RESUMO
Different communities around the world traditionally use Bidens pilosa L. for medicinal purposes, mainly for its anti-inflammatory, antinociceptive, and antioxidant properties; it is used as an ingredient in teas or herbal medicines for the treatment of pain, inflammation, and immunological disorders. Several studies have been conducted that prove the immunomodulatory properties of this plant; however, it is not known whether the immunomodulatory properties of B. pilosa are mediated by its ability to modulate antigen-presenting cells (APCs) such as macrophages (MØs) and dendritic cells (DCs) (through polarization or the maturation state, respectively). Different polar and non-polar extracts and fractions were prepared from the aerial part of B. pilosa. Their cytotoxic and immunomodulatory effects were first tested on human peripheral blood mononuclear cells (PBMCs) and phytohemagglutinin (PHA)-stimulated PBMCs, respectively, via an MTT assay. Then, the non-cytotoxic plant extracts and fractions that showed the highest immunomodulatory activity were selected to evaluate their effects on human MØ polarization and DC maturation (cell surface phenotype and cytokine secretion) through multiparametric flow cytometry. Finally, the chemical compounds of the B. pilosa extract that showed the most significant immunomodulatory effects on human APCs were identified using gas chromatography coupled with mass spectrometry. The petroleum ether extract and the ethyl acetate and hydroalcoholic fractions obtained from B. pilosa showed low cytotoxicity and modulated the PHA-stimulated proliferation of PBMCs. Furthermore, the B. pilosa petroleum ether extract induced M2 polarization or a hybrid M1/M2 phenotype in MØs and a semi-mature status in DCs, regardless of exposure to a maturation stimulus. The immunomodulatory activity of the non-polar (petroleum ether) extract of B. pilosa on human PBMC proliferation, M2 polarization of MØs, and semi-mature status in DCs might be attributed to the low-medium polarity components in the extract, such as phytosterol terpenes and fatty acid esters.
Assuntos
Bidens , Humanos , Leucócitos Mononucleares , Cromatografia Gasosa-Espectrometria de Massas , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Anti-Inflamatórios/farmacologia , Solventes , Macrófagos , Fenótipo , Células DendríticasRESUMO
PURPOSE: To assess the effect of a mucoadhesive herbal medicine containing curcuminoids and a glycerinated extract of Bidens pilosa L. (FITOPROT) in association with photobiomodulation (PBM) therapy and a Preventive Oral Care Program (POCP) compared to PBM and POCP in the treatment of radiotherapy (RT)-induced oral mucositis (ROM) and in the quality of life of these patients. METHODS: A double-blind clinical trial was performed with head and neck cancer patients undergoing RT or chemoradiotherapy. Participants were randomized into two groups: Group 1 (n=27): PBM and POCP; and Group 2 (n=25): PBM, POCP and FITOPROT. The PBM protocol was daily irradiation, 660 nm, 25mW, 0.25 J/point from the first until the last day of RT. The FITOPROT was used as mouthwash twice a day. ROM was evaluated based on the scales of the World Health Organization and National Cancer Institute. The quality of life was evaluated using the University of Washington Questionnaire, OHIP-14 and Patient-Reported Oral Mucositis Symptom Scale. The MMAS-8 questionnaire was used to evaluated the adherence to POCP and FITOPROT. Data were collected at baseline, 7th, 14th, 21st, and 30th RT sessions. RESULTS: No statistical differences were found between the groups for the ROM evaluation. Both groups experienced worsening of the quality of life during the RT. No statistically significant differences between groups were observed for any of the instruments evaluated. CONCLUSION: The results suggest that PBM associated with FITOPROT and POCP control the severity of ROM and stabilize the QoL of patients with head and neck cancer. TRIAL REGISTRATION: Brazilian Registry of Clinical Trials (ReBEC-RBR-9vddmr; UTN code: U1111-1193-2066), registered in August 8th, 2017.
Assuntos
Bidens , Neoplasias de Cabeça e Pescoço , Terapia com Luz de Baixa Intensidade , Estomatite , Humanos , Qualidade de Vida , Curcuma , Estomatite/tratamento farmacológico , Estomatite/etiologia , Estomatite/prevenção & controle , Neoplasias de Cabeça e Pescoço/tratamento farmacológico , Neoplasias de Cabeça e Pescoço/radioterapia , Extratos Vegetais/uso terapêutico , Terapia com Luz de Baixa Intensidade/métodosRESUMO
Background: Given the chemical richness of medicinal plants ( Bidens pilosa L. and Croton floccosus) in Ecuador, they are considered the natural source of numerous medicines. Methods: The leaves were dried at 40°C and 50°C and the extracts were characterized by means of phytochemical screening, verifying the presence of secondary metabolites such as alkaloids, reducing sugars, phenols, flavonoids, tannins and saponins. Three extraction processes were carried out, with two solvents of different polarities: hexane and ethanol. The extraction methods that were applied to the leaves of the plants were Soxhlet, ultrasonic bath and maceration, the latter two at room temperature and Soxhlet at the boiling temperature of the solvent. Determination of the total content of phenols and flavonoids is carried out using the Follin-Ciocalteau colorimetric reaction, Quercetin standard, Aluminum Chloride solution measured with a UV-Vis spectrophotometer. The antioxidant activity was performed with the DPPH radical and measured with the same equipment. Results: The highest content of total phenols obtained by employing the Soxhlet method for extraction when the material was dried at 50°C was 48.609 ± 0.370 mg GAE/g of dry sample for Bidens pilosa L. while in the case of Croton floccosus it was 128.212 ± 0.601 mg GAE/g of dry sample obtained from the extraction by means of maceration. Finally, the antioxidant activity against the 1.1-diphenyl-2-picryl-hydrazyl radical was determined, and it was found that the Bidens pilosa L. species performed better and responded better to the test, with an IC 50 value of 239.33 µg/mL, than Croton floccosus (IC 50 of 644.125 µg/mL). Conclusions: The following preliminary phytochemical study of the Bidens pilosa L. and Croton floccosus plants provided important information on the content of secondary metabolites and response to the DPPH radical reported for the first time in Ecuador, which may be future use for medicinal application.
Assuntos
Asteraceae , Bidens , Croton , Euphorbiaceae , Antioxidantes , Extratos Vegetais/farmacologia , Compostos Fitoquímicos , Flavonoides/química , FenóisRESUMO
Plant species with allelopathic effects against weeds have emerged as a potential strategy for the development of ecologically friendly bioherbicides. In this study, the allelopathic effects of the plant species Dipteryx lacunifera Ducke, Ricinus communis L., Piper tuberculatum Jacq., and Jatropha gossypiifolia L. on the weed Bidens bipinnata L. were investigated. In vitro bioassays revealed that aqueous extracts of selected plant species were able to inhibit seed germination and seedling growth of B. bipinnata, highlighting the strongest allelopathic effect evidenced by R. communis. The phytotoxicity of the aqueous extracts was evaluated in pot experiments, which indicated that the foliar application of R. communis and P. tuberculatum extracts on B. bipinnata plants caused yellowing of leaves, affecting the chlorophyll content and reducing growth. The discrimination of the plant extracts by attenuated total reflectance Fourier transform mid-infrared (ATR FT-MIR) spectroscopy combined with principal component analysis (PCA) indicated the presence of allelochemical compounds, such as phenolics and terpenoids, which may be associated with allelopathic activity. Overall, this study provides valuable information about the substantial allelopathic inhibitory effects of the plant species R. communis and P. tuberculatum on the weed B. bipinnata, which may be used for the development of eco-friendly bioherbicides.
Assuntos
Alelopatia , Bidens , Herbicidas , Bidens/efeitos dos fármacos , Germinação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Daninhas/efeitos dos fármacosRESUMO
Select herbicides with different mechanism of action is a satisfactory option for resistant weed control. Then, the present work aimed to study the efficiency of different herbicides and their mixtures on Bidens pilosa (blackjack) and Euphorbia heterophylla (wild poinsettia) biotypes, resistant to ALS herbicides in two development stages. The trials we arranged in a completely randomized design with four replications. The treatments tested were (g a.i/a.e ha-1): imazethapyr at 70 and 140 (WG formulation) + 1.0% Assist; imazethapyr at 57.6 and 72 (SL formulation) + 1.0% Assist; imazapic + imazethapyr at 56 and 70 + 1.0% Assist; glyphosate + imazethapyr (596); saflufenacil + glyphosate at 35 + 720 + 0.5% Dash in tank mix, glyphosate at 720 and, a control without herbicide application. Control efficiency was evaluated, as well as dry matter accumulation at the end of the studies. Plants of both species were more susceptible to herbicides at the early stage of development (2 to 4 leaves). The treatments with saflufenacil + glyphosate, (imazethapyr + glyphosate) and glyphosate promoted the best controls, regardless of the species studied and the application stage. The mixture with saflufenacil provided the highest control speed, and the mixture (imazethapyr + glyphosate) was less efficient among three excellent treatments when applied to plants in the 4-6 leaf stage. The treatments (imazethapyr, in both formulations) and (imazethapyr + imazapic) were ineffective in controlling the studied biotypes, regardless of dose and developmental stage studied.
Assuntos
Acetolactato Sintase , Euphorbia , Bidens , Resistência a Herbicidas , Controle de Plantas Daninhas , HerbicidasRESUMO
BACKGROUND: Oral mucositis (OM) is the significant complication of radio/chemotherapy treatment. This study evaluated the safety and efficacy of a mucoadhesive phytomedication containing curcuminoids and Bidens pilosa L. (FITOPROT) in the prevention/treatment of OM. METHODS: Sixty-two patients were randomized into the group's intervention and placebo. Adverse effect assessment, OM grading, pain, and saliva collection were carried at the 1st, 15th, 21st, and final of radiotherapy (RT). Inflammatory salivary mediators were measured. RESULTS: FITOPROT decreased the severity of OM from the 15th to the final RT, while the placebo showed an increase in the severity (p < 0.05). Intervention group had a lower number of patients with ulcerated OM at the final RT (p < 0.05). Phytomedication prevented increases of IL-8 levels and reduced the salivary nitrite during RT. CONCLUSIONS: FITOPROT does not promote adverse effects, it appears to be effective at reducing the severity of OM, and it controls the concentration of pro-inflammatory mediators.
Assuntos
Bidens , Neoplasias de Cabeça e Pescoço , Estomatite , Quimiorradioterapia , Diarileptanoides/uso terapêutico , Método Duplo-Cego , Humanos , Estomatite/etiologia , Estomatite/prevenção & controleRESUMO
FITOPROT, which contains curcuminoids and Bidens pilosa L. extract, is an innovative mucoadhesive formulation indicated for the topical treatment of chemoradiotherapy-induced oral mucositis (OM) in patients with advanced and visible oral squamous cell carcinoma. The formulation is used as a mouthwash directly on tumor tissue of patients with advanced neoplasms, without triggering cancer cell proliferation or tumor invasiveness. Thus, the aim of this study was to evaluate the biological effects of FITOPROT on an oral squamous cell carcinoma cell line (SCC-4). The viability of SCC-4 cells was assessed after exposure to FITOPROT using MTT reduction assay. The effects of the mucoadhesive formulation on cell cycle progression and cell death parameters were evaluated using flow cytometry. In addition, the inflammatory profile of the tumor cells was evaluated using the cytometric bead array (CBA) assay. FITOPROT promoted a concentration-dependent decrease in cell viability and cell cycle arrest at the G2/M phase (p < 0.05). Mitochondrial membrane potential was also altered after exposure to the formulation (p < 0.05), in parallel with a reduction in VEGF and IL-8 production (p = 0.01 and p = 0.05, respectively). In summary, the results indicate that FITOPROT reduces SCC-4 cell viability, promotes cell cycle arrest, modulates mitochondrial membrane potential, and exhibits antiangiogenic and anti-inflammatory properties, thus indicating its potential for topical use in patients with OM and visible tumors in the mouth.
Assuntos
Bidens , Carcinoma de Células Escamosas , Neoplasias Bucais , Apoptose , Carcinoma de Células Escamosas/tratamento farmacológico , Linhagem Celular , Proliferação de Células , Diarileptanoides , Humanos , Neoplasias Bucais/tratamento farmacológicoRESUMO
Cyclic imides belong to a well-known class of organic compounds with various biological activities, promoting a great interest in compounds with this functional group. Due to the structural complexity of some molecules and their spectra, it is necessary to use several spectrometric methods associated with auxiliary tools, such as the theoretical calculation for the structural elucidation of complex structures. In this work, the synthesis of epoxy derivatives of 5-methylhexahydroisoindole-1,3-diones was carried out in five steps. Diels-Alder reaction of isoprene and maleic anhydride followed by reaction with m-anisidine afforded the amide (2). Esterification of amide (2) with methanol in the presence of sulfuric acid provided the ester (3) that cyclized in situ to give imides 4 and 4-ent. Epoxidation of 4 and 4-ent with meta-chloroperbenzoic acid (MCPBA) afforded 5a and 5b. The diastereomers were separated by silica gel flash column chromatography, and their structures were determined by analyses of the spectrometric methods. Their structures were confirmed by matching the calculated 1H and 13C NMR chemical shifts of (5a and 5b) with the experimental data of the diastereomers using MAE, CP3, and DP4 statistical analyses. Biological assays were carried out to evaluate the potential herbicide activity of the imides. Compounds 5a and 5b inhibited root growth of the weed Bidens pilosa by more than 70% at all the concentrations evaluated.
Assuntos
Compostos de Epóxi , Herbicidas , Imidas , Sementes/crescimento & desenvolvimento , Bidens/crescimento & desenvolvimento , Cucumis sativus/crescimento & desenvolvimento , Compostos de Epóxi/síntese química , Compostos de Epóxi/química , Herbicidas/síntese química , Herbicidas/química , Imidas/síntese química , Imidas/química , Lactuca/crescimento & desenvolvimento , Estrutura Molecular , Sorghum/crescimento & desenvolvimentoRESUMO
The aim of this study was to assess the protective effects of oral and topical treatment with Bidens pilosa (BP) against carbon tetrachloride (CCl4)- induced toxicity. Fifty-six rats were divided into seven groups: A: CCl4 only; B: CCl4+oral BP; C: CCl4 and topical BP; D: CCl4+oral and topical BP; E: oral BP only; F: negative control; and G: positive control (cyclophosphamide). The animals were treated for 10 weeks. Blood samples were collected for tests of hepatic and renal function, and fragments of the liver, spleen, pancreas, kidney, and intestine were collected for histopathological analyses. Cells from the femoral bone marrow were used for a micronucleus test and 'comet assay'. Statistically significant differences were observed in the levels of gamma-glutamyl transpeptidase (GGT), albumin, urea and creatinine, hepatic inflammation, renal tubular lesion, and inflammation of the intestinal mucosa between the BP-treated groups and untreated group. The median number of micronuclei in group A was 4.00, in group G was 9.00 and in the other groups was 0.00. Group A had the lowest number of cells with a score of 0 and the greatest number with scores of 3 and 4, similar to the results obtained from group G using the 'comet assay'. Thus, BP effectively protected against the toxic effects of CCl4 on the liver, kidney, and intestine and exerted an antimutagenic effect on rats exposed to CCl4.
Assuntos
Anti-Inflamatórios/farmacologia , Antimutagênicos/farmacologia , Bidens , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Medicamentos de Ervas Chinesas/farmacologia , Nefropatias/prevenção & controle , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Animais , Tetracloreto de Carbono , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Ensaio Cometa , Dano ao DNA , Modelos Animais de Doenças , Rim/metabolismo , Rim/patologia , Nefropatias/induzido quimicamente , Nefropatias/metabolismo , Nefropatias/patologia , Fígado/metabolismo , Fígado/patologia , Masculino , Micronúcleos com Defeito Cromossômico/induzido quimicamente , Micronúcleos com Defeito Cromossômico/efeitos dos fármacos , Testes para Micronúcleos , Ratos WistarRESUMO
AIMS: Sclerotinia sclerotiorum, the causal agent of white mold, can infect several host species, including economically important crops. In this study, we propose and validate a new in vitro system able to mimic the conditions of interaction with the host and promote the induction of S. sclerotiorum effectors. METHODS AND RESULTS: For culture media production, we selected three plant species, common bean (Phaseolus vulgaris L, cv. Requinte.), maize (Zea mays, cv. BRS1030) and beggarticks (Bidens pilosa). To validate this system as an in vitro inducer of effectors, the qRT-PCR technique was used to investigate the expression profile of some S. sclerotiorum effector genes in each growth medium at different times after inoculation. CONCLUSION: The results obtained in this study provide a validation of a new method to study S. sclerotiorum during mimetic interaction with different hosts. Although leaf extract does not fully represent the plant environment, the presence of plant components in the culture medium seems to induce effector genes, mimicking in planta conditions. The use of MEVM is simpler than in planta growth, bypasses problems such as the amount of mycelium produced, as well as contamination of host cells during transcriptomic and proteomic analyses. SIGNIFICANCE AND IMPACT OF THE STUDY: We have devised MEVM media as a model mimicking the interaction of S. sclerotiorum and its hosts and used it to evaluate in vitro expression of effectors normally expressed only in planta.