated hypolipidemic and hypoglycemic properties and recovered the liver glycogen; and iv) prevented the HOMA-IR index increase in the diabetic group. Therefore, the ASc can be a positive factor for increasing the availability of substrates with significant protective actions, such as adenosine. Moreover, by maintaining glycogen and HOMA-IR levels, the extract could modulate the hyperglycemic state through the direct peripheral glucose uptake., Conclusions: Our data revealed that the short-term treatment with ASc has an important protective role under pathophysiological conditions caused by the early stage of DM. These results enhance our understanding of the effect of the ASc on the purinergic system in DM.

Ethnopharmacological Relevance: Scutia buxifolia, a native tree popularly known as "coronilha", is widely used in Brazilian folk medicine for diuretic and anti-hypertensive purposes., Aim of the Study: We investigated the effects of a butanolic (BuOH) soluble fraction of the hydroethanolic extract (HESB) of bark of Scutia buxifolia on both blood pressure and urinary excretion of rats. The involvement of the nitric oxide/guanylate cyclase pathway in the hypotensive effect found was also explored., Material and Methods: We tested the effect of the BuOH soluble fraction of HESB on the mean arterial pressure (MAP) of anesthetized rats. The fraction was administered at doses of 1, 3 and 10mg/kg (i.v.) in normotensive rats during continuous infusion of vehicle (10 μl/min), or phenylephrine (4 μg/kg/min), or l-NAME (7 mg/kg/min), two approaches able to induce a sustained hypertensive state. In some experiments, a bolus injection of ODQ (2mg/kg) was administered in animals infused with phenylephrine before the administration of the BuOH soluble fraction of HESB. We also measured the effects of the BuOH soluble fraction on the MAP of spontaneously hypertensive rats (SHR). Separate groups of rats were treated orally with either HESB (10, 30 or 100mg/kg), or its BuOH soluble fraction (3, 10 or 30 mg/kg), and were subjected to measurement of diuresis and blood pressure., Results: The BuOH soluble fraction of HESB (10mg/kg, i.v.) reduced the MAP of both phenylephrine-infused and SHR rats by 20.6 ± 6.0 and 41.8 ± 8.3 mm Hg, respectively. However, no hypotensive effect was found in normotensive animals infused with l-NAME, a non-selective inhibitor of nitric oxide synthase, or animals previously treated with the soluble guanylate cyclase inhibitor ODQ. The urinary excretion was increased by 70% at 6-8h after a single oral administration of the BuOH soluble fraction of HESB (10mg/kg), without change in urinary density, pH, or Na(+) and K(+) concentrations. In addition, MAP was lower 3h after the acute oral treatment with the BuOH soluble fraction (82.1 ± 3.8 mm Hg), compared with MAP of animals from the control group (97 ± 3.2 mm Hg)., Conclusion: This study demonstrates that the BuOH soluble fraction of the hydroethanolic bark of Scutia buxifolia, which has its bark used in folk medicine for the treatment of hypertension mainly by its presumed diuretic properties, possesses both diuretic and hypotensive effects in rats, and that at least the hypotensive effect is fully dependent on activation of the nitric oxide/guanylate cyclase pathway., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

Phenolic compounds of unripe and ripe sweet orange peels were determined using a high-performance liquid chromatography separation method with diode array detector (HPLC-DAD). The in vitro antioxidant properties and the EC50 (concentration required to obtain a 50% antioxidant effect) values were also determined. The predominant phenolic compounds were quercitrin, rutin, and quercetin with values of 18.77 ± 0.01 mg/mL, 18.65 ± 0.03 mg/mL, and 10.39 ± 0.01 mg/mL respectively in unripe orange peel and 22.61 ± 0.01 mg/mL, 17.93 ± 0.03 mg/mL, and 14.03 ± 0.02 mg/mL respectively in ripe orange peel. The antioxidant properties revealed 2,2'-azino-bis(3-ethyl benzothiazoline-6-sulfonic acid) diammonium salt (ABTS) scavenging ability of both unripe and ripe orange peels respectively as 14.68 ± 0.01 and 16.89 ± 0.02 mmol TEAC/g, the Ferric Reducing Antioxidant Properties (FRAP) as 70.69 ± 0.01 and 91.38 ± 0.01 mg gallic acid equivalents/100g, total phenol content as 5.27 ± 0.03 and 9.40 ± 0.01 mg gallic acid equivalents/g and total flavonoid content as 3.30 ± 0.30 and 4.20 ± 0.02 mg quercetin equivalent/g. The antioxidant assays showed enhanced potency of extract from ripe orange peel with EC50 values of 2.71 ± 0.03 mg/mL for 2,2-diphenyl-1-picrylhydrazyl (DPPH), 0.67 ± 0.03 mg/mL for hydroxyl radicals (OH*), 0.57 ± 0.02 mg/mL for Fe(2+) chelation, and 0.63 ± 0.06 mg/mL for malondialdehyde (MDA), and was more potent than unripe orange peel.

Background: Considering that adjuvant arthritis is an experimental model of arthritis widely used for preclinical testing of numerous anti-arthritic agents, which were taken by a large number of patients worldwide, it is of great interest to investigate the therapeutic action of compounds with anti-inflammatory properties, such as Uncaria tomentosa extract. Moreover, there are no studies demonstrating the effect of U. tomentosa on the metabolism of adenine nucleotides published so far. Thus, the purpose of the present study is to investigate the effects of U. tomentosa extract on E-NTPDase and E-ADA activities in lymphocytes of Complete Freund's Adjuvant (CFA) arthritis induced rats., Methods: To evaluate the effect of U. tomentosa extract on the activity of E-NTPDase and ADA in lymphocytes, the rats were submitted to an experimental adjuvant arthritis model. Peripheral lymphocytes were isolated and E-NTPDase and E-ADA activities were determined. Data were analyzed by a one- or two-way ANOVA. Post hoc analyses were carried out by the Student-Newman-Keuls (SNK) Multiple Comparison Test., Results: E-NTPDase activity was increased in arthritic untreated. Arthritic rats which received U. tomentosa extract, presented similar results to the control group. However, results obtained for adenosine hydrolysis by E-ADA were not altered in arthritic rats. U. tomentosa extract did not alter E-NTPDase and E-ADA activity in healthy animals., Conclusions: The present investigation supports the hypothesis that the increased E-NTPDase activity verified in arthritic rats might be an attempt to maintain basal levels of ATP and ADP in the extracellular medium, since the arthritis induction causes tissue damage and, consequently, large amounts of ATP are released into this milieu. Also, it highlights the possibility to use U. tomentosa extract as an adjuvant to treat arthritis.

Oxidative stress has been implicated in several pathologies including neurological disorders. Centella asiatica is a popular medicinal plant which has long been used to treat neurological disturbances in Ayurvedic medicine. In the present study, we quantified of compounds by high performance liquid chromatography (HPLC) and examined the phenolic content of infusion, ethyl acetate, n-butanolic and dichloromethane fractions. Furthermore, we analyzed the ability of the extracts from C. asiatica to scavenge the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) radical as well as total antioxidant activity through the reduction of molybdenum (VI) (Mo(6+)) to molybdenum (V) (Mo(5+)). Finally, we examined the antioxidant effect of extracts against oxidant agents, quinolinic acid (QA) and sodium nitroprusside (SNP), on homogenates of different brain regions (cerebral cortex, striatum and hippocampus). The HPLC analysis revealed that flavonoids, triterpene glycoside, tannins, phenolic acids were present in the extracts of C. asiatica and also the phenolic content assay demonstrated that ethyl acetate fraction is rich in these compounds. Besides, the ethyl acetate fraction presented the highest antioxidant effect by decreasing the lipid peroxidation in brain regions induced by QA. On the other hand, when the pro-oxidant agent was SNP, the potency of infusion, ethyl acetate and dichloromethane fractions was equivalent. Ethyl acetate fraction from C. asiatica also protected against thiol oxidation induced by SNP and QA. Thus, the therapeutic potential of C. asiatica in neurological diseases could be associated to its antioxidant activity.

American foulbrood (AFB) is a serious worldwide spreading disease in bees caused by Paenibacillus larvae. Plants extracts are known to decrease or inhibit the growth of these bacteria. The purpose of this study was to evaluate the antimicrobial activity of Calendula. officinalis, Cariniana domestica, and Nasturtium officinale extracts against the P. larvae and to evaluate the toxicity of the extracts in bees. In vitro activity against P. larvae of the extracts was evaluated by micro dilution method and the minimal inhibitory concentrations (MICs) were also determined. The concentrations used in the toxicity test were established based on the MIC values and by the spraying application method. The P. larvae was susceptible to the evaluated crude extract of C. officinalis and N. officinale. To C. domestica, only the ethyl acetate (EtAc) fraction and n-butanol (BuOH) fractions had activity against P. larvae. Toxicity analysis in bees showed no toxicity for N. officinale crude extract and for C. domestica BuOH fraction during 15 days of treatment, however, some deaths of bees occurred during the first three days of treatment with C. officinalis and C. domestica EtAc fraction. The results with these species were firstly described and showed that N. officinale crude extract and C. domestica BuOH fraction both presented not toxic effects in the concentration tested by the spraying application method, and can be a useful alternative for treatment or prevention of AFB.

This study aimed to evaluate the repellent effect of tea tree (Melaleuca alternifolia) and andiroba (Carapa guianensis) essential oils on two species of flies (Haemotobia irritans and Chrysomya megacephala). For the in vitro studies, free-living adult flies were captured and reared in the laboratory. To verify the repellency effect, an apparatus was constructed where H. irritans and C. megacephala were exposed to andiroba and tea tree oils (5.0%), as well as to a known repellent (citronella, 5.0%) to validate the test. The study demonstrated that all three oils used showed in vitro repellent effect against both species of flies. It is possible to conclude that the essential oils (tea tree and andiroba) have repellent effect on these species of flies used in this study.

Context: Murraya paniculata (Linn) JACK (Rutaceae) is used in traditional medicine in the treatment of diabetes, inflammation, and microbial disorders., Objective: This study determined the polyphenol composition and antimicrobial and acute toxicological activity of the hydroethanolic extract of M. paniculata leaves (EEMp)., Materials and Methods: Chemical composition was evaluated by the Folin-Ciocalteu and AlCl3 assays and by HPLC-DAD. Antibacterial and modulatory activity was determined by the microdilution method. Toxicity was assessed with a single dose of EEMp administered orally at doses of 2000 and 5000 mg/kg body weight/day in male and female Swiss mice., Results: Total phenolic content of the EEMp samples varied from 66.5 to 396.8 mg gallic acid equivalent/g of extract and flavonoid content varied from 0.3 to 31.1 mg quercetin equivalent/g of extract. The principal component identified by HPLC-DAD assay was ellagic acid. The results of oral acute toxicity showed no mortality, changes in hematological parameters, or CNS and ANS toxicities in rats. Biochemical analysis showed a significant increase in glucose and glutamic oxaloacetic transaminase activity and reduction in triglycerides and cholesterol for 5000 and 2000 mg/kg doses, respectively, when compared with the control group. Histopathological evaluation showed no significant microscopic changes. EEMp showed essentially no antimicrobial activity, but when aminoglycosides were combined with EEMp their MIC was reduced., Conclusions: Significant effects were observed in the acute toxicity assay, but they had no clinical relevance. The results suggest that M. paniculata could be used as a source of natural products with antibacterial resistance-modifying activity, with lower toxicity.

This study aimed to verify the effect of the treatment with A. satureioides essential oil (free and nanoencapsulated forms) and diminazene aceturate on hematological and biochemical variables in rats infected by Trypanosoma evansi. The 56 rats were divided into seven groups with eight rats each. Groups A, C and D were composed by uninfected animals, and groups B, E, F and G were formed by infected rats with T. evansi. Rats from groups A and B were used as negative and positive control, respectively. Rats from the groups C and E were treated with A. satureioides essential oil, and groups D and F were treated with A. satureioides nanoencapsulated essential oil. Groups C, D, E and F received one dose of oil (1.5 mL kg(-1)) during five consecutive days orally. Group G was treated with diminazene aceturate (D.A.) in therapeutic dose (3.5 mg kg(-1)) in an only dose. The blood samples were collected on day 5 PI for analyses of hematological (erythrocytes and leukocytes count, hemoglobin concentration, hematocrit, mean corpuscular and mean corpuscular hemoglobin concentration) and biochemical (glucose, triglycerides, cholesterol, alanine aminotransferase (ALT), aspartate aminotransferase (AST), albumin, urea and creatinine) variables. A. satureioides administered was able to maintain low parasitemia, mainly the nanoencapsulated form, on 5 days post infection. On the infected animals with T. evansi treated with A. satureioides essential oil (free and nanocapsules) the number of total leucocytes, lymphocytes and monocytes present was similar to uninfected rats, and different from infected and not-treated animals (leukocytosis). Treatment with A. satureioides in free form elevated levels of ALT and AST, demonstrating liver damage; however, treatment with nanoencapsulated form did not cause elevation of these enzymes. Finally, treatments inhibited the increase in creatinine levels caused by infection for T. evansi. In summary, the nanoencapsulated form showed better activity on the trypanosome; it did not cause liver toxicity and prevented renal damage., (Copyright © 2014 Elsevier Inc. All rights reserved.)

The jaboticaba tree, Plinia trunciflora (O. Berg) Kausel, is popularly named "jabuticabeira" in Brazil and is used in folk medicine to treat diabetes and chronic inflammation of the tonsils, but studies evaluating the central effects of this species are limited. This study evaluated the antidepressant-like and antioxidant effects of P. trunciflora (PT) aqueous extract, in which five different anthocyanins were identified. PT showed significant ferric-reduction power and DPPH radical scavenging activity in vitro and reduced lipid peroxidation both in vitro and ex vivo. At the behavioural level, PT (400 and 800 mg/kg, i.p.) dose-dependently reduced immobility time in the tail suspension test in Swiss male mice. The identification of bioactive compounds accompanied by the in vitro and ex vivo antioxidant activity of PT suggests that these activities might be related to the antidepressant-like activity of P. trunciflora.

This study was designed to determine the antioxidant properties and inhibitory effects of extract from Moringa oleifera leaves on angiotensin-I-converting enzyme (ACE) and arginase activities in vitro. The extract was prepared and phenolic (total phenols and flavonoid) contents, radical (nitric oxide (NO), hydroxyl (OH)) scavenging abilities, and Fe(2+)-chelating ability were assessed. Characterization of the phenolic constituents was done via high performance liquid chromatography-diode array detection (HPLC-DAD) analysis. Furthermore, the effects of the extract on Fe(2+)-induced MDA production in rats' penile tissue homogenate as well as its action on ACE and arginase activities were also determined. The extract scavenged NO (∗) , OH (∗) , chelated Fe(2+), and inhibited MDA production in a dose-dependent pattern with IC50 values of 1.36, 0.52, and 0.38 mg/mL and 194.23 µg/mL, respectively. Gallic acid, chlorogenic acid, quercetin, and kaempferol were the most abundant phenolic compounds identified in the leaf extract. The extract also inhibited ACE and arginase activities in a dose-dependent pattern and their IC50 values were 303.03 and 159.59 µg/mL, respectively. The phenolic contents, inhibition of ACE, arginase, and Fe(2+)-induced MDA production, and radical (OH (∗) , NO (∗) ) scavenging and Fe(2+)-chelating abilities could be some of the possible mechanisms by which M. oleifera leaves could be used in the treatment and/or management of erectile dysfunction.

Silymarin is a standardized extract from the dried seeds of the milk thistle (Silybum marianum L. Gaertn.) clinically used as an antihepatotoxic agent. The aim of this study was to investigate the antibacterial and antifungal activity of silymarin and its major constituent (silibinin) against different microbial strains and their modulatory effect on drugs utilized in clinical practice. Silymarin demonstrated antimicrobial activity of little significance against the bacterial strains tested, with MIC (minimum inhibitory concentration) values of 512 µg/mL. Meanwhile, silibinin showed significant activity against Escherichia coli with a MIC of 64 µg/mL. The results for the antifungal activity of silymarin and silibinin demonstrated a MIC of 1024 µg/mL for all strains. Silymarin and silibinin appear to have promising potential, showing synergistic properties when combined with antibacterial drugs, which should prompt further studies along this line.

Huntington's disease (HD) is an autosomal dominant neurodegenerative disease. Accordingly, 3-nitropropionic acid (3-NP) has been found to effectively produce HD-like symptoms. Luehea divaricata (L. divaricata), popularly known in Brazil as "açoita-cavalo," may act as a neuroprotective agent in vitro and in vivo. We evaluated the hypothesis that the aqueous extract of L. divaricata could prevent behavioral and oxidative alterations induced by 3-NP in rats. 25 adult Wistar male rats were divided into 5 groups: (1) control, (2) L. divaricata (1000 mg/kg), (3) 3-NP, (4) L. divaricata (500 mg/kg) + 3-NP, and (5) L. divaricata (1000 mg/kg) + 3-NP. Groups 2, 4, and 5 received L. divaricata via intragastric gavage daily for 10 days. Animals in groups 3, 4, and 5 received 20 mg/kg 3-NP daily from days 8-10. At day 10, parameters of locomotor activity and biochemical evaluations were performed. Indeed, rats treated with 3-NP showed decreased locomotor activity compared to controls. Additionally, 3-NP increased levels of reactive oxygen species and lipid peroxidation and decreased ratio of GSH/GSSG and acetylcholinesterase activity in cortex and/or striatum. Our results suggest that rats pretreated with L. divaricata prior to 3-NP treatment showed neuroprotective effects when compared to 3-NP treated controls, which may be due to its antioxidant properties.

This study aimed to determine the effect of lyophilized aqueous extracts of Scutia buxifolia on NTPDase and 5'-nucleotidase activity on platelets and lymphocytes as well as the profile of the platelet aggregation. In vitro tests were used to investigate the effect of the aqueous crude extract obtained from S. buxifolia leaves (SbL) and stem bark (SbS) on enzymatic activities and platelet aggregation. The platelets and lymphocytes were exposed to lyophilized aqueous extracts of S. buxifolia at concentrations of 1-200 μg/mL in the presence of ATP, ADP, AMP as substrates, during the enzymatic assay, as well as the platelet aggregation. The results showed that SbS and SbL potently inhibited NTPDase and 5'-nucleotidase in platelets and lymphocytes. ADP-induced aggregation was inhibited by the SbS (50, 100, and 200 μg/mL) and SbL (200 μg/mL). In addition, these results suggest that S. buxifolia have compounds, such as gallic acid, chlorogenic acid, caffeic acid, quercetin, rutin, and kaempferol, which cause a decrease the NTPDase and 5'-nucleotidase activity, resulting in alterations in adenine nucleotide levels and protection against ADP-induced platelet aggregation.

This study sought to determine the protective effect of dietary inclusion of sorghum leaf sheath dye on cisplatin-induced hepatotoxicity and oxidative stress in rats. Adult male rats were randomly divided into four groups with six animals in each group. Groups I and II were fed a basal diet, while groups III and IV were fed diets containing 0.5% and 1% sorghum leaf sheath dye, respectively, for 20 days before cisplatin administration. Hepatotoxicity was induced by a single dose of cisplatin (7 mg/kg body weight, i.p.), and the experiment was terminated at 3 days after cisplatin injection. The liver and plasma were studied for hepatotoxicity and antioxidant capacity. Cisplatin caused a significant (P<.05) alteration in plasma and liver enzymatic (catalase, glutathione-S-transferase [GST], and superoxide dismutase [SOD]) and nonenzymatic (glutathione [GSH] and vitamin C) antioxidant indices with a concomitant increase in the malondialdehyde (MDA) content; however, there was a significant (P<.05) restoration of the antioxidant status coupled with a significant (P<.05) decrease in the tissue MDA content, after consumption of diets containing sorghum leaf sheath dye. Furthermore, dietary inclusion of sorghum leaf sheath dye caused a marked reduction in the activities of alanine aminotransferase and aspartate aminotransferase after cisplatin administration. However, the ability of the dye to prevent significant cisplatin-induced alteration of both plasma and liver antioxidant indices suggests an antioxidant mechanism of action. Hence, this protective effect of Sorghum bicolor leaf sheath dye against cisplatin-induced hepatotoxicity in rats reflects its potential and beneficial role in the prevention of liver damage associated with cisplatin administration.

The aim of this study was to evaluate the effects of treatment with free and nanoencapsulated essential oil of Achyrocline satureioides on trypanosomosis and its oxidative/antioxidants variables in liver and kidney of rats infected experimentally with Trypanosoma evansi. For that, 48 rats were divided into six groups (A-F), eight animals each group. Groups A, C and D were composed of uninfected animals, while animals in groups B, E and F were inoculated intraperitoneally with T. evansi. Groups A and B were used as controls, negative and positive, respectively. Groups C and E receive oil (orally), as well as the animals in groups D and F were treated with nanoencapsulated essential oil. The treatment was not able to eliminate the parasites, but it remained the levels of parasitemia low. The carbonyl levels in liver and kidney did not differ between groups. Infected animals (group B) showed an increase in the TBARS levels and a decrease in the CAT activity and NPSH levels in liver and kidney, compared with the same parameters in the control (group A). Treatment with A. satureioides (groups C and D) did not influence the TBARS levels and CAT activity in the liver, but it increased the CAT activity in kidneys of the animals of group C. NPSH levels decreased in liver in the groups treated with nanoencapsulated essential oil (groups D and F). An interesting result observed was that the animals infected and then treated with essential oil of A. satureioides (groups E and F) did not differ from animals of group A for TBARS, CAT and NPSH, unlike what happened with the animals of group B. Therefore, the treatment with essential oil did not eliminate the parasites from the bloodstream, but it reduced the number of trypanosomes, mainly by its nanoencapsulated form. The same occurred with the lipid peroxidation in the liver. However, the treatments reduced the oxidative damage, and it led to the activation of the antioxidant enzymes. We believe that the association of this natural product with a trypanocidal drug may enhance its curative effect., (Copyright © 2014 Elsevier GmbH. All rights reserved.)

Ethnopharmacological Relevance: Sandpaper [Ficus exasperata Vahl (Moraceae)] leaf has been reportedly used in folklore for the management/treatment of cardiovascular diseases with little/or no scientific basis for their action. This study sought to investigate the effect of dietary supplementation of sandpaper leaf on angiotensin-I converting enzyme (ACE) activity in hypercholesterolemia as well as the effect of their phenolic extract on this enzyme in vitro., Materials and Methods: The phenolic extract was prepared, then, the inhibitory effect of the leaf extract on ACE was determined in vitro. Thereafter, the effect of dietary supplementation of sandpaper leaf on angiotensin-I converting enzyme (ACE) activity in high cholesterol diet fed rats for 14 days was evaluated as well as some biochemical parameters., Results: The result revealed that under in vitro condition, the phenolic extract inhibited ACE (IC50=14.7µg/mL) in a dose-dependent manner (0-10µg/mL). Feeding high cholesterol diets to rats caused a significant (P<0.05) increase in the ACE activity. However, there was a significant (P<0.05) decrease in the ACE activity as a result of supplementation with the sand paper leaves. Furthermore, there was a significant (P<0.05) increase in the plasma lipid profile with a concomitant increase in malondialdehyde (MDA) content in rat liver and heart tissues. However, supplementing the diet with sandpaper leaf (either 10% or 20%) caused a significant (P<0.05) decrease in the plasma total cholesterol (TC), triglyceride (TG), very low density lipoprotein-cholesterol (VLDL-C), and low-density lipoprotein-cholesterol levels (LDL-C), and in MDA content in the tissues. Conversely, supplementation caused a significant (P<0.05) increase in plasma high-density lipoprotein-cholesterol level when compared with the control diet. Reversed phase HPLC analysis of the extract revealed Quercitrin (43.7mg/g), chlorogenic acid (42.8mg/g) and caffeic acid (33.9mg/g) as the major phenolics in the leaf., Conclusion: The inhibition of ACE activity and prevention of hypercholesterolemia by sandpaper leaf could be part of the possible mechanism underlying its anti-hypertensive property which could lay credence to its use in folk medicine. However, these activities may be directly/indirectly attributed to the polyphenolics present., (Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.)

Background: Syzygium aromaticum (L.) Merr. & Perry (clove) bud is an important spice used in the preparation of several delicacies and in folklore for diabetes management. The present study was convened to assess the effects of dietary clove bud powder (CBP) on biochemical parameters in a type 2 diabetes rat model, induced by a combination of high-fat diet and low-dose streptozotocin (35 mg kg⁻¹) for 30 days., Results: Diabetic rats were placed on dietary regimen containing 20-40 g kg⁻¹ clove bud powder. The results revealed that there was no significant (P > 0.05) difference in the average feed intake and weight changes between the rat groups. Furthermore, supplementation with CBP gradually reduced blood glucose level in diabetic rat compared to control diabetic rats without CBP supplementation (DBC). Moreover, reduced activity of α-glucosidase was observed in CBP and metformin-treated rat groups when compared to that of the DBC rat group. In addition, the DBC group had significantly (P < 0.05) higher lipid concentrations (except for high-density lipoprotein cholesterol) when compared to all other groups. Furthermore, CBP had significantly (P < 0.05) reduced activity of liver enzymes (alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase) and showed elevated levels of antioxidant status (glutathione, ascorbic acid, superoxide dismutase and catalase)., Conclusion: The results suggest that the clove bud diet may attenuate hyperglycemia, hyperlipidemia, hepatotoxicity and oxidative stress in the type 2 diabetic condition., (© 2014 Society of Chemical Industry.)

Gastric ulcers affect many people around the world and their development is a result of the imbalance between aggressive and protective factors in the gastric mucosa. Scutia buxifolia, commonly known as coronilha, has attracted the interest of the scientific community due to its pharmacological properties and its potential therapeutic applications. In this study, the preventive effects of the crude extract of Scutia buxifolia (ceSb) against gastric ulcer induced by 70% ethanol were evaluated in male Wistar rats. In addition, the composition of ceSb was clarified by high-performance liquid chromatography (HPLC). S. buxifolia extract (100, 200 and 400 mg/kg body weight) attenuated oxidative and histopathological features induced by ethanol. Moreover, all evaluated doses of ceSb caused significant (P<0.001 and P<0.0001) and dose-dependent increase in sulfhydryl groups (NPSH) levels, catalase (CAT) and superoxide dismutase (SOD) activities. Furthermore, the administration of ceSb reversed the increase in lipid peroxidation produced by ethanol. The protective effect of the extract could be attributed to antioxidant compounds present in the ceSb, such as flavonoids and phenolic acids, which were quantified by HPLC. Thus, an antioxidant effect of the extract leads to a protection on gastric tissue. These results indicate that S. buxifolia could have a beneficial role against ethanol toxicity by preventing oxidative stress and gastric tissue injury.

Resveratrol and curcumin are natural antioxidants found in the human diet that have been used in the prevention and treatment of different diseases associated with oxidative stress. Aiming to improve the antioxidant effects of resveratrol and curcumin, lipid-core nanocapsules containing the combination of both polyphenols were developed. Physicochemical characteristics were evaluated and compared to the formulations containing each polyphenol individually. Co-encapsulation did not influence nanotechnological characteristics, and all formulations presented mean diameter around 200 nm, low polydispersity index, and encapsulation efficiency close to 100%. Nanoencapsulation increases the photostability of resveratrol and curcumin, and co-encapsulation improves resveratrol photostability. The in vitro antioxidant activity of polyphenols against HO radicals was enhanced by nanoencapsulation, and a better effect was observed after their co-nanoencapsulation. Also, nanocapsules exhibited controlled release profile, for both polyphenols. The results showed that the strategy to co-encapsulate resveratrol and curcumin is a promising approach to improve the performance of medicines used to prevent and treat diseases associated with oxidative stress., (Copyright © 2014 Elsevier B.V. All rights reserved.)

The volatile oil from the stem bark of Scutia buxifolia (Rhamnaceae) has been obtained by hydrodistillation and analyzed by GC-MS. Twenty-one components were identified representing 99.93 % of the total oil composition, spathulenol (35.87%), β-cubebene (17.26%), germacrene D (6.43%), linalool (5.19%), carvacrol (4.05%) were the main components of S. buxifolia essential oil. Antioxidant and antimicrobial properties of the essential oil were evaluated by free radical scavenging (DPPH) assay and micro broth dilution method, respectively. S. buxifolia essential oil presented interesting radical scavenging activity (IC50 = 15.03 ± 0.11 µg/mL). The antibacterial assay showed that S. buxifolia stem bark essential oil was moderately active against the Staphylococcus aureus and Micrococcus sp. (MIC = 500 µg/mL) and Escherichia coli (250 µg/mL). To the best of our knowledge, this is the first study on the composition, antioxidant and antimicrobial activities of essential oil from the S. buxifolia collected from Brazil.

Objective: This study aimed to investigate the effect of the leaf extracts of Syzygium jambos and Solanum guaraniticum on the δ-aminolevulinate dehydratase (δ-ALA-D) activity, their antioxidant activity and potential protective action on oxidatively stressed erythrocytes, in order to demonstrate the safety or toxicity of the plant., Methods: In erythrocyte samples, the effect of both extracts on δ-ALA-D activity, H2O2-induced oxidative stress, and 2,2'azobis (2-amidinopropane) (AAPH)-induced hemolysis was evaluated, as well as some antioxidant mechanisms., Results: Both extracts inhibited δ-ALA-D activity (S. guaraniticum > S. jambos), and an involvement of the zinc ion of the δ-ALA-D structure on the inhibition of enzyme activity was verified. S. jambos leaf extract showed marked efficiency in countering H2O2-induced lipid peroxidation and in maintaining cellular integrity against AAPH-induced hemolysis. Furthermore, S. jambos exhibited greater H2O2 scavenging activity and stronger reduction power than S. guaraniticum., Discussion: Both extracts bear potent antioxidant property as an important beneficial effect. However, the inhibition of δ-ALA-D activity suggests a possible harmful effect of these vegetal preparations and indicates the need for further investigation regarding their toxicological properties. All together, these data represent a significant contribution to the knowledge of these plants, both to the scientific community and to the folk medicine.

Aqueous-methanolic extract of Parkia biglobosa bark (PBB) was screened for its polyphenolic constituents, in vitro antioxidant activity, and effect on mitochondria redox status. The in vitro antioxidant activity was assessed by using the scavenging abilities and the reducing powers of 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) diammonium salt radical cation against Fe(3+). Subsequently, the ability of PBB to inhibit lipid peroxidation induced by FeSO(4) (10 μm) and its metal-chelating potential were investigated. The effects of the extract on basal reactive oxygen species (ROS) generation and on the mitochondrial membrane potential (ΔΨm) in isolated mitochondria were determined by using 2', 7'-dichlorodihydrofluorescin (DCFH) oxidation and safranin fluorescence, respectively. PBB mitigated the Fe(II)-induced lipid peroxidation in rat tissues and showed dose-dependent scavenging of DPPH (IC(50): 98.33 ± 10.0 μg/mL) and ABTS. (trolox equivalent antioxidant concentration, TEAC value = 0.05), with considerable ferric-reducing and moderate metal-chelating abilities. PBB caused slight decreases in both the liver and the brain mitochondria potentials and resulted in a significant decrease (p < 0.001) in DCFH oxidation. Screening for polyphenolics using high-performance liquid chromatography coupled to a diode array detector (HPLC-DAD) revealed the presence of caffeic acid, gallic acid, catechin, epigalocatechin, rutin, and quercetin. These results demonstrate for the first time the considerable in vitro antioxidant activity and favorable effect of PBB on mitochondria redox status and provide justification for the use of the plant in ethnomedicine., (Copyright © 2014. Published by Elsevier B.V.)

The transient receptor potential ankyrin 1 (TRPA1) has been identified as a relevant target for the development of novel analgesics. Gallic acid (GA) is a polyphenolic compound commonly found in green tea and various berries and possesses a wide range of biological activities. The goal of this study was to identify GA as a TRPA1 antagonist and observe its antinociceptive effects in different pain models. First, we evaluated the ability of GA to affect cinnamaldehyde-induced calcium influx. Then, we observed the antinociceptive and antiedematogenic effects of GA (3-100 mg/kg) oral administration after the intraplantar (i.pl.) injection of TRPA1 agonists (allyl isothiocyanate, cinnamaldehyde, or hydrogen peroxide-H2O2) in either an inflammatory pain model (carrageenan i.pl. injection) or a neuropathic pain model (chronic constriction injury) in male Swiss mice (25-35 g). GA reduced the calcium influx mediated by TRPA1 activation. Moreover, the oral administration of GA decreased the spontaneous nociception triggered by allyl isothiocyanate, cinnamaldehyde, and H2O2. Carrageenan-induced allodynia and edema were largely reduced by the pretreatment with GA. Moreover, the administration of GA was also capable of decreasing cold and mechanical allodynia in a neuropathic pain model. Finally, GA was absorbed after oral administration and did not produce any detectable side effects. In conclusion, we found that GA is a TRPA1 antagonist with antinociceptive properties in relevant models of clinical pain without detectable side effects, which makes it a good candidate for the treatment of painful conditions.