RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Casearia decandra (guaçatonga) is popularly used as an anti-inflammatory. We investigated the antioxidant and anti-inflammatory effect of C.decandra leaves (CdE) ethanolic extract and of the rutin standard (present in the CdE). MATERIALS AND METHODS: Male adult Swiss mice were used (25-30 g; 5-6 animals by a group). CdE phytochemical analysis was performed by HPLC method. The antioxidant potential of CdE and rutin was assessed by different methods. Topical anti-inflammatory effect of CdE (0.001-1mg/ear) and rutin (0.003-0.03mg/ear) was evaluated by ear edema formation and inflammatory cells infiltration (MPO activity and histology) on a skin inflammation model induced by topical application of croton oil (1mg/ear). RESULTS: Rutin (27.81 ± 1.11 mg/g) was identified in CdE by HPLC analysis. The required amounts of CdE, rutin and ascorbic acid to reduce the initial concentration of radical DPPH by 50% (IC50) were 7.77 (6.31-9.57) µg/mL, 3.62 (3.26-4.01) µg/mL and 3.74 (3.37-4.14) µg/mL with a radical DPPH reduction of 91 ± 1.2%, 91 ± 0.5%, and 96 ± 0.44% (at 30 µg/mL), respectively. Moreover, CdE and rutin presented H2O2 scavenging activity with H2O2 levels reduction of 41 ± 7% and 46 ± 6%, respectively and SOD-like activity of 60 ± 4% and 51 ± 14%, respectively. On the other hand, just rutin presented nitric oxide scavenging activity of 54 ± 6%. CdE and rutin topically applied inhibited the ear edema with a maximum inhibition of 70 ± 5% (1 mg/ear) and 78 ± 10% (0.03 mg/ear), respectively. Treatments reduced the MPO activity (42 ± 4% to CdE; 1mg/ear and 30 ± 8% to rutin; 0.03 mg/ear). Histologically, the topical treatments also reduced the dermis thickness and the inflammatory cells infiltration. CONCLUSION: We demonstrated the antioxidant and anti-inflammatory effect of C.decandra leaves and rutin. Its antioxidant potential may contribute to inflammatory process attenuation, supporting the C.decandra leaves used as a promising alternative in the therapy of the inflammatory diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Casearia/química , Dermatite de Contato/tratamento farmacológico , Extratos Vegetais/farmacologia , Administração Cutânea , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Antioxidantes/isolamento & purificação , Antioxidantes/uso terapêutico , Óleo de Cróton/toxicidade , Dermatite de Contato/etiologia , Dermatite de Contato/patologia , Modelos Animais de Doenças , Etanol/química , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Rutina/farmacologia , Pele/efeitos dos fármacos , Pele/patologiaRESUMO
Scolicidal agents are important in the treatment of cystic echinococcosis. This study evaluated the scolicidal activity of the plant Blepharocalyx salicifolius (H.B.K.) Berg against Echinococcus ortleppi protoscoleces. The parasite species was identified by amplifying a fragment of the gene cytochrome c oxidase subunit 1 (COX 1). B. salicifolius crude extract at concentrations of 100, 200, 300 and 400 mg/mL was analyzed at different times (5, 10, 15, 30, 45 and 60 min). N-butanol and ethyl acetate fractions (100 and 200 mg/ mL) were also analyzed at 5, 10, 15 and 30 min. Both fractions showed 100% scolicidal activity at the concentration of 200 mg/mL at 5 min. Gallic acid, identified as the major compound of the ethyl acetate fraction- was responsible for the observed scolicidal activity. The results showed that crude extract and fractions of B. salicifolius have scolicidal effect against E. ortleppi protoscoleces.
Assuntos
Anti-Helmínticos/farmacologia , Echinococcus/efeitos dos fármacos , Myrtaceae/química , Extratos Vegetais/farmacologia , Animais , Relação Dose-Resposta a Droga , Testes de Sensibilidade ParasitáriaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Vitex megapotamica (Spreng) Moldenke has been used in South American folk medicine to treat inflammatory diseases. However, the effects of V. megapotamica on animal models of nociception and depression have not been evaluated. AIM OF THE STUDY: This study investigated whether the crude leaf extract of V. megapotamica exhibits antinociceptive and antidepressant-like effects in a Freund's adjuvant-induced chronic inflammation and depression model. MATERIALS AND METHODS: Chronic inflammation was induced in rats by the intraplantar administration of complete Freund's adjuvant (CFA; 100µl). The effect of oral crude extract of V. megapotamica (VmE; 3-30mg/kg, p.o.) on nociception (thermal hyperalgesia, mechanical allodynia and arthritis score), inflammation (edema, myeloperoxidase activity), immobility (forced swimming test), locomotor activity (open field), gastrointestinal transit, hyperalgesia and naloxone-precipitated morphine withdrawal syndrome was evaluated. Naloxone (0.4mg/kg, i.p.) was used to investigate the involvement of opioid system in the currently described effects of VmE. RESULTS: Crude extract caused antinociceptive/antidepressant-like effects in the CFA-induced chronic inflammation model, which was prevented by naloxone. The VmE extract (10mg/kg, p.o.) did not alter the locomotor activity, gastrointestinal function and inflammatory parameters and did not cause hyperalgesia. CONCLUSION: V. megapotamica induces opioid-dependent antinociception and antidepressant-like effect, without anti-inflammatory activity. The results support the use of VmE as analgesic and antidepressant.
Assuntos
Analgésicos/farmacologia , Antidepressivos/farmacologia , Comportamento Animal/efeitos dos fármacos , Depressão/prevenção & controle , Hiperalgesia/prevenção & controle , Atividade Motora/efeitos dos fármacos , Nociceptividade/efeitos dos fármacos , Extratos Vegetais/farmacologia , Vitex/química , Administração Oral , Analgésicos/administração & dosagem , Analgésicos/isolamento & purificação , Animais , Antidepressivos/administração & dosagem , Antidepressivos/isolamento & purificação , Depressão/etiologia , Depressão/psicologia , Modelos Animais de Doenças , Adjuvante de Freund , Hiperalgesia/etiologia , Hiperalgesia/fisiopatologia , Inflamação/induzido quimicamente , Masculino , Naloxona/farmacologia , Antagonistas de Entorpecentes/farmacologia , Limiar da Dor/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Plantas Medicinais , Ratos Wistar , Tempo de Reação/efeitos dos fármacos , Natação , Fatores de TempoRESUMO
Solanum corymbiflorum is popularly known as "baga-de-veado" and its leaves are applied on inflamed legs, scabies, tick bite, boils, mastitis, low back pain and otitis. The aim of this study was evaluate anti-inflammatory in vivo activity and relate this activity with antioxidant compounds present in the extract of S. corymbiflorum leaves. The extract from S. corymbiflorum leaves topically applied was able to reduce the croton oil-induced ear edema and myeloperoxidase (MPO) activity with maximum inhibition of 87±3% and 45±7%, rescpectively in the dose of 1mg/ear. Similar results were found for positive control dexamethasone, which presented inhibitions of ear edema and MPO activity of 89±3% and 50±3%, respectively in a dose of 0.1mg/ear. These findings are due, at least in part, the presence of polyphenols (195.28mg GAE/g) and flavonoids, as chlorogenic acid (59.27mg/g), rutin (12.72mg/g), rosmarinic acid, caffeic acid and gallic acid found by high performance liquid chromatography (HPLC) analysis. This species showed potencial antioxidant by 1,1-diphenyl-2-picrylhydrazyl (DPPH), and carbonyl groups in proteins methods which may be related with the presence of this compounds. This species possess anti-inflammatory activity confirming their popular use for the local treatment of skin inflammatory disorders.
Assuntos
Anti-Inflamatórios/farmacologia , Folhas de Planta/química , Solanum/química , Administração Tópica , Animais , Anti-Inflamatórios/administração & dosagem , Antioxidantes/farmacologia , Compostos de Bifenilo , Cromatografia Líquida de Alta Pressão , Dexametasona/farmacologia , Edema/induzido quimicamente , Edema/prevenção & controle , Flavonoides/análise , Masculino , Camundongos , Peroxidase/metabolismo , Picratos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/análise , Carbonilação Proteica/efeitos dos fármacosRESUMO
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.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Rhamnaceae/química , Géis/química , Modelos Lineares , Casca de Planta/química , Extratos Vegetais/química , Reprodutibilidade dos Testes , Sensibilidade e EspecificidadeRESUMO
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.
RESUMO
The aim of this study was to evaluate the potential positive effect of black grape juice (BGJ) on lipid peroxidation considering Total Body Irradiation (TBI) in Wistar rats. As a potential feasible means of evaluation in situ, blood serum lactate dehydrogenase (LDH) levels were evaluated as a marker for heart damage from acute radiation syndrome (ARS). Twenty rats were divided into four groups, two of them being irradiated by gamma-rays from a Co-60 source. Animals were treated by gavage with 2 mL per day of BGJ or placebo for one week before and 4 days after 6 Gy whole body gamma-irradiation, when they were euthanasiated. LDH on serum and lipid peroxidation on heart tissue were evaluated. High concentration of metabolites from lipid peroxidation in heart, and high LDH level on serum were found only in gamma-irradiated group given placebo, mainly at the first 24 h after radiation. Phytochemical analysis of BGJ was performed by determining total phenolics, flavonoids, and tannins followed by a high-performance liquid chromatography (HPLC/DAD) analysis, which showed resveratrol as the major constituent. Results suggest that BGJ is a good protective candidate compound against heart damage from ARS and its effects suggest its use as a radiomodifier.
Assuntos
Raios gama , Coração/efeitos dos fármacos , Extratos Vegetais/farmacologia , Lesões Experimentais por Radiação/tratamento farmacológico , Protetores contra Radiação/farmacologia , Vitis/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Flavonoides/química , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Frutas/química , Coração/efeitos da radiação , L-Lactato Desidrogenase/metabolismo , Peroxidação de Lipídeos , Masculino , Malondialdeído/metabolismo , Fenóis/química , Fenóis/farmacologia , Fenóis/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Lesões Experimentais por Radiação/metabolismo , Protetores contra Radiação/química , Protetores contra Radiação/uso terapêutico , Ratos , Ratos Wistar , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Irradiação Corporal TotalRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Viola tricolor, popularly known as heartsease has been empirically used in several skin disorders, including burns. AIM OF THE STUDY: The objective of this study was investigate the antinociceptive and antiinflammatory effect of a gel containing extract of Viola tricolor flowers on thermal burn induced by UVB irradiation and to perform gel stability study. METHODS: The antinociceptive and antiinflammatory effect were evaluated by static and dynamic mechanical allodynia model, paw edema, and neutrophilic cell infiltration. Metabolites compounds were quantified by HPLC. The gel stability study was performed analyzing organoleptical aspects, besides pH, viscosity, and quantification of rutin by HPLC. RESULTS: In the results were evidenced changes in threshold in statical and dynamic mechanical allodynia (I(max)=100 ± 10% and 49 ± 10%, respectively), paw edema (I(max)=61 ± 6%), and myeloperoxidase activity (I(max)=89 ± 5%). Such effects may be attributed, in part, to rutin, salicylic and chlorogenic acids, and others compounds found in this species. No important changes were detected in the stability study, in all aspects analyzed in temperature below 25 °C. CONCLUSION: These findings suggest that Viola tricolor gel has an antinociceptive and antiinflammatory effect in the ultraviolet-B-induced burn, since maintain the temperature below 25 °C.
Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Extratos Vegetais/uso terapêutico , Queimadura Solar/tratamento farmacológico , Viola , Animais , Modelos Animais de Doenças , Estabilidade de Medicamentos , Edema/tratamento farmacológico , Edema/imunologia , Flores , Géis , Hiperalgesia/tratamento farmacológico , Hiperalgesia/imunologia , Masculino , Neutrófilos/imunologia , Ratos , Ratos Wistar , Queimadura Solar/imunologiaRESUMO
Vitex megapotamica (Sprengel) Moldenke belongs to the Verbenaceae family and is popularly known as "tarumã". The antioxidant capacity of fractions and crude extract from the leaves of V. megapotamica were determined in this study through the capacity to remove reactive species and phenolic compounds were quantified in the various fractions. The IC50 (DPPH) ranged from 14.17 ± 0.76 to 37.63 ± 0.98 µg/mL. The ethyl acetate fraction might contain the strongest lipid peroxidation inhibitory compounds with an IC50 of 16.36 ± 5.09 µg/mL, being also the one with the highest content of polyphenols (522.4 ± 1.12 mg/g), flavonoids (220.48 ± 0.30 mg/g) and condensed tannins (3.86 ± 0.53 mg/g). Compounds quantified by HPLC/DAD in the crude extract and fractions were chlorogenic and rosmarinic acids. Higher dosages of the extracts were more effective in reducing levels of plasma protein carbonyls and were also shown to be able to remove reactive species by a 2',7'-dichlorofluorescein diacetate assay, reducing oxidative stress in all tested fractions. Results obtained indicated that V. megapotamica exhibits good potential to prevent diseases caused by the overproduction of free radicals and it might also be used as a potential source of natural antioxidant agents.
Assuntos
Antioxidantes/análise , Flavonoides/análise , Polifenóis/análise , Taninos/análise , Vitex/química , Antioxidantes/química , Antioxidantes/farmacologia , Ácido Clorogênico/análise , Cromatografia Líquida de Alta Pressão , Cinamatos/análise , Depsídeos/análise , Flavonoides/química , Flavonoides/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Folhas de Planta/química , Polifenóis/química , Polifenóis/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Taninos/química , Taninos/farmacologia , Ácido RosmarínicoRESUMO
Nowadays there is an increase in the number of people taking herbals worldwide. Scutia buxifolia is used for the treatment of hypertension, but little is known about its action on liver. Thirty-two Wistar rats were divided into four groups: control and groups treated during 30 days with 100, 200 and 400 mg of lyophilized aqueous extract of S. buxifolia (SBSB)/kg of body weight. This study was planned to explore hepatotoxic effect of SBSB, which was assessed by serum transaminases (ALT and AST). Thiobarbituric acid reactive substances (TBARS) levels were determined in liver, along with thiols content (NPSH), catalase (CAT) activity and, superoxide dismutase (SOD) enzymes. Histopathological studies of liver tissue were performed. Flavonoids and phenolics were quantified in SBSB by high performance liquid chromatography with diode array detection (HPLC/DAD). We did not observe alterations on redox status (TBARS, NPSH, CAT and, SOD) in the control and experimental groups. An increase on AST activity was only observed at 200 mg of SBSB, whereas ALT score was not affected by SBSB. Moreover, no morphological alterations were observed on the hepatocytes, matching the analysed biochemical parameters. This way, we conclude that SBSB was not toxic.
Assuntos
Fígado/efeitos dos fármacos , Extratos Vegetais/toxicidade , Rhamnaceae/metabolismo , Animais , Antioxidantes/análise , Catalase/efeitos dos fármacos , Catalase/metabolismo , Flavonoides/análise , Medicina Herbária , Testes de Função Hepática , Oxirredução/efeitos dos fármacos , Ratos , Ratos Wistar , Superóxido Dismutase/efeitos dos fármacos , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/análise , Transaminases/efeitos dos fármacosRESUMO
As farmácias magistrais têm se mostrado uma alternativa quando o paciente procura medicamentos com doses personalizadas ou custos mais baixos, o que resultou em um crescente aumento pela procura de medicamentos manipulados. Porém, apesar das vantagens, estes medicamentos não passam por um rígido controle de qualidade, o que pode colocar o tratamento do paciente em risco. Este trabalho teve como objetivos validar metodologia analítica e avaliar a qualidade das cápsulas de cloridrato de metformina manipuladas por sete farmácias de Santa Maria RS. O método validado mostrou-se seletivo, linear, preciso, exato e robusto, podendo ser utilizado para a determinação quantitativa de cloridrato de metformina em cápsulas. As cápsulas produzidas pelas farmácias A, B, D, F e G cumpriram com os requisitos mínimos de controle de qualidade e as cápsulas manipuladas pelas farmácias C e E foram reprovadas nos testes de doseamento e uniformidade de doses unitárias.
Compounding pharmacies have proved a useful alternative when patients look for drugs fitted to their needs in dose number and size, or for less expensive drug forms, leading to an increasing demand for compounded drugs. However, despite the advantages, these drugs do not always go through a strict quality control, which may be detrimental to patient care. The aim of the present study is to validate an analytical method and use it to assess the quality of metformin hydrochloride capsules obtained from seven different compounding pharmacies in Santa Maria, RS (Brazil). The validated method proved to be selective, linear, precise, accurate and robust and can be used for the quantitative determination of metformin hydrochloride in capsules. The capsules compounded by pharmacies A, B, D, F and G met the minimum requirements of quality control, while those from pharmacies C and E failed in the assays of dose and uniformity of dosage units.
Assuntos
Cápsulas/química , Composição de Medicamentos , Metformina , Controle de QualidadeRESUMO
The honeybee disease American foulbrood (AFB) is a serious problem since its causative agent (Paenibacillus larvae) has become increasingly resistant to conventional antibiotics. One of the feasible alternative treatments being used for control of this disease are plants extracts. The aim of the present work was to evaluate the effect of crude extract and fractions of Scutia buxifolia against six Paenibacillus species, including P. larvae, and its potential use for the control of AFB. In vitro activity of S. buxifolia samples against Paenibacillus species were evaluated by the disk diffusion and microdilution methods, and the minimal inhibitory concentration (MIC) were also determined. All Paenibacillus species were sensitive to crude extract and fractions of S. buxifolia. The dichloromethane (DC) fraction showed the better MIC (1.56 mg/mL), followed by ethyl acetate (EtAc) (6.25 mg/mL), n-butanol (BuOH) (25 mg/mL) and Crude extract (CE) (50 mg/mL). Toxic effect of S. buxifolia crude extracts and fractions against bees were also evaluated by the spraying application method of the same concentrations of MICs. The samples tested showed no toxic effects for the bees after 15 days of observation. These results are first time described for this species and showed that S. buxifolia presented a important activity against Paenibacillus species and proved to be a natural alternative for the prevention/control of AFB.
Assuntos
Anti-Infecciosos/farmacologia , Abelhas/microbiologia , Infecções por Bactérias Gram-Positivas/veterinária , Viabilidade Microbiana/efeitos dos fármacos , Paenibacillus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Rhamnaceae , Animais , Anti-Infecciosos/química , Anti-Infecciosos/toxicidade , Abelhas/efeitos dos fármacos , Fracionamento Químico , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Estimativa de Kaplan-Meier , Larva/efeitos dos fármacos , Larva/microbiologia , Longevidade/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Paenibacillus/patogenicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidadeRESUMO
Heartsease, also known as wild pansy (Viola tricolor L.), contains considerable amounts of polyphenols: 109.32 ± 1.29 mg of Gallic acid equivalent/g of extract. This study investigates their phytoconstituents and antioxidant capacity and validates a method for the quantification of rutin in the crude extract of the flowers of V. tricolor and in the extract incorporated in gel. Much better antioxidant capacity was found for the extract [inhibition concentration (IC50) of 16.00 ± 0.78 µg/mL] than the standard ascorbic acid (IC50 of 16.57 ± 0.95 µg/mL); these excellent results may be attributable to the amounts of polyphenols, flavonoids and condensed tannins. The high-performance liquid chromatography method for the quantification of rutin in the extract and gel was linear, sensitive, precise, specific, accurate and robust. This validated method can be used to control the quality of the extract and the gel.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/análise , Rutina/análise , Viola/química , Antioxidantes/análise , Antioxidantes/isolamento & purificação , Géis/análise , Extratos Vegetais/isolamento & purificação , Rutina/isolamento & purificaçãoRESUMO
The essential oils obtained by hydrodistillation from the leaves of Tabernaemontana catharinensis had their composition analysed by GC-MS. A total of 18 substances were identified, consisting of a complex mixture of sesquiterpenes (83.52%), monoterpenes (5.46%) and triterpenes (4.56%). The main components in the oil were ß-caryophyllene (56.87%), α-cadinol (12.52%), 8S,13-cedran-diol (5.41%), α-terpineol (3.99%), ß-eudesmol (2.54%), caryophyllene oxide (2.51%) and ethyl iso-allocholate (2.03%) along with ß-cubebene, γ-cadinene, cubenol, 1,8-cineol, o-cymene, curcumenol, spathulenol, friedeline and ß-sitosterol as minor constituents. An antioxidant property was tested with the oil obtained by means of 1,1-diphenyl-2-picrylhydrazyl assay; the oil presented interesting radical scavenging activity. To the best of our knowledge, this is the first study of the composition and antioxidant activity of essential oil from the T. catharinensis collected from Brazil.
Assuntos
Antioxidantes/química , Óleos Voláteis/química , Folhas de Planta/química , Tabernaemontana/química , Monoterpenos Cicloexânicos , Cicloexanóis/química , Cicloexenos/química , Eucaliptol , Monoterpenos/química , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Sesquiterpenos de Eudesmano/química , Sitosteroides/química , Terpenos/químicaRESUMO
This study is designed to examine the chemical composition and antioxidant activity of the essential oil of Vitex megapotamica. Gas chromatography-mass spectrometry analysis resulted in the detection of 27 components, representing 92.36% of the total oil composition. The main components in the oil were butylated hydroxytoluene (BHT) (34.17%), phytol (12.66%), α-caryophyllene (11.84%), δ-elemene (10.65%), ß-caryophyllene (7.82%), γ-elemene (4.24%) and germacrene D (2.82%). The antioxidant activity of the oil was evaluated in terms of their free-radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl. The oil showed percentage inhibition of 35.62% and 75.25% at concentrations of 76 and 101.6 mg mL(-1), respectively. BHT (36.30%) was also determined by HPLC-DAD in the hexane fraction from the leaves. To the best of our knowledge, this is the first study of the composition and antioxidant activity of the essential oil of the species V. megapotamica.
Assuntos
Antioxidantes/química , Óleos Voláteis/química , Vitex/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo , Hidroxitolueno Butilado/análise , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis/isolamento & purificação , Picratos , Folhas de Planta/químicaRESUMO
Jatropha isabellei Müll Arg. belongs to the family Euphorbiaceae. The antioxidant capacity of this plant was evaluated by the DPPH method and inhibition of thiobarbituric acid reactive substances (TBARS). Ethyl acetate fraction demonstrated the best antioxidant capacity against the DPPH free radical and its profile was similar to ascorbic acid. This fraction also presented the best results of phenolics, flavonoids and condensed tannins, showing a positive relation between the phenolic content and antioxidant activity. All fractions and the crude extract were able to inhibit significantly the TBARS production induced by Fe(II) for the two tested concentrations, reaching the basal levels. In this test, ethyl acetate and dichloromethane fraction showed good values for inhibitory concentration. The dichloromethane fraction showed the best results against the fungi Sporothrix schenckii and Fusarium proliferatum and the bacterium of Micrococcus genus. This fraction allowed the isolation of acetil aleuritolic acid and a mixture of sitosterol 3-O-ß-D-glucoside and stigmasterol, described for the first time in this species.
Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Jatropha/química , Animais , Anti-Infecciosos/química , Antioxidantes/química , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Avaliação Pré-Clínica de Medicamentos/métodos , Flavonoides/análise , Sequestradores de Radicais Livres/farmacologia , Fusarium/efeitos dos fármacos , Glucosídeos/química , Glucosídeos/isolamento & purificação , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Estrutura Molecular , Fenóis/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos Wistar , Sitosteroides/química , Sitosteroides/isolamento & purificação , Sporothrix/efeitos dos fármacos , Estigmasterol/isolamento & purificação , Taninos/análise , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Triterpenos/isolamento & purificaçãoRESUMO
Este trabalho teve como objetivo principal comparar, através do estudo de equivalência farmacêutica e do perfil de dissolução in vitro, oito medicamentos genéricos contendo paracetamol 750 mg, comercializados na região central do Rio Grande do Sul. As análises foram realizadas em conformidade com a monografia do paracetamol comprimidos, descrita na Farmacopeia Brasileira (2010). Os genéricos A, B, D, E, F, G e H são equivalentes farmacêuticos do medicamento referência, pois foram aprovados em todos os testes a que foram submetidos. O Genérico C, no entanto, foi reprovado no doseamento. Quando avaliados em relação ao perfil de dissolução, pelos critérios descritos na RDC 31/2010, somente o genérico E não possui o mesmo perfil de dissolução que o medicamento referência, porém quando comparados pela eficiência de dissolução (ED) podemos verificar que somente os Genéricos G, H, F e A possuem a mesma ED que o medicamento referência.
The aim of this study was to compare, by testing their pharmaceutical equivalence and dissolution profiles in vitro, eight generic medicines containing 750 mg paracetamol, marketed in the central region of Rio Grande do Sul (Brazil). Analyses were carried out in accordance with the monograph on paracetamol tablets in the Brazilian Pharmacopoeia (2010). The generic medicines A, B, D, E, F, G and H are pharmaceutically equivalent to the drug reference, since they passed all the tests they underwent. Of all the samples analyzed, only drug E did not have the same dissolution profile as the reference drug, a fact that may interfere with the interchangeability of these products, which is required of a drug being marketed as a generic. Regarding dissolution efficiency (DE), the ANOVA showed a significant difference between the products, so the Tukey test was applied, showing that only the generics A, F, G and H have the same DE as the reference drug.
Assuntos
Acetaminofen/farmacocinética , Medicamentos Genéricos , Solubilidade , Controle de QualidadeRESUMO
Solanum guaraniticum is a shrub belonging to the Solanaceae family popularly known in Brazil as jurubeba or false-jurubeba. The aim of this study was to evaluate the antioxidant activity of crude extract and chloroform, ethyl acetate and n-butanol fractions from its leaves, verifying the ability to remove reactive species and identify and quantify phenolic compounds. The ethyl acetate fraction showed the highest amount of total polyphenols (546.57 ± 2.35 mg gallic acid equivalent/g) and the lowest IC(50) (9.11 ± 0.75 µg/mL) by the DPPH method. Furthermore, the chloroform fraction presented the highest content of flavonoids (75.73 ± 0.34 mg rutin equivalents/g), tannins (56.03 ± 0.68 mg catechin equivalents/g) and alkaloids (10.79 ± 0.06 mg/g). This fraction was effective in the scavenging of reactive species by 2',7'-dichlorofluorescein diacetate assay, in addition to completely reducing protein carbonyl content and reducing lipid peroxidation at basal levels even at low concentrations. Chlorogenic, caffeic and rosmarinic acids were identified and quantified by HPLC/DAD. These results show that S. guaraniticum is rich in phenolic compounds and has potential as an antioxidant.