ABSTRACT
This study aimed to evaluate the chemical composition and antioxidant activity of phenolic extracts from monofloral and polyfloral honey samples obtained from different Brazilian regions. The chemical composition (total content of phenolic compounds and flavonoids) of extracts were measured by using colorimetric assays and analyzed by high performance liquid chromatographic (HPLC-DAD). The antioxidant activity was evaluated by chemical and biochemical assays (reducing power assay, 1,1-diphenyl-2-picrylhydrazyl (DPPHâ ) and 2,2-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTSâ +) scavenger assays. It was also investigated the ability of extracts in attenuate lipid peroxidation induced by Fe2+ in phospholipids. The obtained results clearly demonstrated that the botanical origin and geographical region of honey collection influenced the chemical composition and antioxidant activity of extracts. Furthermore, the samples were constituted by phenolic acids and flavonoids, which p-coumaric acid was predominant among the compounds identified. All samples were able to scavenge free radicals and inhibit lipid peroxidation, and good correlations were obtained between the flavonoid content and honey color. In conclusion, the obtained extracts were constituted by antioxidant compounds, which reinforce the usage of honey in human diets, and demonstrated that the region of honey collection strong influenced in the chemical composition and, consequently, its biological effect.
Subject(s)
Antioxidants , Honey , Lipid Peroxidation , Phenols , Honey/analysis , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Phenols/pharmacology , Phenols/chemistry , Phenols/isolation & purification , Phenols/analysis , Brazil , Lipid Peroxidation/drug effects , Chromatography, High Pressure Liquid , Flavonoids/pharmacology , Flavonoids/chemistry , Flavonoids/analysis , Flavonoids/isolation & purification , Biphenyl Compounds/antagonists & inhibitors , Picrates/antagonists & inhibitors , Flowers/chemistry , Benzothiazoles/antagonists & inhibitors , Sulfonic Acids/antagonists & inhibitorsABSTRACT
The exploitation of forest resources, especially non-timber forest products, has effects on different biological levels, from the biochemical level of an organism to the ecosystem level. The present study addresses the effects of different management strategies (protected area, managed area, and an area where the species is cultivated in agroforestry systems) in reproductive phenology, fruit features, and phytochemical profiles of Dimorphandra gardneriana (Leguminosae), a tree species, pioneer, and socioeconomically important plant of the Brazilian Savanna. Its fruits are exploited by extractivist communities to obtain rutin and quercetin, which are internationally traded bioflavonoids (two of the ten most exported phytochemicals in Brazil). The results showed that the effects on these parameters were characterized as positive, increasing according to the level of exploitation. The agroforestry system had higher yields of flavonoids of economic interest, viable fruits and seeds, followed by the management area and the protected area. Finally, knowledge about the planting effects on fava d'anta fruit production can be a great ally for effectively managing forest resources. A varied system of exploitation implies greater and more stable economic returns for extractive communities, favoring the conservation of the species in protected areas.
Subject(s)
Ecosystem , Fabaceae , Flavonoids , Brazil , Conservation of Natural Resources , Environmental Monitoring , Trees , Tropical ClimateABSTRACT
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.
Subject(s)
Antioxidants/pharmacology , Drosophila melanogaster/drug effects , Ilex paraguariensis/chemistry , Malonates/toxicity , Plant Extracts/pharmacology , Animals , Female , Locomotion/drug effects , Male , Sulfhydryl Compounds/metabolism , Thiobarbituric Acid Reactive Substances/metabolismABSTRACT
Walnut (Tetracarpidium conophorum Müll. Arg) has been reported to be an essential ingredient in folklore medicine for sexual enhancement with little scientific validation. Hence, this study investigated the effects of walnut supplemented diet on sexual behaviour and biochemical parameters relevant to erection in male Wistar rats. Forty animals used in this study were divided into five groups (nâ¯=â¯8); Group 1 - normal control rats fed with basal diet, Group II - rats fed diet supplemented with 10% processed walnut, Group III - rats fed diet supplemented with 10% raw walnut, Group IV - rats fed diet supplemented with 20% processed walnut and Group V - rats fed diet supplemented with 20% raw walnut. Behavioural studies (copulation tendency and anxiety) associated with sexual function, measurement of nitric oxide (NO) levels, adenosine deaminase (ADA), arginase and acetylcholinesterase (AChE) activities in the Corpus cavernosum as well as characterization of bioactive components of the nut were evaluated. Marked reductions in ADA and arginase activities and a concomitant increase (% inclusion dependent) in the level of NO as well as enhanced sexual behaviours were observed in rat fed supplemented walnut when compared to the control. Furthermore, analysis of the walnut using high performance liquid chromatography indicated the presence of some polyphenols. From our findings, it showed that walnut improves sexual behaviour and modulates activities of key enzymes relevant to erection in male rats which may justify its used in traditional medicine.
ABSTRACT
Copaifera officinalis L. possesses traditional uses as an analgesic, anti-inflammatory, and antiseptic. However, until now the antinociceptive effect and the mechanism of action were not described for Copaifera officinalis L. oil and no compound present in this oil was identified to be responsible for its biological effects. The goal of this study was to identify the presence of kaurenoic acid in Copaifera officinalis oil and investigate its antinociceptive effect, mechanism of action, and possible adverse effects in mice. The quantification of kaurenoic acid in Copaifera officinalis oil was done by HPLC-DAD technique. Male and female albino Swiss mice (25-35 g) were used to test the antinociceptive effect of Copaifera officinalis (10 mg/kg, intragastric) or kaurenoic acid (1 mg/kg) in the tail-flick test, intraplantar injection of capsaicin, allyl isothiocyanate (AITC) or complete Freund's adjuvant (CFA). Copaifera officinalis oil and kaurenoic acid caused the antinociceptive effect in the tail-flick test in a dose-dependent manner, and their effect was reversed by naloxone (an opioid antagonist). Copaifera officinalis oil or kaurenoic acid reduced the nociception caused by capsaicin or AITC and produced an anti-allodynic effect in the CFA model (after acute or repeated administration for 7 days). Possible adverse effects were also observed, and non-detectable adverse effect was observed for the intragastric administration of Copaiba officinalis oil or kaurenoic acid and in the same way, the treatments were neither genotoxic nor mutagenic at the doses tested. Thus, Copaiba officinalis oil, and kaurenoic acid possess antinociceptive action without adverse effects.
Subject(s)
Analgesics/pharmacology , Diterpenes/pharmacology , Fabaceae/chemistry , Nociception/drug effects , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Capsaicin/pharmacology , Female , Freund's Adjuvant/pharmacology , Hyperalgesia/drug therapy , Hyperalgesia/metabolism , Male , Mice , Pain Measurement/methodsABSTRACT
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 ß-caryophyllene (28.15%) as the major components. EOLM (0.12-0.48 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 (0.12-0.48 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 > 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.
Subject(s)
Drosophila melanogaster/chemistry , Lantana/toxicity , Animals , Antioxidants/pharmacokinetics , Antioxidants/therapeutic use , Gas Chromatography-Mass Spectrometry/methods , Humans , Lantana/metabolism , Oils, Volatile/pharmacokinetics , Oils, Volatile/toxicity , Plant Extracts/pharmacokinetics , Plant Extracts/toxicityABSTRACT
Arthritis is a chronic inflammatory disease which reduces the life quality of affected individuals. Therapeutic tools used for treating inflammatory pain are associated with several undesirable effects. Buddleja thyrsoides Lam., known as 'Barbasco' or 'Cambara', is mostly used in several disorders and possesses antirheumatic, anti-inflammatory, and analgesic properties. Here, we investigated the antinociceptive and anti-inflammatory effects of the B. thyrsoides crude extract applied orally and topically in acute pain models and an arthritic pain model induced by complete Freund's adjuvant (CFA) paw injection in male mice (25-30â g). The high-performance liquid chromatography (HPLC) of the B. thyrsoides extract crude revealed the presence of the lupeol, stigmasterol, and ß-sitosterol. The stability study of the B. thyrsoides gel did not show relevant changes at low temperatures. The oral treatment with the B. thrysoides extract prevented the capsaicin-induced spontaneous nociception and the acetic acid-induced abdominal writhing, but did not alter the thermal threshold in the tail immersion test. The B. thyrsoides antinociceptive effect was not reversed by naloxone in the capsaicin test. The B. thyrsoides oral or topical treatment reversed the CFA-induced mechanical allodynia and thermal hyperalgesia with maximum inhibition (Imax) of 69 ± 6 and 68 ± 5% as well as 78 ± 15 and 87 ± 12%, respectively. Moreover, the topical but not oral treatment inhibited the CFA-induced cell infiltration, but did not reduce the paw edema significantly. The oral treatment with B. thyrsoides did not cause adverse effects. These findings suggest that the oral or topical treatment with B. thyrsoides presents antinociceptive actions in an arthritic pain model without causing adverse effects.
Subject(s)
Analgesics, Non-Narcotic/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Arthritis, Experimental/drug therapy , Buddleja/chemistry , Plant Extracts/therapeutic use , Plant Leaves/chemistry , Acute Pain/drug therapy , Administration, Cutaneous , Administration, Oral , Analgesics, Non-Narcotic/administration & dosage , Analgesics, Non-Narcotic/adverse effects , Analgesics, Non-Narcotic/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Brazil , Buddleja/growth & development , Drug Stability , Drug Storage , Ethnopharmacology , Gels , Hot Temperature/adverse effects , Male , Mice , Pentacyclic Triterpenes/administration & dosage , Pentacyclic Triterpenes/adverse effects , Pentacyclic Triterpenes/analysis , Pentacyclic Triterpenes/therapeutic use , Plant Extracts/administration & dosage , Plant Extracts/adverse effects , Plant Extracts/chemistry , Plant Leaves/growth & development , Sitosterols/administration & dosage , Sitosterols/adverse effects , Sitosterols/analysis , Sitosterols/therapeutic use , Stigmasterol/administration & dosage , Stigmasterol/adverse effects , Stigmasterol/analysis , Stigmasterol/therapeutic use , ViscosityABSTRACT
Carya illinoensis is a widespread species, belonging to the Juglandaceae family, commonly known as Pecan. Popularly, the leaves have been used in the treatment of smoking as a hypoglycemic, cleansing, astringent, keratolytic, antioxidant, and antimicrobial agent. The following research aimed to identify for the first time the phytochemical compounds present in the leaves of C. illinoensis and carry out the determination of antimicrobial activity of aqueous and ethanolic extracts. The antimicrobial activity was tested against 20 microorganisms by determining the minimum inhibitory concentration (MIC). Phenolic acids (gallic acid and ellagic acid), flavonoids (rutin), and tannins (catechins and epicatechins) were identified by HPLC-DAD and may be partially responsible for the antimicrobial activity against Gram-positive, Gram-negative, and yeast. The results showed MIC values between 25 mg/mL and 0.78 mg/mL. The extracts were also able to inhibit the production of germ tubes by Candida albicans.
Subject(s)
Antifungal Agents/analysis , Antifungal Agents/pharmacology , Bacteria/drug effects , Carya/chemistry , Phytochemicals/analysis , Phytochemicals/pharmacology , Yeasts/drug effects , Antifungal Agents/isolation & purification , Chromatography, High Pressure Liquid , Flavonoids/analysis , Flavonoids/isolation & purification , Flavonoids/pharmacology , Hydroxybenzoates/analysis , Hydroxybenzoates/isolation & purification , Hydroxybenzoates/pharmacology , Microbial Sensitivity Tests , Phytochemicals/isolation & purification , Plant Leaves/chemistry , Tannins/analysis , Tannins/isolation & purification , Tannins/pharmacologyABSTRACT
The association of herbal products with standard antimicrobial drugs has recently gained more attention as a hope to overcome infectious diseases caused by multidrug-resistant microorganisms. Here, we investigated for the first time the antimicrobial (antifungal and antibacterial) activity of ethanolic and aqueous extracts of R. echinus against multiresistant strains of bacteria (E. coli, P. aeruginosa and S. aureus) and fungi (C. albicans, C. krusei and C. tropicalis), as well as potential to enhance the activity of antibiotics drugs. In addition, both extract were chemically characterized and their toxicity was assessed in Artemia salina. Our results demonstrate that aqueous extract of R. echinus caused a significant increase in the activity of antibiotics gentamicin and imipenem, while the ethanolic extract strongly enhanced the antibiotic activity of gentamicin, amikacin, imipenem and ciprofloxacin against P. aeruginosa. However, neither the ethanolic nor the aqueous extracts significantly affect the antibiotic activity of the drugs when tested against S. aureus. Phytochemical analysis of the extracts indicated ellagic acid, caffeic acid and chlorogenic acid as the major components which can be at least in part responsible for the enhanced activity of antibiotics. None of the extracts showed toxicity in A. salina even at the highest concentration tested (1000 µg/mL). All together, our results suggest that the leaf extract of R. echinus can be an effective source of modulating agents.
Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Plant Extracts/pharmacology , Tracheophyta/chemistry , Animals , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemistry , Artemia/drug effects , Bacteria/drug effects , Candida/drug effects , Escherichia coli/drug effects , Microbial Sensitivity Tests , Plant Extracts/chemistry , Plant Leaves/chemistry , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effectsABSTRACT
Calyptranthes tricona is a species (Myrtaceae) native to South Brazil. Plants belonging to this family are folkloric used for analgesia, inflammation, and infectious diseases. However, little is known about the toxic potential of C. tricona. The present study aimed to evaluate the antioxidant activity of C. tricona ethanol and hexane leaf extracts, as well as verify their effect on human lymphocytes and MCF-7 cells. The extracts were subjected to preliminary phytochemical screening, antioxidant activity using DPPH and ORAC methods. Genotoxic and mutagenic effects in cultured human lymphocytes were assessed using the comet assay and the micronucleus assay, respectively. In addition, cell viability by MTT assay and fluorometric analysis of mitochondrial potential and caspases-9 activity were performed in order to verify the possible effects of both extracts on H2O2-induced cell death of MCF-7 cells. Our findings revealed that the phenol content and the antioxidant activity were only present in the ethanol extract. Also, the phytochemical screening presented steroids, triterpenoids, condensed tannins, and flavones as the main compounds. However, both extracts were capable of inducing concentration-dependent DNA damage in human lymphocytes. When treating MCF-7 cells with the extracts, both of them inhibited MCF-7 cell death in response to oxidative stress through a decrease of mitochondrial depolarization and caspases-9 activity. Thus, our results need to be considered in future in vitro and in vivo studies of C. tricona effects. In the meanwhile, we recommend caution in the acute/chronic use of this homemade preparation for medicinal purpose.
Subject(s)
DNA Damage , Hydrogen Peroxide/pharmacology , Lymphocytes/metabolism , Myrtaceae/chemistry , Oxidative Stress/drug effects , Plant Extracts/pharmacology , Cell Death/drug effects , Female , Humans , Lymphocytes/pathology , MCF-7 Cells , Plant Extracts/chemistryABSTRACT
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.
Subject(s)
Antioxidants/metabolism , Chelating Agents/metabolism , Mercury/metabolism , Plant Leaves/chemistry , Psidium/chemistry , Saccharomyces cerevisiae/drug effects , Biphenyl Compounds/chemistry , Lipid Peroxidation/drug effects , Picrates/chemistry , Plant Extracts/chemistry , Saccharomyces cerevisiae/physiologyABSTRACT
Maytenus ilicifolia Mart. ex Reissek is a plant commonly used in folklore medicine in the management of gastric diseases in South America. This study explores the effects of a supratherapeutic dose of aqueous and ethanol extracts of M. ilicifolia (1360 mg/kg) on fertility and neurobehavioral status in male and pregnant rats. A battery of sensory-motor developmental endpoints was carried out to assess impairments on pups of dams orally treated with the aqueous extract of M. ilicifolia during the organogenesis period of pregnancy (GD 9 through GD 14). The neuromotor maturation reflexes and physical developments of the offspring were not significantly different between the groups (p < 0.05). Also, the hippocampal morphology revealed no indices of cell loss in the CA1, CA2, CA3 and CA4 areas. As second protocol, some fertility aspects were investigated in young post pubertal male Wistar rats treated with the ethanol extract for 30 days. The semen quality and testicular tissue morphology of male rats treated with the ethanol extract of M. ilicifolia remained unaffected upon treatment. Thus, the results indicate that the high-dose of M. ilicifolia extracts have no neurotoxic potential on offspring and seem not to affect the sperm quality of male rats.
Subject(s)
Behavior, Animal/drug effects , Fertility/drug effects , Maytenus/chemistry , Medicine, Traditional/adverse effects , Plant Extracts/adverse effects , Stomach Diseases/drug therapy , Animals , Ethanol/chemistry , Female , Male , Organogenesis/drug effects , Pregnancy , Rats , Rats, Wistar , Semen Analysis , South America , Testis/drug effects , Water/chemistryABSTRACT
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.
Subject(s)
Erectile Dysfunction/metabolism , Fruit/chemistry , Malondialdehyde/metabolism , Penis/metabolism , Plant Extracts/therapeutic use , Plantago , Animals , Chromatography, High Pressure Liquid/methods , Dose-Response Relationship, Drug , Erectile Dysfunction/drug therapy , Male , Malondialdehyde/analysis , Penis/chemistry , Penis/drug effects , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Rats , Rats, WistarABSTRACT
This study evaluates, for the first time, the antibiofilm, antimicrobial and antiparasitic potential of crude extract and fractions of stems of Equisetum hyemale against several infectious agents (bacteria, fungi, Mycobacterium and Trypanosomes) by broth microdilution technique and investigates the phenolic composition of the plant by high performance liquid chromatography. The crude extract and fractions showed antimicrobial activity, as they were capable of inhibiting the growth of bacteria in minimal inhibitory concentrations (MICs) ranging from 52.4 mg/mL to 3.27 mg/mL. For Candida species, the MICs ranged from 52.4 mg/mL to 6.5 mg/mL, and for Mycobacterium species from 2.5 mg/mL to 0.625 mg/mL. The dichloromethane fraction was able to reduce 83% of Pseudomonas aeruginosa biofilm formation and 51% of Candida albicans biofilms. The n-butanol fraction presents an important protozoal effect, reducing 100% of Trypanosoma evansi trypomastigotes after 9 h of exposure. The HPLC analysis revealed that the major substances are rosmarinic acid in dichloromethane fraction (7.38 ± 0.08 mg/g FS) and chlorogenic acid in ethyl acetate fraction (8.4 ± 0.26 mg/g FS). The crude extract and fractions of E. hyemale can be both useful and effective agents as a sustainable alternative for the treatment and prevention of several infectious agents.
Subject(s)
Anti-Infective Agents/pharmacology , Bacteria/drug effects , Biofilms/drug effects , Candida/drug effects , Equisetum/chemistry , Plant Extracts/pharmacology , Trypanosoma/drug effects , Anti-Infective Agents/isolation & purification , Chromatography, Liquid , Microbial Sensitivity Tests , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Extracts/isolation & purificationABSTRACT
Long-term treatment with fluphenazine is associated with manifestation of extrapyramidal side effects, such as tardive dyskinesia. The molecular mechanisms related to the pathophysiology of TD remain unclear, and several hypotheses, including a role for oxidative stress, have been proposed. Harpagophytum procumbens is an herbal medicine used mainly due to anti-inflammatory effects, but it also exhibits antioxidant effects. We investigated the effect of ethyl acetate fraction of H. procumbens (EAF HP) in fluphenazine-induced orofacial dyskinesia by evaluating behavioral parameters at different times (vacuous chewing movements (VCM's) and locomotor and exploratory activity), biochemical serological analyses, and biochemical markers of oxidative stress of the liver, kidney, cortex, and striatum. Chronic administration of fluphenazine (25 mg/kg, intramuscular (i.m) significantly increased the VCMs at all analyzed times (2, 7, 14, and 21 days), and this was inhibited by EAF HP (especially at a dose of 30 mg/kg). Fluphenazine decreased locomotion and exploratory activity, and EAF HP did not improve this decrease. Fluphenazine induced oxidative damage, as identified by changes in catalase activity and ROS levels in the cortex and striatum, which was reduced by EAF HP, especially in the striatum. In the cortex, EAF HP was protective against fluphenazine-induced changes in catalase activity but not against the increase in ROS level. Furthermore, EAF HP was shown to be safe, since affected serum biochemical parameters or parameters of oxidative stress in the liver and kidney. These findings suggest that the H. procumbens is a promising therapeutic agent for the treatment of involuntary oral movements.
Subject(s)
Acetates/chemistry , Antioxidants/pharmacology , Antipsychotic Agents/toxicity , Brain/drug effects , Fluphenazine/toxicity , Harpagophytum/chemistry , Mastication/drug effects , Oxidative Stress/drug effects , Plant Extracts/pharmacology , Tardive Dyskinesia/drug therapy , Animals , Antioxidants/therapeutic use , Brain/metabolism , Exploratory Behavior/drug effects , Free Radical Scavengers/pharmacology , Free Radical Scavengers/therapeutic use , Male , Motor Activity/drug effects , Plant Extracts/therapeutic use , Rats, Wistar , Solvents , Tardive Dyskinesia/chemically induced , Tardive Dyskinesia/metabolism , Tardive Dyskinesia/psychologyABSTRACT
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 4â% supplementation of turmeric, respectively, and groups 6 and 7 included normotensive and hypertensive rats treated with 4â% 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.
Subject(s)
Acetylcholinesterase/metabolism , Butyrylcholinesterase/metabolism , Curcuma , Cytokines/metabolism , Hypertension/diet therapy , Plant Preparations/therapeutic use , Zingiber officinale , Animals , Cholinergic Agents/isolation & purification , Cholinergic Agents/pharmacology , Hypertension/enzymology , Male , Purinergic Agents/isolation & purification , Purinergic Agents/pharmacology , Rats , Rats, Wistar , Rhizome , T-Lymphocytes/drug effects , T-Lymphocytes/metabolismABSTRACT
CONTEXT: Croton campestris A.St.-Hil. (Euphorbiaceae) is a species native to Northeast Brazil used by traditional communities for the treatment of a variety of health problems. However, potential toxicological effects of this plant are unknown. OBJECTIVE: The potential toxicity of the hydroalcoholic extract of C. campestris leaves on Drosophila melanogaster insect model, additionally with phytochemical constitution and cellular mechanisms mediating the action of extract were analysed in this study. MATERIALS AND METHODS: Constituents of the extract were evaluated by HPLC. In vitro antioxidant potential of extract was analysed by DPPH, ABTS and FRAP. Flies injected culture medium mixed with extract (0.1-50 mg/mL) for 72 h. After, ROS production was evaluated by DCF-DA oxidation. Phosphorylation of MAPK signalling pathway was investigated by Western blotting method. Activity of antioxidant enzymes was analysed in homogenates. RESULTS: Major components of the extract include quercetin (38.11 ± 0.06 mg/g), caffeic acid (20.06 ± 0.17 mg/g) and kaempferol (15.45 ± 0.05 mg/g). Consumption of the extract impaired locomotor performance and induced fly death of flies (LC50 of 26.51 mg/mL). Augmented ROS formation and SOD, CAT and GST activity were observed from 0.1 mg/mL. JNK and p38 kinases phosphorylation was modulated and Paraquat-induced toxicity was augmented by extract. DISCUSSION AND CONCLUSION: Our data show important toxicological effects of C. campestris leading to increased mortality and impaired locomotor performance accompanied by induction of cell stress markers in flies. The study draws attention to the indiscriminate use of plant extracts.
Subject(s)
Croton , Drosophila melanogaster/drug effects , Oxidants/toxicity , Oxidative Stress/drug effects , Plant Extracts/toxicity , Animals , Cell Survival/drug effects , Cell Survival/physiology , Dose-Response Relationship, Drug , Drosophila melanogaster/metabolism , Free Radical Scavengers/isolation & purification , Free Radical Scavengers/toxicity , Oxidants/isolation & purification , Oxidative Stress/physiology , Plant Extracts/isolation & purification , Plant Leaves , Survival Rate/trendsABSTRACT
Context Melissa officinalis subsp. inodora Bornm. (Lamiaceae) has been used since ancient times in folk medicine against various diseases, but it has not been investigated against protozoa. Objective To evaluate the activities of M. officinalis against Leishmania braziliensis, Leishmania infantum and Trypanosoma cruzi as well as its cytotoxicity in fibroblast cell line. Materials and methods The fresh leaves were chopped into 1 cm(2) pieces, washed and macerated with 99.9% of ethanol for 72 h at room temperature. Antiparasitic activity of M. officinalis was accessed by direct counting of cells after serial dilution, while the cytotoxicity of M. officinalis was evaluated in fibroblast cell line (NCTC929) by measuring the reduction of resazurin. The test duration was 24 h. High-performance liquid chromatography (HPLC) was used to characterise the extract. Results The extract at concentrations of 250 and 125 µg/mL inhibited 80.39 and 54.27% of promastigote (LC50 value = 105.78 µg/mL) form of L. infantum, 80.59 and 68.61% of L. brasiliensis (LC50 value = 110.69 µg/mL) and against epimastigote (LC50 value = 245.23 µg/mL) forms of T. cruzi with an inhibition of 54.45 and 22.26%, respectively, was observed. The maximum toxicity was noted at 500 µg/mL with 95.41% (LC50 value = 141.01 µg/mL). The HPLC analysis identified caffeic acid and rutin as the major compounds. Discussion The inhibition of the parasites is considered clinically relevant (< 500 µg/mL). Rutin and caffeic acids may be responsible for the antiprotozoal effect of the extract. Conclusion The ethanol extract of M. officinalis can be considered a potential alternative source of natural products with antileishmania and antitrypanosoma activities.
Subject(s)
Antiprotozoal Agents/pharmacology , Chromatography, High Pressure Liquid , Kinetoplastida/drug effects , Melissa , Phenols/pharmacology , Plant Extracts/pharmacology , Antiprotozoal Agents/isolation & purification , Antiprotozoal Agents/toxicity , Cell Line , Cell Survival/drug effects , Dose-Response Relationship, Drug , Fibroblasts/drug effects , Fibroblasts/pathology , Kinetoplastida/growth & development , Leishmania braziliensis/drug effects , Leishmania infantum/drug effects , Lethal Dose 50 , Melissa/chemistry , Parasitic Sensitivity Tests , Phenols/isolation & purification , Phenols/toxicity , Phytotherapy , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Plant Leaves , Plants, Medicinal , Spectrophotometry , Trypanosoma cruzi/drug effectsABSTRACT
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.
Subject(s)
Antioxidants/pharmacology , Brain Chemistry/drug effects , Centella/chemistry , Lipid Peroxidation/drug effects , Nitroprusside/pharmacology , Oxidants/pharmacology , Quinolinic Acid/pharmacology , Triterpenes/pharmacology , Acetates , Animals , Free Radical Scavengers/pharmacology , Male , Molybdenum/chemistry , Oxidation-Reduction , Plant Extracts , Rats , Rats, Wistar , SolventsABSTRACT
Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammation, coughs, and infectious diseases. However, no information is available on the potential antioxidant, cytotoxicity and genotoxicity of this plant. In this study, the polyphenolic constituents, antioxidant capacity and potential toxic effects of aqueous and ethanolic extracts of R. echinus on human erythrocytes and leukocytes were investigated for the first time. R. echinus extracts showed the presence of Gallic, chlorogenic, caffeic and ellagic acids, rutin, quercitrin and quercetin. Aqueous and ethanolic extracts of R. echinus exhibited antioxidant activity in DPPH radical scavenging with IC50 = 111.9 µg/mL (EtOH extract) and IC50 = 227.9 µg/mL (aqueous extract). The extracts inhibited Fe(2+) (10 µM) induced thiobarbituric acid reactive substances (TBARS) formation in rat brain and liver homogenates. The extracts (30-480 µg/mL) did not induce genotoxicity, cytotoxicity or osmotic fragility in human blood cells. The findings of this present study therefore suggest that the therapeutic effect of R. echinus may be, in part, related to its antioxidant potential. Nevertheless, further in vitro and in vivo studies are required to ascertain the safety margin of its use in folk medicine.