RESUMO
Plant extracts are complex mixtures that are difficult to characterize, and mass spectrometry is one of the main techniques currently used in dereplication processes. Fridericia chica is a species with medicinal uses in Latin American countries, used in the treatment of inflammatory and infectious diseases. Extracts of this plant species are characterized by the presence of anthocyanidins. In this study, using high-resolution mass spectrometry coupled with liquid chromatography, it was possible to determine the molecular formula of thirty-nine flavonoids. Fragmentation analysis, ultraviolet spectrum and nuclear magnetic resonance data allowed the partial characterization of the structures of these compounds. The spectral dataset allowed the identification of a series of flavones in addition to the desoxyanthocyanidins common in extracts of the species. The occurrence of some of the proposed structures is uncommon in extracts of species of the Bignoniaceae family, and they are reported for the first time in the extract of this species. Quantitative analyses of total flavonoids confirmed the high content of these constituents in the species, with 4.09 ± 0.34 mg/g of dry plant material. The extract under study showed low in vitro cytotoxicity with CC50 ≥ 296.7 ± 1.4 µg/mL for Vero, LLC-MK2 and MRC-5 cell lines. In antiviral activity assays, inhibition of the cytopathic effects of Dengue, Zika and Mayaro viruses was observed, with EC50 values ranging between 30.1 and 40.9 µg/mL. The best result was observed against the Mayaro virus, with an EC50 of 30.1 µg/mL.
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Bignoniaceae , Flavonas , Infecção por Zika virus , Zika virus , Antocianinas/análise , Antivirais/análise , Antivirais/farmacologia , Bignoniaceae/química , Flavonas/análise , Flavonas/farmacologia , Flavonoides/análise , Flavonoides/farmacologia , Espectrometria de Massas , Extratos Vegetais/química , Folhas de Planta/químicaRESUMO
Bisphosphonates are drugs used to treat bone disorders. The chronic use of bisphosphonates is associated with the occurrence of medication-related osteonecrosis of the jaw (MRONJ). Previous data reported the positive effects of Geranylgeraniol on different cell types treated with Bisphosphonates. Foregoing work done by our research group demonstrated the wound healing capacity of Fridericia chica (Bonpl.) L.G.Lohmann standardized ethanol extract. Herein in vitro cytoprotective synergistic effect of the association of F. chica extract associated with an enriched geranylgeraniol fraction on keratinocytes exposed to zoledronic acid is reported. An association of F. chica at 1 and 5 µg/mL with geranylgeraniol at 15 µg/mL, increased cell viability by 73.5% and 71.1%, respectively. This treatment did not increase tumor cells viability; whereas the clonogenic potential assessment showed that, the association with F. chica (5 µg/mL) reversed the effects of zoledronic acid on the cells. This study provides data for a potential treatment for MRONJ.
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Anthocyanidins are found in nature mainly as pelargonidin, cyanidin, peonidin, delphinidin, petunidin, and malvidin derivatives. These compounds are found free or as glycoside derivatives which are responsible for the color (red, blue, and violet) of some foods and are responsible for attracting seed dispersers. They are grouped into 3-hydroxyanthocyanidins, 3-deoxyanthocyanidins (3D-anth), and O-methylated anthocyanidins. A new method was developed and validated to quantify 3D-anth in plant-rich extracts. To test the new method, Arrabidaea chica Verlot was selected as it is widely used in folk medicine, and it is rich in 3D-anth. The new method was developed by HPLC-DAD and expressed 3D-anth as carajurin content. Carajurin was chosen as the reference standard due to its role as a biological marker for the antileishmanial activity for A. chica. The selected method used a silica-based phenyl column, a mobile phase composed of potassium dihydrogen phosphate buffer, acetonitrile, and methanol, in a gradient elution mode and detection at 480 nm. The method reliability was confirmed by verifying selectivity, linearity, precision, recovery, and robustness. This method contributes to quality control and development of a possible active pharmaceutical ingredient from A. chica as well as it can be used to evaluate 3D-anth in plant extracts with chemical ecology interest.
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Fridericia chica (Bonpl.) L.G. Lohmann (synonym Arrabidaea chica Verlot) is widely used in Brazilian folk medicine. Considering overcoming pitfalls of scaling up production of plant extracts, herein the effects of N2 atmosphere for extract spray-drying process is reported. Samples were monitored by in vitro antioxidant activity and microbiological evaluation. The drying atmosphere influenced 3-deoxyanthocyanines content when using air as atomizing gas, decreasing carajurin (37.5%) content with concomitant increase in luteolin yield (24.1%). Both drying processes preserved the pharmacological activity. In the cell migration test with HaCaT cells, the extract dried under air flow (5 µg/mL) promoted wound closure by 78% (12 hours) whereas the extract dried using N2 flow promoted 49% (12 hours), with 98% closure (12 hours) for the positive control. The antimicrobial evaluation for Staphylococcus aureus did not differ within drying atmospheres, with MIC (minimum inhibitory concentration) at 0.39 mg/mL. Therefore, the drying process reported herein did not interfere with the biological activity's outcome.
Assuntos
Bignoniaceae , Antioxidantes/farmacologia , Atmosfera , Extratos Vegetais/farmacologia , CicatrizaçãoRESUMO
Acknowledging the need of identifying new compounds for the treatment of leishmaniasis, this study aimed to evaluate, from in vitro trials, the activity of flavones from Arrabidaea chica against L. amazonensis. The chromatographic profiles of the hydroethanolic extract and a flavone-rich fraction (ACFF) from A. chica were determined by high-performance liquid chromatography coupled with a diode-array UV-Vis detector (HPLC-DAD-UV) and electrospray ionization mass spectrometry in tandem (LC-ESI-MS-MS). The flavones luteolin (1) and apigenin (2), isolated from chromatographic techniques and identified by Nuclear Magnetic Resonance of 1H and 13C, were also quantified in ACFF, showing 190.7 mg/g and apigenin 12.4 mg/g, respectively. The other flavones were identified by comparing their spectroscopic data with those of the literature. The in vitro activity was assayed against promastigotes and intramacrophagic amastigote forms of L. amazonensis. Cytotoxicity tests were performed with peritoneal macrophages of BALB/c mice. Nitrite quantification was performed with Griess reagent. Ultrastructural investigations were obtained by transmission electron microscopy. Anti-Leishmania assays indicated that the IC50 values for ACFF, apigenin, and luteolin were obtained at 40.42 ± 0.10 and 31.51 ± 1.13 µg/mL against promastigotes, respectively. ACFF and luteolin have concentration-dependent cytotoxicity. ACFF and luteolin also inhibited the intra-macrophagic parasite (IC50 3.575 ± 1.13 and 11.78 ± 1.24 µg/mL, respectively), with a selectivity index of 11.44 for ACFF. Promastigotes exposed to ACFF and luteolin exhibited ultrastructural changes, such as intense cytoplasm vacuolization and mitochondrial swelling. These findings data evidence the antileishmanial action of flavone-rich fractions of A. chica against L. amazonensis, encouraging further studies.
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INTRODUCTION: Osteonecrosis of the jaw is a condition associated with intraoral ulceration and bone necrosis induced by antiresorptive medications, such as zoledronic acid, a bisphosphonate. Previous data on Arrabidaea chica (H&B.) Verlot wound healing activity prompted the study reported herein on A. chica standardized hydro alcoholic extract in vitro cytoprotective activity data on epithelial and osteoblastic cells exposed to zoledronic acid (ZA). METHODS: Primary human gingival fibroblasts and murine pre-osteoblasts were treated with ZA 10 µM together with 5 or 10 µg.mL-1 A. chica extract for 24h and 48 h. At both times, cells were submitted to viability assay and caspase 3/7 activation evaluation. Statistical analysis used one-way ANOVA and p=0.05. RESULTS: In cell viability assay, a drastic damage effect of ZA appeared after 48 h in both epithelial (55.8%) and pre-osteoblastic cells (39.7%). When treated with ZA in combination with A. chica extract, cells showed higher viability values: 74.1%-82.3% for fibroblasts and 66% for pre-osteoblasts. Furthermore, the combined treatment presented lower caspase 3/7 activation in fibroblasts and pre-osteoblasts. CONCLUSION: At low concentrations, A. chica extract showed promising cytoprotective effects against ZA-induced damage actions; however, further in vitro and in vivo studies are required to establish the mechanism of action.
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Fridericia chica, Bignoniaceae, is a tropical tree-creeper used as a traditional remedy for a number of diseases, highlighting inflammation. Our objective was to corroborate the popular anti-inflammatory use of the hydroethanolic extract from the leaves (HEFc) and of its isolated 4',6,7-trihydroxy-5-methoxyflavone (5-O-methylscutellarein) [1], described here for the first time. Quantitative analysis indicated 8.77 ± 0.23 mg/g of this compound in the extract. Neither HEFc nor [1] was cytotoxic in vitro. In LPS-induced peritonitis in mice, oral pre-treatment with HEFc or [1] led to decreased leukocyte migration to the peritoneal cavity and a reduction in the concentrations of pro-inflammatory cytokines (TNFα and IL-1ß). Also, the anti-inflammatory cytokine IL-10 was enhanced following treatment with [1]. Overall, these results validate the traditional use of Fridericia chica as anti-inflammatory, and indicate that the compound 5-O-methylscutellarein may participate in this effect.
Assuntos
Anti-Inflamatórios/isolamento & purificação , Bignoniaceae/química , Flavonas/isolamento & purificação , Inflamação/tratamento farmacológico , Animais , Anti-Inflamatórios/farmacologia , Movimento Celular , Citocinas/análise , Citocinas/efeitos dos fármacos , Flavonas/farmacologia , Inflamação/induzido quimicamente , Leucócitos/citologia , Camundongos , Cavidade Peritoneal/patologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/químicaRESUMO
Advanced wound dressings capable of interacting with lesions and changing the wound microenvironment to improve healing are promising to increase the therapeutic efficacy of this class of biomaterials. Aiming at the production of bioactive wound dressings with the ability to control the wound microenvironment, biomaterials of three different chemical compositions, but with the same architecture, were produced and compared. Electrospinning was employed to build up a biomimetic extracellular matrix (ECM) layer consisting of poly(caprolactone) (PCL), 50/50 dl-lactide/glycolide copolymer (PDLG) and poly(l-lactide) (PLLA). As a post-treatment to broaden the bioactivity of the dressings, an alginate coating was applied to sheathe and functionalize the surface of the hydrophobic electrospun wound dressings, in combination with the extract of the plant Arrabidaea chica Verlot, known for its anti-inflammatory and healing promotion properties. Wettable bioactive structures capable to interact with media simulating lesion microenvironments, with tensile strength and elongation at break ranging respectively from 155 to 273â¯MPa and from 0.94 to 1.39% were obtained. In simulated exudative microenvironment, water vapor transmission rate (WVTR) values around 700â¯g/m2/day were observed, while water vapor permeability rates (WVPR) reached about 300â¯g/m2/day. In simulated dehydrated microenvironment, values of WVTR around 200â¯g/m2/day and WVPR around 175â¯g/m2/day were attained.
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Bandagens , Materiais Revestidos Biocompatíveis/farmacologia , Fenômenos Mecânicos , Cicatrização , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Liberação Controlada de Fármacos , Íons , Testes de Sensibilidade Microbiana , Permeabilidade , Extratos Vegetais/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Vapor , Termogravimetria , Fatores de Tempo , Água/química , Difração de Raios XRESUMO
Ultraviolet radiation (UVR) exposure causes various injurious effects to human skin by generating reactive oxygen species (ROS). Excessive ROS production can lead to oxidative stress which may damage cellular components like lipids and proteins and causing photoaging. The use of natural photochemopreventive agents with antioxidant properties is an important alternative to improve the effectiveness of sunscreens and reduce skin photodamage. A crude extract (CE) from the leaves of Arrabidaea chica underwent partition by a liquid-liquid method. The hexane fraction (FH), chloroform fraction (FC), and ethyl acetate fraction (FEA) were obtained. The antioxidant capacity of the CE, FH, FC, and FEA was studied in a cell-free system using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and the xanthine/luminol/xanthine oxidase system. The FC had the best antioxidant activity. We also evaluated the photochemoprotective effect of A. chica in protecting L929 fibroblasts against UV-A- and UV-B-induced cell damage. A. chica inhibited the extended production of ROS up to 3h. Posttreatment with the CE and FC attenuated UV-induced cell damage through scavenging mechanisms, including the quenching of intracellular ROS and mitochondrial O2- and preventing lipid peroxidation. These results suggest that A. chica may be a promising non-sunscreen photoprotector that can improve the effectiveness of commercial sunscreens.
Assuntos
Bignoniaceae/química , Sequestradores de Radicais Livres/química , Peroxidação de Lipídeos/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Raios Ultravioleta , Bignoniaceae/metabolismo , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Sequestradores de Radicais Livres/farmacologia , Humanos , Peroxidação de Lipídeos/efeitos da radiação , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Substâncias Protetoras/química , Espécies Reativas de Oxigênio/metabolismo , Superóxidos/metabolismoRESUMO
INTRODUCTION: Oral mucositis is an iatrogenic condition of erythematous inflammatory changes which tends to occur on buccal and labial surfaces, the ventral surface of the tongue, the floor of the mouth and the soft palate of patients receiving chemotherapy. This protocol of ongoing randomised parallel group clinical trial aims to access the therapeutic effect of an herbal gel containing 2.5% Arrabidaea chica Verlot standardised extract on oral mucositis in patients with head and neck cancer compared with low-level laser therapy. METHODS AND ANALYSIS: Patients with head and neck cancer held at Clinics Hospital of University of Campinas, Sao Paulo, who develop early signs/symptoms of oral mucositis are eligible. Baseline characteristics of participants include oral mucositis grade and quality of life assessments. Enrolment started in November 2017 with allocation of patients to one of the study groups by means of randomisation. Patients will be treated either with Arrabidaea chica or laser until wound healing. Monitoring includes daily assessment of mucositis grade and diameter measurement by photographs and millimetre periodontal probe. Treatments will be concluded once mucositis is healed. A blinded assessor will evaluate mucositis cure after referred by the study team. At this point, the gel tube will be weighed to indirectly assess patient's compliance. At close-out, data will be analysed by a blinded researcher following the procedures described in the statistical analyses. ETHICS AND DISSEMINATION: This clinical trial was approved by the ethics committee of research in humans at the Faculty of Medical Sciences of University of Campinas (report no. 1,613,563/2016). Results from this trial will be communicated in peer-reviewed publications and scientific presentations. TRIAL REGISTRATION NUMBER: RBR-5×4397.
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Protocolos Antineoplásicos/normas , Bignoniaceae , Terapia com Luz de Baixa Intensidade/métodos , Extratos Vegetais/uso terapêutico , Estomatite/tratamento farmacológico , Feminino , Neoplasias de Cabeça e Pescoço/complicações , Humanos , Masculino , Ensaios Clínicos Controlados Aleatórios como AssuntoRESUMO
BACKGROUND: Approximately 6-7 million people are infected with Trypanosoma cruzi, the etiological agent of Chagas' disease. Only two therapeutic compounds have been found to be useful against this disease: nifurtimox and benznidazole. These drugs have been effective in the acute phase of the disease but less effective in the chronic phase; they also have many side effects. Thus, the search for new compounds with trypanocidal action is necessary. Natural products can be the source of many important substances for the development of drugs to treat this infection. The present study evaluated the biological activity of an extract and fractions of Arrabidaea chica against T. cruzi and observed morphological and ultrastructural characteristics of parasites exposed to the isolated compound pheophorbide a. METHODS: The crude hydroethanolic extract of A. chica was prepared. Fractions were obtained by partition and separated by liquid chromatography. RESULTS: We observed a progressive increase in activity against epimastigote, trypomastigote, and amastigote forms of the parasite over the course of the fractionation process. Interestingly, we isolated a compound known as a photosensitizer that is used in photodynamic therapy. This method of treatment involving a photosensitizer, activation light and molecular oxygen is of great importance due to its selectivity. Pheophorbide a had activity against the protozoan in the presence of light and caused morphological and ultrastructural changes, demonstrating its potential in photodynamic therapy. CONCLUSIONS: Based on the ability of pheophorbide a to eliminate bloodstream forms of T. cruzi, we suggest its use in blood banks for hemoprophylaxis.
Assuntos
Clorofila/análogos & derivados , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/farmacologia , Extratos Vegetais/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Linhagem Celular , Clorofila/farmacologia , HaplorrinosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Arrabidaea chica (Bignoniacea) has been used in popular medicine in Brazil to treat inflammation, skin diseases and leukemia. This work aimed to investigate the anti-inflammatory and antitumoral activities of the A. chica aqueous (AE) and ethanol (EE) extracts. MATERIALS AND METHODS: The murine sponge model was used to evaluate the anti-inflammatory and antiangiogenic activities of AE and EE. Accumulation of neutrophil and macrophage in the implants were determined by assaying myeloperoxidase and N-acetyl-glucosaminidase activities and the neovascularization evaluated by the amount of hemoglobin present in the implant using the Drabkin method. The antitumoral activity was evaluated using the MTT colorimetric method against Jurkat, HL60 and MCF-7 cells. Semi-purified fractions F1-F4 from the EE extract were obtained by a liquid-liquid solvent extraction method and their in vitro anti-proliferative effects were also investigated. RESULTS: Ethanol and aqueous extracts of A. chica decreased neutrophil accumulation and hemoglobin content in the sponge implants without altering the level of cytokines (IL-2, IL- 4, IL-5, IFN-γ, TNF-α and VEGF) and the albumin/globulin ratio in the serum of treated animals. There was no sign of toxicity (clinical, laboratory or histopathology). The ethanol extract presented antiproliferative activity (IC50 21.5-36.3 µg/mL) against HL60 and Jurkat cell lineages and proapoptotic activity at 50 µg/mL in HL60 cells. The fraction F1 also demonstrated significant antiproliferative activity (IC50 38.5 µg/mL) and proapoptotic activity against HL60 cells in a dose dependent manner. CONCLUSIONS: Aqueous and ethanol extracts of A. chica attenuate the inflammatory and angiogenic components of the subcutaneous fibrovascular tissue induced by the synthetic matrix in mice. In addition, the ethanol extract from Arrabidaea chica and its fraction F1 presented in vitro antiproliferative activity and could be useful for developing potential chemopreventive substances.
Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Bignoniaceae , Neovascularização Patológica/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Bignoniaceae/química , Proliferação de Células/efeitos dos fármacos , Citocinas/biossíntese , Células HL-60/efeitos dos fármacos , Humanos , Células Jurkat/efeitos dos fármacos , Células MCF-7/efeitos dos fármacos , Masculino , Camundongos , Folhas de Planta/química , Fator de Necrose Tumoral alfa/biossíntese , Fator A de Crescimento do Endotélio Vascular/biossínteseRESUMO
Natural products using plants have received considerable attention because of their potential to treat various diseases. Arrabidaea chica (Humb. & Bonpl.) B. Verlot is a native tropical American vine with healing properties employed in folk medicine for wound healing, inflammation, and gastrointestinal colic. Applying nanotechnology to plant extracts has revealed an advantageous strategy for herbal drugs considering the numerous features that nanostructured systems offer, including solubility, bioavailability, and pharmacological activity enhancement. The present study reports the preparation and characterization of chitosan-sodium tripolyphosphate nanoparticles (NPs) charged with A. chica standardized extract (AcE). Particle size and zeta potential were measured using a Zetasizer Nano ZS. The NP morphological characteristics were observed using scanning electron microscopy. Our studies indicated that the chitosan/sodium tripolyphosphate mass ratio of 5 and volume ratio of 10 were found to be the best condition to achieve the lowest NP sizes, with an average hydrodynamic diameter of 150±13 nm and a zeta potential of +45±2 mV. Particle size decreased with AcE addition (60±10.2 nm), suggesting an interaction between the extract's composition and polymers. The NP biocompatibility was evaluated using human skin fibroblasts. AcE-NP demonstrated capability of maintaining cell viability at the lowest concentrations tested, stimulating cell proliferation at higher concentrations. Antiulcerogenic activity of AcE-NP was also evaluated with an acute gastric ulcer experimental model induced by ethanol and indomethacin. NPs loaded with A. chica extract reduced the ulcerative lesion index using lower doses compared with the free extract, suggesting that extract encapsulation in chitosan NPs allowed for a dose reduction for a gastroprotective effect. The AcE encapsulation offers an approach for further application of the A. chica extract that could be considered a potential candidate for ulcer-healing pharmaceutical systems.
Assuntos
Bignoniaceae/química , Quitosana/química , Portadores de Fármacos/química , Nanopartículas/química , Extratos Vegetais/farmacologia , Polifosfatos/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Modelos Animais de Doenças , Etanol/efeitos adversos , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Humanos , Indometacina/efeitos adversos , Masculino , Tamanho da Partícula , Compostos Fitoquímicos , Ratos , Ratos Wistar , Pele/citologia , Pele/efeitos dos fármacos , Pele/metabolismo , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológicoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Arrabidaea chica (Bignoniaceae) is a vine native to the Amazon Rainforest, popularly known as "crajiru" and whose infusion and decoction of the leaves are used to treat diseases such as gastric ulcers, inflammations, infections, anemia, herpes, jaundice among others. It is also used as a natural dye. This work aimed to evaluate the in vitro and in vivo toxicity, antimicrobial activity including analysis of chemical constitution of the hydroethanolic extract of the leaves of Arrabidaea chica (HEAc). MATERIALS AND METHODS: Acute and subchronic toxicity of HEAc was evaluated in mice and rats, respectively, and by Alamar blue (cytotoxicity assay) using CHO-K1 cells. Antimicrobial activity of HEAc was tested by broth microdilution method using a panel of bacteria and yeast of clinical interest. The preliminary phytochemical analysis of HEAc was performed by electrospray ionization mass spectrometry [ESI(+)-MS]. Secondary metabolites were quantified by colorimetric methods. RESULTS: When administered in vivo at doses up to 3000 mg/kg v.o., HEAc did not cause any signs and symptoms of acute toxicity in mice and no cytotoxicity in CHO-K1 cells. Administration for 30 days caused leukocytosis (200 mg/kg) and reversible reductions in non-dose dependent of body weight, total weight gain and feed intake in rats given 200mg/kg and 500 mg/kg of HEAc, but were not accompanied by behavioral and clinical changes (laboratory and histopathological) that may have demonstrated evidences of subchronic toxicity HEAc demonstrated a pronounced activity against Helicobacter pylori (MIC=12.5 µg/mL) and moderate activity against Enterococcus faecalis (MIC=100 µg/mL) in broth microdilution. Preliminary phytochemical analysis of HEAc by colorimetric methods revealed that mainly the presence of phenolic compounds (16.6%), especially flavones and flavonols (4.02%). [ESI(+)-MS] fingerprint analyses of HEAc revealed the presence of 3-deoxyanthocyanidins and kaempferol. CONCLUSION: Our data provide evidence that HEAc is safe and can be useful in infections related to Helicobacter pylori and Enterococcus faecalis. Phytochemical analysis revealed the predominant presence of flavones and flavonols, possibly involved in the antimicrobial action of HEAc.
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Antibacterianos/farmacologia , Bignoniaceae , Extratos Vegetais/farmacologia , Animais , Antibacterianos/toxicidade , Bactérias/efeitos dos fármacos , Células CHO , Cricetulus , Enterococcus faecalis/efeitos dos fármacos , Etanol/química , Feminino , Helicobacter pylori/efeitos dos fármacos , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Extratos Vegetais/toxicidade , Folhas de Planta , Ratos , Ratos Wistar , Solventes/química , Água/químicaRESUMO
BACKGROUND: Folk medicine uses preparations of Arrabidaea chica (pariri) leaves to treat various liver pathologies. We evaluated the effects of the hydroethanolic extract of these leaves (CHEE) on an in vivo model of liver intoxication. MATERIALS AND METHODS: Different groups of rats were treated orally for 7 days with CHEE at doses of 300, 500 or 600 mg/kg or silymarin at 35 mg/kg. The control group received only 0.5 ml of distilled water. After 7 days of treatment, both the groups received CCl(4), and activities of glutamic pyruvic transaminase (GPT), glutamic oxaloacetic transaminase (GOT) and bilirubin level were assessed. The ability of CHEE to suppress hepatic injury triggered by CCl(4) was evaluated based on suppression (%) of activities of GOT, GPT and bilirubin levels. RESULTS: The chromatograms of the CHEE obtained at 330 and 400 nm show features of two main classes of secondary metabolites: quinones and flavonoids. The administration of 300, 500 or 600 mg/kg of CHEE resulted in the reduction of GPT levels by 85.34%, 88.59% and 93.72%, respectively. The suppression of GOT levels was 56.86%, 65.27% and 68.95%, respectively, and that of plasma bilirubin was 83.81%, 83.12% and 84.14%, respectively. These results demonstrate the protective character of CHEE and its ability to maintain the functional integrity of hepatic cells. CONCLUSIONS: The results obtained are possibly due to the presence of quinones and flavonoids in A. chica CHEE, both detected using high performance liquid chromatography.
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The aim of this study was to investigate the effect of Arrabidaea chica (Humb. & Bonpl.) B. Verl., Bignoniaceae, extracts on Ehrlich solid tumor development in Swiss mice. Leaves of A. chica were extracted with two distinct solvents, ethanol and water. The phytochemical analysis of the extracts indicated different classes of secondary metabolites like as anthocyanidins, flavonoids, tannins and saponins. Ethanol (EE) and aqueous (AE) extracts at 30 mg/kg reduced the development of Ehrlich solid tumor after ten days of oral treatment. The EE group presented increase in neutrophil count, α1 and β globulin values, and decrease of α2 globulin values. Furthermore, EE reduced the percentage of CD4+ T cells in blood but did not alter the percentage of inflammatory mononuclear cells associated with tumor suggesting a direct action of EE on tumor cells. Reduced tumor development observed in AE group was accompanied by a lower percentage of CD4+ T lymphocytes in blood. At the tumor microenvironment, this treatment decreased the percentage of CD3+ T cells, especially due to a reduction of CD8+ T subpopulation and NK cells. The antitumor activity presented by the AE is possibly related to an anti-inflammatory activity. None of the extracts produced toxic effects in animals. In conclusion, the ethanol and aqueous extracts of A. chica have immunomodulatory and antitumor activities attributed to the presence of flavonoids, such as kaempferol. These effects appear to be related to different mechanisms of action for each extract. This study demonstrates the potential of A. chica as an antitumor agent confirming its use in traditional popular medicine.
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Arrabidaea chica (Humb. & Bonpl.) B. Verlt. é uma Bignoniaceae amplamente utilizada na medicina popular como anti-inflamatório e adstringente, e para várias doenças como cólicas intestinais, diarréias, anemias e enfermidades da pele. Devido as suas propriedades biológicas e a produção de corante a espécie passou a ser utilizada pela indústria cosmética. A utilização de produtos naturais de origem vegetal implica no controle de qualidade farmacobotânico e em ensaios de pureza que compõem as especificações técnicas da espécie. Para isso foi realizada a descrição anatômica das folhas jovens e maduras de A. chica a partir de observações realizadas ao microscópio óptico, a partir de cortes histológicos. As folhas são hipoestomáticas e dorsiventrais com mesofilo heterogêneo. No pecíolo, a epiderme é uniestratificada contendo tricomas e dotada de cutícula delgada. Os testes farmacopéicos incluíram a determinação da distribuição granulométrica do pó da planta, determinação do teor de umidade e de cinzas totais, além da abordagem fitoquímica da tintura, visando estabelecer parâmetros para seu controle de qualidade.
Arrabidaea chica (Humb. & Bonpl.) B. Verlt. is a Bignoniaceae widely used in the popular medicine as anti-inflammatory and astringent agent, and for some illnesses as intestinal colic, diarrhoeas, anaemia and diseases of the skin. Its biological properties and dye biosynthesis lead the species to be used in the cosmetic industry. The use of natural products of vegetal origin implies in pharmacognostic quality control and purity assays that compose the technical specifications of the material. Therefore, the anatomical description of mature and young leaves of A. chica was carried through the use of optic microscopy on histological preparations. The leaves are hipostomatic and dorsiventral with heterogeneous mesophile. In petiole, the epidermis is unistratified, it contains trachoma and it is endowed with thin cuticle. The pharmacopoeia assays included the determination of the grain size distribution of the plant drug, the determination of humidity and the total ashes, beyond the phytochemistry approach of tincture, to establish parameters for its quality control.
RESUMO
Amazônia brasileira oferece um apreciável potencial de plantas com propriedades terapêuticas, embora a maioria seja pouco conhecida. Dessa forma, com o objetivo de verificar a potencialidade nutricional de ervas medicinais, determinou-se a concentração de Ca, Mg, Fe, Cu e Zn nas folhas e nos chás das espécies: Piper callosum Ruiz & Pav., Piperaceae, Mikania lindleyana DC., Asteraceae e Arrabidaea chica (Humb. & Bonpl.) B. Verl., Bignoniaceae. As amostras de plantas depois de terem sido processadas, foram submetidas a digestão e em seguida realizada as leituras dos metais em um espectrofotômetro de absorção atômica. Para o chá de Arrabidaea chica foram detectados teores de Ca (6955 a 20058 mg/L), Mg (2390 a 3094 mg/L) e Fe (40 a 61 mg/L). Para o chá de Mikania lindleyana além da presença de altos valores de Ca (17722 a 22336 mg/L), Mg (4531 a 9370 mg/L) e Fe (20 a 87 mg/L) foram encontrados de 7 a 16 mg/L de Cu e 9 a 41 mg/L de Zn. O chá do Piper callosum apresentou em média 2036 a 4344 mg/L de Ca, 618 a 4023 mg/L de Mg e 39 a 60 mg/L de Fe. Comparando-se os resultados dos minerais com os valores recomendados pela Organização Mundial da Saúde, conclui-se que os metais presentes nos chás das plantas poderiam contribuir na complementação das dietas alimentares das pessoas que as utilizam.
The Amazonian Brazilian offers an appreciable potential of plants with therapeutic properties, although most are little known. In this way, with the objective of verifying the potentiality nutritional of medicinal herbs, a work was developed to determine the concentration of Ca, Mg, Fe, Cu and Zn in the leaves and in the teas of these species: Piper callosum Ruiz & Pav., Piperaceae, Mikania lindleyana DC., Asteraceae e Arrabidaea chica (Humb. & Bonpl.) B. Verl., Bignoniaceae. After the plants samples have been processed, they were submitted to digestion and soon afterwards the metals were analyzed in an spectrophotometer of Atomic Absorption. The results showed the follow yields: for the tea of Arrabidaea chica Ca were detected (6955 to 20058 mg/L), Mg (2390 to 3094 mg/L) and Fe (40 to 61 mg/L). For the tea of Mikania lindleyana besides the presence of high values of Ca (17722 to 22336 mg/L), Mg (4531 to 9370 mg/L) and Fe (20 to 87 mg/L) they were found from 7 to 16 mg/L of Cu and 9 to 41 mg/L of Zn. The tea of the Piper callosum presented 2036 to 4344 mg/L of Ca, 618 to 4023 mg/L of Mg and 39 to 60 mg/L of Fe. Being compared the results of the minerals with the values recommended by the Health World Organization, is possible that the present metals in the teas of the plants could contribute in the complementation of the people's alimentary diets that use these medicinal plants.
RESUMO
O estudo investigou o efeito antiinflamatório do extrato aquoso da Arrabidaea chica (Humb. & Bonpl.) B. Verl., Bignoniaceae, popularmente conhecida como "crajiru", sobre o edema induzido por venenos de serpentes amazônicas dos gêneros Brothrops e Crotalus, em camundongos albinos, por via oral, intraperitoneal e subcutânea. O efeito anti-edematogênico foi avaliado pela medição do diâmetro dos coxins das patas posteriores, sendo medidos as 1, 3, 6, 12 e 24 horas, para B. atrox e 1, 3 e 6 horas para Crotalus durissus ruruima, e também avaliado por histopatologia. O estudo mostrou que o efeito inibitório do extrato aquoso para o gênero Bothrops, pelas vias subcutânea e intraperitoneal (12 horas) foi de 55,87 por cento e 65,70 por cento, respectivamente. Para o gênero Crotalus o efeito inibitório do extrato pela via subcutânea após 3 horas foi de 33,55 por cento e após 6 horas de 79,81 por cento. Pela via intraperitoneal após 3 horas foi de 48,02 por cento e após 6 horas de 92,52 por cento. Na análise histopatológica, o infiltrado de granulócitos e a miocitólise foram os efeitos inflamatórios inibidos mais significativamente. Os resultados sugerem a presença no extrato aquoso de A. chica de substâncias com atividade inibitória sobre os efeitos inflamatórios dos venenos das serpentes Bothrops atrox e Crotalus durissus ruruima.
The study investigated the anti-inflammatory effects of the aqueous extract (EAq), the Arrabidaea chica (Humb. & Bonpl.) B. Verl., Bignoniaceae, known as the "crajiru", tested on the paw oedema induced in inflammatory process by venoms Amazon snakes from the Bothrops and Crotalus species, on albino mice. This process was done by an oral, intraperitoneal and subcutaneous way. The cushions thickness was measured at time breaks of 1, 3, 6, 12 and 24 hours, Bothrops genus and 1, 3 and 6 hours, Crotalus genus, and a histopathologic analysis was made. The Bothrops genus, was used as an inhibitory effect for the subcutaneous and intraperitoneal way (12 hours), and it had an inhibition of 55.87 percent and 65.70 percent, respectively. For the Crotalus genus, the inhibitory effect for the subcutaneous way after 3 hours was the 33.55 percent and 79.81 percent, after 6 hours. The intraperitoneal way affect after 3 hours had an inhibition of 48.02 percent and 92.52 percent after 6 hours. For the histopathological analysis, the leucocytes infiltration and the miocitolisis were the most expressive parameters and thus inhibited. The results suggest the presence of active principles with anti-inflammatory effects.
RESUMO
Arrabidaea chica (HBK.) Verlot (Bignoniaceae) vernacular name "Pariri", is a climbing shrub, widespread from South Mexico to Guyana and central Brazil and is traditionally indicated to treat symptoms of inflammations and skin affections. Its ethanol extract was chemically investigated and tested against yeasts and dermatophytic fungi. The trypanocidal activity of the same extract was also evaluated. This work reports the isolation of three flavonoids, the total growth inhibition of Trichophyton mentagrophytes and a significant trypanocidal effect of the ethanol extract and its fractions. No relevant acute toxicity was detected even at a dose of 1000 mg/kg.
Arrabidaea chica (HBK.) Verlot (Bignoniaceae) popularmente, "Pariri", é um arbusto escandente, distribuído do sul do México até a Guiana e Brasil central e é tradicionalmente indicado para tratar sintomas de inflamações e afecções da pele. Seu extrato etanólico foi quimicamente investigado e testado contra leveduras e fungos dermatófitos. A atividade tripanocida do mesmo extrato foi também avaliada. Este trabalho reporta o isolamento de três flavonóides, a inibição total do crescimento de Trichophyton mentagrophytes e um significante efeito tripanocida do extrato etanólico e de suas frações. Não foi detectada qualquer toxicidade aguda relevante, mesmo a uma dose de 1000 mg/kg.