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Many of the species used in popular medicine do not have their biological activities already proven by scientific studies. Among these species, the endemic South American Philodendron bipinnatifidum Schott ex Endl deserves special attention since it is already in use in popular medicine for inflammation cases, such as erysipelas, orchitis and ulcers. This study evaluated the antioxidant, antimicrobial and antidiabetic activities of extracts of the hastes de P. bipinnatifidum. The ethanolic extract showed a significant antioxidant potential. The ethyl acetate extract resulted in high antimicrobial activity against Streptococcus pyogenes. The most significant biological activity of ethyl acetate extract relates to its chemical composition when compared with ethanolic extract, which showed the highest concentration of bioactive compounds. In vitro antidiabetic activity was only evaluated for ethyl acetate extract, resulting in inhibition of intestinal disaccharidases (maltase and sucrase) at concentration of 500 μg/mL.

Active principles found in plants may aid in antiparasitic treatments, however it is important to evaluate if they do not have cytotoxicity. The leishmanicidal and trypanocidal activities of Tarenaya spinosa were evaluated, as well as the cytotoxic potential of their extracts, as well as the phytochemical and antioxidant profile. The phytochemical profile was described by Nuclear Magnetic Resonance of Hydrogen (1H-NMR) and High Performance Liquid Chromatography (HPLC-DAD). The antiparasitic activity was performed with the promastigote forms of Leishmania spp. and epimastigotes from Trypanosoma cruzi. Cytotoxicity was assessed using NCTC mammalian clone 929 fibroblasts. The antioxidant potential was assessed with the DPPH free radical. The ethanolic extract (EETS) and aqueous (EATS) presented terpenes, steroids, nitrogen compounds, sugars, phenolic compounds (simple phenylpropanoides and coumarins), flavonoids and chacolnas. The polyphenolic profile showed that caffeic acid was the major compound of both extracts. It was observed that the EETS showed a significant antileishmania activity against L. brasiliensis (LC50 81.75 μg/mL) and L. infantum (LC50 141.6 μg/mL), whereas EATS had low antileishmania activity. Against T. cruzi, the extracts presented LC50 > 1000 μg/mL. The extracts of T. spinosa present high antioxidant activity, with EETS having an IC50 of 377.7 μg/mL and EATS IC50 of 445.8 μg/mL. However, EETS was toxic to fibroblasts with an LC50 of 397.9 μg/mL, whereas no cytotoxicity was observed for EATS. Therefore, EATS is a promising source of antioxidant compounds since it does not present cytotoxicity.

Graphical abstract, Highlights • Capsicum annuum reverses rotenone-induced reduction tyrosine hydroxylase activity. • C. annuum potentiates the ameliorative effect of L-DOPA on rotenone-induced motor dysfunction. • C. annuum attenuates rotenone-induced oxidative stress in the brain., Rotenone is a natural pesticide and environmental neurotoxin which mimics key aspects of Parkinson’s disease. This study evaluated the effect of ethyl acetate extract of Capsicum annuum L. (C. annuum) in rotenone-intoxicated rats. Oral doses of C. annuum extract (50, 100 & 200 mg kg−1) and rotenone (2 mg kg−1 i.p.) were co-administered for 25 days during which rearing behavior was monitored. Biochemical alterations in the levels of tyrosine hydroxylase (TH), monoamine oxidase (MAO), superoxide dismutase (SOD) as well as reduced and oxidized glutathione (GSH) were estimated. Decrease in rearing behavior resulting from rotenone exposure was ameliorated by 200 mg kg−1 of C. annuum. Furthermore, rotenone exposure significantly (P

The increasing use of high-quality cassava flour (HQCF) for the baking of food products makes it imperative to improve its antioxidant and pasting attributes. Therefore, the phenolics composition, antioxidant and pasting properties of HQCF substituted with 10% and 20% Brachystegia eurycoma seed flour (BSF) were evaluated in this study. The HPLC-DAD profile of the phenolics revealed that chlorogenic acid, caffeic acid, rutin and quercetin levels in the blends increased significantly (p

Spices and herbs have antioxidant, anti-inflammatory, and anti-microbial properties, amongst others. These characteristics are attributable to their composition, such as high polyphenol and flavonoid contents that are responsible for their antioxidative properties. Methanolic extracts of Ocimum basilicum (OB), Xylopia aethiopica (XA), and Piper guineensis (PG) were evaluated to profile their phenolic compounds and in vitro antioxidant properties. High performance liquid chromatography with diode-array detection phenolic compounds profiling revealed that quercetin, quercitrin, and isoquercitrin are the most prevalent phenolic compound in OB, XA, and PG, respectively. All the extracts possessed good antioxidant activity. XA showed the highest total phenolic content of 29.50 mg gallic acid equivalents/g, a total flavonoid content of 21.17 mg quercetin equivalents/g, 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical scavenging abilities of 29% and 88.23%, respectively, and a nitric oxide scavenging activity of 44.13 mg/g. Thus, the XA methanolic extract demonstrated a high content of phenolic compounds and significant antioxidative properties, with prospective potency to prevent oxidative damage and promote better cardiovascular health.

Whole grain cereals are important dietary sources for management of metabolic diseases due to the bioactive components they contain. Hence, this study investigated enzymes (pancreatic lipase, α-amylase, α-glucosidase, xanthine oxidase and angiotensin 1-converting enzyme) inhibitory property, antioxidant activity and phenolics profile of raw and roasted red sorghum (Sorghum bicolor) grains in vitro. Extracts of flours of raw and roasted (150 °C and 180 °C, for 20 min) grains were assayed for enzymes inhibitory and antioxidant activities using spectrophotometric methods; while their phenolic constituents were characterized using HPLC-DAD. The raw grains exhibited strong enzymes inhibitory and antioxidant activities, and contained phenolic acids (gallic, chlorogenic, caffeic, ellagic and p-coumaric acids) and flavonoids (quercetin, luteolin and apigenin). However, whereas the enzymes inhibitory activity and levels of the phenolic compounds in the grains decreased significantly (p

Research has shown that different processing techniques affect the bioactive components in grain foods and their bioactivities. Hence, this study evaluated effect of roasting temperature (150 and 180 °C; 20 min) on phenolics composition, enzymes (pancreatic lipase, angiotensin 1-converting enzyme, α-amylase, α-glucosidase and xanthine oxidase) inhibitory and antioxidant properties of whole cowpea (Vigna unguiculata) pulses. Phenolic compounds were characterized using HPLC–DAD; enzymes inhibitory and antioxidant activities were assayed by spectrophotometric methods. Extract of raw cowpea contained flavonoids (catechin, quercitrin, quercetin, kaempferol and apigenin) and phenolic acids (gallic and caffeic acids). The extract strongly inhibited all the enzymes tested and displayed potent antioxidant activity. However, the levels of individual phenolics and enzymes inhibitory activity decreased significantly (p

Artocarpus heterophyllus Lam (Moraceae) stem bark has been used locally in managing diabetes mellitus with sparse scientific information. This study investigates the in vitro antioxidant potential of polyphenolic-rich extract of A heterophyllus stem bark as well as its antidiabetic activity in streptozotocin-induced diabetic rats. Fifty male Wistar rats were used with the induction of diabetes by a single intraperitoneal injection of streptozotocin (45 mg/kg body weight) and were orally administered 400 mg/kg free and bound phenols of A heterophyllus stem bark. The animals were sacrificed on the 28th day of the experiment using the cervical dislocation method; antihyperglycemia and anti-inflammatory parameters were subsequently assessed. The polyphenolic extracts demonstrated antioxidant potentials (such as hydrogen peroxide and diphenyl-1-picrylhydrazyl), as well as strong inhibitory activity against amylase and glucosidase. There was a significant ( P < .05) increase in glycogen, insulin concentration, pancreatic β-cell scores (HOMA-β), antioxidant enzymes and hexokinase activities, as well as glucose transporter concentration in diabetic animals administered the extracts and metformin. Also, a significant ( P < .05) reduction in fasting blood glucose, lipid peroxidation, glucose-6-phosphatase, and all anti-inflammatory parameters were observed in diabetic rats administered the extracts and metformin. The extracts demonstrated antidiabetic potential, which may be useful in the management of diabetes mellitus

There are some genes associated to the risk of chronic diseases that present potential nutrigenetic response, such as the human manganese-dependent superoxide dismutase gene (Val16Ala-SOD2, rs4880) for which homozygous genotypes (VV and AA) are associated with higher basal superoxide (S) and hydrogen peroxide (HP) levels, respectively. It is possible that the VV- and AA-imbalance could be attenuated by selenium(Se)-rich foods such as Brazil nut (BN). To test this hypothesis, we conducted an in vitro protocol triggering a chemical S-HP imbalance by exposure of dermal fibroblast cells (HFF-1) to paraquat, which generates high S levels (VV-like treatment) and porphyrin (MnTBAP), which generates high HP levels (AA-like treatment). Modulation of cell growth and pro-oxidative and antioxidant markers were evaluated. BN aqueous extract (BNAE) most effective concentration which increased cell growth and decreased oxidative metabolism indicators of imbalanced cells was 75 ng Se/mL. However, this effect was not directly affected by the S-HP imbalance: in AA-SOD2-like cells, thioredoxin reductase (TrxR-1) gene was upregulated and in VV-SOD2-like cells an upregulation of glutathione peroxidase (GPx-1) gene expression was observed, however, this regulation occured in a homeostatic manner. These results suggest that BNAE was able to minimize negative effects in both directions of the S-HP imbalance, by modulation of different oxidative-metabolic pathways.

Several species of the genus Ceiba (Malvaceae) are ethnopharmacologically used. Thus, this study aimed to investigate the in vitro beneficial properties of the aqueous stem bark extract of Ceiba speciosa. The extract presented a great amount of phenolic compounds (117.4 ± 6.2 mg GAE/g). The antioxidant activity was assessed by DPPH (IC50 = 42.87 μg/mL), ORAC (2351.17 μmol TE/g) and FRAP (235.94 μM FeSO4/g) methods. In addition, the extract reduced MCF-7 cell viability as assessed by MTT. However, it prevented mitochondrial membrane depolarization and reduced caspase-9 activity induced by hydrogen peroxide. In conclusion, these findings indicate the extract is an excellent source of natural antioxidants and is able to protect ROS-induced cell death. Therefore, C. speciosa extract may possess beneficial properties for application in pharmaceutical industry as an antioxidant. However, further studies to better elucidate its mechanisms and to isolate its active compounds are required.

RESUMO O mel é um produto natural que apresenta várias propriedades benéficas para a saúde, tais como atividade antinflamatória, antioxidante e antimicrobiana, as quais dependem de sua composição. Neste contexto, as propriedades físico-químicas (cor, pH, conteúdo de cinzas, umidade, açúcares e compostos fenólicos totais) e a atividade antioxidadente (capacidade de remoção do radical DPPH) de méis de abelhas Apis mellifera de Santarém, na principal região de produção de mel na Amazônia Oriental, Brasil, foram avaliadas. A maioria das amostras teve cor escura e apresentaram-se ácidas. Os teores de cinzas e a umidade variaram de 0,112 a 0,318 e de 14,751 a 17,514, respectivamente. O teor de açúcares redutores vairou entre 62,873 e 91,563%. O teor total de compostos fenólicos foi mais elevado que os já reportados na literatura, variando entre 15,22 e 16,51 mg g−1 e 17,70 e 18,94 mg g−1 para amostras de mel protegidas e expostas à radiação UV, respectivamente. A quercetina foi encontrada apenas no mel que foi protegido da luz, com teores variando entre 0,24 e 0,43 mg g−1. A ausência de quercetina nas amostras de mel expostas à luz sugere que a radiação UV pode ter degradado esse composto. Todas as amostras apresentaram máxima capacidade de remover o radical DPPH próxima a 50%. Houve correlação inversa entre a cor e o pH, cinzas, açúcares redutores e teor de umidade, e correlação positiva entre a cor e o teor de composto fenólicos e a atividade antioxidante.

The lipid lowering, antihypertensive, hepatoprotective and antioxidant activities of Ethiopian pepper (Xylopia aethiopica) supplemented diet in hypercholesterolemic rats were investigated in this study. Animals were divided into five groups (n = 7); normal control rats (NC); untreated hypercholeterolemic rats (Hyper-C diet); hypercholesterolemic rats treated with oral dose of 1 mg/kg of simvastatin (Hyper-C diet + STATIN); hypercholesterolemic rats treated with 2% (Hyper-C diet + 2%ETP) or 4% (Hyper-C diet + 4%ETP) supplementation of ETP. ETP-supplemented diets (2% and 4%ETP) reduced total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL) and concomitantly increased high-density lipoprotein (HDL). There was no significant difference between the TG and LDL levels of groups fed with Hyper-C diet + 4%ETP and Hyper-C diet + STATIN. Furthermore, Hyper-C diet + 4%ETP significantly reduced plasma angiotensin-I converting enzyme (ACE) levels compared to Hyper-C diet + 2%ETP and Hyper-C diet + STATIN. Furthermore, elevated serum levels of ALT, AST and ALP induced by the high cholesterol diet were reversed by ETP and STATIN supplemented diet. Rutin, quercetin and ellagic acid were the dominant phenolic compounds in ETP as revealed by high performance liquid chromatography analysis. The observed hypolipidemic, antihypertensive and hepatoprotective effects exhibited by ETP suggest its potentials to prevent lipid abnormalities and associated risk factors, and this could be attributed to its phenolic constituents.

Tithonia diversifolia (Hemsl.) A. Gray leaves have long been used to manage neurodegenerative diseases without scientific basis. This study characterized the phenolic constituents, evaluated the antioxidant properties of phenolic extracts from T. diversifolia leaves used as traditional medicine in Africa and its inhibition of key enzymes linked to Alzheimer’s disease. The extract was rich in phenolic acids (gallic acid, chlorogenic acid, caffeic acid and p-coumaric acid) and flavonoids (apigenin) and had 1,1-diphenyl-2-picryl-hydrazil radical scavenging abilities (IC50 = 41.05 μg. mL−1), 2,2-Azino-bis3-ethylbenthiazoline-6sulphonic acid radical scavenging ability (IC50 = 33.51 μg. mL−1), iron chelation (IC50 = 38.50 μg. mL−1), reducing power (Fe3+- Fe2+) (7.34 AAEmg/100 g), inhibited acetylcholinesterase (IC50 = 39.27 μg mL−1) and butyrylcholinesterase (IC50 = 35.01 μg mL−1) activities. These results reveal the leaf as a rich source of phenolic compounds with antioxidant and cholinesterase inhibitory activity. Keywords: Tithonia diversifolia leaves, Antioxidant activity, Cholinergic enzymes, Alzheimer’s disease

This study aimed to characterize different extracts/fractions obtained from Cymbopogon citratus according to their chemical composition and antioxidant properties. Plant leaves were submitted to extractions with different solvents, and the antioxidant capability of each fraction was analyzed using different methods (E1–E4). The ethyl acetate fraction from extraction procedure 1 (E1) presented a high polyphenolic content and antioxidant capability. Therefore, in E2, the pH of the aqueous phases was modified to fractionate the compounds in the ethyl acetate extractions. Interestingly, the fraction obtained at pH 4 presented a higher antioxidant activity than AcOEt F1. Furthermore, it was verified that the essential oil removal improved the extraction of polyphenols in ethyl acetate fractions. The antioxidant activity of these fractions was comparable to ascorbic acid, and could also inhibit TBARS production in phospholipids comparatively to vitamin E. Such fraction will be further explored to isolate the active chemicals, and to evaluate its toxicity and antioxidant actions in vivo.

Highlights • A focused on the erectogenic potentials of two tropical pumpkin seeds was established. • The antioxidant properties of these seed varieties were also discussed. • The inhibitory effects of the seeds on key enzymes relevant to ED were critically explored. • The potentials of the seeds to manage ED were recommended.

The infusions of Baccharis trimera (Asteraceae) are traditionally used in Brazil as a tea to treat liver disorders. It is one of the major constituents in herbal formulations used for the treatment of liver disorders and other diseases. The present study was therefore, aimed to evaluate the potential in vitro and in vivo antioxidant activities and phenolic profile of Baccharis trimera . High performance liquid chromatography coupled with DAD analysis indicated that the gallic acid, rutin and quercetin were the main phenolic compounds present in aqueous extract. The aqueous extract showed inhibition against thiobarbituric acid reactive species (TBARS), induced by different prooxidants (10 μM FeSO 4 and 5 μM sodium nitroprusside) in rat liver, brain and phospholipid homogenates from egg yolk. Moreover, the free radical scavenging activities of the extract was determined by the quenching of DPPH (IC 50, 415.2 ± 15.2 μg/ml) and hydroxyl radicals in deoxyribose assays. The administration of extract at 100 mg/kg and 250 mg/kg dose significantly reduced the lipid peroxidation, increased the catalase activity and enhanced the levels of ascorbic acid and reduced glutathione in the liver of mice. Thus, oxidative stress in brain and liver could be managed/prevented by dietary intake of Baccharis trimera.

Mercury (Hg) is widely distributed in the environment and is known to produce several adverse effects in organisms. The aim of the present study was to examine the in vitro antioxidant activity and Hg chelating ability of the hydroalcoholic extract of Psidium guajava leaves (HEPG). In addition, the potential protective effects of HEPG against Hg(II) were evaluated using a yeast model (Saccharomyces cerevisiae). HEPG was found to exert significant antioxidant activity in 2,2-diphenyl-1-picrylhydrazyl scavenger and inhibition of lipid peroxidation induced by Fe(II) assays in a concentration-dependent manner. The extract also exhibited significant Hg(II) chelating activity. In yeast, Hg(II) induced a significant decrease in cell viability. In contrast, HEPG partially prevented the fall in cell viability induced by Hg(II). In conclusion, HEPG exhibited protective effects against Hg(II)-mediated toxicity, which may be related to both antioxidant and Hg(II)-chelating activities.

Diet is a key component for development and longevity of organisms. Here, the fruit fly was used to evaluate the detrimental effects caused by consumption of high-sucrose diets (HSD), namely phenotypic responses linked to insulin signaling and oxidative stress. The protective effects of extracts from medicinal plants Syzygium cumini and Bauhinia forficata were investigated. HSD intake (15% and 30%) delayed the time to pupation and reduced the number of white pupae. In adult flies, the intake of diets was associated with mortality and increased levels of glucose+trehalose, triacylglycerols and hydrogen peroxide. Indeed, 30% HSD induced body-weight loss, mitochondrial dysfunction and changes in acetylcholinesterase, δ-aminolevulinate dehydratase and antioxidant enzymes activity. Catalase, superoxide dismutase, keap1, HSP70, dILP-5 and Insulin receptor mRNA levels were over-expressed in flies emerged from 30% HSD. The extract treatments blunted the developmental alterations elicited by diets. Syzygium cumini extract was more efficient than B. forficata in reducing hyperglycaemia, redox disturbances and the changes in mRNA expression of insulin receptor.

Tea from the bark and leaves of Guazuma ulmifolia Lam. (Malvaceae) are used in several countries in South and Central America in cases of gastrointestinal and skin problems, among other diseases. The aim of this study was to characterize the chemical composition and its antioxidant, anticholinesterase and antifungal activity to correlate these with the popular use of this plant. The antioxidant activity was evaluated by DPPH method and the anticholinesterase action by inhibiting the acetylcholinesterase enzyme, with an adaptation to thin layer chromatography. In the antifungal assay, the minimum inhibitory concentration (MIC) was determined by the microdilution broth method at concentrations ranging from 1024 to 1 μg/mL, moreover a modulated test on the antibiotic fluconazole was performed at concentrations from 1024 to 8 μg/mL. Assays were performed in triplicates and plate readings were performed in an ELISA spectrophotometer. The ethanol extract showed antioxidant activity (EC 50 : 119.85 ± 2.42 μg/mL), significant anticholinesterase activity (growth inhibition zone of 1.0 cm, near the physostigmine standard), and low antifungal activity was observed against standard strains of Candida. Nevertheless, the extract showed a significant fluconazole modulatory effect, with potentiation of the antifungal action against Candida tropicalis . The chemical study of the ethanol extract from Guazuma ulmifolia leaves revealed the presence of flavonoids and phenolic acids with recognized antioxidant potential. The antioxidant activity combined with anticholinesterase potential corroborates, in part, with the use of G. ulmifolia in the treatment of gastrointestinal disorders.

Context: Plantain fruit pulp has been used as a natural remedy to manage erectile dysfunction (ED) in traditional medicine. However, the potency of the peel has not been examined with respect to ED management. Objective: This study investigated and compared the inhibitory potential of unripe (UPP) and ripe (RPP) plantain peels on some enzymes associated with ED and Fe2+-induced oxidative stress in albino rat penile homogenate in vitro. Materials and method: Aqueous extract of the peels was prepared and the effect on phosphodiesterase-5 (PDE-5), arginase, acetylcholinesterase (AChE), angiotensin-I converting enzyme (ACE) and Fe2+-induced malonyladehyde in isolated albino rat penile homogenate were investigated. Phenolic constituents of the peels powder were characterized using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). Result: Extract from UPP had higher PDE-5 (IC50 = 3.10 μg/mL), arginase (IC50 = 0.96 μg/mL), AChE (IC50 = 6.30 μg/mL) and ACE (IC50 = 0.41 μg/mL) inhibitory ability compared with RPP (PDE-5, IC50 = 4.33 μg/mL; arginase, IC50 = 1.34 μg/mL; AChE, IC50 = 8.64 μg/mL; ACE, IC50 = 0.63 μg/mL). The extract from UPP also had higher inhibition of Fe2+-induced lipid peroxidation. HPLC-DAD analysis revealed that gallic and caffeic acids, rutin, quercitrin and quercetin were abundant in UPP, while catechin, kaempferol, chlorogenic and ellagic acids were the dominant phenolic compounds in RPP. Discussion and conclusion: Inhibition of enzymes associated with ED and lipid peroxidation could be linked with the phenolic compounds. However, UPP appeared to be more potent.

This study sought to characterize the soluble free and bound phenolic compounds from shaddock (Citrus maxima) peels and investigate their effect on 3-hydroxy-methyl-3-glutaryl coenzyme A reductase (HMG-CoA reductase) and glutathione-linked enzymes in colon (Caco-2) cells. The radicals scavenging ability and the protective ability of the phenolic extracts against pro-oxidant induced oxidative damage in Caco-2 cells and rat colon homogenates were also investigated. The free phenolics were extracted with 80% acetone (v/v), while bound phenolics were extracted from the alkaline (NaOH) and acid (HCl) hydrolyzed residue with ethyl acetate. HPLC fingerprinting revealed the presence of gallic acid, catechin, chlorogenic acid, caffeic acid, ellagic acid, epicatechin, rutin, quercitrin and quercetin in the extracts. The results revealed that the extracts inhibited HMG-CoA reductase activity and increased the activities of glutathione reductase and glutathione peroxidase in Caco-2 cells. The extracts inhibited peroxyl radical induced oxidation of membrane lipids in Caco-2 cells and malondialdehyde production in rat colon homogenates. Furthermore, the phenolic extracts scavenged radicals [2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl (OH)] and chelated Fe2+ in a concentration-dependent manner. This study showed that shaddock peels could serve as a dietary means or nutraceutical source for protecting the colon from degeneration.

Context: Syzygium cumini (L.) Skeels (Myrtaceae) is a medicinal plant widely used in folk medicine for the treatment of diabetes mellitus (DM). However, studies on the use of this plant and of nanoparticle formulations against DM-related fungal infections are scarce. Objective: To evaluate the effect of the treatments with aqueous seed extract of S. cumini (ASc) and ASc-loaded polymeric nanoparticles (NPASc) on biochemical parameters in Candida albicans-infected diabetic rats. Materials and methods: Male Wistar rats were divided into eight groups: Control, DM, C. albicans, C. albicans + ASc, C. albicans + NPASc, DM + C. albicans, DM + C. albicans + ASc and DM + C. albicans + NPASc. Rats were daily treated with ASc or NPASc (100 mg/kg) for 21 days. Biochemical parameters in serum and urine, advanced oxidation protein product (AOPP) and TBARS levels in the serum, kidney, liver and pancreas and N-acetyl-β-d-glucosaminidase (NAG) activities in kidney and urine were evaluated. Results: Biochemical and oxidative stress parameters increased in rats with DM and/or candidiasis. NPASc was more effective than ASc in decreasing glucose (56%), cholesterol (33%) and creatinine (51%) levels; serum (16%) and pancreatic (46%) AOPP and renal (48%) TBARS levels when compared with DM + C. albicans group. In C. albicans group, both treatments decreased NAG activity but did not decrease creatinine levels. Conclusions: These data suggest that the use of nanotechnology is able to improve plant extract properties such as antioxidant activity that may be useful in diabetes-related complications.

Background and objectives: Natural products such as essential oils with antioxidant potential can reduce the level of oxidative stress and prevent the oxidation of biomolecules. In the present study, we investigated the antioxidant potential of Lantana montevidensis leaf essential oil (EOLM) in chemical and biological models using Drosophila melanogaster. Materials and methods: in addition, the chemical components of the oil were identified and quantified by gas chromatography coupled to mass spectrometry (GC-MS), and the percentage compositions were obtained from electronic integration measurements using flame ionization detection (FID). Results: our results demonstrated that EOLM is rich in terpenes with Germacrene-D (31.27%) and &beta, caryophyllene (28.15%) as the major components. EOLM (0.12&ndash, 0.48 g/mL) was ineffective in scavenging DPPH radical, and chelating Fe(II), but showed reducing activity at 0.24 g/mL and 0.48 g/mL. In in vivo studies, exposure of D. melanogaster to EOLM (0.12&ndash, 0.48 g/mL) for 5 h resulted in 10% mortality, no change in oxidative stress parameters such as total thiol, non-protein thiol, and malondialdehyde contents, in comparison to control (p &gt, 0.05). Conclusions: taken together, our results indicate EOLM may not be toxic at the concentrations tested, and thus may not be suitable for the development of new botanical insecticides, such as fumigants or spray-type control agents against Drosophila melanogaster.

Methylmalonic acidemia is a genetic disease characterized by accumulation of organic acids, such as methylmalonic (MMA) and malonic (MA) acids. Considering that the accumulation of MMA and MA causes several damages due to oxidative stress, antioxidants are thought to play a pivotal role in preventing deleterious effects associated with exposure to such compounds. Ilex paraguariensis (IP) was used here to test the hypothesis that supplementation with the aqueous extract of this plant could exert protective effect against MMA or MA induced mortality, behavioral and/or biochemical changes in Drosophila melanogaster (DM). Initially, a curve time- and dose–response to MMA (1–10 mM), MA (1–10 mM) and IP (63–500 μM) was performed. Thereafter, flies were concomitantly exposed to MA (5 mM), MMA (5 mM) and/or IP (250 μg/mL) during 15 days for survival assay, and for 48 hs to MA (1 or 5 mM), MMA (1 or 5 mM) and/or IP (250 μg/mL) for subsequent investigations. Both MMA and MA exposure resulted in higher incidence of mortality, a worse performance in the negative geotaxis assay and increased locomotion in open-field test as compared with control group. Furthermore, a marked increase in non-protein thiol (NPSH) and in thiobarbituric acid reactive substances (TBARS) levels, decrease in superoxide dismutase (SOD), catalase and acetylcholinesterase (AChE) activities, and decrease in MTT and resazurin reduction were noted in MMA or MA treated groups. IP treatment offered significant protection against all alterations associated to MMA or MA exposure. This study confirm the hypothesis that supplementation with IP offers protection against changes associated to MMA or MA exposure in DM, due, at least in part, to its antioxidant effect.

A complex mixture of organic contaminants and metals is associated with neuron-fertility disorders and studies have demonstrated that phenolic antioxidants from herbal origin, possesses a strong protective potential. This study aimed to investigate the protection of phenolic croton zambesicus (C-ZAMB) leaves against neuro-ovarian damage in rats exposed to chronic mixture of anthropogenic toxicants (EOMABRSL). The animals were divided into five groups (n = 10): Group I was given 0.5 ml of distilled water only; Group II received 0.5 ml of EOMABRSL for 98 days; Group III received 0.5 ml of EOMABRSL for 70 days and withdrew for 28 days; Group IV received 0.5 ml of EOMABRSL for 70 days +400 mg/kg phenolic C-ZAMB for 28 days; Group V received 400 mg/kg C-ZAMB only for 28 days via oral route. Both non-withdrawal and withdrawal EOMABRSL-exposed animals exhibited neuro-ovarian impairment by up-regulating neuronal 51 eco-nucleotidase (51ENT), acetylcholinesterase (AChE), butrylcholinesterase (BuChE), synaptosomal monoamine oxidase-A (MAO-A) with altered cerebral antioxidants. Similarly, exposure to EOMABRSL for 98 and 70 days caused ovarian injury by amplifying the activity of 51ENT with corresponding decline of fertility index, lactate dehydrogenase (LDH) and Δ5 17β-hydroxyl steroid dehydrogenase (Δ517β-HSD). EOMABRSL intoxication also increased the neuro-ovarian MDA content with reduced numbers of neonates. Phenolic antioxidants from C-ZAMB leaves identified by High Pressure Liquid Chromatography (HPLC) ameliorated the chronic EOMABRSL intoxication. The treatment also prevented ovarian lesions by depleting MDA content and improved antioxidant status. Thus, confirming its neuro-ovarian protection.

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 CO2 and compressed propane extraction. The extraction with compressed propane yielded 2.72 wt%, whereas with supercritical CO2 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 CO2 and pressurized propane, respectively. The antioxidant activity was more pronounced for the supercritical CO2 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 CO2.

The aim of this study was to evaluate the effect of β-caryophyllene on hypercholesterolemia using a model of hyperlipidemia induced by Triton WR-1339 in rats, as well as its possible effect on hepatic antioxidant enzymes. Thus, total cholesterol, triglycerides, low-density lipoprotein (LDL) cholesterol, and high-density lipoprotein (HDL) cholesterol were measured in serum, while reactive oxygen species (ROS), thiobarbituric acid reactive substances (TBARS), hepatic 3-hydroxy-3-methylglutayl coenzyme A (HMG-CoA) reductase, superoxide dismutase (SOD), and catalase (CAT) activities were measured in the hepatic tissue. In addition, seric concentrations of β-caryophyllene were measured to perform correlation studies. Serum samples from hypercholesterolemic rats show higher (p

Context: Ficus capensis Thunb (Moraceae) is a medicinal plant widely grown in tropical and subtropical regions with the leaf decoction commonly taken in traditional folklore as fertility agent in men for ages. Aim: This study investigated the effects of aqueous extract from Ficus capensis leaves on angiotensin-I-converting enzyme (ACE), acetylcholinesterase (AChE) and arginase activities in vitro. The antioxidant properties of the extract as typified by the abilities to scavenge radicals [nitric oxide (NO), hydroxyl (OH)], chelate Fe2+ and inhibit Fe2+ -induced lipid peroxidation were also assessed. Methods: The aqueous extract (1:10 w/v) of Ficus capensis leaves was prepared and the ability of the extract to inhibit arginase, angiotensin I –converting enzyme (ACE), acetylcholinesterase (AChE) and antioxidant properties of the extract in rat’s penile tissue in vitro was investigated using various spectrophotometric methods. Phenolic constituent was carried-out using high performance liquid chromatography coupled with diode array detection (HPLC - DAD). Results: The extract inhibited ACE (IC50 = 52.17), AChE (IC50 = 172.60 μg/mL) and arginase (IC50 = 112.50 μg/mL) activities in a dose-dependent pattern. Gallic acid, quercetin, caffeic acid, ellagic acid, rutin and chlorogenic acid were the most abundant phenolic compounds identified in the sample. Furthermore, extract scavenged NO (IC50 = 0.12 μg/mL) and OH (IC50 = 0.53 μg/mL) radicals, chelated Fe2+ (IC50 = 0.16 μg/mL) and inhibited Fe2+ lipid peroxidation (IC50 = 435.17 μg/mL) dose-dependently. Conclusion: Inhibition of ACE, AChE, arginase, Fe2+ -induced lipid peroxidation as well as radical scavenging and Fe2+ -chelating abilities could be some of the possible mechanisms by which F. capensis leaves could be used in the treatment/management of erectile dysfunction (ED). Keywords: Ficus capensis, Erectile dysfunction, ACE, Arginase, AChE, Polyphenols

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 (400–800 mg/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.

This study sought to assess the effects of bitter gourd leaf extracts (methanol and aqueous) on enzyme linked with hypertension (angiotensin-I-converting enzyme and some pro-oxidants (iron sulfate, sodium nitroprusside, and cisplatin]–induced lipid peroxidation in rat kidney homogenates. Chromatographic analysis of the extract was done using high-performance liquid chromatography–diode array detection. The results revealed that methanol extract (IC50 = 109.63 µg/mL) had significantly ( P < .05) higher angiotensin-I converting enzyme inhibitory activity than aqueous extract (IC50 = 182.95 µg/mL). Similarly, methanol extract had significantly ( P < .05) higher inhibitory effect on Fe2+- and cisplatin-induced lipid peroxidation than aqueous extract. However, there was no significant ( P > .05) difference in the inhibition of sodium nitroprusside–induced lipid peroxidation of both extracts. High-performance liquid chromatography–diode array detection analysis revealed the presence of quercetin, caffeic, gallic, and chlorogenic acids in the leaf. Thus, inhibition of angiotensin-I converting enzyme activity and the antioxidant properties of the extracts could be linked to the presence of phenolic phytochemicals.

Syzygium cumini seeds were used for the preparation of an aqueous extract (ASc) and of polymeric nanoparticles containing ASc (NPASc) with the aim to evaluate and compare their in vitro efficacy against the complications of Diabetes mellitus (DM) and the in vivo toxicity. NPASc were produced by the emulsification/evaporation solvent technique, employing poly-e-caprolactone, a biocompatible polymer. The antioxidant activity of both ASc and NPASc was evaluated by the scavenging of DPPH radicals and by the ferric reducing antioxidant power assay (FRAP). The in vitro efficacy of both formulations against oxidized LDL particles (ox-LDL) and fungal species was also assessed. NPASc presented properties compatible with nanometric systems, and chromatogram analysis demonstrated that the composition of S. cumini was not affected. The antioxidant properties of the extract were also maintained in the new formulation. Indeed, both formulations showed high protection against ox-LDL. The antifungal activity of NPASc against Candida guilliermondii and Candida haemulonii was superior to that observed for the ASc. No acute toxicity was observed in the Artemia salina lethality assay and in rats. These findings highlight the possibility of expanding the use of S. cumini to ameliorate the chronic complications of DM. The lack of toxicity of the nanoparticles indicates that NPASc might be a safe candidate for drug delivery systems.

Purpose– The purpose of this paper is to focus on the antioxidant properties of two phenolic-rich varieties of Nigerian local rice and their anti-cholinesterase potential afterin vitro-simulated gastrointestinal digestion, with the aim of establishing their actual antioxidant and nutraceutical potential after their passage through the gastrointestinal tract upon consumption.Design/methodology/approach– Two local rice varieties, commonly referred to as “Gboko” and “Ofada” rice commonly grown in Benue State, a middle belt region of Nigeria and south western regions of Nigeria, respectively, were locally processed. Each of the processed grains were divided into two portions; one portion was left uncooked, while the second portion was boiled conventionally as eaten, dried and subsequently milled into powder. The milled samples of the raw and boiled rice were treated with acidified methanol to obtain the methanol extracts; another portion of each samples was subjected toin vitroenzyme digestion using standard methods to mimic human digestion; and the third portion was treated using the same scheme ofin vitrodigestion without the sets of enzyme which was used to serve as a control for enzyme treatment. The quali-quantitative phenolic profiles of the two local varieties were carried out with the aid of high-performance liquid chromatography with diode-array detection (HPLC-DAD) method. The antioxidant potential and anti-cholinesterase action of the methanolic extracts, the simulatedin vitrodigested model and the enzyme-treated controls of the rice samples were determined using standard methods and data obtained were subjected to ANOVA; the differences of means were separated using Duncan’s multiple range test (DMRT).Findings– The quali-quantitative assessment of phenolic compounds in the two studied local varieties revealed the presence of some phenolic acids and flavonoids, with a decreased level of most of the identified phenolic compounds after boiling.In vitroenzyme-digested rice for both raw and boiled rice samples showed significantly higher total phenolic content, total flavonoid content, ferric-reducing antioxidant power, 2, 2′-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS+) scavenging and NO− inhibitory activities than the aqueous-methanolic extracts and the enzyme-treated controls. The aqueous-methanolic extracts displayed a higher 1, 1 diphenyl-2-picrylhdrazyl radical scavenging activity and inhibited Fe2+-induced lipid oxidation in rat’s brain and liver homogenate than that displayed by thein vitroenzyme-digested samples.In vitroenzyme-digested and boiled “Gboko” and “Ofada” rice and raw “Ofada” rice have the potential of inhibiting acetylcholine esterase (AChE) activity. While methanolic extracts of raw and boiled “Ofada” and “Gboko” rice exhibited the potential to inhibit butrylcholinesterase activity. The result of this paper indicates that the selected rice varieties possess antioxidant capacities which are better released after the simulatedin vitroenzyme digestion; the result also showed the anti-cholinesterase potential of the studied rice grains and, therefore, they can be considered as nutraceutical health supplements.Originality/value– The paper has demonstrated the antioxidant potentials of the phenolic-containing two Nigerian local rice varieties and established their anti-cholinesterase potential after simulatedin vitroenzyme digestion.

The main objective of this work to evaluate the antioxidant activity of Ilex paraguariensis (popularly known as yerba mate) and to perform a biochemical analysis in rats using fruit extracts. Usually, yerba mate is consumed as tea leaves in typical drinks in south Brazil, Argentina and Uruguay. Its fruit has a strong purple color, indicative of the presence of phenolic compounds such as anthocyanins, which have great antioxidant potential. The extract obtained with acidified ethanol afforded the larger amount of anthocyanins (43.79 mg/g), total phenolic (62.25 mg GAE/100 g sample) and provided the best antioxidant activity to catch the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical (IC50 = 3.61 ± 0.045 mg/ml). The extract was effective in reducing 36% and 42% of total cholesterol and triglycerides serum levels, respectively, as well as on maltase activity, though reduction in blood glucose levels or an increase in glycogen content was not observed.

Diminazene aceturate (DA) is the active component of some trypanocidal drugs used for the treatment of animals infected with trypanosomosis and babesiosis. Residues of DA may cause hepatotoxic and nephrotoxic effects. Therefore, the purpose of this study was to investigate the occurrence of oxidative stress, i.e., changes in the antioxidant defense system of rats treated with a single dose of 3.5 mg kg(-1) of DA. All treatments were intramuscularly administered, and evaluations were performed on days 7 and 21 post-treatment (PT). Liver and kidney samples were collected and evaluated by histopathology and oxidative stress parameters (thiobarbituric acid-reactive species, catalase, superoxide dismutase, carbonyl, non-protein thiols, and reduced glutathione). Finally, blood was collected to determine seric DA concentration. Superoxide dismutase (SOD) and catalase (CAT) activities in liver and kidney of rats were dramatically inhibited (p 0.05) compared to the control group on day 21 PT. This difference is related to the concomitant increase (p 0.05) in malondialdehyde (MDA) content, which was identified by an increase in thiobarbituric acid-reactive species (TBARS) levels. The carbonyl levels did not differ between groups (p 0.05). Both non-protein thiols (NPSH) and glutathione (GSH) levels in liver and kidney decreased (p 0.05) on day 21 PT. Chromatographic analyses showed lower levels of DA on day 21 PT compared to day 7 PT. A negative correlation was observed between DA concentration in serum and lipid peroxidation in liver and kidney tissues on 21 days PT. Histopathology revealed vacuolar degeneration in liver and kidney samples on day 21 PT. Our findings indicate that DA could cause oxidative damage to liver and kidney of rats.